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Drug Interactions between Lamprene and sirolimus protein-bound

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

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Interactions between your drugs

Major

clofazimine sirolimus protein-bound

Applies to: Lamprene (clofazimine) and sirolimus protein-bound

Consumer information for this interaction is not currently available.

ADJUST DOSE: Coadministration of protein-bound sirolimus intravenous suspension with moderate or weak inhibitors of CYP450 3A4 may increase the systemic exposure to sirolimus, which is primarily metabolized by the isoenzyme and also a substrate of the P-glycoprotein (P-gp) efflux transporter. No formal studies evaluating the drug interaction potential of protein-bound sirolimus have been conducted. However, significant increases in systemic exposure have been reported for oral sirolimus coadministered with moderate dual inhibitors of CYP450 3A4 and P-gp such as diltiazem, erythromycin and verapamil, all of which are also substrates of CYP450 3A4 and P-gp. When 10 mg of sirolimus oral solution was administered with 120 mg of diltiazem in 18 healthy volunteers, sirolimus peak plasma concentration (Cmax) and systemic exposure (AUC) increased by 1.4- and 1.6-fold, respectively. Sirolimus did not affect the pharmacokinetics of either diltiazem or its metabolites, desacetyldiltiazem and desmethyldiltiazem. When sirolimus oral solution 2 mg once a day was coadministered with erythromycin ethylsuccinate 800 mg every 8 hours to steady state in 24 healthy volunteers, sirolimus Cmax and AUC increased by 4.4- and 4.2-fold, respectively, while erythromycin Cmax and AUC increased by 1.6- and 1.7-fold, respectively. Likewise, when sirolimus oral solution 2 mg once a day was coadministered with verapamil 180 mg every 12 hours to steady state in 25 healthy volunteers, sirolimus Cmax and AUC increased by 2.3- and 2.2-fold, respectively, while Cmax and AUC of the pharmacologically active S(-) enantiomer of verapamil both increased by 1.5-fold. Increased exposures to sirolimus may increase the risk of adverse effects such stomatitis, nausea, diarrhea, vomiting, myelosuppression, infections, hypokalemia, hyperglycemia, interstitial lung disease, edema, rash, alopecia, and hemorrhage.

MANAGEMENT: When administered concomitantly with moderate or weak CYP450 3A4 inhibitors, the manufacturer recommends reducing the dosage of protein-bound sirolimus intravenous suspension to 56 mg/m2. Clinical response and toxicities should be closely monitored, and the dosage of protein-bound sirolimus further adjusted as necessary. In addition, patients may also require monitoring for potentially increased effects of concomitant CYP450 3A4 inhibitors, as many are also substrates of CYP450 3A4 and/or P-gp and may be impacted by sirolimus. The prescribing information for concomitant medications should be consulted.

References

  1. (2001) "Product Information. Rapamune (sirolimus)." Wyeth-Ayerst Laboratories
  2. Claesson K, Brattstrom C, Burke JT (2001) "Sirolimus and erythromycin interaction: two cases." Transplant Proc, 33, p. 2136
  3. Cerner Multum, Inc. "UK Summary of Product Characteristics."
  4. Cerner Multum, Inc. "Australian Product Information."
  5. (2022) "Product Information. Fyarro (sirolimus protein-bound)." Aadi Bioscience, Inc.
View all 5 references

Drug and food interactions

Moderate

sirolimus protein-bound food

Applies to: sirolimus protein-bound

Grapefruit juice may increase the blood levels of sirolimus protein-bound. However, this has not been studied, and it is not known to what extent grapefruit juice may interact with sirolimus protein-bound. High blood levels of sirolimus protein-bound can increase side effects such as mouth sores and inflammation, nausea, diarrhea, vomiting, abdominal pain, decreased appetite, increased blood sugar, rash, hair loss, lung or breathing problems, and impaired bone marrow function resulting in low numbers of different types of blood cells. You may also be more likely to develop anemia, bleeding problems, or infections due to low blood cell counts. The manufacturer recommends avoiding grapefruit and grapefruit juice during treatment with sirolimus protein-bound. Talk to your doctor if you have any questions or concerns. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.

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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.