Prazepam

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Prazepam
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150px
Systematic (IUPAC) name
7-chloro- 1-(cyclopropylmethyl)- 5-phenyl- 1,3-dihydro- 2H- 1,4-benzodiazepin- 2-one
Clinical data
Pregnancy
category
  •  ?
Routes of
administration		 Oral
Legal status
Legal status
Pharmacokinetic data
Bioavailability ?
Metabolism Hepatic
Biological half-life 36-200 hours
Excretion Renal
Identifiers
CAS Number 2955-38-6
ATC code N05BA11 (WHO)
DrugBank DB01588
Synonyms 9-chloro- 2-(cyclopropylmethyl)- 6-phenyl- 2,5-diazabicyclo[5.4.0]undeca- 5,8,10,12- tetraen- 3-one
Chemical data
Formula C19H17ClN2O
Molar mass 324.8[[Script error: No such module "String".]]
  (verify)
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Prazepam is a benzodiazepine derivative drug. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties.[1] Prazepam is a prodrug for desmethyldiazepam which is an active metabolite of prazepam. Desmethyldiazepam is responsible for the therapeutic effects of prazepam.[2]

Prazepam is marketed for anxiolytic use under the trade names Centrac, Centrax, Demetrin, Lysanxia, Mono Demetrin, Pozapam, Prasepine, Prazene, Reapam and Trepidan.

Indications

Prazepam is indicated for the short term treatment of anxiety. After short term therapy the dose is usually gradually tapered off to reduce or avoid any withdrawal or rebound effects.[3][4] Desmethyldiazepam, an active metabolite, has a very long half life of 29 to 224 hours which contributes to the therapeutic effects of prazepam.[5][6]

Side effects

Side effects of prazepam are less profound than with other benzodiazepines.[7] Excessive drowsiness and with longer term use drug dependence are the most common side effects of prazepam.[8][9] Side effects such as fatigue or "feeling spacey" can also occur but less commonly than with other benzodiazepines. Other side effects include feebleness, clumsiness, lethargic, clouded thinking and mental slowness.[10][11][12]

Tolerance, dependence and withdrawal

See also: Benzodiazepine withdrawal syndrome

Tolerance and dependence can develop with long term use of prazepam and upon cessation or reduction in dosage a benzodiazepine withdrawal syndrome may occur with symptoms such as tremulousness, dysphoria, psychomotor agitation, tachycardia and sweating. In severe cases hallucinations, psychosis and seizures can occur. Withdrawal related psychosis is generally unresponsive to antipsychotic mediations. The risk and severity of the withdrawal syndrome increases the higher the dose and the longer prazepam is taken for.[13] Tolerance, dependence and withdrawal problems may be less severe than with other benzodiazepines such as diazepam.[14] It may be because tolerance is slower to develop with prazepam than with other benzodiazepines.[15] Abrupt or over-rapid discontinuation of prazepam after long term use even at low dosage may result in a protracted withdrawal syndrome.[16]

Benzodiazepines can induce serious problems of addiction which is one of the main reasons for their use being restricted to short term use. A survey in Senegal found that the majority of doctors believed that their training in this area was generally poor. Recommendations for national authorities to take urgent action regarding the rational use of benzodiazepines.[17] Another study in Dakar found that almost one fifth of doctors ignored prescribing guidelines regarding short term use of benzodiazepines and almost three quarters of doctors regarded their training and knowledge of benzodiazepines to be inadequate. More training regarding benzodiazepines has been recommended for doctors.[18]

Contraindications and special caution

Benzodiazepines require special precaution if used in the elderly, during pregnancy, in children, alcohol or drug-dependent individuals and individuals with comorbid psychiatric disorders.[19]

Mechanism of action

Prazepam exerts its therapeutic effects primarily via modulating the benzodiazepine receptor which in turn enhances GABA function in the brain.[20] Prazepam like other benzodiazepines has anticonvulsant properties but its anticonvulsant properties are not as potent as other benzodiazepines when tested in animal studies.[21][22][23][24]

Pharmacokinetics

Prazepam is metabolised into descyclopropylmethylprazepam (also known as desmethyldiazepam) and 3-hydroxyprazepam which is further metabolised into oxazepam.[25][26][27][28][29] Prazepam is a prodrug for descyclopropylmethylprazepam/desmethyldiazepam (also known as norprazepam or nordiazepam) which is responsible for most of the therapeutic activity of prazepam rather than prazepam itself.[13][20][30][31]

Interactions

Prazepam may interact with cimetidine.[32] Alcohol in combination with prazepam increases the adverse effects, particularly performance impairing side effects and drowsiness.[33]

Trade names

File:Prazepam DOJ.jpg

Prazepam is available under different trade names in the following countries; Austria: Demetrin, Belgium: Lysanxia, France: Lysanxia, Germany: Demetrin; Mono Demetrin, Greece: Centrac, Ireland: Centrax, Italy: Prazene; Trepidan, Netherlands: Reapam, Portugal: Demetrin, South Africa: Demetrin, Switzerland: Demetrin, Thailand: Pozapam; Prasepine.[34]

