Products
Diazoxide is commercially available in capsule form (Proglicem). It has been approved in many countries since 1978.
Structure and properties
Diazoxide (C8H7ClN2O2S, Mr = 230.7 g/mol) exists as a white powder that is practically insoluble in water. It is a benzothiadiazine derivative and structurally related to the thiazides, but is not diuretic.
Effects
Diazoxide (ATC C02DA01, ATC V03AH01) has hyperglycemic, antihypertensive, and antidiuretic properties. It causes a rapid and dose-dependent increase in blood glucose levels. The effects are attributed to inhibition of insunlin release. Diazoxide opens ATP-dependent potassium channels on pancreatic beta cells. Blood glucose begins to rise after about one hour and the effect usually does not last longer than 8 hours. The half-life is about 28 hours.
Indications
- Endocrine-active tumors (islet cell adenoma/carcinoma or extrapancreatic malignancies) with hypoglycemia. Long-term treatment is indicated for nonresponse to surgical treatment.
- Leucine sensitivity with hypoglycemia.
- Therapy refractory malignant hypertension in renal failure.
Dosage
According to the professional information. The dose is adjusted individually. Capsules are taken two to three times daily.
Contraindications
- Hypersensitivity, including to thiazides
- Pheochromocytoma
- Diabetes mellitus
Full precautions can be found in the drug label.
Interactions
Insulins and antidiabetic agents such as the sulfonylureas may antagonize the effects.
Adverse effects
The most common potential adverse effects include:
- Neutropenia, thrombocytopenia.
- Hyperglycemia to ketoacidosis and hyperosmolar coma.
- Hyperuricemia
- Headache, dizziness
- Fluid retention, low blood pressure, rapid heart rate, palpitations.
- Gastrointestinal disorders, loss of taste.
- Skin rash, photosensitivity, hirsutism.
- Hypokalemia, sodium retention
- Weakness
