Peringatan Keamanan

LD50

Oral LD50, mouse 437-498 mg/kg F4375
Oral LD50, rat 328-370 mg/kg F4375

Carcinogenesis, Mutagenesis, Impairment of Fertility

No evidence of carcinogenicity was seen in mouse and rat models administered memantine at doses equivalent to supratherapeutic human doses FDA label. Additionally, no genotoxic potential was noted when a battery of assays was performed. No effects on fertility or reproductive performance were noted in rats given to 18 mg/kg/day (equivalent to 9 times the maximum recommended human dose) orally from 14 days preceding mating through gestation and lactation in females, or for 60 preceding mating activity in males animals FDA label.

Use in pregnancy

This drug is considered a pregnancy category B drug, meaning no sufficiently controlled and adequate studies of memantine in pregnant women have been performed. This drug should be taken during pregnancy only if the potential benefit justifies the possible fetal risk FDA label.

Use in nursing

It is unknown whether memantine is excreted in human milk. Due to that fact that many drugs are found excreted in human milk, caution should be observed when this drug is taken by a nursing mother FDA label.

Memantine

DB01043

small molecule approved investigational

Deskripsi

Initially approved by the FDA in 2013, memantine is an N-methyl-D-aspartate (NMDA) receptor antagonist used in the management of Alzheimer's Disease (AD). It is different from many other Alzheimer's Disease medications, as it works by a different mechanism than the cholinesterase enzyme inhibitors normally employed in the management of Alzheimer's disease A1639. Memantine blocks the effects of glutamate, a neurotransmitter in the brain that leads to neuronal excitability and excessive stimulation in Alzheimer's Disease T556.

In 2010, it was estimated that 36 million people worldwide live with Alzheimer's Disease. In 2013, this number increased to 44 million. Almost doubling every 20 years, the prevalence of Alzheimer's Disease is predicted to reach 66 million by 2030 and to 115 million by 2050 F4366. In December 2013, the G8 dementia summit concluded that dementia should be considered a global priority with the objective of developing a cure or a disease-modifying therapy by the year 2025 L5953, F4366.

Struktur Molekul 2D

Berat 179.3018
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal elimination half-life of memantine ranges from 60 to 80 hours in humans.[A251130,L42570] Following administration of a single oral dose of 10 mg/kg memantine in rats, the elimination half-life was 2.36 ± 0.20 hours. Following a single intravenous dose of 2 mg/kg in rats, the elimination half-life was 2.28 ± 0.48 hours.[A251125]
Volume Distribusi The mean volume of distribution of memantine is 9-11 L/kg [FDA label].
Klirens (Clearance) This drug is cleared by active tubular secretion in the kidneys. Tubular reabsorption of this drug is pH dependent [FDA label].

Absorpsi

After an oral dose, memantine is well absorbed. Its peak drug concentrations are attained in about 3-7 hours. Memantine shows linear pharmacokinetics when given at normal therapeutic doses. This drug can be taken without regard to food, as there is no effect of food on memantine absorption FDA label.

Metabolisme

This drug is partially metabolized in the liver. The hepatic CYP450 enzyme system does not majorly contribute to the metabolism of this drug FDA label.

Rute Eliminasi

This drug is mainly excreted in the urine. Approximately 48% of administered memantine is excreted unchanged in urine FDA label. The remainder of the drug is metabolized to three main metabolites. These metabolites are the N-glucuronide conjugate, 6-hydroxy memantine, and 1-nitroso-deaminated memantine, which show minimal NMDA receptor antagonist activity FDA label.

