Carvedilol

CLINICAL USE

Beta-adrenoceptor blocker with alpha1-blocking action:

Hypertension, angina and heart failure

DOSE IN NORMAL RENAL FUNCTION

Hypertension: 12.5–50 mg daily in single or divided doses

Angina: 12.5–25 mg twice daily

Heart failure: 3.125–25 mg twice daily (50 mg twice daily if wt>85 kg)

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :406.5

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :>98

%Excreted unchanged in urine &nbsp &nbsp : <2

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :2

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :6–10/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:Unlikely dialysability. Dose as in normal renal function. Start with low doses and titrate according to response

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Not dialysed. Dose as in normal renal function. Start with low doses and titrate according to response

HDF/high flux &nbsp :Unknown dialysability. Dose as in normal renal function. Start with low doses and titrate according to response

CAV/VVHD &nbsp &nbsp &nbsp:Unlikely dialysability. Dose as in normal renal function. Start with low doses and titrate according to response

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Anaesthetics: enhanced hypotensive effect Analgesics: NSAIDs antagonise hypotensive effectAnti-arrhythmics: increased risk of myocardial depression and bradycardia; increased risk of bradycardia, myocardial depression and AV block with amiodarone

Antibacterials: concentration reduced by rifampicin

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 mefloquine

Antipsychotics 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

Ciclosporin: increased trough concentration, reduce dose by 20% in affected patients

Diuretics: enhanced hypotensive effect Moxisylyte: possible severe postural hypotension

Sympathomimetics: 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

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Comments

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OTHER INFORMATION

First pass elimination of 60–75% following oral administration

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