Metiprajlon

Metiprilon
Klinički podaci
Prodajno ime	Dimerin, Noctan, Nodular, Noludar
Drugs.com	Monografija
Farmakokinetički podaci
Poluvreme eliminacije	6-16 h
Identifikatori
CAS broj	125-64-4
ATC kod	N05CE02 (WHO)
PubChem	CID 4162
DrugBank	DB01107
ChemSpider	4018
ChEMBL	CHEMBL1200790
Hemijski podaci
Formula	C10H17NO2
Molarna masa	183,248
	SMILES CCC1(CC)C(=O)NCC(C)C1=O; ;
	InChI InChI=1S/C10H17NO2/c1-4-10(5-2)8(12)7(3)6-11-9(10)13/h7H,4-6H2,1-3H3,(H,11,13) ; Key:SIDLZWOQUZRBRU-UHFFFAOYSA-N ;

Metiprajlon, ili Noludar, je sedativ porodice derivata piperidindiona koji je prvi razvilo preduzeće Hofman-La Roš.^[1] Ovaj lek se koristio za lečenje nesanice, ali se sada retko koristi, jer su ga zamenili noviji lekovi sa manje neželjenih efekata, kao što su benzodiazepini.^[2]

Osobine

Metiprilon je organsko jedinjenje, koje sadrži 10 atoma ugljenika i ima molekulsku masu od 183,248 Da.^[3]^[4]^[5]^[6]^[7]

Osobina	Vrednost
Broj akceptora vodonika	2
Broj donora vodonika	1
Broj rotacionih veza	2
Particioni koeficijent^[8] (ALogP)	1,5
Rastvorljivost^[9] (logS, log(mol/L))	-1,8
Polarna površina^[10] (PSA, Å²)	46,2

Reference

^ US granted 2680116, Frick H, Lutz AH, "Piperidiones and Process for the Manufacture thereof", issued 1954-06-01, assigned to Hoffmann-La Roche
^ Lomen P, Linet OI (1976). „Hypnotic efficacy of triazolam and methyprylon ininsomniac in-patients”. The Journal of International Medical Research. 4 (1): 55—8. PMID 16792. S2CID 12500779. doi:10.1177/030006057600400108.
^ Contos DA, Dixon KF, Guthrie RM, Gerber N, Mays DC: Nonlinear elimination of methyprylon (noludar) in an overdosed patient: correlation of clinical effects with plasma concentration. J Pharm Sci. 1991 Aug;Contos, D. A.; Dixon, K. F.; Guthrie, R. M.; Gerber, N.; Mays, D. C. (1991). „Nonlinear elimination of methyprylon (Noludar) in an overdosed patient: Correlation of clinical effects with plasma concentration”. Journal of Pharmaceutical Sciences. 80 (8): 768—71. Bibcode:1991JPhmS..80..768C. PMID 1686463. doi:10.1002/jps.2600800813. . .
^ Gwilt PR, Pankaskie MC, Thornburg JE, Zustiak R, Shoenthal DR: Pharmacokinetics of methyprylon following a single oral dose. J Pharm Sci. 1985 Sep;Gwilt, P. R.; Pankaskie, M. C.; Thornburg, J. E.; Zustiak, R.; Shoenthal, D. R. (1985). „Pharmacokinetics of methyprylon following a single oral dose”. Journal of Pharmaceutical Sciences. 74 (9): 1001—3. Bibcode:1985JPhmS..74.1001G. PMID 2866242. doi:10.1002/jps.2600740920. . .
^ Lomen P, Linet OI: Hypnotic efficacy of triazolam and methyprylon ininsomniac in-patients. Lomen, P.; Linet, O. I. (1976). „Hypnotic efficacy of triazolam and methyprylon ininsomniac in-patients”. Journal of International Medical Research. 4 (1): 55—8. PMID 16792. doi:10.1177/030006057600400108. ;. .
^ 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, A. C.; Wishart, D. S. (2011). „DrugBank 3.0: A comprehensive resource for 'omics' research on drugs”. Nucleic Acids Research. 39 (Database issue): D1035—41. PMC 3013709 . PMID 21059682. doi:10.1093/nar/gkq1126.
^ Wishart, D. S.; Knox, C.; Guo, A. C.; Cheng, D.; Shrivastava, S.; Tzur, D.; Gautam, B.; Hassanali, M. (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.
^ . doi:10.1021/jp980230o. Недостаје или је празан параметар |title= (помоћ)
^ Tetko, I. V.; Tanchuk, V. Y.; Kasheva, T. N.; Villa, A. E. (2001). „Estimation of aqueous solubility of chemical compounds using E-state indices”. Journal of Chemical Information and Computer Sciences. 41 (6): 1488—1493. PMID 11749573. doi:10.1021/ci000392t.
^ 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”. Journal of Medicinal Chemistry. 43 (20): 3714—3717. PMID 11020286. doi:10.1021/jm000942e.

