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1. ANTIPSYCHOTIC AGENTS
a. Typical Antipsychotics
a.1 PHENOTHIAZINES
a.1.1 ALIPHATIC
Brand Name:
- A: Well absorbed following IM administration. PO – Onset:30–60 min. Peak: unknown. Duration: 4–6 hr
- D: Widely distributed; high CNS concentrations. Crosses the placenta; enters breast milk. Protein Binding: _90%.
- M & E: Highly metabolized by the liver and GI mucosa. Some metabolites are active. Half-life: 30 hr.
Drug-Drug and Drug-Food Interactions:
Indications:
- Schizophrenia and other psychoses particularly paranoia (delusions and feelings of persecution), mania (overactive
behaviour and hypomania (elated moods and excitability), anxiety, agitation and violent or dangerously impulsive
behaviour.
Contraindications:
- Are allergic (hypersensitive) to Chlorpromazine, other phenothiazines or to any of the other ingredients in the tablets
- have a low number of blood cells (bone marrow depression)
- have urine retention due to a prostate disorder
- have an increased pressure in the eye (glaucoma)
- are taking a dopaminergic antiparkinsonism drug
- Breastfeeding
Side Effects:
Adverse Reaction:
- Musculoskeletal: you have movements that you cannot control, mainly of the tongue, mouth, jaw, arms and legs trembling,
muscle stiffness or spasm, slow movement
- CNS: seizure
- Hypersensitivity: allergic reactions
- EENT: mouth ulcers, increased saliva secretions, stuffy nose
- GI: abdominal pain, constipation, upset stomach, cramping, indigestion
- Respiratory: shortness of breath,
- Skin: jaundice
- CV: palpitations, chest pain
- Hemato: thrombocytopenia
Nursing Responsibilities:
- A:
Assess patient’s mental status (orientation, mood, behavior) before and periodically throughout therapy.
Monitor blood pressure (sitting, standing, lying), pulse, and respiratory rate before and frequently during the period of
dosage adjustment.
Observe patient carefully when administering medication to ensure medication is actually taken and not hoarded.
- D: Disturbed thought process
- P: Patient will have a decrease in excitable, paranoic, or withdrawn behavior.
- I:
PO: Administer with food, milk, or a full glass of water to minimize gastric irritation.
Dilute most concentrates in 120 mL of distilled or acidified tap water or fruit juice just before administration.
- E:
Decrease in excitable, paranoic, or withdrawn behavior.
Relief of nausea and vomiting.
Relief of intractable hiccups.
a.1.2 PIPERIDINE
Brand Name: Mellaril
- Adults: The usual starting dose for adult schizophrenic patients is 50-100 mg three times a day, with a gradual increment to
a maximum of 800 mg daily if necessary. Once effective control of symptoms has been achieved, the dosage may be
reduced gradually to determine the minimum maintenance dose. The total daily dosage ranges from 200-800 mg, divided
into two to four doses.
- Pediatric Patients: For pediatric patients with schizophrenia who are unresponsive to other agents, the recommended initial
dose is 0.5 mg/kg/day given in divided doses. Dosage may be increased gradually until optimum therapeutic effect is
obtained or the maximum dose of 3 mg/kg/day has been reached.
- A: Absorption varies with administration route. Oral tablet absorption is erratic and variable, with onset ranging from 1/2 to
1 hour. Oral concentrates and suspensions are much more predictable. Peak: 2-4hrs. Duration: 4-6hrs
- D: Distributed widely throughout the body, including breast milk. Steady state serum level is achieved within 4 to 7 days.
Drug is 91% to 99% protein-bound.
- M & E: Metabolized extensively by the liver and forms the active metabolite mesoridazine. Mostly excreted as metabolites
in urine; some is excreted in feces by way of the biliary tract.
- Fluvoxamine: Concentrations of thioridazine and its two active metabolites, mesoridazine and sulforidazine, increased
three-fold following co-administration of fluvoxamine.
- Propranolol: Concurrent administration of propranolol (100-800 mg daily) has been reported to produce increases in
plasma levels of thioridazine (approximately 50%-400%) and its metabolites (approximately 80%-300%).
- Pindolol: Concurrent administration of pindolol and thioridazine have resulted in moderate, dose-related increases in the
serum levels of thioridazine and two of its metabolites, as well as higher than expected serum pindolol levels.
- Caffeine: Increased metabolism of drug
Indications:
- Management of schizophrenic patients who fail to respond adequately to treatment with other antipsychotic drugs
Contraindications:
- Mellaril® (thioridazine HCl) use should be avoided in combination with other drugs that are known to prolong the QTc
interval and in patients with congenital long QT syndrome or a history of cardiac arrhythmias
- Mellaril is contraindicated in severe central nervous system depression or comatose states from any cause including drug
induced central nervous system depression.
Side Effects:
Adverse Reaction:
Nursing Responsibilities:
- A:
Assess patient’s mental status (orientation, mood, behavior) before and periodically throughout therapy.
Monitor blood pressure (sitting, standing, lying), pulse, and respiratory rate before and frequently during the period of
dosage adjustment.
Observe patient carefully when administering medication to ensure medication is actually taken and not hoarded.
- D: Disturbed thought process
- P: Patient will have a decrease in excitable, paranoic, or withdrawn behavior.
- I:
PO: Administer with food, milk, or a full glass of water to minimize gastric irritation.
Dilute most concentrates in 120 mL of distilled or acidified tap water or fruit juice just before administration.
- E:
Decrease in excitable, paranoic, or withdrawn behavior.
Relief of nausea and vomiting.
Relief of intractable hiccups.
a.1.3 PIPERAZINE
- Psychotic disorders.
Adults: Initially, 0.5 to 10 mg fluphenazine hydrochloride P.O. daily in divided doses q 6 to 8 hours; may increase
cautiously to 20 mg. Maintenance dosage is 1 to 5 mg P.O. daily. I.M. doses are one-third to one-half that of oral doses;
the usual starting dose is 1.25 mg I.M. The initial total daily dose is 2.5 to 10 mg divided and given every 6 to 8 hours.
For the enanthate and decanoate formulations, 12.5 to 25 mg I.M. q 3 to 6 weeks.
- A: Rate and extent of absorption vary with route of administration; oral tablet absorption is erratic and variable. IM: Onset:
less than 1hr. Peak: 1 ½-2hrs. Duration: 6-8hrs.
