Diazoxide

(die-az-ox-ide)

PCaution when used during lactation : Caution when used during pregnancy

Molecule Info

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Indication(s) & Dosage

Diazoxide is used to treat hypoglycemia  caused by certain conditions in which too much insulin is produced. Too much insulin can cause low blood sugar. This drug works by preventing insulin release from the pancreas, helping to return the blood sugar to normal levels. Diazoxide is a thiazide drug, but has no diuretic effects like other thiazides. 

Diazoxide Injection is indicated for short-term use in the emergency reduction of blood pressure in severe, nonmalignant and malignant hypertension in hospitalized adults; and in acute severe hypertension in hospitalized children, when prompt and urgent decrease of diastolic pressure is required. Treatment with orally effective antihypertensive agents should not be instituted until blood pressure has stabilized. The use of Diazoxide Injection for longer than 10 days is not recommended.Diazoxide Injection is ineffective against hypertension due to pheochromocytoma.Hypoglycaemia  Adult: 3-5 mg/kg daily in 2 or 3 divided doses.  Maintenance: 3-8 mg/kg daily up to 1 g daily in patients with insulinomas. Child: Neonates and infants: 5 mg/kg bid.  Maintenance: 3-9 mg/kg daily up to 20 mg/kg daily may be required.  Doses may be given via IV admin if necessary.  Renal impairment: Dose reductions may be necessary.  Intravenous  Hypertensive crisis  Adult: 1-3 mg/kg within 30 sec, repeated after 5-15 min if required.  Max: 150 mg/dose.  Renal impairment: Dose reductions may be necessarySpecial Populations: Dose reduction in renal impairment.

Overdosage

Hypotension, hyperglycemia.  Treatment is symptomatic.  Hypotension may be controlled with the Trendelenburg maneuver and if necessary, IV fluids and sympathomimetic agents, such as dopamine or norepinephrine.  Hypoglycaemia may be treated with Oral   hypoglycaemias or insulin, if severe.

Contraindications

Acute aortic dissection, conditions in which increase in cardiac output is detrimental, compensatory hypertension, coronary or cerebral insufficiency, poor cardiac reserve, hypersensitivity to diazoxide, thiazides or sulfonamide-derived drugs.

Special Precautions

Impaired cardiac or cerebral circulation; aortic coarctation; arteriovenous shunt; renal impairment.  Monitor BP and glucose levels regularly in prolonged therapy.  Treatment period >10 days is not recommended.  Pregnancy.

Adverse Drug Reaction(s)

Hypotension; hyperglycaemia; oedema; dysgeusia; nausea; anorexia and other GI disturbances; mild hyperuricaemia; extrapyramidal symptoms; eosinophilia and thrombocytopaenia; dyspnoea; hypertrichosis; headache; dizziness; tinnitus and blurred vision; hypersensitivity.  IV: Coronary ischaemia, cardiac arrhythmias, cerebral ischaemia, impaired renal function, vasodilatation symptoms, burning sensation in the vein used for inj.

Drug Interactions

Diuretics; other antihypertensives; vasodilators; chlorpromazine; phenytoin.  Diazoxie should not be administered in patients who have received other antihypertensives within 6 hr.

Lab Interference

Insulin response to glucagon.  Blood glucose concentrations, BUN concentrations, serum characterization tests.  Creatinine clearance, urinary blood count, excretion of electrolytes.

Pregnancy Category (FDA)

Category C: Either studies in animals have revealed adverse effects on the foetus and there are no controlled studies in women or studies in women and animals are not available.  Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

 

Pharmacology

Diazoxide increases the conc of glucose in the plasma and inhibits the secretion of insulin by the β-cells of the pancreas, and may increase the hepatic output of glucose.  When given IV, it produces a fall in BP by causing vasodilation of the arterioles, thus a reduction in peripheral resistance.  It has an antidiuretic action and produces fluid and electrolyte retention. Onset: Oral:  1 hr.  IV: 1 min. Duration: 2-12 hr.  Absorption: Readily absorbed from the GI tract after Oral   admin.  Distribution: >90% bound to plasma proteins.  Crosses the placenta and blood brain barrier.  Metabolism: Partly metabolised in the liver.  Excretion: Plasma half-life ranges from 20-45 hr.

ATC Classification

C02DA01 - diazoxide; Belongs to the class of thiazide derivative agents acting on arteriolar smooth muscle.  Used in the treatment of hypertension.  V03AH01 - diazoxide; Belongs to the class of drugs used in the treatment of hypoglycemia.

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