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

Stem definition	Drug id	CAS RN
antihyperglycaemics	1301	29094-61-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: glypidizine glidiazinamide K 4024 K-4024 K4024 glipizide dipazide glibenese glipizid glucotrol glucozide glupizide glydiazinamide melizide napizide sucrazide	An oral hypoglycemic agent which is rapidly absorbed and completely metabolized. Molecular weight: 445.54 Formula: C21H27N5O4S CLOGP: 2.60 LIPINSKI: 0 HAC: 9 HDO: 3 TPSA: 130.15 ALOGS: -4.43 ROTB: 6 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

glypidizine
glidiazinamide
K 4024
K-4024
K4024
glipizide
dipazide
glibenese
glipizid
glucotrol
glucozide
glupizide
glydiazinamide
melizide
napizide
sucrazide

An oral hypoglycemic agent which is rapidly absorbed and completely metabolized.

Molecular weight: 445.54
Formula: C21H27N5O4S
CLOGP: 2.60
LIPINSKI: 0
HAC: 9
HDO: 3
TPSA: 130.15
ALOGS: -4.43
ROTB: 6

Status: OFP

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

Drug dosage:

Dose	Unit	Route
10	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	95 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
EoM (Fraction excreted unchanged in urine)	4.50 %	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	3.30 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.96 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
CL (Clearance)	0.56 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.16 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.02 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.01 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
May 8, 1984	FDA	PFIZER

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
Blood glucose increased	683.95	12.09	482	35613	83274	63369653
Hypoglycaemia	417.90	12.09	314	35781	59751	63393176
Cardiac failure congestive	326.25	12.09	328	35767	92105	63360822
Blood glucose decreased	288.85	12.09	168	35927	20784	63432143
Coronary artery disease	198.21	12.09	157	35938	32220	63420707
Myocardial infarction	197.50	12.09	263	35832	99630	63353297
Diabetes mellitus inadequate control	151.61	12.09	99	35996	15027	63437900
Product residue present	129.23	12.09	57	36038	3922	63449005
Cerebrovascular accident	122.48	12.09	220	35875	107804	63345123
Contraindicated product administered	109.78	12.09	3	36092	217645	63235282

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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
Hypoglycaemia	674.42	12.16	520	37152	54120	34865139
Blood glucose increased	528.47	12.16	492	37180	66226	34853033
Cardiac failure congestive	305.54	12.16	411	37261	82859	34836400
Myocardial infarction	270.79	12.16	475	37197	120610	34798649
Coronary artery disease	193.29	12.16	249	37423	48056	34871203
Blood glucose decreased	182.87	12.16	135	37537	13102	34906157
Completed suicide	141.71	12.16	321	37351	97847	34821412
Off label use	119.88	12.16	167	37505	419357	34499902
Glycosylated haemoglobin increased	92.02	12.16	85	37587	11275	34907984
Cerebrovascular accident	91.28	12.16	248	37424	84563	34834696

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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
Hypoglycaemia	1081.43	11.54	752	56338	100842	79586456
Blood glucose increased	824.40	11.54	672	56418	114303	79572995
Cardiac failure congestive	525.36	11.54	576	56514	141826	79545472
Myocardial infarction	476.97	11.54	622	56468	183507	79503791
Blood glucose decreased	360.36	11.54	228	56862	26006	79661292
Coronary artery disease	340.28	11.54	319	56771	65155	79622143
Cerebrovascular accident	205.06	11.54	385	56705	154907	79532391
Completed suicide	174.47	11.54	476	56614	245291	79442007
Off label use	157.46	11.54	255	56835	906960	78780338
Glycosylated haemoglobin increased	149.21	11.54	118	56972	19142	79668156

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FDA Adverse Event Reporting System (Pediatric)

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Pharmacologic Action:

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Source	Code	Description
ATC	A10BB07	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Sulfonylureas
CHEBI has role	CHEBI:35526	antidiabetic
CHEBI has role	CHEBI:77194	ATP:pantothenate 4-phosphotransferase inhibitor
CHEBI has role	CHEBI:90415	insulin secretagogues
FDA CS	M0020795	Sulfonylurea Compounds
FDA EPC	N0000175608	Sulfonylurea
MeSH PA	D007004	Hypoglycemic 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
Diabetes mellitus type 2	indication	44054006	DOID:9352
Alcoholism	contraindication	7200002
Asthenia	contraindication	13791008
Myocardial infarction	contraindication	22298006	DOID:5844
Acute vomiting	contraindication	23971007
Alcohol intoxication	contraindication	25702006
Shock	contraindication	27942005
Dehydration	contraindication	34095006
Infectious disease	contraindication	40733004
Hepatic porphyria	contraindication	55056006	DOID:3133

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🐶 Veterinary Drug Use

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🐶 Veterinary products

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Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	5.31	acidic
pKa2	11.71	acidic
pKa3	12.9	acidic
pKa4	3.19	Basic
pKa5	0.2	Basic

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Orange Book patent data (new drug applications)

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Orange Book exclusivity data (new drug applications)

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Sulfonylurea receptor 1, Kir6.2	Ion channel	Q09428 Q14654	ABCC8_HUMAN KCJ11_HUMAN	BLOCKER	Kd	9.10		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE

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External reference:

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ID	Source
000913	NDDF
151822	RXNORM
26124005	SNOMEDCT_US
3090	INN_ID
3478	PUBCHEM_CID
387143009	SNOMEDCT_US
4018508	VUID
4018508	VANDF
4783	MMSL
574	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Glipizide	HUMAN PRESCRIPTION DRUG LABEL	1	0378-1105	TABLET	5 mg	ORAL	ANDA	25 sections
Glipizide	HUMAN PRESCRIPTION DRUG LABEL	1	0378-1105	TABLET	5 mg	ORAL	ANDA	25 sections
Glipizide	HUMAN PRESCRIPTION DRUG LABEL	1	0378-1110	TABLET	10 mg	ORAL	ANDA	25 sections
Glipizide	HUMAN PRESCRIPTION DRUG LABEL	1	0378-1110	TABLET	10 mg	ORAL	ANDA	25 sections
Glipizide	HUMAN PRESCRIPTION DRUG LABEL	1	0591-0460	TABLET	5 mg	ORAL	ANDA	13 sections
Glipizide	HUMAN PRESCRIPTION DRUG LABEL	1	0591-0460	TABLET	5 mg	ORAL	ANDA	13 sections
Glipizide	HUMAN PRESCRIPTION DRUG LABEL	1	0591-0461	TABLET	10 mg	ORAL	ANDA	13 sections
Glipizide	HUMAN PRESCRIPTION DRUG LABEL	1	0591-0461	TABLET	10 mg	ORAL	ANDA	13 sections
Glipizide	HUMAN PRESCRIPTION DRUG LABEL	1	0615-7968	TABLET	5 mg	ORAL	ANDA	20 sections
Glipizide	HUMAN PRESCRIPTION DRUG LABEL	1	0615-7969	TABLET	10 mg	ORAL	ANDA	20 sections

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