Fármacos para Epoc

Albuterol (salbutamol): Drug information
Pharmacologic Category
 Beta2 Agonist
Dosing: Adult
Bronchospasm:
Metered-dose inhaler (90 mcg/puff): 2 puffs every 4-6 hours as needed (NAEPP, 2007):
Metered-dose inhaler (100 mcg/puff): Airomir [Canadian product]:
Acute treatment: 1-2 puffs; additional puffs may be necessary if inadequate relief however
patients should be advised to promptly consult health care provider or seek medical
attention if no relief from acute treatment
Maintenance: 1-2 puffs 3-4 times daily (maximum: 8 puffs daily)
Nebulization solution: 2.5 mg 3-4 times daily as needed; Quick relief: 1.25-5 mg every 4 to 8
hours as needed (NAEPP, 2007)
Oral: Note: Oral is not the preferred route for treatment of asthma; inhalation via nebulization or
MDI is preferred (NAEPP, 2007).
Regular release: 2-4 mg/dose 3-4 times daily; maximum dose not to exceed 32 mg
daily(divided doses)
Extended release: 8 mg every 12 hours; maximum dose not to exceed 32 mg/day (divided
doses). A 4 mg dose every 12 hours may be sufficient in some patients, such as
adults of low body weight.
I.V. continuous infusion [Canadian product]: Severe bronchospasm and status asthmaticus:
Initial: 5 mcg/minute; may increase up to 10-20 mcg/minute at 15- to 30-minute intervals if
needed
Exacerbation of asthma (acute, severe) (NAEPP, 2007):
Metered-dose inhaler: 4-8 puffs every 20 minutes for up to 4 hours, then every 1-4 hours as
needed
Nebulization solution: 2.5-5 mg every 20 minutes for 3 doses, then 2.5-10 mg every 1-4 hours
as needed, or 10-15 mg/hour by continuous nebulization
Exercise-induced bronchospasm (prevention):
Metered-dose inhaler (90 mcg/puff): 2 puffs 5-30 minutes prior to exercise
Metered-dose inhaler (100 mcg/puff): Airomir [Canadian product]: 2 puffs 30 minutes prior to
exercise
Dosing: Pediatric
(For additional information see "Albuterol (salbutamol): Pediatric drug information")
Bronchospasm:
Metered-dose inhaler (90 mcg/puff): (NAEPP, 2007): Quick relief:
Children ≤4 years: 2 puffs every 4-6 hours as needed
Children 5-11 years: 2 puffs every 4-6 hours as needed
Children ≥12 years: 2 puffs every 4-6 hours as needed
Children 6-11 years:
Acute treatment: 1 puff; additional puffs may be necessary if inadequate relief;

however, patients should be advised to promptly consult health care provider
or seek medical attention if no relief from acute treatment
Maintenance: 1 puff; may increase to maximum of 1 puff 4 times daily
Children ≥12 years: Refer to adult dosing.
Nebulization solution:
Manufacturer's recommendations:
Children 2-12 years (AccuNeb): 0.63-1.25 mg 3-4 times daily as needed
Children ≥12 years: 2.5 mg 3-4 times daily as needed
NIH Guidelines, 2007: Quick relief:
Children ≤4 years: 0.63-2.5 mg every 4-6 hours as needed
Children ≥5 years: 1.25-5 mg every 4-8 hours as needed
Oral: Note: Oral is not the preferred route for treatment of asthma; inhalation via nebulization or
MDI is preferred (NAEPP, 2007).
Regular release:
Children 2-6 years: 0.1-0.2 mg/kg/dose 3 times daily (maximum: 12 mg daily)
Children 6-12 years: 2 mg/dose 3-4 times daily (maximum: 24 mg daily)
Children >12 years: 2-4 mg/dose 3-4 times daily (maximum: 32 mg daily)
Extended release:
Children 6-12 years: 4 mg every 12 hours (maximum: 24 mg daily)
Children >12 years: 8 mg every 12 hours (maximum: 32 mg daily)
Exacerbation of asthma (acute, severe) (NAEPP, 2007):
Metered-dose inhaler (90 mcg/puff):

Children <12 years: 4-8 puffs every 20 minutes for 3 doses, then every 1-4 hours as
needed
Children ≥12 years: 4-8 puffs every 20 minutes for up to 4 hours, then every 1-4 hours as
needed
Nebulization solution:
Children <12 years: 0.15 mg/kg (minimum: 2.5 mg) every 20 minutes for 3 doses, then
0.15-0.3 mg/kg (maximum: 10 mg) every 1-4 hours as needed, or 0.5 mg/kg/hour by
continuous nebulization
Children ≥12 years: 2.5-5 mg every 20 minutes for 3 doses, then 2.5-10 mg every 1-4
hours as needed, or 10-15 mg/hour by continuous nebulization
Exercise-induced bronchospasm (prevention):
Metered-dose inhaler (90 mcg/puff):
Children ≤4 years: 1-2 puffs 5 minutes prior to exercise (NAEPP, 2007):
Children >4 years: 2 puffs 5-30 minutes prior to exercise
Children 6-11 years: 1 puff 30 minutes prior to exercise
Dosing: Geriatric
Inhalation: Refer to adult dosing.
Bronchospasm (treatment): Oral, regular release: 2 mg 3-4 times daily; maximum: 8 mg 4 times
daily
Dosing: Renal Impairment

Use with caution in patients with renal impairment. No dosage adjustment required (including
patients on hemodialysis, peritoneal dialysis, or CRRT; Aronoff, 2007).
Dosing: Hepatic Impairment

No dosage adjustment provided in manufacturer's labeling.
Dosage Forms: U.S.

Excipient information presented when available (limited, particularly for generics); consult specific
product labeling. [DSC] = Discontinued product
Aerosol Solution, Inhalation:
ProAir HFA: 90 mcg/actuation (8.5 g)
Proventil HFA: 90 mcg/actuation (6.7 g)
Ventolin HFA: 90 mcg/actuation (8 g, 18 g)

Nebulization Solution, Inhalation:
Generic: 0.63 mg/3 mL (3 mL); 0.083% [2.5 mg/3 mL] (3 mL); 0.5% [2.5 mg/0.5 mL] (20 mL)
Nebulization Solution, Inhalation [preservative free]:
AccuNeb: 0.63 mg/3 mL (3 mL [DSC]); 1.25 mg/3 mL (3 mL [DSC])
Generic: 0.63 mg/3 mL (3 mL); 1.25 mg/3 mL (3 mL); 0.083% [2.5 mg/3 mL] (3 mL); 0.5% [2.5
mg/0.5 mL] (1 ea)
Syrup, Oral:
Generic: 2 mg/5 mL (473 mL)
Tablet, Oral:
Generic: 2 mg, 4 mg
Tablet Extended Release 12 Hour, Oral:
VoSpire ER: 4 mg [contains fd&c blue #1 aluminum lake, fd&c yellow #10 aluminum lake]
VoSpire ER: 8 mg
Generic: 4 mg, 8 mg
Dosage Forms: Canada

product labeling.
Aerosol, for oral inhalation:
Airomir: 100 mcg/inhalation (3.7 g) [chlorofluorocarbon free; 100 metered actuations]
Airomir: 100 mcg/inhalation (6.7 g) [chlorofluorocarbon free; 200 metered actuations]
Injection, solution, as sulphate:
Ventolin I.V.: 1 mg/1mL (5 mL)
Dosage Forms Considerations

ProAir HFA 8.5 g canisters and Proventil HFA 6.7 g canisters contain 200 inhalations.
Ventolin HFA 18 g canisters contain 200 inhalations and the 8 g canisters contain 60 inhalations.
Generic Equivalent Available: U.S.

May be product dependent
Administration
Metered-dose inhaler: Shake well before use; prime prior to first use, and whenever inhaler has not
been used for >2 weeks or when it has been dropped, by releasing 3-4 test sprays into the air
(away from face). Airomir™ Canadian product labeling recommends releasing a minimum of 4
test sprays when priming. HFA inhalers should be cleaned with warm water at least once per
week; allow to air dry completely prior to use. A spacer device or valved holding chamber is
recommended for use with metered-dose inhalers.
Nebulization solution: Concentrated solution should be diluted prior to use. Blow-by administration is
not recommended, use a mask device if patient unable to hold mouthpiece in mouth for
administration.
Infusion solution [Canadian product]: Do not inject undiluted. Reduce concentration by at least 50%
before infusing. Administer as a continuous infusion via infusion pump.
Oral: Do not crush or chew extended release tablets.
Compatibility
Intravenous solution: Stable in water for injection, NS, D5W, and D5NS when mixed in PC bags or
glass bottles. Avoid addition of other medications to infusion solution.
Solution for nebulization: Compatible with cromolyn sodium, budesonide inhalation suspension,
ipratropium solution for nebulization
Use
Treatment or prevention of bronchospasm in patients with reversible obstructive airway disease;
prevention of exercise-induced bronchospasm
Medication Safety Issues

Sound-alike/look-alike issues:
Albuterol may be confused with Albutein, atenolol
Proventil may be confused with Bentyl, PriLOSEC, Prinivil
Salbutamol may be confused with salmeterol
Ventolin may be confused with phentolamine, Benylin, Vantin
Adverse Reactions Significant

Incidence of adverse effects is dependent upon age of patient, dose, and route of administration.
Cardiovascular: Angina pectoris, atrial fibrillation, cardiac arrhythmia, chest discomfort, chest pain,
extrasystoles, flushing, hypertension, hypotension, palpitations, supraventricular tachycardia,
tachycardia
Central nervous system: Central nervous system stimulation, dizziness, drowsiness, headache,
insomnia, irritability, migraine, nervousness, nightmares, restlessness, seizure, vertigo
Dermatologic: Diaphoresis, skin rash, urticaria
Endocrine & metabolic: Hyperglycemia, hypokalemia, lactic acidosis
Gastrointestinal: Diarrhea, dysgeusia, dyspepsia, gastroenteritis, nausea, vomiting, xerostomia
Genitourinary: Difficulty in micturition
Hematologic & oncologic: Lymphadenopathy

Hypersensitivity: Anaphylaxis, angioedema, hypersensitivity reaction
Local: Pain at injection site
Neuromuscular & skeletal: Muscle cramps, musculoskeletal pain, tremor, weakness
Otic: Otitis media
Respiratory: Bronchospasm, cough, epistaxis, exacerbation of asthma, laryngitis, oropharyngeal

edema, oropharyngeal irritation, pharyngitis, rhinitis, upper respiratory tract inflammation, viral
upper respiratory tract infection
<1% (Limited to important or life-threatening): Glossitis, hoarseness, ischemic heart disease,

metabolic acidosis, pulmonary edema, throat irritation, tongue ulcer
Contraindications
Hypersensitivity to albuterol or any component of the formulation
Injection formulation [Canadian product]: Hypersensitivity to albuterol or any component of the

formulation; tachyarrhythmias; risk of abortion during first or second trimester
Warnings/Precautions
Concerns related to adverse effects:
• Bronchospasm: Rarely, paradoxical bronchospasm may occur with use of inhaled

bronchodilating agents; this should be distinguished from inadequate response.
• Hypersensitivity reactions: Immediate hypersensitivity reactions (urticaria, angioedema, rash,

bronchospasm) have been reported.
Disease-related concerns:
• Asthma: Appropriate use: Optimize anti-inflammatory treatment before initiating maintenance

treatment with albuterol. Do not use as a component of chronic therapy without an anti-
inflammatory agent. Only the mildest forms of asthma (Step 1 and/or exercise-induced)
would not require concurrent use based upon asthma guidelines.
• Cardiovascular disease: Use with caution in patients with cardiovascular disease (arrhythmia
or hypertension or HF); beta-agonists may cause elevation in blood pressure, heart rate
and result in CNS stimulation/excitation. Beta2-agonists may also increase risk of
arrhythmias.
• Diabetes: Use with caution in patients with diabetes mellitus; beta2-agonists may increase
serum glucose.
• Glaucoma: Use with caution in patients with glaucoma; may elevate intraocular pressure.
• Hyperthyroidism: Use with caution in hyperthyroidism; may stimulate thyroid activity.
• Hypokalemia: Use with caution in patients with hypokalemia; beta2-agonists may decrease
serum potassium.
• Seizures: Use with caution in patients with seizure disorders; beta-agonists may result in CNS
stimulation/excitation.
Special populations:
• Pediatrics: Face masks should be used in children <4 years of age.
Other warnings/precautions:
• Appropriate use: Do not exceed recommended dose; serious adverse events, including
fatalities, have been associated with excessive use of inhaled sympathomimetics.
• Patient information: Patients must be instructed to seek medical attention in cases where acute
symptoms are not relieved or a previous level of response is diminished. The need to
increase frequency of use may indicate deterioration of asthma, and treatment must not
be delayed. A spacer device or valved holding chamber is recommended when using a
metered-dose inhaler.
Metabolism/Transport Effects
None known.
Drug Interactions
(For additional information: Launch Lexi-Interact™ Drug Interactions Program)
AtoMOXetine: May enhance the tachycardic effect of Beta2-Agonists. Risk C: Monitor therapy
AtoMOXetine: May enhance the hypertensive effect of Sympathomimetics. AtoMOXetine may

enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Atosiban: Beta2-Agonists may enhance the adverse/toxic effect of Atosiban. Specifically, there may
be an increased risk for pulmonary edema and/or dyspnea. Risk C: Monitor therapy
Beta-Blockers (Beta1 Selective): May diminish the bronchodilatory effect of Beta2-Agonists. Of

particular concern with nonselective beta-blockers or higher doses of the beta1 selective beta-
blockers. Risk C: Monitor therapy
Beta-Blockers (Nonselective): May diminish the bronchodilatory effect of Beta2-Agonists. Risk X:

Avoid combination
Betahistine: May diminish the therapeutic effect of Beta2-Agonists. Risk C: Monitor therapy
Cannabinoid-Containing Products: May enhance the tachycardic effect of

Sympathomimetics. Exceptions:Cannabidiol. Risk C: Monitor therapy
Iobenguane I 123: Sympathomimetics may diminish the therapeutic effect of Iobenguane I

123. Risk X: Avoid combination
Linezolid: May enhance the hypertensive effect of Sympathomimetics. Management: Reduce initial
doses of sympathomimetic agents, and closely monitor for enhanced pressor response, in
patients receiving linezolid. Specific dose adjustment recommendations are not presently
available. Risk D: Consider therapy modification
Loop Diuretics: Beta2-Agonists may enhance the hypokalemic effect of Loop Diuretics. Risk C:
Monitor therapy
MAO Inhibitors: May enhance the adverse/toxic effect of Beta2-Agonists. Risk C: Monitor therapy
Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Risk C:

