diazoxide

CLINICAL USE

Treatment of hypertensive emergencies including severe hypertension associated with renal diseaseHypoglycaemia

DOSE IN NORMAL RENAL FUNCTION

Hypertension: IV: 1–3 mg/kg; maximum single dose: 150 mg, repeat after 5–15 minutesHypoglycaemia: Oral: 3–5 mg/kg in 2–3 divided doses; adjust according to response, usually 3–8 mg/kg; total doses up to 1 g have been used

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :230.7

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :>90

%Excreted unchanged in urine &nbsp &nbsp : 50

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :0.2–0.3

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :20-45/30–60

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 &nbsp &nbsp : Dose as in normal renal function

10 to 20 &nbsp &nbsp : Dose as in normal renal function

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : Start with a lower dose and increase gradually according to response. Use with caution

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Dialysed. Dose as in GFR <10 mL/min

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Dialysed. Dose as in GFR <10 mL/min

HDF/high flux &nbsp :Dialysed. Dose as in GFR <10 mL/min

CAV/VVHD &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in normal renal function

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugsAntihypertensives and vasodilators: enhanced hypotensive effectMAOIs: withdraw at least 14 days before starting diazoxidePhenytoin: may reduce phenytoin levels

ADMINISTRATION

Reconstition

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Route

IV bolus, oral

Rate of Administration

<30 seconds

Comments

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OTHER INFORMATION

Single doses above 300 mg have been associated with angina and myocardial and cerebral infarction. Can cause sodium and water retention

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