Monograph
R01AD12 - Fluticasone Furoate |
Propably not porphyrinogenic |
PNP |
Rationale
Plasma concentration is not quantifiable following nasal administration of fluticasone furoate, and hepatic exposure is therefore insignificant.
Chemical description
Corticosteroid ester
Therapeutic characteristics
Fluticasone furoate nasal spray is indicated for the treatment of the symptoms of allergic rhinitis.
Hepatic exposure
Following intranasal dosing of 110 µg fluticasone furoate (maximum recommended dose) once daily the plasma concentration was < 10 pg/mL (Rosenblut 2007). This is equivalent to 18.5 pM and systemic exposure is therefore insignificant.
Metabolism and pharmacokinetics
Fluticasone furoate is rapidly and extensively metabolized by CYP3A4 (SPC).
Fluticasone furoate is not suspected to be an inducer or a mechanism-based inhibitor of CYP enzymes (Hisaka 2010, Isoherranen 2009, Pelkonen 2008). There are no drug-drug interactions with fluconasole furoate as perpetrator (interaktionsdatabasen.dk, SPC).
IPNet drug reports
Uneventful use reported in 1 patient with acute porphyria.
References
| # | Citation details | PMID |
|---|---|---|
| * | Scientific articles | |
| 1. | Prediction of pharmacokinetic drug-drug interaction caused by changes in cytochrome P450 activity using in vivo information.
Hisaka A, Ohno Y, et al. Pharmacol Ther. 2010 Feb;125(2):230-48. |
|
| 2. | Qualitative analysis of the role of metabolites in inhibitory drug-drug interactions: literature evaluation based on the metabolism and transport drug interaction database.
Isoherranen N, Hachad H, et al. Chem Res Toxicol. 2009 Feb;22(2):294-8. |
|
| 3. | Inhibition and induction of human cytochrome P450 enzymes: current status.
Pelkonen O, Turpeinen M, et al. Arch Toxicol. 2008 Oct;82(10):667-715. |
18618097 |
| 4. | Long-term safety of fluticasone furoate nasal spray in adults and adolescents with perennial allergic rhinitis.
Rosenblut A, Bardin PG, et al. Allergy. 2007 Sep;62(9):1071-7. |
17686110 |
| * | Drug interaction databases | |
| 5. | Interaktionsdatabasen. Fluticasone furoate.
|
|
| * | Summary of Product Characteristics | |
| 6. | The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). (Avamys).
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