Monitor therapy
Tedizolid: May enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the
tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Thiazide Diuretics: Beta2-Agonists may enhance the hypokalemic effect of Thiazide Diuretics. Risk
C: Monitor therapy
Tricyclic Antidepressants: May enhance the adverse/toxic effect of Beta2-Agonists. Risk C: Monitor
therapy
Pregnancy Risk Factor

C (show table)
Pregnancy Implications
Adverse events were observed in some animal reproduction studies. Albuterol crosses the placenta
(Boulton, 1997). Congenital anomalies (cleft palate, limb defects) have rarely been reported
following maternal use during pregnancy. Multiple medications were used in most cases, no specific
pattern of defects has been reported, and no relationship to albuterol has been established. The
amount of albuterol available systemically following inhalation is significantly less in comparison to
oral doses.
Uncontrolled asthma is associated with adverse events on pregnancy (increased risk of perinatal
mortality, preeclampsia, preterm birth, low birth weight infants). Albuterol is the preferred short
acting beta agonist when treatment for asthma is needed during pregnancy (NAEPP, 2005;
NAEPP, 2007).
Albuterol may affect uterine contractility. Maternal pulmonary edema and other adverse events have
been reported when albuterol was used for tocolysis. Albuterol is not approved for use as a
tocolytic; use caution when needed to treat bronchospasm in pregnant women. Use of the injection
(Canadian product; not available in the U.S.) is specifically contraindicated in women during the first
or second trimester who may be at risk of threatened abortion.
Lactation
Excretion in breast milk unknown/not recommended
Breast-Feeding Considerations
It is not known if albuterol is excreted into breast milk. The amount of albuterol available
systemically following inhalation is significantly less in comparison to oral doses. According to the
manufacturer, the decision to continue or discontinue breast-feeding during therapy should take into
account the risk of exposure to the infant and the benefits of treatment to the mother. The use of
beta-2-receptor agonists are not considered a contraindication to breast feeding (NAEPP, 2005).
Pricing: U.S.
Aerosol solution (ProAir HFA Inhalation)
108 (90 Base) mcg/ACT (8.5 g): $56.63
Aerosol solution (Proventil HFA Inhalation)
108 (90 Base) mcg/ACT (6.7 g): $68.82
Aerosol solution (Ventolin HFA Inhalation)
108 (90 Base) mcg/ACT (8 g): $20.41
Nebulization (Albuterol Sulfate Inhalation)
0.63 mg/3 mL (3 mL): $1.66
1.25 mg/3 mL (3 mL): $1.66
(2.5 MG/3ML) 0.083% (3 mL): $1.33
(5 MG/ML) 0.5% (1): $0.90
(5 MG/ML) 0.5% (20 mL): $19.30
Syrup (Albuterol Sulfate Oral)
2 mg/5 mL (473 mL): $30.79
Tablet, 12-hour (Albuterol Sulfate ER Oral)
4 mg (100): $140.23
8 mg (100): $262.94
Tablet, 12-hour (VoSpire ER Oral)
4 mg (100): $232.81
8 mg (100): $436.53
Tablets (Albuterol Sulfate Oral)
2 mg (100): $1756.63
4 mg (100): $1756.63
Disclaimer: The pricing data provide a representative AWP and/or AAWP price from a single
manufacturer of the brand and/or generic product, respectively. The pricing data should be used for
benchmarking purposes only, and as such should not be used to set or adjudicate any prices for
reimbursement or purchasing functions. Pricing data is updated monthly.
Monitoring Parameters
FEV1, peak flow, and/or other pulmonary function tests; blood pressure, heart rate; CNS stimulation;
serum glucose, serum potassium; asthma symptoms; arterial or capillary blood gases (if patients
condition warrants)
International Brand Names
 Aero-Vent (PH);
 Aerolin (BR, CN, GR);
 Aeromol (TH);
 Airmax (CO);
 Airomir (AU, CR, FR, GT, HN, LU, NI, NZ, PA, SE, SV, TW, UY);
 Asmacaire (PH);
 Asmadil (BF, BJ, CI, ET, GH, GM, GN, JO, KE, LR, MA, ML, MR, MU, MW, NE, NG, SA, SC, SD,
SL, SN, TN, TZ, UG, ZM, ZW);
 Asmalat (LB);
 Asmalin Pulmoneb (PH);
 Asmatol (AR);
 Asmidon (JP);
 Asmol (SG);
 Asmol CFC-Free (AU);
 Assal (MX);
 Asthalin (IN);
 Asthalin HFA (HK);
 Asthavent (AE, ZA);
 Asvimol (PH);
 Avedox-FC (MX);
 Azmacon (ID);
 Bajapres (CO);
 Bemin (EC);
 Bronchosol (TH);
 Broncolin (MY, PH);
 Broncovaleas (IT);
 Brondisal (ID);
 Brusal (MX);
 Brytolin (PH);
 Butalin (JO, LB, SA);
 Butamol (AU, PY);
 Butavent (MY);
 Buto-Asma (ES, HK, TH);
 Butotal (CN);
 Buventol (AE, AT, CZ, NO, SG, TW);
 Buventol Easyhaler (FR, TH);

 Cotran (TW);
 Cybutol (ID);
 Easyhaler Salbutamol (GB, IE);
 Ecutamol (EC);
 Epaq Inhaler (AU);
 Farcolin (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE);
 Grafalin (ID);
 Hivent DS (PH);
 Huma-Salmol (HU);
 Inbumed (MX);
 Libretin (PH);
 Medolin (SG);
 Mozal (TW);
 Provexel NS (PH);
 Respolin (NZ);
 Sabutal (TW);
 Salamol (MY);
 Salbetol (IN);
 Salbron (ID);
 Salbuflo (PH);
 Salbulin (LU);
 Salbutalan (MX);
 Salbutamol (HU);
 Salbutamol-GW (HU);
 Salbutan (VE);
 Salbutin (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE);
 Salbutol (KP);
 Salbutron SR (KP);
 Salbuven (ID);
 Salbuvent (PE);
 Salmaplon (IN);
 Salomol (TW);
 Saltam (ID);
 Solia (TH);
 Sultanol (AT, DE, JP);
 Teoden (BR);
 Unibron (MX);
 Venalax (PH);
 Venderol (SG);
 Venetlin (JP);
 Ventamol (HK, ID);
 Venterol (TH);
 Venteze (ZA);
 Ventilan (CO, PT);
 Ventilastin Novolizer (DE, FR);
 Ventodisk (LU);
 Ventol (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE);
 Ventolin (AE, AR, AU, BB, BE, BF, BG, BH, BJ, BM, BS, BZ, CH, CI, CL, CY, CZ, DO, EC, EE, EG,
ET, GH, GM, GN, GT, GY, HK, HN, HR, HU, ID, IE, IL, IQ, IR, IT, JM, JO, KE, KP, KW, LB, LR, LU,
LY, MA, ML, MR, MU, MW, MX, MY, NE, NG, NI, NL, NZ, OM, PA, PE, PH, PK, PL, PR, PY, QA,
RU, SA, SC, SD, SL, SN, SR, SV, SY, TH, TN, TR, TT, TW, TZ, UG, UY, VE, YE, ZM, ZW);
 Ventolin CFC-Free (AU);
 Ventoline (DK, FI, FR, NO, SE);
 Volmax (AE, BH, CY, EC, EG, HU, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE);
 Zenmolin (AE, BH, CY, EG, HK, IL, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE);
 Zibil (MX);
 Zomm (PY)
Mechanism of Action
Relaxes bronchial smooth muscle by action on beta2-receptors with little effect on heart rate
Pharmacodynamics and Pharmacokinetics

Onset of action: Peak effect:
Nebulization/oral inhalation: 0.5-2 hours
CFC-propelled albuterol: 10 minutes
Ventolin HFA: 25 minutes
Oral: 2-3 hours
Duration: Nebulization/oral inhalation: 3-4 hours; Oral: 4-6 hours
Metabolism: Hepatic to an inactive sulfate
Half-life elimination: Inhalation: 3.8 hours; Oral: 3.7-5 hours
Excretion: Urine (30% as unchanged drug)

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20. Spiller HA, Ramoska EA, Henretig FM, et al, “A Two-Year Retrospective Study of Accidental
Pediatric Albuterol Ingestions,” Pediatr Emerg Care, 1993, 9(6):338-40. [PubMed 8302698]
21. Udezue E, D'Souza L, and Mahajan M, “Hypokalemia After Normal Doses of Nebulized Albuterol
(Salbutamol),” Am J Emerg Med, 1995, 13(2):168-71. [PubMed 7893301]
22. Wiley JF 2nd, Spiller HA, Krenzelok EP, et al, “Unintentional Albuterol Ingestion in
Children,” Pediatr Emerg Care, 1994, 10(4):193-6. [PubMed 7937293]
Ipratropium (oral inhalation): Drug information
Copyright 1978-2014 Lexicomp, Inc. All rights reserved.

(For additional information see "Ipratropium (oral inhalation): Patient drug information" and see
"Ipratropium (oral inhalation): Pediatric drug information")
For abbreviations and symbols that may be used in Lexicomp (show table)
Brand Names: U.S.
 Atrovent HFA
Brand Names: Canada
 Atrovent HFA;
 Gen-Ipratropium;
 Mylan-Ipratropium Sterinebs;
 Novo-Ipramide;
 Nu-Ipratropium;
 PMS-Ipratropium;
 ratio-Ipratropium UDV;
 Teva-Ipratropium Sterinebs
 Anticholinergic Agent
Dosing: Adult
Asthma exacerbation, acute (NIH Asthma Guidelines, 2007):
Nebulization: 500 mcg every 20 minutes for 3 doses, then as needed. Note: Should be given in
combination with a short-acting beta-adrenergic agonist.
Metered-dose inhaler: 8 inhalations every 20 minutes as needed for up to 3 hours. Note: Should
be given in combination with a short-acting beta-adrenergic agonist.
Bronchospasm associated with COPD:
Nebulization: 500 mcg (one unit-dose vial) 3-4 times/day with doses 6-8 hours apart
Metered-dose inhaler: 2 inhalations 4 times/day, up to 12 inhalations/24 hours
Dosing: Pediatric
(For additional information see "Ipratropium (oral inhalation): Pediatric drug information")
Asthma exacerbation, acute (NIH Asthma Guidelines, 2007):
Nebulization:
Children ≤12 years: 250-500 mcg every 20 minutes for 3 doses, then as needed. Note: Should
Children >12 years: Refer to adult dosing.
Metered-dose inhaler:
Children ≤12 years: 4-8 inhalations every 20 minutes as needed for up to 3 hours. Note: Should
Children >12 years: Refer to adult dosing.
Dosing: Geriatric
Refer to adult dosing.

No dosage adjustment provided in manufacturer’s labeling (has not been studied).

No dosage adjustment provided in manufacturer’s labeling (has not been studied).
Dosage Forms: U.S.

product labeling.
Aerosol Solution, Inhalation, as bromide:
Atrovent HFA: 17 mcg/actuation (12.9 g) [contains alcohol, usp]
Solution, Inhalation, as bromide:
Generic: 0.02% (2.5 mL)
Solution, Inhalation, as bromide [preservative free]:
Generic: 0.02% (2.5 mL)

Atrovent HFA 12.9 g canister contains 200 inhalations.

Administration
Avoid spraying into the eyes.
Atrovent® HFA: Prior to initial use, prime inhaler by releasing 2 test sprays into the air. If the inhaler
has not been used for >3 days, reprime.
Compatibility
Compatible for 1 hour when mixed with albuterol or metaproterenol in a nebulizer.
Use
Anticholinergic bronchodilator used in bronchospasm associated with COPD, bronchitis, and
emphysema

Atrovent® may be confused with Alupent, Serevent®
Ipratropium may be confused with tiotropium

>10%: Respiratory: Bronchitis (10% to 23%), COPD exacerbation (8% to 23%), sinusitis (1% to 11%)
1% to 10%:
Central nervous system: Headache (6% to 7%), dizziness (3%)
Gastrointestinal: Dyspepsia (1% to 5%), nausea (4%), xerostomia (2% to 4%), taste perversion
(1%)
Genitourinary: Urinary tract infection (2% to 10%)
Neuromuscular & skeletal: Back pain (2% to 7%)
Respiratory: Dyspnea (7% to 8%), cough (>3%), rhinitis (>3%), upper respiratory infection (>3%)
Miscellaneous: Flu-like syndrome (4% to 8%)
<1% (Limited to important or life-threatening): Accommodation disorder, anaphylactic reaction,

angioedema, bronchospasm, corneal edema, eye pain (acute), glaucoma, hypersensitivity
reactions, hypotension, intraocular pressure increased, laryngospasm, palpitations, stomatitis,
tachycardia, urinary retention
Contraindications
Hypersensitivity to ipratropium, atropine (and its derivatives), or any component of the formulation
• Bronchospasm: Rarely, paradoxical bronchospasm may occur with use of inhaled

bronchodilating agents; this should be distinguished from inadequate response.

bronchospasm) have been reported.
• Glaucoma: Use with caution in patients with narrow-angle glaucoma.
• Myasthenia gravis: Use with caution in patients with myasthenia gravis.
• Prostatic hyperplasia/bladder neck obstruction: Use with caution in patients with prostatic
hyperplasia or bladder neck obstruction.
• Appropriate use: Inhalation/nebulizer not indicated for the initial treatment of acute episodes
of bronchospasm where rescue therapy is required for rapid response. Should only be
used in acute exacerbations of asthma in conjunction with short-acting beta-adrenergic
agonists for acute episodes.
None known.
Drug Interactions
AbobotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of

AbobotulinumtoxinA.Risk C: Monitor therapy
Acetylcholinesterase Inhibitors: May diminish the therapeutic effect of Anticholinergic Agents.

Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase
Inhibitors. Risk C: Monitor therapy
Aclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid
combination
Analgesics (Opioid): Anticholinergic Agents may enhance the adverse/toxic effect of Analgesics
(Opioid). Specifically, the risk for constipation and urinary retention may be increased with this
combination.Risk C: Monitor therapy
Anticholinergic Agents: Ipratropium (Oral Inhalation) may enhance the anticholinergic effect of
Anticholinergic Agents. Risk X: Avoid combination
Cannabinoid-Containing Products: Anticholinergic Agents may enhance the tachycardic effect of

Cannabinoid-Containing Products. Exceptions: Cannabidiol. Risk C: Monitor therapy
Mianserin: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor
therapy
Mirabegron: Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. Risk C:
Monitor therapy
OnabotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of

OnabotulinumtoxinA.Risk C: Monitor therapy
Potassium Chloride: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium
Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid
using any solid oral dosage form of potassium chloride. Risk X: Avoid combination
Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are
specific to the GI tract. Risk D: Consider therapy modification
RimabotulinumtoxinB: Anticholinergic Agents may enhance the anticholinergic effect of

RimabotulinumtoxinB. Risk C: Monitor therapy
Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management:
Avoid using drugs with substantial anticholinergic effects in patients receiving secretin
whenever possible. If such agents must be used in combination, monitor closely for a
diminished response to secretin. Risk D: Consider therapy modification
Thiazide Diuretics: Anticholinergic Agents may increase the serum concentration of Thiazide
Diuretics.Risk C: Monitor therapy
Tiotropium: Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. Risk X:
Avoid combination
Topiramate: Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. Risk C:
Monitor therapy
Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid
combination

B (show table)
Teratogenic effects were not observed in animal studies. Inhaled ipratropium is recommended for
use as additional therapy for pregnant women with severe asthma exacerbations.
Lactation
Excretion in breast milk unknown/use caution
It is not known if ipratropium (oral inhalation) is excreted in breast milk. The manufacturer
recommends that caution be exercised when administering ipratropium (oral inhalation) to nursing
women.
Pricing: U.S.
Aerosol solution (Atrovent HFA Inhalation)
17 mcg/ACT (12.9 g): $283.78
Solution (Ipratropium Bromide Inhalation)
0.02% (2.5 mL): $1.78
 Aeron (AU);
 Aerotrop (AR, PY);
 Aerovent (EG, IL, IQ, IR, LY, OM, YE);
 Alovent (VE);
 Apovent (IL);
 Aproven (AU);
 Atem (AE, BH, CY, EG, IQ, IR, IT, JO, KW, LB, LY, OM, PK, QA, SA, SY, YE);
 Atrovent (AE, AR, AT, AU, BD, BE, BG, BH, BR, CH, CL, CN, CO, CR, CY, CZ, DK, DO, EC, EE,
FI, FR, GB, GR, GT, HK, HN, ID, IE, JO, JP, KW, LB, MT, MY, NI, NL, NO, NZ, PA, PE, PH, PK,
PL, PT, PY, QA, RU, SA, SE, SG, SK, SV, SY, TR, TW, UY);
 Atrovent Aerosol (NZ);
 Atrovent N (SG);
 Atrovent Nasal (NZ);
 Atrovent UDV (KP);
 I-Patrimol (PE);
 Ipratec (PK);
 Ipravent (IN);
 Ipraxa (NO);
 Iprovent (SG);
 Optra (PK);
 Rinatec (GB, IE)
Mechanism of Action
Blocks the action of acetylcholine at parasympathetic sites in bronchial smooth muscle causing
bronchodilation; local application to nasal mucosa inhibits serous and seromucous gland
secretions.

Onset of action: Bronchodilation: Within 15 minutes
Peak effect: 1-2 hours
Duration: 2-5 hours
Absorption: Negligible
Distribution: 15% of dose reaches lower airways
Protein Binding: ≤9%
Half-life elimination: 2 hours
Excretion: Urine
Tiotropium: Drug information

(For additional information see "Tiotropium: Patient drug information")
Brand Names: U.S.
 Spiriva HandiHaler
Brand Names: Canada
 Spiriva
 Anticholinergic Agent;
 Anticholinergic Agent, Long-Acting
Dosing: Adult
COPD: Oral inhalation: Contents of 1 capsule (18 mcg) inhaled once daily using HandiHaler
device. Note: To ensure drug delivery, the contents of each capsule should be inhaled twice.
Dosing: Geriatric

No dosage adjustment necessary; use caution in CrCl ≤50 mL/minute; monitor closely.

No dosage adjustment necessary.
Dosage Forms: U.S.

product labeling.
Capsule, Inhalation:
Spiriva HandiHaler: 18 mcg [contains milk protein]

product labeling.
Powder, for oral inhalation:
Spiriva: 18 mcg/capsule (10s) [contains lactose]

No
Administration
For oral inhalation only. Capsule should not be swallowed.
Administer once daily at the same time each day. Remove capsule from foil blister immediately
before use. Place capsule in the center chamber of the HandiHaler Inhaler. Must only use the
HandiHaler Inhaler. Close mouthpiece firmly until a click is heard, leaving dustcap open. The
capsule is pierced by pressing and releasing the green piercing button on the side of the
HandiHaler device. Exhale fully. Close lips tightly around mouthpiece; do not exhale into inhaler. Tilt
head slightly back and inhale (rapidly, steadily, and deeply); the capsule vibration (rattle) may be
heard within the device. Hold breath for a few seconds then repeat procedure using the same
tiotropium capsule. Throw away empty capsule by tipping into a trash can without touching it; do not
leave in inhaler. Keep capsules and inhaler dry.
Use
Chronic obstructive pulmonary disease: Maintenance treatment of bronchospasm associated
with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema;
reduction of COPD exacerbations

Spiriva may be confused with Inspra, Serevent
Tiotropium may be confused with ipratropium

Administration issues:
Spiriva capsules for inhalation are for administration via HandiHaler device and are not for
oral use

>10%:
Gastrointestinal: Xerostomia (5% to 16%)
Respiratory: Upper respiratory tract infection (41%), pharyngitis (9% to 13%), sinusitis (7% to
11%)
1% to 10%:
Cardiovascular: Chest pain (1% to 7%), edema (dependent, 5%)
Central nervous system: Headache (6%), insomnia (4%), depression (1% to 4%), dysphonia
(1% to 3%)
Dermatologic: Rash (4%)
Endocrine & metabolic: Hypercholesterolemia (1% to 3%), hyperglycemia (1% to 3%)

Gastrointestinal: Dyspepsia (6%), abdominal pain (5%), constipation (4% to 5%), vomiting (4%),
gastroesophageal reflux (1% to 3%), stomatitis (including ulcerative; 1% to 3%)
Genitourinary: Urinary tract infection (7%)
Neuromuscular & skeletal: Arthralgia (4%), myalgia (4%), arthritis (≥3%), leg pain (1% to 3%),
paresthesia (1% to 3%), skeletal pain (1% to 3%)
Ocular: Cataract (1% to 3%)
Respiratory: Rhinitis (6%), epistaxis (4%), cough (≥3%), laryngitis (1% to 3%)
Miscellaneous: Infection (4%), moniliasis (4%), flu-like syndrome (≥3%), allergic reaction (1% to
3%), herpes zoster (1% to 3%)
<1% (Limited to important or life-threatening): Angioedema; application site irritation (glossitis, mouth
ulceration, pharyngolaryngeal pain); atrial fibrillation, blurred vision, candidiasis (oral), dizziness,
dehydration, dry skin, dysphagia, gingivitis, glaucoma, hoarseness, hypersensitivity reactions,
ileus (paralytic), intestinal obstruction, intraocular pressure increased, joint swelling, palpitation,
paradoxical bronchospasm, pruritus, pupil dilation (if powder comes in contact with eyes), skin
infection, skin ulcer, supraventricular tachycardia, tachycardia, throat irritation, urinary difficulty,
urinary retention, urticaria
Contraindications
Hypersensitivity to ipratropium, tiotropium, or any component of the formulation
• Bronchospasm: Paradoxical bronchospasm may occur with use of inhaled agents; discontinue
use and consider other therapy if bronchospasm occurs.
• CNS effects: May cause dizziness and blurred vision; patients must be cautioned about
performing tasks that require mental alertness (eg, operating machinery or driving).

bronchospasm, anaphylaxis, itching) have been reported. Discontinue immediately if
signs/symptoms occur. Use with caution in patients with a history of hypersensitivity to
atropine.
• Glaucoma: May worsen symptoms of narrow-angle glaucoma; use with caution.
• Prostatic hyperplasia/bladder neck obstruction: May worsen the symptoms of prostatic

hyperplasia and/or bladder neck obstruction; use with caution.
• Renal impairment: Use with caution in patients with moderate-to-severe renal impairment (CrCl
≤50 mL/minute); monitor closely for anticholinergic adverse events.
Dosage form specific issues:
• Lactose: Capsule for oral inhalation contains lactose; use with caution in patients with severe
milk protein allergy.
• Appropriate administration: Not indicated for the initial (rescue) treatment of acute episodes of
bronchospasm.
• Appropriate use: The contents of Spiriva capsules are for inhalation only via the HandiHaler
device. Capsules should not be swallowed; there have been reports of incorrect
administration (swallowing of the capsules).
• Avoid ocular contact: Avoid inadvertent instillation of powder into the eyes; may dilate pupils
and/or cause blurred vision.
Substrate of CYP2D6 (minor), CYP3A4 (minor); Note:Assignment of Major/Minor substrate status
based on clinically relevant drug interaction potential
Drug Interactions
AbobotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of

AbobotulinumtoxinA.Risk C: Monitor therapy
Acetylcholinesterase Inhibitors: May diminish the therapeutic effect of Anticholinergic Agents.

Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase
Inhibitors. Risk C: Monitor therapy
Aclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid
combination
Analgesics (Opioid): Anticholinergic Agents may enhance the adverse/toxic effect of Analgesics
(Opioid). Specifically, the risk for constipation and urinary retention may be increased with this
combination.Risk C: Monitor therapy
Anticholinergic Agents: May enhance the anticholinergic effect of Tiotropium. Exceptions: Ketotifen
(Ophthalmic). Risk X: Avoid combination
Anticholinergic Agents: May enhance the adverse/toxic effect of other Anticholinergic

Agents. Exceptions:Levocabastine (Nasal). Risk C: Monitor therapy
Cannabinoid-Containing Products: Anticholinergic Agents may enhance the tachycardic effect of

Cannabinoid-Containing Products. Exceptions: Cannabidiol. Risk C: Monitor therapy
Ipratropium (Oral Inhalation): May enhance the anticholinergic effect of Anticholinergic Agents. Risk
X: Avoid combination
Mianserin: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor
therapy
Mirabegron: Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. Risk C:
Monitor therapy
OnabotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of
OnabotulinumtoxinA.Risk C: Monitor therapy
Peginterferon Alfa-2b: May decrease the serum concentration of CYP2D6 Substrates. Risk C:
Monitor therapy
Potassium Chloride: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium
Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid
using any solid oral dosage form of potassium chloride. Risk X: Avoid combination
Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are
specific to the GI tract. Risk D: Consider therapy modification
RimabotulinumtoxinB: Anticholinergic Agents may enhance the anticholinergic effect of

RimabotulinumtoxinB. Risk C: Monitor therapy
Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management:
Avoid using drugs with substantial anticholinergic effects in patients receiving secretin
whenever possible. If such agents must be used in combination, monitor closely for a
diminished response to secretin. Risk D: Consider therapy modification
Thiazide Diuretics: Anticholinergic Agents may increase the serum concentration of Thiazide
Diuretics.Risk C: Monitor therapy
Topiramate: Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. Risk C:
Monitor therapy
Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid
combination

C (show table)
Adverse events have been observed in animal reproduction studies.
Lactation
It is not known if tiotropium is excreted in breast milk. The manufacturer recommends that caution
be exercised when administering tiotropium to nursing women.
Pricing: U.S.
Capsules (Spiriva HandiHaler Inhalation)
18 mcg (30): $337.14
FEV1, peak flow (or other pulmonary function studies); anticholinergic adverse reactions (patients
with CrCl ≤50 mL/min); signs and symptoms of narrow angle glaucoma and urinary retention
 Favint (NZ);
 Spiriva (AE, AR, AT, AU, BE, BG, BH, BO, BR, CH, CL, CN, CO, CR, CY, CZ, DE, DK, DO, EC,
EG, ES, FI, FR, GB, GR, GT, HK, HN, ID, IE, IL, IQ, IR, IT, JO, KP, KW, LB, LY, MX, MY, NI, NL,
NO, NZ, OM, PA, PE, PH, PL, PR, PT, PY, QA, RU, SA, SE, SG, SV, SY, TH, TR, TW, UY, VE,
YE);
 Spiriva Respimat (AE, CN, CY, ID, KP, MY, PH, SG);
 Teromar (CO);
 Tiova Rotacaps (IN)
Mechanism of Action
Competitively and reversibly inhibits the action of acetylcholine at type 3 muscarinic (M 3) receptors
in bronchial smooth muscle causing bronchodilation

Absorption: Poorly absorbed from GI tract, systemic absorption may occur from lung
Distribution: Vd: 32 L/kg
Protein binding: 72%
Metabolism: Hepatic (minimal), via CYP2D6 and CYP3A4
Bioavailability: Following inhalation, 19.5%; oral solution: 2% to 3%
Half-life elimination: 5 to 6 days
Time to peak, plasma: 5 minutes (following inhalation)
Excretion: Urine (14% of an inhaled dose); feces (primarily nonabsorbed drug)

REFERENCES
1. Adams SG, Anzueto A, Briggs DD Jr, et al, “Tiotropium in COPD Patients Not Previously Receiving
Maintenance Respiratory Medications,” Respir Med, 2006, 100(9):1495-503. [PubMed 16698259]
2. Gross NJ, “Tiotropium Bromide,” Chest, 2004, 126(6):1946-53. [PubMed 15596697]
3. Hvizdos KM and Goa KL, “Tiotropium Bromide,” Drugs, 2002 62(8):1195-203. [PubMed 12010082]
4. Maltais F, Hamilton A, Marciniuk D, et al, “Improvements in Symptom-Limited Exercise
Performance Over 8 H With Once-Daily Tiotropium in Patients With COPD,” Chest, 2005,
128(3):1168-78.[PubMed 16162703]
5. Niewoehner DE, Rice K, Cote C, et al, “Prevention of Exacerbations of Chronic Obstructive
Pulmonary Disease With Tiotropium, a Once-Daily Inhaled Anticholinergic Bronchodilator: A
Randomized Trial,” Ann Intern Med, 2005, 143(5):317-26. [PubMed 16144890]
6. Rodrigo GJ and Nannini LJ, “Tiotropium for the Treatment of Stable Chronic Obstructive Pulmonary
Disease: A Systematic Review With Meta-Analysis,” Pulm Pharmacol Ther, 2007, 20(5):495-
502.[PubMed 16621638]
7. Spiriva HandiHaler (tiotropium bromide) [prescribing information]. Ridgefield, CT: Boehringer
Ingelheim; April 2014.
Theophylline: Drug information

