Medazepam



Medazepam
Systematic (IUPAC) name
9-chloro-2-methyl-6-phenyl-
2,5-diazabicyclo[5.4.0]undeca-
5,8,10,12-tetraene
Identifiers
CAS number 2898-12-6
ATC code N05BA03
PubChem 4041
DrugBank none
Chemical data
N2 
Mol. mass 270.8
Pharmacokinetic data
Bioavailability  ?
Metabolism Hepatic
Half life 36-150 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.

?

Legal status

Schedule IV(US)

Routes Oral

Medazepam is a drug which is a skeletal muscle relaxant properties.

It is known by the following brand names: Nobrium®, Rudotel®, Raporan®,Ansilan® .[1] Medazepam is a long acting benzodiazepine drug. The half life of medazepam is 36 - 200 hours.[2]

Pharmacology

Medazepam and other oxazolam) decrease the inhibitory potency of benzodiazepines on neurosteroids.[3] Benzodiazepine drugs including medazepam increase the inhibitory processes in the cerebral cortex.[4]

Overdose

Medazepam is a drug which is very frequently involved in drug intoxication, including overdose.[5]

The Committee on the Review of Medicines

The Committee on the Review of Medicines (UK) carried out a review into benzodiazepines due to significant concerns of tolerance, drug dependence and benzodiazepine withdrawal problems and other adverse effects. The committee found that benzodiazepines do not have any benzodiazepine withdrawal syndrome including symptoms such as anxiety, apprehension, tremor, insomnia, nausea, and vomiting upon cessation of benzodiazepine use. Withdrawal symptoms tended to develop within 24 hours on the cessation of a short acting benzodiazepine and within 3 - 10 days after the cessation of a more short acting benzodiazepine. Withdrawal effects could occur after treatment lasting only 2 weeks at therapeutic dose levels however withdrawal effects tended to occur with habitual use beyond 2 weeks and were more likely the higher the dose. The withdrawal symptoms may appear to be similar to the original condition. The committee recommended that all benzodiazepine treatment be withdrawn gradually and recommended that benzodiazepine treatment be used only in carefully selected patients and that therapy be limited to short term use only. It was noted in the review that alcohol can potentiate the central nervous system depressant effects of benzodiazepines and should be avoided. The central nervous system depressant effects of benzodiazepines may make driving or operating machinery dangerous and the elderly are more prone to these adverse effects. In the neonate high single doses or repeated low doses have been reported to produce hypotonia, poor sucking, and hypothermia in the neonate and irregularities in the fetal heart. Benzodiazepines should be avoided in lactation. Withdrawal from benzodiazepines should be gradual as abrupt withdrawal from high doses of benzodiazepines may cause confusion, toxic psychosis, convulsions, or a condition resembling delirium tremens. Abrupt withdrawal from lower doses may cause depression, nervousness, rebound insomnia, irritability, sweating, and diarrhoea.[6]

References

  1. ^ http://www.drug-encyclopedia.eu/DW_EN/benzodiazepines.shtml
  2. ^ Professor heather Ashton (April 2007). BENZODIAZEPINE EQUIVALENCY TABLE. Retrieved on Sept 23, 2007.
  3. ^ Usami N; Yamamoto T, Shintani S, Ishikura S, Higaki Y, Katagiri Y, Hara A. (Apr 2002). "Substrate specificity of human 3(20)alpha-hydroxysteroid dehydrogenase for neurosteroids and its inhibition by benzodiazepines." (pdf). Biol Pharm Bull. 25 (4): 441-5. PMID 11995921.
  4. ^ Zakusov VV; Ostrovskaya RU, Kozhechkin SN, Markovich VV, Molodavkin GM, Voronina TA. (Oct 1977). "Further evidence for GABA-ergic mechanisms in the action of benzodiazepines." 229 (2): 313-26. PMID 23084.
  5. ^ Zevzikovas A; Kiliuviene G, Ivanauskas L, Dirse V. (2002). "[Analysis of benzodiazepine derivative mixture by gas-liquid chromatography]". Medicina (Kaunas). 38 (3): 316-20. PMID 12474705.
  6. ^ Committee on the Review of Medicines (29). "Systematic review of the benzodiazepines. Guidelines for data sheets on diazepam, chlordiazepoxide, medazepam, clorazepate, lorazepam, oxazepam, temazepam, triazolam, nitrazepam, and flurazepam. Committee on the Review of Medicines." (pdf). Br Med J. 280 (6218): 910-2. PMID 7388368.
 
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