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 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.
^ 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.
^ 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.
^ 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.

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 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.

[9] 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.

[10] 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.

[11] 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.

[12] 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.

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