No

Benzodiazepine

Management of anxiety disorders

C-IV

D

Hypersensitivity to this drug or any component of its formulation (cross-sensitivity with other benzodiazepines may exist); narrow-angle glaucoma; pregnancy

Use with caution in elderly or debilitated patients, patients with hepatic disease (including alcoholics), or renal impairment. Active metabolites with extended half-lives may lead to delayed accumulation and adverse effects. 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.

>10%: Central nervous system: Drowsiness

1% to 10%:

Cardiovascular: Tachycardia, hypotension, bradycardia

Central nervous system: Confusion, headache, apathy, euphoria, disorientation

Dermatologic: Dermatitis, rash

Gastrointestinal: Increased salivation, xerostomia, nausea, sense of seasickness, constipation

Ocular: Blurred vision

<1%: Menstrual irregularities, blood dyscrasias, reflex slowing, drug dependence

CYP3A3/4 enzyme substrate

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 halazepam; 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.

Half-life:

Parent: 14 hours

Active metabolite (desmethyldiazepam): 50-100 hours

Peak level: 1-3 hours

Oral:

Elderly greater than or equal to 70 years or debilitated patients: 20 mg 1-2 times/day and adjust dose accordingly

No information available to require special precautions

>10% of patients experience significant dry mouth; normal salivary flow occurs with cessation of drug therapy

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

Assist patient with ambulation

Monitor for alertness

Tablet: 20 mg, 40 mg