Tocainide is a lidocaine analogue, that does not have significant 1st pass metabolism. It is found in two enantiomers. The R isomer is 4x as potent as the S. orally bioavailable bioavailability is 0.9-1.0. In the blood tocainide is 10-20% protein bound. The Volume of distribution is 2.5-3.5 L/kg. 30-50% is excreted unchanged in the urine. The more active R-isomer is cleared faster in anephric patients or those with severe renal dysfunction. The main metabolite is the glucuronidated tocainide carbamic acid. The glucuronosyl transferase is apparently induced by rifampin. Weak inhibition of Cyp1A2 leads to a mild theophylline interaction. References: Feinberg L, Travis WD, Ferrans V, Sato N, Bernton HF. Pulmonary fibrosis associated with tocainide: report of a case with literature review. Am Rev Respir Dis. 1990 Feb;141(2):505-8. Review. PubMed PMID: 2137316.
纯度:≥98%
CAS:41708-72-9