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galantamine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	1272	357-70-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: galantamine galantamin galantamina lycoremin lycoremine galanthamine (-)-Galantamine (-)-Galanthamine galantamine hydrobromide galanthamine hydrobromide	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. Molecular weight: 287.36 Formula: C17H21NO3 CLOGP: 1.02 LIPINSKI: 0 HAC: 4 HDO: 1 TPSA: 41.93 ALOGS: -2.23 ROTB: 1 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

galantamine
galantamin
galantamina
lycoremin
lycoremine
galanthamine
(-)-Galantamine
(-)-Galanthamine
galantamine hydrobromide
galanthamine hydrobromide

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.

Molecular weight: 287.36
Formula: C17H21NO3
CLOGP: 1.02
LIPINSKI: 0
HAC: 4
HDO: 1
TPSA: 41.93
ALOGS: -2.23
ROTB: 1

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
16	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	99 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
CL (Clearance)	5.60 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	5.30 hours	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	20 %	Benet LZ, Broccatelli F, Oprea TI
Vd (Volume of distribution)	2.30 L/kg	Lombardo F, Berellini G, Obach RS
S (Water solubility)	10 mg/mL	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.45 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.83 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Feb. 28, 2001	FDA	JANSSEN PHARMS

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Orthostatic hypotension	1340.60	42.78	390	7999	35770	63444863
Sedation complication	1330.66	42.78	318	8071	13504	63467129
Creatinine renal clearance decreased	1323.80	42.78	327	8062	15981	63464652
Sedation	1252.33	42.78	376	8013	38433	63442200
Cognitive disorder	1193.89	42.78	395	7994	55420	63425213
Blood calcium decreased	1157.79	42.78	325	8064	26126	63454507
Balance disorder	1019.62	42.78	391	7998	84031	63396602
Depressed level of consciousness	937.43	42.78	339	8050	61739	63418894
Mobility decreased	672.20	42.78	324	8065	120835	63359798
Constipation	662.05	42.78	394	7995	224549	63256084

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Fall	63.39	25.03	84	3051	202801	34750995
Dysphagia	36.77	25.03	36	3099	62345	34891451
Aggression	35.97	25.03	29	3106	38935	34914861
Post-traumatic stress disorder	35.14	25.03	11	3124	1870	34951926
Compartment syndrome	33.79	25.03	12	3123	3006	34950790
Fracture	33.58	25.03	15	3120	6834	34946962
Agitation	31.73	25.03	32	3103	57367	34896429
Hallucination	30.86	25.03	30	3105	51468	34902328
Increased bronchial secretion	26.97	25.03	9	3126	1872	34951924
Loss of consciousness	25.31	25.03	34	3101	82633	34871163

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Sedation complication	1367.90	32.72	334	10307	15335	79718412
Creatinine renal clearance decreased	1318.66	32.72	337	10304	18665	79715082
Orthostatic hypotension	1193.72	32.72	397	10244	55767	79677980
Sedation	1171.66	32.72	384	10257	51511	79682236
Cognitive disorder	1150.30	32.72	408	10233	69518	79664229
Blood calcium decreased	1137.78	32.72	335	10306	31484	79702263
Balance disorder	978.19	32.72	398	10243	98459	79635288
Depressed level of consciousness	870.58	32.72	364	10277	96288	79637459
Mobility decreased	701.82	32.72	336	10305	121839	79611908
Fall	680.77	32.72	541	10100	487088	79246659

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N06DA04	NERVOUS SYSTEM PSYCHOANALEPTICS ANTI-DEMENTIA DRUGS Anticholinesterases
CHEBI has role	CHEBI:37733	EC 3.1.1.8 inhibitor
CHEBI has role	CHEBI:38323	cholinergic drugs
CHEBI has role	CHEBI:38462	acetylcholinesterase inhibitors
CHEBI has role	CHEBI:74530	curare poisoning antidote
CHEBI has role	CHEBI:76924	plant metabolites
FDA EPC	N0000175723	Cholinesterase Inhibitor
FDA MoA	N0000000177	Cholinesterase Inhibitors
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D018678	Cholinergic Agents

