CLINICAL USE


Calcium-channel blocker:Hypertension Angina

DOSE IN NORMAL RENAL FUNCTION

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

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :388.4
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :>99
  • %Excreted unchanged in urine &nbsp &nbsp :
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp :

  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :2.3–7.1

  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :7–12/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
  • <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:Not dialysed. Dose as in normal renal function

  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Not dialysed. Dose as in normal renal function
  • HDF/high flux &nbsp :Not dialysed. Dose as in normal renal function
  • CAV/VVHD &nbsp &nbsp &nbsp: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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