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).

Action ⬆ ⬇

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

Therapeutic effects:

Increased blood glucose.

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

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.

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.

Availability ⬆ ⬇

(Generic available)

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

Assessment ⬆ ⬇

Assess patient for signs of hyperglycemia (drowsiness, fruity breath, increased urination, unusual thirst).
Assess for allergy to sulfonamide drugs.
- Assess patient routinely for signs and symptoms of HF (peripheral edema, dyspnea, rales/crackles, fatigue, weight gain, jugular venous distention). Notify health care professional if these occur.

Lab Test Considerations:

Monitor blood glucose periodically until stabilized. Monitor urine for glucose and ketones during therapy, especially during periods of stress.
- Monitor BUN and creatinine periodically during therapy. May cause ↑ serum glucose, BUN, alkaline phosphatase, AST, sodium, and uric acid levels.
- Monitor hematocrit, platelet count, total and differential leukocyte counts periodically during therapy.
- Monitor AST and serum uric acid levels periodically during therapy.

Toxicity and Overdose:

If severe hypotension occurs, treatment includes Trendelenburg position, volume infusion, and sympathomimetics (norepinephrine).
- Patients who develop marked hyperglycemia must be monitored for 7 days while blood glucose concentrations stabilize.

Implementation ⬆ ⬇

Loop diuretics are commonly given concurrently with this medication to prevent sodium and water retention.
- Solution must be protected from light; keep in carton. Do not administer darkened solution.
PO: Shake oral suspension well before use.

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.

section name header

Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