Dizopiramid |
|
(IUPAC) ime |
(RS)-4-(diizopropilamino)-2-fenil-2-(piridin-2-il)butanamid |
Klinički podaci |
Robne marke | Norpace |
AHFS/Drugs.com | Monografija |
MedlinePlus | a682408 |
Identifikatori |
CAS broj | 3737-09-5 |
ATC kod | C01BA03 |
PubChem[1][2] | 3114 |
DrugBank | DB00280 |
ChemSpider[3] | 3002 |
UNII | GFO928U8MQ Y |
KEGG[4] | D00303 Y |
ChEBI | CHEBI:4657 Y |
ChEMBL[5] | CHEMBL517 Y |
Hemijski podaci |
Formula | C21H29N3O |
Mol. masa | 339,475 g/mol |
SMILES | eMolekuli & PubHem |
InChI | InChI=1S/C21H29N3O/c1-16(2)24(17(3)4)15-13-21(20(22)25,18-10-6-5-7-11-18)19-12-8-9-14-23-19/h5-12,14,16-17H,13,15H2,1-4H3,(H2,22,25) Y Key: UVTNFZQICZKOEM-UHFFFAOYSA-N Y | |
Farmakokinetički podaci |
Bioraspoloživost | Visoka |
Vezivanje za proteine plazme | 50% do 65% |
Metabolizam | Hepatički (CYP3A4-posredovano) |
Poluvreme eliminacije | 6,7 sati (4 do 10 sati) |
Izlučivanje | Renalno (80%) |
Farmakoinformacioni podaci |
Trudnoća | B2(AU) C(US) |
Pravni status | POM (UK) ℞-only (SAD) |
Način primene | Oralno, intravenozno |
Dizopiramid (INN, Norpace, Rythmodan) antiaritmički je lek, koji se koristi za tretiranje ventrikularne tahikardije.[6] On je blokator natrijumovog kanala i stoga se klasifikuje u klasu 1a anti-aritmičkih agenasa.[7][8] Dizopiramid ima negativno inotropno dejstvo na ventrikularni miokard. On znatno umanjuje kontraktilnost.[9][10] Dizopiramid takođe ima antiholinergički uticaj na srce, što uzrokuje mnoštvo nuspojava. Dizopiramid je dostupan u oralnoj i intravenoznoj formi, i ima nizak stepen toksičnosti.[10]
Hemija
Dizopiramid se može sintetisati iz benzil cijanida i 2-bromopiridina:[11]
Reference
- ↑ 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
- ↑ Guyton, Arthur C., Hall, John E. (2006). Textbook of Medical Physiology (11th ed.). Philadelphia: Elsevier Saunders
- ↑ Rizos, I. I., et al. "Effects of Intravenous Disopyramide and Quinidine on Normal Myocardium and on the Characteristics of Arrhythmias: Intraindividual Comparison in Patients with Sustained Ventricular Tachycardia." European heart journal 8.2 (1987): 154-63. Biological Sciences. Web. 10 Feb. 2012
- ↑ Kim, S. Y. SY, and N. L. NL Benowitz. "Poisoning due to Class IA Antiarrhythmic Drugs. Quinidine, Procainamide and Disopyramide." Drug safety : an international journal of medical toxicology and drug experience 5.6 (1990): 393-420. Biological Sciences; Environmental Science and Pollution Management. Web. 12 Feb. 2012.
- ↑ Levites, R. R., and G. J. GJ Anderson. "Electrophysiological Effects of Disopyramide Phosphate during Experimental Myocardial Ischemia." American Heart Journal 98.3 (1979): 339-44. Biological Sciences. Web. 15 Feb. 2012.
- ↑ 10,0 10,1 Mathur, P. P. PP. "Cardiovascular Effects of a Newer Antiarrhythmic Agent, Disopyramide Phosphate." American Heart Journal 84.6 (1972): 764-70. Biological Sciences; Environmental Science and Pollution Management. Web. 15 Feb. 2012
- ↑ U.S. Patent 3.225.054
Literatura
- Guyton, Arthur C., Hall, John E. (2006). Textbook of Medical Physiology (11th ed.). Philadelphia: Elsevier Saunders.
- Rizos, I. I., et al. "Effects of Intravenous Disopyramide and Quinidine on Normal Myocardium and on the Characteristics of Arrhythmias: Intraindividual Comparison in Patients with Sustained Ventricular Tachycardia." European heart journal 8.2 (1987): 154-63. Biological Sciences. Web. 10 Feb. 2012.
- Katzung, Bertram G., Masters, Susan B., Trevor, Anthony J. (2009). Basic and Clinical Pharmacology (11th ed.). New York: McGraw Hill
- Levites, R. R., and G. J. GJ Anderson. "Electrophysiological Effects of Disopyramide Phosphate during Experimental Myocardial Ischemia." American Heart Journal 98.3 (1979): 339-44. Biological Sciences. Web. 15 Feb. 2012.
- Hulting J, Rosenhamer G: Hemodynamic and electrocardiographic effects of disopyramide in patients with ventricular arrhythmia. Acta Med Scand 199:41-51, 1976.
- Mathur, P. P. PP. "Cardiovascular Effects of a Newer Antiarrhythmic Agent, Disopyramide Phosphate." American Heart Journal 84.6 (1972): 764-70. Biological Sciences; Environmental Science and Pollution Management. Web. 15 Feb. 2012.
- Kim, S. Y. SY, and N. L. NL Benowitz. "Poisoning due to Class IA Antiarrhythmic Drugs. Quinidine, Procainamide and Disopyramide." Drug safety : an international journal of medical toxicology and drug experience 5.6 (1990): 393-420. Biological Sciences; Environmental Science and Pollution Management. Web. 12 Feb. 2012.
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