GALANTAMINE HYDROCHLORIDE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C17H21NO3.ClH
Molecular Weight	323.814
Optical Activity	( - )
Defined Stereocenters	3 / 3
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

Cl.COC1=C2O[C@H]3C[C@@H](O)C=C[C@]34CCN(C)CC(C=C1)=C24

InChI

InChIKey=USUHXXKCHSBMOS-XPSHAMGMSA-N

InChI=1S/C17H21NO3.ClH/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;1H/t12-,14-,17-;/m0./s1

HIDE SMILES / InChI

Molecular Formula	ClH
Molecular Weight	36.461
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	C17H21NO3
Molecular Weight	287.3535
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	3 / 3
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021169s031-021224s029-021615s022lbl.pdf
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/mesh/68005702 | https://www.ncbi.nlm.nih.gov/pubmed/12177686

Galantamine (RAZADYNE®, galantamine hydrobromide) is a benzazepine derived from norbelladine. It is found in Galanthus and other Amaryllidaceae. It is a reversible, competitive acetylcholinesterase inhibitor that is used for the treatment of mild to moderate dementia of the Alzheimer’s type. Although the etiology of cognitive impairment in Alzheimer’s disease is not fully understood, it has been reported that acetylcholine-producing neurons degenerate in the brains of patients with Alzheimer’s disease. The degree of this cholinergic loss has been correlated with degree of cognitive impairment and density of amyloid plaques (a neuropathological hallmark of Alzheimer’s disease). While the precise mechanism of galantamine’s (RAZADYNE®, galantamine hydrobromide) action is unknown, it 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 mechanism is correct, galantamine’s (RAZADYNE®, galantamine hydrobromide) effect may lessen as the disease process advances and fewer cholinergic neurons remain functionally intact. There is no evidence that galantamine (RAZADYNE®, galantamine hydrobromide) alters the course of the underlying dementing process.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Acetylcholinesterase 209 Target ID: CHEMBL220 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021169s031-021224s029-021615s022lbl.pdf	Inhibitor 8504		0.35 µM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Alzheimer’s disease 278 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021169s031-021224s029-021615s022lbl.pdf	Palliative		Approved 8583	RAZADYNE Approved Use Galantamine hydrobromide is a cholinesterase inhibitor indicated for the treatment of mild to moderate dementia of the Alzheimer’s type. Launch Date 2001

C_max

Value	Dose	Co-administered	Analyte	Population
84.3 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16238894	24 mg single, oral dose: 24 mg route of administration: Oral experiment type: SINGLE co-administered:		GALANTAMINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

AUC

Value	Dose	Co-administered	Analyte	Population
1050 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16238894	24 mg single, oral dose: 24 mg route of administration: Oral experiment type: SINGLE co-administered:		GALANTAMINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

T_1/2

Value	Dose	Co-administered	Analyte	Population
8.53 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16238894	24 mg single, oral dose: 24 mg route of administration: Oral experiment type: SINGLE co-administered:		GALANTAMINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
82% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021615s021lbl.pdf			GALANTAMINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
8 mg 2 times / day steady, oral Dose: 8 mg, 2 times / day Route: oral Route: steady Dose: 8 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/23552705/	unhealthy, 90 years Health Status: unhealthy Age Group: 90 years Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/23552705/	Disc. AE: Nightmares... AEs leading to discontinuation/dose reduction: Nightmares (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/23552705/
32 mg 1 times / day steady, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: steady Dose: 32 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18088197/	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://pubmed.ncbi.nlm.nih.gov/18088197/	Other AEs: Nausea, Vomiting... Other AEs: Nausea (42%) Vomiting (21%) Diarrhea (16%) Anorexia (15%) Weight loss (8%) Dizziness (15%) Sources: https://pubmed.ncbi.nlm.nih.gov/18088197/

AEs

AE	Significance	Dose	Population
Nightmares	1 patient Disc. AE	8 mg 2 times / day steady, oral Dose: 8 mg, 2 times / day Route: oral Route: steady Dose: 8 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/23552705/	unhealthy, 90 years Health Status: unhealthy Age Group: 90 years Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/23552705/
Anorexia	15%	32 mg 1 times / day steady, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: steady Dose: 32 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18088197/	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://pubmed.ncbi.nlm.nih.gov/18088197/
Dizziness	15%	32 mg 1 times / day steady, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: steady Dose: 32 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18088197/	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://pubmed.ncbi.nlm.nih.gov/18088197/
Diarrhea	16%	32 mg 1 times / day steady, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: steady Dose: 32 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18088197/	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://pubmed.ncbi.nlm.nih.gov/18088197/
Vomiting	21%	32 mg 1 times / day steady, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: steady Dose: 32 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18088197/	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://pubmed.ncbi.nlm.nih.gov/18088197/
Nausea	42%	32 mg 1 times / day steady, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: steady Dose: 32 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18088197/	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://pubmed.ncbi.nlm.nih.gov/18088197/
Weight loss	8%	32 mg 1 times / day steady, oral Highest studied dose Dose: 32 mg, 1 times / day Route: oral Route: steady Dose: 32 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18088197/	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://pubmed.ncbi.nlm.nih.gov/18088197/