- D: Distributed widely into the body, including breast milk. CNS levels of drug are usually higher than those in plasma. Drug is
91% to 99% protein-bound.
- M & E: Metabolized extensively by the liver, but no active metabolites are formed; duration of action is about 6 to 8 hours
after oral administration; 1 to 6 weeks (average, 2 weeks) after I.M. depot administration. Mostly excreted in urine via the
kidneys; some is excreted in feces via the biliary tract.
Indications:
- Psychotic disorders
Contraindications:
- Contraindicated in patients hypersensitive to drug and patients experiencing coma, CNS depression, bone marrow
suppression, other blood dyscrasia, subcortical damage, or liver damage.
Side Effects:
Adverse Reaction:
Nursing Responsibilities:
- A:
Assess patient’s mental status (orientation, mood, behavior) before and periodically throughout therapy.
Monitor blood pressure (sitting, standing, lying), pulse, and respiratory rate before and frequently during the period of
dosage adjustment.
Observe patient carefully when administering medication to ensure medication is actually taken and not hoarded.
- D: Disturbed thought process
- P: Patient will have a decrease in excitable, paranoic, or withdrawn behavior.
- I:
PO: Administer with food, milk, or a full glass of water to minimize gastric irritation.
Dilute most concentrates in 120 mL of distilled or acidified tap water or fruit juice just before administration.
Stop giving drug and notify prescriber immediately if patient shows signs or symptoms of blood dyscrasias (fever,
infection, sore throat, cellulitis, or weakness).
- E:
Decrease in excitable, paranoic, or withdrawn behavior.
a.2 NONPHENOTHIAZINES
1. BUTYROPHENONES
Brand Name:
- A: Rate and extent of absorption vary with route of administration. Oral administration yields 60% bioavailability. PO –
Peak: 3-6hrs.
- D: Distributed widely into body, with high levels in adipose tissue. Drug is 90% to 92% protein-bound.
- M & E: Metabolized extensively by the liver; there may be only one active metabolite that’s less active than parent
drug. About 40% of a given dose is excreted in urine within 5 days; about 15% is excreted in feces via the biliary tract.
- Aluminum- and magnesium-containing antacids and antidiarrheals: Decreases drug absorption. Separate administration
times by 2 hours.
- Antiarrhythmics, disopyramide, procainamide, quinidine: Increases risk of arrhythmias and conduction defects. Avoid use
together.
- Anticholinergics, including antidepressants, antihistamines, antiparkinsonians, atropine, MAO inhibitors, meperidine,
phenothiazines: Causes oversedation, paralytic ileus, visual changes, and severe constipation. Use cautiously.
- Beta blockers: May inhibit haloperidol metabolism, increasing plasma levels and toxicity. Use cautiously.
- Bromocriptine: Antagonizes therapeutic effect of bromocriptine on prolactin secretion. Avoid use together.
- Centrally acting antihypertensives (such as clonidine, guanabenz, guanadrel, guanethidine, methyldopa, reserpine): Inhibits
blood pressure response. Monitor blood pressure carefully.
- CNS depressants, including analgesics, barbiturates, narcotics, tranquilizers, and general, spinal, or epidural anesthetics;
parenteral magnesium sulfate: Increases CNS depression. Avoid use together.
- Dopamine: Decreases vasoconstricting effects. Monitor patient for lack of therapeutic effect.
- Levodopa: Decreases effectiveness and increases toxicity of levodopa. Avoid use together.
- Lithium: May result in severe neurologic toxicity with an encephalitis-like syndrome and a decreased therapeutic response
to haloperidol. Use cautiously; monitor patient.
- Metrizamide: Increases risk of seizures. Avoid use together.
- Nitrates: Causes hypotension. Monitor blood pressure frequently.
- Phenobarbital: Enhances renal excretion. Monitor patient closely.
- Phenytoin: Inhibits metabolism and increases toxicity of phenytoin. Avoid use together.
- Propylthiouracil: Increases risk of agranulocytosis. Avoid use together.
- Rifampin: Decreases haloperidol levels and efficacy. Monitor patient carefully.
- Sympathomimetics, including ephedrine, epinephrine, and phenylephrine (often found in nasal sprays): May decrease
stimulatory and pressor effects of these drugs. Monitor patient carefully.
Indications:
Contraindications:
- Contraindicated in patients hypersensitive to drug and in those experiencing parkinsonism, coma, or CNS depression.
Side Effects:
- GI: constipation, dry mouth, nausea, vomiting, diarrhea
- CNS: lethargy, headache, insomnia, confusion, vertigo
- Skin: rash, other skin reactions, diaphoresis
Adverse Reaction:
- CNS: severe extrapyramidal reactions, tardive dyskinesia, sedation, drowsiness, seizures, neuroleptic malignant syndrome.
- CV: tachycardia, hypotension, hypertension, ECG changes.
- EENT: blurred vision.
- GU: urine retention, menstrual irregularities, priapism.
- Hematologic: leukopenia, leukocytosis.
- Hepatic: jaundice.
- Skin: rash, other skin reactions, diaphoresis.
- Other: gynecomastia.
Nursing Responsibilities:
- A:
Assess mental status (orientation, mood, behavior) prior to and periodically during therapy.
Assess positive (hallucination, delusions) and negative (social isolation) symptoms of schizophrenia.
Monitor BP (sitting, standing, lying) and pulse prior to and frequently during the period of dose adjustment. May cause
QT interval changes on ECG.
- D: Disturbed thought process
- P: Patient will have a decrease in hallucinations, insomnia, agitation, hostility, and delusions
- I:
Direct IV: Diluent: May be administered undiluted for rapid control of acute psychosis or delirium. Concentration: 5
mg/mL. Rate: Administer at a rate of 5 mg/min.
- E:
Decrease in hallucinations, insomnia, agitation, hostility, and delusions.
Decreased tics and vocalization in Tourette’s syndrome.
Improved behavior in children with severe behavioral problems. If no therapeutic effects are seen in 2–4 wk, dosage
may be increased.
2. DIBENZOXAPINES
Brand Name: Loxitane
Classification: Dibenzoxapines
- Psychotic disorders.
