Budesonid

Budesonid
Klinički podaci
Prodajno ime	Bidien, Budeson, Budicort, Cortivent
Drugs.com	Monografija
Način primene	Respiratorno (inhalacija), oralno
Farmakokinetički podaci
Poluvreme eliminacije	2,0 - 3,6 h
Izlučivanje	Renalno
Identifikatori
CAS broj	51333-22-3
ATC kod	A07EA06 (WHO), R03BA02
PubChem	CID 40000
DrugBank	DB01222
ChemSpider	36566
ChEBI	CHEBI:3207
ChEMBL	CHEMBL1370
Hemijski podaci
Formula	C25H34O6
Molarna masa	430,54 g·mol−1
	SMILES [H][C@@]12C[C@H]3OC(CCC)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@H](O)[C@@]1([H])[C@@]2([H])CCC2=CC(=O)C=C[C@]12C; ;
	InChI InChI=1S/C25H34O6/c1-4-5-21-30-20-11-17-16-7-6-14-10-15(27)8-9-23(14,2)22(16)18(28)12-24(17,3)25(20,31-21)19(29)13-26/h8-10,16-18,20-22,26,28H,4-7,11-13H2,1-3H3/t16-,17-,18-,20+,21?,22+,23-,24-,25+/m0/s1; Key:VOVIALXJUBGFJZ-KWVAZRHASA-N ;

Budesonid (BUD), u prodaji pod imenom Pulmicort između ostalih, je lek kortikosteroidnog tipa.^[1] On je dostupan u inhalacionom obliku, kao pilula, nazalni sprej, i u rektalnoj formi.^[1]^[2] Inhalaciona forma se koristi u dugotrajnom tretmanu astme i hronične opstruktivne bolesti pluća (COPD).^[1]^[3]^[4] Nazalni sprej se koristi za alergijski rinitis i nazalne polipe.^[2]^[5] Pilule sa odloženim oslobađanjem i rektalne forme se mogu koristiti za tretman upalnih bolesti creva uključujući Kronovu bolest, ulcerozni kolitis i mikroskopski kolitis.^[6]^[7]

Osobine

Budesonid je organsko jedinjenje, koje sadrži 25 atoma ugljenika i ima molekulsku masu od 430,534 Da.^[8]^[9]

Osobina	Vrednost
Broj akceptora vodonika	6
Broj donora vodonika	2
Broj rotacionih veza	4
Particioni koeficijent^[10] (ALogP)	2,2
Rastvorljivost^[11] (logS, log(mol/L))	-4,2
Polarna površina^[12] (PSA, Å²)	93,1

Reference

^ ^а ^б ^в „Budesonide”. The American Society of Health-System Pharmacists. Приступљено 2. 12. 2015.
^ ^а ^б „Budesonide eent”. The American Society of Health-System Pharmacists. Приступљено 2. 12. 2015.
^ De Coster, DA; Jones, M (2014). . „Tailoring of corticosteroids in COPD management.”. Current respiratory care reports. 3: 121—132. PMID 25089228. doi:10.1007/s13665-014-0084-2.
^ Christophi, GP; Rengarajan, A; Ciorba, MA (2016). . „Rectal budesonide and mesalamine formulations in active ulcerative proctosigmoiditis: efficacy, tolerance, and treatment approach.”. Clinical and experimental gastroenterology. 9: 125—30. PMC 4876845 . PMID 27274301. doi:10.2147/CEG.S80237.
^ Rudmik, L; Schlosser, RJ; Smith, TL; Soler, ZM (2012). . „Impact of topical nasal steroid therapy on symptoms of nasal polyposis: a meta-analysis.”. The Laryngoscope. 122 (7): 1431—7. PMID 22410935. doi:10.1002/lary.23259.
^ Silverman J, Otley A (2011). . „Budesonide in the treatment of inflammatory bowel disease.”. Expert Rev Clin Immunol. 7 (4): 419—28. PMID 21790284. doi:10.1586/eci.11.34.
^ Pardi DS, Tremaine WJ, Carrasco-Labra A (2016). . „American Gastroenterological Association Institute Technical Review on the Medical Management of Microscopic Colitis”. Gastroenterology. 150 (1): 247—274.e11. PMID 26584602. doi:10.1053/j.gastro.2015.11.006.
^ 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—D1041. PMC 3013709 . PMID 21059682. doi:10.1093/nar/gkq1126.
^ Wishart, David S.; Knox, Craig; Guo, An Chi; Cheng, Dean; Shrivastava, Savita; Tzur, Dan; Gautam, Bijaya; Hassanali, Murtaza (2008). . „DrugBank: A knowledgebase for drugs, drug actions and drug targets”. Nucleic Acids Research. 36 (Database issue): D901—D906. 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, Igor V.; Tanchuk, Vsevolod Yu.; Kasheva, Tamara N.; Villa, Alessandro E. P. (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, Peter; Rohde, Bernhard; Selzer, Paul (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

Budesonide

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

[AHFS2015-1] а ^б ^в „Budesonide”. The American Society of Health-System Pharmacists. Приступљено 2. 12. 2015.

[AHFS2015ENT-2] а ^б „Budesonide eent”. The American Society of Health-System Pharmacists. Приступљено 2. 12. 2015.

[3] De Coster, DA; Jones, M (2014). . „Tailoring of corticosteroids in COPD management.”. Current respiratory care reports. 3: 121—132. PMID 25089228. doi:10.1007/s13665-014-0084-2.

[4] Christophi, GP; Rengarajan, A; Ciorba, MA (2016). . „Rectal budesonide and mesalamine formulations in active ulcerative proctosigmoiditis: efficacy, tolerance, and treatment approach.”. Clinical and experimental gastroenterology. 9: 125—30. PMC 4876845 . PMID 27274301. doi:10.2147/CEG.S80237.

[5] Rudmik, L; Schlosser, RJ; Smith, TL; Soler, ZM (2012). . „Impact of topical nasal steroid therapy on symptoms of nasal polyposis: a meta-analysis.”. The Laryngoscope. 122 (7): 1431—7. PMID 22410935. doi:10.1002/lary.23259.

[Sil2011-6] Silverman J, Otley A (2011). . „Budesonide in the treatment of inflammatory bowel disease.”. Expert Rev Clin Immunol. 7 (4): 419—28. PMID 21790284. doi:10.1586/eci.11.34.

[7] Pardi DS, Tremaine WJ, Carrasco-Labra A (2016). . „American Gastroenterological Association Institute Technical Review on the Medical Management of Microscopic Colitis”. Gastroenterology. 150 (1): 247—274.e11. PMID 26584602. doi:10.1053/j.gastro.2015.11.006.

[8] 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—D1041. PMC 3013709 . PMID 21059682. doi:10.1093/nar/gkq1126.

[9] Wishart, David S.; Knox, Craig; Guo, An Chi; Cheng, Dean; Shrivastava, Savita; Tzur, Dan; Gautam, Bijaya; Hassanali, Murtaza (2008). . „DrugBank: A knowledgebase for drugs, drug actions and drug targets”. Nucleic Acids Research. 36 (Database issue): D901—D906. PMC 2238889 . PMID 18048412. doi:10.1093/nar/gkm958.

[10] 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.

[11] Tetko, Igor V.; Tanchuk, Vsevolod Yu.; Kasheva, Tamara N.; Villa, Alessandro E. P. (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.

[12] Ertl, Peter; Rohde, Bernhard; Selzer, Paul (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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