Namzaric is a fixed-dose combination of memantine hydrochloride extended-release, a NMDA receptor antagonist, and donepezil hydrochloride, an acetylcholinesterase inhibitor. Memantine hydrochloride 5 mg tablet: Orange, capsule-shaped, film-coated tablets debossed with ‘C’ on one side and ‘331’ on other side. "Memantine agonist action at dopamine D2High receptors". [30], Memantine acts as an agonist at the dopamine D2 receptor with equal or slightly higher affinity than to the NMDA receptors. [4][5], Memantine is used to treat moderate-to-severe Alzheimer's disease, especially for people who are intolerant of or have a contraindication to AChE (acetylcholinesterase) inhibitors. Mechanism of Action. [13] The UK National Institute of Clinical Excellence (NICE) issued guidance in 2018 recommending consideration of the combination of memantine with donepezil in those with moderate-to-severe dementia. Memantine is a clinically useful drug in many neurological disorders, including Alzheimer's disease. In September 2014 the attorney general of New York, Eric Schneiderman, filed a lawsuit to compel Actavis to keep selling the IR version on the basis of antitrust law. As a result, even normal levels of glutamate can overactivate the glutamate receptors on the nerve cells. [3] Treatment should only be continued if beneficial effects are seen. FIGURE 1 Schematic presentation of the glutamatergic synapse and major ionotropic glutamate receptors - AMPA and NMDA. Comparing Effectiveness, Safety, and Price", "Forest Laboratories' Namenda Is Focus of Lawsuit", "Actavis Confirms Appeals Court Ruling Requiring Continued Distribution of Namenda IR", "Actavis, Others Plotted To Delay Generic Namenda, Suit Says - Law360", "Second Circuit Denies Petition for Actavis Rehearing | David Kleban", "Evaluation of the reinforcing and discriminative stimulus properties of the low-affinity N-methyl-D-aspartate channel blocker memantine", "From PCP to MXE: a comprehensive review of the non-medical use of dissociative drugs: PCP to MXE", "Memantine misuse and social networks: A content analysis of Internet self-reports", Deoxyepinephrine (N-methyldopamine, epinine), Metabotropic glutamate receptor modulators, Glutamate metabolism/transport modulators, Trimetaphan camsilate (trimethaphan camsylate), Muscarinic acetylcholine receptor modulators, Acetylcholine metabolism/transport modulators, Serotonin antagonists and reuptake inhibitors, https://en.wikipedia.org/w/index.php?title=Memantine&oldid=996854006, Short description is different from Wikidata, Chemical articles with unknown parameter in Infobox drug, Wikipedia medicine articles ready to translate, Creative Commons Attribution-ShareAlike License, This page was last edited on 28 December 2020, at 22:48. Proc Natl Acad Sci U S A 2014 May 27 In a preclinical study, researchers identify differences in intracellular signaling for memantine's lack of … It has a role as a dopaminergic agent, an antiparkinson drug, a NMDA receptor antagonist, a neuroprotective agent and an antidepressant. [45] Because of its very long biological half-life, memantine was previously thought not to be a drug of abuse, although a few cases of sporadic recreational use have been described. Memantine is a primary aliphatic amine that is the 3,5-dimethyl derivative of 1-aminoadamantane.A low to moderate affinity uncompetitive (open-channel); NMDA receptor antagonist which binds preferentially to the NMDA receptor-operated cation channels. [8], Memantine has been associated with a modest improvement;[9] with small positive effects on cognition, mood, behavior, and the ability to perform daily activities in moderate-to-severe Alzheimer's disease. Here we review the molecular mechanism of memantine's action and also the basis for the drug's use in these neurological diseases, which are mediated at least in part by excitotoxicity. Persistent activation of central nervous system NMDA receptors by the excitatory amino acid glutamate has been theorized to contribute to the symptoms of … [9] Common adverse drug reactions (≥1% of people) include confusion, dizziness, drowsiness, headache, insomnia, agitation, and/or hallucinations. This overactivation is thought to contribute to neurotoxicity due to … think of a healing plant or healing open wound. The specific mechanism of action per receptor protein is not specific, keeping in mind the conjoined effect of AMPAfication