Roche Updates Package Insert for HIV Protease Inhibitor Saquinavir (Invirase)

Invirase Tablet

Roche Laboratories, Inc. has updated the package insert for their protease inhibitor, saquinavir (Invirase) to include the following drug interaction information and new warnings regarding co-administration of ritonavir-boosted saquinavir with digoxin (used in the treatment of various cardiac conditions).

Updated drug interaction information for 5 products has been added in the package insert revision:

1. Digoxin (see Warnings; see also Clinical Pharmacology Table 2, Precautions, Drug Interactions, Table 6) -- A new warning has been added. Caution should be exercised when saquinavir and digoxin are co-administered. Co-administration results in a significant increase in serum concentration of digoxin; therefore, the serum concentration of digoxin should be monitored and the dose of digoxin may need to be reduced.

2. Garlic capsules (see Warnings; see also Precautions, Drug Interactions) --No data are available for the co-administration of saquinavir/ritonavir with garlic capsules. A warning has been added that the co-administration of garlic capsules and saquinavir is not recommended due to the potential for garlic capsules to induce the metabolism of saquinavir, which may result in sub-therapeutic saquinavir concentrations.

3. Methadone (see Precautions, Drug Interactions; see also Clinical pharmacology, Table 2) -- Methadone levels are decreased and the dosage of methadone may need to be increased when co-administered with saquinavir/ritonavir.

4. Tipranavir/ritonavir (Aptivus/ritonavir) (see Precautions, Drug Interactions) -- Combining saquinavir with tipranavir/ritonavir is not recommended due to a decrease in saquinavir levels with co-administration.

5. Omeprazole (see Precautions, Drug Interactions) -- When saquinavir/ritonavir is co-administered with omeprazole, saquinavir concentrations are increased significantly. If omeprazole or another proton pump inhibitor is taken concomitantly with saquinavir/ritonavir, caution is advised and monitoring for potential saquinavir toxicities is recommended, particularly gastrointestinal symptoms, increased triglycerides, and deep vein thrombosis.

6/13/08

Sources
R Klein (Office of Special Health Issues) and K Struble (Division of Antiviral Drug Products). U.S. Food and Drug Administration (FDA). June 10, 2008.