Actemra Drug Interactions





Full Prescribing Info
Drug Interactions
Population pharmacokinetic analyses did not detect any effect of MTX, non-steroidal anti-inflammatory drugs or corticosteroids on Actemra clearance in RA patients.
Concomitant administration of a single dose of 10 mg/kg Actemra with 10-25 mg MTX once weekly had no clinically significant effect on MTX exposure.
Actemra has not been studied in combination with other biological DMARDs.
The expression of hepatic CYP450 enzymes is suppressed by cytokines, such as IL-6, that stimulate chronic inflammation. Thus, CYP450 expression may be reversed when potent cytokine inhibitory therapy, such as Actemra is introduced.
In vitro studies with cultured human hepatocytes demonstrated that IL-6 caused a reduction in CYP1A2, CYP2C9, CYP2C19, and CYP3A4 enzyme expression. Actemra normalizes expression of these enzymes.
The effect of Actemra on CYP enzymes (except CYP2C19 and CYP2D6) is clinically relevant for CYP450 substrates with a narrow therapeutic index, where the dose is individually adjusted.
In a study in RA patients, levels of simvastatin (CYP3A4) were decreased by 57% one week following a single dose of Actemra, to the level similar or slightly higher than those observed in healthy subjects.
When starting or stopping therapy with Actemra, patients taking medicinal products, which are individually dose-adjusted and are metabolised via CYP450 3A4, 1A2, or 2C9 (e.g. atorvastatin, calcium channel blockers, theophylline, warfarin, phenytoin, ciclosporin, or benzodiazepines) should be monitored as doses of these products may need to be adjusted to maintain their therapeutic effect. Given its long elimination half-life (t1/2), the effect of Actemra on CYP450 enzyme activity may persist for several weeks after stopping therapy.
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