Mifepristone

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Mifegyne; Belgium: Mifegyne; Denmark: Mifegyne; Estonia: Mifegyne; Finland: Mifegyne; France: Mifegyne; Germany: Mifegyne; Greece: Mifegyne; Latvia: Mifegyne; Luxembourg: Mifegyne; Netherlands: Mifegyne; Portugal: Mifegyne; Romania: Mifegyne; Spain: Mifegyne; Sweden: Mifegyne; UK: Mifegyne.

North America

USA: Mifeprex.

Drug combinations

Chemistry

Mifepristone: C~29~H~35~NO~2~. Mw: 429.59. (11β,17β)-11-[4-(Dimethylamino)phenyl]-17-hydroxy-17-(1-propynyl)-estra-4,9-dien-3-one. CAS-84371-65-3 (1998).

Pharmacologic Category

Oxytocics. Abortifacient. Antiprogestin. Antineoplastic Agent, Hormone Antagonist.(ATC-Code: G03XB01).

Mechanism of action

Competitively binds to intracellular progesterone receptor, blocking effects of progesterone. When used for termination of pregnancy, this leads to contraction-inducing activity in myometrium. Also has weak antiglucocorticoid and antiandrogenic properties.

Therapeutic use

Medical termination of intrauterine pregnancy, through day 49 of pregnancy.

Pregnancy and lactiation implications

Used to terminate pregnancy. Prostaglandins (including mifepristone and misoprostol) may have teratogenic effects when used during pregnancy. Breast milk should be discarded for a few days following use of this medication.

Unlabeled use

Treatment of unresectable meningioma. Has been studied in treatment of breast cancer, ovarian cancer, and adrenal cortical carcinoma.

Contraindications

Hypersensitivity to mifepristone, misoprostol, other prostaglandins, or any component of the formulation. Chronic adrenal failure. Porphyrias. Hemorrhagic disorder or concurrent anticoagulant therapy. Pregnancy termination >49 days. Intrauterine device in place. Ectopic pregnancy or undiagnosed adnexal mass. Concurrent long-term corticosteroid therapy. Inadequate or lack of access to emergency medical services.

Warnings and precautions

Bacterial infections reported. Bleeding occurs (might be prolonged and heavy, potentially leading to hypovolemic shock). Use with caution in heavy smokers (>10 cigarettes/day). Use with caution in women >35 years. Confirmation of terminated pregnancy must be made 14 days following treatment.

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