A single-dose study of mexiletine (Kö 1173).
Serum concentrations of mexiletine after a single dose were determined in 8 adult Caucasian males with complex partial seizures who were continuing to receive other antiepileptic drugs. Two patients each received a single dose of either 100, 200, 300, or 400 mg mexiletine. Serum concentrations were determined by two gas chromatographic methods. Serum concentrations ranged up to 795 ng/ml. Peak concentrations occurred 1 to 3 hr after administration of the drug and were significantly different between the 100- and 300-mg, 100- and 400-mg, 200- and 300-mg, and 200- and 400-mg doses. Differences between the other doses were not significant. Serum concentrations declined monoexponentially. Half-life ranged from 2.7 to 7.2 hr. Numerous papers have appeared in the European literature on the use of mexiletine to treat cardiac arrhythmias. Preliminary studies in the United States suggest the use of mexiletine as an adjunct for therapy of epilepsy.
D000328:Adult; D000927:Anticonvulsants / Q000008:administration & dosage*; D004305:Dose-Response Relationship, Drug; D004827:Epilepsy / Q000188:drug therapy*; D006801:Humans; D008297:Male; D008801:Mexiletine / Q000008:administration & dosage* / Q000097:blood / Q000627:therapeutic use; D008875:Middle Aged; D011437:Propylamines / Q000008:administration & dosage*
D000927:Anticonvulsants; D011437:Propylamines; D008801:Mexiletine