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Diazoxide


General


Pronunciation

(dye az OKS ide)


Brand Names: U.S.

  • Proglycem

Indications


Use: Labeled Indications

Hyperinsulinemic hypoglycemia: Management of hypoglycemia due to hyperinsulinism due to the following conditions in adults (ie, inoperable islet cell adenoma or carcinoma, or extrapancreatic malignancy) and infants and children (ie, leucine sensitivity, islet cell hyperplasia, nesidioblastosis, extrapancreatic malignancy, islet cell adenoma, or adenomatosis; may be used preoperatively as a temporary measure, and postoperatively, if hypoglycemia persists).

Note: Consider treatment with diazoxide when other specific medical therapy or surgical management for hypoglycemia due to the above conditions either has been unsuccessful or is not feasible.


Contraindications


Hypersensitivity to diazoxide, other thiazides, or any component of the formulation; functional hypoglycemia


Dosing and Administration


Dosing: Adult

Hyperinsulinemic hypoglycemia: Oral: Initial dose: 3 mg/kg/day divided into 3 equal doses every 8 hours; dosing range: 3 to 8 mg/kg/day divided into 2 or 3 equal doses every 8 to 12 hours. Adjust dose until the desired clinical and laboratory effects are produced. Note: In certain instances, patients with refractory hypoglycemia may require higher doses. Discontinue if no effect after 2 to 3 weeks.


Dosing: Geriatric

Refer to adult dosing.


Dosing: Pediatric

Hyperinsulinemic hypoglycemia: Oral:

Neonates and Infants: Initial dose: 10 mg/kg/day divided into 3 equal doses every 8 hours; dosing range: 8 to 15 mg/kg/day divided into 2 or 3 equal doses every 8 to 12 hours. Adjust dose until the desired clinical and laboratory effects are produced. Discontinue if no effect after 2 to 3 weeks.

Children and Adolescents: Refer to adult dosing.


Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer 's labeling; a reduced dose should be considered (half-life may be prolonged).


Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturer 's labeling.


Administration

Shake suspension well before each use. Assure accuracy of dosage in infants and young children.


Storage

Store at 25 � �C (77 � �F); excursions permitted to 15 � �C to 30 � �C (59 � �F to 86 � �F). Protect from light. Store in carton until contents are used.


Dosage Forms/Strengths


Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Suspension, Oral:

Proglycem: 50 mg/mL (30 mL) [chocolate mint flavor]


Drug Interactions

Antidiabetic Agents: Hyperglycemia-Associated Agents may diminish the therapeutic effect of Antidiabetic Agents. Monitor therapy

Blood Pressure Lowering Agents: Diazoxide may enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Fosphenytoin: Diazoxide may decrease the serum concentration of Fosphenytoin. Total phenytoin concentrations may be affected more than free phenytoin concentrations. Monitor therapy

Phenytoin: Diazoxide may decrease the serum concentration of Phenytoin. Total phenytoin concentrations may be affected more than free phenytoin concentrations. Monitor therapy

Thiazide and Thiazide-Like Diuretics: May enhance the adverse/toxic effect of Diazoxide. Monitor therapy

Thiopental: May enhance the hypotensive effect of Diazoxide. Monitor therapy


Monitoring Parameters

Clinical response, blood glucose, serum uric acid, BUN, creatinine clearance, CBC with differential, AST; urine glucose and ketones (especially under stress conditions and during prolonged treatment); serum electrolytes and uric acid; respiratory distress (neonates and infants [especially those with risk factors for pulmonary hypertension]).


Lab Test Interferences


Test Interactions

Serum renin concentrations and IgG concentrations may be increased. Serum cortisol concentrations may be decreased. May cause a false-negative insulin response to glucagon.


Adverse Reactions


Frequency not defined.

Cardiovascular: Cardiac failure (due to sodium and water retention), hyperosmolar coma (nonketotic), hypertension (transient), hypotension, palpitations, tachycardia

Central nervous system: Anxiety, dizziness, extrapyramidal reaction, headache, insomnia, malaise, paresthesia, peripheral neuritis (poly)

Dermatologic: Cutaneous candidiasis, loss of scalp hair, pruritus, purpura, skin rash

Endocrine & metabolic: Albuminuria, diabetic ketoacidosis, fluid retention, galactorrhea, glycosuria, gout, hirsutism, hyperglycemia, sodium retention

Gastrointestinal: Abdominal pain, acute pancreatitis, ageusia (transient), anorexia, diarrhea, intestinal obstruction, nausea, pancreatic necrosis, vomiting

Genitourinary: Azotemia, decreased urine output, hematuria, lump in breast (enlargement), nephrotic syndrome (reversible), uricosuria

