CLINICAL USE


Calcium-channel blocker:Prophylaxis and treatment of angina Hypertension Raynaud’s phenomenon

DOSE IN NORMAL RENAL FUNCTION

Capsules: 5–20 mg 3 times dailyTablets: 20–40 mg twice dailyMR: 20–90 mg daily

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :346.3
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :92–98
  • %Excreted unchanged in urine &nbsp &nbsp : <1

  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :1.4

  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :1.4–11 (depends on preparation)/Unchanged

    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. Start with small doses
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : Dose as in normal renal function. Start with small doses

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Not dialysed. Dose as in GFR <10 mL/min

  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Not dialysed. Dose as in GFR <10 mL/min
  • HDF/high flux &nbsp :Unknown dialysability. Dose as in GFR <10 mL/min
  • CAV/VVHD &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in GFR 10 to 20 mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs
  • Anaesthetics: enhanced hypotensive effect
  • Antibacterials: metabolism accelerated by rifampicin; concentration increased by quinupristin/dalfopristin
  • 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; occasionally severe hypotension and heart failure with beta-blockers
  • Antivirals: concentration possibly increased by ritonavirCardiac glycosides: digoxin concentration possibly increased
  • Ciclosporin: may increase ciclosporin level, but not a problem in practice; nifedipine concentration may be increased
  • Grapefruit juice: concentration increased – avoid concomitant useInsulin: may impair glucose tolerance Magnesium salts: profound hypotension with IV magnesium
  • Tacrolimus: increased tacrolimus levels Theophylline: possibly increased theophylline concentration

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral

    Rate of Administration

    –

    Comments

    –

    OTHER INFORMATION

    Protein binding decreased in severe renal impairmentAcute renal dysfunction reported Increased incidence of side effects (headache, flushing, dizziness and peripheral oedema) in patients with ERFFor acute use, bite capsule then swallow contents with 10–50 mL water.
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