CLINICAL USE

Beta-1 adrenoceptor blocker:Hypertension Angina Arrhythmias Anxiety

DOSE IN NORMAL RENAL FUNCTION

Hypertension, angina: 80–160 mg daily in 2–3 divided doses; maximum 320 mg dailyArrhythmias: 40–240 mg daily in 2–3 divided dosesAnxiety: 40–80 mg daily in 1–2 divided doses

PHARMACOKINETICS

  • Molecular weight                           :301.8
  • %Protein binding                           :70–80
  • %Excreted unchanged in urine     : <3
  • Volume of distribution (L/kg)       :1.2
  • half-life – normal/ESRD (hrs)      :1–2/unchanged

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50     : Dose as in normal renal function
  • 10 to 20     : Dose as in normal renal function
  • <10           : Dose as in normal renal function

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Unlikely dialysability. Dose as in normal renal function.
  • HD                     :Unlikely dialysability. Dose as in normal renal function.
  • HDF/high flux   :Unknown dialysability. Dose as in normal renal function
  • CAV/VVHD      :Unknown dialysability. Dose as in normal renal function

    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 first dose hypotensive effect with post-synaptic alpha-blockers such as prazosin; increased risk of withdrawal hypertension with clonidine; increased risk of bradycardia and AV block with diltiazem; severe hypotension and heart failure occasionally with nifedipine; asystole, severe hypotension and heart failure with verapamil
  • Antimalarials: increased risk of bradycardia with mefloquine
  • Antipsychotics: enhanced hypotensive effect with phenothiazines
  • Diuretics: enhanced hypotensive effect
  • Moxisylyte: possibly severe postural hypotensionSevere hypertension with adrenaline and noradrenaline (especially with non-selective beta-blockers) and possibly with dopamineTropisetron: increased risk of ventricular arrhythmias – use with caution

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral

    Rate of Administration

    –

    Comments

    –

    OTHER INFORMATION

    Use with caution in patients with chronic obstructive airways disease, asthma or diabetesRhabdomyolysis with myoglobinuria has been reported in severe overdosage with oxprenolol

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