No

Benzodiazepine

Treatment of insomnia

C-IV

X

Hypersensitivity to this drug or any component of its formulation (cross-sensitivity with other benzodiazepines may exist); narrow-angle glaucoma (not in product labeling, however, benzodiazepines are contraindicated); pregnancy

Should be used only after evaluation of potential causes of sleep disturbance. Failure of sleep disturbance to resolve after 7-10 days may indicate psychiatric or medical illness. A worsening of insomnia or the emergence of new abnormalities of thought or behavior may represent unrecognized psychiatric or medical illness and requires immediate and careful evaluation. Use with caution in elderly or debilitated patients, patients with hepatic disease (including alcoholics), or renal impairment. Use with caution in patients with respiratory disease or impaired gag reflex. Avoid use in patients with sleep apnea.

Use caution in patients with depression, particularly if suicidal risk may be present. Use with caution in patients with a history of drug dependence. Benzodiazepines have been associated with dependence and acute withdrawal symptoms on discontinuation or reduction in dose. Acute withdrawal, including seizures, may be precipitated after administration of flumazenil to patients receiving long-term benzodiazepine therapy.

Benzodiazepines have been associated with anterograde amnesia. Paradoxical reactions, including hyperactive or aggressive behavior have been reported with benzodiazepines, particularly in adolescent/pediatric or psychiatric patients. Does not have analgesic, antidepressant, or antipsychotic properties.

Cardiovascular: Palpitations

Central nervous system: Drowsiness, fatigue, ataxia, memory impairment, anxiety, depression, headache, confusion, nervousness, dizziness, incoordination, hypo- and hyperkinesia, agitation, euphoria, paranoid reaction, nightmares, abnormal thinking

Dermatologic: Dermatitis, pruritus, rash

Endocrine & metabolic: Decreased libido, menstrual irregularities

Gastrointestinal: Xerostomia, constipation, diarrhea, dyspepsia, anorexia, abnormal taste perception, nausea, vomiting, increased or decreased appetite, abdominal pain

Genitourinary: Impotence, incontinence

Hematologic: Blood dyscrasias

Neuromuscular & skeletal: Dysarthria, rigidity, tremor, muscle cramps, reflex slowing

Ocular: Blurred vision

Miscellaneous: Drug dependence

Decreased therapeutic effect: Carbamazepine, rifampin, rifabutin may enhance the metabolism of quazepam and decrease its therapeutic effect; consider using an alternative sedative/hypnotic agent

Increased toxicity: Cimetidine, ciprofloxacin, clarithromycin, clozapine, CNS depressants, diltiazem, disulfiram, digoxin, erythromycin, ethanol, fluconazole, fluoxetine, fluvoxamine, grapefruit juice, isoniazid, itraconazole, ketoconazole, labetalol, levodopa, loxapine, metoprolol, metronidazole, miconazole, nefazodone, omeprazole, phenytoin, rifabutin, rifampin, troleandomycin, valproic acid, verapamil may increase the serum level and/or toxicity of quazepam; monitor for altered benzodiazepine response

Binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at several sites within the central nervous system, including the limbic system, reticular formation. Enhancement of the inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to chloride ions. This shift in chloride ions results in hyperpolarization (a less excitable state) and stabilization.

Absorption: Oral: Rapid

Serum half-life:

Parent drug: 25-41 hours

Active metabolite: 40-114 hours

Adults: Oral: Initial: 15 mg at bedtime, in some patients the dose may be reduced to 7.5 mg after a few nights

No information available to require special precautions

>10% of patients will experience dry mouth which disappears with cessation of drug therapy

Avoid alcohol and other CNS depressants; avoid activities needing good psychomotor coordination until CNS effects are known; drug may cause physical or psychological dependence; avoid abrupt discontinuation after prolonged use

Provide safety measures (ie, side rails, night light, call button); remove smoking materials from area; supervise ambulation

Monitor respiratory and cardiovascular status

Tablet: 7.5 mg, 15 mg

Chung M, Hilbert JM, Gural RP, et al, "Multiple Dose Quazepam Kinetics," Clin Pharmacol Ther, 1984, 35(4):520-4.

Hilbert JM, Gural RP, Symchowicz S, et al, "Excretion of Quazepam Into Human Breast Milk," J Clin Pharmacol, 1984, 24(10):457-62.

Martinez HT and Serna CT, "Short-Term Treatment With Quazepam of Insomnia in Geriatric Patients," Clin Ther, 1982, 5(2):174-8.

Winsauer HJ and O'Hair DE, "Quazepam: Short-Term Treatment of Insomnia in Geriatric Outpatients," Curr Ther Res, 1984, 35(2):228-34.