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Clotiazepam
Chemical compound From Wikipedia, the free encyclopedia
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Clotiazepam[3] (marketed under brand name Clozan, Distensan, Trecalmo, Rize, Rizen and Veratran) is a thienodiazepine drug which is a benzodiazepine analog. The clotiazepam molecule differs from benzodiazepines in that the benzene ring has been replaced by a thiophene ring.[4] It possesses anxiolytic,[5] skeletal muscle relaxant,[6] anticonvulsant, sedative properties.[7] Stage 2 NREM sleep is significantly increased by clotiazepam.[8]
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Indications
Clotiazepam has been trialed and found to be effective in the short-term management of anxiety.[9] Clotiazepam is also used as a premedicant in minor surgery in France and Japan, where the drug is commercially available under the brand names Veratran and Rize, respectively.[10][11]
Pharmacokinetics
A cross-over study in six healthy volunteers (median age 28 years) was conducted using single-dose pharmacokinetics of 5 mg clotiazepam drops, oral tablets, and sublingual tablets. The formulations had similar systemic availability. Compared with oral tablets, the sublingual route gave a lower peak concentration and a delayed peak time, while drops gave a greater maximum concentration with a similar peak time. The use of drops is suggested for a more marked initial effect and the sublingual route for easier administration, especially in the elderly.[12]
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Pharmacology
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Perspective
Similar to other benzodiazepines clotiazepam has anxiolytic, sedative, hypnotic, amnesic, anticonvulsant and muscle relaxant pharmacological properties.[7] Clotiazepam binds to the benzodiazepine site of the GABAA receptor where it acts as a full agonist; this action results in an enhanced GABA inhibitory effect at the GABAA receptor which results in the pharmacological effects of clotiazepam.[13]
Clotiazepam has a short elimination half-life and is less prone to accumulation after repeated dosing compared to longer-acting benzodiazepine agents. It is metabolised via oxidation.[14] Clotiazepam is metabolised to hydroxy-clotiazepam and desmethyl-clotiazepam. After oral ingestion of a single 5 mg dose of clotiazepam by three healthy volunteers the drug was rapidly absorbed.[15] The elimination half-life of the drug and its metabolites range from 6.5 hours to 18 hours. Clotiazepam is 99 percent bound to plasma protein.[15] In elderly men the elimination half-life is longer and in elderly women the volume of distribution is increased.[16] Individuals with liver impairment have a reduced volume of distribution as well as a reduced total clearance of clotiazepam; renal impairment does not affect the kinetics of clotiazepam.[17]
The dose equivalent to 10 mg diazepam is thought to be between 5 and 10 mg clotiazepam.
Side effects
Side effects experienced with this product will resemble those of other benzodiazepines. Drowsiness and asthenia are common side effects.[18] There has been a report of reversible hepatitis caused by clotiazepam.[19]
Abuse
Clotiazepam is a recognised drug of abuse.[20]
See also
References
External links
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