Overdose

See also: Benzodiazepine overdose

The symptoms of an overdose of prazepam include sleepiness, agitation and ataxia. Hypotonia may also occur in severe cases. Overdoses in children typically result in more severe symptoms of overdose.[35]

Abuse potential

See also: Benzodiazepine drug misuse

Prazepam like other benzodiazepines has abuse potential and can be habit forming. However, its abuse potential may be lower than other benzodiazepines because it has a slow onset of action.[13][36]

Toxicity

Animal studies have found prazepam taken during pregnancy results in delayed growth and reproductive abnormalities.[37][38][39]

See also

References

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External links

Benzodiazepine derivatives (N05BA, N05CD)
1,4-Benzodiazepines

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  1. ↑ Shader RI, Greenblatt DJ (1979). "Benzodiazepines: some aspects of their clinical pharmacology". Ciba Found. Symp. (74): 141–55. PMID 45081. 
  2. ↑ Jacqmin P, Ansseau M (1988). "Comparison of sublingual and oral prazepam in normal subjects. II. Pharmacokinetic and pharmacodynamic data". Neuropsychobiology. 19 (4): 186–91. doi:10.1159/000118458. PMID 2854609. 
  3. ↑ Rickels K, Sablosky L, Silverman H; et al. (1977). "Prazepam in anxiety: a controlled clinical trial". Compr Psychiatry. 18 (3): 239–49. doi:10.1016/0010-440X(77)90018-9. PMID 858240. 
  4. ↑ Ansseau M, Von Frenckell R (1991). "[Value of prazepam drops in the brief treatment of anxiety disorders]". Encephale (in French). 17 (4): 291–4. PMID 1959497. 
  5. ↑ Breimer DD, Jochemsen R, von Albert HH (1980). "Pharmacokinetics of benzodiazepines. Short-acting versus long-acting". Arzneimittelforschung. 30 (5a): 875–81. PMID 6106488. 
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  8. ↑ Danion JM, Brion S, Escande M; et al. (1984). "[Treatment of anxiety with prazepam, 40 mg. A controlled study versus lorazepam]". Encephale (in French). 10 (3): 135–8. PMID 6389091. 
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  11. ↑ Ansseau M, von Frenckell R, Jacqmin P (1987). "Comparison of sublingual and oral prazepam in normal subjects. I. Clinical data". Neuropsychobiology. 18 (2): 77–82. doi:10.1159/000118397. PMID 3330182. 
  12. ↑ Chabannes JP, Lemoine P (1990). "[Prazepam drops versus 10 mg prazepam tablets in anxious patients in ambulatory care]". Therapie (in French). 45 (6): 467–70. PMID 2080484. 
  13. ↑ 13.0 13.1 13.2 Shader RI, Greenblatt DJ (1981). "The use of benzodiazepines in clinical practice" (PDF). Br J Clin Pharmacol. 11 Suppl 1: 5S–9S. PMC 1401641 Freely accessible. PMID 6133535. 
  14. ↑ Dorman T (1983). "A multi-centre comparison of prazepam and diazepam in the treatment of anxiety". Pharmatherapeutica. 3 (6): 433–40. PMID 6353434. 
  15. ↑ Saletu M, Saletu B, Grünberger J, Mader R, Karobath M (1983). "Clinical symptomatology and computer analyzed EEG before, during and after anxiolytic therapy of alcohol withdrawal patients". Neuropsychobiology. 9 (2-3): 119–34. doi:10.1159/000117949. PMID 6353268. 
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  18. ↑ Dièye AM, Sy AN, Sy GY; et al. (2007). "[Prescription of benzodiazepines by general practitioners in the private sector of Dakar: survey on knowledge and attitudes]". Therapie (in French). 62 (2): 163–8. doi:10.2515/therapie:2007018. PMID 17582318. 
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  27. ↑ Lu XL, Guengerich FP, Yang SK (1991). "Stereoselective metabolism of prazepam and halazepam by human liver microsomes". Drug Metab. Dispos. 19 (3): 637–42. PMID 1680631. 
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  32. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  33. ↑ Girre C, Hirschhorn M, Bertaux L, Palombo S, Fournier PE (1991). "Comparison of performance of healthy volunteers given prazepam alone or combined with ethanol. Relation to drug plasma concentrations". Int Clin Psychopharmacol. 6 (4): 227–38. doi:10.1097/00004850-199100640-00004. PMID 1816280. 
  34. ↑ "Benzodiazepine Names". non-benzodiazepines.org.uk. Retrieved 2009-05-31. 
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  36. ↑ Hakuba A, Matysiakiewicz J (1986). "[The habit-forming effect of prazepam]". Psychiatr. Pol. (in Polish). 20 (3): 232–4. PMID 3797537. 
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  39. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
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