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)       :11.2
  • half-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/min
  • HDF/high flux   :Unknown dialysability. Dose as for GFR <10 mL/min
  • CAV/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 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

    –

    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.

    • Tags:

    Related News

    ffddfd

    Hyperlipidemia