Mexazolam Stats & Data
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DrugBankDescription
Mexazolam (CS-386) is a benzodiazepine indicated for the treatment of anxiety with or without psychoneurotic conditions. Mexazolam's structure is similar to that of other benzodiazepines such as oxazolam and cloxazolam. The use of benzodiazepines in the treatment of anxiety is generally a second line measure.
Mechanism of Action
Mexazolam is a benzodiazepine that binds to benzodiazepine-type receptors, inhibiting gamma-aminobutyric acid.
Metabolism
Mexazolam is rapidly metabolized to the active metabolites chloronordiazepam and chloroxazepam.
Absorption
The active metabolite chloronordiazepam has a Tmax of 1-2h.
Indication
Mexazolam is indicated for the treatment of anxiety with or without psychoneurotic conditions.
Half-life
Mexazolam follows a 2 compartment model with a first half life of 1.4h and a second half life of 76h.
Protein Binding
Mexazolam is >90% protein bound in plasma.
Elimination
Mexazolam is mainly eliminated in the bile and feces, with <10% eliminated as metabolites in the urine. >50% of a dose of mexazolam is eliminated as the metabolite chloroxazepam.
Toxicity
PubChemBenzodiazepines 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.
Carcinogenicity
No indication of carcinogenicity to humans (not listed by IARC).
Tolerance & Pharmacokinetics
drugs.wikiNo tolerance chart. Our decay curves for these drugs were estimates, and a curve can make tolerance look longer-lasting than it is, which is the dangerous direction.
How fast tolerance to these drugs fades after a break has not been measured well enough to draw, so don't count on a dose you used to take still being safe: after time off, start with a much smaller amount and don't use alone. Mixing sedatives with each other, with alcohol or with opioids sharply raises the risk of a fatal overdose. If you've been using regularly, don't stop suddenly: withdrawal from benzodiazepines, alcohol or GHB/GBL can cause seizures or delirium, so get medical help to cut down gradually.
Sources: FRANK: benzodiazepines · Alcohol and Drug Foundation: GHB · FDA 2020: benzodiazepine boxed warning · FDA 2019: gabapentinoids and breathing · NHS: alcohol use disorder