Estradiol with Lomitapide Interaction Details

Brand Names Associated with Estradiol

Brand Names Associated with Lomitapide

Medical Content Editor Dr. Brian Staiger, PharmD
Last updated Nov 13, 2023

Interaction Effect

Increased exposure of lomitapide

Interaction Summary

The concomitant use of lomitapide (a CYP3A4 substrate) with oral contraceptives (weak CYP3A4 inhibitors) may cause increased exposure to lomitapide. When the combined oral contraceptive ethinylestradiol/norgestimate was coadministered with lomitapide, the systemic exposure of lomitapide increased by 30%. If concurrent use is required, the maximum lomitapide dosage is 40 mg daily. When initiating an oral contraceptive in a patient already taking lomitapide 10 mg/day or more, decrease the lomitapide dose by 50%. Then carefully titrate based on response and tolerability to a maximum of 40 mg daily.

Severity

Moderate

Onset

Unspecified

Evidence

Theoretical

How To Manage Interaction

The concomitant use of lomitapide (a CYP3A4 substrate) with oral contraceptives (weak CYP3A4 inhibitors) may cause increased exposure to lomitapide. If concurrent use is required, the maximum lomitapide dosage is 40 mg daily. When initiating an oral contraceptive in a patient already taking lomitapide 10 mg/day or more, decrease the lomitapide dose by 50%. Then carefully titrate based on response and tolerability to a maximum of 40 mg daily.

Mechanism Of Interaction

Inhibition of CYP3A4-mediated lomitapide metabolism

Literature Reports

A) The concomitant administration of the combined oral contraceptive, ethinylestradiol 0.035 mg and norgestimate 0.25 mg daily, with a single 20-mg dose of lomitapide was shown to increase the AUC of lomitapide by 30% and Cmax by 40% compared with lomitapide administered alone .

Estradiol Overview

• Estrogen is used to treat hot flushes ('hot flashes'; sudden strong feelings of heat and sweating) in women who are experiencing menopause ('change of life', the end of monthly menstrual periods). Some brands of estrogen are also used to treat vaginal dryness, itching, or burning, or to prevent osteoporosis (a condition in which the bones become thin and weak and break easily) in women who are experiencing or have experienced menopause. However, women who need a medication only to treat vaginal dryness or only to prevent osteoporosis should consider a different treatment. Some brands of estrogen are also to relieve symptoms of low estrogen in young women who do not produce enough estrogen naturally. Some brands of estrogen are also used to relieve the symptoms of certain types of breast and prostate (a male reproductive gland) cancer. Estrogen is in a class of medications called hormones. It works by replacing estrogen that is normally produced by the body.

Lomitapide Overview

• Lomitapide is used along with diet changes (restriction of cholesterol and fat intake) and other treatments to reduce the amount of low-density lipoprotein (LDL) cholesterol ('bad cholesterol'), total cholesterol, and other fatty substances in the blood in people that have homozygous familial hypercholesterolemia (HoFH; an inherited condition in which cholesterol cannot be removed from the body normally). Lomitapide should not be used to decrease cholesterol levels in people who do not have HoFH. Lomitapide is in a class of medications called cholesterol-lowering medications. It works by slowing the production of cholesterol in the body to decrease the amount of cholesterol that may build up on the walls of the arteries and block blood flow to the heart, brain, and other parts of the body.

• Accumulation of cholesterol and fats along the walls of your arteries (a process known as atherosclerosis) decreases blood flow and, therefore, the oxygen supply to your heart, brain, and other parts of your body. Lowering your blood level of cholesterol and fats may help prevent heart disease, angina (chest pain), strokes, and heart attacks.

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Definitions

Severity Categories

Contraindicated

These drugs, generally, should not be used together simultaneously due to the high risk of severe adverse effects. Combining these medications can lead to dangerous health outcomes and should be strictly avoided unless otherwise instructed by your provider.

Major

This interaction could result in very serious and potentially life-threatening consequences. If you are taking this drug combination, it is very important to be under close medical supervision to minimize severe side effects and ensure your safety. It may be necessary to change a medication or dosage to prevent harm.

Moderate

This interaction has the potential to worsen your medical condition or alter the effectiveness of your treatment. It's important that you are monitored closely and you potentially may need to make adjustments in your treatment plan or drug dosage to maintain optimal health.

Minor

While this interaction is unlikely to cause significant problems, it could intensify side effects or reduce the effectiveness of one or both medications. Monitoring for changes in symptoms and your condition is recommended, and adjustments may be made if needed to manage any increased or more pronounced side effects.

Onset

Rapid: Onset of drug interaction typically occurs within 24 hours of co-administration.

Delayed: Onset of drug interaction typically occurs more than 24 hours after co-administration.

Evidence

Level of documentation of the interaction.

Established: The interaction is documented and substantiated in peer-reviewed medical literature.

Theoretical: This interaction is not fully supported by current medical evidence or well-documented sources, but it is based on known drug mechanisms, drug effects, and other relevant information.

How To Manage The Interaction

Provides a detailed discussion on how patients and clinicians can approach the identified drug interaction as well as offers guidance on what to expect and strategies to potentially mitigate the effects of the interaction. This may include recommendations on adjusting medication dosages, altering the timing of drug administration, or closely monitoring for specific symptoms.

It's important to note that all medical situations are unique, and management approaches should be tailored to individual circumstances. Patients should always consult their healthcare provider for personalized advice and guidance on managing drug interactions effectively.

Mechanism Of Interaction

The theorized or clinically determined reason (i.e., mechanism) why the drug-drug interaction occurs.

Disclaimer: The information provided on this page is for informational purposes only and should not be considered medical advice. Always consult with a qualified healthcare professional regarding your specific circumstances and medical conditions.

Where Does Our Information Come From?

Information for our drug interactions is compiled from several drug compendia, including:

• Gold Standard Drug Database
• Micromedex
• Lexicomp
• DrugBank

The prescribing information for each drug, as published on DailyMED, is also used. 

Individual drug-drug interaction detail pages contain references specific to that interaction. You can click on the reference number within brackets '[]' to see what reference was utilized.

The information posted is fact-checked by HelloPharmacist clinicians and reviewed quarterly.