Adults: Initially, 10 mg P.O. b.i.d. (in severe schizophrenia, 50 mg P.O. daily); usual therapeutic and maintenance
dosage is 60 to 100 mg P.O. daily b.i.d. to q.i.d. (dose varies from patient to patient) or 12.5 to 50 mg I.M. q 4 to 6 hours
or longer. Maximum daily dose is 250 mg. After desired symptom control, change to oral therapy. Don’t administer
drug I.V.
- A: Absorbed rapidly and completely from the GI tract. First-pass metabolism results in lower systemic availability. P.O., I.M.
– Onset:1/2 hr. Peak: 1 1/2-3 hr. Duration. 12 hr
- D: Distributed widely throughout the body, including breast milk. Steady state serum level is achieved within 3 to 4 days.
Drug is 91% to 99% protein-bound.
- M & E: Metabolized extensively by the liver, forming a few active metabolites; duration of action is 12 hours. Mostly
excreted as metabolites in urine; some is excreted in feces by way of the biliary tract. About 50% is excreted in urine and
feces within 24 hours.
Drug-Drug and Drug-Food Interactions:
- Aluminum- and magnesium-containing antacids and antidiarrheals: Decreases loxapine absorption and therapeutic
effects. Separate administration times.
- Antiarrhythmics, disopyramide, quinidine, procainamide: Increases risk of arrhythmias and conduction defects. Use
together cautiously.
- Anticholinergics, including antidepressants, antihistamines, antiparkinsonians, atropine, MAO inhibitors, meperidine,
phenothiazines: Causes oversedation, paralytic ileus, visual changes, and severe constipation. Avoid use together.
- Beta blockers: May inhibit loxapine metabolism, increasing plasma levels and toxicity. Use together cautiously.
- Bromocriptine: May antagonize therapeutic effect of bromocriptine on prolactin secretion. Monitor patient for effect.
- Centrally acting antihypertensives, such as clonidine, guanabenz, guanadrel, guanethidine, methyldopa, and reserpine: May
inhibit blood pressure response. Use together cautiously.
- CNS depressants, including analgesics, anesthetics (general, spinal, and epidural), barbiturates, narcotics, tranquilizers, and
parenteral magnesium sulfate: May cause additive effects.
Indications:
Contraindications:
- Contraindicated in patients hypersensitive to dibenzoxazepines and in patients experiencing coma, severe CNS depression,
or drug-induced depressed states.
Side Effects:
Adverse Reaction:
Nursing Responsibilities:
- A:
Assess mental status (orientation, mood, behavior) prior to and periodically during therapy.
Assess positive (hallucination, delusions) and negative (social isolation) symptoms of schizophrenia.
Monitor BP (sitting, standing, lying) and pulse prior to and frequently during the period of dose adjustment. May cause
QT interval changes on ECG.
- D: Disturbed thought process
- P: Patient will have a decrease in hallucinations, insomnia, agitation, hostility, and delusions
- I:
Direct IV: Diluent: May be administered undiluted for rapid control of acute psychosis or delirium. Concentration: 5
mg/mL. Rate: Administer at a rate of 5 mg/min.
- E:
Decrease in hallucinations, insomnia, agitation, hostility, and delusions.
Decreased tics and vocalization in Tourette’s syndrome.
Improved behavior in children with severe behavioral problems. If no therapeutic effects are seen in 2–4 wk, dosage
may be increased.
3. DIHYDROINDOLONES
Brand Name: Moban
Classification: Dihydroindolones
- Psychotic disorders. Adults: 50 to 75 mg P.O. daily in 3 to 4 divided doses, increased 100 mg daily in 3 to 4 days to a
maximum of 225 mg daily. Maintenance dosage for mild disease is 5 to 15 mg t.i.d. or q.i.d., moderate disease is 10 to 25
mg t.i.d. or q.i.d., and severe disease is up to 225 mg daily.
- Behavioral complications related to mental retardation, mentally retarded schizophrenic child: Children ages 3 to 5: 1 to 2.5
mg P.O. daily as a single dose.
- A: Data are limited, but absorption seems to be rapid. PO – Peak: 1 ½ hr. Duration: 24-36hrs.
- D: Distributed widely into the body. Drug is 90% to 95% protein-bound.
- M & E: Metabolized extensively in the liver. Most of drug is excreted as metabolites in urine; some is excreted in feces by
way of the biliary tract. Overall, 90% of a given dose is excreted within 24 hours.
Indications:
Contraindications:
- MOBAN is contraindicated in severe central nervous system depression (alcohol, barbiturates, narcotics, etc.) or comatose
states, and in patients with known hypersensitivity to the drug.
Side Effects:
- Hepatic: jaundice
- Hemato: leukocytosis
- Hypersensitivity: allergic reactions
Adverse Reaction:
- CNS: extrapyramidal reactions, tardive dyskinesia, sedation, drowsiness, depression, euphoria, pseudoparkinsonism, EEG
changes, dizziness.
- CV: orthostatic hypotension, tachycardia, ECG changes.
- EENT: blurred vision.
- GI: dry mouth, constipation, nausea.
- GU: urine retention, menstrual irregularities, inhibited ejaculation.
- Hematologic: leukopenia
- Skin: mild photosensitivity
- Other: gynecomastia.
Nursing Responsibilities:
- A:
Assess mental status (orientation, mood, behavior) prior to and periodically during therapy.
Assess positive (hallucination, delusions) and negative (social isolation) symptoms of schizophrenia.
Monitor BP (sitting, standing, lying) and pulse prior to and frequently during the period of dose adjustment. May cause
QT interval changes on ECG.
- D: Disturbed thought process
- P: Patient will have a decrease in hallucinations, insomnia, agitation, hostility, and delusions
- I:
Monitor patient for CNS adverse effects, especially drowsiness and extrapyramidal symptoms.
Monitor CBC and liver function tests in long-term therapy.
- E:
Decrease in hallucinations, insomnia, agitation, hostility, and delusions.
Decreased tics and vocalization in Tourette’s syndrome.
Improved behavior in children with severe behavioral problems. If no therapeutic effects are seen in 2–4 wk, dosage
may be increased.
4. THIOXANTHENES
Classification: Thioxanthenes
- Acute agitation. Adults: 4 mg I.M. b.i.d. to q.i.d. Maximum dosage is 30 mg I.M. daily. Change to P.O. form as soon as
possible.
