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Drug Interactions between Sustiva and Tivicay

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

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Interactions between your drugs

Major

efavirenz dolutegravir

Applies to: Sustiva (efavirenz) and Tivicay (dolutegravir)

ADJUST DOSE: Coadministration with potent inducers of UGT1A and CYP450 3A4 isoenzymes such as efavirenz may significantly decrease the plasma concentrations of dolutegravir, which is primarily metabolized by UGT1A1 with some contribution from CYP450 3A4. Dolutegravir is also a substrate of UGT1A3, UGT1A9, and P-glycoprotein in vitro. In 12 study subjects, administration of dolutegravir 50 mg once daily with efavirenz 600 mg once daily decreased dolutegravir peak plasma concentration (Cmax), systemic exposure (AUC) and trough plasma concentration (Cmin; 24 hours postdose) by 39%, 57% and 75%, respectively, compared to administration without efavirenz. Using cross-study comparisons to historical pharmacokinetic data, dolutegravir did not appear to affect the pharmacokinetics of efavirenz.

MANAGEMENT: When prescribed in combination with efavirenz, the dosage of dolutegravir should be increased to 50 mg twice daily for both adults and pediatric patients 12 years of age and older who weigh at least 40 kg. The safety and efficacy of dosages above 50 mg twice daily have not been evaluated. Concomitant use of efavirenz with the fixed-dose combination product containing dolutegravir/lamivudine is not recommended. For concomitant use of efavirenz with the fixed-dose combination product containing abacavir/dolutegravir/lamivudine, it is recommended to administer an additional dose of dolutegravir 50 mg/day, separated from the combination product by 12 hours. Alternative treatment combinations that do not include metabolic inducers should be considered whenever possible for integrase strand transfer inhibitor (INSTI)-experienced patients with certain INSTI-associated resistance substitutions or clinically suspected INSTI resistance.

References

  1. (2013) "Product Information. Tivicay (dolutegravir)." ViiV Healthcare
  2. (2014) "Product Information. Triumeq (abacavir/dolutegravir/lamivudine)." ViiV Healthcare
  3. (2019) "Product Information. Dovato (dolutegravir-lamivudine)." ViiV Healthcare

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Drug and food interactions

Moderate

efavirenz food

Applies to: Sustiva (efavirenz)

ADJUST DOSING INTERVAL: Administration with food increases the plasma concentrations of efavirenz and may increase the frequency of adverse reactions. According to the product labeling, administration of efavirenz capsules (600 mg single dose) with a high-fat/high-caloric meal (894 kcal, 54 g fat, 54% calories from fat) or a reduced-fat/normal-caloric meal (440 kcal, 2 g fat, 4% calories from fat) was associated with mean increases of 39% and 51% in efavirenz peak plasma concentration (Cmax) and 22% and 17% in systemic exposure (AUC), respectively, compared to administration under fasted conditions. For efavirenz tablets, administration of a single 600 mg dose with a high-fat/high-caloric meal (approximately 1000 kcal, 500-600 kcal from fat) resulted in a 79% increase in mean Cmax and a 28% increase in mean AUC of efavirenz relative to administration under fasted conditions.

MANAGEMENT: Efavirenz should be taken on an empty stomach, preferably at bedtime. Dosing at bedtime may improve the tolerability of nervous system symptoms such as dizziness, insomnia, impaired concentration, somnolence, abnormal dreams and hallucinations, although they often resolve on their own after the first 2 to 4 weeks of therapy . Patients should be advised of the potential for additive central nervous system effects when efavirenz is used concomitantly with alcohol or psychoactive drugs, and to avoid driving or operating hazardous machinery until they know how the medication affects them.

References

  1. (2001) "Product Information. Sustiva (efavirenz)." DuPont Pharmaceuticals

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Minor

dolutegravir food

Applies to: Tivicay (dolutegravir)

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.

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

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