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Camazepam
Systematic (IUPAC) name
(9-chloro- 2-methyl- 3-oxo- 6-phenyl- 2,5-diazabicyclo [5.4.0]undeca- 5,8,10,12-tetraen- 4-yl) N,N-dimethylcarbamate
Identifiers
CAS number 36104-80-0
ATC code N05BA15
PubChem 37367
DrugBank ?
Chemical data
Formula C 19H18ClN3O3  
Mol. mass 371.8
Pharmacokinetic data
Bioavailability  ?
Metabolism Hepatic
Half life  ?
Excretion Renal
Therapeutic considerations
Pregnancy cat.  ?
Legal status Schedule IV(US)
Routes Oral

Camazepam (marketed under the brand names Albego, Limpidon, and Paxor) is a benzodiazepine psychoactive drug which is the dimethyl carbamate ester of temazepam, a metabolite of diazepam.[1] Whilst it possesses anxiolytic, anticonvulsant, skeletal muscle relaxant and hypnotic properties[2] it differs from other benzodiazepines in that its anxiolytic properties are particularly marked but has only limited anticonvulsant, hypnotic and skeletal muscle relaxant properties. It is superior to other benzodiazepines due to its lack of typical benzodiazepine side effects such as impaired cognition, reaction times and coordination.[3][4][5][6][7] Camazepam is best suited as an anxiolytic due to its reduced hypnotic effects and reduced cognitive and motor impairing effects. However, with higher doses such as 40 mg of camazepam, impairments similar to those which occur with other benzodiazepines appear such as disrupted sleep pattern and impaired cognitive performance.[8] Animal studies have shown camazepam and its active metabolites have anticonvulsant properties.[9] Skin disorders have been reported with use of camazepam however.[10] Camazepam is believed to increase attention.[11] Camazepam unlike other benzodiazepines does not disrupt normal sleep patterns.[12] Camazepam has been shown in animal experiments to have a very low affinity for benzodiazepine receptors compared to other benzodiazepines.[13] Camazepam is almost completely absorbed into the bloodstream after oral administration with 90 percent bioavailability achieved in humans.[14] Camazepam is metabolised into an active metabolite temazepam.[15] Compared to temazepam, camazepam has shown roughly equal anxiolytic properties, and less anticonvulsant, sedative and motor-impairing properties.

See also

References

  1. ^ Tammaro, A; Picceo; Gemmellaro; Bonaccorso (1977). "Camazepam versus placebo. A double-blind clinical study on geriatric patients suffering from psychic complaints. Short Communication". Arzneimittel-Forschung 27 (11): 2177–8. PMID 23793.  
  2. ^ Lu, XL; Yang (1994). "Enantiomer resolution of camazepam and its derivatives and enantioselective metabolism of camazepam by human liver microsomes.". Journal of Chromatography A 666 (1-2): 249–57. doi:10.1016/0021-9673(94)80387-0. PMID 7911374.  
  3. ^ De Sarro, G; Chimirri; Zappala; Guisti; Lipartiti; De Sarro (1996). "Azirino1, 2-d1, 4benzodiazepine derivatives and related 1,4-benzodiazepines as anticonvulsant agents in DBA/2 mice.". General Pharmacology 27 (7): 1155–62. PMID 8981061.  
  4. ^ De Sarro, G; Gitto; Rizzo; Zappia; De Sarro (1996). "1,4-Benzodiazepine derivatives as anticonvulsant agents in DBA/2 mice.". General Pharmacology 27 (6): 935–41. PMID 8909973.  
  5. ^ De Sarro, G; Chimirri; Mckernan; Quirk; Giusti; De Sarro (1997). "Anticonvulsant activity of azirino1,2-d1,4benzodiazepines and related 1,4-benzodiazepines in mice". Pharmacology, Biochemistry, and Behavior 58 (1): 281–9. doi:10.1016/S0091-3057(96)00565-5. PMID 9264104.  
  6. ^ Guthy, H (1975). "The medicinal treatment of anxiety in alcoholism in the withdrawal stage (author's transl)". Munchener Medizinische Wochenschrift 117 (35): 1387–90. PMID 241014.  
  7. ^ Tallone, G; Ghirardi; Bianchi; Ravaccia; Bruni; Loreti (1980). "Reaction time to acoustic or visual stimuli after administration of camazepam and diazepam in man". Arzneimittel-Forschung 30 (6): 1021–4. PMID 6106497.  
  8. ^ Nicholson, AN; Stone (1982). "Hypnotic activity and effects on performance of lormetazepam and camazepam—analogues of temazepam". British Journal of Clinical Pharmacology 13 (3): 433–9. PMID 6120717. PMC 1402107. http://www.pubmedcentral.nih.gov/picrender.fcgi?artid=1402107&blobtype=pdf.  
  9. ^ Morino, A; Sasaki; Mukai; Sugiyama (1986). "Receptor-mediated model relating anticonvulsant effect to brain levels of camazepam in the presence of its active metabolites". Journal of Pharmacokinetics and Biopharmaceutics 14 (3): 309–21. doi:10.1007/BF01106709. PMID 2878071.  
  10. ^ Stricker, BH (1984). "Skin disorders caused by the use of camazepam (Albego)". Nederlands tijdschrift voor geneeskunde 128 (18): 870–2. PMID 6145108.  
  11. ^ Schmitt, EJ; Rochels; Beck; Mauersberg (1980). "Visual perception under the influence of a tranquilizer (author's transl)". Klinische Monatsblatter fur Augenheilkunde 177 (6): 875–7. doi:10.1055/s-2008-1057748. PMID 6110803.  
  12. ^ Ferrillo, F; Balestra; Carta; Nuvoli; Pintus; Rosadini (1984). "Comparison between the central effects of camazepam and temazepam. Computerized analysis of sleep recordings". Neuropsychobiology 11 (1): 72–6. doi:10.1159/000118055. PMID 6146112.  
  13. ^ Shibuya, T; Field; Watanabe; Sato; Salafsky (1984). "Structure-affinity relationships between several new benzodiazepine derivatives and 3H-diazepam receptor sites". Japanese Journal of Pharmacology 34 (4): 435–40. doi:10.1254/jjp.34.435. PMID 6144807.  
  14. ^ Morino, A; Nakamura; Nakanishi; Tatewaki; Sugiyama (1985). "Species differences in the disposition and metabolism of camazepam". Xenobiotica 15 (12): 1033–43. doi:10.3109/00498258509049098. PMID 2868575.  
  15. ^ Riva, R; Albani; Baruzzi (1982). "Quantitative determination of camazepam and its metabolite temazepam in man by gas-liquid chromatography with electron-capture detection". Il Farmaco; edizione pratica 37 (1): 15–9. PMID 6120096.  

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