- Mild to moderate psychosis. Adults: Initially, 2 mg P.O. t.i.d. May increase gradually to 15 mg daily. Maximum dose is 60
mg daily.
- Severe psychosis. Adults: Initially, 5 mg P.O. b.i.d. May increase gradually to 20 to 30 mg daily. Maximum recommended
dose is 60 mg daily.
Indications:
- Navane is effective in the management of schizophrenia. Navane has not been evaluated in the management of behavioral
complications in patients with mental retardation.
Contraindications:
- Contraindicated in patients hypersensitive to drug and in those experiencing circulatory collapse, coma, CNS depression, or
blood dyscrasia.
Side Effects:
Adverse Reaction:
Nursing Responsibilities:
- A:
Assess patient’s mental status (orientation, mood, behavior) before and periodically throughout therapy.
Monitor blood pressure (sitting, standing, lying), pulse, and respiratory rate before and frequently during the period of
dosage adjustment.
Observe patient carefully when administering medication to ensure medication is actually taken and not hoarded.
- D: Disturbed thought process
- P: Patient will have a decrease in excitable, paranoic, or withdrawn behavior.
- I:
PO: Administer with food, milk, or a full glass of water to minimize gastric irritation.
Dilute the concentrate in 2 to 4 oz (60 to 120 ml) of liquid, preferably water, carbonated drinks, fruit juice, tomato
juice, milk, or pudding.
- E:
Decrease in excitable, paranoic, or withdrawn behavior.
b. Atypical Antipsychotics
- Treatment of schizophrenia in severely ill patients unresponsive to other therapies. Adults: Initially, 12.5 mg P.O. once or
twice daily, adjusted upward at 25 to 50 mg daily (if tolerated) to a daily dose of 300 to 450 mg by end of 2 weeks.
Individual dosage is based on clinical response, patient tolerance, and adverse reactions. Subsequent dosage increases
should occur no more than once or twice weekly and shouldn’t exceed 100 mg. Many patients respond to doses of 300 to
600 mg daily, but some patients require as much as 900 mg daily. Don’t exceed 900 mg daily.
- A: Food doesn’t appear to interfere with bioavailability. Only 27% to 50% of the dose reaches systemic circulation. PO –
Peak: 2 ½ hrs. Duration: 4-12hrs.
- Distribution: About 97% bound to serum proteins.
- M & E: Metabolism is nearly complete; very little unchanged drug appears in the urine. About 50% appears in the urine and
30% in the feces, mostly as metabolites. Elimination half-life appears to be proportional to dose and may range from 4 to 66
hours.
Indications:
- Clozaril is used to treat people with schizophrenia in whom other medicines have not worked.
Contraindications:
- Contraindicated in patients with uncontrolled epilepsy or history of clozapine-induced agranulocytosis; in patients with a
WBC count below 3,500/mm3
- In patients with severe CNS depression or coma
- In patients taking other drugs that suppress bone marrow function
- In those with myelosuppressive disorders.
Side Effects:
Adverse Reaction:
Nursing Responsibilities:
- A:
Monitor patient’s mental status (orientation, mood, behavior) before and periodically during therapy.
Assess weight and BMI initially and throughout therapy. Refer as appropriate for nutritional/weight management and
medical management
- D:
Risk for other-directed violence (Indications)
Disturbed thought process (Indications)
Risk for injury (Side Effects)
- P: Patient will have a decrease in excitable, paranoic, or withdrawn behavior
- I:
PO: Administer capsules with food or milk to decrease gastric irritation.
Leave oral disintegrating tablet in blister until time of use. Do not push tablet through foil. Just before use, peel foil and
gently remove disintegrating tablet. Immediately place tablet in mouth and allow to disintegrate and swallow with
saliva. If 1/2 tablet dose used, destroy other half of tablet.
- E:
Decreased positive symptoms (delusions, hallucinations) of schizophrenia.
Decrease in negative symptoms (social withdrawal, flat, blunt affect) of schizophrenia.
2. ANXIOLYTICS
1. BENZODIAZEPINES
Brand Name:
- A: Well absorbed following oral administration. Rapidly and completely absorbed following IM administration. Sublingual
absorption is more rapid than oral and is similar to IM. PO Peak: 1-6hrs, PO Duration: 8-12hr.
- D: Widely distributed. Crosses the blood-brain barrier. Crosses the placenta; enters breast milk.
- M & E: Highly metabolized by the liver. Half-life: Full-term neonates: 18–73 hr; Older children: 6–17 hr; Adults: 10–16 hr.
Drug-Drug and Drug-Food Interactions:
Indications:
Side Effects:
Adverse Reaction:
- CNS: amnesia, agitation, ataxia, depression, disorientation, dizziness, drowsiness, headache, incoordination, asthenia
- CV (with too rapid I.V. administration): hypotension, bradycardia, tachycardia, apnea, cardiac arrest, cardiovascular –
collapse
- EENT: blurred vision, diplopia, nystagmus
- GI: nausea, abdominal discomfort
- Other: increased or decreased appetite
Nursing Responsibilities:
- A:
Monitor blood pressure, pulse, and respiratory status frequently throughout IV administration. Prolonged high-dose
therapy may lead to psychological or physical dependence.
Restrict the amount of drug available to patient, especially if patient is depressed, suicidal, or has a history of addiction.
- D: Anxiety
- P: Patient will have an improvement in sleep patterns.
- I:
PO: Tablet may also be given sublingually (unlabeled) for more rapid onset.
Take concentrated liquid solution with water, soda, pudding, or applesauce.
IM: Administer IM doses deep into muscle mass at least 2 hr before surgery for optimum effect.
- E:
Increase in sense of well-being.
Decrease in subjective feelings of anxiety without excessive sedation.
Reduction of preoperative anxiety.
Postoperative amnesia.
Improvement in sleep patterns
2. AZAPIRONES
Brand Name:
Classification: Azapirones
- Adults (including the elderly): The recommended starting dose is 5mg two to three times a day, which may be increased
every two to three days. The usual dose you will be maintained on is 15mg to 30mg a day in divided doses. The maximum
daily dosage should not exceed 60mg per day.
- Children: Not recommended.
- Absorption: Absorbed rapidly and completely after oral administration, but extensive first-pass metabolism limits absolute
bioavailability to 1% to 13% of the oral dose. Food slows absorption but increases the amount of unchanged drug in
systemic circulation.