Interaksi Makanan

2 Data
  • 1. Take with a full glass of water.
  • 2. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

1178 Data
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Memantine.
Methylphenidate The risk or severity of adverse effects can be increased when Methylphenidate is combined with Memantine.
Dexmethylphenidate The risk or severity of adverse effects can be increased when Dexmethylphenidate is combined with Memantine.
Metoclopramide The therapeutic efficacy of Memantine can be decreased when used in combination with Metoclopramide.
Ethoxzolamide The excretion of Memantine can be decreased when combined with Ethoxzolamide.
Methazolamide The excretion of Memantine can be decreased when combined with Methazolamide.
Acetazolamide The excretion of Memantine can be decreased when combined with Acetazolamide.
Zonisamide The excretion of Memantine can be decreased when combined with Zonisamide.
Diclofenamide The excretion of Memantine can be decreased when combined with Diclofenamide.
Bupropion The excretion of Memantine can be decreased when combined with Bupropion.
Tramadol The risk or severity of adverse effects can be increased when Tramadol is combined with Memantine.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Memantine.
Profenamine The risk or severity of adverse effects can be increased when Profenamine is combined with Memantine.
Meperidine The risk or severity of adverse effects can be increased when Meperidine is combined with Memantine.
Haloperidol The risk or severity of adverse effects can be increased when Haloperidol is combined with Memantine.
Dextromethorphan The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Memantine.
Procaine The risk or severity of adverse effects can be increased when Procaine is combined with Memantine.
Ethanol The risk or severity of adverse effects can be increased when Ethanol is combined with Memantine.
Amantadine The risk or severity of adverse effects can be increased when Amantadine is combined with Memantine.
Felbamate The risk or severity of adverse effects can be increased when Felbamate is combined with Memantine.
Halothane The risk or severity of adverse effects can be increased when Halothane is combined with Memantine.
Chloroprocaine Memantine may increase the neuromuscular blocking activities of Chloroprocaine.
Orphenadrine The risk or severity of adverse effects can be increased when Orphenadrine is combined with Memantine.
Ketamine The risk or severity of adverse effects can be increased when Ketamine is combined with Memantine.
Tenocyclidine The risk or severity of adverse effects can be increased when Tenocyclidine is combined with Memantine.
Phencyclidine The risk or severity of adverse effects can be increased when Phencyclidine is combined with Memantine.
Agmatine The risk or severity of adverse effects can be increased when Agmatine is combined with Memantine.
Ifenprodil The risk or severity of adverse effects can be increased when Ifenprodil is combined with Memantine.
Dipyridamole The therapeutic efficacy of Memantine can be decreased when used in combination with Dipyridamole.
Ephedrine Memantine may increase the neuromuscular blocking activities of Ephedrine.
Bambuterol Memantine may increase the neuromuscular blocking activities of Bambuterol.
Sar9, Met (O2)11-Substance P Memantine may increase the neuromuscular blocking activities of Sar9, Met (O2)11-Substance P.
Cocaine Memantine may increase the neuromuscular blocking activities of Cocaine.
Trimethaphan Memantine may increase the neuromuscular blocking activities of Trimethaphan.
Doxacurium Memantine may increase the neuromuscular blocking activities of Doxacurium.
Tubocurarine Memantine may increase the neuromuscular blocking activities of Tubocurarine.
Aclidinium Memantine may increase the neuromuscular blocking activities of Aclidinium.
Propacetamol Memantine may increase the neuromuscular blocking activities of Propacetamol.
Clevidipine Memantine may increase the neuromuscular blocking activities of Clevidipine.
Mirabegron Memantine may increase the neuromuscular blocking activities of Mirabegron.
Moxisylyte Memantine may increase the neuromuscular blocking activities of Moxisylyte.
Butyrylthiocholine Memantine may increase the neuromuscular blocking activities of Butyrylthiocholine.
Oxybuprocaine Memantine may increase the neuromuscular blocking activities of Oxybuprocaine.
Benzonatate Memantine may increase the neuromuscular blocking activities of Benzonatate.
Succinylcholine The metabolism of Succinylcholine can be decreased when combined with Memantine.
Cimetidine Cimetidine may decrease the excretion rate of Memantine which could result in a higher serum level.
Nizatidine Nizatidine may decrease the excretion rate of Memantine which could result in a higher serum level.
Ranitidine Ranitidine may decrease the excretion rate of Memantine which could result in a higher serum level.
Famotidine Famotidine may decrease the excretion rate of Memantine which could result in a higher serum level.
Methantheline Methantheline may decrease the excretion rate of Memantine which could result in a higher serum level.
Aluminium Aluminium may decrease the excretion rate of Memantine which could result in a higher serum level.
Magnesium oxide Magnesium oxide may decrease the excretion rate of Memantine which could result in a higher serum level.
Sodium bicarbonate Sodium bicarbonate may decrease the excretion rate of Memantine which could result in a higher serum level.
