Kinetics of oral and intravenous mexiletine: lack of effect of cimetidine and ranitidine.
The pharmacokinetics of mexiletine, a Class I antiarrhythmic drug, was investigated in 6 healthy volunteers after single oral doses and 15 min intravenous infusions of 3 mg/kg. Cimetidine and ranitidine are commonly used H2-receptor antagonists, which interact adversely with many drugs, e.g. inhibition of the metabolism of Class I antiarrhythmics such as lidocaine and quinidine by cimetidine. To investigate the effects of the two drugs on the kinetics of mexiletine, cimetidine 800 mg.day-1 or ranitidine 600 mg.day-1 were administered orally for one week. Neither H2-receptor antagonist altered the distribution and elimination of mexiletine, nor did they affect its overall kinetics, or excretion of the metabolites para- and 4-OH-methylmexiletine after oral and intravenous administration of mexiletine.
Brockmeyer
N H
NH
Department of Medicine, Universitätsklinik Essen, Federal Republic of Germany.
Breithaupt
H
H
Ferdinand
W
W
von Hattingberg
M
M
Ohnhaus
E E
EE
D000284:Administration, Oral; D000328:Adult; D002851:Chromatography, High Pressure Liquid; D002927:Cimetidine / Q000494:pharmacology*; D004347:Drug Interactions; D005260:Female; D006801:Humans; D007275:Injections, Intravenous; D008297:Male; D008801:Mexiletine / Q000008:administration & dosage / Q000493:pharmacokinetics*; D011899:Ranitidine / Q000494:pharmacology*
D008801:Mexiletine; D002927:Cimetidine; D011899:Ranitidine