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Lorazepam information


Lorazepam
Clinical data
Trade namesAtivan, Tavor, Temesta, others[1]
Other nameso-Chloroxazepam
AHFS/Drugs.comMonograph
MedlinePlusa682053
License data
  • US DailyMed: Lorazepam
Pregnancy
category
  • AU: C
Dependence
liability
High[2]
Addiction
liability
Moderate[3][4]
Routes of
administration
orally, intramuscular, intravenous, transdermal
Drug classBenzodiazepine
ATC code
  • N05BA06 (WHO)
Legal status
Legal status
  • AU: S4 (Prescription only)
  • BR: Class B1 (Psychoactive drugs)[6]
  • CA: Schedule IV
  • DE: Prescription only (Anlage III for higher doses)
  • UK: Controlled Drug (Benz) POM
  • US: WARNING[5]Schedule IV
Pharmacokinetic data
Bioavailability85% when taken by mouth
MetabolismLiver glucuronidation
Onset of action1–5 min (IV), 15–30 min (IM)[7]
Elimination half-life10–20 hours[8][9][10]
Duration of action12–24 hours (IV, IM)[7]
ExcretionKidney
Identifiers
IUPAC name
  • 7-Chloro-5-(2-chlorophenyl)-3-hydroxy-1,3-dihydro-1,4-benzodiazepin-2-one
CAS Number
  • 846-49-1 checkY
PubChem CID
  • 3958
DrugBank
  • DB00186 ☒N
ChemSpider
  • 3821 checkY
UNII
  • O26FZP769L
KEGG
  • D00365 checkY
ChEBI
  • CHEBI:6539
ChEMBL
  • ChEMBL580 checkY
CompTox Dashboard (EPA)
  • DTXSID7023225 Edit this at Wikidata
ECHA InfoCard100.011.534 Edit this at Wikidata
Chemical and physical data
FormulaC15H10Cl2N2O2
Molar mass321.16 g·mol−1
3D model (JSmol)
  • Interactive image
SMILES
  • O=C1Nc2ccc(Cl)cc2C(c2ccccc2Cl)=NC1O
InChI
  • InChI=1S/C15H10Cl2N2O2/c16-8-5-6-12-10(7-8)13(19-15(21)14(20)18-12)9-3-1-2-4-11(9)17/h1-7,15,21H,(H,18,20) checkY
  • Key:DIWRORZWFLOCLC-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)
a box of Lorazepam Orion (Lorazepam) tablets

Lorazepam, sold under the brand name Ativan among others, is a benzodiazepine medication.[7] It is used to treat anxiety (including anxiety disorders), trouble sleeping, severe agitation, active seizures including status epilepticus, alcohol withdrawal, and chemotherapy-induced nausea and vomiting.[7] It is also used during surgery to interfere with memory formation and to sedate those who are being mechanically ventilated.[7][11] It is also used, along with other treatments, for acute coronary syndrome due to cocaine use.[7] It can be given orally (by mouth), transdermal (on the skin via a topical gel or patch), intravenously (IV) (injection into a vein), or intramuscularly (injection into a muscle.)[7] When given by injection, onset of effects is between one and thirty minutes and effects last for up to a day.[7]

Common side effects include weakness, sleepiness, low blood pressure, and a decreased effort to breathe.[7] When given intravenously, the person should be closely monitored.[7] Among those who are depressed, there may be an increased risk of suicide.[7][12] With long-term use, larger doses may be required for the same effect.[7] Physical dependence and psychological dependence may also occur.[7] If stopped suddenly after long-term use, benzodiazepine withdrawal syndrome may occur.[7] Older people more often develop adverse effects.[13] In this age group, lorazepam is associated with falls and hip fractures.[14] Due to these concerns, lorazepam use is generally only recommended for up to two to four weeks.[15]

Lorazepam was initially patented in 1963 and went on sale in the United States in 1977.[16][17] It is on the World Health Organization's List of Essential Medicines.[18] It is available as a generic medication.[7] In 2021, it was the 78th most commonly prescribed medication in the United States, with more than 8 million prescriptions.[19][20]

