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Drug Interactions between boceprevir and saquinavir

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

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Interactions between your drugs

Moderate

saquinavir boceprevir

Applies to: saquinavir and boceprevir

MONITOR: Coadministration of boceprevir and some ritonavir-boosted protease inhibitor regimens has been associated with decreased plasma concentrations of both boceprevir and the protease inhibitors. The mechanism of interaction has not been described. In a pharmacokinetic study of 39 healthy volunteers, boceprevir reduced the mean trough plasma concentrations (Cmin) of ritonavir-boosted atazanavir, darunavir, and lopinavir by 49%, 59%, and 43%, respectively. Mean reductions of 34% to 44% were observed in the systemic exposure (AUC) and 25% to 36% were observed in the peak concentration (Cmax) of atazanavir, lopinavir, and darunavir. Conversely, ritonavir-boosted atazanavir did not alter the AUC of boceprevir, whereas ritonavir-boosted darunavir and lopinavir decreased the AUC of boceprevir by 32% and 45%, respectively. When boceprevir (400 mg three times daily for 15 days) was given in combination with ritonavir alone (100 mg once daily for 12 days), boceprevir Cmax and AUC decreased by 27% and 19%, respectively. Data are currently unavailable regarding a potential interaction between boceprevir and other protease inhibitors, whether alone or ritonavir-boosted.

MANAGEMENT: Given the risk of reduced viral susceptibility and resistance development associated with subtherapeutic antiviral drug levels, caution is advised if boceprevir is used in combination with ritonavir-boosted protease inhibitor regimens. Patients coinfected with chronic HCV and HIV who have been started on one of these combinations should be closely monitored for treatment response and potential HCV and HIV virologic rebound. The safety and efficacy of boceprevir has not been established in the HCV/HIV coinfected population. As such, the manufacturer does not recommend the coadministration of boceprevir and ritonavir-boosted HIV protease inhibitors.

References

  1. "Product Information. Victrelis (boceprevir)." Schering-Plough Corporation (2011):
  2. FDA. U.S. Food and Drug Administration "FDA Drug Safety Communication: Important drug interactions between (boceprevir) and ritonavir-boosted human immunodeficiency virus (HIV) protease inhibitor drugs. http://www.fda.gov/Drugs/DrugSafety/ucm291119.htm" (2012):

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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. "Product Information. Invirase (saquinavir)." Roche Laboratories PROD (2001):
  2. 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
  3. Bailey DG, Malcolm J, Arnold O, Spence JD "Grapefruit juice-drug interactions." Br J Clin Pharmacol 46 (1998): 101-10
  4. 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
  5. Cerner Multum, Inc. "UK Summary of Product Characteristics." O 0
  6. Cerner Multum, Inc. "Australian Product Information." O 0
View all 6 references

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Moderate

boceprevir food

Applies to: boceprevir

ADJUST DOSING INTERVAL: Food significantly enhances the oral bioavailability of boceprevir. When given at 800 mg three times daily with food, boceprevir exposure increased by up to 65% relative to administration in the fasting state. The bioavailability of boceprevir was similar regardless of meal type (e.g., high-fat versus low-fat) or whether taken 5 minutes prior to eating, during a meal, or immediately following completion of the meal. Therefore, boceprevir may be taken without regard to either meal type or timing of the meal.

MANAGEMENT: To ensure maximal oral absorption, boceprevir should be administered with a meal or light snack.

References

  1. "Product Information. Victrelis (boceprevir)." Schering-Plough Corporation (2011):

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Therapeutic duplication warnings

Therapeutic duplication is the use of more than one medicine from the same drug category or therapeutic class to treat the same condition. This can be intentional in cases where drugs with similar actions are used together for demonstrated therapeutic benefit. It can also be unintentional in cases where a patient has been treated by more than one doctor, or had prescriptions filled at more than one pharmacy, and can have potentially adverse consequences.

Duplication

Protease inhibitors

Therapeutic duplication

The recommended maximum number of medicines in the 'protease inhibitors' category to be taken concurrently is usually one. Your list includes two medicines belonging to the 'protease inhibitors' category:

  • boceprevir
  • saquinavir

Note: In certain circumstances, the benefits of taking this combination of drugs may outweigh any risks. Always consult your healthcare provider before making changes to your medications or dosage.

See also

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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.

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