has on NMDA receptor availability, might have some correlation, thus hypothetically generating an asynergistic ('negated' in title) mechanism of action. These potentially important differences between memantine and ketamine include effects on gating of blocked channels and binding of memantine to two sites on NMDA receptors. Memantine was first marketed for dementia in Germany in 1989 under the name Axura. [38] The cost of Namenda was $269 to $489 a month in 2012. ScienceDirect ® is a registered trademark of Elsevier B.V. ScienceDirect ® is a registered trademark of Elsevier B.V. [39], In February 2014, as the July 2015 patent expiration for memantine neared, Actavis, which had acquired Forest, announced that it was launching an extended release (XR) form of memantine that could be taken once a day instead of twice a day as needed with the then-current "immediate release" (IR) version, and that it intended to stop selling the IR version in August 2014 and withdraw the marketing authorization. [47], As of August 2017, memantine was marketed under many brand names worldwide including Abixa, Adaxor, Admed, Akatinol, Alceba, Alios, Almenta, Alois, Alzant, Alzer, Alzia, Alzinex, Alzixa, Alzmenda, Alzmex, Axura, Biomentin, Carrier, Cogito, Cognomem, Conexine, Cordure, Dantex, Demantin, Demax, Dementa, Dementexa, Ebitex, Ebixa, Emantin, Emaxin, Esmirtal, Eutebrol, Evy, Ezemantis, Fentina, Korint, Lemix, Lindex, Lindex, Lucidex, Manotin, Mantine, Mantomed, Marbodin, Mardewel, Marixino, Maruxa, Maxiram, Melanda, Memabix, Memamed, Memando, Memantin, Memantina, Memantine, Mémantine, Memantinol, Memantyn, Memanvitae, Memanxa, Memanzaks, Memary, Memax, Memexa, Memigmin, Memikare, Memogen, Memolan, Memorel, Memorix, Memotec, Memox, Memxa, Mentikline, Mentium, Mentixa, Merandex, Merital, Mexia, Mimetix, Mirvedol, Modualz, Morysa, Namenda, Nemdatine, Nemdatine, Nemedan, Neumantine, Neuro-K, Neuroplus, Noojerone, Polmatine, Prilben, Pronervon, Ravemantine, Talentum, Timantila, Tingreks, Tonibral, Tormoro, Valcoxia, Vilimen, Vivimex, Witgen, Xapimant, Ymana, Zalatine, Zemertinex, Zenmem, Zenmen, and Zimerz. [35] In 1998 NTI amended its agreement with Children's to allow Merz to take over development. [34], In the US, some CNS activities were discovered at Children's Hospital of Boston in 1990, and Children's licensed patents covering uses of memantine outside the field of ophthalmology to Neurobiological Technologies (NTI) in 1995. [2], Common side effects include headache, constipation, sleepiness, and dizziness. Because modulation of NMDA receptor activity can increase or decrease excitability of neuronal circuits, subtle differences in the mechanisms of action of NMDA receptor antagonists can strongly impact on their clinical effects. Namzaric contains two approved active components including memantine hydrochloride extended-release, which is an NMDA receptor antagonist, and donepezil hydrochloride, an acetylcholinesterase inhibitor. The principal mechanism of action of memantine is believed to be the blockade of current flow through channels of N-methyl-d-aspartate (NMDA) receptors--a glutamate receptor subfamily broadly involved in brain function. Memantine reduces the actions of chemicals in the brain that may contribute to the symptoms of Alzheimer's disease. [36], In 2000, Merz partnered with Forest to develop the drug for Alzheimer's disease in the U.S. under the name Namenda. We use cookies to help provide and enhance our service and tailor content and ads. Excitotoxicity is defined as excessive exposure to the neurotransmitter glutamate or overstimulation of its membrane receptors, leading to neuronal injury or death. August 24, 2010. Epub 2014 Dec 2. Memantine is believed to slow the neurotoxicity associated with Alzheimer’s disease and other neurodegenerative diseases . Although many may view these data as the first indication of a “disease modifying” mechanism of action for memantine, this is inconsistent with the clinical experience and reports using memantine, where only limited effects are noted. However, when nerve cells are damaged by Alzheimer’s disease, too much glutamate is produced. [46], A study examining self-reported misuse of memantine on the social network reddit shown that the drug was used as a recreational drug and as a nootropic, but also that it was misused in various illnesses as self-medication without strong scientific basis.