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saquinavir

Detailed Prescribing Information

December 2005

 

 

Saquinavir = Fortovase and Invirase
500 mg hard gel cap (Invirase) FDA Approved 12.20.2004 & available 2.18.2005
Dosing Forms 200 mg soft gel caps (Fortovase)
200 mg or 500 mg hard gel caps (Invirase)
Dosing Without boosting: 8x200 mg soft gel caps twice a day with food or 6x200 mg soft gel caps three times a day with food [strongly consider boosting if possible]

With boosting twice a day: 2x500 mg or 5x200 mg hard gel caps + 100 mg ritonavir, both twice a day with food

With boosting once a day: 8x200 mg hard gel caps + 1-2x100 mg ritonavir, both once-a-day with food

Renal dosing: no adjustment is necessary for renal insufficiency
Hepatic dosing: there is no data available
Food dependence Both forms of saquinavir should be taken with food (high or moderate fat)
Adverse Effects Mainly GI disturbance including abdominal pain, diarrhea especially with soft gel form

Also rash, hepatitis, fat redistribution, hyperlipidemia, Type 2 diabetes

Interactions
Saquinavir effect on other drugs:
Saquinavir may increase terfenadine, cisapride, astemizole, pimozide, triazolam, midazolam, ergot derivatives, rifampin or antiarrhythmic medications, which include amiodarone, bepridil, flecainide, propafenone, and quinidine
Saquinavir increases rifabutin levels by approximately 50%
Levels of all erectile dysfunction drugs are increased: the lowest dose of these drugs must be used as a maximum and at intervals not be be decreased beyond every 48-72 hours.
Effect of other drugs on saquinavir:
Clarithromycin increases saquinavir levels by 150-200%
Efavirenz decreases saquinavir levels by 50-60%
Ritonavir increases saquinavir levels
Atazanavir increases saquinavir levels
Omeperazole increases the levels from hard capsule saquinavir 500 mg by 82% in terms of plasma exposure. (1)
Contraindications INVIRASE should not be administered concurrently with terfenadine, cisapride, astemizole, pimozide, triazolam, midazolam, ergot derivatives, rifampin or antiarrhythmic medications, which include amiodarone, bepridil, flecainide, propafenone, and quinidine
Suggested laboratory evaluations Liver profile and glucose monthly x 3 months, then every 3-4 months

Lipid profile q3-4 months

Warnings Concomitant use of INVIRASE with lovastatin or simvastatin is not recommended.
Concomitant use of INVIRASE and St. Johnís wort (hypericum perforatum) or products containing St. Johnís wort is not recommended. Garlic capsules should not be used while taking saquinavir as the sole protease inhibitor due to the risk of decreased saquinavir plasma concentrations. No data are available for the coadministration of INVIRASE/ritonavir and garlic capsules.
Usage Suggestion Hard gel cap form of saquinavir (Invirase) should not be used outside of a boosting strategy (i.e. without ritonavir or another protease inhibitor).

Hard gel cap form (Invirase) is preferred when using a boosting strategy to minimize gastrointestinal side effects from the carrier oil in the soft gel form (Fortovase).

Full Prescribing Information Invirase prescribing information

 

 

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Quick Menu / Table of Contents
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Updated 12.6.2005