Galantamine extended release.
Galantamine inhibits acetylcholinesterase (AChE) to slow acetylcholine hydrolysis, and may also modulate presynaptic nicotinic receptor activation, thereby increasing neurotransmitter concentrations in the synaptic cleft.black triangle Once-daily galantamine extended release (ER) 24 mg and twice-daily galantamine immediate release (IR) 12 mg are bioequivalent in terms of the area under the plasma concentration-time curve from time 0 to 24 hours and steady-state minimum plasma concentration.black triangle Primary endpoints indicated a significantly greater effect of galantamine ER on cognitive performance than placebo, with efficacy similar to galantamine IR, in a randomised, double-blind trial. While galantamine ER did not show a significant effect on the coprimary endpoint of global change, neither did galantamine IR in this study. Exploratory post hoc analyses of global change correcting for study centre and prognostic factors associated with response (baseline Mini-Mental State Examination, Alzheimer's Disease Assessment Scale cognitive score, prior cholinomimetic use) indicated nominal significance in the galantamine ER treatment arm. Secondary endpoints indicated an improvement in activities of daily living and memory- and nonmemory-dependent measures of cognitive performance, but not in measures of behaviour or dichotomised rating of global change. Adverse events occurred in similar proportions of galantamine ER, galantamine IR and placebo recipients.
Robinson
Dean M
DM
Adis International Limited, Auckland, New Zealand. demail@adis.co.nz
Plosker
Greg L
GL
D000544:Alzheimer Disease / Q000188:drug therapy*; D002800:Cholinesterase Inhibitors / Q000008:administration & dosage* / Q000494:pharmacology; D002986:Clinical Trials as Topic; D004333:Drug Administration Routes; D004334:Drug Administration Schedule; D005702:Galantamine / Q000008:administration & dosage* / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50
D002800:Cholinesterase Inhibitors; D005702:Galantamine