(For additional information see "Theophylline: Patient drug information" and see "Theophylline:
Pediatric drug information")
Brand Names: U.S.
 Elixophyllin;
 Theo-24;
 Theochron
Brand Names: Canada
 Apo-Theo LA®;
 Novo-Theophyl SR;
 PMS-Theophylline;
 Pulmophylline;
 ratio-Theo-Bronc;
 Teva-Theophylline SR;
 Theo ER;
 Theolair;
 Uniphyl
 Phosphodiesterase Enzyme Inhibitor, Nonselective
Dosing: Adult
Doses should be individualized based on steady-state serum concentrations and ideal body weight.
Acute symptoms: Loading dose: Oral, I.V.:
Asthma exacerbations: While theophylline may be considered for relief of asthma symptoms,
the role of treating exacerbations is not supported by current practice.
COPD treatment: Theophylline is currently considered second-line intravenous therapy in the

emergency department or hospital setting when there is inadequate or insufficient
response to short acting bronchodilators (Global Initiative for COPD Guidelines, 2013).
If no theophylline received within the previous 24 hours: 4.6 mg/kg loading dose (~5.8
mg/kg hydrous aminophylline) I.V. or 5 mg/kg orally. Loading dose intended to achieve a
serum level of approximately 10 mcg/mL; loading doses should be given intravenously
(preferred) or with a rapidly absorbed oral product (not an extended-release
product). Note: On the average, for every 1 mg/kg theophylline given, blood levels will rise
2 mcg/mL.
If theophylline has been administered in the previous 24 hours: A loading dose is not
recommended without obtaining a serum theophylline concentration. The loading dose
should be calculated as follows:
Dose = (desired serum theophylline concentration - measured serum theophylline

concentration) (Vd)
Acute symptoms: Maintenance dose: I.V.: Note: To achieve a target concentration of 10 mcg/mL
unless otherwise noted. Lower initial doses may be required in patients with reduced
theophylline clearance. Dosage should be adjusted according to serum level measurements
during the first 12- to 24-hour period.
Adults 16-60 years (otherwise healthy, nonsmokers): 0.4 mg/kg/hour; maximum: 900 mg/day
unless serum levels indicate need for larger dose
Adults >60 years: 0.3 mg/kg/hour; maximum: 400 mg/day unless serum levels indicate need for
larger dose
Treatment of chronic conditions: With newer guidelines suggesting lower therapeutic theophylline
ranges, it is unlikely that doses larger than >10 mg/kg/day will be required in children ≥1 year of
age.
Oral solution: Initial dose: 300 mg/day administered in divided doses every 6-8 hours;
Maintenance: 400-600 mg/day (maximum: 600 mg/day)
Oral extended release formulations: Initial dose: 300-400 mg once daily; Maintenance: 400-600
mg once daily (maximum: 600 mg/day)
Dosage adjustment after serum theophylline measurement: Asthma: Within normal limits: Adults:
5-15 mcg/mL: Maintain dosage if tolerated. Recheck serum theophylline concentration at 24-
hour intervals (for acute I.V. dosing) or at 6- to 12-month intervals (for oral dosing). Finer
adjustments in dosage may be needed for some patients. If levels ≥15 mcg/mL, consider 10%
dose reduction to improve safety margin.
Note: Recheck serum theophylline levels after 3 days when using oral dosing, or after 12 hours
(children) or 24 hours (adults) when dosing intravenously. Patients maintained with oral
therapy may be reassessed at 6- to 12-month intervals.
Dosing: Pediatric
(For additional information see "Theophylline: Pediatric drug information")
Doses should be individualized based on steady-state serum concentrations and ideal body weight.
Acute symptoms: Loading dose: Oral, IV: Asthma exacerbations: While theophylline may be
considered for relief of asthma symptoms, the role of treating exacerbations is not supported by
current practice.
If no theophylline received within the previous 24 hours: 4.6 mg/kg loading dose (~5.8
mg/kg hydrous aminophylline) IV or 5 mg/kg orally. Loading dose intended to achieve a
serum level of approximately 10 mcg/mL; loading doses should be given intravenously
(preferred) or with a rapidly absorbed oral product (not an extended-release
product). Note: On the average, for every 1 mg/kg theophylline given, blood levels will rise
2 mcg/mL.
If theophylline has been administered in the previous 24 hours: A loading dose is not
recommended without obtaining a serum theophylline concentration. The loading dose
should be calculated as follows:
Dose = (desired serum theophylline concentration - measured serum theophylline

concentration) (Vd)
Acute symptoms: Maintenance dose: IV: Note: To achieve a target concentration of 10 mcg/mL
unless otherwise noted. Lower initial doses may be required in patients with reduced
theophylline clearance. Dosage should be adjusted according to serum level measurements
during the first 12- to 24-hour period.
Infants 6-52 weeks: mg/kg/hour = (0.008) (age in weeks) + 0.21
Children 1-9 years: 0.8 mg/kg/hour
Children 9-12 years: 0.7 mg/kg/hour
Adolescents 12-16 years (cigarette or marijuana smokers): 0.7 mg/kg/hour
Adolescents 12-16 years (nonsmokers): 0.5 mg/kg/hour; maximum: 900 mg/day unless serum
levels indicate need for larger dose
Treatment of chronic conditions: With newer guidelines suggesting lower therapeutic theophylline
ranges, it is unlikely that doses larger than >10 mg/kg/day will be required in children ≥1 year of
age.
Oral solution:
Infants <1 year: Note: Doses should be adjusted to maintain the peak steady state serum
concentrations. The time to reach steady state will vary based on age and the
presence of risk factors which may affect theophylline clearance.
Full-term Infants and Infants <26 weeks: Total daily dose (mg)= [(0.2 x age in weeks)
+5] x (weight in kg); divide dose into 3 equal amounts and administer at 8-hour
intervals
Full-term Infants and Infants ≥26 weeks and <52 weeks: Total daily dose (mg) = [(0.2
x age in weeks) +5] x (weight in kg); divide dose into 4 equal amounts and
administer at 6-hour intervals
Children ≥1 year and <45 kg: Initial dose: 10-14 mg/kg/day (maximum: 300 mg/day)
administered in divided doses every 4-6 hours; Maintenance: Up to 20 mg/kg/day
(maximum: 600 mg/day)
Children >45 kg: Refer to adult dosing.
Oral extended release formulations:
Children ≥1 year and <45 kg: Initial: 10-14 mg/kg once daily (maximum: 300 mg/day);
Maintenance up to 20 mg/kg/day (maximum: 600 mg/day)
Children >45 kg: Refer to adult dosing.

Dosage adjustment after serum theophylline measurement: Asthma: Within normal limits:
Children: 5-10 mcg/mL: Maintain dosage if tolerated. Recheck serum theophylline concentration
at 24-hour intervals (for acute IV dosing) or at 6- to 12-month intervals (for oral dosing). Finer
adjustments in dosage may be needed for some patients. If levels ≥15 mcg/mL, consider 10%
dose reduction to improve safety margin.
Note: Recheck serum theophylline levels after 3 days when using oral dosing, or after 12 hours
(children) or 24 hours (adults) when dosing intravenously. Patients maintained with oral
therapy may be reassessed at 6- to 12-month intervals.
Dosing: Geriatric
Acute symptoms: Adults >60 years:
Loading dose: Oral, I.V.: Refer to adult dosing.
Maintenance dose: I.V.: 0.3 mg/kg/hour; maximum 400 mg/day unless serum levels indicate
need for larger dose
Chronic conditions: Oral: Adults >60 years: Do not exceed a dose of 400 mg/day
Cardiac decompensation, cor pulmonale, hepatic dysfunction, sepsis with multiorgan failure, shock:

Oral: I.V.:
Infants 1-3 months: Consider dose reduction and frequent monitoring of serum theophylline
concentrations.
Infants >3 months, Children, Adolescents, and Adults: No dosage adjustment necessary.

Oral: Infants, Children, Adolescents, and Adults: No dosage adjustment provided in manufacturer’s
labeling. However, dose reduction and frequent monitoring of serum theophylline concentration
are required in patients with decreased hepatic function (eg, cirrhosis, acute hepatitis,
cholestasis). Maximum dose: 400 mg daily
I.V.: Infants, Children, Adolescents, and Adults: Initial: 0.2 mg/kg/hour; maximum daily dose: 400 mg
daily unless serum concentrations indicate need for larger dose. Use with caution and monitor
serum theophylline concentrations frequently.
Dosing: Obesity
Use ideal body weight for obese patients.
Dosage Forms: U.S.

product labeling.
Capsule Extended Release 24 Hour, Oral:
Theo-24: 100 mg
Theo-24: 200 mg [contains fd&c yellow #10 (quinoline yellow)]
Theo-24: 300 mg [contains brilliant blue fcf (fd&c blue #1), fd&c red #40]
Theo-24: 400 mg [contains fd&c red #40]
Elixir, Oral:
Elixophyllin: 80 mg/15 mL (473 mL) [contains fd&c red #40, saccharin sodium; mixed fruit flavor]
Solution, Intravenous:
Generic: 400 mg (250 mL, 500 mL); 800 mg (500 mL)
Solution, Oral:
Generic: 80 mg/15 mL (473 mL)
Theochron: 100 mg, 200 mg, 300 mg [scored]
Generic: 100 mg, 200 mg, 300 mg, 450 mg
Generic: 400 mg, 600 mg

Administration
I.V.: Administer loading dose over 30 minutes; follow with a continuous infusion as appropriate
Oral: Long-acting preparations should be taken with a full glass of water, swallowed whole, or cut in
half if scored. Do not crush. Extended release capsule forms may be opened and the contents
sprinkled on soft foods; do not chew beads.
Compatibility
Stable in D5W.
Y-site administration:
Compatible: Acyclovir, ampicillin, ampicillin/sulbactam, aztreonam, bivalirudin, cefazolin,

cefotetan, ceftriaxone, cimetidine, cisatracurium, clindamycin, clonidine, dexamethasone
sodium phosphate, dexmedetomidine, diltiazem, dobutamine, dopamine, doxycycline,
erythromycin lactobionate, famotidine, fenoldopam, fentanyl, fluconazole, gentamicin,
haloperidol, heparin, hetastarch in lactate electrolyte injection (Hextend®), hydrocortisone
sodium succinate, lidocaine, linezolid, methyldopate, methylprednisolone sodium
succinate, metronidazole, micafungin, midazolam, milrinone, nafcillin, nitroglycerin,
nitroprusside, oxaliplatin, penicillin G potassium, piperacillin, potassium chloride,
ranitidine, remifentanil, ticarcillin/clavulanate potassium, tigecycline, tobramycin,
vancomycin.
Incompatible: Cefepime, hetastarch in NS, phenytoin. Variable (consult detailed
reference):Ceftazidime.
Compatibility in syringe: Incompatible: Ceftriaxone.
Use
Treatment of symptoms and reversible airway obstruction due to chronic asthma, or other chronic
lung diseases
Note: The Global Initiative for Asthma Guidelines (2009) and the National Heart, Lung and Blood
Institute Guidelines (2007) do not recommend oral theophylline as a long-term control medication
for asthma in children ≤5 years of age; use has been shown to be effective as an add-on (but not
preferred) agent in older children and adults with severe asthma treated with inhaled or oral
glucocorticoids. The guidelines do not recommend theophylline for the treatment of exacerbations
of asthma.
The Global Initiative for Chronic Obstructive Lung Disease Guidelines (2013) suggest that while
higher doses of slow release formulations of theophylline have been proven to be effective for use
in COPD, it is not a preferred agent due to its potential for toxicity.

Frequency not defined. Adverse events observed at therapeutic serum levels:
Cardiovascular: Flutter, tachycardia
Central nervous system: Headache, hyperactivity (children), insomnia, restlessness, seizures,

status epilepticus (nonconvulsive)
Endocrine & metabolic: Hypercalcemia (with concomitant hyperthyroid disease)
Gastrointestinal: Nausea, reflux or ulcer aggravation, vomiting
Genitourinary: Difficulty urinating (elderly males with prostatism)
Neuromuscular & skeletal: Tremor
Renal: Diuresis (transient)
Contraindications
Hypersensitivity to theophylline or any component of the formulation; premixed injection may
contain corn-derived dextrose and its use is contraindicated in patients with allergy to corn-related
products
• Central nervous system: Theophylline-induced nonconvulsive status epilepticus has been

reported (rarely) and should be considered in patients who develop CNS abnormalities.
• Theophylline toxicity: If a patient develops signs and symptoms of theophylline toxicity (eg,
persistent, repetitive vomiting), a serum level should be measured and subsequent doses
held. Theophylline clearance may be decreased in patients with acute pulmonary edema,
congestive heart failure, cor pulmonale, fever, hepatic disease, acute hepatitis, cirrhosis,
hypothyroidism, sepsis with multiorgan failure, and shock; clearance may also be
decreased in neonates, infants <3 months of age with decreased renal function, children
<1 year of age, the elderly >60 years of age, and patients following cessation of
smoking. Note: Elderly >75 years of age have a 16-fold greater risk of death from
theophylline overdose than do 25-year-olds due to reduced clearance in the elderly
patient.
• Cardiovascular disease: Use with caution in patients with tachyarrhythmias (eg, sinus
tachycardia, atrial fibrillation) since use may exacerbate these arrhythmias.
• Hyperthyroidism: Use with caution in patients with hyperthyroidism; use may exacerbate this
condition.
• Peptic ulcer disease: Use with caution in patient with peptic ulcer disease; use may exacerbate
this condition.
• Seizure disorder: Use with caution in patients with a history of seizure disorder; use may
exacerbate this condition.
• Monitoring: Frequent continued monitoring of serum theophylline after therapeutic levels have
been achieved may not be required as long as there is no apparent risk of decreased
theophylline metabolism due to concurrent drug therapies or disease states. Monitoring
serum theophylline concentrations at yearly intervals should be adequate in such cases.
Substrate of CYP1A2 (major), CYP2C9 (minor), CYP2D6 (minor), CYP2E1 (major), CYP3A4
(major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug
interaction potential; Inhibits CYP1A2 (weak)
Drug Interactions
Abiraterone Acetate: May increase the serum concentration of CYP1A2 Substrates. Risk C: Monitor
therapy
Adalimumab: May decrease the serum concentration of Theophylline Derivatives. Risk C: Monitor
therapy
Adenosine: Theophylline Derivatives may diminish the therapeutic effect of Adenosine. Risk D:
Consider therapy modification
Alcohol (Ethyl): May increase the serum concentration of Theophylline. Risk C: Monitor therapy
Allopurinol: May increase the serum concentration of Theophylline Derivatives. Risk C: Monitor
therapy
Aminoglutethimide: May increase the metabolism of Theophylline Derivatives. Risk C: Monitor

therapy
Antithyroid Agents: May increase the serum concentration of Theophylline Derivatives. Risk C:
Monitor therapy
Aprepitant: May increase the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
AtoMOXetine: May enhance the hypertensive effect of Sympathomimetics. AtoMOXetine may

enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Barbiturates: May decrease the serum concentration of Theophylline Derivatives. Risk C: Monitor
therapy
Benzodiazepines: Theophylline Derivatives may diminish the therapeutic effect of

