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Galantamine hydrobromide

Galantamine hydrobromide structure

CAS No:
1953-04-4
Formula:
C17H21NO3.BrH
Chemical Name:
Galantamine hydrobromide
Synonyms:
6H-Benzofuro[3a,3,2-ef][2]benzazepin-6-ol,4a,5,9,10,11,12-hexahydro-3-methoxy-11-methyl-,hydrobromide (1:1),(4aS,6R,8aS)-;Galanthamine,hydrobromide;6H-Benzofuro[3a,3,2-ef][2]benzazepin-6-ol,4a,5,9,10,11,12-hexahydro-3-methoxy-11-methyl-,hydrobromide,(4aS,6R,8aS)-;Galantamine hydrobromide;Nivalin;Nivaline;Galanthamine hydrogen bromide;Nivaline (pharmaceutical);(-)-Galanthamine hydrobromide;Reminyl;Jilkon hydrobromide;Lycoremine hydrobromide;(-)-Galantamine hydrobromide;Razadyne;Tamilin
Categories:
Active Pharmaceutical Ingredients > Nervous System Drugs

Description

Galantamine Hydrobromide is the hydrobromide salt form of galantamine, a tertiary alkaloid obtained synthetically or naturally from the bulbs and flowers of Narcissus and several other genera of the Amaryllidaceae family with anticholinesterase and neurocognitive-enhancing activities. Galantamine competitively and reversibly inhibits acetylcholinesterase, thereby increasing the concentration and enhancing the action of acetylcholine (Ach). In addition, galantamine is a ligand for nicotinic acetylcholine receptors, which may increase the presynaptic release of Ach and activate postsynaptic receptors. This agent may improve neurocognitive function in mild and moderate Alzheimer' s disease and may reduce abstinence-induced cognitive symptoms that promote smoking relapse.|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.

Galantamine hydrobromide Basic Attributes

Molecular Weight：

368.27

Exact Mass：

367.078

EC Number：

217-780-5

UNII：

MJ4PTD2VVW

DSSTox ID：

DTXSID4052768

NCI Thesaurus Code：

C47546

Characteristics

PSA：

41.9

XLogP3：

2.74630

Appearance：

White to Off-White Powder

Melting Point：

255-256 °C @ Solvent: Ethanol, 85%

Refractive Index：

-95 ° (C=1.4, H2O)

Water Solubility：

soluble in water or DMSO;Fairly soluble in hot water; freely soluble in alcohol, acetone, chloroform. Less sol in benzene, ether.

Storage Conditions：

−20°C

Vapor Pressure：

0mmHg at 25°C

Specific rotation：

D20 -93.1° (c = 0.1015 in 15 ml H2O)

Collision Cross Section：

166.7 Å² [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

Safety Information

Hazard category：

6.1

Transport codes：

UN 2811 6.1/PG 3

wgk germany：

hazard class code：

safety instructions：

45-36/37/39-22

RTECS Number：

DF8075000

Marks：

Precautionary statement(s)：

P264, P270, P280, P301+P310, P302+P352, P321, P330, P332+P313, P362, P405, P501

Hazard Statements：

H301

GHS Classification：

|Danger|H301 (99.53%): Toxic if swallowed [Danger Acute toxicity, oral]|P264, P270, P301+P310, P321, P330, P405, and P501|Aggregated GHS information provided by 212 companies from 10 notifications to the ECHA C&L Inventory.

Drug Information

MeSH：

Drugs used to specifically facilitate learning or memory, particularly to prevent the cognitive deficits associated with dementias. These drugs act by a variety of mechanisms. (See all compounds classified as Nootropic Agents.)|Drugs that mimic the effects of parasympathetic nervous system activity. Included here are drugs that directly stimulate muscarinic receptors and drugs that potentiate cholinergic activity, usually by slowing the breakdown of acetylcholine (CHOLINESTERASE INHIBITORS). Drugs that stimulate both sympathetic and parasympathetic postganglionic neurons (GANGLIONIC STIMULANTS) are not included here. (See all compounds classified as Parasympathomimetics.)|Drugs that inhibit cholinesterases. The neurotransmitter ACETYLCHOLINE is rapidly hydrolyzed, and thereby inactivated, by cholinesterases. When cholinesterases are inhibited, the action of endogenously released acetylcholine at cholinergic synapses is potentiated. Cholinesterase inhibitors are widely used clinically for their potentiation of cholinergic inputs to the gastrointestinal tract and urinary bladder, the eye, and skeletal muscles; they are also used for their effects on the heart and the central nervous system. (See all compounds classified as Cholinesterase Inhibitors.)

MeSH Entry Terms：

Galantamin

Galantamine hydrobromide Use and Manufacturing

Uses

anticholinesterase, analgesic, antiAlzheimer

Use Classification：

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:368.3
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:4
Rotatable Bond Count:1
Exact Mass:367.07831
Monoisotopic Mass:367.07831
Topological Polar Surface Area:41.9
Heavy Atom Count:22
Complexity:440
Defined Atom Stereocenter Count:3
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

This product is a cholinesterase inhibitor that can pass through the blood-brain barrier. Pharmacological efficacy tests have shown that this product has a promoting effect on the passive avoidance operation acquisition of mice, and has a significant improvement on the memory consolidation disorder caused by scopolamine and sodium nitrite; it has a good promoting effect on the learning and memory reproduction of the light and dark discrimination operation of rats.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Galantamine Hydrobromide Tablets
Ingredients	Galantamine hydrobromide.
Indication	1. This product has the potential to weaken the therapeutic effect of anticholinergic drugs. 2. It has a synergistic effect when used in combination with cholinergic agents and other cholinesterase inhibitors. 3. This product can improve its bioavailability when used in combination with cimetidine and ketoconazole. 4. It can reduce the efficacy of this product when used in combination with erythromycin. 5. It has been reported that atrioventricular conduction block may occur when this product is used in combination with digoxin.
Specifications	8mg (calculated as galantamine)

Galantamine Hydrobromide Injection
Ingredients	The main ingredient of this product is galanthamine hydrobromide. Its chemical name is 11-methyl-3-methoxy-4?,5,9,10,11,12-hexahydro-6H-benzofuran[3?,2-ef][2]benzazepin-6-ol hydrobromide.
Indication	Not yet clear
Specifications	1ml:5mg
Manufacturer	Shanghai Xudong Haipu Pharmaceutical Co., Ltd.

Galantamine Hydrobromide
Manufacturer	Shanghai Xudong Haipu Pharmaceutical Co., Ltd.

See More Related Drugs

Registered Holders

JUBILANT PHARMOVA LTD

United States
Active
SCINOPHARM TAIWAN, LTD.

Taiwan, China
Active
Sanochemia Pharmazeutika AG

Austria
Active

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