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.
Anvisa (31. 03. 2023). „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] (на језику: португалски). Diário Oficial da União (објављено 2023-04-04). Архивирано из оригинала 03. 08. 2023. г. Приступљено 16. 08. 2023.

Spoljašnje veze

Methyprylon

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

[1] US granted 2680116, Frick H, Lutz AH, "Piperidiones and Process for the Manufacture thereof", issued 1954-06-01, assigned to Hoffmann-La Roche

[2] Lomen P, Linet OI (1976). „Hypnotic efficacy of triazolam and methyprylon ininsomniac in-patients”. The Journal of International Medical Research. 4 (1): 55—8. PMID 16792. S2CID 12500779. doi:10.1177/030006057600400108.

[3] Contos DA, Dixon KF, Guthrie RM, Gerber N, Mays DC: Nonlinear elimination of methyprylon (noludar) in an overdosed patient: correlation of clinical effects with plasma concentration. J Pharm Sci. 1991 Aug;Contos, D. A.; Dixon, K. F.; Guthrie, R. M.; Gerber, N.; Mays, D. C. (1991). „Nonlinear elimination of methyprylon (Noludar) in an overdosed patient: Correlation of clinical effects with plasma concentration”. Journal of Pharmaceutical Sciences. 80 (8): 768—71. Bibcode:1991JPhmS..80..768C. PMID 1686463. doi:10.1002/jps.2600800813. . .

[4] Gwilt PR, Pankaskie MC, Thornburg JE, Zustiak R, Shoenthal DR: Pharmacokinetics of methyprylon following a single oral dose. J Pharm Sci. 1985 Sep;Gwilt, P. R.; Pankaskie, M. C.; Thornburg, J. E.; Zustiak, R.; Shoenthal, D. R. (1985). „Pharmacokinetics of methyprylon following a single oral dose”. Journal of Pharmaceutical Sciences. 74 (9): 1001—3. Bibcode:1985JPhmS..74.1001G. PMID 2866242. doi:10.1002/jps.2600740920. . .

[5] Lomen P, Linet OI: Hypnotic efficacy of triazolam and methyprylon ininsomniac in-patients. Lomen, P.; Linet, O. I. (1976). „Hypnotic efficacy of triazolam and methyprylon ininsomniac in-patients”. Journal of International Medical Research. 4 (1): 55—8. PMID 16792. doi:10.1177/030006057600400108. ;. .

[6] 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, A. C.; Wishart, D. S. (2011). „DrugBank 3.0: A comprehensive resource for 'omics' research on drugs”. Nucleic Acids Research. 39 (Database issue): D1035—41. PMC 3013709 . PMID 21059682. doi:10.1093/nar/gkq1126.

[7] Wishart, D. S.; Knox, C.; Guo, A. C.; Cheng, D.; Shrivastava, S.; Tzur, D.; Gautam, B.; Hassanali, M. (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.

[8] . doi:10.1021/jp980230o. Недостаје или је празан параметар |title= (помоћ)

[9] Tetko, I. V.; Tanchuk, V. Y.; Kasheva, T. N.; Villa, A. E. (2001). „Estimation of aqueous solubility of chemical compounds using E-state indices”. Journal of Chemical Information and Computer Sciences. 41 (6): 1488—1493. PMID 11749573. doi:10.1021/ci000392t.

[10] 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”. Journal of Medicinal Chemistry. 43 (20): 3714—3717. PMID 11020286. doi:10.1021/jm000942e.

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