- Distribution: 95% protein-bound; it doesn’t displace other highly protein-bound drugs such as warfarin.
- M & E: Metabolized in the liver by hydroxylation and oxidation, resulting in at least one pharmacologically active
metabolite, 1, pyrimidinylpiperazine (1-PP). 29% to 63% is excreted in urine in 24 hours, primarily as metabolites; 18% to
38% is excreted in feces.
Drug-Drug and Drug-Food Interactions:
Indications:
Contraindications:
Side Effects:
Adverse Reaction:
Nursing Responsibilities:
- A:
Assess degree and manifestations of anxiety before and periodically during therapy.
Buspirone does not appear to cause physical or psychological dependence or tolerance. However, patients with a
history of drug abuse should be assessed for tolerance or dependence. Restrict amount of drug available to these
patients.
- D;
Anxiety (Indications)
Risk for injury (Side Effects)
- P: Patient will have an increase in sense of well-being.
- I:
PO: May be administered with food to minimize gastric irritation. Food slows but does not alter extent of absorption.
- E:
Decrease in subjective feelings of anxiety. Some improvement may be seen in 7–10 days. Optimal results take 3–4 wk
of therapy. Buspirone is usually used for short-term therapy (3–4 wk). If prescribed for long-term therapy, efficacy
should be periodically assessed.
3. BENZODIAZEPINE ANTAGONIST
Brand Name:
- Anaesthesia:
The recommended starting dose for adults is 0.2 mg administered intravenously over 15 seconds. If the required level
of consciousness is not obtained within 60 seconds, a further dose of 0.1 mg can be injected and repeated at 60-second
intervals, up to a maximum dose of 1.0 mg. The usual dose required lies between 0.3 and 0.6 mg, but may deviate
depending on the patient’s characteristics and the benzodiazepine used.
- Intensive Care:
The recommended initial dose of Flumazenil for adults is 0.3 mg i.v. If the required level of consciousness is not
obtained within 60 seconds, a further dose of 0.1 mg can be injected and repeated at 60-second intervals, up to a total
dose of 2 mg or until the patient awakes. If drowsiness recurs, an intravenous infusion of 0.1 – 0.4 mg/h may be useful.
- None significant.
Indications:
- Complete/partial reversal of effects of benzodiazepines used as general anesthetics, or during diagnostic or therapeutic
procedures.
- Management of intentional or accidental overdose of benzodiazepines.
Contraindications:
Side Effects:
- CNS: Dizziness
- GI: Nausea, vomiting
Adverse Reaction:
- CNS: SEIZURES, dizziness, agitation, confusion, drowsiness, emotional lability, fatigue, headache, sleep disorders. EENT:
abnormal hearing, abnormal vision, blurred vision.
- CV: arrhythmias, chest pain, hypertension.
- GI: nausea, vomiting, hiccups.
- Skin: flushing, sweating.
- Local: pain/injectionsite reactions, phlebitis.
- Neuro: paresthesia.
Nursing Responsibilities:
- A:
Assess level of consciousness and respiratory status before and during therapy. Observe patient for at least 2 hr after
administration for the appearance of resedation. Hypoventilation may occur.
Overdose: Attempt to determine time of ingestion and amount and type of benzodiazepine taken. Knowledge of agent
ingested allows an estimate of duration of CNS depression.
- D:
Risk for injury
Risk for poisoning
- P: Patient will have an improved level of consciousness.
- I:
Ensure that patient has a patent airway before administration of flumazenil.
Observe IV site frequently for redness or irritation. Administer through a free-flowing IV infusion into a large vein to
minimize pain at the injection site.
Institute seizure precautions. Seizures are more likely to occur in patients who are experiencing sedative/hypnotic
withdrawal, patients who have recently received repeated doses of benzodiazepines, or those who have a previous
history of seizure activity. Seizures may be treated with benzodiazepines, barbiturates, or phenytoin. Larger than
normal doses of benzodiazepines may be required.
- E:
Improved level of consciousness.
Decrease in respiratory depression caused by benzodiazepines.
3. ANTIDEPRESSANTS
1. TRICYCLIC ANTIDEPRESSANTS (TCAs)
Brand Name:
- Depression.
Adults: Initially, 75 to 100 mg P.O. daily in divided doses, with 25- to 50-mg increments, up to 200 mg. Or, some
patients can start with lower doses (25 mg P.O.) and dosage is adjusted slowly in 25-mg increments every other day.
Maximum dose is 300 mg daily. Or, entire dosage may be given h.s. Maximum daily dose is 200 mg for outpatients, 300
mg for inpatients, 100 mg for elderly patients.
Elderly patients: Give 30 to 40 mg P.O. daily, not to exceed 100 mg daily. Start therapy at low doses (10 mg) and adjust
slowly.
- Childhood enuresis. Children age 6 and older: 25 to 75 mg P.O. daily, 1 hour before bedtime. Usual dose is 1.5 mg/kg daily
in three divided doses. Maximum dose is 2.5 mg/kg daily.
- Antiarrhythmics (disopyramide, procainamide, quinidine), pimozide, thyroid medication: May increase risk of arrhythmias
and conduction defects. Avoid use together.
- Atropine or other anticholinergic drugs, including antihistamines, antiparkinsonian agents, meperidine, and phenothiazines;
CNS depressants, including analgesics, anesthetics, barbiturates, narcotics, and tranquilizers: Causes oversedation, paralytic
ileus, visual changes, and severe constipation. Avoid use together.
- Barbiturates: Induces imipramine metabolism and decreases therapeutic efficacy. Avoid use together.
- Beta blockers, cimetidine, methylphenidate, hormonal contraceptives, propoxyphene: Inhibits imipramine metabolism,
increasing plasma levels and toxicity. Use together cautiously.
- Centrally acting antihypertensives, such as clonidine, guanabenz, guanadrel, guanethidine, methyldopa, and
reserpine: Decreases hypotensive effects of antihypertensives. Use cautiously.
- Disulfiram or ethchlorvynol: May cause delirium and tachycardia. Observe patient closely.
- Haloperidol and phenothiazines: Decreases metabolism of imipramine, decreasing therapeutic efficacy. Monitor patient
closely.
- Metrizamide: Increases risk of seizures. Monitor patient closely.
