Hyperstat I.V., Proglycem
Classifications: antihypertensive; vasodilator; sulfonylurea; antidiabetic agent; Therapeutic: antihypertensive; antidiabetic agent
Pregnancy Category: C
50 mg capsules; 50 mg/mL suspension; 15 mg/mL injection
Rapid-acting thiazide nondiuretic hypotensive and hyperglycemic agent. In contrast to thiazide diuretics, causes sodium
and water retention thus decreasing urinary output. This is probably due to its increase of proximal tubular reabsorption
of sodium and decrease of glomerular filtration rate. Hypotensive effect may be accompanied by marked reflex increase in
heart rate, cardiac output, and stroke volume; thus cerebral and coronary blood flows are usually maintained.
Reduces peripheral vascular resistance and BP by direct vasodilatory effect on peripheral arteriolar smooth muscles, perhaps
by direct competition for calcium receptor sites.
Intravenously for emergency lowering of BP in hospitalized patients with malignant hypertension, particularly when associated
with renal impairment. Not effective in pheochromocytoma. Commonly used with a diuretic such as furosemide (Lasix) to counteract
diazoxide-induced sodium and water retention. Orally in treatment of various diagnosed hypoglycemic states due to hyperinsulinism
when other medical treatment or surgical management has been unsuccessful or is not feasible.
Hypersensitivity to diazoxide; cerebral bleeding, eclampsia; aortic coarctation; AV shunt, significant coronary artery disease;
pheochromocytoma; pregnancy (category C), lactation. Use of oral diazoxide for functional hypoglycemia or in presence of
increased bilirubin in newborns.
Diabetes mellitus; impaired cerebral or cardiac circulation; impaired renal function; patients taking corticosteroids or
estrogenprogestogen combinations; hyperuricemia, history of gout, uremia; thiazide diuretic hypersensitivity.
Route & Dosage
Adult/Child: IV 13 mg/kg up to 150 mg, repeat at 515 min intervals if necessary
Adult/Child: PO 38 mg/kg/d divided q812h
Neonate/Infant: PO 815 mg/kg/d divided q812h
- Note: Give any prescribed diuretic 3060 min prior to IV diazoxide. Keep patient recumbent 810 h because of possible
additive hypotensive effect.
PREPARE: Direct: Give undiluted.
ADMINISTER: Direct: Give IV by rapid direct injection over 1030 sec. Keep patient recumbent while receiving IV and for at least 30 min
- Check IV injection site frequently. Solution is strongly alkaline. Extravasation of medication into tissues can cause severe
inflammatory reaction. Administer drug by peripheral vein ONLY.
INCOMPATIBILITIES Y-site: Hydralazine, lidocaine, propranolol.
- Do not give darkened solutions. Store capsules, oral suspension, and injectables at 2°30° C (36°86°
F) unless otherwise directed. Protect from light, heat, and freezing.
Adverse Effects (≥1%)CNS:
Headache, weakness, malaise
, dizziness, polyneuritis
, sleepiness, insomnia
, euphoria, anxiety, extrapyramidal signs. CV:
Palpitations, atrial and ventricular arrhythmias, flushing, shock; orthostatic hypotension,
CHF, transient hypertension. Special Senses:
Tinnitus, momentary hearing loss; blurred vision, transient cataracts, subconjunctival hemorrhage, ring scotoma, diplopia
lacrimation, papilledema. GI: Nausea, vomiting,
abdominal discomfort, diarrhea
, ileus, anorexia, transient loss of taste, impaired hepatic
, eosinophilia, decreased Hgb/Hct, decreased IgG. Body as a Whole:
Hypersensitivity (rash, fever, leukopenia
); chest and back pain, muscle cramps. Urogenital:
Decreased urinary output, nephrotic syndrome
(reversible), hematuria, increased nocturia, proteinuria, azotemia; inhibition
of labor. Skin:
Pruritus, flushing, monilial dermatitis, herpes, hirsutism; loss of scalp hair, sweating, sensation of warmth, burning,
or itching. Endocrine:
Advance in bone age (children), hyperglycemia, sodium and water retention, edema,
hyperuricemia, glycosuria, enlargement of breast lump, galactorrhea; decreased immunoglobulinemia, hirsutism.
Diagnostic Test Interference
Diazoxide can cause false-negative response to glucagon.
antagonize effects; thiazide diuretics
may intensify hyperglycemia and antihypertensive effects; phenytoin
increases risk of hyperglycemia, and diazoxide may increase phenytoin metabolism
, causing loss of seizure control
3060 s IV
; 1 h PO. Peak:
5 min IV
212 or more h IV
; 8 h PO. Distribution:
Crosses bloodbrain barrier and placenta. Metabolism:
Partially metabolized in the liver. Elimination:
In urine. Half-Life:
Assessment & Drug Effects
- Monitor for therapeutic effectiveness. Discontinue if not effective in 2 or 3 wk.
- Lab tests: Initial blood glucose, serum electrolytes, and CBC and at regular intervals in patients receiving multiple doses.
- Monitor BP q5min for the first 1530 min or until stabilized, then hourly for balance of drug effect.
- Notify physician immediately if BP continues to fall 30 min or more after IV drug administration. Cause other than drug
effect is probable.
- Monitor pulse: Tachycardia has occurred immediately following IV; palpitation and bradycardia have also been reported.
- Report promptly any change in I&O ratio.
- Observe patient closely for S&S of CHF (see Appendix F).
- Monitor diabetics carefully for loss of glycemic control.
- Evaluate serum electrolyte levels at regular intervals, particularly in patients with impaired renal function; hypokalemia
potentiates hyperglycemic effect of diazoxide.
- Note: In contrast to IV diazoxide, oral administration usually does not produce marked effects on BP. However, do make periodic
measurements of BP and vital signs.
- Monitor S&S for up to 7 d for both oral and parenteral forms; essential because of long half-life of diazoxide.
Patient & Family Education
- Note: Drug may cause hyperglycemia and glycosuria in diabetic and diabetic-prone individuals. Closely monitor blood and urine
glucose; report any abnormalities to physician.
- Report palpitations, chest pain, dizziness, fainting, or severe headache.
- Note: Lanugo-type hirsutism occurs frequently, commonly in children and women. It is reversible with discontinuation of drug.