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946 inhibitor 2252	inhibitor 2438	substrate 1388 inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 2153 CYP2A6 879 CYP4A 20 CYP2C 20 CYP2C19 2057 CYP2E1 1060 P-gp 1741 Kv1.5 27 BSEP 550 MRP2 499 MRP3 246 MRP4 290 ALDH1 41	UGT1A1 479

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
ALDH1 41	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNTc3IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDY1OSJ9fQ%3D%3D	inconclusive [Activation 15.8489 uM]
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/21169lbl.pdf#page=4, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-169_Reminyl_biopharmr.pdf#page=34, https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNjIyIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDY1OSJ9fQ%3D%3D Page: 4, 20, (ClinPharm) 34	no [IC50 >10 uM]
CYP2A6 911	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/21169lbl.pdf#page=4, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-169_Reminyl_biopharmr.pdf#page=34, https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw1MjgyIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDY1OSJ9fQ%3D%3D Page: 4, 20, (ClinPharm) 34	no [IC50 >10 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNjIyIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDY1OSJ9fQ%3D%3D	no [IC50 >10 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzMzk3IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDY1OSJ9fQ%3D%3D	no [IC50 >10 uM]
CYP2E1 1146	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/21169lbl.pdf#page=4, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-169_Reminyl_biopharmr.pdf#page=34, https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw1MjgxIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDY1OSJ9fQ%3D%3D Page: 4, 20, (ClinPharm) 34	no [IC50 >10 uM]
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/21169lbl.pdf#page=4, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-169_Reminyl_biopharmr.pdf#page=34, https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNDAiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMNjU5In19 Page: 4, 20, (ClinPharm) 34	no [IC50 >10 uM]
BSEP 554	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/23956101/	no [IC50 >133 uM]
MRP2 625	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/23956101/	no [IC50 >133 uM]
MRP3 326	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/23956101/	no [IC50 >133 uM]
MRP4 345	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/23956101/	no [IC50 >133 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/21169lbl.pdf#page=4, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-169_Reminyl_biopharmr.pdf#page=34 Page: 4, 20, (ClinPharm) 34	no
CYP4A 34	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/21169lbl.pdf#page=4, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-169_Reminyl_biopharmr.pdf#page=34 Page: 4, 20, (ClinPharm) 34	no
Kv1.5 42	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/15530663/	no
CYP2C 37	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/21169lbl.pdf#page=4, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-169_Reminyl_biopharmr.pdf#page=34, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-169_Reminyl_biopharmr.pdf#page=38 Page: 4, 20, (ClinPharm) 34, 38-39	no	no (co-administration study) Comment: Coadministration of Galantamine (multiple doses) had no effect on the pharmacokinetics of R-/S-Warfarin (CYP2C9 substrate) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/21169lbl.pdf#page=4, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-169_Reminyl_biopharmr.pdf#page=34, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-169_Reminyl_biopharmr.pdf#page=38 Page: 4, 20, (ClinPharm) 34, 38-39
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/21169lbl.pdf#page=4, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-169_Reminyl_biopharmr.pdf#page=38, , https://pubmed.ncbi.nlm.nih.gov/19683513/ Page: 4, 20, (ClinPharm) 38, 40	yes [IC50 0.6 uM]	no (co-administration study) Comment: Coadministration of Galantamine (multiple doses) had no effect on the pharmacokinetics of Digoxin (P-gp substrate) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/21169lbl.pdf#page=4, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-169_Reminyl_biopharmr.pdf#page=38, , https://pubmed.ncbi.nlm.nih.gov/19683513/ Page: 4, 20, (ClinPharm) 38, 40

