WARNINGMIXING OR WITHDRAWAL CAN BE DANGEROUS
Ordinary doses in combination with other depressants can fatally stop breathing. After prolonged dependency, stopping suddenly can also cause seizures or delirium; seek medical help.
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Clotiazepam
Clotiazepam is a thienodiazepine used for anxiety disorders or anxiety-induced insomnia1. It has sedative, anxiolytic, muscle relaxant, and anticonvulsant properties1, and increases stage 2 non-rapid eye movement sleep. Its structure contains a 1,4-diazepine ring fused to a thiophene ring2. It is categorized as a depressant3 and described as habit-forming4.
Dosage & Duration
Dosage
Doses are population estimates that vary widely between individuals.
Duration
Subjective Effects
Pharmacology
Pharmacodynamics
Clotiazepam acts as a full agonist at the benzodiazepine site of the GABA-A receptor and positively modulates GABA-A signaling, increasing the frequency of chloride channel opening and enhancing neuronal inhibition. Clotiazepam has muscle relaxant, anxiolytic, sedative, hypnotic, anticonvulsant, and amnesic effects linked to specific agonist action at a central receptor within the GABA-OMEGA receptor complex that modulates chloride-channel opening4. It also acts as an agonist at the translocator protein, although the functional significance of this secondary interaction is not specified.
Pharmacokinetics
Clotiazepam is rapidly absorbed after oral administration5 and has similar systemic availability in oral, drop, and sublingual formulations. Sublingual administration produces a lower and delayed peak concentration, while drops produce a higher peak concentration at a similar time. It was reported to be more than 99% bound to plasma protein5 and undergoes metabolism in which the liver plays a major role4. A study in three healthy volunteers given a single oral 5-mg dose reported clotiazepam elimination half-lives of 6.5, 7.0, and 17.8 hours; its two metabolites appeared and disappeared approximately in parallel with the parent compound5; half-life is longer in elderly men. Liver impairment reduces volume of distribution and total clearance, whereas renal impairment does not affect its kinetics.
Interactions
An unlisted combination is an unknown one, not a safe one. Check a dedicated combination chart before mixing.
Tolerance
Harm Potential
Addiction & Dependence
Psychological
HighClotiazepam is a recognised drug of abuse and is classified as habit-forming. As a thienodiazepine with benzodiazepine-like activity, it carries significant psychological dependence potential with regular use.
Physical
HighPhysical dependence develops with chronic use, consistent with other benzodiazepine-class substances. Withdrawal syndrome may occur upon discontinuation.
Toxicity
Reversible hepatitis has been described in association with clotiazepam.
History & Culture
Clotiazepam was described in a 1974 U.S. patent assigned to Yoshitomi Pharmaceutical Industries, Ltd., with the synthesis reference dated November 19, 1974. It was marketed under brand names including Clozan, Distensan, Trecalmo, Rize, Rizen, and Veratran6; in France and…
Legality
By Country
United StatesIllegal
United KingdomIllegal
CanadaRestrictedReferences
Citations
Article Status
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