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

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Route

Oral

Rate of Administration

N/A

Comments

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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

See how to identify renal failure stages according to GFR calculation

See how to diagnose irreversible renal disease

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