- Sympathomimetics, including ephedrine, epinephrine, and phenylephrine (often found in nasal sprays): May increase blood
pressure. Patient needs frequent blood pressure checks.
- Warfarin: May prolong PT and cause bleeding. Monitor PT and INR.
Indications:
Contraindications:
- Contraindicated during acute recovery phase of MI, in patients hypersensitive to drug, and in those receiving MAO
inhibitors.
Side Effects:
Adverse Reaction:
- CNS: excitation, tremor, confusion, hallucinations, anxiety, ataxia, paresthesia, nervousness, EEG
changes, seizures, extrapyramidal reactions, CVA.
- CV: tachycardia, ECG changes, hypertension, MI, arrhythmias, heart block, precipitation of heart failure.
- EENT: blurred vision, tinnitus, mydriasis.
- GI: anorexia, paralytic ileus, abdominal cramps.
- GU: testicular swelling, impotence.
- Skin: rash, urticaria, photosensitivity, pruritus.
- Other: gynecomastia, galactorrhea and breast enlargement, altered libido, SIADH, hypersensitivity reaction.
Nursing Responsibilities:
- A:
Monitor BP and pulse rate prior to and during initial therapy.
Monitor plasma levels in treatment-resisant patients.
For overweight/obese individuals, obtain FBS and cholesterol levels. Refer as appropriate for nutrition/weight
management and medical management.
- D:
Ineffective coping (Indications)
Chronic pain (Indications)
Impaired urinary elimination (Indications, Side Effects)
Sexual dysfunction (Side Effects)
- P: Patient will have an ncreased sense of well-being.
- I:
Dose increases should be made at bedtime because of sedation. Dose titration is a slow process; may take weeks to
months. May be given as a single dose at bedtime to minimize sedation during the day.
PO: Administer medication with or immediately following a meal to minimize gastric irritation.
- E:
Increased sense of well-being.
Renewed interest in surroundings.
Increased appetite.
Improved energy level.
Pain relief.
Diminished incidence of enuresis.
Improved sleep in patients treated for depression.
Patient may require 2–6 wk of therapy before full therapeutic effects of medication are noticeable.
Control of bedwetting in children less than 6 yrs.
Decrease in chronic neurogenic pain.
- Depression:
The recommended dose is 20 mg per day. This may be increased by your doctor to a maximum of 40 mg per day.
The exact dose will depend on how your condition responds to treatment
You will normally be asked to keep taking this medicine for at least 6 months
- Panic disorder (panic attacks):
The starting dose is 10 mg per day for the first week before increasing the dose to 20-30 mg per day. The dose may be
increased by your doctor to a maximum of 40 mg per day.
The exact dose will depend on how your condition responds to treatment.
- Older people (above 65 years of age):
The starting dose should be decreased to half of the recommended dose, e.g. 10-20 mg per day. Older people should
not usually receive more than 20 mg per day.
Indications:
- Depression
- Panic disorders including fear of wide open spaces (agoraphobia) or crowds
Contraindications:
- Contraindicated in patients hypersensitive to drug or its components, in those taking MAO inhibitors, and within 14 days of
MAO inhibitor therapy.
Side Effects:
Adverse Reaction:
- CNS: tremor, anxiety, agitation, dizziness, paresthesia, migraine, impaired concentration, amnesia, depression,
apathy, suicide attempt, confusion, fatigue, fever.
- CV: tachycardia, orthostatic hypotension, hypotension.
- EENT: rhinitis, sinusitis, abnormal accommodation.
- GI: diarrhea, anorexia, dyspepsia, vomiting, abdominal pain, taste perversion, increased saliva, flatulence, increased
appetite.
- GU: dysmenorrhea, amenorrhea, ejaculation disorder, impotence, polyuria.
- Metabolic: hyponatremia, weight changes.
- Musculoskeletal: arthralgia, myalgia.
- Respiratory: upper respiratory tract infection, cough.
- Skin: rash, pruritus.
- Other: yawning, decreased libido, SIADH.
Nursing Responsibilities:
- A:
Assess for suicidal tendencies, especially during early therapy and dose changes. Restrict amount of drug available to
patient. Risk may be increased in children, adolescents, and adult.. After starting therapy, children, adolescents, and
young adults should be seen by health care professional at least weekly for 4 wk, every 3 wk for the next 4 wk, and on
advice of health care professional thereafter.
- D:
Ineffective coping (Indications)
Chronic pain (Indications)
Impaired urinary elimination (Indications, Side Effects)
Sexual dysfunction (Side Effects)
- P: Patient will have an increased sense of well-being.
- I:
Dose increases should be made at bedtime because of sedation. Dose titration is a slow process; may take weeks to
months. May be given as a single dose at bedtime to minimize sedation during the day.
PO: Administer medication with or immediately following a meal to minimize gastric irritation.
- E:
Increased sense of well-being.
Renewed interest in surroundings
- Depression. Adults: Initially, 75 mg P.O. daily, in two or three divided doses with food. Increase dosage as tolerated and
needed in increments of 75 mg daily at intervals of no less than 4 days. For moderately depressed outpatients, usual
maximum dose is 225 mg daily. In certain severely depressed patients, dosage may be as high as 375 mg daily divided into
three doses. For extended-release capsules, 75 mg P.O. daily, in a single dose. For some patients, it may be desirable to
start at 37.5 mg P.O. daily for 4 to 7 days before increasing to 75 mg daily. Dosage may be increased at increments of 75 mg
daily q 4 days to a maximum of 225 mg daily.
- Generalized anxiety disorder. Adults: Initially, 75 mg daily (extended-release) in a single dose. Increase dosage as needed in
75-mg daily increments at intervals of at least 4 days. Maximum, 225 mg daily.
- Prevention of major depressive disorder relapse : Adults: 100 to 200 mg (Effexor) P.O. daily or 75 to 225 mg (Effexor XR)
P.O. daily.
- Cimetidine, CNS-active drugs: Significantly increases venlafaxine level in elderly patients and those with hepatic dysfunction
or hypertension.
- MAO inhibitors: May precipitate a syndrome similar to neuroleptic malignant syndrome when used with venlafaxine. Don’t
start venlafaxine within 14 days of stopping an MAO inhibitor; don’t start MAO inhibitor within 7 days of stopping
venlafaxine.
