Duloksetin

Duloksetin
Klinički podaci
Prodajno ime	Cymbalta, Yentreve
Drugs.com	Monografija
Način primene	Oralno
Farmakokinetički podaci
Poluvreme eliminacije	12 h
Izlučivanje	Renalno
Identifikatori
CAS broj	136434-34-9
ATC kod	N06AX21 (WHO)
PubChem	CID 60835
IUPHAR/BPS	202
DrugBank	DB00476
ChemSpider	54822
ChEBI	CHEBI:36795
ChEMBL	CHEMBL1175
Hemijski podaci
Formula	C18H19NOS
Molarna masa	297,415
	SMILES CNCC[C@H](OC1=CC=CC2=CC=CC=C12)C1=CC=CS1; ;
	InChI InChI=1S/C18H19NOS/c1-19-12-11-17(18-10-5-13-21-18)20-16-9-4-7-14-6-2-3-8-15(14)16/h2-10,13,17,19H,11-12H2,1H3/t17-/m0/s1 ; Key:ZEUITGRIYCTCEM-KRWDZBQOSA-N ;

Duloksetin je organsko jedinjenje, koje sadrži 18 atoma ugljenika i ima molekulsku masu od 297,415 Da.^[1]^[2]^[3]^[4]^[5]^[6]^[7]^[8]

Osobine

Osobina	Vrednost
Broj akceptora vodonika	2
Broj donora vodonika	1
Broj rotacionih veza	6
Particioni koeficijent^[9] (ALogP)	3,8
Rastvorljivost^[10] (logS, log(mol/L))	-6,4
Polarna površina^[11] (PSA, Å²)	49,5

Reference

^ Turcotte JE, Debonnel G, de Montigny C, Hebert C, Blier P: Assessment of the serotonin and norepinephrine reuptake blocking properties of duloxetine in healthy subjects. Neuropsychopharmacology. Turcotte, J. E.; Debonnel, G.; De Montigny, C.; Hébert, C.; Blier, P. (2001 May). „Assessment of the serotonin and norepinephrine reuptake blocking properties of duloxetine in healthy subjects”. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. 24 (5): 511—21. PMID 11282251. doi:10.1016/S0893-133X(00)00220-7. Проверите вредност парамет(а)ра за датум: |date= (помоћ)
^ Anttila S, Leinonen E: Duloxetine Eli Lilly. Curr Opin Investig Drugs. Anttila, S.; Leinonen, E. (2002 Aug). „Duloxetine Eli Lilly”. Current Opinion in Investigational Drugs (London, England : 2000). 3 (8): 1217—21. PMID 12211418. Проверите вредност парамет(а)ра за датум: |date= (помоћ)
^ Karpa KD, Cavanaugh JE, Lakoski JM: Duloxetine pharmacology: profile of a dual monoamine modulator. CNS Drug Rev. Karpa, K. D.; Cavanaugh, J. E.; Lakoski, J. M. (2002 Winter). „Duloxetine pharmacology: Profile of a dual monoamine modulator”. CNS Drug Reviews. 8 (4): 361—76. PMC 6741700 . PMID 12481192. doi:10.1111/j.1527-3458.2002.tb00234.x. Проверите вредност парамет(а)ра за датум: |date= (помоћ)
^ van Groeningen CJ, Peters GJ, Pinedo HM: Lack of effectiveness of combined 5-fluorouracil and leucovorin in patients with 5-fluorouracil-resistant advanced colorectal cancer. Eur J Cancer Clin Oncol. Van Groeningen, C. J.; Peters, G. J.; Pinedo, H. M. (1989 Jan). „Lack of effectiveness of combined 5-fluorouracil and leucovorin in patients with 5-fluorouracil-resistant advanced colorectal cancer”. European Journal of Cancer & Clinical Oncology. 25 (1): 45—9. PMID 2784100. doi:10.1016/0277-5379(89)90049-7. Проверите вредност парамет(а)ра за датум: |date= (помоћ)
^ Jost W, Marsalek P: Duloxetine: mechanism of action at the lower urinary tract and Onuf's nucleus. Clin Auton Res. Jost, W.; Marsalek, P. (2004 Aug). „Duloxetine: Mechanism of action at the lower urinary tract and Onuf's nucleus”. Clinical Autonomic Research : Official Journal of the Clinical Autonomic Research Society. 14 (4): 220—7. PMID 15316838. doi:10.1007/s10286-004-0197-8. Проверите вредност парамет(а)ра за датум: |date= (помоћ)
^ Carter NJ, McCormack PL: Duloxetine: a review of its use in the treatment of generalized anxiety disorder. CNS Drugs. 2009;Carter, Natalie J.; McCormack, Paul L. (2009). „Duloxetine”. CNS Drugs. 23 (6): 523—41. PMID 19480470. doi:10.2165/00023210-200923060-00006. ..
^ 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.
^ Ghose, Arup K.; Viswanadhan, Vellarkad N.; Wendoloski, John J. (1998). „Prediction of Hydrophobic (Lipophilic) Properties of Small Organic Molecules Using Fragmental Methods: An Analysis of ALOGP and CLOGP Methods”. The Journal of Physical Chemistry A. 102 (21): 3762—3772. Bibcode:1998JPCA..102.3762G. doi:10.1021/jp980230o.
^ 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.

