Drug/Small Molecule:
diazoxide

2D structure

Overview

Trade Names: Dizoxide; Eudemine; Hyperstat; Hypertonalum; Mutabase; Proglicem; Proglycem
PharmGKB Accession Id: PA449285

Description

A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group. PubChem (source: Drug Bank)

Indication

Used parentally to treat hypertensive emergencies. Also used to treat hypoglycemia secondary to insulinoma. (source: Drug Bank)

ATC Therapeutic Categories

  • C02DA:Thiazide derivatives
  • V03AH:Drugs for treatment of hypoglycemia

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

As a diuretic, diazoxide inhibits active chloride reabsorption at the early distal tubule via the Na-Cl cotransporter, resulting in an increase in the excretion of sodium, chloride, and water. Thiazides like diazoxide also inhibit sodium ion transport across the renal tubular epithelium through binding to the thiazide sensitive sodium-chloride transporter. This results in an increase in potassium excretion via the sodium-potassium exchange mechanism. The antihypertensive mechanism of diazoxide is less well understood although it may be mediated through its action on carbonic anhydrases in the smooth muscle or through its action on the large-conductance calcium-activated potassium (KCa) channel, also found in the smooth muscle. As a antihypoglycemic, diazoxide inhibits insulin release from the pancreas, probably by opening potassium channels in the beta cell membrane. (source: Drug Bank)

Pharmacology

Diazoxide is a potassium channel activator, which causes local relaxation in smooth muscle by increasing membrane permeability to potassium ions. This switches off voltage-gated calcium ion channels which inhibits the generation of an action potential. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic. (source: Drug Bank)

Protein Binding

Very high (more than 90%) to serum proteins. (source: Drug Bank)

Absorption

Readily absorbed following oral administration. (source: Drug Bank)

Toxicity

Oral LD<sub>50</sub> in rat and mouse: 980 mg/kg and 444 mg/kg, respectively. (source: Drug Bank)

Isomeric SMILES Code:

CC1=Nc2ccc(cc2S(=O)(=O)N1)Cl (source: Drug Bank)

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
No phenotype data Genotype Data Available Literature annotations available Not annotated
ABCC8
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  • FA
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Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
ABCC9
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  • FA
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Publications
No phenotype data Genotype Data Available Literature annotations available Has annotations
KCNJ11
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  • FA
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Publications

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
ATP1A1 Uncurated Annotation (source: Drug Bank)
CA1 Uncurated Annotation (source: Drug Bank)
CA2 Uncurated Annotation (source: Drug Bank)
CA4 Uncurated Annotation (source: Drug Bank)
KCNJ11 Uncurated Annotation (source: Drug Bank)
KCNMA1 Uncurated Annotation (source: Drug Bank)
SLC12A3 Uncurated Annotation (source: Drug Bank)

A list of non-curated publications that mention this drug along with other drugs is available.

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB01119
KEGG Compound ID:
C06949
KEGG Drug ID:
D00294
PubChem Compound ID:
3019
PubChem Substance ID:
9164
IUPHAR Ligand ID:
2409

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

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