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

Stem definitionDrug idCAS RN
diuretics, chlorothiazide derivatives 854 364-98-7

Description:

MoleculeDescription

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:

DoseUnitRoute
0.30 g P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.15 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 35 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 34.68 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 90 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.21 L/kg Lombardo F, Berellini G, Obach RS
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
t_half (Half-life) 48 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Jan. 22, 1973 FDA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Insulinoma 84.62 49.38 10 331 98 46685623
Hypoglycaemia 67.43 49.38 22 319 54327 46631394

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hypoglycaemia 67.74 56.30 23 255 50958 29901242

Pharmacologic Action:

SourceCodeDescription
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 receptor agonist
CHEBI has role CHEBI:35523 bronchodilator agents
CHEBI has role CHEBI:35524 sympathomimetic
CHEBI has role CHEBI:35620 vasodilator
CHEBI has role CHEBI:35674 antihypertensive
CHEBI has role CHEBI:38147 cardiotonic drugs
CHEBI has role CHEBI:38633 sodium channel blockers
CHEBI has role CHEBI:64338 atp-sensitive k+ channel opener
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D014665 Vasodilator Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
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
Body fluid retention contraindication 43498006
Decreased cardiac function contraindication 43650005
Uremia contraindication 44730006 DOID:4676
Chronic heart failure contraindication 48447003
Ketoacidosis contraindication 56051008
Cerebrovascular disease contraindication 62914000 DOID:6713
Diabetes mellitus contraindication 73211009 DOID:9351
Hyperglycemia contraindication 80394007 DOID:4195
Gout contraindication 90560007 DOID:13189
Kidney disease contraindication 90708001 DOID:557
Disease of liver contraindication 235856003 DOID:409
Edema contraindication 267038008
Chronic myocardial ischemia contraindication 413844008 DOID:3393
Hypertension due to Aortic Coarctation contraindication
Hypertension due to Arteriovenous Shunt contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Sulfonylurea receptor 1, Kir6.2 Ion channel OPENER EC50 4.63 CHEMBL CHEMBL
Nicotinamide phosphoribosyltransferase Enzyme Kd 3.64 CHEMBL
ATP-sensitive inward rectifier potassium channel 11 Unclassified ACTIVATOR EC50 4.20 IUPHAR

External reference:

IDSource
4018795 VUID
N0000147098 NUI
D00294 KEGG_DRUG
4018795 VANDF
C0012022 UMLSCUI
CHEBI:4495 CHEBI
20J PDB_CHEM_ID
CHEMBL181 ChEMBL_ID
DB01119 DRUGBANK_ID
D003981 MESH_DESCRIPTOR_UI
3019 PUBCHEM_CID
2409 IUPHAR_LIGAND_ID
1294 INN_ID
O5CB12L4FN UNII
202594 RXNORM
2004 MMSL
4574 MMSL
72399 MMSL
d00129 MMSL
000636 NDDF
387328001 SNOMEDCT_US
58905004 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Diazoxide Human Prescription Drug Label 1 0254-1010 SUSPENSION 50 mg ORAL ANDA 22 sections
Proglycem HUMAN PRESCRIPTION DRUG LABEL 1 0575-6200 SUSPENSION 50 mg ORAL NDA 23 sections
Diazoxide HUMAN PRESCRIPTION DRUG LABEL 1 13517-100 SUSPENSION 50 mg ORAL ANDA 24 sections