Clorazepate


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Anxiety Initially, 30 mg/day in divided doses, then may gradually adjust dose to 15-60 mg/day , according to patient's response. Epilepsy; Alcohol withdrawal syndrome Up to 90 mg/day in divided doses.
Dosage Details
Oral
Alcohol withdrawal syndrome, Epilepsy
Adult: 90 mg daily in divided doses.
Child: 9-12 yr old: 60 mg in divided doses.
Elderly: and debilitated patients: Initiate at lower dose and adjust slowly.

Oral
Anxiety
Adult: Initially, 30 mg daily in divided doses, then may gradually adjust dose to 15-60 mg daily , according to patient's response.
Elderly: Initially, 7.5-15 mg daily.
Hepatic Impairment
Initiate at lower dose and adjust slowly.
Contraindications
Hypersensitivity (cross-sensitivity with other benzodiazepines may occur); narrow-angle glaucoma. Patients with depressive or psychotic disorders. child <9 yr. Pregnancy; lactation.
Special Precautions
Elderly, debilitated patients; hepatic disease, alcoholics; renal impairment; resp disease; impaired gag reflex; patients experiencing apnoea during sleep; operating machines or driving; patients on CNS depressant or psychoactive drug therapy; depression, esp those with suicidal tendencies; history of drug-dependence.
Adverse Reactions
Jaundice, hepatic necrosis; extrapyramidal disorders; acute attacks of porphyria in porphyric patients, hypotension; drowsiness, fatigue, ataxia, lightheadedness, memory impairment, insomnia, anxiety, headache, depression, slurred speech, confusion, nervousness, dizziness, irritability; rash; decreased libido; xerostomia, constipation, diarrhoea, decreased salivation, nausea, vomiting, increased or decreased appetite; dysarthria, tremor; blurred vision, diplopia.
Overdosage
Somnolence, impaired coordination, slurred speech, confusion, coma, and diminished reflexes, hypotension, seizures, respiratory depression and apnea also may occur. Treatment is symptomatic and supportive. Flumazenil, a benzodiazepine antagonist, may be used after evaluating the benefits and risks. If recent ingestion, emesis or gastric lavage followed by activated charcoal and a saline cathartic to remove any remaining drug. Monitor pulse, respiration and blood pressure. Admin IV fluids and maintain an adequate airway. IV norepinephrine or metaraminol may be used for hypotension. Haemodialysis is not likely to be useful.
Drug Interactions
Potentiates CNS effects of narcotic analgesics, barbiturates, phenothiazines, ethanol, antihistamines, MAO Inhibitors, sedative-hypnotics, cyclic antidepressants. CYP3A4 inhibitors eg, amprenavir, cimetidine, ciprofloxacin, clarithromycin may increase serum conc and toxicity of clorazepate. Carbamazepine, rifampin and rifabutin may decrease clorazepate therapeutic effects by enhancement of clorazepate metabolism.
Food Interaction
Grapefruit juice increases serum conc or toxicity risk of clorazepate. Herbs or nutraceuticals eg, valerian, St. John's wort, kava kava and gotu kola may increase CNS depression upon concomitant admin with clorazepate.
Action
Description: Clorazepate binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron within the central nervous system, limbic system, reticular formation resulting to an increase in chloride ion permeability which further leads to hyperpolarisation and stabilisation.
Onset: 1-2 hrs.
Duration: 8-24 hrs.
Pharmacokinetics:
Absorption: Following oral administration, complete absorption of the dose from the small intestine.
Distribution: Crosses the placenta and small amounts appear in the urine.
Metabolism: Rapidly activated to desmethyldiazepam via decarboxylation prior to absorption at low stomach pH; hepatic (as active oxazepam).
Excretion: Via urine.
Storage
Store at 15-30°C.
Disclaimer: This information is independently developed by MIMS based on Clorazepate from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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