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Rescriptor
Clinical Pharmacology
Rescriptor
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 |
« |
« | - | |
| Anti-infective Agents | ||||||
| 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) |
Generic Name: Delavirdine Mesylate
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