diazoxide

REMS

PO: Treatment of hypoglycemia associated with hyperinsulinism due to islet cell adenoma carcinoma or extrapancreatic malignancy (in adults) or leucine sensitivity, islet cell hyperplasia, nesidioblastosis, extrapancreatic malignancy, islet cell adenoma, or adenomatosis (in infants and children).

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity; cross-sensitivity to thiazide diuretics may occur;
Functional hypoglycemia

Use Cautiously in:

Diabetes (hyperglycemia accompanies use);
HF;
Gout
Renal impairment;
OB: Safety not established.
Pedi: Newborns and infants with meconium aspiration syndrome, respiratory distress syndrome, transient tachypnea, pneumonia, sepsis, congenital diaphragmatic hernia, or congenital heart disease (may ↑ risk of pulmonary hypertension)
Pedi: Newborns with hyperbilirubinemia (may ↑ risk of kernicterus)

Adv. Reactions/Side Effects ⬆ ⬇

CV: edema, hypotension, tachycardia, HF, palpitations

Derm: hirsutism, rash

Endo: hyperglycemia, DIABETIC KETOACIDOSIS, HYPEROSMOLAR NONKETOTIC COMA, hyperuricemia

GI: abdominal pain, diarrhea, ILEUS, loss of taste, nausea, vomiting

GU: glycosuria

Hemat: neutropenia, thrombocytopenia

MS: weakness

Neuro: headache

Resp: PULMONARY HYPERTENSION

Interactions ⬆ ⬇

Drug-drug:

Concurrent diuretic therapy may potentiate hyperglycemic, hyperuricemic, and hypotensive effects.
May enhance BP lowering response of any antihypertensive.
May ↑ metabolism and ↓ effectiveness of phenytoin.
Corticosteroids may ↑ hyperglycemia.
May ↑ effects of warfarin.
May alter the effects of insulins or oral hypoglycemic agents.

Drug-Natural Products:

Glucosamine may worsen hyperglycemia.

Availability ⬆ ⬇

(Generic available)

Capsules: 100 mg
Oral suspensionchocolate-mint flavor: 50 mg/mL (contains 7.25% alcohol)

Route/Dosage ⬆ ⬇

Hyperinsulinemic Hypoglycemia

PO (Adults and Children ): 1 mg/kg q 8 hr initially, further adjustments made on the basis of response. Usual maintenance dose is 3–8 mg/kg/day given in 2–3 divided doses every 8–12 hr.
PO (Infants and Newborns): 2.7 mg/kg q 8 hr initially, further adjustments made on the basis of response. Usual maintenance dose is 8–15 mg/kg/day in 2–3 divided doses every 8–12 hr.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Inhibits insulin release from the pancreas and decreases peripheral utilization of glucose.

Therapeutic effects:

Increased blood glucose.

Classifications ⬆ ⬇

Therapeutic Classification: hyperglycemic

Pharmacologic Classification: pancreatics

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed following oral administration.

Distribution: Crosses the blood-brain barrier and placenta.

Protein Binding: >90%.

Metabolism/Excretion: 50% metabolized by the liver; 50% excreted unchanged by the kidneys.

Half-Life: 10–36 hr (↑ in renal impairment).

Time/Action Profile ⬆ ⬇

(Blood glucose concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	1 hr	8–12 hr	8 hr

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication as directed, at the same time each day. Do not skip or take extra doses.
- Encourage patient to follow prescribed diet, medication, and exercise regimen to prevent hypoglycemic or hyperglycemic episodes.
- Caution patient that sharing diazoxide with others may be dangerous.
- Review signs of hypoglycemia and hyperglycemia with patient.
- Advise patient not to switch from capsule to oral suspension form without consulting health care professional, because oral suspension produces higher blood concentrations.
- Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
- Advise patient to inform health care professional of medication regimen prior to treatment or surgery.
- Instruct female patients to inform health care professional if pregnancy is planned or suspected or if breastfeeding.
- Emphasize the importance of routine follow-up exams, especially during the first few wk of therapy.

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Indications ⬇