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Drug Interactions between rabeprazole and saquinavir

This report displays the potential drug interactions for the following 2 drugs:

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Interactions between your drugs

Moderate

saquinavir RABEprazole

Applies to: saquinavir and rabeprazole

MONITOR: The concomitant administration of some proton pump inhibitors with saquinavir, with or without ritonavir, may significantly increase exposure to saquinavir. When omeprazole 40 mg once daily and saquinavir/ritonavir 1000 mg/100 mg twice daily were administered to healthy subjects (n=18), the steady-state area under the concentration-time curve (AUC) and maximum plasma concentrations (Cmax) of saquinavir were increased by an average of 82 % (range, 37% to 234%) and 75 % (range, 31% to 234%), respectively, compared to saquinavir/ritonavir. Ritonavir concentrations were not changed significantly. The mechanism is unknown.

MANAGEMENT: Clinical and laboratory monitoring for saquinavir toxicity is recommended during concurrent use of a proton pump inhibitor. According to some authorities, a dose reduction for saquinavir may be considered.

References

  1. (2022) "Product Information. PriLOSEC (omeprazole)." Merck & Co., Inc
  2. (2001) "Product Information. Invirase (saquinavir)." Roche Laboratories
  3. (2001) "Product Information. Nexium (esomeprazole)." Astra-Zeneca Pharmaceuticals
  4. Cerner Multum, Inc. "UK Summary of Product Characteristics."
  5. (2014) "Product Information. NexIUM I.V. (esomeprazole)." Astra-Zeneca Pharmaceuticals
View all 5 references

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Drug and food interactions

Moderate

saquinavir food

Applies to: saquinavir

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

  1. (2001) "Product Information. Invirase (saquinavir)." Roche Laboratories
  2. Kupferschmidt HHT, Fattinger KE, Ha HR, Follath F, Krahenbuhl S (1998) "Grapefruit juice enhances the bioavailability of the HIV protease inhibitor saquinavir in man." Br J Clin Pharmacol, 45, p. 355-9
  3. Bailey DG, Malcolm J, Arnold O, Spence JD (1998) "Grapefruit juice-drug interactions." Br J Clin Pharmacol, 46, p. 101-10
  4. Eagling VA, Profit L, Back DJ (1999) "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, p. 543-52
  5. Cerner Multum, Inc. "UK Summary of Product Characteristics."
  6. Cerner Multum, Inc. "Australian Product Information."
View all 6 references

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Therapeutic duplication warnings

No warnings were found for your selected drugs.

Therapeutic duplication warnings are only returned when drugs within the same group exceed the recommended therapeutic duplication maximum.


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Drug Interaction Classification

These classifications are only a guideline. The relevance of a particular drug interaction to a specific individual is difficult to determine. Always consult your healthcare provider before starting or stopping any medication.
Major Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit.
Moderate Moderately clinically significant. Usually avoid combinations; use it only under special circumstances.
Minor 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.
Unknown No interaction information available.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.