Indications:
- Treatment of depression.
- Treatment of generalized anxiety disorder (GAD), social anxiety disorder (SAD).
- Treatment of panic disorder, with or without agoraphobia.
Contraindications:
- Contraindicated in patients hypersensitive to drug and within 14 days of MAO inhibitor therapy.
Side Effects:
Nursing Responsibilities:
- A: Obtain initial weight, B/P. Assess appearance, behavior, speech pattern, level of interest, mood. Assess risk of suicide
- D:
Ineffective coping (Indications)
Risk for injury (Side Effects)
- P: Patient will have a decreased anxiety.
- I:
Monitor signs/symptoms of depression, B/P, weight.
Assess sleep pattern for evidence of insomnia. Check during waking hours for drowsiness, dizziness, anxiety; provide
assistance as necessary.
Assess appearance, behavior, speech pattern, level of interest, mood for therapeutic response.
Monitor for suicidal ideation (esp. at initiation of therapy or changes in dosage).
- E:
Increased sense of well-being.
Renewed interest in surroundings. Need for therapy should be periodically reassessed. Therapy is usually continued for
several months.
Decreased anxiety.
- Amphetamines, ephedrine, phenylephrine, other related drugs: Enhances pressor effects. Avoid use together.
- Barbiturates, dextromethorphan, narcotics, tricyclic antidepressants, other sedatives: Increases adverse reactions.
- Disulfiram: May cause tachycardia, flushing, or palpitations. Monitor patient closely.
General, spinal anesthetics: Causes severe hypotension and excessive CNS depression. Avoid use together.
- Local anesthetics (lidocaine, procaine): Decreases effectiveness of these drugs; causes poor nerve block. Stop phenelzine for
at least 1 week before giving these drugs.
- OTC cold, hay fever, weight-reduction products: Causes serious CV toxicity. Avoid use together.
- Serotonergic drugs (fluoxetine, fluvoxamine, paroxetine, sertraline), tricyclic antidepressants: Causes serious adverse
effects. At least a 2-week waiting period between drug use is recommended.
Indications:
Contraindications:
- Contraindicated in patients hypersensitive to drug and in those with heart failure, pheochromocytoma, hypertension, liver
disease, or CV disease.
- Also contraindicated during therapy with other MAO inhibitors
Side Effects:
- CNS: dizziness
- GI: anorexia
Adverse Reaction:
- CNS: vertigo, headache, hyperreflexia, tremor, muscle twitching, insomnia, drowsiness, weakness, fatigue.
- CV: orthostatic hypotension, edema.
- GI: dry mouth, nausea, constipation.
- GU: elevated urinary catecholamine levels, sexual disturbances.
- Metabolic: weight gain.
- Skin: diaphoresis.
Nursing Responsibilities:
- A:
Assess mental status (orientation, mood, behavior) and anxiety level frequently. Assess for suicidal tendencies,
especially during early therapy. Restrict amount of drug available to patient.
Monitor BP and pulse before and frequently during therapy. Report significant changes promptly. Headache is often
first symptom of a hypertensive crisis.
Monitor intake and output ratios and daily weight. Assess patient for urinary retention.
- D:
Ineffective coping (Indications)
Ineffective therapeutic regimen management (Patient/Family Teaching)
Risk for falls (Side Effects)
Imbalanced nutrition: more than body requirements (Side Effects)
Sexual dysfunction (Side Effects)
Impaired oral mucous membrane (Side Effects)
- P: The patient will have an increased sense of well-being.
- I:
Do not administer these medications in the evening because the psychomotor stimulating effects may cause insomnia
or other sleep disturbances.
PO: Tablets may be crushed and mixed with food or fluids for patients with difficulty swallowing.
- E:
Improved mood in depressed patients.
Increased sense of well-being.
Decreased anxiety.
Increased appetite.
Improved energy level.
Improved sleep.
5. ATYPICAL ANTIDEPRESSANTS
Brand Name:
- Depression. Adults: Initially, 150 mg daily in divided doses, which can be increased by 50 mg daily q 3 to 4 days. Average
dose ranges from 150 mg to 400 mg daily. Maximum dose is 400 mg daily in outpatients; 600 mg daily in hospitalized
patients.
- Aggressive behavior: Adults: 50 mg P.O. b.i.d.
- Panic disorder: Adults: 300 mg P.O. daily.
- A: Well absorbed from GI tract. Taking drug with food delays absorption and increases amount absorbed by 20%. PO –
Peak: 1-2hrs
- D: Widely distributed throughout the body. Drug isn’t concentrated in any particular tissue, but small amounts may appear
in breast milk. About 90% is protein-bound. Proposed therapeutic drug levels haven’t been established. Steady state plasma
levels are reached in 3 to 7 days, and onset of therapeutic activity occurs in 7 days.
- M&E: Metabolized by the liver; more than 75% of metabolites are excreted within 3 days. Mostly excreted in urine; the rest
is excreted in feces via the biliary tract.
- Antihypertensives, CNS depressants: Causes additive effects of antihypertensives and CNS depressants. Monitor patient
closely. Dosage adjustment may be needed.
- Digoxin, phenytoin: Increases serum levels of digoxin and phenytoin. Monitor patient closely.
- Selective serotonin reuptake inhibitors: Increases risk of serotonin syndrome.
Indications:
Contraindications:
Side Effects:
Adverse Reaction:
- CNS: drowsiness, dizziness, nervousness, fatigue, confusion, tremor, weakness, hostility, anger, nightmares, vivid dreams,
headache, insomnia, generalized tonic-clonic seizures.
- CV: orthostatic hypotension, tachycardia, hypertension, prolonged conduction time on ECG, syncope.
- EENT: blurred vision, tinnitus, nasal congestion.
- GI: dry mouth, dysgeusia, constipation, nausea, vomiting, anorexia.
- GU: urine retention; priapism, possibly leading to impotence; hematuria.
- Hematologic: anemia.
- Metabolic: altered serum glucose levels.
- Respiratory: shortness of breath.
- Skin: rash, urticaria, diaphoresis.
- Other: decreased libido.
Nursing Responsibilities:
- A:
Assess mental status (orientation, mood, behavior) and anxiety level frequently. Assess for suicidal tendencies,
especially during early therapy. Restrict amount of drug available to patient.
