Celiprolol

Products

Celiprolol is commercially available in the form of film-coated tablets (Selectol). It has been approved in many countries since 1987.

Structure and properties

Celiprolol (C20H34ClN3O4, Mr = 415.95 g/mol is a racemate and is present in drugs as celiprolol hydrochloride, a white to pale yellow crystalline powder that is readily soluble in water.

Effects

Celiprolol (ATC C07AB08) has antihypertensive, vasodilator, and antianginal properties. It is a hydrophilic, beta1-selective beta-blocker with intrinsic sympathomimetic activity. The effects are due to competitive and selective antagonism at beta1-adrenoceptors. Celiprolol additionally stimulates beta2 receptors. The half-life is approximately 4 to 5 hours.

Indications

For the treatment of hypertension and angina pectoris (coronary artery disease).

Dosage

According to the SmPC. The tablets are usually taken once daily on an empty stomach.

Contraindications

  • Hypersensitivity
  • Cardiogenic shock
  • Bradycardia
  • SA block, AV block
  • Sinus node syndrome
  • Decompensated heart failure
  • Uremia
  • Asthma attack
  • Untreated pheochromocytoma

For complete precautions, see the drug label.

Interactions

Drug-drug interactions have been described with the following agents:

  • Calcium channel blockers, dihydropiridines.
  • MAO inhibitors
  • Antiarrhythmics
  • Clonidine, guanethidine, reserpine
  • Antidiabetics, insulins
  • NSAIDS
  • Tricyclic antidepressants, phenothiazines
  • Alcohol
  • Narcotics
  • Mefloquine

Adverse effects

The most common possible adverse effects include headache, fatigue, dizziness, insomnia, nightmares, and gastrointestinal disturbances.