Celiprolol hydrochloride

CLINICAL USE

Beta-adrenoceptor blocker:

  • Mild to moderate hypertension

    DOSE IN NORMAL RENAL FUNCTION

    200–400 mg daily

    PHARMACOKINETICS

  • Molecular weight                           :416
  • %Protein binding                           :25
  • %Excreted unchanged in urine     : 12–18
  • Volume of distribution (L/kg)       :4.5
  • half-life – normal/ESRD (hrs)      :5–6/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           : Start low – adjust according to response

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Unknown dialysability. Dose as in GFR <10 mL/min
  • HD                     :Unknown dialysability. Dose as in GFR <10 mL/min
  • HDF/high flux   :Unknown dialysability. Dose as in GFR <10 mL/min
  • 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 MAOIs
  • Antihypertensives: 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 mefloquine
  • Antipsychotics 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

  • Take half to one hour before food
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