Lacidipine

CLINICAL USE

Calcium-channel blocker:Hypertension

DOSE IN NORMAL RENAL FUNCTION

2–6 mg once daily

PHARMACOKINETICS

  • Molecular weight                           :455.5
  • %Protein binding                           :95
  • %Excreted unchanged in urine     : 0
  • Volume of distribution (L/kg)       :0.9–2.3
  • half-life – normal/ESRD (hrs)      :13–19/–

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50     : Dose as in normal renal function
  • 10 to 20     : Dose as in normal renal function
  • <10           : Dose as in normal renal function

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

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