.Pharmacolibrary.Drugs.R_RespiratorySystem.R06A_AntihistaminesForSystemicUse.R06AX02_Cyproheptadine.Cyproheptadine

Information

Cyproheptadine is a first-generation antihistamine with anticholinergic, antiserotonergic, and sedative properties. It is primarily used for the symptomatic relief of allergic conditions such as rhinitis, urticaria, and conjunctivitis. It has also been used for appetite stimulation, migraine prophylaxis, and treatment of serotonin syndrome. Cyproheptadine is an approved drug and is available in many countries.

Pharmacokinetics

Pharmacokinetic parameters for healthy adult volunteers after a single oral dose.

References

1. Paton, DM, & Webster, DR (1985). Clinical pharmacokinetics of H1-receptor antagonists (the antihistamines). Clinical pharmacokinetics 10(6) 477–497. DOI:10.2165/00003088-198510060-00002 PUBMED:https://pubmed.ncbi.nlm.nih.gov/2866055

2. Peña, J, et al., & Merlos, M (2008). Antihistaminic effects of rupatadine and PKPD modelling. European journal of drug metabolism and pharmacokinetics 33(2) 107–116. DOI:10.1007/BF03191027 PUBMED:https://pubmed.ncbi.nlm.nih.gov/18777946

3. Xiong, Y, et al., & Liu, M (2016). CYP3A5*3 and MDR1 C3435T are influencing factors of inter-subject variability in rupatadine pharmacokinetics in healthy Chinese volunteers. European journal of drug metabolism and pharmacokinetics 41(2) 117–124. DOI:10.1007/s13318-014-0236-3 PUBMED:https://pubmed.ncbi.nlm.nih.gov/25427746

Revisions

• 06/2025 initial generated model