Memantine: Difference between revisions

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{{Short description|Medication used to treat Alzheimer's disease}}
== Memantine ==
{{Drugbox
| Verifiedfields = changed
| Watchedfields = changed
| verifiedrevid = 477002015
| IUPAC_name = 3,5-Dimethyladamantan-1-amine
| image = Memantine_structure.svg
| width = 200
| image2 = Memantine-3D-balls.png
| width2 = 200
| tradename = Namenda, others
| Drugs.com =
| MedlinePlus = a604006
| pregnancy_AU = B2
| pregnancy_US = B
| legal_AU = S4
| legal_CA = Rx-only
| legal_UK = POM
| legal_US = Rx-only
| routes_of_administration = [[Oral administration|By mouth]]
| bioavailability = 100%
| protein_bound = 45%
| metabolism = Hepatic (minimal)
| elimination_half-life = 60–100 hours
| excretion = Renal
| CAS_number = 19982-08-2
| ATC_prefix = N06
| ATC_suffix = DX01
| PubChem = 4054
| DrugBank = DB01043
| ChemSpiderID = 3914
| UNII = G7D6I58A25
| KEGG = D08270
| ChEBI = 31432
| ChEMBL = 1088
| IUPHAR_ligand = 4254
| C=12
| H=21
| N=1
| smiles = CC12CC3CC(C1)(CC(C2)(C3)C)N
| StdInChI = 1S/C12H21N/c1-9-4-10-6-12(2,7-11(9)5-10)8-13/h9-11H,4-8,13H2,1-3H3
| StdInChIKey = JHJWZFAPYGJRFN-UHFFFAOYSA-N
}}


'''Memantine''' is a [[medication]] used to treat moderate-to-severe [[Alzheimer's disease]]. It is less preferred than [[acetylcholinesterase inhibitors]] such as [[donepezil]] and [[rivastigmine]]. Memantine is taken by mouth.
[[File:Memantine_structure.svg|Structure of Memantine|thumb|right]]


==Medical uses==
'''Memantine''' is a medication used to treat moderate to severe [[Alzheimer's disease]]. It is an [[NMDA receptor antagonist]] that works by blocking the effects of excessive [[glutamate]] in the brain, which is thought to contribute to the symptoms of Alzheimer's disease. Memantine is not a cure for Alzheimer's, but it can help improve symptoms and slow the progression of the disease in some patients.
Memantine is primarily used for the treatment of [[Alzheimer's disease]]. It is believed to work by blocking [[N-methyl-D-aspartate receptor|NMDA receptors]], which are involved in [[synaptic plasticity]] and [[memory]]. This action helps to reduce the symptoms of Alzheimer's disease, such as [[cognitive decline]] and [[memory loss]].


==Side effects==
== Mechanism of Action ==
Common side effects of memantine include [[dizziness]], [[headache]], [[confusion]], and [[constipation]]. Serious side effects are rare but can include [[hallucinations]], [[hypertension]], and [[seizures]].


==Pharmacology==
Memantine acts as an uncompetitive antagonist at the [[N-methyl-D-aspartate receptor|NMDA receptor]], a type of [[glutamate receptor]] in the brain. Under normal conditions, glutamate is involved in learning and memory by activating NMDA receptors. However, in Alzheimer's disease, excessive glutamate activity can lead to neuronal damage and cognitive decline. Memantine binds to the NMDA receptor with moderate affinity, blocking the effects of excessive glutamate while allowing normal synaptic transmission.
Memantine is an [[NMDA receptor antagonist]]. It binds to the [[NMDA receptor]] with a higher affinity than [[magnesium]] ions, which are naturally present in the [[synapse]]. This binding prevents excessive [[calcium]] influx into the [[neuron]], which can lead to [[neuronal damage]] and [[cell death]].


==Pharmacokinetics==
== Clinical Use ==
Memantine is well absorbed after oral administration, with a bioavailability of nearly 100%. It is minimally metabolized in the [[liver]] and is primarily excreted unchanged in the [[urine]]. The elimination half-life of memantine is between 60 and 100 hours.


==History==
Memantine is primarily used in the management of moderate to severe Alzheimer's disease. It is often prescribed in combination with [[acetylcholinesterase inhibitors]] such as [[donepezil]], [[rivastigmine]], or [[galantamine]]. The combination therapy can provide additional benefits in terms of cognitive function and daily living activities.
Memantine was first synthesized and developed by [[Eli Lilly and Company]] in the 1960s. It was later marketed by [[Merz Pharmaceuticals]] under the brand name Namenda. It was approved for the treatment of Alzheimer's disease in the [[United States]] by the [[Food and Drug Administration]] (FDA) in 2003.


