Izoniazid
Isoniazid (Laniazid, Nidrazid, izonikotinilhidrazin, INH) organsko jedinjenje je primarni lek za prevenciju i tretman tuberkuloze. Ovo jedinjenje je prvi put sintetisano početkom 20. veka,[6] ali je njegovo antituberkolozno dejstvo otkriveno 1950-tih, i tri farmaceuticska preduzeća su istovremeno neuspešno pokušala da patentiraju lek.[7] Lek je initicijalno testiran u Arizoni na Navaho zajednici, koja ima veoma veliki problem sa tuberkulozom i koja nije bila izložena streptomicinu, glavnom tuberkuloznom tretmanu tog vremena.[8]
(IUPAC) ime | |||
---|---|---|---|
izonikotinohidrazid | |||
Klinički podaci | |||
AHFS/Drugs.com | Monografija | ||
MedlinePlus | a682401 | ||
Identifikatori | |||
CAS broj | 54-85-3 | ||
ATC kod | J04AC01 | ||
PubChem[1][2] | 3767 | ||
DrugBank | DB00951 | ||
ChemSpider[3] | 3635 | ||
UNII | V83O1VOZ8L | ||
KEGG[4] | D00346 | ||
ChEBI | CHEBI:6030 | ||
ChEMBL[5] | CHEMBL64 | ||
Hemijski podaci | |||
Formula | C6H7N3O | ||
Mol. masa | 137,139 g/mol | ||
SMILES | eMolekuli & PubHem | ||
| |||
Farmakokinetički podaci | |||
Vezivanje za proteine plazme | Veoma sporo (0-10%) | ||
Metabolizam | jetra; CYP450: 2C19, 3A4 inhibitor | ||
Poluvreme eliminacije | 0,5-1,6 h (brz acetilatori), 2-5 h (spori acetilatori) | ||
Izlučivanje | urine (primarily), feces | ||
Farmakoinformacioni podaci | |||
Trudnoća | ? | ||
Pravni status | samo na recepat (US) | ||
Način primene | oralno, intramuskularno, intravenozno |
Isoniazid je dostupan u obliku tablete, sirupa, i injekcija (za intramuskularnu ili intravenoznu upotrebu). On je dostupan širom sveta. Ovaj lek ima nisku cenu i generalno je dobro tolerisan. On se proizvodi iz izonikotinske kiseline, koja se formira iz 4-metilpiridina.[9]
Povezano
urediReference
uredi- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ Meyer H, Mally J (1912). „On hydrazine derivatives of pyridine carbonic acids” (German). Monatshefte Chemie verwandte Teile anderer Wissenschaften 33: 393–414. DOI:10.1007/BF01517946.PDF fulltext
- ↑ Hans L Riede (2009). „Fourth-generation fluoroquinolones in tuberculosis”. Lancet 373 (9670): 1148–1149. DOI:10.1016/S0140-6736(09)60559-6. PMID 19345815.
- ↑ Jones, David (2002). „The Health Care Experiments at Many Farms: The Navajo, Tuberculosis, and the Limits of Modern Medicine, 1952-1962”. Bulletin of the History of Medicine 76 (4): 749–790.
- ↑ Shinkichi Shimizu, Nanao Watanabe, Toshiaki Kataoka, Takayuki Shoji, Nobuyuki Abe, Sinji Morishita, Hisao Ichimura (2007). „Pyridine and Pyridine Derivatives”. Ullmann's Encyclopedia of Industrial Chemistry. New York: John Wiley & Sons. DOI:10.1002/14356007.a22_399.
Literatura
urediSpoljašnje veze
uredi- Core Curriculum on Tuberculosis (2000) Division of Tuberculosis Elimination, Centers for Disease Control and Prevention
- Isoniazid Overdose: Recognition and Management Arhivirano 2011-11-01 na Wayback Machine-u American Family Physician 1998 Feb 15