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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