Comparative Pharmacology
Head-to-head clinical analysis: MEXILETINE HYDROCHLORIDE versus MEXITIL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: MEXILETINE HYDROCHLORIDE versus MEXITIL.
MEXILETINE HYDROCHLORIDE vs MEXITIL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Class Ib antiarrhythmic agent; blocks sodium channels, decreases action potential duration, and increases the ratio of refractory period to action potential duration.
Mexiletine is a class IB antiarrhythmic agent that blocks voltage-gated sodium channels, reducing the fast inward sodium current during phase 0 of the action potential. It shortens the action potential duration and decreases excitability in cardiac myocytes.
200–300 mg orally every 8 hours; maximum 1200 mg/day. Loading dose: 400 mg orally, then 200 mg after 8 hours if needed. IV use is investigational. Administer with food to reduce GI upset.
200-300 mg orally every 8 hours; maximum 1200 mg/day.
None Documented
None Documented
10-12 hours (prolonged in hepatic impairment, acute MI, and urine pH >6.5)
Terminal half-life: 10-17 hours (mean ~12 hours) in adults with normal renal function. Context: Requires dosing every 8 hours; half-life prolonged in hepatic impairment and congestive heart failure.
Renal: ~90% (10% unchanged, remainder as metabolites); Biliary/fecal: <10%
Renal: ~80-90% as unchanged drug and metabolites (primarily glucuronide conjugates); fecal: ~10-20% via biliary elimination. Impaired renal function prolongs elimination.
Category C
Category C
Antiarrhythmic (Class IB)
Antiarrhythmic (Class IB)