Coadministered Drug
(Postulated Mechanism of Interaction is Inhibition of CYP3A4 by posaconazole)
 
Coadministered Drug Dose/Schedule
 
Posaconazole Dose/Schedule
 
Effect on Bioavailability of Coadministered Drugs

Change in Mean Cmax
(ratio estimate*; 90% CI of the ratio estimate)
 
Change in Mean AUC
(ratio estimate*; 90% CI of the ratio estimate)

* Ratio Estimate is the ratio of coadministered drug plus posaconazole to coadministered drug alone for Cmax or AUC.† The tablet refers to a non-commercial tablet formulation without polymer.‡ The mean terminal half-life of midazolam was increased from 3 hours to 7 to 11 hours during coadministration with posaconazole. 
 
Sirolimus 2-mg single oral dose 400 mg (oral suspension) BID × 16 days ↑ 572%
(6.72; 5.62-8.03) ↑ 788%
(8.88; 7.26-10.9)
Cyclosporine Stable maintenance dose in heart transplant recipients 200 mg (tablets) QD × 10 days† ↑ cyclosporine whole blood trough concentrations
Cyclosporine dose reductions of up to 29% were required
Tacrolimus 0.05-mg/kg single oral dose 400 mg (oral suspension) BID × 7 days ↑ 121%
(2.21; 2.01-2.42) ↑ 358%
(4.58; 4.03-5.19)
Simvastatin 40-mg single oral dose 100 mg (oral suspension) QD × 13 days Simvastatin
↑ 841%
(9.41, 7.13-12.44)
Simvastatin Acid
↑ 817%
(9.17, 7.36-11.43) Simvastatin
↑ 931%
(10.31, 8.40-12.67)
Simvastatin Acid
↑634%
(7.34, 5.82-9.25)
  200 mg (oral suspension) QD × 13 days Simvastatin
↑ 1041%
(11.41, 7.99-16.29)
Simvastatin Acid
↑851%
(9.51, 8.15-11.10) Simvastatin
↑ 960%
(10.60, 8.63-13.02)
Simvastatin Acid
↑748%
(8.48, 7.04-10.23)
Midazolam 0.4-mg single IV dose‡ 200 mg (oral suspension) BID × 7 days ↑ 30%
(1.3; 1.13-1.48) ↑ 362%
(4.62; 4.02-5.3)
 0.4-mg single IV dose‡ 400 mg (oral suspension) BID × 7 days ↑62%
(1.62; 1.41-1.86) ↑524%
(6.24; 5.43-7.16)
 2-mg single oral dose‡ 200 mg (oral suspension) QD × 7 days ↑ 169%
(2.69; 2.46-2.93) ↑ 470%
(5.70; 4.82-6.74)
 2-mg single oral dose‡ 400 mg (oral suspension) BID × 7 days ↑ 138%
(2.38; 2.13-2.66) ↑ 397%
(4.97; 4.46-5.54)
Rifabutin 300 mg QD × 17 days 200 mg (tablets) QD × 10 days† ↑ 31%
(1.31; 1.10-1.57) ↑ 72%
(1.72;1.51-1.95)
Phenytoin 200 mg QD PO × 10 days 200 mg (tablets) QD × 10 days† ↑ 16%
(1.16; 0.85-1.57) ↑ 16%
(1.16; 0.84-1.59)
Ritonavir 100 mg QD × 14 days 400 mg (oral suspension)
BID × 7 days ↑ 49%
(1.49; 1.04-2.15) ↑ 80%
(1.8;1.39-2.31)
Atazanavir 300 mg QD × 14 days 400 mg (oral suspension) BID × 7 days ↑ 155%
(2.55; 1.89-3.45) ↑ 268%
(3.68; 2.89-4.70)
Atazanavir/ ritonavir boosted regimen 300 mg/100 mg QD × 14 days 400 mg (oral suspension) BID × 7 days ↑ 53%
(1.53; 1.13-2.07) ↑ 146%
(2.46; 1.93-3.13)
 
Additional clinical studies demonstrated that no clinically significant ef