Loprazolam Stats & Data
CN1CCN(CC1)C=C1N=C2CN=C(c3ccccc3Cl)c3cc(N(=O)=O)ccc3N2C1=OUTEFBSAVJNEPTR-RGEXLXHISA-NPharmacology
DrugBankDescription
Loprazolam is an imidazobenzodiazepine with anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties. It is indicated for the short-term treatment of insomnia including difficulty in falling asleep and/or frequent nocturnal awakenings. Loprazolam is recommended as a short-term therapy only, due to adverse events associated with the drug including dependence and withdrawal symptoms. It is a positive modulator of GABA-A receptor that enhances the inhibitory neurotransmission. It is not an FDA-approved drug.
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).
Effect Profile
CuratedStrong euphoria and anxiolysis with mild sedation, low cognitive impairment
Tolerance & Pharmacokinetics
drugs.wikiTolerance Decay
Acute tolerance: develops within a single session — the reset numbers above apply after sustained heavy use, not after one binge. Within-session tachyphylaxis usually resets largely overnight.