Name: | Galantamine |
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PubChem Compound ID: | 10827215 |
Description: | A benzazepine derived from norbelladine. It is found in GALANTHUS and other AMARYLLIDACEAE. It is a cholinesterase inhibitor that has been used to reverse the muscular effects of GALLAMINE TRIETHIODIDE and TUBOCURARINE and has been studied as a treatment for ALZHEIMER DISEASE and other central nervous system disorders. |
Molecular formula: | C17H21NO3 |
Molecular weight: | 288.36 g/mol |
Name: | Galantamine |
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Name (isomeric): | DB00674 |
Drug Type: | small molecule |
Description: | A benzazepine derived from norbelladine. It is found in GALANTHUS and other AMARYLLIDACEAE. It is a cholinesterase inhibitor that has been used to reverse the muscular effects of GALLAMINE TRIETHIODIDE and TUBOCURARINE and has been studied as a treatment for ALZHEIMER DISEASE and other central nervous system disorders. |
Synonyms: |
Galanthamine hydrobromide; (-)-Galanthamine; Galanthamine
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Brand: | Lycoremine, Reminyl, Galantamin, Lycoremin, Jilkon |
Category: | Parasympathomimetics, Nootropic Agents, Cholinesterase Inhibitors |
CAS number: | 357-70-0 |
Indication: | For the treatment of mild to moderate dementia of the Alzheimer's type. Has also been investigated in patients with mild cognitive impairment who did not meet the diagnostic criteria for Alzheimer's disease. |
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Pharmacology: |
Galantamine is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor. It is indicated for the treatment of mild to moderate dementia of the Alzheimer's type. An early pathophysiological feature of Alzheimer's disease that is associated with memory loss and cognitive deficits is a deficiency of acetylcholine as a result of selec...
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Galantamine is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor. It is indicated for the treatment of mild to moderate dementia of the Alzheimer's type. An early pathophysiological feature of Alzheimer's disease that is associated with memory loss and cognitive deficits is a deficiency of acetylcholine as a result of selective loss of cholinergic neurons in the cerebral cortex, nucleus basalis, and hippocampus. Galantamine is postulated to exert its therapeutic effect by enhancing cholinergic function. This is accomplished by increasing the concentration of acetylcholine through reversible inhibition of its hydrolysis by acetylcholinesterase. If this proposed mechanism of action is correct, Galantamine's effect may lessen as the disease progresses and fewer cholinergic neurons remain functionally intact. There is no evidence that Galantamine alters the course of the underlying dementing process.
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Mechanism of Action: |
Galantamine is a phenanthrene alkaloid and a reversible, competitive acetylcholinesterase inhibitor. It is not structurally related to other acetylcholinesterase inhibitors. Galantamine's proposed mechanism of action involves the reversible inhibition of acetylcholinesterase, which prevents the hydrolysis of acetycholine, leading to an increased co...
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Galantamine is a phenanthrene alkaloid and a reversible, competitive acetylcholinesterase inhibitor. It is not structurally related to other acetylcholinesterase inhibitors. Galantamine's proposed mechanism of action involves the reversible inhibition of acetylcholinesterase, which prevents the hydrolysis of acetycholine, leading to an increased concentration of acetylcholine at cholinergic synapses. Galantamine also binds allosterically with nicotinic acetylcholine receptors and may possibly potentiate the action of agonists (such as acetylcholine) at these receptors.
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Protein binding: | 18% |
Route of elimination: | Galantamine is metabolized by hepatic cytochrome P450 enzymes, glucuronidated, and excreted unchanged in the urine. |
Half Life: | 7 hours |
Clearance: | 300 mL/min [After IV. or oral administration] |
Toxicity: | LD50=75 mg/kg (rat) |
Affected organisms: | Humans and other mammals |
Food interaction: |
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Drug interaction: |
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UniProt ID: | P22303 | |||||||||||||
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Gene: | ACHE | |||||||||||||
Actions: | inhibitor | |||||||||||||
References: |
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UniProt ID: | P02708 | ||||||
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Gene: | CHRNA1 | ||||||
Actions: | allosteric modulator | ||||||
References: |
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UniProt ID: | P11230 | ||||||
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Gene: | CHRNB1 | ||||||
Actions: | allosteric modulator | ||||||
References: |
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UniProt ID: | Q07001 | ||||||
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Gene: | CHRND | ||||||
Actions: | allosteric modulator | ||||||
References: |
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UniProt ID: | P07510 | ||||||
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Gene: | CHRNG | ||||||
Actions: | allosteric modulator | ||||||
References: |
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UniProt ID: | Q04844 | ||||||
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Gene: | CHRNE | ||||||
Actions: | allosteric modulator | ||||||
References: |
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UniProt ID: | Q15822 | ||||||
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Gene: | CHRNA2 | ||||||
Actions: | allosteric modulator | ||||||
References: |
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UniProt ID: | P32297 | ||||||
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Gene: | CHRNA3 | ||||||
Actions: | allosteric modulator | ||||||
References: |
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UniProt ID: | P43681 | ||||||
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Gene: | CHRNA4 | ||||||
Actions: | allosteric modulator | ||||||
References: |
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UniProt ID: | P30532 | ||||||
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Gene: | CHRNA5 | ||||||
Actions: | allosteric modulator | ||||||
References: |
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UniProt ID: | Q15825 | ||||||
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Gene: | CHRNA6 | ||||||
Actions: | allosteric modulator | ||||||
References: |
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UniProt ID: | P36544 | ||||||
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Gene: | CHRNA7 | ||||||
Actions: | allosteric modulator | ||||||
References: |
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UniProt ID: | Q9UGM1 | ||||||
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Gene: | CHRNA9 | ||||||
Actions: | allosteric modulator | ||||||
References: |
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UniProt ID: | Q9GZZ6 | ||||||
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Gene: | CHRNA10 | ||||||
Actions: | allosteric modulator | ||||||
References: |
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UniProt ID: | P17787 | ||||||
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Gene: | CHRNB2 | ||||||
Actions: | allosteric modulator | ||||||
References: |
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UniProt ID: | Q05901 | ||||||
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Gene: | CHRNB3 | ||||||
Actions: | allosteric modulator | ||||||
References: |
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UniProt ID: | P30926 | ||||||
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Gene: | CHRNB4 | ||||||
Actions: | allosteric modulator | ||||||
References: |
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UniProt ID: | P06276 | |||
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Gene: | BCHE | |||
Actions: | inhibitor | |||
References: |
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UniProt ID: | P08684 | |
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Gene: | CYP3A4 | |
Actions: | substrate | |
References: |
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UniProt ID: | P10635 | |
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Gene: | CYP2D6 | |
Actions: | substrate | |
References: |
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