CLINICAL USE

Beta-adrenoceptor blocker:Hypertension Angina Arrhythmias Migraine Thyrotoxicosis

DOSE IN NORMAL RENAL FUNCTION

Hypertension: 80–240 mg per day Angina, arrhythmias, migraine: 40–160 mg dailyThyrotoxicosis: 80–160 mg daily

PHARMACOKINETICS

  • Molecular weight                           :309.4
  • %Protein binding                           :30
  • %Excreted unchanged in urine     : 73
  • Volume of distribution (L/kg)       :1.9
  • half-life – normal/ESRD (hrs)      :12–24/45

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50     : Start with low dose and increase according to response
  • 10 to 20     : Start with low dose and increase according to response
  • <10           : Start with low dose and increase according to response

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Dialysed. Dose as in GFR
  • <10           : mL/min
  • HD                     :Dialysed. Dose as in GFR
  • <10           : mL/min
  • HDF/high flux   :Dialysed. Dose as in GFR
  • <10           : mL/min
  • CAV/VVHD      :Dialysed. Dose as in GFR=10–20 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

    SPC guidelines for increasing dosing interval for patients with renal impairment may be impractical with respect to patient complianceUnlike most other beta-blockers, nadolol is not metabolised and is excreted unchanged mainly by the kidneys.

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