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Antihistamines

Chapter 69

Outcomes
Identify concepts related to medication classifications and application to manage allergic reactions, conditions of the upper respiratory system, acid indigestion and gastric reflux. Choose nursing interventions related to the applied pharmacokinetics and pharmacodyanmics specific to these medications Implement the nursing process in the administration of medication classes covered herein

Background
Histamines (Predominantly H1)
Endogenous Vessel effects Bronchi effects Stomach effects
Secretes Mucus

Greatest interest
Allergic reactions (mild / anaphylaxis) PUD (Peptic Ulcer Disease)
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Histamine Release
Allergic response
Requires IgE antibodies Prior exposure to allergen

Non-allergic direct stimulation of cells


Some drugs, chemicals, radiocontrast media, plasma expanders - require no prior exposure Cell injury (histamines can cause)

Physio / Pharm Effects


H1 Stimulation

Vasodilation (If this, then?) BP drops, nose gets stuffy,


edema, puffy eyes, etc.

Vessel wall cells contract (If this, then?) Bronchoconstriction (If this, then?) Trouble breathing Itching & pain Mucus secretion CNS effect cognition / memory / sleep

H2 Stimulation

Secretion of gastric acid (If this, then?)


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Allergies & Pharmacology


Mild Allergy
Hay fever, urticaria, mild transfusion rx. Sxms caused by? histamines TX?

Severe
Anaphylactic shock (bronchocontriction, hypotension, & edema of glottis) Sxms caused by? leukotrienes TX? (ch 17) Epi

Other Uses
Common cold runny nose

Antihistamines: 1st Generation


H1 Antagonists (classic antihistamines)
No single prototype
dyphenhydramine [Benadryl]

Highly sedating

MOA
Blockers (1st Gen)
Selectively bind to histaminic receptors Can also bind to nonhistaminic receptor (muscarinic)
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Therapeutic Effects (TE)


Vessels (If blocks histamine, then ?) Capillaries (If blocks, then ?) Sensory nerves (If, then) itching relief Mucous membranes (If, then) CNS
Therapeutic doses (If, then) - sedation Overdose stimulation, seizures esp. in young

Other: relieve N & V, motion sickness


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Clinical uses
Mild allergies, seasonal rhinitis, acute urticaria, allergic conjunctivitis, mild transfusion reactions Some block muscarinic & H1 receptor sites useful for motion sickness
promethazine [Phenergan] and dimenhydrinate [Dramamine]

Insomnia (diphenhydramine [Benadryl])

Adverse Effects
CNS
Sedation = to excess ETOH (If this, then?) Dizziness, lack of coordination, confusion Paradoxical: insomnia, excitation, tremors, convulsions

GI
N, V, Diarrhea / constipation, loss of appetite

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Anticholinergic effects
Dry mouth, throat, nasal passages, thickened secretions, (cautions?) urinary hesitancy, constipation, palpitations

Cardiac Dysrhythmias w some 2nd Gen.


Torsades de pointes, V-fib
terfenadine [Seldane] & astemizole [Hismanal]

Contraindications third trimester Precautions: asthma, children/elderly, urinary retention, HTN, OA glaucoma, prostatic hypertrophy
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DD
ETOH, barbs/benzos/ opioids, antidepressants

Toxicity
Sxms similar to atropine poisoning (anticholinergic), hyperpyrexia (super fever, can kill children) Can lead to death in children via excitation, hallucinations, convulsion, coma, CV collapse, death. Tx: remove and support may use charcoal followed with cathartics

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Antihistamines: 2nd Generation


Prototypes - Fexofenadine [Allegra] EXPENSIVE MOA / TE antagonists of histamine to relieve sxms of allergic rhinitis and urticarias ADME - Do not readily cross B-B barrier therefore non-sedating w minimized anticholinergic SEs Precautions ETOH, drowsiness, liver, kidneys
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Drugs for Treating Allergic Rhinitis, Coughs, Colds


Ch 75

Allergic Rhinitis
Review of sxms Commonly associated disorders Seasonal vs. Perennial

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Antihistamines
First line - oral Prophylaxis first No use against cold Adverse effects
1st gen - sedation, anticholinergic 2nd gen - rare

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Intranasal Glucocorticoids
Prototype: fluticasone (Flonase) Action / Use
Predominantly local anti-inflammatory First line - Most effective against all sxms

Adverse Effects
Drying, burning, or itching (when applied topically) Rare - sore throat, epistaxis and HA Rare - systemic adrenal suppression / slowed growth in children

Dose: Adults 2 sprays of 50 mcg. once daily


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Intranasal Cromolyn
Prototype: cromolyn (NasalCrom) Action / Use
Suppresses release of histamine Best suited for prophylaxis May not see results for week or more

Adverse effects
Negligible

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Sympathomimetics (fight or flight) (Decongestants)


Prototype: phenylephrine (Neo-Synephrine) Action / Uses - Reduce nasal congestion via ?
Topical - rapid and intense Oral - prolonged, moderate, systemic effects Also used in sinusitis and colds

