GALANTAMINE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C17H21NO3
Molecular Weight	287.3535
Optical Activity	( - )
Defined Stereocenters	3 / 3
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

[H][C@]12C[C@@H](O)C=C[C@]13CCN(C)CC4=CC=C(OC)C(O2)=C34

InChI

InChIKey=ASUTZQLVASHGKV-JDFRZJQESA-N

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

HIDE SMILES / InChI

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 207 Target ID: CHEMBL220 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021169s031-021224s029-021615s022lbl.pdf	Inhibitor 8297		0.35 µM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Alzheimer’s disease 272 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021169s031-021224s029-021615s022lbl.pdf	Palliative		Approved 8429	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 n = 1 Health Status: unhealthy Condition: Alzheimer's disease Age Group: 90 years Sex: M Population Size: 1 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 n = 429 Health Status: unhealthy Condition: Alzheimer's disease Age Group: adult Sex: unknown Population Size: 429 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 n = 1 Health Status: unhealthy Condition: Alzheimer's disease Age Group: 90 years Sex: M Population Size: 1 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 n = 429 Health Status: unhealthy Condition: Alzheimer's disease Age Group: adult Sex: unknown Population Size: 429 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 n = 429 Health Status: unhealthy Condition: Alzheimer's disease Age Group: adult Sex: unknown Population Size: 429 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 n = 429 Health Status: unhealthy Condition: Alzheimer's disease Age Group: adult Sex: unknown Population Size: 429 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 n = 429 Health Status: unhealthy Condition: Alzheimer's disease Age Group: adult Sex: unknown Population Size: 429 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 n = 429 Health Status: unhealthy Condition: Alzheimer's disease Age Group: adult Sex: unknown Population Size: 429 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 n = 429 Health Status: unhealthy Condition: Alzheimer's disease Age Group: adult Sex: unknown Population Size: 429 Sources: https://pubmed.ncbi.nlm.nih.gov/18088197/

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1737 inhibitor 1587	inhibitor 1767	substrate 1217 inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1524 CYP2A6 707 CYP4A 19 CYP2C 19 CYP2C19 1478 CYP2E1 882 P-gp 1461 Kv1.5 26 BSEP 402 MRP2 383 MRP3 157 MRP4 204 ALDH1 40	UGT1A1 418

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
ALDH1 40	inhibitor 3277 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNTc3IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDY1OSJ9fQ%3D%3D	inconclusive [Activation 15.8489 uM]
CYP1A2 1692	inhibitor 3277 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 739	inhibitor 3277 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 1553	inhibitor 3277 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNjIyIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDY1OSJ9fQ%3D%3D	no [IC50 >10 uM]
CYP2C9 1819	inhibitor 3277 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzMzk3IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDY1OSJ9fQ%3D%3D	no [IC50 >10 uM]
CYP2E1 970	inhibitor 3277 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 1925	inhibitor 3277 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 403	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/23956101/	no [IC50 >133 uM]
MRP2 475	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/23956101/	no [IC50 >133 uM]
MRP3 207	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/23956101/	no [IC50 >133 uM]
MRP4 238	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/23956101/	no [IC50 >133 uM]
CYP2D6 1891	inhibitor 3277 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 33	inhibitor 3277 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 41	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/15530663/	no
CYP2C 34	inhibitor 3277 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 1650	inhibitor 3277 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 1217	substrate 3367 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 1737	substrate 3367 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 418	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/32520597/	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1647	inhibitor 1626 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
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
Aaron Chemicals	AR0039H4	http://www.aaronchem.com/357-70-0
Achemtek	0104-018749	http://www.achemtek.com/357-70-0
Acorn PharmaTech	ACN-035451	http://www.acornpharmatech.com/
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	A3422	http://www.apexbt.com/furagin.html
ApexBio Technology	A1745	http://www.apexbt.com/galanthamine-hbr.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
CSNpharm	CSN19397	https://www.csnpharm.com/products/galanthamine.html
Chem Scene	CS-1217	http://www.chemscene.com/357-70-0.html
ChemFaces	CFN90743	http://www.chemfaces.com/natural/Galantamine-CFN90743.html
ChemMol	30107850	http://www.chemmol.com/chemmol/30107850.html
Chemenu	CM124392	http://www.chemenu.com/products/CM124392
Chemspace	CSSB00025726588	https://chem-space.com/CSSB00025726588
Clearsynth	CS-O-01567	http://www.clearsynth.com/en/CSO01567.html
DC Chemicals	DCJ-030	http://www.dcchemicals.com//product_show-Galanthamine.html
Lab Network	LN01094084	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01094084
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/
abcr GmbH	AB494689	http://www.abcr.com/shop/en/AB494689
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
mcule	MCULE-7156449246	https://mcule.com/MCULE-7156449246/
mcule	MCULE-7226205054	https://mcule.com/MCULE-7226205054/

