Efavirenz (Page 7 of 11)
Table 8: Effect of Coadministered Drug on Efavirenz Plasma C max , AUC, and C min
Coadministered Drug | Dose | Efavirenz Dose | Number of subjects | Efavirenz (mean % change) | ||
C max (90% CI) | AUC (90% CI) | C min (90%CI) | ||||
Indinavir | 800 mg q8h x 14 days | 200 mg qd x 14 days | 11 | ↔ | ↔ | ↔ |
Lopinavir/ritonavir | 400/100 mg q12h x 9 days | 600 mg qd x 9 days | 11,12 a | ↔ | ↓ 16% (↓ 38-↑15%) | ↓ 16% (↓ 42-↑20%) |
Nelfinavir | 750 mg q8h x 7 days | 600 mg qd x 7 days | 10 | ↓ 12% (↓ 32-↑13%) b | ↓ 12% (↓ 35-↑18%) b | ↓ 21% (↓ 53-↑33%) |
Ritonavir | 500 mg q12h x 8 days | 600 mg qd x 10 days | 9 | ↑ 14% (4-26%) | ↑ 21% (10-34%) | ↑ 25% (7-46%) b |
Saquinavir SGC c | 1200 mg q8h x 10 days | 600 mg qd x 10 days | 13 | ↓ 13% (5-20%) | ↓ 12% (4-19%) | ↓ 14% (2-24%) b |
Tenofovir d | 300 mg qd | 600 mg qd x 14 days | 30 | ↔ | ↔ | ↔ |
Boceprevir | 800 mg tid x 6 days | 600 mg qd x 16 days | NA | ↑ 11% (2-20%) | ↑ 20% (15-26%) | NA |
simeprevir | 150 mg qd x 14 days | 600 mg qd x 14 days | 23 | ↔ | ↓ 10% (5-15%) | ↓ 13% (7-↑19%) |
Azithromycin | 600 mg single dose | 400 mg qd x 7 days | 14 | ↔ | ↔ | ↔ |
Clarithromycin | 500 mg q12h x 7 days | 400 mg qd x 7 days | 12 | ↑ 11% (3-19%) | ↔ | ↔ |
Fluconazole | 200 mg x 7 days | 400 mg qd x 7 days | 10 | ↔ | ↑ 16% (6-26%) | ↑ 22% (5-41%) |
Itraconazole | 200 mg q12h x 14 days | 600 mg qd x 28 days | 16 | ↔ | ↔ | ↔ |
Rifabutin | 300 mg qd x 14 days | 600 mg qd x 14 days | 11 | ↔ | ↔ | ↓ 12% (↓ 24-↑1%) |
Rifampin | 600 mg x 7 days | 600 mg qd x 7 days | 12 | ↓ 20% (11-28%) | ↓ 26% (15-36%) | ↓ 32% (15-46%) |
Voriconazole | 400 mg po q12h x 1 day, then 200 mg po q12h x 8 days 300 mg po q12h days 2-7 400 mg po q12h days 2-7 | 400 mg qd x 9 days 300 mg qd x 7 days 300 mg qd x 7 days | NA NA NA | ↑ 38% e ↓ 14% f (7-21%) ↔ f ↔ | ↑ 44% e ↔ f ↑ 17% f (6-29%) | NA NA NA |
Artemether/ Lumefantrine | Artemether 20 mg/ lumefantrine 120 mg tablets (6 4-tablet doses over 3 days) | 600 mg qd x 26 days | 12 | ↓ 17% | NA | |
Atorvastatin | 10 mg qd x 4 days | 600 mg qd x 15 days | 14 | ↔ | ↔ | ↔ |
Pravastatin | 40 mg qd x 4 days | 600 mg qd x15 days | 11 | ↔ | ↔ | ↔ |
Simvastatin | 40 mg qd x 4 days | 600 mg qd x 15 days | 14 | ↓ 12% (↓ 28-↑ 8%) | ↔ | ↓ 12% (↓ 25-↑ 3%) |
Aluminum hydroxide 400 mg, magnesium hydroxide 400 mg, plus simethicone 40 mg | 30 mL single dose | 400 mg single dose | 17 | ↔ | ↔ | NA |
Carbamazepine | 200 mg qd x 3 days, 200 mg bid x 3 days, then 400 mg qd x 15 days | 600 mg qd x 35 days | 14 | ↓ 21% (15-26%) | ↓ 36% (32-40%) | ↓ 47% (41-53%) |
Cetirizine | 10 mg single Dose | 600 mg qd x 10 days | 11 | ↔ | ↔ | ↔ |
Diltiazem | 240 mg x 14 days | 600 mg qd x 28 days | 12 | ↑ 16% (6-26%) | ↑ 11% (5-18%) | ↑ 13% (1-26%) |
Famotidine | 40 mg single Dose | 400 mg single dose | 17 | ↔ | ↔ | NA |
Paroxetine | 20 mg qd x 14 days | 600 mg qd x 14 days | 12 | ↔ | ↔ | ↔ |
Sertraline | 50 mg qd x 14 days | 600 mg qd x 14 days | 13 | ↑ 11% (6-16%) | ↔ | ↔ |
↑ Indicates increase ↓ Indicates decrease « Indicates no change or a mean increase or decrease of <10%.
a Parallel-group design; n for efavirenz + lopinavir/ritonavir, n for efavirenz alone.
b 95% CI.
c Soft Gelatin Capsule.
d Tenofovir disoproxil fumarate.
e 90% CI not available.
f Relative to steady-state administration of efavirenz (600 mg once daily for 9 days).
NA = not available.
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