.Pharmacolibrary.Drugs.C_CardiovascularSystem.C07A_BetaBlockingAgents.C07AB08_Celiprolol.Celiprolol

Information

Celiprolol is a selective beta-1 adrenergic receptor antagonist with partial agonist activity at beta-2 receptors. It is used primarily as an antihypertensive agent for the treatment of high blood pressure. Celiprolol is approved for use in several countries, particularly in Europe, but not in the United States.

Pharmacokinetics

Healthy adult volunteers, mostly male, after single oral dosing.

References

1. Ieiri, I, et al., & Sugiyama, Y (2012). Microdosing clinical study: pharmacokinetic, pharmacogenomic (SLCO2B1), and interaction (grapefruit juice) profiles of celiprolol following the oral microdose and therapeutic dose. Journal of clinical pharmacology 52(7) 1078–1089. DOI:10.1177/0091270011408612 PUBMED:https://pubmed.ncbi.nlm.nih.gov/21593283

2. Lipka, E, et al., & Amidon, GL (1995). Celiprolol double-peak occurrence and gastric motility: nonlinear mixed effects modeling of bioavailability data obtained in dogs. Journal of pharmacokinetics and biopharmaceutics 23(3) 267–286. DOI:10.1007/BF02354285 PUBMED:https://pubmed.ncbi.nlm.nih.gov/8834196

Revisions

• 06/2025 initial generated model