PubMed

Title	Date	PubMed
Galantamine: a review of its use in Alzheimer's disease.	2000 Nov	11129124
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
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
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
Screening for acetylcholinesterase inhibitors from Amaryllidaceae using silica gel thin-layer chromatography in combination with bioactivity staining.	2001 Apr 27	11358251
Maintaining cognitive function in Alzheimer disease: how effective are current treatments?	2001 Aug	11669506
Medications for the treatment of Alzheimer's disease.	2001 Aug	11515383
Current status and new developments with galantamine in the treatment of Alzheimer's disease.	2001 Dec	11825333
[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: effect on nicotinic receptor binding, acetylcholinesterase inhibition, and learning.	2001 Feb 13	11172080
Galantamine introduced in Europe.	2001 Jan-Feb	11416951
Use of cholinesterase inhibitors for treatment of Alzheimer disease.	2001 Jul	11453078
Use of biomimetic diversity-oriented synthesis to discover galanthamine-like molecules with biological properties beyond those of the natural product.	2001 Jul 11	11439080
Newest developments in dementia treatment and prevention.	2001 Jul-Aug	11505251
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
APOE genotype: no influence on galantamine treatment efficacy nor on rate of decline in Alzheimer's disease.	2001 Mar-Apr	11173877
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: a new alzheimer drug with a past life.	2001 Nov	11724094
Effects of a flexible galantamine dose in Alzheimer's disease: a randomised, controlled trial.	2001 Nov	11606667
Nicotinic receptor modulation: advantages for successful Alzheimer's disease therapy.	2002	12456064
Clinical pharmacokinetics and pharmacodynamics of cholinesterase inhibitors.	2002	12162759
Assessment of Health Economics in Alzheimer's Disease (AHEAD): treatment with galantamine in Sweden.	2002	12141890
Galantamine for Alzheimer's disease.	2002	12137632
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
Efficacy of galantamine in probable vascular dementia and Alzheimer's disease combined with cerebrovascular disease: a randomised trial.	2002 Apr 13	11965273
To what degree does cognitive impairment in Alzheimer's disease predict dependence of patients on caregivers?	2002 Aug 19	12184819
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
The efficacy of cholinesterase inhibitors in treating the behavioural symptoms of dementia.	2002 Jun	12139365
[Nicotinic Receptor, galantamine and Alzheimer disease].	2002 Jun 1-15	12134305
[Rivastigmine: a review of its clinical effectiveness].	2002 Nov 1-15	12436385
The impact of journal advertisements on prescribers of cholinesterase inhibitors.	2002 Oct	12325061
Galantamine provides broad benefits in patients with 'advanced moderate' Alzheimer's disease (MMSE < or = 12) for up to six months.	2002 Sep	12296613
Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block.	2002 Sep 16	12182861
Adjuvant galantamine administration improves negative symptoms in a patient with treatment-refractory schizophrenia.	2002 Sep-Oct	12410061
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.

Name

Type

Language

GALANTAMINE

Official Name

English

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

Common Name

English

GALANTAMINE [USAN]

Common Name

English

galantamine [INN]

Common Name

English

(-)-GALANTHAMINE

Common Name

English

Galantamine [WHO-DD]

Common Name

English

(4aS,6R,8aS)-4a,5,9,10,11,12-Hexahydro-3-methoxy-11-methyl-6H-benzofuro[3a,3,2-ef][2]benzazepin-6-ol

Common Name

English

GALANTAMINE [MI]

Common Name

English

GALANTHAMINE

Common Name

English

(-)-GALANTAMINE

Common Name

English

NSC-100058

Code

English

GALANTAMINE [VANDF]

Common Name

English

GALANTAMINE [HSDB]

Common Name

English

Classification Tree Code System Code

DSLD

4148 (Number of products:1)