Galantamine

Galantamine
Clinical data


Trade names	Razadyne
AHFS/Drugs.com	Monograph
MedlinePlus	a699058
Pregnancy category	B
Routes of administration	Oral
ATC code	N06DA04 (WHO)
Legal status
Legal status	In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability	80 to 100%
Protein binding	18%
Metabolism	Hepatic partially :CYP2D6/3A4 substrate
Biological half-life	7 hours
Excretion	Renal (95%, of which 32% unchanged), fecal (5%)
Identifiers
IUPAC name (4aS,6R,8aS)-5,6,9,10,11,12-Hexahydro-3-methoxy-11-methyl-4aH-[1]benzofuro[3a,3,2-ef][2]benzazepin-6-ol
CAS Number	357-70-0^Y
PubChem CID	9651
IUPHAR/BPS	6693
DrugBank	DB00674^Y
ChemSpider	9272^Y
UNII	0D3Q044KCA
KEGG	D04292^Y
ChEBI	CHEBI:42944^Y
ChEMBL	CHEMBL659^Y
PDB ligand	GNT (PDBe, RCSB PDB)
ECHA InfoCard	100.118.289
Chemical and physical data
Formula	C₁₇H₂₁NO₃
Molar mass	287.354 g/mol
3D model (Jmol)	Interactive image
Melting point	126.5 °C (259.7 °F)
SMILES O(c2c1O[C@H]4C[C@@H](O)/C=C\[C@@]43c1c(cc2)CN(C)CC3)C
InChI InChI=1S/C17H21NO3/c1-18-8-7-17-6-5-12(19)9-14(17)21-16-13(20-2)4-3-11(10-18)15(16)17/h3-6,12,14,19H,7-10H2,1-2H3/t12-,14-,17-/m0/s1^Y Key:ASUTZQLVASHGKV-JDFRZJQESA-N^Y

Galantamine
Uses
treatment of dementia caused by Alzheimer's disease
Who might take
adults who have mid-to-moderate Alzheimer's disease as indicated by the Mini–mental state examination
Precautions
give fluids - drug can cause dehydration, diarrhea, or vomiting watch for Slow heart rate and fainting can cause bladder blockage can cause seizures can cause bleeding in stomach or intestines do not combine with other sleep aid medications do not combine alcohol use with this drug people with Chronic obstructive pulmonary disease should be cautious people with sleep apnea should be cautious
Other options
donepezil and rivastigmine are comparable drugs behavioral, physical, or social therapy may be useful

Galantamine (Nivalin, Razadyne, Razadyne ER, Reminyl, Lycoremine) is used for the treatment of mild to moderate Alzheimer's disease and various other memory impairments, in particular those of vascular origin. It is an alkaloid that is obtained synthetically or from the bulbs and flowers of Galanthus caucasicus (Caucasian snowdrop), Galanthus woronowii (Voronov's snowdrop), and some other members of the family Amaryllidaceae such as Narcissus (daffodil), Leucojum aestivum (snowflake), and Lycoris including Lycoris radiata (red spider lily).

Studies of usage in modern medicine began in the Soviet Union in the 1950s. The active ingredient was extracted, identified, and studied, in particular in relation to its acetylcholinesterase (AChE)-inhibiting properties. The bulk of the work was carried out by Soviet pharmacologists M. D. Mashkovsky and R. P. Kruglikova–Lvova, beginning in 1951. The work of Mashkovsky and Kruglikova-Lvova was the first published work that demonstrated the AChE-inhibiting properties of galantamine.

The first industrial process was developed in Bulgaria by prof. Paskov in 1959 (Nivalin, Sopharma) from a species traditionally used as a popular medicine in Eastern Europe, and, thus, the idea for developing a medicine from these species seems to be based on the local use (i.e., an ethnobotany-driven drug discovery).

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Wikipedia