Aluminum hydroxide Aluminum hydroxide may decrease the excretion rate of Memantine which could result in a higher serum level.
Calcium carbonate Calcium carbonate may decrease the excretion rate of Memantine which could result in a higher serum level.
Metiamide Metiamide may decrease the excretion rate of Memantine which could result in a higher serum level.
Roxatidine acetate Roxatidine acetate may decrease the excretion rate of Memantine which could result in a higher serum level.
Magaldrate Magaldrate may decrease the excretion rate of Memantine which could result in a higher serum level.
Magnesium hydroxide Magnesium hydroxide may decrease the excretion rate of Memantine which could result in a higher serum level.
Magnesium trisilicate Magnesium trisilicate may decrease the excretion rate of Memantine which could result in a higher serum level.
Magnesium carbonate Magnesium carbonate may decrease the excretion rate of Memantine which could result in a higher serum level.
Lafutidine Lafutidine may decrease the excretion rate of Memantine which could result in a higher serum level.
Lavoltidine Lavoltidine may decrease the excretion rate of Memantine which could result in a higher serum level.
Bismuth subnitrate Bismuth subnitrate may decrease the excretion rate of Memantine which could result in a higher serum level.
Magnesium silicate Magnesium silicate may decrease the excretion rate of Memantine which could result in a higher serum level.
Aluminium acetoacetate Aluminium acetoacetate may decrease the excretion rate of Memantine which could result in a higher serum level.
Hydrotalcite Hydrotalcite may decrease the excretion rate of Memantine which could result in a higher serum level.
Magnesium peroxide Magnesium peroxide may decrease the excretion rate of Memantine which could result in a higher serum level.
Almasilate Almasilate may decrease the excretion rate of Memantine which could result in a higher serum level.
Aluminium glycinate Aluminium glycinate may decrease the excretion rate of Memantine which could result in a higher serum level.
Aloglutamol Aloglutamol may decrease the excretion rate of Memantine which could result in a higher serum level.
Niperotidine Niperotidine may decrease the excretion rate of Memantine which could result in a higher serum level.
Calcium silicate Calcium silicate may decrease the excretion rate of Memantine which could result in a higher serum level.
Aluminium phosphate Aluminium phosphate may decrease the excretion rate of Memantine which could result in a higher serum level.
Omeprazole Omeprazole may decrease the excretion rate of Memantine which could result in a higher serum level.
Lansoprazole Lansoprazole may decrease the excretion rate of Memantine which could result in a higher serum level.
Esomeprazole Esomeprazole may decrease the excretion rate of Memantine which could result in a higher serum level.
Dexlansoprazole Dexlansoprazole may decrease the excretion rate of Memantine which could result in a higher serum level.
Dexrabeprazole Dexrabeprazole may decrease the excretion rate of Memantine which could result in a higher serum level.
Pantoprazole Pantoprazole may decrease the excretion rate of Memantine which could result in a higher serum level.
Rabeprazole Rabeprazole may decrease the excretion rate of Memantine which could result in a higher serum level.
Sodium zirconium cyclosilicate Sodium zirconium cyclosilicate may decrease the excretion rate of Memantine which could result in a higher serum level.
Vonoprazan Vonoprazan may decrease the excretion rate of Memantine which could result in a higher serum level.
Risperidone The therapeutic efficacy of Memantine can be decreased when used in combination with Risperidone.
Paliperidone The therapeutic efficacy of Memantine can be decreased when used in combination with Paliperidone.
Bifeprunox The therapeutic efficacy of Memantine can be decreased when used in combination with Bifeprunox.
Iloperidone The therapeutic efficacy of Memantine can be decreased when used in combination with Iloperidone.
Cariprazine The therapeutic efficacy of Memantine can be decreased when used in combination with Cariprazine.
Lumateperone The therapeutic efficacy of Memantine can be decreased when used in combination with Lumateperone.
Sertindole The therapeutic efficacy of Memantine can be decreased when used in combination with Sertindole.
Asenapine The therapeutic efficacy of Memantine can be decreased when used in combination with Asenapine.
Lurasidone The therapeutic efficacy of Memantine can be decreased when used in combination with Lurasidone.
Perospirone The therapeutic efficacy of Memantine can be decreased when used in combination with Perospirone.
Brexpiprazole The therapeutic efficacy of Memantine can be decreased when used in combination with Brexpiprazole.
Blonanserin The therapeutic efficacy of Memantine can be decreased when used in combination with Blonanserin.
Melperone The therapeutic efficacy of Memantine can be decreased when used in combination with Melperone.
Zotepine The therapeutic efficacy of Memantine can be decreased when used in combination with Zotepine.
Brilaroxazine The therapeutic efficacy of Memantine can be decreased when used in combination with Brilaroxazine.
Ziprasidone The therapeutic efficacy of Memantine can be decreased when used in combination with Ziprasidone.
Olanzapine The therapeutic efficacy of Memantine can be decreased when used in combination with Olanzapine.

