Talk:Oxazepam
Oxazepam (also known as Serax, Ceresta) is a short-to-intermediate-acting benzodiazepine. Oxazepam is used for the treatment of anxiety[1] and insomnia and in the control of symptoms of alcohol withdrawal syndrome.
It is a metabolite of diazepam, prazepam, and temazepam,[2] and has moderate amnesic, anxiolytic, anticonvulsant, hypnotic, sedative, and skeletal muscle relaxant properties compared to other benzodiazepines.[3] It was patented in 1962 and approved for medical use in 1964.[4]
Medical uses It is an intermediate-acting benzodiazepine with a slow onset of action,[5] so it is usually prescribed to individuals who have trouble staying asleep, rather than falling asleep. It is commonly prescribed for anxiety disorders with associated tension, irritability, and agitation. It is also prescribed for drug and alcohol withdrawal, and for anxiety associated with depression. Physicians may use oxazepam outside its approved indications to treat social phobia, post-traumatic stress disorder, insomnia, premenstrual syndrome, and other conditions.
Side effects The side effects of oxazepam are similar to those of other benzodiazepines, and may include dizziness, drowsiness, headache, memory impairment, paradoxical excitement, and anterograde amnesia, but does not affect transient global amnesia. Side effects due to rapid decrease in dose or abrupt withdrawal from oxazepam may include abdominal and muscle cramps, convulsions, depression, inability to fall asleep or stay asleep, sweating, tremors, or vomiting.[6]
Interactions As oxazepam is an active metabolite of diazepam, an overlap in possible interactions is likely with other drugs or food, with exception of the pharmacokinetic CYP450 interactions (e.g. with cimetidine). Precautions and following the prescription are required when taking oxazepam (or other benzodiazepines) in combinations with antidepressant medication (SSRIs such as fluoxetine, sertraline, and paroxetine, or multiple reuptake inhibitors such as bupropion, duloxetine, or venlafaxine), potent painkillers (opioids, e.g. morphine, oxycodone or methadone). Concurrent use of these medicines (as well as other benzodiazepines) can interact in a way that is difficult to predict. Drinking alcohol when taking oxazepam is not recommended. Concomitant use of oxazepam and alcohol can lead to increased sedation, severe problems with coordination (ataxia), decreased muscle tone, and in severe cases or in predisposed patients, even to life-threatening intoxications with respiratory depression, coma, and collapse. There is a risk of blood circulation collapse, possibly the same condition as blood circulation syncope, when oxazepam is used in combination with quetiapine, an antipsychotic.
Pharmacology Oxazepam is an intermediate-acting benzodiazepine of the 3-hydroxy family; it acts on benzodiazepine receptors, resulting in increased effect of GABA to the GABAA receptor which results in inhibitory effects on the central nervous system.[7] The half-life of oxazepam is between 6 and 9 hours.[8] It has been shown to suppress cortisol levels. [9] Oxazepam is the most slowly absorbed and has the slowest onset of action of all the common benzodiazepines according to one British study. [10]
Oxazepam is an active metabolite formed during the breakdown of diazepam, nordazepam, and certain similar drugs. It may be safer than many other benzodiazepines in patients with impaired liver function because it does not require hepatic oxidation, but rather, it is simply metabolized by glucuronidation, so oxazepam is less likely to accumulate and cause adverse reactions in the elderly or people with liver disease. Oxazepam is similar to lorazepam in this respect. Preferential storage of oxazepam occurs in some organs, including the heart of the neonate. Absorption by any administered route and the risk of accumulation is significantly increased in the neonate, and withdrawal of oxazepam during pregnancy and breast feeding is recommended, as oxazepam is excreted in breast milk.[11]
- ↑ Janecek, James; Vestre, Norris D.; Schiele, Burtrum C.; Zimmermann, Robert (1966). "Oxazepam in the treatment of anxiety states: A controlled study". Journal of Psychiatric Research. 4 (3): 199–206. doi:10.1016/0022-3956(66)90007-0. ISSN 0022-3956. PMID 20034170.
- ↑ "Oxazepam (IARC Summary & Evaluation, Volume 66, 1996)". IARC.
- ↑ Mandrioli R, Mercolini L, Raggi MA (October 2008). "Benzodiazepine metabolism: an analytical perspective". Curr. Drug Metab. 9 (8): 827–44. doi:10.2174/138920008786049258. PMID 18855614.
- ↑ Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 536. ISBN 9783527607495.
- ↑ Galanter, Marc; Kleber, Herbert D. (1 July 2008). The American Psychiatric Publishing Textbook of Substance Abuse Treatment (4th ed.). United States of America: American Psychiatric Publishing Inc. p. 216. ISBN 978-1-58562-276-4.
- ↑ "Oxazepam Uses, Side Effects & Warnings - Drugs.com". drugs.com.
- ↑ Skerritt JH; Johnston GA. (May 6, 1983). "Enhancement of GABA binding by benzodiazepines and related anxiolytics". Eur J Pharmacol. 89 (3–4): 193–8. doi:10.1016/0014-2999(83)90494-6. PMID 6135616.
- ↑ Sonne, J; Boesgaard, S; Poulsen, H E; Loft, S; Hansen, J M; Døssing, M; Andreasen, F (November 1990). "Pharmacokinetics and pharmacodynamics of oxazepam and metabolism of paracetamol in severe hypothyroidism". British Journal of Clinical Pharmacology. 30 (5): 737–742. doi:10.1111/j.1365-2125.1990.tb03844.x. PMC 1368175. PMID 2271373.
- ↑ Christensen P; Lolk A; Gram LF; Kragh-Sørensen P. (1992). "Benzodiazepine-induced sedation and cortisol suppression. A placebo-controlled comparison of oxazepam and nitrazepam in healthy male volunteers". Psychopharmacology. 106 (4): 511–6. doi:10.1007/BF02244823. PMID 1349754. S2CID 29331503.
- ↑ Serfaty M, Masterton G (1993). "Fatal poisonings attributed to benzodiazepines in Britain during the 1980s". Br J Psychiatry. 163 (3): 386–93. doi:10.1192/bjp.163.3.386. PMID 8104653. S2CID 46001278.
- ↑ Oxazepam is an active metabolite formed during the breakdown of diazepam, nordazepam, and certain similar drugs. It may be safer than many other benzodiazepines in patients with impaired liver function because it does not require hepatic oxidation, but rather, it is simply metabolized by glucuronidation, so oxazepam is less likely to accumulate and cause adverse reactions in the elderly or people with liver disease. Oxazepam is similar to lorazepam in this respect.[30] Preferential storage of oxazepam occurs in some organs, including the heart of the neonate. Absorption by any administered route and the risk of accumulation is significantly increased in the neonate, and withdrawal of oxazepam during pregnancy and breast feeding is recommended, as oxazepam is excreted in breast milk.