Celiprolol: cardioselective beta blocker with beta 2 agonism
Celiprolol (brand names Selectol, Celipres) is a beta 1 selective adrenoceptor antagonist with additional beta 2 agonism and vasodilator action. This unusual combination distinguishes it from classical beta blockers such as propranolol or metoprolol. In Germany celiprolol is rarely used today; internationally, especially in France and Asia, it has retained an established role in hypertension and angina pectoris.
A particular indication is vascular Ehlers Danlos syndrome (vEDS, type IV). The 2010 BBEST trial showed that celiprolol can reduce the frequency of vascular ruptures in patients with vEDS, leading to recommendations in specialised guidelines.
Mechanism of action
Celiprolol has a multidimensional profile:
- Beta 1 selective antagonism with reduced heart rate, contractility and renin release
- Beta 2 partial agonism with mild bronchodilation and peripheral vasodilation
- Direct vasodilation through beta 2 stimulation of vascular muscle
- Low lipophilicity, hence little central effect with less fatigue or nightmares
These properties make celiprolol theoretically favourable in patients with obstructive airway disease or peripheral circulatory problems, since the classical beta blocker adverse effects are attenuated.
In vEDS celiprolol is thought to reduce wall stress in weakened arterial vessels, lowering the risk of dissection and rupture.
Indications
- Arterial hypertension: classical indication, particularly in France
- Stable angina pectoris: attack prophylaxis
- Vascular Ehlers Danlos syndrome (vEDS): off label or specialised indication to reduce vascular complications
- Asthma associated hypertension: theoretically more favourable than other beta blockers due to beta 2 agonism, clinical data limited
Dosing and administration
Hypertension and angina pectoris: starting dose 200 mg once daily in the morning, stepped up to 400 mg per day.
Vascular Ehlers Danlos syndrome: 200 mg in the morning, stepped up to 400 mg per day (or as tolerated), starting at diagnosis with long term therapy.
Take on an empty stomach, at least 30 minutes before breakfast, since food reduces bioavailability.
Renal impairment: dose adjustment in severe impairment. Liver disease: usually no adjustment needed.
Adverse effects
Common: fatigue (less than with classical beta blockers), sleep disturbance, headache, dizziness, gastrointestinal complaints, dry mouth.
Uncommon: bradycardia (less than with classical beta blockers because of beta 2 agonism), hypotension, cold extremities, visual disturbance.
Rare and very rare: AV block, severe hypotension, bronchospasm (rare due to beta 2 agonism), rash, lupus like reactions, masking of hypoglycaemia in diabetes.
Important points:
- Compared with classical beta blockers less fatigue and bronchospasm; still caution in asthma
- Do not stop abruptly: rebound with raised heart rate and blood pressure possible
- In diabetes hypoglycaemia symptoms can be masked, advise patients
- Inform anaesthesia team before surgery; therapy can usually continue
Interactions
- Other antihypertensives: additive effect, dose adjustment as needed
- Calcium channel blockers (verapamil, diltiazem): additive negative inotropic and chronotropic effect, caution
- Digitalis glycosides: additive bradycardia
- Antidiabetics: masking of hypoglycaemia symptoms
- NSAIDs: reduced antihypertensive effect
- Class 1 antiarrhythmics: additive negative inotropic effect
Special considerations
Pregnancy: only with clear indication, data limited.
Breastfeeding: small amounts pass into milk.
Contraindications: cardiogenic shock, severe AV block without pacemaker, sick sinus syndrome, severe bradycardia, acute heart failure, severe asthma in acute phase, phaeochromocytoma without concurrent alpha block.
Vascular Ehlers Danlos syndrome: diagnosis confirmed genetically by COL3A1 mutation. Celiprolol therapy is part of a multimodal concept with lifestyle modification, avoidance of high impact sports, regular imaging of major vessels and close follow up at specialised centres.
End of therapy: taper slowly over at least 2 weeks to avoid rebound.
Patient communication: in vEDS therapy is lifelong. Patients need a sense of self responsibility and realistic expectations about protective effect and limits of pharmacotherapy. In hypertension the focus is on individual selection of the right antihypertensive.
Related substances
- Propranolol, classical non selective beta blocker
- Enalapril, ACE inhibitor as standard antihypertensive
- Nifedipine, calcium channel blocker
- Clopidogrel, platelet inhibitor in cardiovascular care
Frequently asked questions
How does celiprolol differ from other beta blockers?
Celiprolol combines beta 1 antagonism with beta 2 agonism and direct vasodilation. The result is fewer classical beta blocker adverse effects such as fatigue or bronchospasm, with moderate blood pressure lowering and mild peripheral vasodilation. In asthmatics celiprolol is more tolerable than non selective beta blockers but is not entirely risk free.
Why does celiprolol help in vascular Ehlers Danlos syndrome?
In vEDS arteries are structurally weakened by a collagen type III mutation and prone to dissection and rupture. Celiprolol reduces wall stress through a combination of heart rate reduction, mild contractility reduction and peripheral vasodilation. Trials showed a marked reduction in arterial complications.
Can I take celiprolol with asthma?
Because of beta 1 selectivity and beta 2 agonism celiprolol is more tolerable than non selective beta blockers. In acute or severe asthma it should still be used with caution and medical observation. With worsening asthma symptoms therapy should be re evaluated.
How long do I need celiprolol in vEDS?
Lifelong. Vascular Ehlers Danlos syndrome is a genetic chronic disease. Therapy reduces the risk of arterial complications but cannot reverse existing damage. Consistent intake and close follow up at a specialised centre are important.
Sources
- EMA European Medicines Agency
- BfArM German Federal Institute for Drugs and Medical Devices
- AWMF guidelines hypertension and rare diseases
- Gelbe Liste celiprolol monograph
Legal notice and disclaimer
The information on this page is provided for general information only and does not constitute medical advice, diagnosis or treatment recommendation. It does not replace advice from a qualified physician or pharmacist. Medicines should only be used on prescription or after dispensing by a pharmacist. All information is based on the product information available at the time of writing and on recognised scientific sources; the manufacturer's current product information always prevails. Sanoliste assumes no liability for completeness, timeliness or accuracy of the information presented. In a medical emergency call the European emergency number 112.