CLINICAL USE

Hypertension

DOSE IN NORMAL RENAL FUNCTION

250 mg 2–3 times a day, increasing to a maximum dose of 3 g daily

PHARMACOKINETICS

  • Molecular weight                           :238.2
  • %Protein binding                           :<15
  • %Excreted unchanged in urine     : 25–40
  • Volume of distribution (L/kg)       :0.5
  • half-life – normal/ESRD (hrs)      :1.6–2/6–16

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50     : Dose as in normal renal function and adjust according to response
  • 10 to 20     : Dose as in normal renal function and adjust according to response
  • <10           : Dose as in normal renal function and adjust according to response

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Dialysed. Dose as in GFR
  • <10           : mL/min
  • HD                     :Dialysed. Dose as in GFR
  • <10           : mL/min
  • HDF/high flux   :Dialysed. Dose as in GFR
  • <10           : mL/min
  • CAV/VVHD      :Probably dialysed. Dose as in GFR 10 to 20 mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs

  • Anaesthetics: enhanced hypotensive effect
  • Antidepressants: avoid concomitant use with MAOIs
  • Lithium: neurotoxicity (without increased plasma-lithium concentrations)Salbutamol: acute hypotension reported with salbutamol infusions

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral

    Rate of Administration

    –

    Comments

    –

    OTHER INFORMATION

    Active metabolites with long half-life Interferes with serum creatinine measurementOrthostatic hypotension more common in renally impaired patients.

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