Clonazepam
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| Pronunciation | kləˈnazɪpam, kloe-NAZ-e-pam | ||
| Trade names | Klonopin, Rivotril, Paxam,[1] others[2] | ||
| AHFS/Drugs.com | Monograph | ||
| MedlinePlus | a682279 | ||
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| Dependence liability | Physical: Very high Psychological: High | ||
| Addiction liability | High [4][5] | ||
| Routes of administration | By mouth, intramuscular, intravenous, sublingual | ||
| Drug class | Benzodiazepine | ||
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| Pharmacokinetic data | |||
| Bioavailability | 90% | ||
| Protein binding | ≈85% | ||
| Metabolism | Liver (CYP3A)[10] | ||
| Metabolites | 7-aminoclonazepam 7-acetaminoclonazepam 3-hydroxy clonazepam[6][7] | ||
| Onset of action | Within an hour[8] | ||
| Elimination half-life | 19–60 hours[9] | ||
| Duration of action | 8–12 hours[8][1] | ||
| Excretion | Kidney | ||
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| ECHA InfoCard | 100.015.088 | ||
| Chemical and physical data | |||
| Formula | C15H10ClN3O3 | ||
| Molar mass | 315.71 g·mol−1 | ||
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Clonazepam, sold under the brand name Klonopin among others, is a benzodiazepine medication used to prevent and treat anxiety disorders, seizures, bipolar mania, agitation associated with psychosis, obsessive–compulsive disorder (OCD), and akathisia.[10] It is a long-acting[11] tranquilizer of the benzodiazepine class.[10] It possesses anxiolytic, anticonvulsant, sedative, hypnotic, and skeletal muscle relaxant properties. It is typically taken orally (swallowed by mouth) but is also used intravenously.[10][12] Effects begin within one hour and last between eight and twelve hours in adults.[8][1]
Common side effects may include sleepiness, weakness, poor coordination, difficulty concentrating, and agitation. Clonazepam may also decrease memory formation.[10] Long-term use may result in tolerance, dependence, and life-threatening withdrawal symptoms if stopped abruptly.[10][13] Dependence occurs in one-third of people who take benzodiazepines for longer than four weeks.[9] The risk of suicide increases, particularly in people who are already depressed.[10][14] Use during pregnancy may result in harm to the fetus.[10] Clonazepam binds to GABAA receptors, thus increasing the effect of the chief inhibitory neurotransmitter γ-aminobutyric acid (GABA).[9]
Clonazepam was patented in 1960, marketed in 1964, and went on sale in 1975 in the United States from Roche.[15][16] It is available as a generic medication.[10] In 2022, it was the 57th most commonly prescribed medication in the United States, with more than 11 million prescriptions.[17][18] In many areas of the world, it is commonly used as a recreational drug.[19][20]
- ^ a b c "Paxam Data Sheet" (PDF). medsafe.govt.nz. 18 October 2023. Archived (PDF) from the original on 9 December 2023. Retrieved 14 March 2024.
- ^ "Clonazepam International". Drugs.com. Archived from the original on 25 August 2017.
- ^ "Clonazepam Use During Pregnancy". Drugs.com. 4 May 2020. Archived from the original on 28 July 2020. Retrieved 17 May 2020.
- ^ Longo LP, Johnson B (April 2000). "Addiction: Part I. Benzodiazepines--side effects, abuse risk and alternatives". American Family Physician. 61 (7): 2121–2128. PMID 10779253. Archived from the original on 12 May 2008. Retrieved 11 December 2022.
- ^ Hupp JR, Tucker MR, Ellis E (2013). Contemporary Oral and Maxillofacial Surgery - E-Book. Elsevier Health Sciences. p. 679. ISBN 9780323226875.
- ^ Ebel S, Schütz H (February 1977). "[Studies on the detection of clonazepam and its main metabolites considering in particular thin-layer chromatography discrimination of nitrazepam and its major metabolic products (author's transl)]". Arzneimittel-Forschung. 27 (2): 325–337. PMID 577149.
- ^ Steentoft A, Linnet K (January 2009). "Blood concentrations of clonazepam and 7-aminoclonazepam in forensic cases in Denmark for the period 2002-2007". Forensic Science International. 184 (1–3): 74–79. doi:10.1016/j.forsciint.2008.12.004. PMID 19150586.
- ^ a b c Cooper G, ed. (2007). Therapeutic uses of botulinum toxin. Totowa, N.J.: Humana Press. p. 214. ISBN 9781597452472. Archived from the original on 19 August 2016.
- ^ a b c Riss J, Cloyd J, Gates J, Collins S (August 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.
- ^ a b c d e f g h i "Clonazepam". The American Society of Health-System Pharmacists. Archived from the original on 5 September 2015. Retrieved 15 August 2015.
- ^ Basit H, Kahwaji CI (2024). "Clonazepam". StatPearls. Treasure Island (FL): StatPearls Publishing. PMID 32310470. Retrieved 15 March 2024.
- ^ Koubeissi M (2016). "Intravenous Clonazepam in Status Epilepticus". Epilepsy Currents. 16 (2): 89–90. doi:10.5698/1535-7511-16.2.89. PMC 4822737. PMID 27073337.
- ^ Edinoff AN, Nix CA, Hollier J, Sagrera CE, Delacroix BM, Abubakar T, et al. (November 2021). "Benzodiazepines: Uses, Dangers, and Clinical Considerations". Neurology International. 13 (4): 594–607. doi:10.3390/neurolint13040059. PMC 8629021. PMID 34842811.
- ^ Cite error: The named reference
Dodd2017was invoked but never defined (see the help page). - ^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 535. ISBN 9783527607495. Archived from the original on 14 January 2023. Retrieved 28 July 2020.
- ^ Shorter E (2005). "B". A Historical Dictionary of Psychiatry. Oxford University Press. ISBN 9780190292010. Archived from the original on 2 October 2015.
- ^ "The Top 300 of 2022". ClinCalc. Archived from the original on 30 August 2024. Retrieved 30 August 2024.
- ^ "Clonazepam Drug Usage Statistics, United States, 2013 - 2022". ClinCalc. Archived from the original on 29 April 2017. Retrieved 30 August 2024.
- ^ Martino D, Cavanna AE, eds. (2013). Advances in the neurochemistry and neuropharmacology of Tourette Syndrome. Burlington: Elsevier Science. p. 357. ISBN 9780124115613. Archived from the original on 2 October 2015.
In several countries, prescription and use is now severely limited due to abusive recreational use of clonazepam.
- ^ Fisher GL (2009). Encyclopedia of substance abuse prevention, treatment, & recovery. Los Angeles: SAGE. p. 100. ISBN 9781412950848. Archived from the original on 12 August 2016.
frequently abused