Comparative Pharmacology
Head-to-head clinical analysis: EXELON versus RIVASTIGMINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EXELON versus RIVASTIGMINE.
EXELON vs RIVASTIGMINE
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.
Reversible acetylcholinesterase inhibitor that enhances cholinergic function by increasing the concentration of acetylcholine at synaptic sites. Also inhibits butyrylcholinesterase.
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.
1.5 mg orally twice daily initially, titrated by 1.5 mg/dose every 2 weeks to maintenance dose of 3-6 mg twice daily. Alternatively, transdermal patch: 4.6 mg/24h initially, titrate to 9.5 mg/24h after 4 weeks, then 13.3 mg/24h if tolerated.
None Documented
None Documented
Clinical Note
moderateRivastigmine + Dronedarone
"Rivastigmine may increase the bradycardic activities of Dronedarone."
Clinical Note
moderateRivastigmine + Nicotine
"The risk or severity of adverse effects can be increased when Rivastigmine is combined with Nicotine."
Clinical Note
moderateRivastigmine + Amiodarone
"Rivastigmine may increase the bradycardic activities of Amiodarone."
Clinical Note
moderateRivastigmine + Crizotinib
Terminal half-life: ~1.5 hours; clinical context: tid dosing recommended due to rapid elimination.
Terminal half-life ~1.5 h (oral, transdermal); clinical context: due to prolonged binding to acetylcholinesterase (AChE), effective half-life for AChE inhibition is ~10 h; steady state reached in 6-12 weeks.
Renal (97%) with unchanged drug <1%; biliary/fecal as metabolites.
Renal: ~97% total (mostly metabolites, <1% unchanged); fecal: negligible; biliary: minor.
Category C
Category C
Cholinesterase Inhibitor
Cholinesterase Inhibitor
"Rivastigmine may increase the bradycardic activities of Crizotinib."