isradipine

CLINICAL USE

Calcium-channel blocker:Essential hypertension

DOSE IN NORMAL RENAL FUNCTION

Initially 2.5 mg twice daily, increased if necessary to 10 mg twice daily

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :371.4

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :95

%Excreted unchanged in urine &nbsp &nbsp : 0

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :3–4

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :4–8/10–11

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 : Dose as in normal renal function

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Not dialysed. Dose as in normal renal function

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Not dialysed. Dose as in normal renal function

HDF/high flux &nbsp :Not dialysed. Dose as in normal renal function

CAV/VVHD &nbsp &nbsp &nbsp:Not dialysed. Dose as in normal renal function

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Anaesthetics: enhanced hypotensive effect

Antibacterials: metabolism accelerated by rifampicin

Anti-epileptics: effect reduced by carbamazepine, barbiturates, phenytoin and primidone

Antifungals: metabolism possibly inhibited by itraconazole and ketoconazoleAntihypertensives: enhanced hypotensive effect; increased risk of first dose hypotensive effect of post-synaptic alpha-blockers

Antivirals: concentration possibly increased by ritonavir

Grapefruit juice: concentration increased – avoid concomitant useTheophylline: possibly increased theophylline concentration

ADMINISTRATION

Reconstition

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Route

Oral

Rate of Administration

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Comments

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OTHER INFORMATION

In elderly patients, or where hepatic or renal function is impaired, initial dose should be 1.25 mg twice daily. Dose should be increased according to the requirements of the individual patient.

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