Lacidipine

CLINICAL USE


Calcium-channel blocker:Hypertension

DOSE IN NORMAL RENAL FUNCTION

2–6 mg once daily

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :455.5
  • %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 :0.9–2.3

  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :13–19/–

    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:Unknown dialysability. Dose as in normal renal function

  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Unknown dialysability. Dose as in normal renal function
  • HDF/high flux &nbsp :Unknown dialysability. Dose as in normal renal function
  • CAV/VVHD &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in normal renal function

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs
  • Anaesthetics: enhanced hypotensive effect
  • Anti-epileptics: effect possibly 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
  • Ciclosporin: 10 kidney transplant patients on ciclosporin, prednisone and azathioprine were given 4 mg lacidipine daily. A very small increase in the trough serum levels (+6%) and AUC (+14%) of the ciclosporin occurred
  • Grapefruit juice: concentration increased – avoid concomitant useTheophylline: possibly increased theophylline concentration

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral

    Rate of Administration

    –

    Comments

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