Hematologic & oncologic: Decreased hematocrit, decreased hemoglobin, decreased serum immunoglobulins (IgG), eosinophilia, hemorrhage (excessive), lymphadenopathy, neutropenia (transient), thrombocytopenia

Hepatic: Increased serum alkaline phosphatase, increased serum AST

Infection: Herpes virus infection

Neuromuscular & skeletal: Accelerated bone maturation, craniofacial abnormality (children with chronic use), weakness

Ophthalmic: Blurred vision, cataract (transient), diplopia, lacrimation, scotoma (ring), subconjunctival hemorrhage

Renal: Decreased creatinine clearance

Miscellaneous: Fever

<1% (Limited to important or life-threatening): Chest pain, pulmonary hypertension (infants and neonates)


Warnings/Precautions


Special Populations: Renal Function Impairment

Plasma half-life is prolonged.


Warnings/Precautions

Concerns related to adverse effects:

- Abnormal facial features: Development of abnormal facial features was reported in children treated >4 years for hypoglycemia hyperinsulinism.

- Hyperosmolar coma: Nonketotic hyperosmolar coma may occur during treatment; usually in patients with concomitant illness; prompt recognition and treatment are essential. Transient cataracts have been reported which subside following correction of hyperosmolarity.

- Ketoacidosis: Ketoacidosis may occur during treatment, usually in patients with concomitant illness.

Disease-related concerns:

- Heart failure: Use may lead to increased fluid retention due to antidiuretic properties and may precipitate heart failure in patients with compromised cardiac reserve.

- Gout: Use with caution in patients with hyperuricemia or a history of gout.

- Renal impairment: Use with caution in patients with renal impairment; a reduced dose should be considered.

Special populations:

- Pediatric: May displace bilirubin from albumin; use caution in newborns with hyperbilirubinemia. Pulmonary hypertension has been reported in newborns and young infants and was reversible upon drug discontinuation; monitor patients (especially patients with risk factors for pulmonary hypertension) for respiratory distress and discontinue diazoxide if pulmonary hypertension is suspected.

Dosage form specific issues:

- Benzyl alcohol and derivatives: Some dosage forms may contain sodium benzoate/benzoic acid; benzoic acid (benzoate) is a metabolite of benzyl alcohol; large amounts of benzyl alcohol ( ≥99 mg/kg/day) have been associated with a potentially fatal toxicity ( "gasping syndrome " �) in neonates; the "gasping syndrome " � consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension, and cardiovascular collapse (AAP [Inactive" 1997]; CDC 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol derivative with caution in neonates. See manufacturer 's labeling.

- Propylene glycol: Some dosage forms may contain propylene glycol; large amounts are potentially toxic and have been associated hyperosmolality, lactic acidosis, seizures, and respiratory depression; use caution (AAP 1997; Zar 2007).


Pregnancy Risk Factor

C


Pregnancy Considerations

Adverse events have been observed in animal studies. Diazoxide crosses the human placenta and appears in cord blood. Altered carbohydrate metabolism, hyperbilirubinemia, and 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 to 60 days of pregnancy.


Actions


Pharmacology

Opens ATP-dependent potassium channels on pancreatic beta cells in the presence of ATP and Mg2+, resulting in hyperpolarization of the cell and inhibition of insulin release. Diazoxide binds to a different site on the potassium channel than the sulfonylureas (Doyle, 2003).


Excretion

Urine (50% as unchanged drug)


Onset of Action

Hyperglycemic: Oral: Within 1 hour


Duration of Action

Hyperglycemic: Oral: Normal renal function: ≤8 hours


Half-Life Elimination

Oral: Children: 9.5 to 24 hours; Adults: 24 to 36 hours


Protein Binding

>90%


Patient and Family Education


Patient Education

- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

- Patient may experience nausea, vomiting, lack of appetite, diarrhea, change in taste, or loss of strength and energy. Have patient report immediately to prescriber signs of high blood sugar (confusion, feeling sleepy, more thirst, hunger, passing urine more often, flushing, fast breathing, or breath that smells like fruit), signs of pancreatitis (severe abdominal pain, severe back pain, severe nausea, or vomiting), shortness of breath, excessive weight gain, swelling of arms or legs, severe constipation, severe abdominal pain, tachycardia, arrhythmia, bruising, bleeding, severe dizziness, passing out, severe headache, angina, urinary retention, change in amount of urine passed, vision changes, tremors, difficulty moving, hair growth on forehead, back, arms, and legs, or stiffness (HCAHPS).

- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating, and advising patients.

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