nebivolol
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 :405.4 (441.9 as hydrochloride) %Protein binding :98 %Excreted unchanged in urine : <0.5 Volume of distribution (L/kg) :11.2half-life – normal/ESRD (hrs) :10 (32–34 in poor hydroxylators) DOSE IN RENAL IMPAIRMENT
GFR (mL/MIN)
20 to 50 : Initial dose 2.5 mg and adjust according to response 10 to 20 : Initial dose 2.5 mg and adjust according to response <10 : Initial dose 2.5 mg and adjust according to response DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES
CAPD :Not dialysed. Dose as for GFR <10 mL/min HD :Not dialysed. Dose as for GFR <10 mL/minHDF/high flux :Unknown dialysability. Dose as for GFR <10 mL/minCAV/VVHD :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 effectAnti-arrhythmics: increased risk of myocardial depression and bradycardia; increased risk of bradycardia, myocardial depression and AV block with amiodaroneAntidepressants: 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 prazosinAntimalarials: 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 dobutamineTropisetron: increased risk of ventricular arrhythmias – use with caution ADMINISTRATION
Reconstition
– Route
Oral Rate of Administration
–Comments
– 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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