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PubChem
| Name: | Diazoxide |
|---|---|
| PubChem Compound ID: | 3019 |
| Description: | A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group. |
| Molecular formula: | C8H7ClN2O2S |
| Molecular weight: | 230.672 g/mol |
| Synonyms: |
Prestwick1_000087; Lopac-D-9035; NSC76130; Prestwick0_000087; Hyperstat (TN); Diazoxidum [INN-Latin]; Diazoxide; Dizoxide; Proglycem; Spectrum4_001248.
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DrugBank
Identification
| Name: | Diazoxide |
|---|---|
| Name (isomeric): | DB01119 |
| Drug Type: | small molecule |
| Description: | A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group. |
| Brand: | Mutabase, Proglycem, Eudemine, Hypertonalum, Hyperstat, Dizoxide, Proglicem |
| Category: | Diuretics, Thiazide, Vasodilator Agents, Antihypertensive Agents |
| CAS number: | 364-98-7 |
Pharmacology
| Indication: | Used parentally to treat hypertensive emergencies. Also used to treat hypoglycemia secondary to insulinoma. |
|---|---|
| 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. |
| 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 tran...
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| Absorption: | Readily absorbed following oral administration. |
| Protein binding: | Very high (more than 90%) to serum proteins. |
| Biotransformation: | Hepatic. |
| Route of elimination: | Proglycem is extensively bound (more than 90%) to serum proteins, and is excreted in the kidneys. |
| Half Life: | 28 ±8.3 hours in normal adults. |
| Toxicity: | Oral LD50 in rat and mouse: 980 mg/kg and 444 mg/kg, respectively. |
| Affected organisms: | Humans and other mammals |
Interactions
| Drug interaction: |
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Targets
