Acebutolol

CLINICAL USE

Beta-adrenoceptor blocker:

  • Hypertension
  • Angina
  • Arrhythmias

    DOSE IN NORMAL RENAL FUNCTION

  • Hypertension: 400 mg once a day or 200 mg twice a day, increased after 2 weeks to 400 mg twice daily if necessary
  • Angina: 400 mg once a day, or 200 mg twice daily initially. Increase up to 300 mg 3 times daily; maximum 1200 mg
  • Arrhythmias: 400–1200 mg/day (in 2–3 divided doses)

    PHARMACOKINETICS

  • Molecular weight                           :336.4 (372.9 as hydrochloride)
  • %Protein binding                           :26
  • %Excreted unchanged in urine     : 55
  • Volume of distribution (L/kg)       :1.2
  • half-life – normal/ESRD (hrs)      :3–4 (8–13 for active metabolite)/Increased (32 for active metabolite)

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

    25–50 Dose as in normal renal function, but frequency should not exceed once daily in renal impairment10–25 50% of normal dose, but frequency should not exceed once daily in renal impairment

  • <10           : 30–50% of normal dose, but frequency should not exceed once daily in renal impairment

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Unknown dialysability. 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      :Dialysed. Dose as in GFR=10–25 mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs

  • Anaesthetics: enhanced hypotensive effect
  • Analgesics: NSAIDs antagonise hypotensive effect
  • Anti-arrhythmics: increased risk of myocardial depression and bradycardia; increased risk of bradycardia, myocardial depression and AV block with amiodarone
  • Antidepressants: enhanced hypotensive effect with MAOIs
  • Antihypertensives: enhanced hypotensive effect; increased risk of withdrawal hypertension with clonidine; increased risk of first dose hypotensive effect with post-synaptic alpha-blockers such as prazosin
  • Antimalarials: increased risk of bradycardia with mefloquineAntipsychotics enhanced hypotensive effect with phenothiazines
  • Calcium-channel blockers: increased risk of bradycardia and AV block with diltiazem; hypotension and heart failure possible with nifedipine and nisoldipine; asystole, severe hypotension and heart failure with verapamil
  • Diuretics: enhanced hypotensive effect
  • Moxisylyte: possible severe postural hypotensionSympathomimetics: severe hypertension with adrenaline and noradrenaline and possibly with dobutamine
  • Tropisetron: increased risk of ventricular arrhythmias – use with caution

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral

    Rate of Administration

    N/A

    Comments

    –

    OTHER INFORMATION

  • Administration of high doses in severe renal failure cautioned due to accumulation
  • Dose frequency should not exceed once daily in renal impairment
  • Has an active metabolite – diacetolol
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