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Pronunciation
(dye az OKS ide)
Generic Available (U.S.)
No
Brand Names: U.S.
Brand Names: Canada
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Hypoglycemia related to islet cell adenoma, carcinoma, hyperplasia, or adenomatosis; nesidioblastosis; leucine sensitivity; extrapancreatic malignancy
Pregnancy Risk Factor
C
Pregnancy Considerations
Adverse events have been observed in animal studies. Diazoxide crosses the human placenta. Altered carbohydrate metabolism, hyperbilirubinemia, or thrombocytopenia have been reported in the fetus or neonate. Alopecia and hypertrichosis lanuginosa have also been reported in infants following maternal use of diazoxide during the last 19-60 days of pregnancy.
Lactation
Excretion in breast milk unknown/not recommended
Contraindications
Hypersensitivity to diazoxide, thiazides, or other sulfonamide derivatives; functional hypoglycemia
Warnings/Precautions
Disease-related concerns:
• Heart failure: Use may lead to increased fluid retention and may precipitate congestive heart failure in patients with compromised cardiac reserve.
• Gout: Use with caution in patients with hyperuricemia or a history of gout.
• Hepatic impairment: Use with caution in patients with hepatic impairment.
• Renal impairment: Use with caution in patients with renal impairment; a reduced dose should be considered.
Concerns related to adverse effects:
• Hyperosmolar coma: Nonketotic hyperosmolar coma may occur during treatment; usually in patients with concomitant illness. Transient cataracts have been reported which subside following correction of hyperosmolarity.
• Ketoacidosis: Ketoacidosis may occur during treatment, usually in patients with concomitant illness.
Special populations:
• Newborns: May displace bilirubin from albumin; use caution in newborns with hyperbilirubinemia.
Adverse Reactions
Frequency not defined.
Cardiovascular: Hypotension, palpitation, tachycardia
Central nervous system: Anxiety, dizziness, fever, headache, insomnia, malaise, polyneuritis
Dermatologic: Hirsutism, pruritus, purpura, rash, scalp hair loss
Endocrine & metabolic: Breast lump enlargement, diabetic ketoacidosis, fluid retention, galactorrhea, gout, hyperglycemia, hyperosmolar nonketotic coma, sodium retention
Gastrointestinal: Abdominal pain, anorexia, diarrhea, ileus, nausea, pancreatitis, pancreatic necrosis, taste loss (transient), vomiting
Hematologic: Bleeding (excessive), eosinophilia, hemoglobin/hematocrit decreased, neutropenia (transient), thrombocytopenia
Hepatic: Alkaline phosphatase increased, AST increased
Neuromuscular & skeletal: Weakness
Ocular: Blurred vision, cataracts (transient), diplopia, lacrimation, ring scotoma, subconjunctival hemorrhage
Renal: Albuminuria, azotemia, creatinine clearance decreased, glucosuria, hematuria, nephrotic syndrome (reversible), uric acid increased, urinary output decreased
Miscellaneous: Abnormal facial features (children with chronic use), IgG decreased, lymphadenopathy
Metabolism/Transport Effects
None known.
Drug Interactions
Antihypertensives: Diazoxide may enhance the hypotensive effect of Antihypertensives. Risk C: Monitor therapy
Fosphenytoin: Diazoxide may decrease the serum concentration of Fosphenytoin. Total phenytoin concentrations may be affected more than free phenytoin concentrations. Risk C: Monitor therapy
MAO Inhibitors: May enhance the orthostatic hypotensive effect of Orthostatic Hypotension Producing Agents. Risk C: Monitor therapy
Phenytoin: Diazoxide may decrease the serum concentration of Phenytoin. Total phenytoin concentrations may be affected more than free phenytoin concentrations. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Herb/Nutraceutical: Avoid herbs with hypotensive properties (black cohosh, California poppy, coleus, golden seal, hawthorn, mistletoe, periwinkle, quinine, shepherd's purse); may enhance the hypotensive effect of diazoxide. Avoid herbs with hypertensive properties (bayberry, blue cohosh, cayenne, ephedra, ginger, ginseng [American], kola, licorice); may diminish the antihypertensive effect of diazoxide.
Storage
Suspension: Store at controlled room temperature of 25°C (77°F). Protect from light.
Mechanism of Action
Activates potassium channels. Inhibits insulin release from the pancreas
Pharmacodynamics/Kinetics
Onset of action: Hyperglycemic: Oral: ~1 hour
Duration: Hyperglycemic: Oral: Normal renal function: 8 hours
Protein binding: >90%
Half-life elimination: Oral: Children: 9-24 hours; Adults: 24-36 hours
Excretion: Urine
Dosage
Oral: Hyperinsulinemic hypoglycemia:
Newborns and Infants: Initial dose: 10 mg/kg/day; dosing range: 8-15 mg/kg/day in divided doses every 8-12 hours
Children and Adults: Initial dose: 3 mg/kg/day; dosing range: 3-8 mg/kg/day in divided doses every 8-12 hours. Note: In certain instances, patients with refractory hypoglycemia may require higher doses.
Dosing adjustment in renal impairment: Half-life may be prolonged with renal impairment; a reduced dose should be considered.
Monitoring Parameters
Blood glucose, serum uric acid, BUN, creatinine clearance, CBC with differential, AST; urine glucose and ketones
Dental Health: Effects on Dental Treatment
No significant effects or complications reported
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
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
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Suspension, oral:
Proglycem®: 50 mg/mL (30 mL) [contains ethanol ~7.25%, propylene glycol, sodium benzoate; chocolate-mint flavor]
Pricing: U.S. (www.drugstore.com)
Suspension (Proglycem)
50 mg/mL (30): $195.99
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.
International Brand Names
Lexi-Comp.com
Last full review/revision January 2012
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