Land: Kanada
Tungumál: enska
Heimild: Health Canada
MEMANTINE HYDROCHLORIDE
SIVEM PHARMACEUTICALS ULC
N06DX01
MEMANTINE
10MG
TABLET
MEMANTINE HYDROCHLORIDE 10MG
ORAL
100
Prescription
MISCELLANEOUS CENTRAL NERVOUS SYSTEM AGENTS
Active ingredient group (AIG) number: 0150423001; AHFS:
APPROVED
2015-10-05
_ _ _MEMANTINE Product monograph _ _Page 1 of 35_ PRODUCT MONOGRAPH PR MEMANTINE Memantine Hydrochloride Tablets 10 mg N-methyl-D-aspartate (NMDA) receptor antagonist Sivem Pharmaceuticals ULC 4705 Dobrin Street Saint-Laurent, Quebec H4R 2P7 www.sivem.ca Date of Preparation: March 23, 2018 Submission Control No.: 213938 _ _ _MEMANTINE Product monograph _ _Page 2 of 35_ PR MEMANTINE Memantine Hydrochloride Tablets 10 mg THERAPEUTIC CLASSIFICATION N-methyl-D-aspartate (NMDA) receptor antagonist ACTION AND CLINICAL PHARMACOLOGY 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 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 Lestu allt skjalið