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Drug Interactions between AccessPak for HIV PEP Expanded with Viracept and naldemedine

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

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Interactions between your drugs

Moderate

nelfinavir naldemedine

Applies to: AccessPak for HIV PEP Expanded with Viracept (emtricitabine / nelfinavir / tenofovir) and naldemedine

MONITOR: Coadministration with potent inhibitors of CYP450 3A4 may increase the plasma concentrations of naldemedine, which is primarily metabolized by CYP450 3A4 to nor-naldemedine and to a minor extent by UGT1A3 to naldemedine 3-G. Both metabolites have demonstrated antagonistic activity for opioid receptors, but with less potency than the parent drug. According to the product labeling, administration of naldemedine with 200 mg once daily itraconazole, a potent CYP450 3A4 and P-gp inhibitor, increased naldemedine peak plasma concentration (Cmax) by 12% and systemic exposure (AUC) by 191% compared to naldemedine administered alone. When administered with 200 mg once daily fluconazole, a moderate CYP450 3A4 inhibitor, naldemedine Cmax and AUC increased by 38% and 90%, respectively. When administered with a single 600 mg dose of cyclosporine, a potent P-gp but weak CYP450 3A4 inhibitor, naldemedine Cmax and AUC increased by 45% and 78%, respectively. Increased exposure to naldemedine may precipitate opioid withdrawal symptoms such as hyperhidrosis, lacrimation, rhinorrhea, chills, diarrhea, abdominal pain, anxiety, insomnia, irritability, restlessness, and yawning.

MANAGEMENT: Caution is advised during concomitant use of naldemedine with potent inhibitors of CYP450 3A4. Patients should be closely monitored for potential opioid withdrawal symptoms as well as other adverse effects of naldemedine.

References

  1. Cerner Multum, Inc. "UK Summary of Product Characteristics." O 0
  2. "Product Information. Symproic (naldemedine)." Shionogi USA Inc (2017):

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Drug and food interactions

Moderate

naldemedine food

Applies to: naldemedine

GENERALLY AVOID: Grapefruit juice may increase the plasma concentrations of naldemedine. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit. In pharmacokinetic studies, naldemedine systemic exposure (AUC) was increased approximately 90% by the moderate CYP450 3A4 inhibitor fluconazole and nearly 200% by the potent inhibitor itraconazole. The interaction has not been studied with grapefruit juice. In general, the effect of grapefruit juice is concentration-, dose- and preparation-dependent, and can vary widely among brands. Certain preparations of grapefruit juice (e.g., high dose, double strength) have sometimes demonstrated potent inhibition of CYP450 3A4, while other preparations (e.g., low dose, single strength) have typically demonstrated moderate inhibition. Increased exposure to naldemedine may precipitate opioid withdrawal symptoms such as hyperhidrosis, lacrimation, rhinorrhea, chills, diarrhea, abdominal pain, anxiety, insomnia, irritability, restlessness, and yawning.

Food does not significantly affect the overall bioavailability of naldemedine. When administered with a high-fat meal, the rate of naldemedine absorption was decreased, but not the extent. Specifically, naldemedine peak plasma concentration (Cmax) was decreased by approximately 35% and time to achieve Cmax was delayed from 0.75 hours in the fasted state to 2.5 hours in the fed state, while naldemedine AUC was not significantly changed.

MANAGEMENT: Naldemedine may be taken with or without food. Patients should avoid consumption of grapefruit and grapefruit juice during treatment with naldemedine.

References

  1. "Product Information. Symproic (naldemedine)." Shionogi USA Inc (2017):

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Minor

tenofovir food

Applies to: AccessPak for HIV PEP Expanded with Viracept (emtricitabine / nelfinavir / tenofovir)

Food enhances the oral absorption and bioavailability of tenofovir, the active entity of tenofovir disoproxil fumarate. According to the product labeling, administration of the drug following a high-fat meal increased the mean peak plasma concentration (Cmax) and area under the concentration-time curve (AUC) of tenofovir by approximately 14% and 40%, respectively, compared to administration in the fasting state. However, administration with a light meal did not significantly affect the pharmacokinetics of tenofovir compared to administration in the fasting state. Food delays the time to reach tenofovir Cmax by approximately 1 hour. Tenofovir disoproxil fumarate may be administered without regard to meals.

References

  1. "Product Information. Viread (tenofovir)." Gilead Sciences (2001):

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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.

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