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP2D6 1388	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/21169lbl.pdf#page=2, https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/21169lbl.pdf#page=4, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-169_Reminyl_biopharmr.pdf#page=15, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-169_Reminyl_biopharmr.pdf#page=45, https://pubmed.ncbi.nlm.nih.gov/10634129/ Page: 2, 4, 19-20, (ClinPharm) 15, 38, 42-23, 45	major [Km 187 uM]	yes (co-administration study) Comment: Vmax = 5.2 nmol/mg protein/h (Pharmacogenetics, 9, 661 (1999)); Coadministration (multiple doses) of ketoconazole (strong CYP3A4 inhibitor, CYP2D6 inhibitor) and paroxetin (strong CYP2D6 inhibitor) increased Galantamine AUC by 30% and 40%. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/21169lbl.pdf#page=2, https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/21169lbl.pdf#page=4, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-169_Reminyl_biopharmr.pdf#page=15, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-169_Reminyl_biopharmr.pdf#page=45, https://pubmed.ncbi.nlm.nih.gov/10634129/ Page: 2, 4, 19-20, (ClinPharm) 15, 38, 42-23, 45
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/21169lbl.pdf#page=2, https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/21169lbl.pdf#page=4, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-169_Reminyl_biopharmr.pdf#page=15, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-169_Reminyl_biopharmr.pdf#page=38 Page: 2, 4, 19-20, (ClinPharm) 15, 38, 42-44	major	yes (co-administration study) Comment: Coadministration (multiple doses) of ketoconazole (strong CYP3A4 inhibitor, CYP2D6 inhibitor) increased Galantamine AUC by 30%. Coadministration of erythromycin (moderate CYP3A4 inhibitor) increased Galantamine AUC by only 10%. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/21169lbl.pdf#page=2, https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/21169lbl.pdf#page=4, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-169_Reminyl_biopharmr.pdf#page=15, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-169_Reminyl_biopharmr.pdf#page=38 Page: 2, 4, 19-20, (ClinPharm) 15, 38, 42-44
UGT1A1 479	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/32520597/	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.pmda.go.jp/drugs/2011/P201100024/80015500_23000AMX00426_A100_1.pdf, https://pubmed.ncbi.nlm.nih.gov/22366430/ Page: 17.0

Sourcing

Vendor/Aggregator	ID	URL
3B Scientific (Wuhan) Corp	3B2-5422	http://www.3bsc.com/index/pro_info.php?id=85224
AA Blocks	AA0038PC	https://www.aablocks.com/goods/Goods/detail?id=AA0038PC
Aaron Chemicals	AR0039H4	http://www.aaronchem.com/357-70-0
abcr GmbH	AB494689	http://www.abcr.com/shop/en/AB494689
Achemtek	0104-018749	http://www.achemtek.com/357-70-0
Acorn PharmaTech	ACN-035451	http://www.acornpharmatech.com/
AEchem Scientific Corp., USA	AE1-015932	http://www.aechemsc.com/info_products/AE1-015932.php
AHH Chemical co.,ltd	MT-52053	http://www.ahhchemical.com/product/MT-52053.html
AHH Chemical co.,ltd	NP-0540	http://www.ahhchemical.com/product/NP-0540.html
Ambeed	A697166	https://www.ambeed.com/products/357-70-0.html
Angene	AGN-PC-0RB8F4	http://www.angenechemical.com/productshow/AGN-PC-0RB8F4.html
ApexBio Technology	A1745	http://www.apexbt.com/galanthamine-hbr.html
ApexBio Technology	A3422	http://www.apexbt.com/furagin.html
ApexBio Technology	A3423	http://www.apexbt.com/galanthamine.html
Aurora Fine Chemicals LLC	K04.008.117	http://online.aurorafinechemicals.com/info?ID=K04.008.117
Aurum Pharmatech LLC	W-5162	http://www.Aurumpharmatech.com/Product/ProductDetails/W_5162
AvaChem Scientific	1543B	http://www.avachem.com/productSearch.asp?1543B
BLD Pharm	BD8903	http://www.bldpharm.com/products/357-70-0.html
Chem Scene	CS-1217	http://www.chemscene.com/357-70-0.html
Chemenu	CM124392	http://www.chemenu.com/products/CM124392
ChemFaces	CFN90743	http://www.chemfaces.com/natural/Galantamine-CFN90743.html
ChemMol	30107850	http://www.chemmol.com/chemmol/30107850.html
Chemspace	CSSB00025726588	https://chem-space.com/CSSB00025726588
Clearsynth	CS-O-01567	http://www.clearsynth.com/en/CSO01567.html
CSNpharm	CSN19397	https://www.csnpharm.com/products/galanthamine.html
DC Chemicals	DCJ-030	http://www.dcchemicals.com//product_show-Galanthamine.html
eNovation Chemicals	D582252	https://www.enovationchem.com/ProductDetails.asp?ProductID=D582252
eNovation Chemicals	Y1043960	https://www.enovationchem.com/ProductDetails.asp?ProductID=Y1043960
iChemical	EBD2184763	http://www.ichemical.com/products/357-70-0.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs
Lab Network	LN01094084	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01094084
mcule	MCULE-7156449246	https://mcule.com/MCULE-7156449246/
mcule	MCULE-7226205054	https://mcule.com/MCULE-7226205054/
MedChem Express	HY-76299	https://www.medchemexpress.com/Galanthamine.html
MuseChem	I003311	https://www.musechem.com/product/I003311.html
OChem	3076	http://www.ocheminc.com/index.php?act=psearch&pid=357G700
Parchem	29043	http://www.parchem.com/chemical-supplier-distributor/Galantamine-019043.aspx
Parchem	29044	http://www.parchem.com/chemical-supplier-distributor/Galantamine-Hydrobromide-019044.aspx
Parchem	29045	http://www.parchem.com/chemical-supplier-distributor/Galantamine-Hydrobromide-019045.aspx
Parchem	29046	http://www.parchem.com/chemical-supplier-distributor/Galanthamine-019046.aspx
Selleck Chemicals	S3866	http://www.selleckchem.com/products/galanthamine.html
Smolecule	S528644	http://www.smolecule.com/products/s528644
Smolecule	S748849	https://www.smolecule.com/products/s748849
THE BioTek	bt-268966	https://www.thebiotek.com/product/inhibitors/bt-268966
TripleBond	CG0028	http://www.triplebond-canada.com/prod/1357/

