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

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Route

Oral

Rate of Administration

–

Comments

Take half to one hour before food

See how to identify renal failure stages according to GFR calculation

See how to diagnose irreversible renal disease

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