Clorazepate
Mechanism :
Clorazepate is a benzodiazepine. Thus, it acts by binding to GABA-A receptors and increasing their affinity to GABA, an inhibitory neurotransmitter. On binding to the receptor, GABA causes opening of the chloride channels resulting in a hyperpolarized state of the cell membrane. This prevents the transmission of impulses hence resulting in CNS depression which may present as sedation, skeletal muscle relaxation and anticonvulsant activity. Acting as pre synaptic inhibitons suppressing transmission of sizure impulses.
Indication :
- Generalized Anxiety Disorder
- Acute Alcohol Withdrawal
- Partial Seizures
Contraindications :
- Benzodiazepine hypersensitivity
- Narrow Angle Glaucoma
- Caution in:
- Concomitant use of other CNS depressants, Pulmonary disease
- Concomitant use of alcohol/ drugs of potential abuse
- Depression and/or suicidal ideation
- Porphyria
- Psychosis
- Respiratory depression due to other underlying conditions, respiratory insufficienciency sleep apnea.
- Those using heavy machinery and/or driving
4. Avoid abrupt cessation
Dosing :
Tablets available in following doses: 3.75 mg, 7.5 mg, 15 mg.
In Pediatric patients, Clorazepat is only indicated for partial seizures as adjunctive therapy.
<9 Years: Safety and efficacy not established.
9-12 years: 3.75 mg to 7.5 mg PO BID, increase by not more than 7.5 mg per week
Maximum dose: 60 mg/day.
Adverse Effect :
Severe:
- Suicidal Ideation
- Neonatal Respiratory Depression
- Neonatal Abstinence Syndrome
- Teratogenesis
Common:
- Dizziness
- Drowsiness
- Blurred vision
- Dry mouth
- Headache
- Confusion
- Nervousness
- Gastro intentinal complaints
Interaction :
- When used concomitantly with opioids, the risk of respiratory depression and sedation are increased. Thus limitation of dose and duration is advised
- Action of benzodiazepines can be potentiated by phenothiazines, narcotics, barbiturates, MAO inhibitor or other antidepressants.
Hepatic Dose :
Guidelines not available