Adverse effects
Rebound congestion CNS stimulation Cardiovascular Hemorrhagic stroke w phenylporpanolamine Abuse (pseudoephedrine and ephedrine)
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Sympathamometics (contd)
Nasal sprays
2 3 sprays every 4 hours needed not to exceed 5 consecutive days (to reduce dependence)
What cocaine is

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Anticholinergics
Prototype: ipratropium bromide (Atrovent) Action / Use
Blocks cholinergic receptors and inhibits secretions to relieve rhinorrea in allergic rhinitis and asthma No systemic effects

SEs: drying, irritation


Dry mouth, throat, etc.
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Leukotriene Antagonist
Prototype: montelukast (Singulair) Action / Uses;
Blocks binding of leukotrienes to receptors thereby relieving nasal congestion
Leukotrienes normally vasodilate and increase vascular permeability, causing congestion

Adverse Effects: None significant


Table 75-1 in book

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Treatment of Coughs

Antitussives
Antitussives (cough suppressants)
Actions / use: elevate cough threshold in common cold and URTI
Opioid (codeine and hydrocodone) best (stops cough in the brain)
Dosage: codeine 10 to 20 mg up to 6 times daily

Nonopioid (dextromethorphan) - best


Opioid derivative w/o euphoria or dependence Can lead to mind-body dissociation equal to PCP

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Expectorants
Prototype - guaifenesin (Mucinex)
MOA / Use increases flow of respiratory tract secretions
Dont use for COPD or something else read the friggin book

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Mucolytics
Prototype acetylcysteine (Mucomyst)
Can also use hypertonic saline

MOA / Use directly thins secretions ADME


Inhalation delivery

Adverse effects
Can trigger bronchospasm
Antidote for tylenol!

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Colds
Drug regimen
Symptomatic Combination products
Decongestants Antitussives Analgesics Antihistamines - anticholinergic to suppress mucus Caffeine

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Treatment of Severe Allergy


Chapter 17

Adrenergic Agonist
Prototype - epinephrine MOA/Use
Direct receptor binding ( 1&2, 1&2) mimicing the sympathetic nervous system
Also known as sympathomimetic & catecholamine (think of these to mean stimulation)

ADME
Broken down quickly in stomach & significant 1st pass effect (cant take it PO) Cant cross blood-brain Discolors (pink/brownish) as it degrades (If, then?) 29 (Throw it away!)

TEs (Therapeutic Effects)


Vasoconstriction (most common use)
Hemostasis Augments local anesthetic via vascontriction Elevates blood pressure Restores beating heart Bronchodilates

TOC for anaphylactic shock Mydriasis (rare use)

Adverse effects:
HTN, necrosis, bradycardia w HTN, tachycardia, tremor, chest pain, elevated blood sugar
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Table 17-3
DD
MAOIs TCAs General anesthestics (myocardial effects)

Precautions
IV admin can cause potentially fatal effect check concentrations! Insure patent and healthy IV site (you dont want epi going into the tissues
The range can be from 1:100,000 to 1:1,000 make sure to read the label!!!!
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EpiPen
Anaphylactic deaths
PCN, venoms & foods

Device: EpiPen & EpiPen Jr. Storage & Replacement


Room temp dark do NOT refrigerate

Injection Duration 10-20 mins SEs


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Selected Drugs for Peptic Ulcer Disease (PUD)


Chapter 76

Histamine2-Receptor Antagonists
Prototype: cimetadine (Tagamet)
First choice for gastric / duodenal ulcers Action / Uses:
Promote healing through acid reduction GERD, Aspiration Pneumonitis (aspiration of acid in the lungs) in obese & gyne prior to anesthesia

Adverse effects
Low incidence of gynecomastia (breasts devlpmnt in men), reduced libido, impotence, CNS depression / excitement, pneumonia

DD
Inhibits hepatic drug metabolism therefore? Major Drugs of concern warfarin, phenytoin, theophylline, lidocaine
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Famotidine (Pepsid)
For Heartburn, acid indigestion, sour stomach Cut dose in renal compromise/failure No antiandrogenic effects No effect on hepatic metabolism of other drugs
Doesnt cause a lot of the things that Tagamet does
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Proton Pump Inhibitors


Prototype - omeprazole (Prilosec) Action / Uses suppress secretion of gastric acid
Irreversible - days - up to weeks after cessation Superior to H2RAs

Adverse effects
HA, diarrhea, N & V Long term may increase risk of CA

ADME give 30 min before meal once daily DD, DF


Reduced absorption of atazanavir, ketocanazole and itracanazole NOT recommended concurrently with atazanavir

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Antacids
Prototypes - magnesium hydroxide / aluminum hydroxide Action / Uses alkaline agents that neutralize acid & decrease destruction of gut wall
And prophylactically to prevent aspiration pneumonia

ADME
Take regularly to promote healing In PUD: 1 and 3 hr after each meal & at bedtime Goal is gastric pH greater than 5

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Adverse effects
Constipation (aluminum base) / Diarrhea (magnesium base) Sodium loading High levels in renal failure clients

DD may interfere with absorption of other drugs

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