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Clinical Pharmacology
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Clinical Pharmacology

Sustiva

Table 2: Effect of Coadministered Drug on Efavirenz Plasma Cmax and AUC

  Efavirenz (% change)
Coadministere
d Drug
Dose
Efavirenz
Dose
Number of
Subjects
Cmax
(mean
[90% CI])
AUC
(mean [90%
CI])
Indinavir
800 mg q8h
x 14 days
200 mg x 14
days
11
«
«
Lopinavir/
ritonavir
400/100 mg
q12h x 9
days
600 mg x 9
days
11,12a
«
↓(16%)

[↓38-↑15%]
Nelfinavir
750 mg q8h
x 7 days
600 mg x 7
days
10
«
«
Ritonavir
500 mg q12h
x 8 days
600 mg x 10
days
9
↑(14%)
[4-26%]
↑(21%)
[10-34%]
Saquinavir
SGCb
1200 mg q8h
x 10 days
600 mg x 10
days
13
↓(13%)
[5-20%]
↓(12%)
[4-19%]
Azithromycin
600 mg
single dose
400 mg x 7
days
14
«
«
Clarithromycin
500 mg q12h
x 7 days
400 mg x 7
days
12
↑(11%)
[3-19%]
«
Fluconazole
200 mg x
7 days
400 mg x 7
days
10
«
↑(16%)
[6-26%]
Rifabutin
300 mg qd x
14 days
600 mg x 14
days
11
«
«
Rifampin
600 mg x
7 days
600 mg x 7
days
12
↓(20%)
[11-28%]
↓(26%)
[15-36%]
Aluminum
  hydroxide
  400 mg,
  magnesium
  hydroxide
  400 mg, plus
  simethicone
  40 mg 		30 mL single
dose		 400 mg
single dose		 17 « «
Cetirizine
10 mg single
dose
600 mg x 10
days
11
«
↓(8%)
[4-11%]
Ethinyl
estradiol
50 m g single
dose
400 mg x 10days
13
«
«
Famotidine
40 mg single
dose
400 mg
single dose
17
«
«
Paroxetine
20 mg qd x
14 days
600 mg x 14
days
12
«
«
Sertraline
50 mg qd x
14 days
600 mg x 14
days
13
↑(11%)
[6-16%]
«
Voriconazole
400 mg po
q12h x 1 day
then 200 mg
po q12h x 8
days
 400 mg x 9
days		 ¾ ↑(38%)c ↑(44%)c

↑Indicates increase ¯ Indicates decrease « Indicates no change
aParallel-group design; n for efavirenz + lopinavir/ritonavir, n for efavirenz alone.
bSoft Gelatin Capsule.
c90% CI not available.

Brand Name: Sustiva
Generic Name: Efavirenz
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