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Diazoxide

Catalog No. DB01119 Name DrugBank
CAS Number 364-98-7 Website http://www.ualberta.ca/
M. F. C8H7ClN2O2S Telephone (780) 492-3111
M. W. 230.67138 Fax (780) 492-1071
Purity Email david.wishart@ualberta.ca
Storage Chembase ID: 990

SYNONYMS

IUPAC name
7-chloro-3-methyl-4H-1$l^{6},2,4-benzothiadiazine-1,1-dione
IUPAC Traditional name
diazoxide
Brand Name
Hypertonalum
Eudemine
Proglycem
Proglicem
Dizoxide
Hyperstat
Mutabase

DATABASE IDS

PubChem CID 3019
PubChem SID 46508027
CAS Number 364-98-7

PROPERTIES

Hydrophobicity(logP) 1.3
Solubility 2850 mg/L

DETAILS

Description (English)
Item Information
Drug Groups approved
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]
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.
Toxicity Oral LD50 in rat and mouse: 980 mg/kg and 444 mg/kg, respectively.
Affected Organisms
Humans and other mammals
Biotransformation Hepatic.
Absorption Readily absorbed following oral administration.
Half Life 28 ±8.3 hours in normal adults.
Protein Binding Very high (more than 90%) to serum proteins.
Elimination Proglycem is extensively bound (more than 90%) to serum proteins, and is excreted in the kidneys.
External Links
Wikipedia
Drugs.com

REFERENCES