Drug intelligence / Profile preview

bentazepam

Development stage
Unknown
Modality
Small Molecules
Administration
Oral
01

Overview

Bentazepam is a thienodiazepine and benzodiazepine analog used primarily as a short-acting anxiolytic. It possesses anxiolytic, anticonvulsant, sedative, and skeletal muscle relaxant properties. Its mechanism of action involves acting as a positive allosteric modulator at the GABA-A receptor by binding at the interface between alpha (α) and gamma (γ) subunits—specifically α1, α2, α3, and α5—thereby enhancing the inhibitory effects of gamma-aminobutyric acid (GABA) in the central nervous system. This results in increased neuronal inhibition leading to its clinical effects. Bentazepam has an oral route of administration with peak plasma concentrations reached approximately 2.5 hours after dosing and an elimination half-life of 2–4 hours. Adverse effects can include dry mouth, somnolence, asthenia, dyspepsia, constipation, nausea; rare but serious risks include drug-induced lymphocytic colitis and severe liver damage[1][4][6].

Brand names
Tiadipona
Other names
bentazepamthiadiponetiadipona
02

Targets

Gamma-aminobutyric acid type A receptor alpha-3 subunit-containing complexα5-GABAAR (Gamma-aminobutyric acid type A receptor alpha5beta2gamma2 subtype (GABAA receptor alpha5beta2gamma2 subtype))Gamma-aminobutyric acid type A receptor alpha-2 subunit-containing complexGABRA1 (Gamma-aminobutyric acid type A receptor alpha 1 subunit)

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