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

Stem definition	Drug id	CAS RN
diuretics, chlorothiazide derivatives	854	364-98-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: diazoxide dizoxide hyperstat hypertonalum proglicem	A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group. Molecular weight: 230.67 Formula: C8H7ClN2O2S CLOGP: 1.20 LIPINSKI: 0 HAC: 4 HDO: 1 TPSA: 58.53 ALOGS: -2.68 ROTB: 0 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

diazoxide
dizoxide
hyperstat
hypertonalum
proglicem

A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group.

Molecular weight: 230.67
Formula: C8H7ClN2O2S
CLOGP: 1.20
LIPINSKI: 0
HAC: 4
HDO: 1
TPSA: 58.53
ALOGS: -2.68
ROTB: 0

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.30	g	P

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	90 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	48 hours	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	35 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	34.68 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
Vd (Volume of distribution)	0.21 L/kg	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.07 mg/mL	Bocci G, Oprea TI, Benet LZ
CL (Clearance)	0.06 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.06 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Jan. 22, 1973	FDA

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
Hyperglycaemic hyperosmolar nonketotic syndrome	62.77	41.92	10	439	979	63487594
Hypoglycaemia	50.21	41.92	18	431	60047	63428526
Insulinoma	49.15	41.92	6	443	81	63488492

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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	59.99	56.52	22	336	54618	34901955

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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	81.59	37.91	30	570	101564	79642224
Insulinoma	73.08	37.91	9	591	123	79743665
Hyperglycaemic hyperosmolar nonketotic syndrome	53.68	37.91	10	590	2293	79741495

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C02DA01	CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ARTERIOLAR SMOOTH MUSCLE, AGENTS ACTING ON Thiazide derivatives
ATC	V03AH01	VARIOUS ALL OTHER THERAPEUTIC PRODUCTS ALL OTHER THERAPEUTIC PRODUCTS Drugs for treatment of hypoglycemia
CHEBI has role	CHEBI:35498	diuretics
CHEBI has role	CHEBI:35522	beta-adrenergic agonists
CHEBI has role	CHEBI:35523	bronchodilator
CHEBI has role	CHEBI:35524	sympathomimetic
CHEBI has role	CHEBI:35620	vasodilator agents
CHEBI has role	CHEBI:35674	antihypertensive drugs
CHEBI has role	CHEBI:38147	cardiotonic drugs
CHEBI has role	CHEBI:38633	sodium channel blockers

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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
Islet cell hyperplasia	indication	42681006	DOID:13317
Hyperinsulinism	indication	83469008	DOID:2018
Insulinoma	indication	302822000	DOID:3892
Hypertensive urgency	indication	443482000
Hypertensive Emergencies	indication
Hypertensive Emergency associated with Pregnancy	off-label use
Hyperkalemia	contraindication	14140009
Orthostatic hypotension	contraindication	28651003
Hyperuricemia	contraindication	35885006	DOID:1920
Hypokalemia	contraindication	43339004

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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	8.8	acidic
pKa2	5.51	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
Sulfonylurea receptor 1, Kir6.2	Ion channel	Q09428 Q14654	ABCC8_HUMAN KCJ11_HUMAN	OPENER	EC50	4.63	CHEMBL	CHEMBL
Nicotinamide phosphoribosyltransferase	Enzyme	P43490	NAMPT_HUMAN		Kd	3.64	CHEMBL
ATP-sensitive inward rectifier potassium channel 11	Ion channel		KCJ11_MOUSE	ACTIVATOR	EC50	4.20	IUPHAR

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External reference:

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ID	Source
000636	NDDF
1294	INN_ID
2004	MMSL
202594	RXNORM
20J	PDB_CHEM_ID
2409	IUPHAR_LIGAND_ID
3019	PUBCHEM_CID
387328001	SNOMEDCT_US
4018795	VUID
4018795	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Diazoxide	Human Prescription Drug Label	1	0254-1010	SUSPENSION	50 mg	ORAL	ANDA	22 sections
Diazoxide	Human Prescription Drug Label	1	0254-1010	SUSPENSION	50 mg	ORAL	ANDA	22 sections
Diazoxide	HUMAN PRESCRIPTION DRUG LABEL	1	13517-100	SUSPENSION	50 mg	ORAL	ANDA	24 sections
Diazoxide	HUMAN PRESCRIPTION DRUG LABEL	1	13517-100	SUSPENSION	50 mg	ORAL	ANDA	24 sections
Diazoxide Oral Solution	HUMAN PRESCRIPTION DRUG LABEL	1	80432-057	SUSPENSION	50 mg	ORAL	ANDA	20 sections
Proglycem	HUMAN PRESCRIPTION DRUG LABEL	1	0575-6200	SUSPENSION	50 mg	ORAL	NDA	23 sections
Proglycem	HUMAN PRESCRIPTION DRUG LABEL	1	0575-6200	SUSPENSION	50 mg	ORAL	NDA	23 sections
Proglycem	HUMAN PRESCRIPTION DRUG LABEL	1	0575-6200	SUSPENSION	50 mg	ORAL	NDA	23 sections

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