PubMed

Title	Date	PubMed
Accurate prediction of the bound conformation of galanthamine in the active site of Torpedo californica acetylcholinesterase using molecular docking.	2001	11449566
Pharmacokinetic rationale for switching from donepezil to galantamine.	2001	11396871
Therapeutic continuity in Alzheimer's disease: switching patients to galantamine. Panel discussion: recommendations for prescribers.	2001	11396870
Switching previous therapies for Alzheimer's disease to galantamine.	2001	11396869
Effects of washout and dose-escalation periods on the efficacy, safety, and tolerability of galantamine in patients previously treated with donepezil: ongoing clinical trials.	2001	11396868
Pharmacokinetic profiles of current therapies for Alzheimer's disease: implications for switching to galantamine.	2001	11396867
Therapeutic continuity in Alzheimer's disease: switching patients to galantamine. Introduction.	2001	11396866
Galantamine for Alzheimer's disease.	2001	11279727
Clinical and cost-effectiveness of donepezil, rivastigmine and galantamine for Alzheimer's disease: a rapid and systematic review.	2001	11262420
Cholinesterase inhibitors for Alzheimer's disease.	2001	11217870
Muscarinic agonists and antagonists in the treatment of Alzheimer's disease.	2001 Apr	11421251
FDA approves galantamine for Alzheimer's disease.	2001 Apr 15	11329755
Screening for acetylcholinesterase inhibitors from Amaryllidaceae using silica gel thin-layer chromatography in combination with bioactivity staining.	2001 Apr 27	11358251
Current status and new developments with galantamine in the treatment of Alzheimer's disease.	2001 Dec	11825333
Galantamine: new preparation. The fourth cholinesterase inhibitor for Alzheimer's disease.	2001 Dec	11824442
[Alzheimer dementia. Comparison of the effectiveness of cholinesterase inhibitors and gingko].	2001 Dec 13	11824165
Galantamine, a cholinesterase inhibitor that allosterically modulates nicotinic receptors: effects on the course of Alzheimer's disease.	2001 Feb 1	11230880
Allosteric sensitization of nicotinic receptors by galantamine, a new treatment strategy for Alzheimer's disease.	2001 Feb 1	11230879
Galantamine introduced in Europe.	2001 Jan-Feb	11416951
Use of biomimetic diversity-oriented synthesis to discover galanthamine-like molecules with biological properties beyond those of the natural product.	2001 Jul 11	11439080
Galantamine (reminyl) for Alzheimer's disease.	2001 Jun 25	11426189
Differential increase in cerebrospinal fluid-acetylcholinesterase after treatment with acetylcholinesterase inhibitors in patients with Alzheimer's disease.	2001 Mar 16	11226635
The pharmacological rationale for treating vascular dementia with galantamine (Reminyl).	2001 May	11406923
Meeting the challenges of vascular dementia. Introduction.	2001 May	11406921
Alzheimer's disease and related disorders.	2001 May	11349485
Galantamine hydrobromide.	2001 Nov 15	11760913
Nicotinic receptor modulation: advantages for successful Alzheimer's disease therapy.	2002	12456064
Galantamine: a pharmacoeconomic review of its use in Alzheimer's disease.	2002	12381243
Clinical pharmacokinetics and pharmacodynamics of cholinesterase inhibitors.	2002	12162759
[New theory! Galantamine and nicotinic-cholinergic transmission].	2002	12162069
Cholinergic medication for neuroleptic-induced tardive dyskinesia.	2002	12137608
Understanding and managing behavioural symptoms in Alzheimer's disease and related dementias: focus on rivastigmine.	2002	12094826
A non-cholinergic, trophic action of acetylcholinesterase on hippocampal neurones in vitro: molecular mechanisms.	2002	12031351
Efficacy of galantamine in probable vascular dementia and Alzheimer's disease combined with cerebrovascular disease: a randomised trial.	2002 Apr 13	11965273
Unconventional ligands and modulators of nicotinic receptors.	2002 Dec	12436414
Pd asymmetric allylic alkylation (AAA). A powerful synthetic tool.	2002 Jan	11824567
A rapid TLC bioautographic method for the detection of acetylcholinesterase and butyrylcholinesterase inhibitors in plants.	2002 Jan-Feb	11899607
Medical treatment of Alzheimer's disease: past, present, and future.	2002 Jul	12182092
Galantamine for treatment-resistant schizophrenia.	2002 Jul	12091212
[Nicotinic Receptor, galantamine and Alzheimer disease].	2002 Jun 1-15	12134305
[Latest therapies for treating dementia].	2002 May 15	12031225
[Dementing disorders. What benefits do the new anti-dementia drugs have?].	2002 May 6	12070846
[Rivastigmine: a review of its clinical effectiveness].	2002 Nov 1-15	12436385
[Treatment of Alzheimer's disease].	2002 Nov 1-15	12436384
Treatment options: the latest evidence with galantamine (Reminyl).	2002 Nov 15	12417370
Galantamine improved cognition and global functioning in vascular dementia or Alzheimer disease with cerebrovascular disease.	2002 Nov-Dec	12418842
The impact of journal advertisements on prescribers of cholinesterase inhibitors.	2002 Oct	12325061
The cholinergic approach for the treatment of vascular dementia: evidence from pre-clinical and clinical studies.	2002 Oct-Nov	12450245
Galantamine provides broad benefits in patients with 'advanced moderate' Alzheimer's disease (MMSE < or = 12) for up to six months.	2002 Sep	12296613
Galantamine--a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer's disease.	2002 Summer	12177686

