Metaclazepam
- none
- 7-bromo-5-(2-chlorophenyl)-2-(methoxymethyl)-1-methyl-2,3-dihydro-1,4-benzodiazepine
- 84031-17-4 Y
- 71272
- 64398 Y
- C2N2B1303L
- ChEMBL1290783
- DTXSID40905121
- Interactive image
- ClC1=CC=CC=C1C2=NCC(COC)N(C)C3=C2C=C(Br)C=C3
- InChI=1S/C18H18BrClN2O/c1-22-13(11-23-2)10-21-18(14-5-3-4-6-16(14)20)15-9-12(19)7-8-17(15)22/h3-9,13H,10-11H2,1-2H3 Y
- Key:WABYCCJHARSRBH-UHFFFAOYSA-N Y
Metaclazepam[1] (marketed under the brand name Talis) is a drug which is a benzodiazepine derivative.[2][3] It is a relatively selective anxiolytic with less sedative or muscle relaxant properties than other benzodiazepines such as diazepam or bromazepam.[4] It has an active metabolite N-desmethylmetaclazepam, which is the main metabolite of metaclazepam.[5] There is no significant difference in metabolism between younger and older individuals.[6]
Metaclazepam is slightly more effective as an anxiolytic than bromazepam,[7] or diazepam,[8] with a 15 mg dose of metaclazepam equivalent to 4 mg of bromazepam.[9] Metaclazepam can interact with alcohol producing additive sedative-hypnotic effects.[6][10] Fatigue is a common side effect from metaclazepam at high doses.[11] Small amounts of metaclazepam as well as its metabolites enter into human breast milk.[12]
See also
References
- ^ US 4098786
- ^ Borchers F, Achtert G, Hausleiter HJ, Zeugner H (1984). "Metabolism and pharmacokinetics of metaclazepam (Talis), Part III: Determination of the chemical structure of metabolites in dogs, rabbits and men". European Journal of Drug Metabolism and Pharmacokinetics. 9 (4): 325–46. doi:10.1007/bf03189684. PMID 6532806. S2CID 12290664.
- ^ Althaus W, Block J, Förster A, Kühnhold M, Meister D, Wischniewski M (September 1986). "Analytical profile of metaclazepam". Arzneimittel-Forschung. 36 (9): 1302–6. PMID 3790179.
- ^ Buschmann G, Kühl UG, Rohte O (1985). "General pharmacology of the anxiolytic compound metaclazepam in comparison to other benzodiazepines". Arzneimittel-Forschung. 35 (11): 1643–55. PMID 2868732.
- ^ Gielsdorf W, Molz KH, Hausleiter HJ, Achtert G, Philipp P (1986). "Pharmacokinetic profile of metaclazepam (Talis), a new 1.4-benzodiazepine. Influence of different dosage regimens on the pharmacokinetic profile of metaclazepam and its main metabolite under steady-state conditions". European Journal of Drug Metabolism and Pharmacokinetics. 11 (3): 205–10. doi:10.1007/bf03189848. PMID 3816876. S2CID 8493668.
- ^ a b Molz KH, Gielsdorf W, Rasper J, Jaeger H, Hausleiter HJ, Achtert G, Philipp P (1985). "Comparison of the pharmacokinetic profile of metaclazepam in old and young volunteers". European Journal of Clinical Pharmacology. 29 (2): 247–9. doi:10.1007/bf00547431. PMID 4076323. S2CID 8017809.
- ^ Bilone F, Roncari R (1988). "A double-blind comparison of the anxiolytic activity of two benzodiazepines, metaclazepam and bromazepam, in anxiety neurosis". Current Medical Research and Opinion. 11 (1): 45–7. doi:10.1185/03007998809111130. PMID 2898321.
- ^ Laakmann G, Blaschke D, Hippius H, Schewe S (May 1989). "Double-blind study of metaclazepam versus diazepam treatment of outpatients with anxiety syndrome". Pharmacopsychiatry. 22 (3): 120–5. doi:10.1055/s-2007-1014593. PMID 2568645.
- ^ Marano P, Patti F, Nicoletti F (1988). "Controlled study on the anxiolytic activity of a newly-developed benzodiazepine, metaclazepam". Current Medical Research and Opinion. 11 (1): 41–4. doi:10.1185/03007998809111129. PMID 2898320.
- ^ Schmidt V (1983). "[Experimental studies on the interaction of alcohol and metaclazepam]". Beiträge zur Gerichtlichen Medizin. 41: 413–7. PMID 6639614.
- ^ Laakmann G, Blaschke D, Hippius H, Schewe S (May 1988). "Double-blind randomized trial of the benzodiazepine derivative metaclazepam as compared with placebo treatment of outpatients with anxiety syndromes". Pharmacopsychiatry. 21 (3): 136–43. doi:10.1055/s-2007-1014665. PMID 2900514.
- ^ Schotter A, Müller R, Günther C, Hausleiter HJ, Achtert G (November 1989). "Transfer of metaclazepam and its metabolites into breast milk". Arzneimittel-Forschung. 39 (11): 1468–70. PMID 2575907.
- v
- t
- e
- 2-Oxoquazepam
- 3-Hydroxyphenazepam
- Bromazepam
- BMS-906024*
- Camazepam
- Carburazepam
- Chlordiazepoxide
- Cinazepam
- Cinolazepam
- Clonazepam
- Cloniprazepam
- Clorazepate
- Cyprazepam
- Delorazepam
- Demoxepam
- Desmethylflunitrazepam
- Devazepide*
- Diazepam
- Diclazepam
- Difludiazepam
- Doxefazepam
- Elfazepam
- Ethyl carfluzepate
- Ethyl dirazepate
- Ethyl loflazepate
- Flubromazepam
- Fletazepam
- Fludiazepam
- Flunitrazepam
- Flurazepam
- Flutemazepam
- Flutoprazepam
- Fosazepam
- Gidazepam
- Halazepam
- Iclazepam
- Irazepine*
- Kenazepine
- Ketazolam
- Lorazepam
- Lormetazepam
- Lufuradom*
- Meclonazepam
- Medazepam
- Menitrazepam
- Metaclazepam
- Motrazepam
- N-Desalkylflurazepam
- Nifoxipam
- Nimetazepam
- Nitemazepam
- Nitrazepam
- Nitrazepate
- Nordazepam
- Nortetrazepam
- Oxazepam
- Phenazepam
- Pinazepam
- Pivoxazepam
- Prazepam
- Proflazepam
- Quazepam
- QH-II-66
- Reclazepam
- RO4491533*
- Ro05-4082
- Ro5-4864*
- Ro07-5220
- Ro07-9749
- Ro20-8065
- Ro20-8552
- SH-I-048A
- Sulazepam
- Temazepam
- Tetrazepam
- Tifluadom*
- Timelotem*
- Tolufazepam
- Triflunordazepam
- Tuclazepam
- Uldazepam