Benzgalantamine Gluconate

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C24H25NO4.C6H12O7
Molecular Weight	587.6149
Optical Activity	UNSPECIFIED
Defined Stereocenters	7 / 7
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O.COC1=CC=C2CN(C)CC[C@@]34C=C[C@@H](C[C@@H]3OC1=C24)OC(=O)C5=CC=CC=C5

InChI

InChIKey=YOMFDYFCNHSIAU-MXJKWOHVSA-N

InChI=1S/C24H25NO4.C6H12O7/c1-25-13-12-24-11-10-18(28-23(26)16-6-4-3-5-7-16)14-20(24)29-22-19(27-2)9-8-17(15-25)21(22)24;7-1-2(8)3(9)4(10)5(11)6(12)13/h3-11,18,20H,12-15H2,1-2H3;2-5,7-11H,1H2,(H,12,13)/t18-,20-,24-;2-,3-,4+,5-/m01/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 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
Galantamine for Alzheimer's disease.	2001	11687119
Pharmacokinetic profiles of current therapies for Alzheimer's disease: implications for switching to galantamine.	2001	11396867
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
[Perspectives for drug treatment in Alzheimer's disease].	2001 Dec	11937989
Galantamine: new preparation. The fourth cholinesterase inhibitor for Alzheimer's disease.	2001 Dec	11824442
Unsafe prescription medication switching recommendations.	2001 Dec	11813938
[Alzheimer dementia. Comparison of the effectiveness of cholinesterase inhibitors and gingko].	2001 Dec 13	11824165
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
Featured CME topic: dementia. Medication update.	2001 Jul	11531174
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
Alzheimer's disease and related disorders.	2001 May	11349485
Effects of a flexible galantamine dose in Alzheimer's disease: a randomised, controlled trial.	2001 Nov	11606667
[New theory! Galantamine and nicotinic-cholinergic transmission].	2002	12162069
A non-cholinergic, trophic action of acetylcholinesterase on hippocampal neurones in vitro: molecular mechanisms.	2002	12031351
Unconventional ligands and modulators of nicotinic receptors.	2002 Dec	12436414
New drugs 2002, part 1.	2002 Jan	12352750
A rapid TLC bioautographic method for the detection of acetylcholinesterase and butyrylcholinesterase inhibitors in plants.	2002 Jan-Feb	11899607
Switching cholinesterase inhibitors in patients with Alzheimer's disease.	2002 Jun	12139369
Evidence that the clinical effects of cholinesterase inhibitors are related to potency and targeting of action.	2002 Jun	12139368
The tolerability and safety of cholinesterase inhibitors in the treatment of dementia.	2002 Jun	12139367
The efficacy of cholinesterase inhibitors in treating the behavioural symptoms of dementia.	2002 Jun	12139365
[Rivastigmine: a review of its clinical effectiveness].	2002 Nov 1-15	12436385
[Treatment of Alzheimer's disease].	2002 Nov 1-15	12436384
Use of galantamine to treat vascular dementia.	2002 Nov 9	12433549
Acetylcholinesterase inhibitory activity of some Amaryllidaceae alkaloids and Narcissus extracts.	2002 Oct 11	12270757
The cholinergic approach for the treatment of vascular dementia: evidence from pre-clinical and clinical studies.	2002 Oct-Nov	12450245
Adjuvant galantamine administration improves negative symptoms in a patient with treatment-refractory schizophrenia.	2002 Sep-Oct	12410061

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

Benzgalantamine Gluconate

Official Name

English

ZUNVEYL

Preferred Name

English

MEMOGAIN GLUCONATE

Common Name

English

D-Gluconic acid, compd. with (4aS,6R,8aS)-4a,5,9,10,11,12-hexahydro-3-methoxy-11-methyl-6H-benzofuro[3a,3,2-ef][2]benzazepin-6-yl benzoate (1:1)

Systematic Name

English

Galantamine benzoate gluconate

Common Name

English

GLN-1062 GLUCONATE

Code

English

ALPHA-1062 gluconate

Code

English

GLUCONIC ACID SALT OF GALANTAMINE BENZOATE

Common Name

English

BENZGALANTAMINE GLUCONATE [USAN]

Common Name

English

Code System Code Type Description

PUBCHEM

155491118