Patents

Sample Use Guides

In Vivo Use Guide

The recommended starting dosage of RAZADYNE® tablets is 4 mg twice a day (8 mg/day). The dosage should be increased to the initial maintenance dosage of 8 mg twice a day (16 mg/day) after a minimum of 4 weeks. A further increase to 12 mg twice a day (24 mg/day) should be attempted after a minimum of 4 weeks at 8 mg twice a day (16 mg/day). Dosage increases should be based upon assessment of clinical benefit and tolerability of the previous dose.

Route of Administration: Oral

In Vitro Use Guide

Galanthamine was evaluated as inhibitor of human acetylcholinesterase activity from samples of postmortem human brain, fresh brain cortex biopsies and human erythrocytes. The respective galanthamine concentration exerting a half maximal effect (IC50) on acetylcholinesterase in postmortem human brain frontal cortex was 3.2 uM versus 2.8 uM in the hippocampus region. In addition, galanthamine was 10-fold less potent in inhibiting the enzyme activity from human brain that from human erythrocytes.

Substance Class	Chemical Created by `admin` on `Tue Apr 01 18:12:54 GMT 2025` Edited by `admin` on `Tue Apr 01 18:12:54 GMT 2025`
Record UNII	HV8VV786RM
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

(-)-GALANTHAMINE HYDROCHLORIDE

Preferred Name

English

GALANTAMINE HYDROCHLORIDE

Common Name

English

6H-BENZOFURO(3A,3,2-EF)(2)BENZAZEPIN-6-OL, 4A,5,9,10,11,12-HEXAHYDRO-3-METHOXY-11-METHYL-, HYDROCHLORIDE (1:1), (4AS,6R,8AS)-

Systematic Name

English

Galantamine hydrochloride [WHO-DD]

Common Name

English

6H-BENZOFURO(3A,3,2-EF)(2)BENZAZEPIN-6-OL, 4A,5,9,10,11,12-HEXAHYDRO-3-METHOXY-11-METHYL-, HYDROCHLORIDE, (4AS,6R,8AS)-

Systematic Name

English

GALANTAMINE HYDROCHLORIDE [MI]

Common Name

English

GALANTHAMINE, HYDROCHLORIDE

Common Name

English

Code System Code Type Description

PUBCHEM

11702557