CLINICAL USE


Beta-adrenoceptor blocker:Hypertension Phaeochromocytoma Angina Arrhythmias Anxiety Migraine prophylaxis

DOSE IN NORMAL RENAL FUNCTION

Hypertension: 40–160 mg twice daily Phaeochromocytoma: 60 mg daily for 3 days before surgery, or 30 mg daily if unsuitable for surgeryAngina: 120–240 mg daily in divided doses Arrhythmias: 10–40 mg 3–4 times daily Anxiety: 40 mg 1–3 times daily Prophylaxis after an MI: 40 mg 4 times daily then 80 mg twice dailyMigraine and essential tremor: 80–160 mg dailyIV: 1 mg over 1 minute repeated after 2 minutes to a maximum of 10 mg (5 mg with anaesthesia)

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :295.8
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :80–95
  • %Excreted unchanged in urine &nbsp &nbsp : <5
  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :4
  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :2–6/Unchanged

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50 &nbsp &nbsp : Dose as in normal renal function
  • 10 to 20 &nbsp &nbsp : Start with small doses and increase according to response
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : Start with small doses and increase according to response

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Not dialysed. Dose as in GFR <10 mL/min
  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Not dialysed. Dose as in GFR <10 mL/min
  • HDF/high flux &nbsp :Unknown dialysability. Dose as in GFR <10 mL/min
  • CAV/VVHD &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in GFR 10 to 20 mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs

  • Anaesthetics: enhanced hypotensive effect; risk of bupivacaine toxicity increased
  • 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; concentration increased by propafenone
  • Antibacterials: metabolism increased by rifampicin
  • Antidepressants: enhanced hypotensive effect with MAOIs; concentration increased by fluvoxamine; concentration of imipramine increasedAntihypertensives; 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; concentration of both drugs increased with chlorpromazine
  • 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 hypotensionPropranolol hydrochloride.618 PROPRANOLOL HYDROCHLORIDe
  • Sympathomimetics: severe hypertension with adrenaline and noradrenaline and possibly with dobutamineTropisetron: increased risk of ventricular arrhythmias – use with caution

    ADMINISTRATION

    Reconstition

    Route

    Oral, IV

    Rate of Administration

    Comments

    OTHER INFORMATION

    Non-selective active metabolites accumulate in renal impairment. Consider metoprolol or atenololMay reduce renal blood flow in severe renal impairment.
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