Drug/Small Molecule:

triazolam

Withdrawn in the United Kingdom due to risk of psychiatric adverse drug reactions. This drug continues to be available in the U.S. Internationally, triazolam is a Schedule IV drug under the Convention on Psychotropic Substances. (source: Drug Bank)

For the short-term treatment of insomnia. (source: Drug Bank)

Benzodiazepines bind nonspecifically to bezodiazepine 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 (GABA_A) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell. (source: Drug Bank)

A short-acting benzodiazepine used as a hypnotic agent in the treatment of insomnia. Some countries temporarily withdrew triazolam from the market because of concerns about adverse reactions, mostly psychological, associated with higher dose ranges. Its use at lower doses with appropriate care and labeling has been reaffirmed by the FDA and most other countries. Triazolam has a shorter half-life than chlordiazepoxide, flurazepam, and prazepam and does not generate active metabolites. (source: Drug Bank)

Hepatic. Small amounts of unmetabolized triazolam appear in the urine. (source: Drug Bank)

Bioavailability is 44% (oral) and 53% (sublingual). (source: Drug Bank)

Symptoms of overdose include drowsiness, slurred speech, motor inco-ordination, coma, and respiratory depression. (source: Drug Bank)

Cc1nnc2n1-c3ccc(cc3C(=NC2)c4ccccc4Cl)Cl (source: Drug Bank)