Target Protein

Glutamate (NMDA) receptor GRIN1
5-hydroxytryptamine receptor 3A HTR3A
Neuronal acetylcholine receptor subunit alpha-7 CHRNA7
D(2) dopamine receptor DRD2
Glutamate receptor ionotropic, NMDA 1 GRIN1
GABA(A) Receptor GABRA1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 10029935
    Cacabelos R, Takeda M, Winblad B: The glutamatergic system and neurodegeneration in dementia: preventive strategies in Alzheimer's disease. Int J Geriatr Psychiatry. 1999 Jan;14(1):3-47.
  • PMID: 14530799
    Rogawski MA, Wenk GL: The neuropharmacological basis for the use of memantine in the treatment of Alzheimer's disease. CNS Drug Rev. 2003 Fall;9(3):275-308.
  • PMID: 16906789
    Robinson DM, Keating GM: Memantine: a review of its use in Alzheimer's disease. Drugs. 2006;66(11):1515-34.
  • PMID: 11026482
    Rogawski MA: Low affinity channel blocking (uncompetitive) NMDA receptor antagonists as therapeutic agents--toward an understanding of their favorable tolerability. Amino Acids. 2000;19(1):133-49.
  • PMID: 11403963
    Rammes G, Rupprecht R, Ferrari U, Zieglgansberger W, Parsons CG: The N-methyl-D-aspartate receptor channel blockers memantine, MRZ 2/579 and other amino-alkyl-cyclohexanes antagonise 5-HT(3) receptor currents in cultured HEK-293 and N1E-115 cell systems in a non-competitive manner. Neurosci Lett. 2001 Jun 22;306(1-2):81-4.
  • PMID: 28922160
    Kishi T, Matsunaga S, Oya K, Nomura I, Ikuta T, Iwata N: Memantine for Alzheimer's Disease: An Updated Systematic Review and Meta-analysis. J Alzheimers Dis. 2017;60(2):401-425. doi: 10.3233/JAD-170424.
  • PMID: 26310825
    Lee SH, Kim SH, Noh YH, Choi BM, Noh GJ, Park WD, Kim EJ, Cho IH, Bae CS: Pharmacokinetics of Memantine after a Single and Multiple Dose of Oral and Patch Administration in Rats. Basic Clin Pharmacol Toxicol. 2016 Feb;118(2):122-7. doi: 10.1111/bcpt.12479. Epub 2015 Sep 28.
  • PMID: 23371894
    Noetzli M, Guidi M, Ebbing K, Eyer S, Wilhelm L, Michon A, Thomazic V, Alnawaqil AM, Maurer S, Zumbach S, Giannakopoulos P, von Gunten A, Csajka C, Eap CB: Population pharmacokinetic study of memantine: effects of clinical and genetic factors. Clin Pharmacokinet. 2013 Mar;52(3):211-23. doi: 10.1007/s40262-013-0032-2.
Textbook
  • Brianne Kuns; Dona Varghese (2019). StatPearls: Memantine. StatPearls Publishing.

Contoh Produk & Brand

Produk: 527 • International brands: 3
Produk
  • Act Memantine
    Tablet • 10 mg • Oral • Canada • Approved
  • Act Memantine
    Tablet • 5 mg • Oral • Canada • Approved
  • Apo-memantine
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Axura
    Tablet, film coated • 10 mg • Oral • EU • Approved
  • Axura
    Tablet, film coated • 10 mg • Oral • EU • Approved
  • Axura
    Tablet, film coated • 10 mg • Oral • EU • Approved
  • Axura
    Tablet, film coated • 10 mg • Oral • EU • Approved
  • Axura
    Tablet, film coated • 10 mg • Oral • EU • Approved
Menampilkan 8 dari 527 produk.
International Brands
  • Abixa
  • Akatinol
  • Memox

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul