Mifepristone-oral

Mifepristone is a synthetic steroid with antiprogesterone and antiglucocorticoid effects. It is used for terminating pregnancy and treating people with Cushing syndrome. Progesterone is a female hormone and the principal progestational hormone. Progesterone prepares the uterus (the womb) to receive and sustain the fertilized egg andis an important hormone for sustaining pregnancy. Mifepristone terminates early pregnancy by blocking the activity of progesterone at progesterone receptors. It also stimulates contraction of the uterus. Early pregnancy is considered to be = 49 days (7weeks) since the last menstrual period began. Mifepristone must be used in combination with misoprostol for the purpose of termination of pregnancy. The FDA approved this combination treatment in September 2000.

Cortisol is a metabolite (break down product) of the hormone cortisone. Cortisol is an essential factor in many processes including the proper metabolism of starches, and it is the major natural glucocorticoid in humans. People with Cushing syndrome produce too much cortisol, and, among many other effects, develop high glucose (sugar) levels in the blood. Mifepristone reduces blood glucose levels in people with Cushing syndrome by blocking the activity of cortisol.

Yes

Treatment with mifepristone and misoprostol requires three separate office visits.

• Day 1: Three 200 mg tablets (600 mg) of mifepristone are taken as a single dose.
• Day 3: 400 mcg of misoprostol is given orally unless abortion has been confirmed.
• Day 14: No medication administered. Patient returns for a post-treatment examination to confirm that a complete termination of pregnancy has occurred.

The dose for treating Cushing syndrome is 300 mg daily initially. The dose may be increased to 1200 mg daily.

Ketoconazole, itraconazole (Sporanox), erythromycin, and grapefruit juice may increase blood levels of mifepristone by inhibiting the enzyme responsible for metabolizing (breaking down) mifepristone. Rifampin, dexamethasone, St. John's Wort, phenytoin, phenobarbital, and carbamazepine may decrease blood levels of mifepristone by increasing the activity of the enzyme responsible for metabolizing mifepristone and decrease the effectiveness of mifepristone. Mifepristone may inhibit liver enzymes which are responsible for the metabolism of various drugs, resulting in increased blood levels of these drugs.

Before taking mifepristone, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: kidney disease, liver disease, vaginal bleeding of unknown cause, problems with the lining of the uterus (endometrial hyperplasia, endometrial cancer), mineral imbalance (low level of potassium in the blood), heart disease (such as coronary artery disease), high blood pressure.

This drug may make you dizzy. Do not drive, use machinery, or do any activity that requires alertness until you are sure you can perform such activities safely. Limit alcoholic beverages.

Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

Mifepristone may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can rarely cause serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that need medical attention right away.

The risk of QT prolongation may be increased if you have certain medical conditions or are taking other drugs that may cause QT prolongation. Before using mifepristone, tell your doctor or pharmacist of all the drugs you take and if you have any of the following conditions: certain heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of certain heart problems (QT prolongation in the EKG, sudden cardiac death).

Low levels of potassium or magnesium in the blood may also increase your risk of QT prolongation. This risk may increase if you use certain drugs (such as diuretics/"water pills") or if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about using mifepristone safely.

Older adults may be more sensitive to the side effects of this drug, especially QT prolongation (see above).

Mifepristone must not be used during pregnancy. It may cause a loss of pregnancy. If you become pregnant or think you may be pregnant, tell your doctor right away. (See also Warning section.) Since this drug can be absorbed through the skin and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication.

This medication passes into breast milk. Consult your doctor before breast-feeding.

If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

Notes

Do not share this medication with others.

Laboratory and/or medical tests (such as potassium levels, thyroid function, blood pressure) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

Missed Dose

If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip themissed dose and resume your usual dosing schedule. Do not double the dose to catch up.

Storage

Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.Information last revised July 2016. Copyright(c) 2016 First Databank, Inc.