celiprolol

Celiprolol is a beta-adrenergic receptor blocker (beta-blocker) with intrinsic sympathomimetic activity and vasodilating properties. It is relatively selective for the beta-1 receptor at therapeutic doses and thus reduces heart rate and myocardial contractility while maintaining some resting sympathetic activity. The vasodilatory effect is thought to involve endothelium-derived nitric oxide.

Uses: Celiprolol has been marketed for the treatment of hypertension, and in some countries is used for angina. It is not licensed in the United States and availability varies internationally.

Pharmacokinetics: It is administered orally. It undergoes hepatic metabolism and is excreted in urine and feces. Onset and duration depend on dose; food effects vary. Dose adjustments may be needed in hepatic impairment.

Adverse effects: Common adverse effects include bradycardia, hypotension, dizziness, fatigue, and cold extremities. As with other beta-blockers, bronchospasm can occur in patients with asthma or COPD. It can mask signs of hypoglycemia in diabetic patients. Caution in patients with conduction abnormalities or heart failure.

Other notes: In vascular Ehlers-Danlos syndrome, a randomized trial reported a reduction in arterial events with celiprolol, but the evidence is limited and guidelines do not universally endorse its use for this indication. In general, consult local guidelines regarding regulatory status and dosing.