Benzodiazepines. Risk D: Consider therapy modification
Beta-Blockers (Beta1 Selective): May diminish the bronchodilatory effect of Theophylline

Derivatives. Management: Monitor for reduced theophylline efficacy during concomitant use
with any beta-blocker. Beta-1 selective agents are less likely to antagonize theophylline than
nonselective agents, but selectivity may be lost at higher doses. Risk C: Monitor therapy
Beta-Blockers (Nonselective): May diminish the bronchodilatory effect of Theophylline

Derivatives. Risk D: Consider therapy modification
Bosentan: May decrease the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Cannabinoid-Containing Products: May enhance the tachycardic effect of

Sympathomimetics. Exceptions:Cannabidiol. Risk C: Monitor therapy
Cannabis: May decrease the serum concentration of CYP1A2 Substrates. Risk C: Monitor therapy
CarBAMazepine: May decrease the serum concentration of Theophylline Derivatives. Theophylline

Derivatives may decrease the serum concentration of CarBAMazepine. Management: Seek
alternatives to this combination when possible. If these agents are used together, monitor
closely for decreased serum concentrations/therapeutic effects of both medications. Risk D:
Ceritinib: May increase the serum concentration of CYP3A4 Substrates. Management: Use of
ceritinib with a narrow therapeutic index CYP3A substrate (e.g., alfentanil, cyclosporine,
dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, tacrolimus) should be
avoided when possible.Risk C: Monitor therapy
Cimetidine: May decrease the metabolism of Theophylline Derivatives. Risk D: Consider therapy
modification
Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Risk X: Avoid
combination
CYP1A2 Inducers (Strong): May increase the metabolism of CYP1A2 Substrates. Management:
Consider an alternative for one of the interacting drugs. Some combinations may be
specifically contraindicated. Consult appropriate manufacturer labeling. Risk D: Consider
therapy modification
CYP1A2 Inhibitors (Moderate): May decrease the metabolism of CYP1A2 Substrates. Risk C:
Monitor therapy
CYP1A2 Inhibitors (Strong): May decrease the metabolism of CYP1A2 Substrates. Risk D:
CYP3A4 Inducers (Strong): May increase the metabolism of CYP3A4 Substrates. Management:
Monitor therapy
CYP3A4 Inhibitors (Strong): May decrease the metabolism of CYP3A4 Substrates. Risk D:
Cyproterone: May decrease the serum concentration of CYP1A2 Substrates. Risk C: Monitor
therapy
Cyproterone: May decrease the serum concentration of CYP2E1 Substrates. Risk C: Monitor
therapy
Dabrafenib: May decrease the serum concentration of CYP3A4 Substrates. Management: Seek
alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be
avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). Risk
D: Consider therapy modification
Dasatinib: May increase the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Deferasirox: May increase the serum concentration of Theophylline. Risk X: Avoid combination
Disulfiram: May increase the serum concentration of Theophylline Derivatives. Risk C: Monitor
therapy
Estrogen Derivatives: May increase the serum concentration of Theophylline Derivatives. Risk C:
Monitor therapy
Febuxostat: May increase serum concentrations of the active metabolite(s) of Theophylline

Derivatives. Specifically, concentrations of 1-methylxanthine, a metabolite of unknown clinical
importance, may become elevated. Risk C: Monitor therapy
FluvoxaMINE: May decrease the metabolism of Theophylline Derivatives. Risk D: Consider therapy
modification
Formoterol: Theophylline Derivatives may enhance the adverse/toxic effect of Formoterol.

Theophylline Derivatives may enhance the hypokalemic effect of Formoterol. Risk C: Monitor
therapy
Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates. Risk C: Monitor
therapy
Fosphenytoin: May decrease the serum concentration of Theophylline Derivatives. Theophylline
Derivatives may decrease the serum concentration of Fosphenytoin. Management: Seek
alternatives when possible. If used together, monitor for decreased concentrations/effects of
phenytoin or theophylline if the other agent is initiated/dose increased, or increased
concentrations/effects if the other is discontinued/dose decreased. Risk D: Consider therapy
modification
Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates. Risk X:
Avoid combination
Idelalisib: May increase the serum concentration of CYP3A4 Substrates. Risk X: Avoid combination
Indacaterol: Theophylline Derivatives may enhance the adverse/toxic effect of Indacaterol.

Theophylline Derivatives may enhance the hypokalemic effect of Indacaterol. Risk C: Monitor
therapy
Interferons: May decrease the metabolism of Theophylline Derivatives. Risk C: Monitor therapy
Iobenguane I 123: Sympathomimetics may diminish the therapeutic effect of Iobenguane I

123. Risk X: Avoid combination
Isoniazid: May increase the serum concentration of Theophylline Derivatives. Risk C: Monitor
therapy
Isoproterenol: May decrease the serum concentration of Theophylline Derivatives. Risk C: Monitor
therapy
Ivacaftor: May increase the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Linezolid: May enhance the hypertensive effect of Sympathomimetics. Management: Reduce initial
doses of sympathomimetic agents, and closely monitor for enhanced pressor response, in
patients receiving linezolid. Specific dose adjustment recommendations are not presently
available. Risk D: Consider therapy modification
Lithium: Theophylline Derivatives may decrease the serum concentration of Lithium. Risk C:
Monitor therapy
Luliconazole: May increase the serum concentration of CYP3A4 Substrates. Risk C: Monitor
therapy
Macrolide Antibiotics: May decrease the metabolism of Theophylline

Derivatives. Exceptions: Azithromycin (Systemic); Fidaxomicin; Spiramycin;
Telithromycin. Risk D: Consider therapy modification
Methotrexate: May increase the serum concentration of Theophylline Derivatives. Risk C: Monitor
therapy
Metreleptin: May decrease the serum concentration of Theophylline. Metreleptin may increase the
serum concentration of Theophylline. Risk C: Monitor therapy
Mexiletine: May decrease the metabolism of Theophylline Derivatives. Risk D: Consider therapy
modification
Mifepristone: May increase the serum concentration of CYP3A4 Substrates. Management: Minimize
doses of CYP3A4 substrates, and monitor for increased concentrations/toxicity, during and 2
weeks following treatment with mifepristone. Avoid cyclosporine, dihydroergotamine,
ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus. Risk D: Consider therapy
modification
Mitotane: May decrease the serum concentration of CYP3A4 Substrates. Management: Doses of
CYP3A4 substrates may need to be adjusted substantially when used in patients being
treated with mitotane.Risk D: Consider therapy modification
Olodaterol: Theophylline Derivatives may enhance the adverse/toxic effect of Olodaterol.

Theophylline Derivatives may enhance the hypokalemic effect of Olodaterol. Risk C: Monitor
therapy
Pancuronium: Theophylline Derivatives may enhance the adverse/toxic effect of Pancuronium.

Theophylline Derivatives may diminish the neuromuscular-blocking effect of Pancuronium.
Management: Pancuronium dosage adjustment may be necessary to induce paralysis in
patients receiving concomitant theophylline derivatives. Monitor closely for adverse effects
(e.g., cardiac effects) with concomitant use of these agents. Risk D: Consider therapy
modification
Peginterferon Alfa-2b: May decrease the serum concentration of CYP2D6 Substrates. Risk C:
Monitor therapy
Pentoxifylline: May increase the serum concentration of Theophylline Derivatives. Risk C: Monitor
therapy
Phenytoin: May decrease the serum concentration of Theophylline Derivatives. Theophylline

Derivatives may decrease the serum concentration of Phenytoin. Management: Seek
alternatives when possible. If used together, monitor for decreased concentrations/effects of
phenytoin or theophylline if the other agent is initiated/dose increased, or increased
concentrations/effects if the other is discontinued/dose decreased. Risk D: Consider therapy
modification
Propafenone: May increase the serum concentration of Theophylline Derivatives. Risk C: Monitor
therapy
Protease Inhibitors: May decrease the serum concentration of Theophylline

Derivatives. Exceptions:Fosamprenavir. Risk C: Monitor therapy
QuiNINE: May increase the serum concentration of Theophylline Derivatives. Risk C: Monitor
therapy
Quinolone Antibiotics: May decrease the metabolism of Theophylline Derivatives. Ciprofloxacin and
enoxacin are of greatest concern. Theophylline/quinolone therapy might augment the seizure-
producing potential of each of the individual agents. Exceptions: Gemifloxacin; Levofloxacin
(Systemic); Lomefloxacin; Moxifloxacin (Systemic); Nalidixic Acid; Sparfloxacin. Risk D:
Regadenoson: Theophylline may diminish the vasodilatory effect of Regadenoson. Risk D:

Riociguat: Theophylline Derivatives may enhance the hypotensive effect of Riociguat. Risk X: Avoid
combination
Siltuximab: May decrease the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Simeprevir: May increase the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
St Johns Wort: May decrease the serum concentration of CYP3A4 Substrates. Management:
Stiripentol: May increase the serum concentration of Theophylline. Risk X: Avoid combination
Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Risk C:

Monitor therapy
Tedizolid: May enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the
tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Thiabendazole: May decrease the metabolism of Theophylline Derivatives. Risk D: Consider

Thyroid Products: May increase the metabolism of Theophylline Derivatives. Risk C: Monitor
therapy
Ticlopidine: May decrease the metabolism of Theophylline Derivatives. Risk C: Monitor therapy
Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Risk C: Monitor
therapy
Vemurafenib: May increase the serum concentration of CYP1A2 Substrates. Management:

Consider alternatives to such combinations whenever possible, particularly if the CYP1A2
substrate has a relatively narrow therapeutic index. Risk D: Consider therapy modification
Zafirlukast: May increase the serum concentration of Theophylline Derivatives. Theophylline

Derivatives may decrease the serum concentration of Zafirlukast. Risk C: Monitor therapy
Zileuton: May increase the serum concentration of Theophylline. Risk D: Consider therapy
modification
Food Interactions
Ethanol: Ethanol may decrease theophylline clearance. Management: Avoid or limit ethanol.
Food: Food does not appreciably affect the absorption of liquid, fast-release products, and most
sustained release products; however, food may induce a sudden release (dose-dumping) of
once-daily sustained release products resulting in an increase in serum drug levels and
potential toxicity. Changes in diet may affect the elimination of theophylline; charbroiled foods
may increase elimination, reducing half-life by 50%. Management: Should be taken with water
1 hour before or 2 hours after meals. Avoid extremes of dietary protein and carbohydrate
intake.

C (show table)
Teratogenic effects were observed in animal reproduction studies. Theophylline crosses the
placenta; adverse effects may be seen in the newborn. Use is generally safe when used at the
recommended doses (serum concentrations 5-12 mcg/mL) however maternal adverse events may
be increased and efficacy may be decreased in pregnant women. Theophylline metabolism may
change during pregnancy; the half-life is similar to that observed in otherwise healthy, nonsmoking
adults with asthma during the first and second trimesters (~8.7 hours), but may increase to 13 hours
(range: 8-18 hours) during the third trimester. The volume of distribution is also increased during the
third trimester. Monitor serum levels. The recommendations for the use of theophylline in pregnant
women with asthma are similar to those used in nonpregnant adults (National Heart, Lung, and
Blood Institute Guidelines, 2004).
Lactation
Enters breast milk/compatible
The concentration of theophylline in breast milk is similar to the maternal serum concentration.
Irritability may be observed in the nursing infant. Serious adverse events in the infant are unlikely
unless toxic serum levels are present in the mother.
Dietary Considerations
Should be taken with water 1 hour before or 2 hours after meals. Premixed injection may contain
corn-derived dextrose and its use is contraindicated in patients with allergy to corn-related products.
Pricing: U.S.
Capsule ER 24 Hour Therapy Pack (Theo-24 Oral)
100 mg (100): $164.08
200 mg (100): $243.85
300 mg (100): $299.70
400 mg (100): $421.72
Elixir (Elixophyllin Oral)
80 mg/15 mL (473 mL): $104.94
Solution (Theophylline in D5W Intravenous)
0.8 mg/mL 5% (500 mL): $5.22
1.6 mg/mL 5% (250 mL): $6.61
Solution (Theophylline Oral)
80 mg/15 mL (473 mL): $111.75
Tablet, 12-hour (Theochron Oral)
100 mg (100): $23.05
200 mg (100): $36.94

300 mg (100): $60.48
Tablet, 12-hour (Theophylline ER Oral)
100 mg (100): $44.30
200 mg (100): $56.99
300 mg (100): $68.16
450 mg (100): $94.84
Tablet, 24-hour (Theophylline ER Oral)
400 mg (100): $135.76
600 mg (100): $196.17
Monitor heart rate, CNS effects (insomnia, irritability); respiratory rate (COPD patients often have
resting controlled respiratory rates in low 20s); arterial or capillary blood gases (if applicable)
Theophylline levels: Serum theophylline levels should be monitored prior to making dose increases;
in the presence of signs or symptoms of toxicity; or when a new illness, worsening of a
present illness, or medication changes occur that may change theophylline clearance
IV loading dose: Measure serum concentrations 30 minutes after the end of an IV loading
dose
IV infusion: Measure serum concentrations one half-life after starting a continuous infusion,
then every 12-24 hours
Reference Range
Therapeutic levels: Asthma:
Children: 5-10 mcg/mL
Adults: 5-15 mcg/mL
 Aerobin (DE);
 Austyn (KP);
 Bronchoretard (DE);
 Bronsolvan (ID);
 Bufabron (ID);
 Ditenaten (DE);
 Duralyn-CR (TH);
 Egifilin (HU);
 Elixine (CL);
 Eteophyl (KP);
 Etipramid (CN);
 Euphyllin (PL);
 Euphyllin Retard (ID);
 Euphyllin Retard Mite (ID);
 Euphylong (AE, BH, CY, EG, HK, HU, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE);
 Euphylong Retardkaps (DE);

