For the oral lead-in rilpivirine treatment and in case missed doses are replaced by oral rilpivirine treatment, refer to the oral rilpivirine tablet package insert for information about drug interactions.
Medicinal products that affect rilpivirine exposure: Rilpivirine is primarily metabolised by cytochrome P450 (CYP)3A. Medicinal products that induce or inhibit CYP3A may thus affect the clearance of rilpivirine (see Pharmacology: Pharmacokinetics under Actions).
Co-administration of rilpivirine and medicinal products that induce CYP3A has been observed to decrease the plasma concentrations of rilpivirine, which could reduce the therapeutic effect of rilpivirine.
Co-administration of rilpivirine and medicinal products that inhibit CYP3A has been observed to increase the plasma concentrations of rilpivirine.
When using oral rilpivirine, proton pump inhibitors are contraindicated (see rilpivirine tablet package insert, Contraindications).
Medicinal products that are affected by the use of rilpivirine: Rilpivirine is not likely to have a clinically relevant effect on the exposure of medicinal products metabolised by CYP enzymes.
Rilpivirine inhibits P-glycoprotein in vitro (IC50 is 9.2 μM). In a clinical study, oral rilpivirine (25 mg once daily) did not significantly affect the pharmacokinetics of digoxin.
Rilpivirine is an in vitro inhibitor of the transporter MATE-2K with an IC50 of <2.7 nM. The clinical implications of this finding are currently unknown.
Interaction table: Selected established and theoretical interactions between rilpivirine and co-administered medicinal products are listed in Tables 12a and 12b and are based on the studies conducted with oral rilpivirine or are potential drug interactions that may occur (increase is indicated as "↑", decrease as "↓", no change as "↔", not applicable as "NA", confidence interval as "CI"). (See Tables 12a and 12b.)
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QT prolonging medicinal products: Oral rilpivirine at the recommended dose of 25 mg once daily is not associated with a clinically relevant effect on QTc. Rilpivirine plasma concentrations after REKAMBYS injections at the recommended dose of 600 mg monthly or 900 mg every 2 months, are comparable to those achieved with oral rilpivirine at a dose of 25 mg qd. In a study of healthy subjects, supratherapeutic doses of oral rilpivirine (75 mg once daily and 300 mg once daily) have been shown to prolong the QTc interval of the ECG (see Pharmacology: Pharmacodynamics under Actions). REKAMBYS should be used with caution when co-administered with a medicinal product with a known risk of Torsade de Pointes (see Precautions).