Spirapril hidrohlorid (Renormax) je ACE inhibitor antihipertenzivni lek koji se koristi u tretmanu hipertenzije. On pripada dikarboksilnoj grupi ACE inhibitora.
Spirapril
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(IUPAC) ime
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(8S)-7-[(2S)-2- {[(2S)-1-etoksi-1-okso-4-fenilbutan-2-il]amino}propanoil]-1,4-ditia-7-azaspiro[4.4]nonan-8-karboksilna kiselina
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Klinički podaci
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AHFS/Drugs.com
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Internacionalno ime leka
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Identifikatori
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CAS broj
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83647-97-6
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ATC kod
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C09AA11
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PubChem[1][2]
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5311447
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DrugBank
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DB01348
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ChemSpider[3]
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4470933
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UNII
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96U2K78I3V Y
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KEGG[4]
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D08529 Y
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ChEMBL[5]
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CHEMBL431 Y
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Hemijski podaci
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Formula
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C22H30N2O5S2
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Mol. masa
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466,616 g/mol
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SMILES
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eMolekuli & PubHem
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InChI |
InChI=1S/C22H30N2O5S2/c1-3-29-21(28)17(10-9-16-7-5-4-6-8-16)23-15(2)19(25)24-14-22(30-11-12-31-22)13-18(24)20(26)27/h4-8,15,17-18,23H,3,9-14H2,1-2H3,(H,26,27)/t15-,17-,18-/m0/s1 Y Key: HRWCVUIFMSZDJS-SZMVWBNQSA-N Y |
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Farmakokinetički podaci
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Bioraspoloživost
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50%
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Metabolizam
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konvertuje se u spiraprilat
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Poluvreme eliminacije
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30 do 35 sati
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Izlučivanje
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Hepatički i renalno
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Farmakoinformacioni podaci
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Trudnoća
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?
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Pravni status
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℞ Prescription only
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Način primene
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Oralno
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Poput mnogih ACE inhibitora, ovaj lek je prolek koji se konvertuje do aktivnog metabolita spiraprilata nakon oralne administracije. Za razliku od drugih članova grupe, on se eliminiše renalnim i hepatičkim putem, te je podesniji za primenu kod pacijenata sa renalnim oštećenjima.[6][7]
- ↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
- ↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
- ↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit
- ↑ Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H.
- ↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit
- ↑ Shohat J, Wittenberg C, Erman A, Rosenfeld J, Boner G (1999). „Acute and chronic effects of spirapril, alone or in combination with isradipine on kidney function and blood pressure in patients with reduced kidney function and hypertension.”. Scand J Urol Nephrol 33 (1): 57–62. DOI:10.1080/003655999750016294. PMID 10100366.
- ↑ Noble S, Sorkin E (1995). „Spirapril. A preliminary review of its pharmacology and therapeutic efficacy in the treatment of hypertension.”. Drugs 49 (5): 750–66. PMID 7601014.
- ↑ Ghose, A.K., Viswanadhan V.N., and 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. DOI:10.1021/ci000392t. PMID 11749573. edit
- ↑ 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. DOI:10.1021/jm000942e. PMID 11020286. edit
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