Comparative Pharmacology
Head-to-head clinical analysis: EXELON versus REVERSOL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EXELON versus REVERSOL.
EXELON vs REVERSOL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Exelon (rivastigmine) is a reversible, non-competitive acetylcholinesterase and butyrylcholinesterase inhibitor, increasing acetylcholine levels in the brain.
Reversal agent for neuromuscular blockade; inhibits acetylcholinesterase, increasing acetylcholine concentration at nicotinic receptors to reverse nondepolarizing neuromuscular blocking agents.
Initial: 1.5 mg orally twice daily; after 2 weeks increase to 3 mg twice daily; then after 2 weeks increase to 4.5 mg twice daily; then after 2 weeks increase to 6 mg twice daily (maximum). For transdermal patch: initial 4.6 mg/24 hr applied once daily; after 4 weeks increase to 9.5 mg/24 hr; may increase to 13.3 mg/24 hr after additional 4 weeks.
0.25-0.5 mg/kg IV bolus over 10 seconds, repeated if necessary up to a maximum total dose of 2 mg/kg.
None Documented
None Documented
Terminal half-life: ~1.5 hours; clinical context: tid dosing recommended due to rapid elimination.
Terminal elimination half-life is 8-12 hours in healthy adults (mean 10 hours). In hepatic impairment, increases up to 18 hours; in severe renal impairment (CrCl <30 mL/min), half-life may extend to 24 hours.
Renal (97%) with unchanged drug <1%; biliary/fecal as metabolites.
Primarily renal excretion of unchanged drug (60-70%). Fecal elimination accounts for 20-25% via biliary secretion. Minor metabolism (<10%) with metabolites also renally cleared.
Category C
Category C
Cholinesterase Inhibitor
Cholinesterase Inhibitor