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单词 mifepristone
释义

mifepristone

enUK

mi·fep·ri·stone

M0288750 (mĭ-fĕp′rĭ-stōn′)n. A synthetic steroid, C29H35NO2, that blocks the action of progesterone and is used in combination with misoprostol to induce abortion in early pregnancy. Also called RU 486.
[(a)mi(no) + alteration of phe(nyl) + pr(opyl) + alteration of est(radiol) + -one.]

mifepristone

(mɪˈfɛprɪˌstəʊn) n (Pharmacology) an antiprogestogenic steroid, used in the medical termination of pregnancy. Formula: C29H35NO2[C20: from aminophenol + propyne + oestradiol + -one]

mif•e•pris•tone

(ˌmɪf əˈprɪs toʊn)
n. an antigestational drug that prevents a fertilized egg from attaching to the uterine wall by blocking the action of progesterone. [1985–90; probably alter. of (a)mi(no)phe(nol) + pr(opyl) + est(radiol) + -one]
Thesaurus
Noun1.mifepristone - an abortion-inducing drug (trade name RU_486) developed in Francemifepristone - an abortion-inducing drug (trade name RU_486) developed in France; when taken during the first five weeks of pregnancy it blocks the action of progesterone so that the uterus sloughs off the embryoabortion pill, RU 486aborticide, abortifacient, abortion-inducing drug - a drug (or other chemical agent) that causes abortion
Translations

mifepristone

enUK

mifepristone

an antiprogestogenic steroid, used in the medical termination of pregnancy. Formula: C29H35NO2

mifepristone

enUK

Mifepristone

 

Definition

Mifepristone is a pill that can be taken as an alternative to a surgical abortion.

Purpose

This medication most often is used for ending early pregnancies. In 2003, studies were surfacing reporting other possible uses for mifepristone, at least at low doses. These studies included its possible use in treating psychotic depression. Low-dose mifepristone also showed success as a treatment for uterine fibroids, or benign growths in the muscular tissue of a woman's uterus. However, many uses of the drug other than for abortions were still experimental, even if promising.Mifespristone's primary use for medical abortions is preferred by many over surgical approaches to abortions. It has emerged as a form of emergency contraception when taken at low does within a short time period following possible conception.

Precautions

Women who are more than seven weeks pregnant (or 49 days since their last menstrual period) should not take mifepristone. Other reasons to avoid mifepristone include: use of an intrauterine device (IUD), ectopic pregnancy, use of blood thinners, bleeding disorders, use of steroid medications, allergies to mifepristone or similar drugs and lack of access to medical help within two weeks after the treatment. When the drug is used at low doses as emergency contraception, it poses few side effects.

Description

Mifepristone, sold commercially under the name Mifeprex, also is known as RU-486, the abortion pill, the early option pill for medical abortion. While it has been used for many years in Europe, mifepristone has only been available for use in the United States since the U.S. Food and Drug Administration (FDA) approved it in 2000 for use in abortion. More than 37,000 abortions were performed using the pill in the first six months of 2001.This drug causes pregnancy to end by blocking the female hormone progesterone. The lack of progesterone makes the uterus shed its lining, which causes bleeding similar to a menstrual period. Three days after taking mifepristone, women are given a second drug, misprostol, to cause uterine contractions that expel the contents of the uterus. Most women are able remain in their own home while they pass the fetus.

Preparation

Before taking mifepristone, health care providers likely will give the woman a urine or blood test to be sure that she is, in fact, pregnant. They also may give her some counseling and support. Once she has made the decision to use mifepristone, they will ask her to sign a written statement that she has decided to end her pregnancy.

Aftercare

Using mifepristone and misoprostol causes heavy bleeding and cramping. Doctors can offer pain medicine, such as Motrin, to ease the cramps. For two weeks after treatment with mifepristone, health care providers likely will ask patients to abstain from sexual intercourse, heavy lifting and strenuous exercise. They also may advise against breast-feeding, since scientists are not sure if the drug is present in breast milk.Physicians require patients to come in for a follow-up visit 14 days after their first dose of mifepristone to verify that they are no longer pregnant and that they are properly healing.

