CLINICAL USE


Calcium-channel blocker:Prophylaxis and treatment of angina Mild to moderate hypertension

DOSE IN NORMAL RENAL FUNCTION

20–40 mg 3 times daily

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :516
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :>99
  • %Excreted unchanged in urine &nbsp &nbsp : <1

  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :0.8

  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :8.6/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:Unlikely to be 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 possibly 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 ritonavirCardiac glycosides: digoxin concentration increased
  • Ciclosporin: concentration of ciclosporin increased
  • Grapefruit juice: concentration increased – avoid concomitant use
  • Tacrolimus: may increase tacrolimus levels Theophylline: possibly increased theophylline concentration

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral

    Rate of Administration

    –

    Comments

    Administration of nicardipine with food appears to reduce the bioavailability and delay the achievement of peak plasma concentrations

    OTHER INFORMATION

    Extensively metabolised in the liver and excreted in the urine and faeces, mainly as inactive metabolitesNicardipine blood levels may be elevated in some renally impaired patients. Therefore, start with a low dose and titrate to BP and response. The dose interval may also need to be extended to 12 hourly
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