Camazepam Explained

Watchedfields:changed
Verifiedrevid:447550704
Iupac Name:7-chloro-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl N,N-dimethylcarbamate
Width:222
Width2:180
Pregnancy Category:?
Legal Br:B1
Legal Br Comment:[1]
Legal Ca:Schedule IV
Legal De:Anlage III
Legal Uk:Class C
Legal Us:Schedule IV
Routes Of Administration:Oral
Bioavailability:90%
Metabolism:Hepatic
Elimination Half-Life:6,4-10,5 hours
Excretion:Renal
Cas Number:36104-80-0
Atc Prefix:N05
Atc Suffix:BA15
Pubchem:37367
Drugbank:DB01489
Chemspiderid:34285
Unii:HZ3XRH03C3
Kegg:D07315
Chembl:1095282
C:19
H:18
Cl:1
N:3
O:3
Smiles:ClC1=CC2=C(C=C1)N(C)C(C(N=C2C3=CC=CC=C3)OC(N(C)C)=O)=O
Stdinchi:1S/C19H18ClN3O3/c1-22(2)19(25)26-17-18(24)23(3)15-10-9-13(20)11-14(15)16(21-17)12-7-5-4-6-8-12/h4-11,17H,1-3H3
Stdinchikey:PXBVEXGRHZFEOF-UHFFFAOYSA-N

Camazepam[2] is a benzodiazepine psychoactive drug, marketed under the brand names Albego, Limpidon and Paxor. It is the dimethyl carbamate ester of temazepam, a metabolite of diazepam.[3] While it possesses anxiolytic, anticonvulsant, skeletal muscle relaxant and hypnotic properties[4] it differs from other benzodiazepines in that its anxiolytic properties are particularly prominent but has comparatively limited anticonvulsant, hypnotic and skeletal muscle relaxant properties.

Pharmacology

Camazepam, like others benzodiazepines, produce a variety of therapeutic and adverse effects by binding to the benzodiazepine receptor site on the GABAA receptor and modulating the function of the GABA receptor, the most prolific inhibitory receptor within the brain. The GABA chemical and receptor system mediates inhibitory or calming effects of camazepam on the nervous system.Compared to other benzodiazepines, it has reduced side effects such as impaired cognition, reaction times and coordination,[5] [6] [7] [8] [9] which makes it best suited as an anxiolytic because of these reduced sides effects.Animal studies have shown camazepam and its active metabolites possess anticonvulsant properties.[10] Unlike other benzodiazepines it does not disrupt normal sleep patterns.[11] Camazepam has been shown in animal experiments to have a very low affinity for benzodiazepine receptors compared to other benzodiazepines.[12] Compared to temazepam, camazepam has shown roughly equal anxiolytic properties, and less anticonvulsant, sedative, and motor-impairing properties.

Pharmacokinetics

Following oral administration, camazepam is almost completely absorbed into the bloodstream, with 90 percent bioavailability achieved in humans.[13] In the human camazepam is metabolised into the active metabolite temazepam.[14] Studies in dogs have shown that the half-life of the terminal elimination phase ranged from 6.4 to 10.5 h.[15]

Medical uses

Camazepam is indicated for the short-term treatment of insomnia and anxiety.[16] As with other benzodiazepines, its use should be reserved for patients in which the sleep disorder is severe, disabling, or causes marked distress.[17]

Adverse effects

With higher doses, such as 40 mg of camazepam, impairments similar to those caused by other benzodiazepines manifest as disrupted sleep patterns and impaired cognitive performance.[18] Skin disorders have been reported with use of camazepam however.[19] One study has shown that camazepam may increase attention.[20]

Research has demonstrated that Camazepam exhibits competitive binding to benzodiazepine receptors within the brain, albeit with a relatively modest affinity in animal models. This interaction with benzodiazepine receptors, facilitated by both Camazepam and its active metabolites, is accountable for the medication's anticonvulsant properties.https://pubchem.ncbi.nlm.nih.gov/compound/Camazepam#section=Toxicity

Contraindications

Use of camazepam is contraindicated in subjects with known hypersensitivity to drug or allergy to other drugs in the benzodiazepine class or any excipients contained in the pharmaceutical form. Use of camazepam should be avoided or carefully monitored by medical professionals in individuals with the following conditions: myasthenia gravis, severe liver deficiencies (e.g., cirrhosis), severe sleep apnea, pre-existing respiratory depression or cronic pulmonary insufficiency.[21]