Risks

Other common side effects include: fatigue, headaches, dizziness, nausea, vomiting, diarrhea and low-back pain.Since pregnancy hormones are in flux after a medical abortion, many women have emotional side-effects, such as mood swings, depression or a mild case of the blues. These feelings usually subside when hormones stabilize a few weeks later. For those who feel stuck in their grief or anger about the situation, counseling or support groups may offer relief.

Normal results

Most women feel better after about two weeks. Bleeding and spotting usually occurs for 9-16 days, but may last for a month.

Abnormal results

In some cases, mifepristone does not completely end the pregnancy. If the fetus is still left inside the uterus, a doctor may recommend a surgical abortion, or a procedure called dilation and curettage (D and C). About five to eight of every 100 women who take mifepristone go on to have a surgical abortion, according to the FDA. During a D and C, which usually is done at a hospital or clinic under a local anesthetic, a physician dilates the cervix, then uses an instrument to scrape any residual tissue away from the walls of the uterus. This allows the heavy bleeding to eventually stop so a woman can return to her normal cycle sooner.

Key terms

Dilation and curettage (D and C) — During this surgical procedure, a physician dilates the cervix, then uses an instrument to scrape tissue away from the walls of the uterus.Misprostol — A drug used in combination with mifepristone to cause uterine contractions that expel the contents of the uterus.

Resources

Periodicals

"Abortion Pills Account For 5% of U.S. Abortions." Medical Letter on the CDC and FDA February 9, 2003: 7."The Abortion Pill's Grim Progress." Mother Jones 24 (January 1, 1999).Grimes, David A, Mitchell D. Creinin. "Induced Abortion: an Overview for Internists." Annals of Internal Medicine April 20, 2004: 620-627."Low-dose Mifepristone Blocks Pregnancy by Altering Ovarian Function." Drug Week March 5, 2004: 107."Treatments for Depression with Psychosis." Harvard Mental Health Letter August 2003.Walling, Anne D. "Low-dose Mifepristone Shrinks Uterine Fibroids." American Family Physician September 1, 2003: 956.

mifepristone

 [mĭf″ĕ-pris´tōn] an antiprogestin used with misoprostol or other prostaglandin to terminate pregnancy in the first trimester; administered orally. Called also RU-486.

mifepristone (RU-486)

Korlym, Mifegyne (UK), Mifeprex

Pharmacologic class: Synthetic steroid

Therapeutic class: Antiprogestational agent, abortifacient

Pregnancy risk category NR

FDA Box Warning

• Rare cases of serious and sometimes fatal infections and bleeding have followed spontaneous, surgical, and medical abortions, including after mifepristone use. Before starting drug, inform patient of risk of these serious events and discuss medication guide and patient agreement. Ensure that patient knows whom to call and what to do, including going to emergency department (ED) if none of provided contacts are reachable; if she experiences sustained fever, severe abdominal pain, prolonged heavy bleeding, or syncope; or if she has abdominal pain or discomfort or general malaise (including weakness, nausea, vomiting, or diarrhea) more than 24 hours after taking drug.

• Patients with serious bacterial infections and sepsis may present without fever, bacteremia, or significant pelvic examination findings after abortion. Rare deaths have occurred in patients without fever, with or without abdominal pain, but with leukocytosis with marked left shift, tachycardia, hemoconcentration, and general malaise. Maintain high index of suspicion to rule out serious infection and sepsis.

• Advise patient to take medication guide with her if she visits ED or another health care provider who didn't prescribe drug, so provider will be aware that patient is undergoing medical abortion.

• Be aware that pregnancy must be excluded before initiation of treatment with Korlym. Patients must avoid pregnancy during treatment and for 1 month after therapy ends by using a nonhormonal, medically acceptable method of contraception; if patient has had a surgical sterilization, no additional contraception is needed. Pregnancy must also be excluded if treatment is interrupted for more than 14 days in females of childbearing potential.

Action

Antagonizes progesterone receptor sites, inhibiting activity of endogenous and exogenous progesterone and stimulating uterine contractions, which causes fetus to separate from placental wall

Availability

Tablets: 200 mg, 300 mg

Indications and dosages

Termination of intrauterine pregnancy through day 49 of pregnancy

Adults: On day 1, mifepristone 600 mg P.O. as a single dose. On day 3, misoprostol 400 mcg P.O. (unless abortion has been confirmed).

