Chlorazepate
Chlorazepate Uses, Dosage, Side Effects, Food Interaction and all others data.
A water-soluble benzodiazepine derivative effective in the treatment of anxiety. It has also muscle relaxant and anticonvulsant actions.
Clorazepate is a member of the group of drugs called benzodiazepines. Pharmacologically, clorazepate has the characteristics of the benzodiazepines. It has depressant effects on the central nervous system. The primary metabolite, nordiazepam, quickly appears in the blood stream. Studies in healthy men have shown that clorazenate has depressant effects on the central nervous system. Since orally administered clorazepate dipotassium is rapidly decarboxylated to form nordiazepam, there is essentially no circulating parent drug.
Trade Name | Chlorazepate |
Generic | Clorazepic acid |
Clorazepic acid Other Names | Chlorazepate, Clorazepate, Clorazepic acid |
Type | |
Formula | C16H11ClN2O3 |
Weight | Average: 314.723 Monoisotopic: 314.045819935 |
Protein binding | The protein binding of nordiazepam in plasma is high (97-98%). |
Groups | Approved, Illicit |
Therapeutic Class | |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Chlorazepate is a benzodiazepine used to treat anxiety, partial seizures, and alcohol withdrawal.
For the management of anxiety disorders or for the short-term relief of the symptoms of anxiety. Also used as adjunctive therapy in the management of partial seizures and for the symptomatic relief of acute alcohol withdrawal.
Chlorazepate is also used to associated treatment for these conditions: Acute Alcohol Withdrawal, Generalized Anxiety Disorder (GAD), Partial-Onset Seizures, Acute Anxiety
How Chlorazepate works
Benzodiazepines bind nonspecifically to benzodiazepine receptors BNZ1, which mediates sleep, and BNZ2, which affects affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of the inhibitory neurotransmitter GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.
Toxicity
Oral LD50 in rats is 1320 mg/kg. In monkeys, oral LD50 exceed 1600 mg/kg. Symptoms of overdose include confusion, coma, impaired coordination, sleepiness, and slowed reaction time.
Food Interaction
- Avoid alcohol.
- Take with or without food. The absorption is unaffected by food.
Elimination Route
Rapidly absorbed following oral administration (bioavailability is 91%).
Half Life
The serum half-life is about 2 days. Nordiazepam, the primary metabolite, quickly appears in the blood and is eliminated from the plasma with an apparent half-life of about 40 to 50 hours.
Elimination Route
The drug is metabolized in the liver and excreted primarily in the urine.
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