Drug intelligence / Profile preview

tetrazepam

Development stage
Discontinued
Modality
Small Molecules
Administration
Oral
01

Overview

Tetrazepam is a benzodiazepine derivative with muscle relaxant properties and relatively mild sedative effects compared to other drugs in its class. It acts as an agonist at the benzodiazepine binding site of the GABA-A receptor complex in the central nervous system. By enhancing the effect of gamma-aminobutyric acid (GABA), it increases neuronal inhibition and produces anxiolytic (anti-anxiety), anticonvulsant (anti-seizure), and muscle relaxant effects. Tetrazepam is unusual among benzodiazepines due to its cyclohexenyl group at position 5 instead of the typical phenyl ring. It has been used primarily for treating painful muscle contractures and spasticity but also for anxiety disorders such as panic attacks and rarely for depression or premenstrual syndrome. The drug is rapidly absorbed orally with an intermediate half-life (~15 hours) and is metabolized mainly into inactive metabolites; small amounts are converted into diazepam or its active metabolites[1][2][6][7]. Due to concerns about serious skin reactions and limited efficacy compared to alternatives, marketing authorization was withdrawn in Europe[7].

Brand names
ClinoxanEpsipamMyolastanMusarilRelaxamSpasmorelaxMiozepamMusapamMyopamPanosTetra-saarTetramduraTetraratio
02

Targets

TSPO (Translocator Protein (18 kDa))BZD site (GABA-A receptor benzodiazepine site)

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