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Rescriptor

Clinical Pharmacology
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Clinical Pharmacology

In vitro and in vivo studies have shown that delavirdine reduces CYP3A activity and inhibits its own metabolism. In vitro studies have also shown that delavirdine reduces CYP2C9, CYP2D6, and CYP2C19 activity. Inhibition of hepatic CYP3A activity by delavirdine is reversible within 1 week after discontinuation of drug.

Special Populations

Hepatic or Renal Impairment: The pharmacokinetics of delavirdine in patients with hepatic or renal impairment have not been investigated (see PRECAUTIONS).

Age: The pharmacokinetics of delavirdine have not been adequately studied in patients <16 years or >65 years of age.

Gender: Data from population pharmacokinetics suggest that the plasma concentrations of delavirdine tend to be higher in females than in males. However, this difference is not considered to be clinically significant.

Race: No significant differences in the mean trough delavirdine concentrations were observed between different racial or ethnic groups.

Drug Interactions (see also PRECAUTIONS: DRUG INTERACTIONS)

Specific drug interaction studies were performed with delavirdine and a number of drugs. Table 1 summarizes the effects of delavirdine on the geometric mean AUC, Cmax and Cmin of coadministered drugs. Table 2 shows the effects of coadministered drugs on the geometric mean AUC, Cmax and Cmin of delavirdine.

FOR INFORMATION REGARDING CLINICAL RECOMMENDATIONS, SEE CONTRAINDICATIONS, WARNINGS, AND PRECAUTIONS: DRUG INTERACTIONS.

Table 1. Pharmacokinetic Parameters for Coadministered Drugs in the Presence of Delavirdine.

Coadministered Drug
Dose of
Coadministered Drug
Dose of
RESCRIPTOR
n
% Change in Pharmacokinetic Parameters of Coadministered Drug (90% CI)
Cmax
AUC
Cmin
HIV-Protease Inhibitors
Indinavir
400 mg tid
x 7 days
400 mg tid
x 7 days
28
¯36*
(¯52-¯14)
«*
↑118*
(↑16-↑312)
 
600 mg tid
x 7 days
400 mg tid
x 7 days
28
«
↑53*
(↑7-↑120)
↑298*
(↑104- ↑678)
Nelfinavir
750 mg tid
x 14 days
400 mg tid
x 7 days
12
↑88
(↑66-↑113)
↑107
(↑83-↑135)
↑136
(↑103- ↑175)
Saquinavir
Soft gel
capsule 1000
mg tid
x 28 days
400 mg tid
x 28 days
20
↑98
(↑4-↑277)
↑121
(↑14-↑340)
↑199
(↑37-↑553)
Nucleoside Reverse Transcriptase Inhibitors
Didanosine
(buffered
tablets)
125 or 250 mg
bid x 28 days
400 mg tid x
28 days
9
¯20§
(¯44-↑15)
¯21§
(¯40-↑5)
-
200 mg tid
for >38 days
100 mg qid to
400 mg tid for
8-10 days
34
«
«
-
Clarithromycin
500 mg bid
x 15 days
300 mg tid
x 30 days
6
-
↑100
-
Rifabutin
300 mg qd for
15-99 days
400-1000 mg
tid for 45-129
days
5
↑128
(↑71-↑203)
↑230
(↑119- ↑396)
↑452
(↑246- ↑781)
Brand Name: Rescriptor
Generic Name: Delavirdine Mesylate
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