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Oxazepam
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| Systematic (IUPAC) name | |
| 9-chloro-4-hydroxy-6-phenyl- 2,5-diazabicyclo[5.4.0]undeca- 5,8,10,12-tetraen-3-one |
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| Identifiers | |
| CAS number | |
| ATC code | N05 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C15H11ClN2O2 |
| Mol. mass | 286.71 |
| Pharmacokinetic data | |
| Bioavailability | 95.5% |
| Metabolism | Hepatic |
| Half life | 4-14 hours |
| Excretion | Renal |
| Therapeutic considerations | |
| Pregnancy cat. |
? |
| Legal status |
Schedule IV(US) |
| Routes | Oral |
Oxazepam (marketed under brand names Alepam, Murelax, Opamox, Oxascand, Serax, Serepax, Seresta, Sobril, Vaben) is a drug which is a benzodiazepine derivative. It has moderate anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties compared to other benzodiazepines.
Contents |
Pharmacology
Oxazepam is an intermediate acting benzodiazepine. Oxazepam acts on benzodiazepine receptors resulting in increased effect of GABA to the GABAA receptor which results in inhibitory effects on the central nervous system.[1][2] The half-life of oxazepam is 4-15 hours.[3] Oxazepam has been shown to suppress cortisol levels.[4]
Oxazepam is an active metabolite formed during the breakdown of diazepam, nordazepam, and certain similar drugs. Oxazepam 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 via glucuronidation. This means that 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. (1) There is preferential storage of oxazepam 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 it is recommended to withdraw oxazepam during pregnancy and breast feeding as oxazepam is excreted in breast milk.[5]
Indications
It is an intermediate acting benzodiazepine with a slow onset of action, 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.
Dependence
Oxazepam as with other benzodiazepine drugs can cause tolerance, physical dependence, addiction and what is known as the benzodiazepine withdrawal syndrome. Withdrawal from oxazepam or other benzodiazepines often leads to withdrawal symptoms which are similar to those seen during alcohol and barbiturate withdrawal. The higher the dose and the longer the drug is taken the greater the risk of experiencing unpleasant withdrawal symptoms. Withdrawal symptoms can however occur at standard dosages and also after short term use. Benzodiazepine treatment should be discontinued as soon as possible via a slow and gradual dose reduction regime.[6]
Dosage
- Mild/moderate anxiety - 10 to 15mg, 3 to 4 times daily
- Severe anxiety - 15 to 30mg, 3 to 4 times daily
- Symptoms related to alcohol withdrawal - 15 to 30mg, 3 to 4 times daily
Availability
In the United Kingdom, oxazepam is available generically in the form of 10mg, 15mg and 30mg tablets.
Side effects
The side effects of oxazepam are similar in nature to those of other benzodiazepines.
Side effects may include: Dizziness, drowsiness, headache, memory impairment, paradoxical excitement, transient 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, vomiting[7]
Interactions
As oxazepam is an active metabolite of diazepam, there is likely an overlap in possible interactions with other drugs or food, with exception of the pharmacokinetic CYP450 interactions (e.g. with cimetidine). Take precautions, and follow closely the prescription of your doctor, when taking oxazepam (or other benozodiazepines) in combinations with antidepressant medication (SSRIs such as Prozac, Zoloft, and Paxil, or multiple reuptake inhibitors such as Wellbutrin, Cymbalta, or Effexor), 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 pre-estimate. Do not drink alcohol while taking oxazepam. Concomitant use of oxazepam and alcohol can lead to increased sedation, severe problems with coordination (ataxiae), decreased muscle tone and in severe cases or in predisposed patients even to life-threatening intoxications with coma and collapse. Concomitant use of alcohol and oxazepam (as well as other benzodiazepines) also increases the risk of an addiction.citation needed
Special precautions
Benzodiazepines including oxazepam are lipophilic drugs and rapidly penetrate membranes and therefore rapidly cross over into the placenta with significant uptake of the drug. Use of benzodiazepines in late pregnancy especially high doses may result in floppy infant syndrome.[8]
Pregnancy
Oxazepam when taken during late in pregnancy, the third trimester, causes a definite risk to the neonate including a severe benzodiazepine withdrawal syndrome in the neonate with symptoms including hypotonia, and reluctance to suck, to apnoeic spells, cyanosis, and impaired metabolic responses to cold stress. Floppy infant syndrome and sedation in the new born may also occur. Symptoms of floppy infant syndrome and the neonatal benzodiazepine withdrawal syndrome have been reported to persist from hours to months after birth.[9]
Carcinogenicity
Oxazepam is listed a possible carcinogen (Group 2b) by the IARC.