Hyperglycemia secondary to hypercortisolism in adults with endogenous Cushing's syndrome who have type 2 diabetes or glucose intolerance and have failed surgery or aren't candidates for surgery

Adults: Initially, 300 mg P.O. daily; increase based on clinical response and tolerability in 300-mg increments to a maximum of 1,200 mg daily. Don't exceed 20 mg/kg/day.

Dosage Adjustment

• Renal impairment (Korlym)

• Mild to moderate hepatic impairment (Korlym)

• Concurrent use of strong P450 CYP3A inhibitors (Korlym)

Contraindications

• Hypersensitivity to drug, misoprostol, or other prostaglandins

• Confirmed or suspected ectopic pregnancy or adnexal mass

• Chronic adrenal failure

• Bleeding disorders

• Concurrent anticoagulant therapy or long-term corticosteroid therapy

• Presence of intrauterine device (IUD)

• Inherited porphyrias

• Concomitant treatment with systemic corticosteroids for serious medical conditions or illnesses (Korlym)

• Concurrent use of simvastatin or lovastatin and CYP3A substrates with narrow therapeutic range (Korlym)

• History of unexplained vaginal bleeding or endometrial hyperplasia with atypia or endometrial carcinoma (Korlym)

• Pregnancy (Korlym)

Precautions

Use cautiously in:

• cardiovascular, respiratory, renal, or hepatic disorders; hypertension; type 1 diabetes mellitus; anemia; jaundice; seizure disorder; cervicitis; infected endocervical lesions; acute vaginitis; uterine scarring

• hypokalemia, underlying heart conditions including heart failure and coronary vascular disease (Korlym)

• hemorrhagic disorders or concurrent use of anticoagulants (Korlym)

• concurrent use of QT interval-prolonging drugs, patients with potassium channel variants resulting in long QT interval (avoid Korlym use)

• concurrent use of drugs metabolized by CYP2B6 and moderate CYP3A inhibitors (Korlym)

• concurrent use of CYP3A inducers (such as rifampin, rifabutin, rifapentin, phenobarbital, phenytoin, carbamazepine, and St. John's wort) or hormonal contraceptives (avoid use)

• concurrent use of strong CYP3A inhibitors (use Korlym with extreme caution and only when necessary; limit dosage to 300 mg)

• concurrent use of drugs metabolized by CYP2C8/2C9 (use lowest dose of CYP2C8/2C9 substrates when used with Korlym)

• breastfeeding patients (Korlym)

• children (Korlym; safety and efficacy not established).

Administration

• Before giving dose for termination of pregnancy, make sure patient doesn't have an IUD in place.

• Correct hypokalemia before starting Korlym.

• Give for termination of pregnancy only in health care facility under supervision of health care provider qualified to assess pregnancy stage and rule out ectopic pregnancy.

• Administer with fluids, but not with grapefruit juice.

• When giving for termination of pregnancy, confirm pregnancy termination 14 days after initial dose.

Adverse reactions

CNS: dizziness, fainting, headache, weakness, fatigue, insomnia, asthenia, anxiety, syncope, rigors

CV: hypertension, QT-interval prolongation (Korlym)

EENT: sinusitis

GI: nausea, vomiting, diarrhea, abdominal cramping, dyspepsia

GU: vaginitis, leukorrhea, uterine cramping, pelvic pain; endometrial hypertrophy, cystic dilatation of endometrial glands, vaginal bleeding (Korlym); uterine hemorrhage

Hematologic: anemia

Metabolic: hypokalemia, adrenal insufficiency (Korlym)

Musculoskeletal: leg pain, back pain, arthralgia

Skin: rash (Korlym)

Other: viral infections; fever, decreased appetite, peripheral edema, opportunistic infections (Korlym)

Interactions

Drug-drug. CYP2C8/2C9 substrates: increased plasma concentrations of these drugs

CYP3A inducers (such as carbamazepine, phenobarbital, phenytoin, rifabutin, rifampin, rifapentin): decreased mifepristone concentrations

CYP3A substrates with narrow therapeutic range (such as cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, tacrolimus): increased exposure of these drugs and effects

Drugs metabolized by CYP2B6 (bupropion, efavirenz): significantly increased exposure of these drugs

Drugs metabolized by CYP3A (lovastatin, simvastatin): increased risk of myopathy and rhabdomyolysis

