Clorazepate
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Clorazepate
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| Systematic (IUPAC) name | |
| Potassium 7-chloro-2,3-dihydro-2-oxo-5-phenyl- 1H-1,4-benzodiazepine-3-carboxylate with potassium hydroxide |
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| Identifiers | |
| CAS number | 57109-90-7 |
| ATC code | N05BA05 |
| PubChem | 22312 |
| DrugBank | APRD00881 |
| Chemical data | |
| Formula | C16H11ClK2N2O4 (dipotassium salt) |
| Mol. weight | 408.9 (Dipotassium salt) |
| Pharmacokinetic data | |
| Bioavailability | 91% |
| Metabolism | Hepatic |
| Half life | 36-100 hours |
| Excretion | Renal |
| Therapeutic considerations | |
| Pregnancy cat. |
D (USA) |
| Legal status |
Schedule IV(US) |
| Routes | Oral |
Clorazepate (marketed under the brand names Tranxene® and Tranxilium®) is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties.
Clorazepate has been discontinued since February 2006 in the UK.
[edit] Indications
Clorazepate is used in the treatment of anxiety disorders and insomnia. It may also be prescribed as an anticonvulsant or muscle relaxant.
Clorazepate is principally prescribed in the treatment of alcohol withdrawal and epilepsy, although it is also a useful anxiolytic because of its long half-life. The normal starting dosage range of clorazepate is 15-60 mg 2-4 x per day. Dosages as high as 90-120 mg per day may be used in the treatment of acute alcohol withdrawal. Clorazepate is available in 3.75, 7.5, and 15 mg capsules or tablets. Clorazepate SD (controlled release) is available in 11.25 and 22.5 mg tablets. Clorazepate SD is only prescribed when the patient has become adjusted to a certain dosage, and is taken once a day. Clorazepate is available in generic form. Clorazepate begins to act on the central nervous system within one or two hours, and its effects may be felt for an entire day or longer in some individuals. It is contraindicated for those with impaired renal or hepatic function. Clorazepate is listed under Schedule IV of the Controlled Substances Act. Clorazepate was approved for use in the United States by the Food and Drug Administration in 1972.
[edit] Interactions
All sedatives are likely to magnify the effects of Tranxene® on the central nervous system. Cimetidine inhibits breakdown of clorazepate, and leads to increased levels of the drug in the system.
