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Celiprolol

Editor: Updated Class:

ADMINISTRATION ROUTES:

PO

ALTERNATIVE NAMES:

Celol, Selectol

ICU INDICATIONS:

  1. Hypertension
  2. Acute myocardial infarction
  3. Secondary prevention in patients with coronary artery disease
  4. Angina
  5. Rate control

Note: Celiprolol may be used with caution in patients with asthma or COPD (see WARNINGS)

PRESENTATION AND ADMINISTRATION:

PO:

Celol 200 mg tablets (yellow)

Should be taken on an empty stomach. Absorption is significantly affected by food. Unknown effects with NG feed – consider alternatives.

DOSAGE:

PO:

Begin at 200 mg once daily. Increase to up to 600 mg daily

DOSAGE IN RENAL FAILURE AND RENAL REPLACEMENT THERAPY:

Dose in renal impairment

GFR (ml/min) DOSE
<10 150-300 mg once daily
10-20 dose as in normal renal function
>20-50 dose as in normal renal function

Dose in renal replacement therapy

MODALITY DOSE
CAPD 150-300 mg once daily
HD 150-300 mg once daily
CVVHDF dose as in normal renal function

DOSAGE IN PAEDIATRICS: PO:

5-10 mg/kg once daily

CLINICAL PHARMACOLOGY:

Celiprolol is a cardioselective beta-blocker, whose beta-blocking action results from a selective competitive blockade at the level of the beta-1 receptors; it is a partial agonist at beta-2 receptors. The vasodilative effect of Celiprolol probably results in part from its partial agonist properties at the level of the beta-2 receptors. Celiprolol lacks a membrane stabilising effect. It is devoid of any cardiodepressive effect at the doses used in clinical practice. It does not appear to have bronchoconstrictive effect at therapeutic doses.

CONTRAINDICATIONS:

  1. Sinus bradycardia
  2. Heart block greater than first degree
  3. Cardiogenic shock
  4. Overt cardiac failure

WARNINGS:

Cardiac Failure

Sympathetic stimulation is necessary in supporting circulatory function in congestive heart failure, and beta blockade carries the potential hazard of further depressing myocardial contractility and precipitating more severe failure.

Discontinuation of therapy

Discontinuation of therapy in a patient with coronary artery disease may lead to rebound angina, arrhythmia or myocardial infarction.

Diabetes and Hypoglycaemia

Beta blockers may mask tachycardia occurring with hypoglycaemia.

Thyrotoxicosis

Beta-adrenergic blockade may mask certain clinical signs (e.g., tachycardia) of hyperthyroidism. Abrupt withdrawal of beta blockade might precipitate a thyroid storm.

Asthma

Due to its beta-1 selective blocking and beta-2 agonist properties, celiprolol may be used with caution in asthmatics out of acute episodes and in patients with compensated chronic obstructive pulmonary disease (see CLINICAL PHARMACOLOGY). It may still precipitate bronchospasm in these patients and should be used with caution.

PRECAUTIONS:

General:

Celiprolol may aggravate peripheral arterial circulatory disorders

Laboratory Tests:

No tests in addition to routine ICU tests are required

Drug/Laboratory Test Interactions:

None known

IMPORTANT DRUG INTERACTIONS IN ICU:

Beta blockers may exacerbate the rebound hypertension which can follow the withdrawal of clonidine

ADVERSE REACTIONS:

Body as a Whole:

Tiredness, fatigue

Cardiovascular System:

Bradycardia , cold extremities, hypotension, leg pain

Respiratory System:

Wheeziness, dyspnoea

Digestive System:

Diarrhoea, nausea

Nervous System:

Dizziness, vertigo, light-headedness