indication

Used to treat insomnia.

pharmacology

Quazepam is a benzodiazepine derivative. The main pharmacological action of quazepam is the enhancement of the neurotransmitter, GABA at the GABA_A receptor.

mechanism of action

Benzodiazepines bind nonspecifically to benzodiazepine receptors, which affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABA_A) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of the inhibitory neurotransmitter GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.

biotransformation

Hepatic.

absorption

Bioavailability is 29-35% following oral administration.

half life

39 hours

drug interactions

Cimetidine: Cimetidine may increase the effect of the benzodiazepine, quazepam.

Clozapine: Increased risk of toxicity

Fluconazole: Fluconazole may increase the effect of the benzodiazepine, quazepam.

Indinavir: The protease inhibitor, indinavir, may increase the effect of the benzodiazepine, quazepam.

Itraconazole: Itraconazole may increase the effect of the benzodiazepine, quazepam.

Ketoconazole: Ketoconazole may increase the effect of the benzodiazepine, quazepam.

Nelfinavir: The protease inhibitor, nelfinavir, may increase the effect of the benzodiazepine, quazepam.

Omeprazole: Omeprazole may increase the effect of the benzodiazepine, quazepam.

Tipranavir: Tipranavir may decrease the metabolism and clearance of Quazepam. Consider alternate therapy or monitor for Quazepam toxic effects if Tipranavir is initiated or dose increased.

Triprolidine: The CNS depressants, Triprolidine and Quazepam, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.