R06AX28 - Rupatadine |
Probably not porphyrinogenic |
PNP |
Rationale
Metabolised by CYP3A4 but not a clinically significant inducer or inhibitor of any CYP450 isoenzymes. No indication of porphyrinogenic effects connected with the pharmacodynamic properties of the medicine.
Chemical description
Rupatadine is a selective histamine H1 receptor antagonist and platelet activating factor (PAF) antagonist.[DrugBank]
Therapeutic characteristics
Rupatadine is used to treat allergic rhinitis. It is administered orally once-daily. [DrugBank]
Metabolism and pharmacokinetics
Rupatadine is metabolised by oxidation, primarily mediated by CYP3A4, with CYP2C9, CYP2C19 and CYP2D6 involved to a lesser extent. [DrugBank] Its active metabolite desloratadine is considered probably not porphyrinogenic.
Rupatadine was shown to inhibit CYP3A4, CYP2C19, CYP2D6 and CYP2E1 in human liver microsomes in vitro. However, these effects were at concentrations >100 times higher than the clinical Cmax, and inhibition at therapeutic concentrations is therefore not expected. [AUSPAR]
Similar drugs
References
| # | Citation details | PubMed ID |
|---|---|---|
| Drug reference publications | ||
| 1. | DrugBank {rupatadine}
Access Date: 2025-November-19 |
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| Summary of Product Characteristics | ||
| 2. | SmPC {Rupatadine}.
Aspire Pharma Ltd. Date of revision of text: 28 March 2022
Access Date: 2026-November-19 |
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| Other sources | ||
| 3. | Other monograph
Therapeutic Goods Administration. Australian Public Assessment Report for Rupatadine (Rupfin). May 2011
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Tradenames