==Research==
== Side Effects ==
Research is ongoing to explore the potential use of memantine in other [[neurological disorders]], such as [[Parkinson's disease]], [[Huntington's disease]], and [[multiple sclerosis]]. Studies are also being conducted to investigate its effects on [[depression]] and [[anxiety]].
 
Common side effects of memantine include dizziness, headache, confusion, and constipation. Less common side effects may include [[hallucinations]], [[hypertension]], and [[fatigue]]. Patients are advised to report any unusual symptoms to their healthcare provider.
 
== Dosage and Administration ==
 
Memantine is available in tablet form, as an oral solution, and as an extended-release capsule. The typical starting dose is 5 mg per day, which is gradually increased to a maintenance dose of 20 mg per day. The extended-release form is usually started at 7 mg per day and increased to a maximum of 28 mg per day.
 
== Pharmacokinetics ==
 
Memantine is well absorbed from the gastrointestinal tract, with a bioavailability of approximately 100%. It is partially metabolized in the liver and excreted primarily in the urine. The half-life of memantine is about 60 to 80 hours, allowing for once-daily dosing.
 
[[File:Memantine_ball-and-stick_model.png|Ball-and-stick model of Memantine|thumb|left]]
 
== History ==
 
Memantine was first synthesized in the late 1960s and was initially used as an antiviral agent. Its potential for treating Alzheimer's disease was discovered in the 1980s, and it was approved for this use in Europe in 2002 and in the United States in 2003.
 
== Related Pages ==


==See also==
* [[Alzheimer's disease]]
* [[Alzheimer's disease]]
* [[Acetylcholinesterase inhibitors]]
* [[NMDA receptor]]
* [[NMDA receptor]]
* [[Donepezil]]
* [[Glutamate]]
* [[Rivastigmine]]
* [[Acetylcholinesterase inhibitor]]
[[Category:Alzheimer's disease]]
 
[[Category:NMDA receptor antagonists]]
[[Category:NMDA receptor antagonists]]
[[Category:Drugs acting on the nervous system]]
[[Category:Alzheimer's disease treatments]]
[[Category:Adamantanes]]
[[Category:Merz Pharmaceuticals brands]]
[[Category:Medicine]]
{{medicine-stub}}
<gallery>
File:Memantine structure.svg|Memantine
File:Memantine ball-and-stick model.png|Memantine
</gallery>
<gallery>
File:Memantine structure.svg|Memantine
File:Memantine ball-and-stick model.png|Memantine
</gallery>

Latest revision as of 11:16, 23 March 2025

Memantine[edit]

Structure of Memantine

Memantine is a medication used to treat moderate to severe Alzheimer's disease. It is an NMDA receptor antagonist that works by blocking the effects of excessive glutamate in the brain, which is thought to contribute to the symptoms of Alzheimer's disease. Memantine is not a cure for Alzheimer's, but it can help improve symptoms and slow the progression of the disease in some patients.

Mechanism of Action[edit]

Memantine acts as an uncompetitive antagonist at the NMDA receptor, a type of glutamate receptor in the brain. Under normal conditions, glutamate is involved in learning and memory by activating NMDA receptors. However, in Alzheimer's disease, excessive glutamate activity can lead to neuronal damage and cognitive decline. Memantine binds to the NMDA receptor with moderate affinity, blocking the effects of excessive glutamate while allowing normal synaptic transmission.

Clinical Use[edit]

Memantine is primarily used in the management of moderate to severe Alzheimer's disease. It is often prescribed in combination with acetylcholinesterase inhibitors such as donepezil, rivastigmine, or galantamine. The combination therapy can provide additional benefits in terms of cognitive function and daily living activities.

Side Effects[edit]

Common side effects of memantine include dizziness, headache, confusion, and constipation. Less common side effects may include hallucinations, hypertension, and fatigue. Patients are advised to report any unusual symptoms to their healthcare provider.

Dosage and Administration[edit]

Memantine is available in tablet form, as an oral solution, and as an extended-release capsule. The typical starting dose is 5 mg per day, which is gradually increased to a maintenance dose of 20 mg per day. The extended-release form is usually started at 7 mg per day and increased to a maximum of 28 mg per day.

Pharmacokinetics[edit]

Memantine is well absorbed from the gastrointestinal tract, with a bioavailability of approximately 100%. It is partially metabolized in the liver and excreted primarily in the urine. The half-life of memantine is about 60 to 80 hours, allowing for once-daily dosing.

Ball-and-stick model of Memantine

History[edit]

Memantine was first synthesized in the late 1960s and was initially used as an antiviral agent. Its potential for treating Alzheimer's disease was discovered in the 1980s, and it was approved for this use in Europe in 2002 and in the United States in 2003.

Related Pages[edit]