Saquinavir and Alcohol/Food Interactions
There are 2 alcohol/food/lifestyle interactions with saquinavir.
saquinavir food
Moderate Food Interaction
ADJUST DOSING INTERVAL: Food significantly increases the absorption of saquinavir.
MONITOR: Coadministration with grapefruit juice may increase the plasma concentrations of saquinavir. The primary mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruits. In eight healthy volunteers, ingestion of 400 mL of grapefruit juice prior to administration of a 600 mg dose of saquinavir mesylate increased the area under the plasma concentration-time curve and oral bioavailability of saquinavir by 50% and 100%, respectively, compared to water; however, the increase is not considered clinically relevant. A high degree of intersubject variability in the grapefruit juice effect was also observed. The extent to which this interaction may occur with the saquinavir free base soft gelatin capsule is unknown. However, the saquinavir soft gelatin capsule formulation is no longer commercially available.
MANAGEMENT: Saquinavir mesylate should be taken with meals or within 2 hours after eating to enhance bioavailability. Patients should be advised to avoid the consumption of large amounts of grapefruit and grapefruit juice during saquinavir therapy unless otherwise directed by their doctor, as the interaction is unreliable and subject to a high degree of interpatient variation.
References
- "Product Information. Invirase (saquinavir)." Roche Laboratories PROD (2001):
- Kupferschmidt HHT, Fattinger KE, Ha HR, Follath F, Krahenbuhl S "Grapefruit juice enhances the bioavailability of the HIV protease inhibitor saquinavir in man." Br J Clin Pharmacol 45 (1998): 355-9
- Bailey DG, Malcolm J, Arnold O, Spence JD "Grapefruit juice-drug interactions." Br J Clin Pharmacol 46 (1998): 101-10
- Eagling VA, Profit L, Back DJ "Inhibition of the CYP3A4-mediated metabolism and P-glycoprotein-mediated transport of the HIV-I protease inhibitor saquinavir by grapefruit juice components." Br J Clin Pharmacol 48 (1999): 543-52
- Cerner Multum, Inc. "UK Summary of Product Characteristics." O 0
- Cerner Multum, Inc. "Australian Product Information." O 0
High Cholesterol (Hyperlipoproteinemia, Hypertriglyceridemia, Sitosterolemia)
Moderate Potential Hazard, Moderate plausibility
PIs - hyperlipidemia
Treatment with ritonavir alone or in combination with other protease inhibitors (e.g., lopinavir, saquinavir, tipranavir, fosamprenavir) has resulted in substantial increases in the concentration of total cholesterol and triglycerides. These effects have also been reported with other protease inhibitors but may be the most dramatic with ritonavir. The clinical significance of these elevations is unclear. Marked elevation in triglyceride levels is a risk factor for development of pancreatitis. Triglyceride and cholesterol testing is recommended before starting ritonavir (with or without other protease inhibitors) and periodically during therapy. Lipid disorders should be managed as clinically appropriate.
References
- "Product Information. Norvir (ritonavir)." AbbVie US LLC SUPPL-25 (2022):
- "Product Information. Reyataz (atazanavir)." Bristol-Myers Squibb SUPPL-44 (2020):
- "Product Information. Lexiva (fosamprenavir)." ViiV Healthcare SUPPL-41 (2019):
- "Product Information. Kaletra (lopinavir-ritonavir)." AbbVie US LLC SUPPL-54 (2020):
- "Product Information. Invirase (saquinavir)." Roche Laboratories SUPPL-25 (2020):
- "Product Information. Aptivus (tipranavir)." Boehringer Ingelheim SUPPL-21 (2020):
Saquinavir drug interactions
There are 681 drug interactions with saquinavir.
Saquinavir disease interactions
There are 6 disease interactions with saquinavir which include:
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Drug Interaction Classification
Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit. | |
Moderately clinically significant. Usually avoid combinations; use it only under special circumstances. | |
Minimally clinically significant. Minimize risk; assess risk and consider an alternative drug, take steps to circumvent the interaction risk and/or institute a monitoring plan. | |
No interaction information available. |
Further information
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