CLORAZEPATE DIPOTASSIUM

CLORAZEPATE DIPOTASSIUM
(klor-az'e-pate)
Novoclopate , Tranxene, Tranxene-SD
Classifications: anxiolytic; sedative-hypnotic; anticonvulsant; benzodiazepine;
Therapeutic: antianxiety agent
; sedative-hypnotic; anticonvulsant
Prototype: Lorazepam
Pregnancy Category: D
Controlled Substance: Schedule IV

Availability

3.75 mg, 7.5 mg, 15 mg capsules and tablets; 11.25 mg, 22.5 mg long acting tablets

Action

Anxiolytic benzodiazepine with moderately rapid onset of action and a long half-life. Benzodiazepines exert their effects through enhancement of GABA-benzodiazepine receptor complex. GABA is an inhibitory neurotransmitter. Clorazepate has depressant effects on the CNS, thus controlling anxiety associated with stress and also resulting in sedative effects.

Therapeutic Effect

Effective in controlling anxiety and withdrawal symptoms of alcohol.

Uses

Management of anxiety disorders, short-term relief of anxiety symptoms, as adjunct in management of partial seizures, and symptomatic relief of acute alcohol withdrawal.

Contraindications

Hypersensitivity to clorazepate and other benzodiazepines; acute narrow-angle glaucoma; depressive neuroses; pulmonary disease, COPD; psychotic reactions, drug abusers. Safe use during pregnancy (category D), lactation, and in children <9 y not established.

Cautious Use

Older adults; debilitated patients; hepatic disease; kidney disease; Parkinson's disease; neuromuscular disease; seizure disorders; bipolar disorder, mania, history of suicidal ideation.

Route & Dosage

Anxiety
Adult: PO 15 mg/d h.s., may increase to 15–60 mg/d in divided doses (max: 60 mg/d)

Acute Alcohol Withdrawal
Adult: PO 30 mg followed by 30–60 mg in divided doses (max: 90 mg/d), taper by 15 mg/d over 4 d to 7.5–15 mg/d until patient is stable

Partial Seizures
Adult: PO 7.5 mg t.i.d.
Child (9–12 y): PO 3.75–7.5 mg b.i.d., may increase by no more than 3.75 mg/wk (max: 60 mg/d)

Administration

Oral
  • Give with food to minimize gastric distress. Give antacid no less than 1 h before or 1 h after drug ingestion.
  • Ensure that sustained-release form of drug is not chewed or crushed. It must be swallowed whole.
  • Taper drug dose gradually over several days when drug is to be discontinued. Abrupt termination may lead to memory impairment, severe GI symptoms, muscle pain, restlessness, irritability, fatigue, insomnia.
  • Store in light-resistant container at 15°–30° C (59°–86° F) unless otherwise specified.

Adverse Effects (≥1%)

Body as a Whole: Allergic reactions. CV: Hypotension. GI: GI disturbances, abnormal liver function tests, xerostomia. Hematologic: Decreased Hct, blood dyscrasias. CNS: Drowsiness, ataxia, dizziness, headache, paradoxical excitement, mental confusion, insomnia. Special Senses: Diplopia, blurred vision.

Interactions

Drug: Alcohol and other cns depressants compound CNS depression; clorazepate increases effects of cimetidine, disulfiram, causing excessive sedation. Herbal: Ginkgo may decrease anticonvulsant effectiveness.

Pharmacokinetics

Absorption: Decarboxylated in stomach; absorbed as active metabolite, desmethyldiazepam. Peak: 1 h. Duration: 24 h. Distribution: Crosses placenta; distributed into breast milk. Metabolism: In liver to oxazepam. Elimination: Primarily in urine. Half-Life: 30–200 h.

Nursing Implications

Assessment & Drug Effects

  • Drowsiness, a common side effect, is more likely to occur at initiation of therapy and with dose increments on successive days.
  • Lab tests: Periodic blood counts and tests of liver and kidney function should be performed throughout therapy.
  • Monitor patient with history of cardiovascular disease in early therapy for drug-induced responses. If systolic BP drops more than 20 mm Hg or if there is a sudden increase in pulse rate, withhold drug and notify physician.

Patient & Family Education

  • Take drug as prescribed and do not change dose or abruptly stop taking the drug without physician's approval.
  • Do not self-dose with OTC drugs (cold remedies, sleep medications, antacids) without consulting physician.
  • Avoid driving and other potentially hazardous activities until reaction to drug is known.
  • Do not use alcohol and other CNS depressants while on clorazepate therapy.
  • If a woman becomes pregnant during therapy or intends to become pregnant, communicate with physician about the desirability of discontinuing the drug.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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