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Drug Interactions between Aerodiol and cobicistat / darunavir

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

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Interactions between your drugs

Moderate

estradiol darunavir

Applies to: Aerodiol (estradiol) and cobicistat / darunavir

MONITOR: Coadministration with darunavir may increase the plasma concentrations of drugs that are substrates of the CYP450 3A4 isoenzyme. The mechanism is decreased clearance due to inhibition of CYP450 3A4 activity by darunavir.

MANAGEMENT: Caution is advised if darunavir must be used concurrently with medications that undergo metabolism by CYP450 3A4, particularly those with a narrow therapeutic range. Dosage adjustments as well as clinical and laboratory monitoring may be appropriate for some drugs whenever darunavir is added to or withdrawn from therapy.

References

  1. "Product Information. Prezista (darunavir)." Ortho Biotech Inc (2006):

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Moderate

estradiol cobicistat

Applies to: Aerodiol (estradiol) and cobicistat / darunavir

ADDITIONAL CONTRACEPTION RECOMMENDED: Coadministration with cobicistat and elvitegravir may alter the plasma concentrations of contraceptive hormones. The exact mechanism of interaction has not been described. In 13 study subjects, administration of ethinyl estradiol 0.025 mg and norgestimate 0.18 to 0.25 mg once daily in combination with elvitegravir 150 mg plus cobicistat 150 mg once daily decreased the mean ethinyl estradiol peak plasma concentration (Cmax), systemic exposure (AUC) and trough plasma concentration (Cmin) by 6%, 25% and 44%, respectively. In contrast, norgestimate Cmax, AUC and Cmin increased by 2.08-, 2.26- and 2.67-fold, respectively. Clinical effects of increased progestogen levels are not fully known, but may include increased risk of insulin resistance, dyslipidemia, acne, and venous thrombosis.

MANAGEMENT: The potential risks and benefits of using norgestimate-containing contraceptives in combination with cobicistat and elvitegravir should be considered, particularly in women who have risk factors for insulin resistance, dyslipidemia, acne, and venous thrombosis. Coadministration of cobicistat and elvitegravir with other hormonal contraceptives (e.g., contraceptive patch, contraceptive vaginal ring, or injectable contraceptives), oral contraceptives containing progestogens other than norgestimate, or less than 25 mcg of ethinyl estradiol has not been studied and is not recommended. Some authorities recommend that hormonal contraceptives containing at least 30 mcg of ethinyl estradiol with norgestimate should be used in combination with the multi-ingredient antiretroviral formulations containing elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate or elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide. However, the long term effects of increased progesterone exposure are not known. Alternative, nonhormonal methods of contraception may be considered.

References

  1. Cerner Multum, Inc. "UK Summary of Product Characteristics." O 0
  2. Cerner Multum, Inc. "Australian Product Information." O 0
  3. "Product Information. Stribild (cobicistat/elvitegravir/emtricitabine/tenofov)." Gilead Sciences (2012):

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Drug and food interactions

Moderate

darunavir food

Applies to: cobicistat / darunavir

ADJUST DOSING INTERVAL: Food enhances the absorption and oral bioavailability of darunavir administered in combination with low-dose ritonavir. The mechanism is unknown. When administered with food, the peak plasma concentration (Cmax) and area under the plasma concentration-time curve (AUC) of darunavir were approximately 30% higher than when administered in the fasting state. Darunavir exposure was similar for the range of meals studied. The total caloric content of the various meals evaluated ranged from 240 Kcal (12 grams fat) to 928 Kcal (56 grams fat).

MANAGEMENT: To ensure maximal oral absorption, darunavir coadministered with ritonavir should be taken with food. The type of food is not important.

References

  1. "Product Information. Prezista (darunavir)." Ortho Biotech Inc (2006):

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Minor

estradiol food

Applies to: Aerodiol (estradiol)

Coadministration with grapefruit juice may increase the bioavailability of oral estrogens. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall induced by certain compounds present in grapefruits. In a small, randomized, crossover study, the administration of ethinyl estradiol with grapefruit juice (compared to herbal tea) increased peak plasma drug concentration (Cmax) by 37% and area under the concentration-time curve (AUC) by 28%. Based on these findings, grapefruit juice is unlikely to affect the overall safety profile of ethinyl estradiol. However, as with other drug interactions involving grapefruit juice, the pharmacokinetic alterations are subject to a high degree of interpatient variability. Also, the effect on other estrogens has not been studied.

References

  1. Weber A, Jager R, Borner A, et al. "Can grapefruit juice influence ethinyl estradiol bioavailability?" Contraception 53 (1996): 41-7
  2. Schubert W, Eriksson U, Edgar B, Cullberg G, Hedner T "Flavonoids in grapefruit juice inhibit the in vitro hepatic metabolism of 17B-estradiol." Eur J Drug Metab Pharmacokinet 20 (1995): 219-24

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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

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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