  1. ^ "Lorazepam". The Drug Gene Interaction Database. Archived from the original on 5 August 2016. Retrieved 18 May 2016.
  2. ^ Edmunds M, Mayhew M (2013). Pharmacology for the Primary Care Provider (4th ed.). Mosby. p. 545. ISBN 978-0-323-08790-2. Archived from the original on 14 January 2023. Retrieved 13 July 2020.
  3. ^ Clinical Addiction Psychiatry. Cambridge University Press. 2010. p. 156. ISBN 978-1-139-49169-3. Archived from the original on 8 September 2017.
  4. ^ Ries RK (2009). Principles of addiction medicine (4 ed.). Philadelphia: Wolters Kluwer/Lippincott Williams & Wilkins. p. 106. ISBN 978-0-7817-7477-2. Archived from the original on 8 September 2017.
  5. ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 October 2023.
  6. ^ Anvisa (31 March 2023). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 4 April 2023). Archived from the original on 3 August 2023. Retrieved 16 August 2023.
  7. ^ a b c d e f g h i j k l m n o "Lorazepam". drugs.com. American Society of Health-System Pharmacists. 29 June 2016. Archived from the original on 5 June 2016. Retrieved 15 July 2016.
  8. ^ Greenblatt DJ, Shader RI, Franke K, Maclaughlin DS, Harmatz JS, Allen MD, Werner A, Woo E (1991). "Pharmacokinetics and bioavailability of intravenous, intramuscular, and oral lorazepam in humans". Journal of Pharmaceutical Sciences. 68 (1): 57–63. doi:10.1002/jps.2600680119. PMID 31453.
  9. ^ Greenblatt DJ, von Moltke LL, Ehrenberg BL, Harmatz JS, Corbett KE, Wallace DW, Shader RI (2000). "Kinetics and dynamics of lorazepam during and after continuous intravenous infusion". Critical Care Medicine. 28 (8): 2750–2757. doi:10.1097/00003246-200008000-00011. PMID 10966246. S2CID 42138460.
  10. ^ Papini O, da Cunha SP, da Silva Mathes Ado C, Bertucci C, Moisés EC, de Barros Duarte L, de Carvalho Cavalli R, Lanchote VL (2006). "Kinetic disposition of lorazepam with a focus on the glucuronidation capacity, transplacental transfer in parturients and racemization in biological samples". Journal of Pharmaceutical and Biomedical Analysis. 40 (2): 397–403. doi:10.1016/j.jpba.2005.07.021. PMID 16143486.
  11. ^ "Lorazepam: MedlinePlus Drug Information". medlineplus.gov. 1 October 2010. Archived from the original on 19 August 2016. Retrieved 16 July 2016.
  12. ^ Dodds TJ (March 2017). "Prescribed Benzodiazepines and Suicide Risk: A Review of the Literature". The Primary Care Companion for CNS Disorders. 19 (2). doi:10.4088/PCC.16r02037. PMID 28257172.
  13. ^ Riss J, Cloyd J, Gates J, Collins S (2008). "Benzodiazepines in epilepsy: pharmacology and pharmacokinetics". Acta Neurologica Scandinavica. 118 (2): 69–86. doi:10.1111/j.1600-0404.2008.01004.x. PMID 18384456. S2CID 24453988.
  14. ^ Mets MA, Volkerts ER, Olivier B, Verster JC (2010). "Effect of hypnotic drugs on body balance and standing steadiness". Sleep Medicine Reviews. 14 (4): 259–267. doi:10.1016/j.smrv.2009.10.008. PMID 20171127.
  15. ^ "Ativan (lorazepam) Tablets Rx only" (PDF). Food and Drug Administration. March 2007. Archived (PDF) from the original on 17 September 2011. In general, benzodiazepines should be prescribed for short periods only (e.g. 2–4 weeks). Extension of the treatment period should not take place without reevaluation of the need for continued therapy. Continuous long-term use of product is not recommended.
  16. ^ Shorter E (2005). "B". A Historical Dictionary of Psychiatry. Oxford University Press. ISBN 978-0-19-029201-0. Archived from the original on 28 March 2017.
  17. ^ US patent 3296249, Stanley C. Bell, "5-monocyclic aryl-1, 3-dihydro-2h-1, 4-benzodiazepin-2-ones", published 1967-01-03, issued 1967-01-03, assigned to American Home Products 
  18. ^ World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
  19. ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
  20. ^ "Lorazepam - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.

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