 Franol (TH);
 Lasma (AE, BH, CY, EG, GB, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE);
 Meridian AP (UY);
 Nefoben (AR);
 Neulin-SR (NZ, TW);
 Nosma (TW);
 Nuelin (AU, BB, BM, BS, BZ, DK, FI, GY, JM, NO, NZ, PH, PR, SG, SR, TT, VE);
 Nuelin SA (AE, BF, BH, BJ, CI, CR, CY, EG, ET, GH, GM, GN, IE, IQ, IR, JO, KE, KW, LB, LR, LY,
MA, ML, MR, MU, MW, NE, NG, OM, PA, QA, SA, SC, SD, SL, SN, SY, TN, TZ, UG, YE, ZA, ZM,
ZW);
 Nuelin SR (AE, AU, BH, CY, EG, HK, IQ, IR, JO, KW, LB, LY, MY, OM, QA, SA, SG, SY, TH, YE);
 Pediaphyllin PL (LU);
 Pharmafil (MX);
 Phylobid (BF, BJ, CI, ET, GH, GM, GN, IN, KE, LR, MA, ML, MR, MU, MW, NE, NG, SC, SD, SL,
SN, TN, TZ, UG, ZA, ZM, ZW);
 Quibron T SR (ID);
 Retafyllin (EE, HU);
 Slo-Phyllin (AE, BH, CY, EG, GB, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE);
 Slo-Theo (HK);
 Solosin (DE);
 Somofillina (IT);
 Teoclear (KP);
 Teoclear LA (AR);
 Teofilina Retard (CO, EC);
 Teolin (HR);
 Teolong (BR, PY);
 Teoplus (DO, GT, HN, NI, SV);
 Teosona (AR);
 Teotard (BG, EE, HR, RU);
 Theo PA (IN);
 Theo-2 (BE, LU);
 Theo-24 (IT);
 Theo-Bros (GR);
 Theo-Dur (AR, CZ, DK, FI, GR, IT, JP, LU, MY, NO, PK, SA, SE, TR);
 Theoclear (KP);
 Theolair (CH, ES, IT, LU, NL);
 Theolair S (PE);
 Theolan (KP);
 Theolin (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE);
 Theolin SR (SG);
 Theolong (JP);
 Theophar (AE, BH, KW, QA, SA);
 Theophtard (HU);
 Theophyllin-ratiopharm (LU);
 Theophylline Bruneau (LU);
 Theoplus Retard (AT, GR);

 Theospirex (HU);
 Theospirex Retard (AT);
 Theostat (LU);
 Theostat LP (FR);
 Theotard (IL);
 Uni-Dur (HR);
 Unicontin (PT);
 Unicontin-400 Continus (IN);
 Unidur (AE);
 Unifyl Retard (CH);

 Uniphyllin (TW);
 Uniphyllin Continus (AE, BF, BH, BJ, CI, CY, ET, GB, GH, GM, GN, KE, LR, MA, ML, MR, MU, MW,
NE, NG, SC, SD, SL, SN, TN, TZ, UG, ZA, ZM, ZW);
 Uniphylline (JO);
 Xanthium (LU)
Mechanism of Action
Causes bronchodilatation, diuresis, CNS and cardiac stimulation, and gastric acid secretion by
blocking phosphodiesterase which increases tissue concentrations of cyclic adenine
monophosphate (cAMP) which in turn promotes catecholamine stimulation of lipolysis,
glycogenolysis, and gluconeogenesis and induces release of epinephrine from adrenal medulla
cells

Absorption: Oral: Dosage form dependent
Distribution: 0.45 L/kg (range: 0.3-0.7 L/kg) based on ideal body weight; distributes poorly into body
fat; Vdmay increase in premature neonates, patients with hepatic cirrhosis, acidemia
(uncorrected), the elderly
Metabolism: Children >1 year and Adults: Hepatic; involves CYP1A2, 2E1 and 3A4; forms active
metabolites (caffeine and 3-methylxanthine)
Protein binding: 40%, primarily to albumin
Half-life elimination: Highly variable and dependent upon age, liver function, cardiac function, lung
disease, and smoking history
Premature infants, postnatal age 3-15 days: 30 hours (range: 17-43 hours)
Premature infants, postnatal age 25-57 days: 20 hours (range: 9.4-30.6 hours)
Children 6-17 years: 3.7 hours (range: 1.5-5.9 hours)
Adults 16-60 years with asthma, nonsmoking, otherwise healthy: 8.7 hours (range: 6.1-12.8
hours)
Time to peak, serum:
Oral: Liquid: 1 hour
I.V.: Within 30 minutes

Excretion: Urine
Neonates: 50% as unchanged theophylline
Children >3 months and Adults: ~10% as unchanged theophylline

REFERENCES
1. Expert Panel Report 3, “Guidelines for the Diagnosis and Management of Asthma,” Clinical Practice
Guidelines, National Institutes of Health, National Heart, Lung, and Blood Institute, NIH Publication
No. 08-4051, prepublication 2007. Available
athttp://www.nhlbi.nih.gov/guidelines/asthma/asthgdln.htm
2. Global Strategy for Asthma Management and Prevention, Global Initiative for Asthma (GINA) 2011.
Available at http://www.ginasthma.org
3. Global Strategy for the Diagnosis, Management and Prevention of COPD, Global Initiative for
Chronic Obstructive Lung Disease (GOLD), 2013. Available at http://www.goldcopd.com
4. Lougheed MD, Lemière C, Dell SD, et al, “Canadian Thoracic Society Asthma Management
Continuum - 2010 Consensus Summary for Children Six Years of Age and Over, and Adults,” Can
Respir J, 2010, 17(1):15-24. [PubMed 20186367]
5. National Heart, Lung, and Blood Institute; National Asthma Education and Prevention Program
Asthma and Pregnancy Working Group, “NAEPP Expert Panel Report. Managing Asthma During
Pregnancy: Recommendations for Pharmacologic Treatment - 2004 Update,” J Allergy Clin
Immunol, 2005, 115(1):34-46. [PubMed 15637545]
Fluticasone (oral inhalation): Drug information

(For additional information see "Fluticasone (oral inhalation): Patient drug information" and see
"Fluticasone (oral inhalation): Pediatric drug information")
Brand Names: U.S.
 Flovent Diskus;
 Flovent HFA
Brand Names: Canada
 Flovent Diskus;
 Flovent HFA
 Corticosteroid, Inhalant (Oral)
Dosing: Adult
Asthma: Inhalation, oral: Note: Titrate to the lowest effective dose once asthma stability is achieved
Arnuity Ellipta: Dosing based on previous asthma therapy: Note: May increase dose after 2 weeks
of therapy in patients who are not adequately controlled.
No prior treatment with inhaled corticosteroids: Initial: 100 mcg once daily; maximum: 200 mcg
once daily
Prior treatment with inhaled corticosteroids: Initial: 100 to 200 mcg once daily; maximum: 200
mcg once daily
Flovent HFA:
U.S. labeling: Dosing based on previous asthma therapy: Note: May increase dose after 2
weeks of therapy in patients who are not adequately controlled.
Bronchodilator alone: Initial: 88 mcg twice daily; maximum: 440 mcg twice daily
Inhaled corticosteroids: Initial: 88 to 220 mcg twice daily (initial dose >88 mcg twice daily
may be considered in patients previously requiring higher doses of inhaled
corticosteroids); maximum: 440 mcg twice daily
Oral corticosteroids (OCS): Initial: 440 mcg twice daily; maximum: 880 mcg twice daily.
Asthma Guidelines (NAEPP, 2007) (administer in divided doses twice daily):
“Low” dose: 88 to 264 mcg/day
“Medium” dose: >264 to 440 mcg/day
“High” dose: >440 mcg/day
Canadian labeling: Note: May increase dose after ~1 week of therapy in patients who are not
adequately controlled.
Mild asthma: 100 to 250 mcg twice daily
Moderate asthma: 250 to 500 mcg twice daily
Severe asthma: 500 mcg twice daily; may increase up to 1000 mcg twice daily in very
severe patients (eg, patients using oral corticosteroids [OCS])
Flovent Diskus:
U.S. labeling: Note: May increase dose after 2 weeks of therapy in patients who are not
Dosing based on previous asthma therapy:
Bronchodilator alone: Initial: 100 mcg twice daily; maximum: 500 mcg twice daily
Inhaled corticosteroids: Initial: 100 to 250 mcg twice daily; maximum: 500 mcg twice
daily; initial dose >100 mcg twice daily may be considered in patients with
poorer asthma control or those previously requiring high ranges of inhaled
corticosteroids
Oral corticosteroids (OCS): Initial: 500 to 1000 mcg twice daily; maximum: 1000 mcg
twice daily
“Low” dose: 100 to 300 mcg/day
“Medium” dose: >300 to 500 mcg/day
“High” dose: >500 mcg/day
Canadian labeling: Note: May increase dose after ~1 week of therapy in patients who are not
Mild asthma: 100 to 250 mcg twice daily
Moderate asthma: 250 to 500 mcg twice daily
Severe asthma: 500 mcg twice daily; may increase up to 1000 mcg twice daily in very
severe patients (eg, patients using oral corticosteroids [OCS])
Conversion from oral systemic corticosteroids to orally inhaled corticosteroids: When

converting from oral corticosteroids (OCS) to orally inhaled corticosteroids, initiate oral
inhalation therapy in patients whose asthma is previously stabilized on OCS. Gradual OCS dose
reductions should begin ~7 days after starting inhaled therapy. U.S. labeling recommends
reducing prednisone dose no more rapidly than 2.5 to 5 mg/day (or equivalent of other OCS)
weekly. The Canadian labeling recommends decreasing the daily dose of prednisone by 1 mg
(or equivalent of other OCS) no more rapidly than weekly in adults who are closely monitored
or every 10 days if not closely monitored. If adrenal insufficiency occurs, resume OCS therapy;
initiate a more gradual withdrawal. When transitioning from systemic to inhaled corticosteroids,
supplemental systemic corticosteroid therapy may be necessary during periods of stress or
during severe asthma attacks.
Dosing: Pediatric
(For additional information see "Fluticasone (oral inhalation): Pediatric drug information")
Asthma: Inhalation, oral: Note: Titrate to lowest effective dose once asthma stability achieved.
Arnuity Ellipta: Adolescents ≥12 years: Refer to adult dosing.
Flovent HFA:
U.S. labeling:
Children 4 to 11 years: Initial: 88 mcg twice daily; maximum: 88 mcg twice daily

“Low” dose:
0 to 4 years: 176 mcg/day
5 to 11 years: 88 to 176 mcg/day
≥12 years: 88 to 264 mcg/day
“Medium” dose:
0 to 4 years: >176 to 352 mcg/day
≥12 years: >264 to 440 mcg/day
“High” dose:
0 to 4 years: >352 mcg/day
≥12 years: >440 mcg/day
Canadian labeling:
Children 1 to 3 years: 100 mcg twice daily
Children 4 to 15 years: 100 mcg twice daily. Note: Canadian labeling recommends Flovent
HFA be administered as a minimum of 2 inhalations twice daily; therefore, patients
requiring lower or higher dosages than 100 mcg twice daily should use Flovent
Diskus.
Adolescents ≥16 years and Adults: Refer to adult dosing.
Flovent Diskus:
U.S. labeling:
Children 4 to 11 years: Initial: 50 mcg twice daily; may increase to maximum dose of 100
mcg twice daily in patients not adequately controlled after 2 weeks of therapy. Initial
dose >50 mcg twice daily may be considered in patients with poorer asthma control
or those previously requiring high ranges of inhaled corticosteroids.
Adolescents: Refer to adult dosing.
“Low” dose:
5 to 11 years: 100 to 200 mcg/day
≥12 years: 100 to 300 mcg/day
“Medium” dose:

≥12 years: >300 to 500 mcg/day
“High” dose:
≥12 years: >500 mcg/day
Canadian labeling:
Children 4 to 16 years: Initial: 50 to 100 mcg twice daily; may increase up to 200 mcg twice
daily after ~1 week of therapy in patients not adequately controlled
Adolescents ≥16 years: Refer to adult dosing.
Conversion from oral systemic corticosteroids to orally inhaled corticosteroids: When

converting from oral corticosteroids (OCS) to orally inhaled corticosteroids, initiate oral
inhalation therapy in patients whose asthma is previously stabilized on OCS. Gradual OCS dose
reductions should begin ~7 days after starting inhaled therapy. U.S. labeling recommends
reducing prednisone dose no more rapidly than 2.5 to 5 mg/day (or equivalent of other OCS)
weekly in children ≥12 years but does not provide a recommendation for children <12 years. A
similar approach to OCS dose reduction would however seem advisable. The Canadian labeling
recommends decreasing the daily dose of prednisone by 1 mg (or equivalent of other OCS)
every 8 days in children who are closely monitored or every 20 days if not closely monitored. If
adrenal insufficiency occurs, resume OCS therapy; initiate a more gradual withdrawal. When
transitioning from systemic to inhaled corticosteroids, supplemental systemic corticosteroid
therapy may be necessary during periods of stress or during severe asthma attacks.
Dosing: Geriatric

Arnuity Ellipta: No dosage adjustment necessary.
Flovent Diskus and Flovent HFA: There are no dosage adjustment provided in the manufacturer's
labeling (has not been studied).

There are no dosage adjustment provided in the manufacturer's labeling (has not been studied);
however, fluticasone is primarily cleared in the liver and plasma levels may be increased in patients
with hepatic impairment. Use with caution and closely monitor.
Dosage Forms: U.S.

product labeling.
Aerosol, Inhalation, as propionate:
Flovent HFA: 44 mcg/actuation (10.6 g); 110 mcg/actuation (12 g); 220 mcg/actuation (12 g)
Aerosol Powder Breath Activated, Inhalation, as propionate:
Flovent Diskus: 50 mcg/blister (60 ea); 100 mcg/blister (28 ea, 60 ea); 250 mcg/blister (28 ea,
60 ea) [contains lactose]

product labeling.
Aerosol, for oral inhalation, as propionate:
Flovent HFA: 50 mcg/inhalation (120 actuations); 125 mcg/inhalation (60 or 120 actuations);
250 mcg/inhalation (60 or 120 actuations)
Powder, for oral inhalation, as propionate:
Flovent Diskus: 50 mcg (60s) [contains lactose; prefilled blister pack]

Flovent HFA 10.6 g and 12 g canisters contain 120 inhalations.

