DIAZOXIDE
(dye-az-ox'ide)
Hyperstat I. V., Proglycem
Classifications: cardiovascular agent; antihypertensive; vasodilator; sulfonylurea
Prototype: Hydralazine
Pregnancy Category: C

Availability

50 mg capsules; 50 mg/mL suspension; 15 mg/mL injection

Actions

Rapid-acting thiazide nondiuretic hypotensive and hyperglycemic agent. In contrast to thiazide diuretics, causes sodium and water retention and decreases urinary output, probably because it increases proximal tubular reabsorption of sodium and decreases glomerular filtration rate. Hypotensive effect may be accompanied by marked reflex increase in heart rate, cardiac output, and stroke volume; thus cerebral and coronary blood flow are usually maintained.

Therapeutic Effects

Reduces peripheral vascular resistance and BP by direct vasodilatory effect on peripheral arteriolar smooth muscles, perhaps by direct competition for calcium receptor sites.

Uses

Intravenously for emergency lowering of BP in hospitalized patients with malignant hypertension, particularly when associated with renal impairment. Not effective in pheochromocytoma. Commonly used with a diuretic such as furosemide (Lasix) to counteract diazoxide-induced sodium and water retention. Orally in treatment of various diagnosed hypoglycemic states due to hyperinsulinism when other medical treatment or surgical management has been unsuccessful or is not feasible.

Contraindications

Hypersensitivity to diazoxide or to other thiazides; cerebral bleeding, eclampsia; aortic coarctation; AV shunt, significant coronary artery disease. Safe use during pregnancy (category C) or lactation is not established. Use of oral diazoxide for functional hypoglycemia or in presence of increased bilirubin in newborns.

Cautious Use

Diabetes mellitus; impaired cerebral or cardiac circulation; impaired renal function; patients taking corticosteroids or estrogen–progestogen combinations; hyperuricemia, history of gout, uremia.

Route & Dosage

Severe Hypertension
Adult/Child: IV 1–3 mg/kg up to 150 mg, repeat at 5–15 min intervals if necessary

Hypoglycemia
Adult/Child: PO 3–8 mg/kg/d divided q8–12h
Neonate/Infant: PO 8–15 mg/kg/d divided q8–12h

Administration

Intravenous
  • Note: Give any prescribed diuretic 30–60 min prior to IV diazoxide. Keep patient recumbent 8–10 h because of possible additive hypotensive effect.

PREPARE: Direct: Give undiluted.  

ADMINISTER: Direct: Give IV by rapid direct injection over 10–30 s. Keep patient recumbent while receiving IV and for at least 30 min following administration.  

  • Check IV injection site frequently. Solution is strongly alkaline. Extravasation of medication into tissues can cause severe inflammatory reaction. Administer drug by peripheral vein ONLY.

Adverse Effects (1%)

CNS: Headache, weakness, malaise, dizziness, polyneuritis, sleepiness, insomnia, euphoria, anxiety, extrapyramidal signs. CV: Palpitations, atrial and ventricular arrhythmias, flushing, shock; orthostatic hypotension, CHF, transient hypertension. Special Senses: Tinnitus, momentary hearing loss; blurred vision, transient cataracts, subconjunctival hemorrhage, ring scotoma, diplopia, lacrimation, papilledema. GI: Nausea, vomiting, abdominal discomfort, diarrhea, constipation, ileus, anorexia, transient loss of taste, impaired hepatic function. Hematologic: Transient neutropenia, eosinophilia, decreased Hgb/Hct, decreased IgG. Body as a Whole: Hypersensitivity (rash, fever, leukopenia); chest and back pain, muscle cramps. Urogenital: Decreased urinary output, nephrotic syndrome (reversible), hematuria, increased nocturia, proteinuria, azotemia; inhibition of labor. Skin: Pruritus, flushing, monilial dermatitis, herpes, hirsutism; loss of scalp hair, sweating, sensation of warmth, burning, or itching. Endocrine: Advance in bone age (children), hyperglycemia, sodium and water retention, edema, hyperuricemia, glycosuria, enlargement of breast lump, galactorrhea; decreased immunoglobulinemia, hirsutism.

Diagnostic Test Interference

Diazoxide can cause false-negative response to glucagon.

Interactions

Drug: sulfonylureas antagonize effects; thiazide diuretics may intensify hyperglycemia and antihypertensive effects; phenytoin increases risk of hyperglycemia, and diazoxide may increase phenytoin metabolism, causing loss of seizure control.

Pharmacokinetics

Onset: 30–60 s IV; 1 h PO. Peak: 5 min IV. Duration: 2–12 or more h IV; 8 h PO. Distribution: Crosses blood–brain barrier and placenta. Metabolism: Partially metabolized in the liver. Elimination: Excreted in urine. Half-Life: 21–45 h.

Nursing Implications

Assessment & Drug Effects

Patient & Family Education


Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug