Maa: Kanada
Kieli: englanti
Lähde: Health Canada
MEMANTINE HYDROCHLORIDE
APOTEX INC
N06DX01
MEMANTINE
10MG
TABLET
MEMANTINE HYDROCHLORIDE 10MG
ORAL
30/100
Prescription
MISCELLANEOUS CENTRAL NERVOUS SYSTEM AGENTS
Active ingredient group (AIG) number: 0150423001; AHFS:
APPROVED
2011-06-02
PRODUCT MONOGRAPH PR APO-MEMANTINE Memantine Hydrochloride Tablets USP 10 mg N-METHYL-D-ASPARTATE (NMDA) RECEPTOR ANTAGONIST APOTEX INC. 150 SIGNET DRIVE TORONTO, ON M9L 1T9 DATE OF REVISION : OCTOBER 23, 2018 SUBMISSION CONTROL NUMBER: 220434 _ _ _ _ _Page 2 of 36 _ PR APO-MEMANTINE Memantine Hydrochloride Tablets USP 10 mg THERAPEUTIC CLASSIFICATION N-methyl-D-aspartate (NMDA) receptor antagonist ACTION AND CLINICAL PHARMACOLOGY 1 Persistent activation of the central nervous system N-methyl-D-aspartate (NMDA) receptors by the excitatory amino acid glutamate has been hypothesized to contribute to the symptomatology of Alzheimer’s disease. Memantine is postulated to exert its therapeutic effect through its action as a low to moderate affinity uncompetitive (open channel) NMDA receptor antagonist, which binds preferentially to the NMDA receptor-operated cation channels. It blocks the effects of pathologically elevated sustained levels of glutamate that may lead to neuronal dysfunction. There is no clinical evidence that memantine prevents or slows neurodegeneration or alters the course of the underlying dementing process in patients with Alzheimer’s disease. Memantine exhibits low to negligible affinity for other receptors (GABA, benzodiazepine, dopamine, adrenergic, noradrenergic, histamine and glycine) or voltage-dependent Ca 2+ , Na + or K + channels. In addition, it does not directly affect the acetylcholine receptor or cholinergic transmission, which have been implicated in the cholinomimetic side effects (e.g., increased gastric acid secretion, nausea and vomiting) seen with acetylcholinesterase inhibitors. Memantine showed antagonist effects at the 5HT 3 receptor with a potency similar to that for the NMDA receptor. PHARMACOKINETICS 2 ABSORPTION Orally administered memantine is completely absorbed. Oral bioavailability is almost 100%. Time to maximum plasma concentration (t max ) following single oral doses of 10 to 40 mg memantine ranged between 3 to 8 hours. It has a terminal elimination half-life of Lue koko asiakirja