Glutamate is another chemical that helps to send messages between nerve cells in the brain. [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. By binding to the NMDA receptor with a higher affinity than Mg 2+ ions, memantine is able to inhibit the prolonged influx of Ca 2+ ions [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. Memantine is used for the treatment of moderate to severe dementia associated with Alzheimer's. [31], It acts as an agonist at the σ1 receptor with a low Ki of 2.6 μM (2600 nM). Memantine may also be used for purposes not listed in this medication guide. Memantine is, in general, well tolerated. Excessive activation causes a buildup of these calcium ions, which then leads to the death of the nerve cell. The next day I slinked around the house ( you'll know what I mean if you've ever taken a high dosage of Memantine) and started to research memantine's action of mechanism. This overactivation is thought to contribute to neurotoxicity due to … 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. Due to this low affinity, therapeutic concentrations of memantine are most likely too low to have any sigmaergic effect as a typical therapeutic dose is 20 mg, however excessive doses of memantine taken for recreational purposes many times greater than prescribed doses may indeed activate this receptor. [10][11] There does not appear to be any benefit in mild disease.[12]. [40][41], In December 2014, a judge granted New York State its request and issued an injunction, preventing Actavis from withdrawing the IR version until generic versions could launch. Persistent activation of central nervous system NMDA receptors by the excitatory amino acid glutamate has been theorized to contribute to the symptoms of … Surprisingly, other drugs that block NMDA receptor channels, such as ketamine, exhibit serious deleterious effects. Megan Brooks. Memantine is a clinically useful drug in many neurological disorders, including Alzheimer's disease. However the supply of the XR version ran short, so Actavis extended the deadline until the fall. Agent for Alzheimer's Dementia Pharmacology (Mechanism of Action) ❖ Memantine is though to exert its therapeutic effect through its action as a low to moderate affinity uncompetitive (open-channel) NMDA receptor antagonist ❖ It bind preferentially to the NMDA receptor-operated cation channels to reduce their persistent activation Memantine's Unique Mechanism of Action Uncovered. Memantine is the first in a novel class of Alzheimer's disease medications ... (15 February 1997). This drug can help reduce the activity of glutamate, an excitatory neurotransmitter which can play a role in Alzheimer’s dementia. These data, however, are extremely important in two key regards. It has a role as a dopaminergic agent, an antiparkinson drug, a NMDA receptor antagonist, a neuroprotective agent and an antidepressant. This is a tactic to thwart generic competition called "product hopping". Later it was discovered to have CNS activity, and was developed by Merz for dementia in Germany; the NMDA activity was discovered after trials had already begun. [3] Treatment should only be continued if beneficial effects are seen. The analysis included double-blind, randomized, placebo-controlled trials of memantine in … As the mechanism of action of memantine differs from the widely used cholineste-rase inhibitors, combination therapy could be complementary or synergistic. [2][3] It is less preferred than acetylcholinesterase inhibitors such as donepezil. [1], It was also marketed in some countries as a combination drug with donepezil under the brands Namzaric, Neuroplus Dual, and Tonibral MD. [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. MECHANISM OF ACTION. 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. Patient/caregiver was instructed upon therapeutic uses and mechanism of action of Memantine as follows: Memantine is a medication reducing the activity of the neurotransmitter glutamic acid on NMDA receptors in the brain. Namzaric contains two approved active components including memantine hydrochloride extended-release, which is an NMDA receptor antagonist, and donepezil hydrochloride, an acetylcholinesterase inhibitor. 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. Mechanism of action Continuous activation of the N-methyl-D-aspartate (NMDA) receptors in the central nervous system caused by glutamate is thought to cause some of the Alzheimer's disease symptoms. Memantine works differently from donepezil, rivastigmine and galantamine. [6][7] One guideline recommends memantine or an AChE inhibitor be considered in people in the early-to-mid stage of dementia. [3] In 2017, it was the 149th most commonly prescribed medication in the United States, with more than four million prescriptions. Copyright © 2006 Elsevier Ltd. All rights reserved. Memantine’s main mechanism is through glutamate NMDA receptor inhibition in the brain. When these receptors (also known as NMDA receptors) are activated, calcium ions enter the nerve cells. try out memantine so get a better memory, try prednisone for weakness but don't overdo it. Memantine reduces the actions of chemicals in the brain that may contribute to the symptoms of Alzheimer's disease. Memantine About Memantine N-Methyl-D-Aspartate Receptor Antagonist, dopamine D2 agonist, Antidementia agent,In Alzheimer`s disease. [2], Memantine was approved for medical use in the United States in 2003. namenda. Surprisingly, other drugs that block NMDA receptor channels, such as ketamine, exhibit serious deleterious effects. In fact, this issue was addressed in a recently published trial.10 In a multicentric trial, about 400 patients Memantine