diazoxide indications/contra

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

Drug dosage:

DoseUnitRoute
0.30 g P

Approvals:

DateAgencyCompanyOrphan
Jan. 22, 1973 FDA

FDA Adverse Event Reporting System

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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 92.24 72.57 21 142 14297 3371399

Pharmacologic Action:

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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:35674 antihypertensive agent
CHEBI has role CHEBI:35524 sympathomimetic agent
CHEBI has role CHEBI:38147 cardiotonic drug
CHEBI has role CHEBI:35523 bronchodilator agent
CHEBI has role CHEBI:35522 beta-adrenergic agonist
CHEBI has role CHEBI:35498 diuretic
CHEBI has role CHEBI:35620 vasodilator agent
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D014665 Vasodilator Agents

Drug Use (View source of the data)

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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
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:2527
Disease of liver contraindication 235856003 DOID:409
Edema contraindication 267038008
Chronic myocardial ischemia contraindication 413844008 DOID:3393
Hypertension due to Arteriovenous Shunt contraindication
Hypertension due to Aortic Coarctation contraindication
Hypertensive Emergency associated with Pregnancy off-label use

Acid dissociation constants calculated using MoKa v3.0.0

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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:

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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:

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IDSource
2409 IUPHAR_LIGAND_ID
4018795 VUID
N0000147098 NUI
C0012022 UMLSCUI
D00294 KEGG_DRUG
DB01119 DRUGBANK_ID
3019 PUBCHEM_CID
3327 RXNORM
387328001 SNOMEDCT_US
58905004 SNOMEDCT_US
4574 MMSL
d00129 MMSL
4018795 VANDF
72399 MMSL
N0000006338 NDFRT
N0000147098 NDFRT
000636 NDDF
CHEMBL181 ChEMBL_ID
CHEBI:4495 CHEBI
D003981 MESH_DESCRIPTOR_UI
O5CB12L4FN UNII
1294 INN_ID
20J PDB_CHEM_ID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Proglycem HUMAN PRESCRIPTION DRUG LABEL 1 0575-6200 SUSPENSION 50 mg ORAL NDA 13 sections