Interaction Checker
No Interaction Expected
Raltegravir (RAL)
Ethinylestradiol
Quality of Evidence: Low
Summary:
Coadministration of raltegravir and a triphasic oral contraceptive containing ethinylestradiol and norgestimate had no significant effect on ethinylestradiol pharmacokinetics. Exposure of norelgestromin (the active metabolite of norgestimate) increased by 14% (AUC), 29% (Cmax) and 10% (Cmin). The effects are not considered to be clinically important and no dose adjustment is required for oral contraceptives containing ethinylestradiol and norgestimate when coadministered with twice daily or once daily raltegravir. Note, use of ethinylestradiol as part of gender affirming treatment is not recommended due to thrombotic risks.
Description:
Coadministration of ethinylestradiol/norgestimate and raltegravir (400 mg twice daily) decreased ethinylestradiol AUC by 2% and increased Cmax by 6%. Norelgestromin AUC and Cmax increased by 14% and 29%. These findings can be extended to raltegravir 1,200 mg once daily. No dosage adjustment required for raltegravir (400 mg twice daily and 1,200 mg once daily) or hormonal contraceptives (estrogen- and/or progesterone-based).
Isentress 600 mg Summary of Product Characteristics, Merck Sharp & Dohme Ltd, September 2021.
In drug interaction studies performed using raltegravir film-coated tablets 400 mg twice daily dose, raltegravir did not have a clinically meaningful effect on the pharmacokinetics of ethinylestradiol/norgestimate. No dose adjustment is required when raltegravir 400 mg twice daily or 1200 mg once daily is coadministered.
Isentress Prescribing Information, Merck & Co Inc, August 2021.
Coadministration of raltegravir (400 mg twice daily) and a triphasic oral contraceptive containing ethinyl estradiol and norgestimate was studied in 19 HIV- women. Coadministration had no significant effect on ethinyl estradiol pharmacokinetics (2% decrease in AUC, 6% increase in Cmax, 1% increase in Cmin). Exposure of the active metabolite of norgestimate increased by 14% (AUC), 29% (Cmax) and 10% (Cmin). The effects are not considered to be clinically important and no dose adjustment is required for oral contraceptives containing ethinyl estradiol and norgestimate when coadministered with raltegravir.
Effect of raltegravir on estradiol and norgestimate plasma pharmacokinetics following oral contraceptive administration in healthy women. Anderson MS, Hanley WD, Moreau AT, et al. Br J Clin Pharmacol, 2011, 71(4): 616-620.
View all available interactions with Raltegravir (RAL) by clicking here.
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