No
Product Availability
Arnuity Ellipta (fluticasone furoate): FDA approved August 2014; anticipated availability is currently
unknown. Consult prescribing information for additional information.
Administration
Aerosol inhalation: Flovent HFA: Shake container thoroughly before using. Take 3-5 deep breaths.
Use inhaler on inspiration. Allow 1 full minute between inhalations. Rinse mouth with water after
use to reduce aftertaste and incidence of candidiasis; do not swallow. Inhaler must be primed
before first use, when not used for 7 days, or if dropped. To prime the first time, release 4 sprays
into air; shake well before each spray and spray away from face. If dropped or not used for 7
days, prime by releasing a single test spray. Patient should contact pharmacy for refill when the
dose counter reads “020”. Discard device when the dose counter reads “000”. Do not use “float”
test to determine contents.
Powder for oral inhalation:
Arnuity Ellipta: Administer the dose at the same time every day. Do not shake inhaler. When
ready to use, open and prepare mouthpiece of the inhaler and slide the cover down to
activate the first dose. Exhale fully (not into mouthpiece), take one deep breath through
mouth without blocking air vents and hold breath for about 3 to 4 seconds. If the cover is
opened and closed without inhaling the medicine, the dose will be lost. The lost dose will
be held in the inhaler, but it will no longer be available to be inhaled. It is not possible to
accidentally take a double dose or an extra dose in one inhalation. Following
administration, rinse mouth with water after use (do not swallow). Routine cleaning of the
inhaler is not required; may clean the mouthpiece if needed, using a dry tissue, before the
cover is closed. Discard inhaler after 30 sprays or when the counter reads "0".
Flovent Diskus: Do not use with a spacer device. Do not exhale into Diskus. Do not wash or
take apart. Use in horizontal position. Mouth should be rinsed with water after use (do not
swallow). Discard after 6 weeks (50 mcg diskus) or after 2 months (100 mcg and 250 mcg
diskus) once removed from protective pouch or when the dose counter reads “0”,
whichever comes first (device is not reusable).
Use
Asthma:
Arnuity Ellipta: Maintenance treatment of asthma as prophylactic therapy in patients 12 years

and older
Flovent Diskus and Flovent HFA: Maintenance treatment of asthma as prophylactic therapy in
patients 4 years and older; for patients requiring oral corticosteroid therapy for asthma to
assist in total discontinuation or reduction of total oral dose
Limitations of use: Not indicated for relief of acute bronchospasm

Flovent may be confused with Flonase

International issues:
Allegro: Brand name for fluticasone [Israel], but also the brand name for frovatriptan [Germany]
Allegro [Israel] may be confused with Allegra and Allegra-D brand names for fexofenadine and
fexofenadine/pseudoephedrine, respectively [U.S., Canada, and multiple international
markets]
Flovent [U.S., Canada] may be confused with Flogen brand name for naproxen [Mexico];
Flogene brand name for piroxicam [Brazil]

>10%:
Central nervous system: Malaise/fatigue (16%), headache (2% to 14%)
Gastrointestinal: Oral candidiasis (≤31%)
Neuromuscular & skeletal: Arthralgia/articular rheumatism (17%), musculoskeletal pain (2% to

12%)
Respiratory: Sinusitis/sinus infection (≤33%), upper respiratory tract infection (≤31%), throat
irritation (3% to 22%), nasal congestion/blockage (16%), rhinitis (≤13%)
1% to 10%:
Central nervous system: Pain (10%), fever (1% to 7%)
Dermatologic: Rash (8%), pruritus (6%)
Gastrointestinal: Nausea/vomiting (1% to 9%), gastrointestinal infection (including viral; 1% to

5%), gastrointestinal discomfort/pain (1% to 4%)
Neuromuscular & skeletal: Muscle injury (≤5%)
Respiratory: Hoarseness/dysphonia (2% to 9%), cough (1% to 9%), viral respiratory infection
(1% to 9%), bronchitis (≤8%), upper respiratory tract inflammation (≤5%)
Miscellaneous: Viral infection (≤5%)
Postmarketing and/or case reports: Aggression, agitation, anaphylactic reaction (rare with both
products; Diskus® - some patients with severe milk allergy), angioedema, anxiety, aphonia,
asthma exacerbation, behavioral changes (eg, hyperactivity and irritability in children; rare),
bone mineral density decreased, bronchospasm (immediate and delayed), cataracts, chest
tightness, Churg-Strauss syndrome, contusion, Cushingoid features, cutaneous
hypersensitivity, depression, dyspnea, ecchymoses, eosinophilia, facial edema, growth velocity
reduction in children/adolescents, HPA axis suppression, hyperglycemia, hypersensitivity
reactions (immediate and delayed), laryngitis, migraine, muscle rigidity/stiffness/tightness,
oropharyngeal edema, osteoporosis, paradoxical bronchospasm, pneumonia, restlessness,
throat soreness, tooth discoloration, urticaria, vasculitis, wheeze
Contraindications
Hypersensitivity to fluticasone or any component of the formulation; severe hypersensitivity to milk
proteins or lactose (Arnuity Ellipta and Flovent Diskus); primary treatment of status
asthmaticus or other acute episodes of asthma requiring intensive measures
Documentation of allergenic cross-reactivity for corticosteroids in this class is limited. However,

because of similarities in chemical structure and/or pharmacologic actions, the possibility of
cross-sensitivity cannot be ruled out with certainty.
Canadian labeling: Additional contraindications (not in U.S. labeling): Moderate-to-severe

bronchiectasis; untreated fungal, bacterial or tubercular infections of the respiratory tract
• Adrenal suppression: May cause hypercorticism or suppression of hypothalamic-pituitary-

adrenal (HPA) axis in sensitive patients. HPA axis suppression may lead to adrenal crisis.
Withdrawal and discontinuation of a corticosteroid should be done slowly and carefully.
Particular care is required when patients are transferred from systemic corticosteroids to
inhaled corticosteroids due to possible adrenal insufficiency or withdrawal from steroids,
including an increase in allergic symptoms. Patients receiving ≥20 mg per day of
prednisone (or equivalent) may be most susceptible. Fatalities have occurred due to
adrenal insufficiency in asthmatic patients during and after transfer from systemic
corticosteroids to aerosol steroids; aerosol steroids do not provide the systemic steroid
needed to treat patients having trauma, surgery, or infections.
• Bronchospasm: May occur with wheezing after inhalation; if this occurs, stop steroid and treat
with a fast-acting bronchodilator.
• Hypersensitivity: Hypersensitivity reactions including, allergic dermatitis, anaphylaxis,

angioedema, bronchospasm, flushing, hypotension, urticaria, and rash have been
reported.
• Immunosuppression: Prolonged use of corticosteroids may increase the incidence of

secondary infection, mask acute infection (including fungal infections), prolong or
exacerbate viral infections, or limit response to vaccines. Avoid use if possible in patients
with ocular herpes; active or quiescent tuberculosis infections of the respiratory tract; or
viral, fungal, or bacterial or parasitic systemic infections (Canadian labeling contraindicates
use with untreated respiratory infections). Exposure to chickenpox and measles should be
avoided; if the patient is exposed, prophylaxis with varicella zoster immune globulin or
pooled intramuscular immunoglobulin, respectively, may be indicated; if chickenpox
develops, treatment with antiviral agents may be considered. With oral inhalation, local
yeast infections (eg, oropharyngeal candidiasis) may occur; patient should rinse mouth
with water and spit after each use to reduce incidence.
• Kaposi's sarcoma: Prolonged treatment with corticosteroids has been associated with the
development of Kaposi's sarcoma (case reports); if noted, discontinuation of therapy
should be considered.
• Psychiatric disturbances: Corticosteroid use may cause psychiatric disturbances, including

depression, euphoria, insomnia, mood swings, and personality changes. Preexisting
psychiatric conditions may be exacerbated by corticosteroid use.
• Vasculitis: Rare cases of vasculitis (Churg-Strauss syndrome) or other systemic eosinophilic

conditions can occur; often associated with decrease and/or withdrawal of oral
corticosteroid therapy following initiation of inhaled corticosteroid.
• Asthma: Supplemental steroids (oral or parenteral) may be needed during stress or severe
asthma attacks. Not to be used in status asthmaticus or for the relief of acute
bronchospasm.
• Bone mineral density: Use with caution in patients with major risk factors for decreased bone
mineral count such as prolonged immobilization, family history of osteoporosis,
postmenopausal status, tobacco use, advanced age, poor nutrition, or chronic use of drugs
that can reduce bone mass (eg, anticonvulsants or oral corticosteroids); long-term use of
inhaled corticosteroids have been associated with decreases in bone mineral density.
• Cardiovascular disease: Use with caution in patients with HF; long-term use has been
associated with fluid retention and hypertension.
• Diabetes: Use with caution in patients with diabetes mellitus; may alter glucose
production/regulation leading to hyperglycemia.
• Gastrointestinal disease: Use with caution in patients with GI diseases (diverticulitis, peptic
ulcer, ulcerative colitis) due to perforation risk.
• Hepatic impairment: Use with caution in patients with hepatic impairment, including cirrhosis;
long-term use has been associated with fluid retention. Impairment of liver function may
lead to accumulation of fluticasone in plasma. Monitor patients for corticosteroid related
adverse effects.
• Myasthenia gravis: Use with caution in patients with myasthenia gravis; exacerbation of
symptoms has occurred, especially during initial treatment with corticosteroids.
• Myocardial infarct (MI): Use with caution following acute MI; corticosteroids have been
associated with myocardial rupture.
• Ocular disease: Use with caution in patients with cataracts and/or glaucoma; increased
intraocular pressure, open-angle glaucoma, and cataracts have occurred with prolonged
use. Consider routine eye exams in chronic users.
• Seizure disorders: Use with caution in patients with a history of seizure disorder; seizures have
been reported with adrenal crisis.
• Thyroid disease: Changes in thyroid status may necessitate dosage adjustments; metabolic
clearance of corticosteroids increases in hyperthyroid patients and decreases in
hypothyroid ones.
Concurrent drug therapy issues:
• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or

frequency adjustment, additional monitoring, and/or selection of alternative therapy.
Consult drug interactions database for more detailed information.
Special populations:
• Pediatrics: Orally-inhaled corticosteroids may cause a reduction in growth velocity in pediatric

patients (~1 centimeter per year [range: 0.3-1.8 cm per year] and related to dose and
duration of exposure). To minimize the systemic effects of orally-inhaled corticosteroids,
each patient should be titrated to the lowest effective dose. Growth should be routinely
monitored in pediatric patients.
Dosage form specific issues:
• Arnuity Ellipta and Flovent Diskus: Contains lactose; very rare anaphylactic reactions have
been reported in patients with severe milk protein allergy.
• Discontinuation of systemic corticosteroids: Withdraw systemic corticosteroid therapy with

gradual tapering of dose; consider reducing the daily prednisone dose by 2.5 to 5 mg on
a weekly basis beginning after at least 1 week of inhalation therapy. Monitor lung function,
beta-agonist use, asthma symptoms, and for signs and symptoms of adrenal insufficiency
(fatigue, lassitude, weakness, nausea and vomiting, hypotension) during withdrawal.
• Transfer to oral inhaler: When transferring to oral inhaler, previously-suppressed allergic

conditions (rhinitis, conjunctivitis, eczema) may be unmasked.
Substrate of CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on
clinically relevant drug interaction potential
Drug Interactions
Aldesleukin: Corticosteroids may diminish the antineoplastic effect of Aldesleukin. Risk X: Avoid
combination
Amphotericin B: Corticosteroids (Orally Inhaled) may enhance the hypokalemic effect of

Amphotericin B.Risk C: Monitor therapy
Antidiabetic Agents: Corticosteroids (Orally Inhaled) may diminish the hypoglycemic effect of
Antidiabetic Agents. In some instances, corticosteroid-mediated HPA axis suppression has led
to episodes of acute adrenal crisis, which may manifest as enhanced hypoglycemia,
particularly in the setting of insulin or other antidiabetic agent use. Risk C: Monitor therapy
Aprepitant: May increase the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
BCG: Immunosuppressants may diminish the therapeutic effect of BCG. Risk X: Avoid combination
Ceritinib: Corticosteroids may enhance the hyperglycemic effect of Ceritinib. Risk C: Monitor
therapy
Ceritinib: May increase the serum concentration of CYP3A4 Substrates. Management: Use of
ceritinib with a narrow therapeutic index CYP3A substrate (e.g., alfentanil, cyclosporine,
dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, tacrolimus) should be
avoided when possible.Risk C: Monitor therapy
Cobicistat: May increase the serum concentration of Fluticasone (Oral Inhalation). Risk X: Avoid
combination
Coccidioidin Skin Test: Immunosuppressants may diminish the diagnostic effect of Coccidioidin
Skin Test.Risk C: Monitor therapy
Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Risk X: Avoid
combination
Corticorelin: Corticosteroids may diminish the therapeutic effect of Corticorelin. Specifically, the
plasma ACTH response to corticorelin may be blunted by recent or current corticosteroid
therapy. Risk C: Monitor therapy
Monitor therapy
CYP3A4 Inhibitors (Strong): May increase the serum concentration of Fluticasone (Oral Inhalation).
Management: Use of orally inhaled fluticasone propionate with strong CYP3A4 inhibitors is not
recommended. Use of orally inhaled fluticasone furoate with strong CYP3A4 inhibitors should
be done with caution. Monitor patients using such a combination more closely. Risk D:
Dasatinib: May increase the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Deferasirox: Corticosteroids may enhance the adverse/toxic effect of Deferasirox. Specifically, the
risk for GI ulceration/irritation or GI bleeding may be increased. Risk C: Monitor therapy
Denosumab: May enhance the adverse/toxic effect of Immunosuppressants. Specifically, the risk
for serious infections may be increased. Risk C: Monitor therapy
Echinacea: May diminish the therapeutic effect of Immunosuppressants. Risk D: Consider therapy
modification
Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates. Risk C: Monitor
therapy
Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates. Risk X:
Avoid combination
Hyaluronidase: Corticosteroids may diminish the therapeutic effect of Hyaluronidase. Management:

Patients receiving corticosteroids (particularly at larger doses) may not experience the desired
clinical response to standard doses of hyaluronidase. Larger doses of hyaluronidase may be
required. Risk D: Consider therapy modification
Idelalisib: May increase the serum concentration of CYP3A4 Substrates. Risk X: Avoid combination
Ivacaftor: May increase the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Leflunomide: Immunosuppressants may enhance the adverse/toxic effect of Leflunomide.