Spoljašnje veze

Duloxetine

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

[1] Turcotte JE, Debonnel G, de Montigny C, Hebert C, Blier P: Assessment of the serotonin and norepinephrine reuptake blocking properties of duloxetine in healthy subjects. Neuropsychopharmacology. Turcotte, J. E.; Debonnel, G.; De Montigny, C.; Hébert, C.; Blier, P. (2001 May). „Assessment of the serotonin and norepinephrine reuptake blocking properties of duloxetine in healthy subjects”. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. 24 (5): 511—21. PMID 11282251. doi:10.1016/S0893-133X(00)00220-7. Проверите вредност парамет(а)ра за датум: |date= (помоћ)

[2] Anttila S, Leinonen E: Duloxetine Eli Lilly. Curr Opin Investig Drugs. Anttila, S.; Leinonen, E. (2002 Aug). „Duloxetine Eli Lilly”. Current Opinion in Investigational Drugs (London, England : 2000). 3 (8): 1217—21. PMID 12211418. Проверите вредност парамет(а)ра за датум: |date= (помоћ)

[3] Karpa KD, Cavanaugh JE, Lakoski JM: Duloxetine pharmacology: profile of a dual monoamine modulator. CNS Drug Rev. Karpa, K. D.; Cavanaugh, J. E.; Lakoski, J. M. (2002 Winter). „Duloxetine pharmacology: Profile of a dual monoamine modulator”. CNS Drug Reviews. 8 (4): 361—76. PMC 6741700 . PMID 12481192. doi:10.1111/j.1527-3458.2002.tb00234.x. Проверите вредност парамет(а)ра за датум: |date= (помоћ)

[4] van Groeningen CJ, Peters GJ, Pinedo HM: Lack of effectiveness of combined 5-fluorouracil and leucovorin in patients with 5-fluorouracil-resistant advanced colorectal cancer. Eur J Cancer Clin Oncol. Van Groeningen, C. J.; Peters, G. J.; Pinedo, H. M. (1989 Jan). „Lack of effectiveness of combined 5-fluorouracil and leucovorin in patients with 5-fluorouracil-resistant advanced colorectal cancer”. European Journal of Cancer & Clinical Oncology. 25 (1): 45—9. PMID 2784100. doi:10.1016/0277-5379(89)90049-7. Проверите вредност парамет(а)ра за датум: |date= (помоћ)

[5] Jost W, Marsalek P: Duloxetine: mechanism of action at the lower urinary tract and Onuf's nucleus. Clin Auton Res. Jost, W.; Marsalek, P. (2004 Aug). „Duloxetine: Mechanism of action at the lower urinary tract and Onuf's nucleus”. Clinical Autonomic Research : Official Journal of the Clinical Autonomic Research Society. 14 (4): 220—7. PMID 15316838. doi:10.1007/s10286-004-0197-8. Проверите вредност парамет(а)ра за датум: |date= (помоћ)

[6] Carter NJ, McCormack PL: Duloxetine: a review of its use in the treatment of generalized anxiety disorder. CNS Drugs. 2009;Carter, Natalie J.; McCormack, Paul L. (2009). „Duloxetine”. CNS Drugs. 23 (6): 523—41. PMID 19480470. doi:10.2165/00023210-200923060-00006. ..

[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, 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.

[8] 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.

[9] Ghose, Arup K.; Viswanadhan, Vellarkad N.; Wendoloski, John J. (1998). „Prediction of Hydrophobic (Lipophilic) Properties of Small Organic Molecules Using Fragmental Methods: An Analysis of ALOGP and CLOGP Methods”. The Journal of Physical Chemistry A. 102 (21): 3762—3772. Bibcode:1998JPCA..102.3762G. doi:10.1021/jp980230o.

[10] 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.

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

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