Drug Reference for FDA Approved Alzheimer's Disease Drugs @ Neurotransmitter.net
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Initial Approval: Product Insert: RxList: Epocrates: Empirical Formula: Molecular Mass: |
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Possible Mechanisms of Action: Donepezil is a selective and reversible acetylcholinesterase inhibitor (1). Donepezil is a mixed type inhibitor of acetycholinesterase, meaning that it exhibits both noncompetitive and competitive components of inhibition (1). |
Chemical Class: PubChem 2D Structure: |
Generic Name: Common Chemical Name: Major Metabolites: Database Search Links: |
Initial Approval: Product Insert: [Link] (ER) RxList: Epocrates: Empirical Formula: Molecular Mass: |
Indications: |
Possible Mechanisms of Action: Galantamine is a competitive and reversible inhibitor of acetylcholinesterase (2). The drug also acts as a positive allosteric modulator at nicotinic acetylcholine receptors including the alpha4beta2 subtype (3). |
Chemical Class: PubChem 2D Structure: |
Generic Name: IUPAC Name: Major Metabolites: Dosage Forms/Routes: Database Search Links: |
Initial Approval: Product Insert: RxList: Epocrates: Empirical Formula: Molecular Mass: |
Indications: |
Possible Mechanisms of Action: |
Chemical Class: PubChem 2D Structure: |
Generic Name: IUPAC Name: Major Metabolite: Database Search Links: |
Initial Approval: Product Insert: RxList: Epocrates: Empirical Formula: Molecular Mass: |
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Possible Mechanisms of Action: Rivastigmine is a slowly reversible (pseudo-irreversible) inhibitor of acetylcholinesterase and butyrylcholinesterase (8). Rivastigmine inhibits acetylcholinesterase in a noncompetitive manner (9). |
Chemical Class: PubChem 2D Structure: |
Generic Name: Common Chemical Name: Major Metabolites: Database Search Links: |
Initial Approval: Product Insert: RxList: Epocrates: Empirical Formula: Molecular Mass: |
Indications: |
Possible Mechanisms of Action: Tacrine is a reversible acetylcholinesterase inhibitor (1). Tacrine is a mixed type inhibitor of acetycholinesterase, meaning that it exhibits both noncompetitive and competitive components of inhibition (1). Tacrine is also a reversible inhibitor of butyrylcholinesterase (1). |
Chemical Class: 2D Structure: |
References:
1. Snape MF, Misra A, Murray TK, De Souza RJ, Williams JL, Cross AJ, Green AR.
A comparative study in rats of the in vitro and in vivo pharmacology of the acetylcholinesterase inhibitors tacrine, donepezil and NXX-066.
Neuropharmacology. 1999 Jan;38(1):181-93. [Abstract]
2. Lilienfeld S.
Galantamine--a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer's disease.
CNS Drug Rev. 2002 Summer;8(2):159-76. [Abstract]
3. Samochocki M, Zerlin M, Jostock R, Groot Kormelink PJ, Luyten WH, Albuquerque EX, Maelicke A.
Galantamine is an allosterically potentiating ligand of the human alpha4/beta2 nAChR.
Acta Neurol Scand Suppl 2000;176:68-73 [Abstract]
4. Mobius HJ.
Pharmacologic rationale for memantine in chronic cerebral hypoperfusion, especially vascular dementia.
Alzheimer Dis Assoc Disord. 1999 Oct-Dec;13 Suppl 3:S172-8. [Abstract]
5. Reiser G, Binmoller FJ, Koch R.
Memantine (1-amino-3,5-dimethyladamantane) blocks the serotonin-induced depolarization response in a neuronal cell line.
Brain Res. 1988 Mar 8;443(1-2):338-44. [Abstract]
6. 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. [Abstract]
7. Buisson, Bruno, Bertrand, Daniel
Open-Channel Blockers at the Human alpha 4beta 2 Neuronal Nicotinic Acetylcholine Receptor
Mol Pharmacol 1998 53: 555-563 [Full Text]
8. Poirier J.
Evidence that the clinical effects of cholinesterase inhibitors are related to potency and targeting of action.
Int J Clin Pract Suppl. 2002 Jun;(127):6-19. [Abstract]
9. Spencer CM, Noble S.
Rivastigmine. A review of its use in Alzheimer's disease.
Drugs Aging. 1998 Nov;13(5):391-411. [Abstract]
10. Aracava Y, Pereira EF, Maelicke A, Albuquerque EX.
Memantine blocks alpha7* nicotinic acetylcholine receptors more potently than n-methyl-D-aspartate receptors in rat hippocampal neurons.
J Pharmacol Exp Ther. 2005 Mar;312(3):1195-205. [Abstract]