Diazepam

benzodiazepine sedative From Wikipedia, the free encyclopedia

Diazepam

Diazepam (brand names: Valium, Dialar, Diazemuls, Diazepam Desitin, Diazepam RecTubes, Stesolid and Tensium) is a benzodiazepine. It acts to reduce anxiety (as an anxiolytic medication).[13]

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Diazepam
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Clinical data
Pronunciation/dˈæzɪpæm/ dy-AZ-ip-am
Trade namesValium, Vazepam, Valtoco, others[1]
AHFS/Drugs.comMonograph
MedlinePlusa682047
License data
Pregnancy
category
Dependence
liability
High[3]
Addiction
liability
Moderate[4][5]
Routes of
administration
oral, intramuscular, intravenous, rectal, nasal,[6] buccal film
Drug classBenzodiazepine
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only) [2]
  • BR: Class B1 (Psychoactive drugs)
  • CA: Schedule IV
  • DE: Prescription only (Anlage III for higher doses)
  • NZ: Class C
  • UK: POM (Prescription only) [7][8]
  • US: Schedule IV [9][10]
  • UN: Psychotropic Schedule IV
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability76% (64–97%) oral, 81% (62–98%) rectal[11]
MetabolismLiverCYP2B6 (minor route) to desmethyldiazepam, CYP2C19 (major route) to inactive metabolites, CYP3A4 (major route) to temazepam
Metabolites
  • Nordiazepam
  • Temazepam[12]
Elimination half-life(50 h); 20–100 h (32–200 h for main active metabolite desmethyldiazepam)[9][7][8]
ExcretionKidney
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
ECHA InfoCard100.006.476
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It is made mostly to treat anxiety,[14] certain forms of epilepsy,[14] muscle spasms (seizures[14]), fits,[14] and sleeping problems[verification needed]. It can also be taken to help people relax before an operation or other medical or dental treatments. This is known as a pre-med.[14] Compared to similar medications, its half-life is on the longer end.

It works by increasing the levels of a calming chemical in the brain called GABA (gamma-aminobutyric acid). Like with other benzodiazepines, there is a risk of addiction if it is used for long periods of time. For this reason the drug used for 2-4 weeks maximum to avoid dependence.[14]

Diazepam was patented in 1959 by Hoffmann-La Roche.[15][16][17] It has been one of the most prescribed medications in the world since 1963[15] many times. In 1985, the patent ended. There are now 500 or more brands available on the market.[15] It is on the World Health Organization's List of Essential Medicines.[18]

Prescribing

It has been the most prescribed medicine in the United States many times. It was the best-selling medication between 1968 and 1982 in America.[15] There, it sold more than 2 billion tablets in 1978 alone.[15] In 2022, it was the 169th most popular medication in the United States, with more than 3 million prescriptions.[19][20]

Use

It is sometimes used recreationally to cause a calming effect. Diazepam has caused huge problems in Scotland in the past.[21]

References

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