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Drug Interactions between abacavir / dolutegravir / lamivudine and etravirine

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

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Interactions between your drugs

Major

etravirine dolutegravir

Applies to: etravirine and abacavir / dolutegravir / lamivudine

GENERALLY AVOID: Coadministration with etravirine may significantly decrease the plasma concentrations of dolutegravir. The exact mechanism of interaction has not been established, but may rely partially on etravirine induction of dolutegravir metabolism via CYP450 3A4 and UGT1A1. In 16 study subjects, administration of dolutegravir 50 mg once daily with etravirine 200 mg twice daily decreased dolutegravir peak plasma concentration (Cmax), systemic exposure (AUC) and trough plasma concentration (Cmin; 24 hours postdose) by 52%, 71% and 88%, respectively, compared to administration without etravirine. These effects were mitigated by coadministration of darunavir/ritonavir or lopinavir/ritonavir. When the same dosage of dolutegravir was given with etravirine 200 mg and darunavir/ritonavir 600 mg/100 mg twice daily to 9 study subjects, dolutegravir Cmax, AUC and Cmin decreased by just 12%, 25% and 37%, respectively. When given with etravirine 200 mg plus lopinavir/ritonavir 400 mg/100 mg twice daily to 8 study subjects, dolutegravir Cmax, AUC and Cmin increased by 7%, 11% and 28%, respectively. Although not studied, the interaction between dolutegravir and etravirine is also expected to be mitigated by atazanavir/ritonavir. Using cross-study comparisons to historical pharmacokinetic data, dolutegravir did not appear to affect the pharmacokinetics of etravirine, atazanavir, darunavir, lopinavir, or ritonavir.

MANAGEMENT: Dolutegravir should not be used with etravirine unless also coadministered with atazanavir/ritonavir, darunavir/ritonavir, or lopinavir/ritonavir. Concomitant use of etravirine with the fixed-dose combination products containing abacavir/dolutegravir/lamivudine or dolutegravir/lamivudine is not recommended.

References

  1. Cerner Multum, Inc. "UK Summary of Product Characteristics."
  2. Cerner Multum, Inc. "Australian Product Information."
  3. (2013) "Product Information. Tivicay (dolutegravir)." ViiV Healthcare
  4. (2014) "Product Information. Triumeq (abacavir/dolutegravir/lamivudine)." ViiV Healthcare
  5. (2019) "Product Information. Dovato (dolutegravir-lamivudine)." ViiV Healthcare
View all 5 references

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Drug and food interactions

Moderate

etravirine food

Applies to: etravirine

ADJUST DOSING INTERVAL: Coadministration with food increases the oral bioavailability of etravirine. The mechanism is unknown. Compared to administration following a meal, the systemic exposure (AUC) to etravirine was decreased by about 50% when the drug was administered under fasting conditions. The types of meal studied (ranging from 345 kilocalories containing 17 grams fat to 1160 kilocalories containing 70 grams fat) did not appear to make a difference with respect to impact on etravirine bioavailability.

MANAGEMENT: Etravirine should always be administered following a meal.

References

  1. (2008) "Product Information. Intelence (etravirine)." Ortho Biotech Inc

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Minor

dolutegravir food

Applies to: abacavir / dolutegravir / lamivudine

Food increases the extent of absorption and slows the rate of absorption of dolutegravir. When administered with a low-, moderate- or high-fat meal, dolutegravir peak plasma concentration (Cmax) increased by 46%, 52% and 67%, systemic exposure (AUC) increased by 33%, 41% and 66%, and time to reach Cmax (Tmax) increased from 2 hours to 3, 4 and 5 hours, respectively, compared to administration under fasted conditions. Dolutegravir may be taken with or without food.

References

  1. (2013) "Product Information. Tivicay (dolutegravir)." ViiV Healthcare

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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.