Contraindications
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Please help improve this section by expanding it. Further information might be found on the talk page or at requests for expansion. (June 2008) |
Overdose
Symptoms of overdose include:
- Somnolence
- Confusion
- Impaired motor function
- Coma
- Hypoventilation (respiratory depression)
- Hypotensioncitation needed
Abuse
Benzodiazepines, including diazepam, oxazepam, nitrazepam, and flunitrazepam accounted for the largest volume of forged drug prescriptions in Sweden 1982-1986, a total of 52% of drug forgeries were for benzodiazepines, suggesting benzodiazepines were a major prescription drug class of abuse.[10]
Legal Status
Oxazepam is a Schedule IV drug under the Convention on Psychotropic Substances [1].
Usage
Oxazepam along with diazepam, nitrazepam and temazepam, were the four benzodiazepines listed on the pharmaceutical benefits scheme and represented 82% of the benzodiazepine prescriptions in Australia in 1990-1991.[11]
References
- ^ Skerritt JH; Johnston GA. (6). "Enhancement of GABA binding by benzodiazepines and related anxiolytics". Eur J Pharmacol. 89 (3-4): 193–8. doi:. PMID 6135616.
- ^ Oelschläger H. (4). "[Chemical and pharmacologic aspects of benzodiazepines]". Schweiz Rundsch Med Prax. 78 (27-28): 766–72. PMID 2570451.
- ^ Professor heather Ashton (April 2007). "BENZODIAZEPINE EQUIVALENCY TABLE". Retrieved on Sept 23, 2007.
- ^ 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:. PMID 1349754.
- ^ Olive G; Dreux C. (Jan 1977). "Pharmacologic bases of use of benzodiazepines in peréinatal medicine". Arch Fr Pediatr. 34(1): 74–89. PMID 851373.
- ^ MacKinnon GL; Parker WA. (1982). "Benzodiazepine withdrawal syndrome: a literature review and evaluation". The American journal of drug and alcohol abuse. 9 (1): 19–33. doi:. PMID 6133446.
- ^ Oxazepam patient advice including side effects
- ^ Kanto JH. (May 1982). "Use of benzodiazepines during pregnancy, labour and lactation, with particular reference to pharmacokinetic considerations". Drugs. 23 (5): 354–80. doi:. PMID 6124415.
- ^ McElhatton PR. (Nov-Dec 1994). "The effects of benzodiazepine use during pregnancy and lactation". Reprod Toxicol. 8 (6): 461–75. doi:. PMID 7881198.
- ^ Bergman U; Dahl-Puustinen ML. (1989). "Use of prescription forgeries in a drug abuse surveillance network". Eur J Clin Pharmacol. 36 (6): 621–3. doi:. PMID 2776820.
- ^ Mant A; Whicker SD, McManus P, Birkett DJ, Edmonds D, Dumbrell D. (Dec 1993). "Benzodiazepine utilisation in Australia: report from a new pharmacoepidemiological database". Aust J Public Health. 17 (4): 345–9. PMID 7911332.
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Wikipedia content modification information:
- This page was last modified on 7 September 2008, at 14:15.
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