Specifically, the risk for hematologic toxicity such as pancytopenia, agranulocytosis, and/or
thrombocytopenia may be increased. Management: Consider not using a leflunomide loading
dose in patients receiving other immunosuppressants. Patients receiving both leflunomide and
another immunosuppressant should be monitored for bone marrow suppression at least
monthly. Risk D: Consider therapy modification
Loop Diuretics: Corticosteroids (Orally Inhaled) may enhance the hypokalemic effect of Loop
Diuretics. Risk C: Monitor therapy
Luliconazole: May increase the serum concentration of CYP3A4 Substrates. Risk C: Monitor
therapy
Mifepristone: May increase the serum concentration of CYP3A4 Substrates. Management: Minimize
doses of CYP3A4 substrates, and monitor for increased concentrations/toxicity, during and 2
weeks following treatment with mifepristone. Avoid cyclosporine, dihydroergotamine,
ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus. Risk D: Consider therapy
modification
Natalizumab: Immunosuppressants may enhance the adverse/toxic effect of Natalizumab.

Specifically, the risk of concurrent infection may be increased. Risk X: Avoid combination
Pimecrolimus: May enhance the adverse/toxic effect of Immunosuppressants. Risk X: Avoid

combination
Simeprevir: May increase the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Sipuleucel-T: Immunosuppressants may diminish the therapeutic effect of Sipuleucel-T. Risk C:

Monitor therapy
Stiripentol: May increase the serum concentration of CYP3A4 Substrates. Management: Use of
stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index
should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4
substrate used with stiripentol requires closer monitoring. Risk D: Consider therapy
modification
Tacrolimus (Topical): May enhance the adverse/toxic effect of Immunosuppressants. Risk X: Avoid
combination
Telaprevir: May increase the serum concentration of Corticosteroids. Corticosteroids may decrease
the serum concentration of Telaprevir. Management: Concurrent use of telaprevir and
systemic corticosteroids is not recommended. When possible, consider alternatives. If used
together, employ extra caution and monitor closely for excessive corticosteroid effects and
diminished telaprevir effects.Risk D: Consider therapy modification
Thiazide Diuretics: Corticosteroids (Orally Inhaled) may enhance the hypokalemic effect of Thiazide
Diuretics. Risk C: Monitor therapy
Tipranavir: May increase the serum concentration of Fluticasone (Oral Inhalation). Risk X: Avoid
combination
Tofacitinib: Immunosuppressants may enhance the immunosuppressive effect of Tofacitinib.

Management: Concurrent use with antirheumatic doses of methotrexate or nonbiologic
disease modifying antirheumatic drugs (DMARDs) is permitted, and this warning seems
particularly focused on more potent immunosuppressants. Risk X: Avoid combination
Trastuzumab: May enhance the neutropenic effect of Immunosuppressants. Risk C: Monitor

therapy
Vaccines (Inactivated): Immunosuppressants may diminish the therapeutic effect of Vaccines

(Inactivated).Risk C: Monitor therapy

C (show table)
Adverse events were observed in some animal reproduction studies. Hypoadrenalism may occur in
infants born to mothers receiving corticosteroids during pregnancy. Based on available data, an
overall increased risk of congenital malformations or a decrease in fetal growth has not been
associated with maternal use of inhaled corticosteroids during pregnancy (Bakhireva, 2005;
NAEPP, 2005; Namazy, 2004). Uncontrolled asthma is associated with adverse events in
pregnancy (increased risk of perinatal mortality, pre-eclampsia, preterm birth, low birth weight
infants). Inhaled corticosteroids are recommended for the treatment of asthma during pregnancy
(most information available using budesonide) (ACOG, 2008; NAEPP, 2005).
Lactation
Systemic corticosteroids are excreted in human milk. It is not known if sufficient quantities of
fluticasone are absorbed following inhalation to produce detectable amounts in breast milk. The
manufacturer recommends that caution be exercised when administering fluticasone to nursing
women. The use of inhaled corticosteroids is not considered a contraindication to breast-feeding
(NAEPP, 2005).
Dietary Considerations
Arnuity Ellipta and Flovent Diskus contains lactose; very rare anaphylactic reactions have been
reported in patients with severe milk protein allergy.
Pricing: U.S.
Aerosol (Flovent HFA Inhalation)
44 mcg/ACT (10.6 g): $163.01
110 mcg/ACT (12 g): $218.24
220 mcg/ACT (12 g): $338.98
Aerosol powder (Flovent Diskus Inhalation)
50 mcg/blister (60): $154.58
100 mcg/blister (28): $100.61
250 mcg/blister (28): $134.71
Growth (adolescents and children via stadiometry); signs/symptoms of HPA axis
suppression/adrenal insufficiency; possible eosinophilic conditions (including Churg-Strauss
syndrome); FEV1, peak flow, and/or other pulmonary function tests; asthma symptoms; bone
mineral density; hepatic impairment
 Allegro (IL);
 Allevisone (TW);
 Atemur Mite (DE);

 Axotide (CH);
 Dalman AQ (HK);
 Flixonas (PK);
 Flixonase (AR, AT, AU, BE, BR, CZ, DK, DO, EC, EE, FI, FR, GB, HK, HN, ID, IE, IL, IT, KP, MY,
NL, PA, PE, PL, PY, RU, SG, SV, TH, TR, TW, UY, VE);
 Flixotaide (PT);
 Flixotide (AE, AR, AT, BE, BG, BH, BR, CL, CN, CR, CY, CZ, DK, EC, EE, EG, FI, FR, GB, GR,
GT, HK, HN, ID, IE, IL, IQ, IR, IT, JM, JO, KP, KW, LB, LY, MY, NI, NL, NZ, OM, PA, PE, PH, PY,
QA, RU, SA, SE, SG, SV, SY, TH, TT, TW, UY, VE, YE);
 Flixotide Inhaler (AU);
 Flixotide Nebules (AU);
 Flixovate (FR);
 Flohale (AE);
 Flomist (MY);
 Flutaide (PT);
 Flutica (DE);
 Flutide (DE, NO, SE);

 Flutimar HFA (CO);
 Flutinasal (GR);
 Flutinase (CH);
 Flutitrim (SG);
 Flutivate (BR, DE, NO);
 Fluzone (GT);
 Futisone (TW);
 Lutisone (HK);
 Medicort (ID);
 Nasofan (HK);
 Nasoflo (PH);
 Zoflut (IN)
Mechanism of Action
Fluticasone belongs to a group of corticosteroids which utilizes a fluorocarbothioate ester linkage at
the 17 carbon position; extremely potent vasoconstrictive and anti-inflammatory activity. The
effectiveness of inhaled fluticasone is due to its direct local effect.

Onset of action: Maximal benefit may take 1 to 2 weeks or longer
Absorption: Absorbed systemically primarily via lungs, minimal GI absorption (<1%) due to
presystemic metabolism
Distribution: 4.2 L/kg
Protein binding: >99%
Metabolism: Hepatic via CYP3A4 to 17β-carboxylic acid (negligible activity)
Bioavailability: Oral inhalation: 13.9%; Flovent Diskus: ~8%
Half-life elimination: I.V.: ~8 hours; Oral inhalation (plasma elimination phase following repeat dosing):
24 hours
Time to peak, plasma: 0.5 to 1 hour
Excretion: Feces (as parent drug and metabolites); urine (<5% as metabolites)
REFERENCES
1. ACOG Committee on Practice Bulletins-Obstetrics, "ACOG Practice Bulletin: Clinical Management

Guidelines for Obstetrician-Gynecologists Number 90, February 2008: Asthma in
Pregnancy," Obstet Gynecol, 2008, 111(2 Pt 1):457-64. [PubMed 18238988]
2. Arnuity Ellipta (fluticasone furoate inhalation powder) [prescribing information]. Research Triangle
Park, NC: GlaxoSmithKline; August 2014.
3. Bakhireva LN, Jones KL, Schatz M, et al, “Asthma Medication Use in Pregnancy and Fetal
Growth,”J Allergy Clin Immunol, 2005, 116(3):503-9. [PubMed 16159616]
4. Flovent Diskus (fluticasone propionate inhalation powder) [prescribing information]. Research
Triangle Park, NC: GlaxoSmithKline; April 2014.
5. Flovent HFA (fluticasone propionate inhalation aerosol) [prescribing information]. Research Triangle
Park, NC: GlaxoSmithKline; July 2013.
6. Global Strategy for Asthma Management and Prevention, Global Initiative for Asthma (GINA) 2011.
Available at http://www.ginasthma.org
7. Goedert JJ, Vitale F, Lauria C, et al, “Risk Factors for Classical Kaposi's Sarcoma,” J Natl Cancer
Inst, 2002, 94(22):1712-8. [PubMed 12441327]
8. Lougheed MD, Lemière C, Dell SD, et al, “Canadian Thoracic Society Asthma Management
Continuum - 2010 Consensus Summary for Children Six Years of Age and Over, and Adults,” Can
Respir J, 2010, 17(1):15-24. [PubMed 20186367]
9. Namazy J, Schatz M, Long L, et al, “Use of Inhaled Steroids by Pregnant Asthmatic Women Does
Not Reduce Intrauterine Growth,” J Allergy Clin Immunol, 2004, 113(3):427-32. [PubMed 15007341]
10. National Asthma Education and Prevention Program (NAEPP), Expert Panel Report 3, "Guidelines
for the Diagnosis and Management of Asthma," Clinical Practice Guidelines, National Institutes of
Health, National Heart, Lung, and Blood Institute, NIH Publication No. 08-4051, prepublication
2007. Available at http://www.nhlbi.nih.gov/guidelines/asthma/asthgdln.htm
11. National Asthma Education and Prevention Program (NAEPP) Working Group Report on “Managing
Asthma During Pregnancy: Recommendations for Pharmacologic Treatment,” National Institutes of
Health, National Heart, Lung, and Blood Institute, NIH Publication No. 05-5236, March 2005.
Available at http://www.nhlbi.nih.gov/health/prof/lung/asthma/astpreg/astpreg_full.pdf
12. Todd GR, Acerini CL, Buck JJ, et al, "Acute Adrenal Crisis in Asthmatics Treated With High-Dose
Fluticasone Propionate," Eur Respir J, 2002, 19(6):1207-9. [PubMed 12108877]
13. Todd GR, Acerini CL, Ross-Russell R, et al, "Survey of Adrenal Crisis Associated With Inhaled
Corticosteroids in the United Kingdom," Arch Dis Child, 2002, 87(6):457-61. [PubMed 12456538]

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Albuterol (salbutamol): Drug information

Metered-dose inhaler (100 mcg/puff): Airomir [Canadian product]:

Maintenance: 1-2 puffs 3-4 times daily (maximum: 8 puffs daily)

Exacerbation of asthma (acute, severe) (NAEPP, 2007):

Exercise-induced bronchospasm (prevention):

Metered-dose inhaler (90 mcg/puff): 2 puffs 5-30 minutes prior to exercise

Metered-dose inhaler (90 mcg/puff): (NAEPP, 2007): Quick relief:

Children ≤4 years: 2 puffs every 4-6 hours as needed

Children 5-11 years: 2 puffs every 4-6 hours as needed

Children ≥12 years: 2 puffs every 4-6 hours as needed

Metered-dose inhaler (100 mcg/puff): Airomir [Canadian product]:

Children 6-11 years:

Acute treatment: 1 puff; additional puffs may be necessary if inadequate relief;

Maintenance: 1 puff; may increase to maximum of 1 puff 4 times daily

Children ≥12 years: Refer to adult dosing.

Children 2-12 years (AccuNeb): 0.63-1.25 mg 3-4 times daily as needed

Children ≥12 years: 2.5 mg 3-4 times daily as needed

NIH Guidelines, 2007: Quick relief:

Children ≤4 years: 0.63-2.5 mg every 4-6 hours as needed

Children ≥5 years: 1.25-5 mg every 4-8 hours as needed

Children ≥12 years: Refer to adult dosing.

Children 2-6 years: 0.1-0.2 mg/kg/dose 3 times daily (maximum: 12 mg daily)

Children 6-12 years: 2 mg/dose 3-4 times daily (maximum: 24 mg daily)

Children 6-12 years: 4 mg every 12 hours (maximum: 24 mg daily)

Children >12 years: 8 mg every 12 hours (maximum: 32 mg daily)

Exacerbation of asthma (acute, severe) (NAEPP, 2007):

Metered-dose inhaler (90 mcg/puff):

Exercise-induced bronchospasm (prevention):

Metered-dose inhaler (90 mcg/puff):

Children ≤4 years: 1-2 puffs 5 minutes prior to exercise (NAEPP, 2007):

Children >4 years: 2 puffs 5-30 minutes prior to exercise

Metered-dose inhaler (100 mcg/puff): Airomir [Canadian product]:

Children 6-11 years: 1 puff 30 minutes prior to exercise

Children ≥12 years: Refer to adult dosing.

Dosing: Renal Impairment

Dosing: Hepatic Impairment

Dosage Forms: U.S.

Aerosol Solution, Inhalation:

ProAir HFA: 90 mcg/actuation (8.5 g)

Proventil HFA: 90 mcg/actuation (6.7 g)

Ventolin HFA: 90 mcg/actuation (8 g, 18 g)

Nebulization Solution, Inhalation [preservative free]:

AccuNeb: 0.63 mg/3 mL (3 mL [DSC]); 1.25 mg/3 mL (3 mL [DSC])

Generic: 2 mg/5 mL (473 mL)

Tablet Extended Release 12 Hour, Oral:

Dosage Forms: Canada

Aerosol, for oral inhalation:

Airomir: 100 mcg/inhalation (3.7 g) [chlorofluorocarbon free; 100 metered actuations]

Airomir: 100 mcg/inhalation (6.7 g) [chlorofluorocarbon free; 200 metered actuations]

Injection, solution, as sulphate:

Ventolin I.V.: 1 mg/1mL (5 mL)

Dosage Forms Considerations

Generic Equivalent Available: U.S.

Oral: Do not crush or chew extended release tablets.

Medication Safety Issues

Albuterol may be confused with Albutein, atenolol

Proventil may be confused with Bentyl, PriLOSEC, Prinivil

Salbutamol may be confused with salmeterol

Ventolin may be confused with phentolamine, Benylin, Vantin

Adverse Reactions Significant

Dermatologic: Diaphoresis, skin rash, urticaria

Endocrine & metabolic: Hyperglycemia, hypokalemia, lactic acidosis

Gastrointestinal: Diarrhea, dysgeusia, dyspepsia, gastroenteritis, nausea, vomiting, xerostomia