Kvazepam

Kvazepam
Klinički podaci
Prodajno ime	Cetrane, Doral, Dormalin, Oniria
Drugs.com	Monografija
Način primene	Oralno
Farmakokinetički podaci
Poluvreme eliminacije	39 h
Identifikatori
CAS broj	36735-22-5
ATC kod	N05CD10 (WHO)
PubChem	CID 4999
DrugBank	DB01589
ChemSpider	4825
KEGG	C07336
ChEMBL	CHEMBL1200472
Hemijski podaci
Formula	C17H11ClF4N2S
Molarna masa	386,794
	SMILES FC1=CC=CC=C1C1=NCC(=S)N(CC(F)(F)F)C2=C1C=C(Cl)C=C2; ;
	InChI InChI=1S/C17H11ClF4N2S/c18-10-5-6-14-12(7-10)16(11-3-1-2-4-13(11)19)23-8-15(25)24(14)9-17(20,21)22/h1-7H,8-9H2 ; Key:IKMPWMZBZSAONZ-UHFFFAOYSA-N ;
Fizički podaci
Tačka topljenja	1.375—139 °C (2.507—282 °F)

Kvazepam, koji se, između ostalog, prodaje pod brendom Doral, je lek derivata benzodiazepina sa relativno dugotrajnim dejstvom koji je razvila korporacija Šering tokom 1970-ih.^[1] Kvazepam se koristi za lečenje nesanice, uključujući indukciju spavanja i održavanje sna.^[2] Kvazepam izaziva umanjenje motoričke funkcije i ima relativno (i jedinstveno) selektivna hipnotička i antikonvulzivna svojstva sa znatno manjim potencijalom predoziranja od drugih benzodiazepina (zbog njegove nove selektivnosti za dati podtip receptora).^[3]^[4] Kvazepam je efikasan hipnotik koji indukuje i održava san bez ometanja arhitekture spavanja.^[5]

Patentiran je 1970. godine i ušao je u medicinsku upotrebu 1985. godine.^[6]

Osobine

Kvazepam je organsko jedinjenje, koje sadrži 17 atoma ugljenika i ima molekulsku masu od 386,794 Da.^[7]^[8]

Osobina	Vrednost
Broj akceptora vodonika	2
Broj donora vodonika	0
Broj rotacionih veza	3
Particioni koeficijent^[9] (ALogP)	5,9
Rastvorljivost^[10] (logS, log(mol/L))	-8,3
Polarna površina^[11] (PSA, Å²)	47,7

Vidi još

2-Oksokvazepam

Reference

^ US Patent 3845039
^ Mendels J (фебруар 1994). „Evaluation of the safety and efficacy of quazepam for the treatment of insomnia in psychiatric outpatients”. The Journal of Clinical Psychiatry. 55 (2): 60—65. PMID 7915708.
^ Yasui M, Kato A, Kanemasa T, Murata S, Nishitomi K, Koike K, et al. (јун 2005). „[Pharmacological profiles of benzodiazepinergic hypnotics and correlations with receptor subtypes]”. Nihon Shinkei Seishin Yakurigaku Zasshi = Japanese Journal of Psychopharmacology. 25 (3): 143—151. PMID 16045197.
^ Ongini E, Parravicini L, Bamonte F, Guzzon V, Iorio LC, Barnett A (1982). „Pharmacological studies with quazepam, a new benzodiazepine hypnotic”. Arzneimittel-Forschung. 32 (11): 1456—1462. PMID 6129857.
^ Roth T, Tietz EI, Kramer M, Kaffeman M (1979). „The effect of a single dose of quazepam (Sch-16134) on the sleep of chronic insomniacs”. The Journal of International Medical Research. 7 (6): 583—587. PMID 42593. S2CID 36725411. doi:10.1177/030006057900700620.
^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery (на језику: енглески). John Wiley & Sons. стр. 538. ISBN 9783527607495.
^ Knox C, Law V, Jewison T, Liu P, Ly S, Frolkis A, Pon A, Banco K, Mak C, Neveu V, Djoumbou Y, Eisner R, Guo AC, Wishart DS (2011). „DrugBank 3.0: a comprehensive resource for omics research on drugs”. Nucleic Acids Res. 39 (Database issue): D1035—41. PMC 3013709  . PMID 21059682. doi:10.1093/nar/gkq1126. уреди
^ David S. Wishart; Craig Knox; An Chi Guo; Dean Cheng; Savita Shrivastava; Dan Tzur; Bijaya Gautam; Murtaza Hassanali (2008). „DrugBank: a knowledgebase for drugs, drug actions and drug targets”. Nucleic acids research. 36 (Database issue): D901—6. PMC 2238889  . PMID 18048412. doi:10.1093/nar/gkm958. уреди
^ Ghose, A.K.; Viswanadhan V.N. & Wendoloski, J.J. (1998). „Prediction of Hydrophobic (Lipophilic) Properties of Small Organic Molecules Using Fragment Methods: An Analysis of AlogP and CLogP Methods”. J. Phys. Chem. A. 102: 3762—3772. doi:10.1021/jp980230o.
^ Tetko IV, Tanchuk VY, Kasheva TN, Villa AE (2001). „Estimation of Aqueous Solubility of Chemical Compounds Using E-State Indices”. Chem Inf. Comput. Sci. 41: 1488—1493. PMID 11749573. doi:10.1021/ci000392t. уреди
^ Ertl P.; Rohde B.; Selzer P. (2000). „Fast calculation of molecular polar surface area as a sum of fragment based contributions and its application to the prediction of drug transport properties”. J. Med. Chem. 43: 3714—3717. PMID 11020286. doi:10.1021/jm000942e. уреди