Monitor BP and pulse before and frequently during therapy. Report significant changes promptly. Headache is often
first symptom of a hypertensive crisis.
Monitor intake and output ratios and daily weight. Assess patient for urinary retention.
- D:
Ineffective coping (Indications)
Ineffective therapeutic regimen management (Patient/Family Teaching)
Risk for falls (Side Effects)
Imbalanced nutrition: more than body requirements (Side Effects)
Sexual dysfunction (Side Effects)
Impaired oral mucous membrane (Side Effects)
- P: The patient will have an increased sense of well-being.
- I:
Do not administer these medications in the evening because the psychomotor stimulating effects may cause insomnia
or other sleep disturbances.
PO: Tablets may be crushed and mixed with food or fluids for patients with difficulty swallowing.
- E:
Improved mood in depressed patients.
Increased sense of well-being.
Decreased anxiety.
Increased appetite.
Improved energy level.
Improved sleep.
-
- Depression. Adults: Initially, 100 mg P.O. b.i.d. or 75 mg P.O. t.i.d. If needed, increase after 3 days to usual dosage of 100
mg P.O. t.i.d. If no response occurs after several weeks of therapy, consider increasing dosage to 150 mg t.i.d. Maximum,
450 mg daily. For sustained-release tablets, start with 150 mg P.O. q morning; increase to target dosage of 150 mg P.O.
b.i.d. as tolerated as early as day 4 of dosing. If no response after several weeks of therapy, increase to 200 mg b.i.d.
Maximum, 400 mg daily.
- Levodopa, MAO inhibitors, phenothiazines, recent and rapid withdrawal of benzodiazepines, tricyclic
antidepressants: Increase risk of adverse effects, including seizures.
Indications:
Contraindications:
Side Effects:
Adverse Reaction:
- CNS: seizures, anxiety, delusions, euphoria, hostility, impaired sleep quality, insomnia, sedation, tremor, akinesia, akathisia,
agitation, dizziness, syncope, fatigue, fever.
- CV: hypertension, hypotension, palpitations, tachycardia.
- EENT: blurred vision.
- GI: taste disturbance, increased appetite, constipation, dyspepsia, diarrhea.
- GU: impotence, menstrual complaints, urinary frequency, urine retention.
- Metabolic: hyperglycemia.
- Musculoskeletal: arthritis.
- Skin: pruritus, rash, cutaneous temperature disturbance, excessive diaphoresis.
- Other: chills, decreased libido.
Nursing Responsibilities:
- A: Monitor mood changes. Inform health care professional if patient demonstrates significant increase in anxiety,
nervousness, or insomnia.
- D: Ineffective coping (Indications)
- P: Patient will have an increased sense of well-being.
- I:
Administer doses in equally spaced time increments during the day to minimize the risk of seizures.
Risk of seizures increases four fold in doses greater than 450 mg per day.
PO: Swallow sustained-release or extended-release tablets whole; do not break, crush, or chew.
May be administered with food to lessen GI irritation.
- E:
Increased sense of well-being.
Renewed interest in surroundings. Acute episodes of depression may require several months of treatment.
5. MOOD STABILIZERS
Brand Name: Negretol
Classification: Iminostilbenes
- A: Absorption is slow but complete. Suspension produces earlier, higher peak, and lower trough levels. Peak: 4-5hr.
Duration: 6-12hrs.
- D: Widely distributed. Crosses the blood-brain barrier. Crosses the placenta rapidly and enters breast milk in high
concentrations. Protein Binding: Carbamazepine—75–90%; epoxide—50%.
- M & E: Extensively metabolized in the liver by cytochrome P450 3A4 to active epoxide metabolite; epoxide metabolite has
anticonvulsant and antineuralgic activity. Half-life: Carbamazapine—single dose—25– 65 hr, chronic dosing—Children—8–
14 hr; Adults—12–17 hr; epoxide—34_9 hr.
Drug-Drug and Drug-Food Interactions:
- CYP3A4 inhibitors (e.g., cimetidine, clarithromycin, azole antifungals, protease inhibitors) may increase concentration.
- CYP3A4 inducers (e.g., rifampin, phenytoin) may decrease concentration/effects.
- May decrease concentration/effects of hormonal contraceptives, warfarin, trazodone.
Indications:
Contraindications:
Side Effects:
Adverse Reaction:
- CNS: ataxia, drowsiness, fatigue, psychosis, syncope, vertigo, headache, worsening of seizures
- CV: hypertension, hypotension, arrhythmias, atrioventricular block, aggravation of coronary artery disease, heart failure
- EENT: blurred vision, diplopia, nystagmus, corneal opacities, conjunctivitis, pharyngeal dryness
- GI: nausea, vomiting, diarrhea, abdominal pain, stomatitis, glossitis, dry mouth, anorexia
- GU: urinary hesitancy, retention, or frequency; albuminuria; glycosuria; erectile dysfunction
- Hematologic: eosinophilia, lymphadenopathy, agranulocytosis, aplastic anemia, thrombocytopenia, leukopenia
- Hepatic: hepatitis
- Metabolic: syndrome of inappropriate antidiuretic hormone secretion
- Respiratory: pneumonitis
- Skin: photosensitivity, rash, urticaria, diaphoresis, erythema multiforme, Stevens-Johnson syndrome
- Other: weight gain, chills, fever
Nursing Responsibilities:
- A:
CBC, serum iron determination, urinalysis, BUN should be performed before therapy begins and periodically during
therapy.
Seizures: Review history of seizure disorder (intensity, frequency, duration, level of consciousness [LOC]).
Initiate seizure precautions.
Neuralgia: Assess facial pain, stimuli that may cause facial pain.
Bipolar: Assess mental status, cognitive abilities
- D:
Disturbed thought process
Risk for injury
Chronic pain
- P: Patient will have an absence or reduction of seizure activity
- I:
Administer medication with food to minimize gastric irritation.
May take at bedtime to reduce daytime sedation.
Tablets may be crushed if patient has difficulty swallowing.
Do not crush or chew extended-release tablets.
- E:
Absence or reduction of seizure activity.
Decrease in trigeminal neuralgia pain. Patients with trigeminal neuralgia who are pain-free should be re-evaluated
every 3 mo to determine minimum effective dose.
Decreased mania and depressive symptoms in Bipolar I disorder.