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Alzheimer's disease	indication	26929004	DOID:10652
Diffuse Lewy body disease	off-label use	80098002
Moderate to Severe Alzheimer's Type Dementia	off-label use
Peptic ulcer	contraindication	13200003	DOID:750
Chronic obstructive lung disease	contraindication	13645005	DOID:3083
Gastrointestinal ulcer	contraindication	40845000
Bradycardia	contraindication	48867003
Duodenal ulcer disease	contraindication	51868009	DOID:1724
Acute nephropathy	contraindication	58574008
Hepatic failure	contraindication	59927004

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.14	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Acetylcholinesterase	Enzyme	P22303	ACES_HUMAN	INHIBITOR	Ki	7.21	CHEMBL	CHEMBL
Cholinesterase	Enzyme	P06276	CHLE_HUMAN		Ki	6.72	CHEMBL
Acetylcholinesterase	Enzyme		ACES_TORCA		IC50	6.44	CHEMBL
Acetylcholinesterase	Enzyme		ACES_MOUSE		IC50	5.60	CHEMBL
Butyrylcholinesterase; Protein Bche	Enzyme		Q9JKC1_RAT		IC50	5.23	CHEMBL
Acetylcholinesterase	Enzyme		ACES_RAT		IC50	6.27	CHEMBL
Acetylcholinesterase	Enzyme		ACES_ELEEL		Ki	6.37	CHEMBL
Acetylcholinesterase	Enzyme		ACES_BOVIN		IC50	5.06	CHEMBL
Butyrylcholinesterase	Enzyme		Q9N1N9_HORSE		Ki	5.10	CHEMBL
Cholinesterase	Enzyme		CHLE_HORSE		Ki	5.03	CHEMBL

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External reference:

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ID	Source
GNT	PDB_CHEM_ID
007026	NDDF
007027	NDDF
0D3Q044KCA	UNII
129482002	SNOMEDCT_US
1392	INN_ID
147848	MMSL
15913	MMSL
1953-04-4	SECONDARY_CAS_RN
323377002	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Galantamine	HUMAN PRESCRIPTION DRUG LABEL	1	0591-3496	CAPSULE, EXTENDED RELEASE	8 mg	ORAL	ANDA	25 sections
Galantamine	HUMAN PRESCRIPTION DRUG LABEL	1	0591-3496	CAPSULE, EXTENDED RELEASE	8 mg	ORAL	ANDA	25 sections
Galantamine	HUMAN PRESCRIPTION DRUG LABEL	1	0591-3497	CAPSULE, EXTENDED RELEASE	16 mg	ORAL	ANDA	25 sections
Galantamine	HUMAN PRESCRIPTION DRUG LABEL	1	0591-3497	CAPSULE, EXTENDED RELEASE	16 mg	ORAL	ANDA	25 sections
Galantamine	HUMAN PRESCRIPTION DRUG LABEL	1	0591-3498	CAPSULE, EXTENDED RELEASE	24 mg	ORAL	ANDA	25 sections
Galantamine	HUMAN PRESCRIPTION DRUG LABEL	1	0591-3498	CAPSULE, EXTENDED RELEASE	24 mg	ORAL	ANDA	25 sections
Galantamine	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7104	TABLET, FILM COATED	4 mg	ORAL	ANDA	26 sections
Galantamine Hydrobromide	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0137	SOLUTION	4 mg	ORAL	ANDA	25 sections
Galantamine Hydrobromide	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0137	SOLUTION	4 mg	ORAL	ANDA	25 sections
galantamine hydrobromide	HUMAN PRESCRIPTION DRUG LABEL	1	10147-0881	TABLET, FILM COATED	4 mg	ORAL	NDA	28 sections

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