Comparative Pharmacology
Head-to-head clinical analysis: ARICEPT versus RIVASTIGMINE TARTRATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ARICEPT versus RIVASTIGMINE TARTRATE.
ARICEPT vs RIVASTIGMINE TARTRATE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Reversible inhibitor of acetylcholinesterase, increasing acetylcholine levels in the synaptic cleft of the central nervous system.
Reversible, non-competitive inhibitor of acetylcholinesterase and butyrylcholinesterase, increasing acetylcholine concentration in the CNS.
Initial: 5 mg orally once daily for 4-6 weeks; may increase to 10 mg once daily. Maximum: 10 mg per day. Route: oral. Frequency: once daily.
Initial 1.5 mg orally twice daily; increase by 1.5 mg twice daily at ≥2-week intervals to maximum 6 mg twice daily if tolerated.
None Documented
None Documented
70 hours (terminal elimination half-life; steady-state reached in 15-21 days; once-daily dosing appropriate)
The terminal elimination half-life is approximately 1.5 hours after oral administration. However, due to slow dissociation from the cholinesterase enzyme, the pharmacodynamic half-life (duration of enzyme inhibition) is about 10 hours, supporting twice-daily dosing.
Renal (57% unchanged drug, 17% as metabolites), fecal (30%), biliary (minimal)
Rivastigmine is extensively metabolized by cholinesterase-mediated hydrolysis to the inactive decarbamylated metabolite, NAP226-90, which is then excreted renally. Approximately 97% of a dose is excreted in urine as metabolites (<1% as parent drug), and about 0.4% in feces. Renal elimination accounts for >90% of total clearance.
Category C
Category C
Cholinesterase Inhibitor
Cholinesterase Inhibitor