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Pronunciation |
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(dye
az OKS
ide) |
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U.S. Brand
Names |
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Hyperstat® I.V.; Proglycem®
Oral |
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Generic
Available |
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Yes: Injection |
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Pharmacological Index |
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Antihypoglycemic Agent; Vasodilator |
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Use |
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Oral: Hypoglycemia related to islet cell adenoma, carcinoma, hyperplasia, or
adenomatosis, nesidioblastosis, leucine sensitivity, or extrapancreatic
malignancy
I.V.: Severe hypertension |
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Pregnancy Risk
Factor |
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C |
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Contraindications |
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Hypersensitivity to diazoxide, thiazides, or other sulfonamide derivatives;
hypertension associated with aortic coarctation, arteriovenous shunts,
pheochromocytoma, dissecting aortic aneurysm |
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Warnings/Precautions |
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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) |
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Adverse
Reactions |
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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 |
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Overdosage/Toxicology |
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Symptoms of overdose include hyperglycemia, ketoacidosis, hypotension
Treatment: Insulin, fluid, and electrolyte restoration; I.V. pressors may be
needed to support blood pressure |
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Drug
Interactions |
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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 |
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Stability |
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Protect from light, heat, and freezing; avoid using darkened
solutions |
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Mechanism of
Action |
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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 |
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Pharmacodynamics/Kinetics |
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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 |
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Usual Dosage |
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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 |
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Monitoring
Parameters |
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Blood pressure, blood glucose, serum uric acid; intravenous administration
requires cardiac monitor and blood pressure monitor |
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Test
Interactions |
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False-negative insulin response to glucagon |
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Mental Health: Effects
on Mental Status |
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May cause dizziness; may rarely cause extrapyramidal
symptoms |
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Mental Health:
Effects on Psychiatric
Treatment |
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May cause leukopenia; use caution with clozapine and
carbamazepine |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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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.
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Nursing
Implications |
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Extravasation can be treated with warm compresses; monitor blood glucose
daily in patients receiving I.V. therapy |
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Dosage Forms |
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Capsule (Proglycem®): 50 mg
Injection (Hyperstat®): 15 mg/mL (1 mL, 20 mL)
Suspension, oral (chocolate-mint flavor) (Proglycem®):
50 mg/mL (30 mL) |
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References |
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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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