Literatura

Hardman JG, Limbird LE, Gilman AG (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10. изд.). New York: McGraw-Hill. ISBN 0071354697. doi:10.1036/0071422803.
Thomas L. Lemke; David A. Williams, ур. (2007). Foye's Principles of Medicinal Chemistry (6. изд.). Baltimore: Lippincott Willams & Wilkins. ISBN 0781768799.

Spoljašnje veze

Quazepam

Molimo Vas, obratite pažnju na važno upozorenje
u vezi sa temama iz oblasti medicine (zdravlja).

[1] US Patent 3845039

[2] Mendels J (фебруар 1994). „Evaluation of the safety and efficacy of quazepam for the treatment of insomnia in psychiatric outpatients”. The Journal of Clinical Psychiatry. 55 (2): 60—65. PMID 7915708.

[3] Yasui M, Kato A, Kanemasa T, Murata S, Nishitomi K, Koike K, et al. (јун 2005). „[Pharmacological profiles of benzodiazepinergic hypnotics and correlations with receptor subtypes]”. Nihon Shinkei Seishin Yakurigaku Zasshi = Japanese Journal of Psychopharmacology. 25 (3): 143—151. PMID 16045197.

[4] Ongini E, Parravicini L, Bamonte F, Guzzon V, Iorio LC, Barnett A (1982). „Pharmacological studies with quazepam, a new benzodiazepine hypnotic”. Arzneimittel-Forschung. 32 (11): 1456—1462. PMID 6129857.

[5] Roth T, Tietz EI, Kramer M, Kaffeman M (1979). „The effect of a single dose of quazepam (Sch-16134) on the sleep of chronic insomniacs”. The Journal of International Medical Research. 7 (6): 583—587. PMID 42593. S2CID 36725411. doi:10.1177/030006057900700620.

[Fis2006-6] Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery (на језику: енглески). John Wiley & Sons. стр. 538. ISBN 9783527607495.

[7] Knox C, Law V, Jewison T, Liu P, Ly S, Frolkis A, Pon A, Banco K, Mak C, Neveu V, Djoumbou Y, Eisner R, Guo AC, Wishart DS (2011). „DrugBank 3.0: a comprehensive resource for omics research on drugs”. Nucleic Acids Res. 39 (Database issue): D1035—41. PMC 3013709  . PMID 21059682. doi:10.1093/nar/gkq1126. уреди

[8] David S. Wishart; Craig Knox; An Chi Guo; Dean Cheng; Savita Shrivastava; Dan Tzur; Bijaya Gautam; Murtaza Hassanali (2008). „DrugBank: a knowledgebase for drugs, drug actions and drug targets”. Nucleic acids research. 36 (Database issue): D901—6. PMC 2238889  . PMID 18048412. doi:10.1093/nar/gkm958. уреди

[9] Ghose, A.K.; Viswanadhan V.N. & Wendoloski, J.J. (1998). „Prediction of Hydrophobic (Lipophilic) Properties of Small Organic Molecules Using Fragment Methods: An Analysis of AlogP and CLogP Methods”. J. Phys. Chem. A. 102: 3762—3772. doi:10.1021/jp980230o.

[10] Tetko IV, Tanchuk VY, Kasheva TN, Villa AE (2001). „Estimation of Aqueous Solubility of Chemical Compounds Using E-State Indices”. Chem Inf. Comput. Sci. 41: 1488—1493. PMID 11749573. doi:10.1021/ci000392t. уреди

[11] Ertl P.; Rohde B.; Selzer P. (2000). „Fast calculation of molecular polar surface area as a sum of fragment based contributions and its application to the prediction of drug transport properties”. J. Med. Chem. 43: 3714—3717. PMID 11020286. doi:10.1021/jm000942e. уреди

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