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Diazoxide
Pronunciation
U.S. Brand Names
Generic Available
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Stability
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Monitoring Parameters
Test Interactions
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(dye az OKS ide)

U.S. Brand Names
Hyperstat® I.V.; Proglycem® Oral

Generic Available

Yes: Injection


Pharmacological Index

Antihypoglycemic Agent; Vasodilator


Use

Oral: Hypoglycemia related to islet cell adenoma, carcinoma, hyperplasia, or adenomatosis, nesidioblastosis, leucine sensitivity, or extrapancreatic malignancy

I.V.: Severe hypertension


Pregnancy Risk Factor

C


Contraindications

Hypersensitivity to diazoxide, thiazides, or other sulfonamide derivatives; hypertension associated with aortic coarctation, arteriovenous shunts, pheochromocytoma, dissecting aortic aneurysm


Warnings/Precautions

Diabetes mellitus, renal or liver disease, coronary artery disease, or cerebral vascular insufficiency; patients may require a diuretic with repeated I.V. doses; use caution when reducing severely elevated blood pressure (use 150 mg minibolus only)


Adverse Reactions

1% to 10%:

Cardiovascular: Hypotension

Central nervous system: Dizziness

Gastrointestinal: Nausea, vomiting

Neuromuscular & skeletal: Weakness

<1%: Tachycardia, flushing, angina, myocardial infarction, seizures, headache, extrapyramidal symptoms and development of abnormal facies with chronic oral use, cerebral infarction, rash, hirsutism, cellulitis, hyperglycemia, ketoacidosis, sodium and water retention, hyperuricemia, inhibition of labor, anorexia, constipation, leukopenia, thrombocytopenia, pain, burning, phlebitis upon extravasation


Overdosage/Toxicology

Symptoms of overdose include hyperglycemia, ketoacidosis, hypotension

Treatment: Insulin, fluid, and electrolyte restoration; I.V. pressors may be needed to support blood pressure


Drug Interactions

Decreased effect: Diazoxide may increase phenytoin metabolism or free fraction

Increased toxicity:

Diuretics and hypotensive agents may potentiate diazoxide adverse effects

Diazoxide may decrease warfarin protein binding


Stability

Protect from light, heat, and freezing; avoid using darkened solutions


Mechanism of Action

Inhibits insulin release from the pancreas; produces direct smooth muscle relaxation of the peripheral arterioles which results in decrease in blood pressure and reflex increase in heart rate and cardiac output


Pharmacodynamics/Kinetics

Hyperglycemic effect: Oral: Onset of action: Within 1 hour; Duration (normal renal function): 8 hours

Hypotensive effect: I.V.: Peak: Within 5 minutes; Duration: Usually 3-12 hours

Protein binding: 90%

Half-life: Children: 9-24 hours; Adults: 20-36 hours; End-stage renal disease: >30 hours

Elimination: 50% excreted unchanged in urine


Usual Dosage

Hypertension: Children and Adults: I.V.: 1-3 mg/kg up to a maximum of 150 mg in a single injection; repeat dose in 5-15 minutes until blood pressure adequately reduced; repeat administration at intervals of 4-24 hours; monitor the blood pressure closely; do not use longer than 10 days

Hyperinsulinemic hypoglycemia: Oral: Note: Use lower dose listed as initial dose

Newborns and Infants: 8-15 mg/kg/day in divided doses every 8-12 hours

Children and Adults: 3-8 mg/kg/day in divided doses every 8-12 hours

Dosing adjustment in renal impairment: None

Dialysis: Elimination is not enhanced via hemo- or peritoneal dialysis; supplemental dose is not necessary


Monitoring Parameters

Blood pressure, blood glucose, serum uric acid; intravenous administration requires cardiac monitor and blood pressure monitor


Test Interactions

False-negative insulin response to glucagon


Mental Health: Effects on Mental Status

May cause dizziness; may rarely cause extrapyramidal symptoms


Mental Health: Effects on Psychiatric Treatment

May cause leukopenia; use caution with clozapine and carbamazepine


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

No effects or complications reported


Patient Information

I.V. emergency treatment of hypertension: Remain lying down for at least 1 hour following infusion. When up, change positions from sitting or lying to standing slowly.

Oral treatment of hypoglycemia: Monitor serum glucose as directed by prescriber. Report significant changes in serum glucose levels, increased swelling of extremities, increased weight, unresolved constipation, GI upset (eg, nausea, vomiting, constipation, anorexia), chest pain, or palpitations.

Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Consult prescriber if breast-feeding.


Nursing Implications

Extravasation can be treated with warm compresses; monitor blood glucose daily in patients receiving I.V. therapy


Dosage Forms

Capsule (Proglycem®): 50 mg

Injection (Hyperstat®): 15 mg/mL (1 mL, 20 mL)

Suspension, oral (chocolate-mint flavor) (Proglycem®): 50 mg/mL (30 mL)


References

Lancaster-Smith M, Leigh NI, and Thompson HM, "Death Following Nonketotic Hyperglycemic Coma During Diazoxide Therapy and Peritoneal Dialysis," Postgrad Med J, 1974, 50:175-9.


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