was first marketed for dementia in Germany in 1989 under the name Axura. "Mechanism of memantine block of NMDA-activated channels in rat ... Caruso C, Lasaga M (February 2008). Memantine is a clinically useful drug in many neurological disorders, including Alzheimer's disease. Neuroprotective and symptomatological action of memantine relevant for alzheimer’s disease — a unified glutamatergic hypothesis on the mechanism of action. Memantine acts as a non-competitive antagonist at the 5-HT3 receptor, with a potency similar to that for the NMDA receptor. Memantine mechanism of action. [19], Memantine appears to be generally well tolerated by children with autism spectrum disorder. [20], A dysfunction of glutamatergic neurotransmission, manifested as neuronal excitotoxicity, is hypothesized to be involved in the etiology of Alzheimer's disease. [18] Despite isolated reports, recreational use of memantine is rare due to the drug's long duration and limited availability. Copyright © 2021 Elsevier B.V. or its licensors or contributors. 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. [44], One preclinical study on monkeys showed that memantine was capable of inducing a PCP-like intoxication. Memantine hydrochloride should be administered with caution to patients with severe hepatic impairment [see Clinical Pharmacology (12.3)]. Targeting the glutamatergic system, specifically NMDA receptors, offers a novel approach to treatment in view of the limited efficacy of existing drugs targeting the cholinergic system. 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 … However, when nerve cells are damaged by Alzheimer’s disease, too much glutamate is produced. [33], Memantine was first synthesized and patented by Eli Lilly and Company in 1968 as an anti-diabetic agent, but it was ineffective at lowering blood sugar. Mechanism of Action. According to a theory known as the excitotoxicity theory, lower energy levels in the nerve cells of people with HD cause them to be overly sensitive to glutamate. Common Questions and Answers about Memantine mechanism of action. Memantine is an NMDA antagonist (AKA Glutamate receptor antagonist) NMDA receptor found on post synaptic membrane; Prevents the binding of glutamate to NMDA receptor; Therefore, prevents excitotoxicity by preventing the influx of Ca 2+ into the post synaptic membrane; By preventing excitotoxicity, memantine helps prevent neurodegeneration think of a healing plant or healing open wound. [34], In 2000, Merz partnered with Suntory for the Japanese market and with Lundbeck for other markets including Europe;[37] the drug was originally marketed by Lundbeck under the name Ebixa. Although the drug does improve cognitive abilities as it’s mechanism of action, it is most likely to occur only in the use of individuals suffering from dementia or other brain injuries. As a result, even normal levels of glutamate can overactivate the glutamate receptors on the nerve cells. [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. Alpha-7 nAChR upregulates quickly in response to antagonism, which could explain the cognitive-enhancing effects of chronic memantine treatment. 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. [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. the different state of mind you experience with memantine treatment and the new ways of thinking it creates can make you stumble a little the first time. (For more on the excitotoxicity theor… FIGURE 1 Schematic presentation of the glutamatergic synapse and major ionotropic glutamate receptors - AMPA and NMDA. The unusual therapeutic utility of memantine probably results from inhibitory mechanisms shared with ketamine, combined with actions specific to memantine. 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. We use cookies to help provide and enhance our service and tailor content and ads. Synapse 62 (2): 149-53. 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. - "Neuroprotective and symptomatological action of memantine relevant for alzheimer’s disease — a unified glutamatergic hypothesis on the mechanism of action" August 24, 2010. [30], Memantine acts as an agonist at the dopamine D2 receptor with equal or slightly higher affinity than to the NMDA receptors. 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. 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. [38] The cost of Namenda was $269 to $489 a month in 2012. Memantine is classified as an NMDA receptor antagonist. [9] Common adverse drug reactions (≥1% of people) include confusion, dizziness, drowsiness, headache, insomnia, agitation, and/or hallucinations. Mechanism of Action. [42][43] In August 2015, Actavis' request was denied. [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. [2] It is available as a generic medication. By continuing you agree to the use of cookies. Excitotoxicity is defined as excessive exposure to the neurotransmitter glutamate or overstimulation of its membrane receptors, leading to neuronal injury or death. Memantine HCL is not known to cause addiction but, used in high dosages and in conjunction with other substances, can lead to dangerous side effects. [2], Common side effects include headache, constipation, sleepiness, and dizziness. Surprisingly, other drugs that block NMDA receptor channels, such as ketamine, exhibit serious deleterious effects. [2][3] Severe side effects may include blood clots, psychosis, and heart failure. [36], In 2000, Merz partnered with Forest to develop the drug for Alzheimer's disease in the U.S. under the name Namenda. [35] In 1998 NTI amended its agreement with Children's to allow Merz to take over development. ScienceDirect ® is a registered trademark of Elsevier B.V. ScienceDirect ® is a registered trademark of Elsevier B.V. [24][25][26] The interaction of memantine with NMDA receptors plays a major role in the symptomatic improvement that the drug produces in Alzheimer's disease. [9][17], Like many other NMDA antagonists, memantine behaves as a dissociative anesthetic at supratherapeutic doses. [28][29] It has been shown that the number of nicotinic receptors in the brain are reduced in Alzheimer's disease, even in the absence of a general decrease in the number of neurons, and nicotinic receptor agonists are viewed as interesting targets for anti-Alzheimer drugs. It can be noted that memantine is an antagonist at Alpha-7 nAChR, which may contribute to initial worsening of cognitive function during early memantine treatment. Memantine is an antagonist at N-methyl-D-aspartate (NMDA) receptors with a low to moderate binding affinity. Memantine when added to donepezil in those with moderate-to-severe dementia resulted in "limited improvements" in a 2017 review. [18] Also memantine seems to lack effects such as euphoria or hallucinations. [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 medication used to treat moderate-to-severe Alzheimer's disease. Memantine acts as a non-competitive antagonist at different neuronal nicotinic acetylcholine receptors (nAChRs) at potencies possibly similar to the NMDA and 5-HT3 receptors, but this is difficult to ascertain with accuracy because of the rapid desensitization of nAChR responses in these experiments. Memantine pharmacology is complex as is the pharmacology of any medication working in the brain. [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. [15][16] Recent scientific journal reports are showing guarded promise with severe obsessive compulsive disorder. Wojciech Danysz 1, Chris G. Parsons 1, Hans-JÖrg MÖbius 1, Albrecht StÖffler 1 & Memantine is used to treat moderate to severe dementia of the Alzheimer's type. Mechanism of Action. Curr Opin Pharmacol. Properties of Memantine and Mechanism of Action Structural Formula of Memantine Memantine is a NMDA Receptor Channel Antagonist Kinetics of NMDA-Receptor Blockade ... – A free PowerPoint PPT presentation (displayed as a Flash slide show) on PowerShow.com - id: 6607c3-NjNkZ Mechanism of Action of Memantine Memantine in an uncompetitive (low to moderate affinity to) NMDA (N-methyl-D-aspartate) receptor antagonist. We conducted a systematic review and meta-analysis on whether memantine was beneficial for the treatment of depressive symptoms in major depressive disorder (MDD) and bipolar disorder (BD). Memantine is believed to slow the neurotoxicity associated with Alzheimer’s disease and other neurodegenerative diseases . [14] Effects in autism are unclear. [1], Medication used to treat moderate-to-severe Alzheimer's disease, InChI=1S/C12H21N/c1-10-3-9-4-11(2,6-10)8-12(13,5-9)7-10/h9H,3-8,13H2,1-2H3, NICE review of technology appraisal guidance 111 January 18, 2011, National Institute of Clinical Excellence, antagonist at glutamatergic NMDA receptors, nicotinic acetylcholine receptors (nAChRs), Discovery and development of memantine and related compounds, "Memantine Hydrochloride Monograph for Professionals", "Memantine Hydrochloride - Drug Usage Statistics", Alzheimer's disease - donepezil, galantamine, rivastigmine and memantine (review): final appraisal determination, "Medication appropriateness tool for co-morbid health conditions in dementia: consensus recommendations from a multidisciplinary expert panel", "Lack of evidence for the efficacy of memantine in mild Alzheimer disease", "Treatment effects between monotherapy of donepezil versus combination with memantine for Alzheimer disease: A meta-analysis", "Overview | Dementia: assessment, management and support for people living with dementia and their carers | Guidance | NICE", "mGluR5 antagonist-induced psychoactive properties: MTEP drug discrimination, a pharmacologically selective non-NMDA effect with apparent lack of reinforcing properties", 10.1002/(SICI)1099-1166(199901)14:1<3::AID-GPS897>3.0.CO;2-7, "The neuropharmacological basis for the use of memantine in the treatment of Alzheimer's disease", "Memantine preferentially blocks extrasynaptic over synaptic NMDA receptor currents in hippocampal autapses", "Open-channel blockers at the human alpha4beta2 neuronal nicotinic acetylcholine receptor", "Memantine blocks alpha7* nicotinic acetylcholine receptors more potently than n-methyl-D-aspartate receptors in rat hippocampal neurons", "Pharms - Memantine (also Namenda) : Erowid Exp: Main Index", "Form 10-KSB For the fiscal year ended June 30, 1996", "Lundbeck signs memantine licensing agreement for Merz+Co", "Evaluating Prescription Drugs Used to Treat: Alzheimer's Disease. 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Be administered with caution to patients with severe hepatic impairment [ see Clinical pharmacology ( )... Memantine seems to lack effects such as euphoria or hallucinations 7 ] One guideline recommends memantine an... Various other neurotransmitters in the brain s dementia or its licensors or contributors or its licensors or contributors insights! Md reviewing Gideons ES et al resulted in `` limited improvements '' in a 2017 review as the of! 35 ] in August 2015, Actavis ' memantine mechanism of action animation was denied ] Despite isolated reports, recreational of... Are extremely important in two key regards continuing you agree to the death of the XR version ran,... Tolerated by children with autism spectrum disorder overstimulation of its membrane receptors, leading to neuronal or... A 2017 review Alzheimer ’ s dementia be used for purposes not listed in this medication guide rare...