Diazepam
Benzodiazepine sedative / From Wikipedia, the free encyclopedia
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Diazepam, sold under the brand name Valium among others, is a medicine of the benzodiazepine family that acts as an anxiolytic.[13] It is used to treat a range of conditions, including anxiety, seizures, alcohol withdrawal syndrome, muscle spasms, insomnia, and restless legs syndrome.[13] It may also be used to cause memory loss during certain medical procedures.[14][15] It can be taken orally (by mouth), as a suppository inserted into the rectum, intramuscularly (injected into muscle), intravenously (injection into a vein) or used as a nasal spray.[6][15] When injected intravenously, effects begin in one to five minutes and last up to an hour.[15] When taken by mouth, effects begin after 15 to 60 minutes.[16]
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Pronunciation | /daɪˈæzɪpæm/ dy-AZ-ip-am |
Trade names | Valium, Vazepam, Valtoco, others[1] |
AHFS/Drugs.com | Monograph |
MedlinePlus | a682047 |
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Dependence liability | High[3] |
Addiction liability | Moderate[4][5] |
Routes of administration | oral, intramuscular, intravenous, rectal, nasal,[6] buccal film |
Drug class | Benzodiazepine |
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Bioavailability | 76% (64–97%) oral, 81% (62–98%) rectal[11] |
Metabolism | Liver – CYP2B6 (minor route) to desmethyldiazepam, CYP2C19 (major route) to inactive metabolites, CYP3A4 (major route) to temazepam |
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Elimination half-life | (50 h); 20–100 h (32–200 h for main active metabolite desmethyldiazepam)[10][7][8] |
Excretion | Kidney |
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ECHA InfoCard | 100.006.476 |
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Formula | C16H13ClN2O |
Molar mass | 284.74 g·mol−1 |
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Common side effects include sleepiness and trouble with coordination.[10][15] Serious side effects are rare.[13] They include increased risk of suicide, decreased breathing, and an increased risk of seizures if used too frequently in those with epilepsy.[13][15][17] Occasionally, excitement or agitation may occur.[18][19] Long-term use can result in tolerance, dependence, and withdrawal symptoms on dose reduction.[13] Abrupt stopping after long-term use can be potentially dangerous.[13] After stopping, cognitive problems may persist for six months or longer.[18] It is not recommended during pregnancy or breastfeeding.[15] Its mechanism of action works by increasing the effect of the neurotransmitter gamma-aminobutyric acid (GABA).[18]
Diazepam was patented in 1959 by Hoffmann-La Roche.[13][20][21] It has been one of the most frequently prescribed medications in the world since its launch in 1963.[13] In the United States it was the best-selling medication between 1968 and 1982, selling more than 2 billion tablets in 1978 alone.[13] In 2021, it was the 149th most commonly prescribed medication in the United States, with more than 3 million prescriptions.[22][23] In 1985, the patent ended, and there are more than 500 brands available on the market.[13] It is on the World Health Organization's List of Essential Medicines.[24]