CLINICAL USE

Calcium-channel blocker:Hypertension Angina

DOSE IN NORMAL RENAL FUNCTION

10–40 mg daily (varies, depending on indication)

PHARMACOKINETICS

  • Molecular weight                           :388.4
  • %Protein binding                           :>99
  • %Excreted unchanged in urine     :
  • <10           :
  • Volume of distribution (L/kg)       :2.3–7.1
  • half-life – normal/ESRD (hrs)      :7–12/Unchanged

    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                :Not dialysed. Dose as in normal renal function
  • HD                     :Not dialysed. Dose as in normal renal function
  • HDF/high flux   :Not dialysed. Dose as in normal renal function
  • CAV/VVHD      :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: concentration reduced by phenytoin and possibly carbamazepine, barbiturates and primidone
  • Antifungals: metabolism possibly inhibited by itraconazole and ketoconazole avoid; avoid with fluconazoleAntihypertensives: 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 ritonavir
  • Grapefruit juice: concentration increased – avoid concomitant useTheophylline: possibly increased theophylline concentration

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral

    Rate of Administration

    –

    Comments

    –

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