Drug reference

Mifepristone

Progestogen · Obstetrics

ProgestogenObstetrics

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

12 major

incl. contraindicated

PREGNANCY

FDA category + note

Top interactionssee all 12 →

GlucocorticoidsContraindicatedTextbookG&G 14e
AbarelixSevereDatabaseDDInter
AbirateroneSevereDatabaseDDInter
AcalabrutinibSevereDatabaseDDInter

Mechanism

Mifepristone, an antiprogestogenic steroid, sensitises the myometrium to prostaglandin-induced contractions and ripens the cervix. This facilitates the process of medical abortion by allowing it to occur in a shorter time and with a lower dose of prostaglandin.

Indications

Cervical ripening before mechanical cervical dilatation for termination of pregnancy of up to 84 days gestation (under close medical supervision)Facilitating medical abortion (pre-treatment to sensitize the uterus to subsequent administration of a prostaglandin)Termination of pregnancy (followed by administration of a prostaglandin)Inducing medical abortion (off-label, based on RCOG guidelines)termination of early pregnancy (in combination with prostaglandins)management of excess glucocorticoid production (Cushing syndrome)control of hyperglycemia in adults secondary to endogenous cushing syndrome who have type 2 diabetesintractable cushing syndrome (off-label)termination of early pregnancyMedical termination of pregnancy (up to 7 weeks, in combination with misoprostol)cushing's syndrome (inoperable adrenal carcinoma)cushing's syndrome (patients with ectopic acth secretion)Termination of pregnancy (up to 7 weeks)Cervical ripening (before surgical abortion or induction of labour)Postcoital contraceptiveOnce-a-month contraceptiveInduction of labourCushing’s syndrome (palliative for inoperable cases)Hypercortisolism associated with Cushing’s Syndrome Caused by Ectopic ACTH Production (to improve glucose intolerance and hypertension)

Dosing

Adult: 200 mg by mouth for 1 dose, to be taken 36-48 hours before procedure for cervical ripening.

Pharmacokinetics

Peak effect

peak plasma levels occur within several hours

Half-life

20 to 40 h (slowly cleared, bound by α1-acid glycoprotein)

Bioavailability

good (oral)

Metabolism

by CYP3A4 to mono- and didemethylated products (pharmacologically active)

Excretion

predominantly in the feces (as metabolic products)

Contraindications

chronic glucocorticoid therapy

Side effects

Common

vaginal bleedingabdominal painuterine crampsnauseavomitingdiarrheaDiarrhoeaProlonged bleedingFailed abortionAnorexiaTirednessAbdominal discomfortLoose motions

Serious

severe bleeding (requiring blood transfusion, rare)
serious infections (e.g., Clostridium sordellii sepsis)
adrenal insufficiency (at high doses)
hypertension
hypokalemia

Pregnancy & lactation

Pregnancy

Drug interactions

Glucocorticoids

Contraindicated

Textbook

Increases both corticotropin and adrenal steroid levels in the plasma, and at high doses, can result in adrenal insufficiency.

Women receiving chronic glucocorticoid therapy should not be given mifepristone due to its antiglucocorticoid activity. High doses of mifepristone can lead to adrenal insufficiency.

Source: G&G 14e

Abarelix

Severe

Database

Drug interaction classified as: synergy

Source: DDInter

Abiraterone

Severe

Database

Drug interaction classified as: synergy

Source: DDInter

Acalabrutinib