nebivolol.txt

CLINICAL USE

Beta-adrenoceptor blocker:Essential hypertension Adjunct in heart failure

DOSE IN NORMAL RENAL FUNCTION

Hypertension: 2.5–5 mg once dailyAdjunct in heart failure: 1.25–10 mg once daily

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :405.4 (441.9 as hydrochloride)

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

%Excreted unchanged in urine &nbsp &nbsp : <0.5

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :11.2

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :10 (32–34 in poor hydroxylators)

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 &nbsp &nbsp : Initial dose 2.5 mg and adjust according to response

10 to 20 &nbsp &nbsp : Initial dose 2.5 mg and adjust according to response

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : Initial dose 2.5 mg and adjust according to response

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Not dialysed. Dose as for GFR <10 mL/min

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Not dialysed. Dose as for GFR <10 mL/min

HDF/high flux &nbsp :Unknown dialysability. Dose as for GFR <10 mL/min

CAV/VVHD &nbsp &nbsp &nbsp:Not dialysed. Dose as for GFR 10 to 20 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 MAOIsAntihypertensives; 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 hypotension

Sympathomimetics: severe hypertension with adrenaline and noradrenaline and possibly with dobutamineTropisetron: 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

38% of the dose is excreted in the urine as active metabolitesIn a trial of 10 patients with renal artery stenosis given nebivolol 5 mg daily, plasma renin activity significantly decreased, although serum aldosterone levels did not change to any great extent. In addition, there was no change in effective renal plasma flow, GFR, renal blood flow, or renal vascular resistance. Renal function remained well-preserved.

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