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 | |
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ABCC8 |
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Publications |
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ABCC9 |
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Publications |
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KCNJ11 |
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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 |
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(source: Drug Bank) |
| CA1 |
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(source: Drug Bank) |
| CA2 |
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(source: Drug Bank) |
| CA4 |
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(source: Drug Bank) |
| KCNJ11 |
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(source: Drug Bank) |
| KCNMA1 |
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(source: Drug Bank) |
| SLC12A3 |
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(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.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
Common Searches
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.