Glucocorticoids: antagonized glucocorticoid effect

Moderate CYP3A inhibitors (such as amprenavir, aprepitant, atazanavir, ciprofloxacin, darunavir/ritonavir, diltiazem, erythromycin, fluconazole, imatinib, verapamil), strong CYP3A inhibitors (such as amprenavir, boceprevir, clarithromycin, conivaptan, fosamprenavir, indinavir, itraconazole, lopinavir, mibefradil, nefazodone, nelfinavir, posaconazole, ritonavir, saquinavir, telaprevir, telithromycin, voriconazole): increased plasma mifepristone concentration

Oral contraceptives: decreased oral contraceptive effectiveness

Drug-diagnostic tests. Hematocrit, hemoglobin: decreased values

Potassium: decreased level

Red blood cells: decreased count

Drug-food. Grapefruit juice: increased mifepristone blood level and effects

Drug-herbs. St. John's wort: decreased mifepristone blood level and effects

Patient monitoring

• Assess vital signs, breath sounds, and bowel sounds.

• Monitor uterine contractions and type and amount of vaginal bleeding.

• Evaluate CBC.

• Monitor serum potassium level 1 to 2 weeks after starting or increasing Korlym dosage and periodically thereafter.

See Closely monitor patient taking Korlym for signs and symptoms of adrenal insufficiency, including weakness, nausea, increased fatigue, hypotension, and hypoglycemia. If adrenal insufficiency is suspected, discontinue drug immediately and administer glucocorticoids without delay. May resume Korlym at a lower dosage after resolution of adrenal insufficiency.

• Be aware that patients with endogenous Cushing's syndrome are at risk for opportunistic infections such as Pneumocystis jiroveci pneumonia while taking Korlym. Monitor patient for respiratory distress shortly after Korlym initiation. Initiate appropriate diagnostic tests and treat P. jiroveci as indicated.

Patient teaching

When used for termination of pregnancy:

• After administration, tell patient she will need to return in 48 hours for a prostaglandin drug or to verify pregnancy termination.

• Tell patient she will have contractions for 3 or more hours after receiving drug and that vaginal bleeding may last 9 to 16 days.

See Instruct patient to contact prescriber if she has persistent or extremely heavy vaginal bleeding, extreme fatigue, or orthostatic hypotension.

Caution patient that vaginal bleeding does not prove that complete abortion has occurred. Tell her she will need follow-up appointment 2 weeks later to verify pregnancy termination.

• Inform patient that she is at risk for pregnancy right after abortion is complete. Encourage appropriate contraceptive decision.

When used for hyperglycemia secondary to hypercortisolism in patients with endogenous Cushing's syndrome:

See Instruct patient to recognize and report signs and symptoms of hypokalemia, respiratory infections, and adrenal insufficiency.

• Advise patient not to take drug with grapefruit juice and not to use herbal products without consulting prescriber.

When used for either indication:

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, and herbs mentioned above.

mife·pris·tone

(mif'pris-tōn), Synthetic chemical compound with antiprogesterone properties used for early pregnancy termination; the substance binds with glucocorticoid receptors resulting in increased adrenal gland secretion. Synonym(s): RU-486

mifepristone

An antiprogestin used with misoprostol, a PGE1 analogue, as a morning-after contraceptive for early pregnancy termination.

mifepristone

RU 486 Obstetrics An antiprogestin used as a morning-after contraceptive, with misoprostol, a PGE1 analogue, for early pregnancy termination. Cf Late abortion.

mi·fe·pris·tone

(RU-486) (mif'ĕ-pris-tōn) Synthetic chemical compound with antiprogesterone properties used for early pregnancy termination.
Synonym(s): RU-486.

mifepristone

A progesterone antagonist drug also known as RU-486. When given in early pregnancy mifepristone causes the detachment of the blastocyst, the production of prostaglandins that prompt contraction of the womb and softening of the cervix. The result is abortion of the conceptus. A brand name is Mifegyne.

mifepristone

enUK
  • noun

Synonyms for mifepristone

noun an abortion-inducing drug (trade name RU_486) developed in France

Synonyms

  • abortion pill
  • RU 486

Related Words

  • aborticide
  • abortifacient
  • abortion-inducing drug
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