Wirkstoffe & Arzneimittelsicherheit

Wechselwirkungen · Intelence

INTELENCE 25 mg tablets INTELENCE 100 mg tablets INTELENCE 200 mg tablets · Abschnitt 4.5 · PDF-Seite 13–14

HOS-119744 · Präparat HOS-095005

13  IMMUNOSUPPRESSANTS Cyclosporin Not studied. Etravirine is expected to decrease Co-administration with Sirolimus plasma concentrations of cyclosporine, systemic Tacrolimus sirolimus and tacrolimus. immunosuppressants should be done with caution because plasma concentrations of cyclosporin, sirolimus and tacrolimus may be affected when co-administered with INTELENCE. NARCOTIC ANALGESICS Methadone R(-) methadone No changes in methadone individual dose ranging AUC ↔ 1.06 (0.99-1.13) dosage were required based from 60 mg to 130 mg Cmin ↔ 1.10 (1.02-1.19) on clinical status during or once daily Cmax ↔ 1.02 (0.96-1.09) after the period of S(+) methadone INTELENCE AUC ↔ 0.89 (0.82-0.96) co-administration. Cmin ↔ 0.89 (0.81-0.98) Cmax ↔ 0.89 (0.83-0.97) etravirine AUC ↔a Cmin ↔a Cmax ↔a PHOSPHODIESTERASE, TYPE 5 (PDE-5) INHIBITORS Sildenafil 50 mg single sildenafil Concomitant use of PDE-5 dose AUC ↓ 0.43 (0.36-0.51) inhibitors with INTELENCE Tadalafil Cmin ND may require dose adjustment Vardenafil Cmax ↓ 0.55 (0.40-0.75) of the PDE-5 inhibitor to N-desmethyl-sildenafil attain the desired clinical AUC ↓ 0.59 (0.52-0.68) effect. Cmin ND Cmax ↓ 0.75 (0.59-0.96) PLATELET AGGREGGATION INHIBITORS Clopidogrel In vitro data show that etravirine has inhibitory As a precaution it is properties on CYP2C19. It is therefore possible recommended that that etravirine may inhibit the metabolism of concomitant use of etravirine clopidogrel to its active metabolite by such and clopidogrel should be inhibition of CYP2C19 in vivo. The clinical discouraged. relevance of this interaction has not been demonstrated. PROTON PUMP INHIBITORS Omeprazole etravirine INTELENCE can be 40 mg once daily AUC ↑ 1.41 (1.22-1.62) co-administered with proton Cmin ND pump inhibitors without dose Cmax ↑ 1.17 (0.96-1.43) adjustments. SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRIS) Paroxetine paroxetine INTELENCE can be 20 mg once daily AUC ↔ 1.03 (0.90-1.18) co-administered with Cmin ↓ 0.87 (0.75-1.02) paroxetine without dose Cmax ↔ 1.06 (0.95-1.20) adjustments. etravirine AUC ↔ 1.01 (0.93-1.10) Cmin ↔ 1.07 (0.98-1.17) Cmax ↔ 1.05 (0.96-1.15) a Comparison based on historic control. b Study was conducted with tenofovir disoproxil fumarate 300 mg once daily Note: In drug-drug interaction studies, different formulations and/or doses of etravirine were used which led to similar exposures and, therefore, interactions relevant for one formulation are relevant for the other.

Originalpassage; keine automatisch abgeleitete Schwere, Häufigkeit oder Kausalität. Auch verneinte Befunde und nicht untersuchte Kombinationen bleiben sichtbar.

RxNorm-Namen im Text (wörtliche Treffer, Rolle nicht bewertet): paroxetine (HOS-086246) tadalafil (HOS-086316) methadone (HOS-086198) serotonin (HOS-085477) clopidogrel (HOS-087927) tacrolimus (HOS-085202) tenofovir disoproxil fumarate (HOS-110471) sirolimus (HOS-085172) sildenafil (HOS-086162) cyclosporine (HOS-084512) omeprazole (HOS-085912) vardenafil (HOS-086163)