Ortho-est

Food Interaction

[Minor] 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.

Estropipate Cholesterol interaction

[Moderate] Although estrogens have generally favorable effects on plasma lipids, including increases in HDL and decreases in total cholesterol and LDL, they have also been associated with significant elevations in triglyceride levels, particularly when high dosages are used.

Severe hyperlipidemia is known to sometimes cause pancreatitis.

Patients with preexisting hyperlipidemia may require closer monitoring during estrogen therapy, and adjustments made accordingly in their lipid-lowering regimen.

Estropipate Hypertension interaction

[Major] The risk of myocardial infarction and strokes, including those associated with oral contraceptive use and some estrogen use, is increased in patients with hypertension.

Moreover, estrogens (and progestogens) may elevate blood pressure and worsen the hypertension, thus compounding the risk.

Clinically significant blood pressure increases have been reported during estrogen therapy, particularly in patients receiving high dosages or treated with oral contraceptive combinations having high progestational activity.

These effects also increase with duration of therapy and patient age.

Therapy with estrogens should be administered cautiously in patients with preexisting hypertension.

Patients should be monitored for changes in cardiovascular status, and their antihypertensive regimen adjusted or estrogen therapy withdrawn as necessary.

In patients requiring contraception, alternative methods should be considered for those who are hypertensive, over age 35, and smoke.

Ortho-est Drug Interaction

Moderate: levothyroxine, levothyroxineUnknown: duloxetine, duloxetine, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, pregabalin, pregabalin, esomeprazole, esomeprazole, omeprazole, omeprazole, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol, alprazolam, alprazolam

Ortho-est Disease Interaction

Major: abnormal vaginal bleeding, carcinomas (estrogenic), hypercalcemia in breast cancer, hypertension, thromboembolism/cardiovascular, hepatic neoplasmsModerate: angioedema, gallbladder disease, hypercalcemia, hyperlipidemia, liver disease, melasma, depression, fluid retention, glucose intolerance, retinal thrombosis, thyroid function tests

Innovators Monograph

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