See also

External links

Notes and References

  1. Web site: Anvisa . Brazilian Health Regulatory Agency . 2023-03-31 . RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial . Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control. live . https://web.archive.org/web/20230803143925/https://www.in.gov.br/en/web/dou/-/resolucao-rdc-n-784-de-31-de-marco-de-2023-474904992 . 2023-08-03 . 2023-08-16 . . pt-BR . 2023-04-04.
  2. DE . 2142181 . 1,4 Benzodiazepine derivatives and process for their production . 23 December 1976 . Siphar S A, Lugano (Schweiz) . . .
  3. Tammaro A, Picceo MT, Gemmellaro P, Bonaccorso O . Camazepam versus placebo. A double-blind clinical study on geriatric patients suffering from psychic complaints. Short Communication . Arzneimittel-Forschung . 27 . 11 . 2177–2178 . 1977 . 23793 .
  4. Lu XL, Yang SK . Enantiomer resolution of camazepam and its derivatives and enantioselective metabolism of camazepam by human liver microsomes . Journal of Chromatography A . 666 . 1–2 . 249–257 . April 1994 . 7911374 . 10.1016/0021-9673(94)80387-0 .
  5. De Sarro G, Chimirri A, Zappala M, Guisti P, Lipartiti M, De Sarro A . Azirino[1,2-d][1,4]benzodiazepine derivatives and related 1,4-benzodiazepines as anticonvulsant agents in DBA/2 mice . General Pharmacology . 27 . 7 . 1155–1162 . October 1996 . 8981061 . 10.1016/S0306-3623(96)00049-3 .
  6. De Sarro G, Gitto R, Rizzo M, Zappia M, De Sarro A . 1,4-Benzodiazepine derivatives as anticonvulsant agents in DBA/2 mice . General Pharmacology . 27 . 6 . 935–941 . September 1996 . 8909973 . 10.1016/0306-3623(95)02147-7 .
  7. De Sarro G, Chimirri A, McKernan R, Quirk K, Giusti P, De Sarro A . Anticonvulsant activity of azirino[1,2-d][1,4]benzodiazepines and related 1,4-benzodiazepines in mice . Pharmacology, Biochemistry, and Behavior . 58 . 1 . 281–289 . September 1997 . 9264104 . 10.1016/S0091-3057(96)00565-5 . 24492818 .
  8. Guthy H . [The medicinal treatment of anxiety in alcoholism in the withdrawal stage (author's transl)] . Munchener Medizinische Wochenschrift . 117 . 35 . 1387–1390 . August 1975 . 241014 .
  9. Tallone G, Ghirardi P, Bianchi MC, Ravaccia F, Bruni G, Loreti P . Reaction time to acoustic or visual stimuli after administration of camazepam and diazepam in man . Arzneimittel-Forschung . 30 . 6 . 1021–1024 . 1980 . 6106497 .
  10. Morino A, Sasaki H, Mukai H, Sugiyama M . 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 . 309–321 . June 1986 . 2878071 . 10.1007/BF01106709 . 28921744 .
  11. Ferrillo F, Balestra V, Carta F, Nuvoli G, Pintus C, Rosadini G . Comparison between the central effects of camazepam and temazepam. Computerized analysis of sleep recordings . Neuropsychobiology . 11 . 1 . 72–76 . 1984 . 6146112 . 10.1159/000118055 .
  12. Shibuya T, Field R, Watanabe Y, Sato K, Salafsky B . Structure-affinity relationships between several new benzodiazepine derivatives and 3H-diazepam receptor sites . Japanese Journal of Pharmacology . 34 . 4 . 435–440 . April 1984 . 6144807 . 10.1254/jjp.34.435 . free .
  13. Morino A, Nakamura A, Nakanishi K, Tatewaki N, Sugiyama M . Species differences in the disposition and metabolism of camazepam . Xenobiotica; the Fate of Foreign Compounds in Biological Systems . 15 . 12 . 1033–1043 . December 1985 . 2868575 . 10.3109/00498258509049098 .
  14. Riva R, Albani F, Baruzzi A . Quantitative determination of camazepam and its metabolite temazepam in man by gas-liquid chromatography with electron-capture detection . Il Farmaco; Edizione Pratica . 37 . 1 . 15–19 . January 1982 . 6120096 .
  15. Legheand J, Cuisinaud G, Bernard N, Riotte M, Sassard J . Pharmacokinetics of intravenous camazepam in dogs . Arzneimittel-Forschung . 32 . 7 . 752–756 . 1982 . 6127087 .
  16. Web site: Camazepam (PIM 678). 2021-09-09. inchem.org.
  17. Web site: PubChem . Camazepam . 2021-09-09. U.S National Library of Medicine . en.
  18. Nicholson AN, Stone BM . Hypnotic activity and effects on performance of lormetazepam and camazepam--analogues of temazepam . British Journal of Clinical Pharmacology . 13 . 3 . 433–439 . March 1982 . 6120717 . 1402107 . 10.1111/j.1365-2125.1982.tb01398.x .
  19. Stricker BH . [Skin disorders caused by the use of camazepam (Albego)] . Nederlands Tijdschrift voor Geneeskunde . 128 . 18 . 870–872 . May 1984 . 6145108 .
  20. Schmitt EJ, Rochels R, Beck D, Mauersberg L . [Visual perception under the influence of a tranquilizer (author's transl)] . Klinische Monatsblätter für Augenheilkunde . 177 . 6 . 875–877 . December 1980 . 6110803 . 10.1055/s-2008-1057748 . 260193671 .
  21. Simon ST, Higginson IJ, Booth S, Harding R, Weingärtner V, Bausewein C . Benzodiazepines for the relief of breathlessness in advanced malignant and non-malignant diseases in adults . The Cochrane Database of Systematic Reviews . 2016 . 10 . CD007354 . October 2016 . 27764523 . 6464146 . 10.1002/14651858.CD007354.pub3 .

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Camazepam".

Except where otherwise indicated, Everything.Explained.Today is © Copyright 2009-2024, A B Cryer, All Rights Reserved. Cookie policy.