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CAS No.1953-04-4
Chemical Name:Galantamine Hydrobromide
SynonymsNIVALIN;NIVALIN, HBR;GALANTAMINE HBR;GALANTHAMINE HBR;GALANTAMINE HYDROBROMIDE;GALANTHAMINE HYDROBROMIDE;GALANTHAMIDE HYDROBROMIDE;GALANTHAMINE HYDROBROMIDUM;(-)-Galanthaminium bromide;galantamine HBr 8% pellets
CBNumber:CB2439815
Molecular Formula:C17H22BrNO3
Formula Weight:368.27
Outline
Galantamine hydrobromide also called as 11-methyl-3-methoxy-4a, 5, 9, 10, 11, 12-hexahydro-6H-benzene and furan [3a, 3, 2-ef] [2] benzazepine-6-ol hydrobromide, is an alkaloid isolated from Lycoris plants. In the 1960 s, China had first successfully isolated it from domestic Medicago Lycoris and Lycoris radiata, and had recorded into the Chinese Pharmacopoeia in 1977. The hydrobromide salt is white crystalline powder and is odorless with bitter taste. It is soluble in water, slightly soluble in ethanol but insoluble in chloroform, acetone, and ether. The absorption coefficient (50 ug in 1Â ml of water): at 289nm wavelength, it has an absorption coefficient of 79.6~86.2. It is mainly applied to myasthenia gravis, poliomyelitis sequelae and resting stage as well as being used for the treatment of children with cerebral paralysis, polyneuritis, radiculitis and sensory motor disorders caused by nerve disorders or trauma. It is clinically also used for the treatment of Alzheimer's disease as well as treatment of dementia and memory disorders caused by the organic disease of the brain with significant therapeutic effect.Â
Galantamine is a kind of phenanthridine alkaloids discovered by the Soviet scholars 50 years ago. It is the inhibitor of the reversible cholinesterase (ChE) and can selectively inhibit the real cholinesterase (AChE). Galantamine belongs to the second generation of acetylcholinesterase inhibitor drugs with its pharmaceutical composition being same as the extracted alkaloids of the European Mountain narcissus bulb. This kind of herbal medicine has already had a history of 30 years of clinical application in some countries and regions for the treatment of reversal neuromuscular blockade, myasthenia gravis, and children with cerebral palsy psychosis.
Cholinesterase inhibitors
Galantamine hydrobromide is the hydrobromide salt of galantamine and is a cholinesterase inhibitor can be extracted from Amaryllidaceae Lycoris plant. The III-phase clinical trials in the United Kingdom in 1998 have showed that this drug had dual mechanism of action of both inhibiting acetylcholinesterase and regulating nicotinic receptors. Therefore, galantamine can improve the cognitive abilities of Alzheimer's patients and has been already applied as the drug of the treatment of mild to severe Alzheimer's disease (AD) drugs and has entered into market in EC countries. "Chinese Pharmacopoeia" has included the both the raw material and injection of galantamine hydrobromide. It is clinically mainly used for the treatment of poliomyelitis (polio) sequelae, muscular dystrophy and myasthenia gravis. It can be used to substitute neostigmine methyl-sulfate for antagonism of tubocurarine but with weak performance with the usage amount being ten times as high as the usage amount of neostigmine methyl-sulfate. Intravenous injection of 0.5 mg/kg of galantamine hydrobromide can quickly reverse the central anticholinergic effects caused through injection of scopolamine hydrobromide. It can also be used for treating children cerebral palsy, traumatic sensorimotor disorders, multiple neuritis and radiculitis.
Physical and Chemical Properties
It is white crystalline powder and is odorless with bitter taste. It is soluble in water, slightly soluble in ethanol and insoluble in acetone, chloroform, ether and benzene.
Uses
It can be used for the treatment of neurological diseases and trauma-induced movement disorders, multiple neuritis, and radiculitis.
Cholinesterase inhibitors can reverse the process of scopolamine-induced amnesia.
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