Penkrofton

General characteristics. Structure:

Active agent: Mifepristone — 200 mg.

Excipients: starch corn — 264 mg, lactose (sugar milk) — 80 mg, cellulose microcrystallic — 36 mg, calcium stearate 1-water — 6 mg, silicon dioxide colloid (aerosil of the A-300 brand) — 14 mg.

Pharmacological properties:

Pharmacodynamics. Пенкрофтон® — synthetic steroid antigestagenny means (blocks effect of progesterone at the level of receptors), has no gestagenny activity. Antagonism with glucocorticosteroids is noted (due to the competition at the level of receptors). Increases sokratitelny ability and sensitivity of a myometrium to prostaglandins. Effect of drug is resulted by desquamation of a decidua and an ekspulsiya of fetal egg. 

 

Pharmacokinetics. After a single dose of drug inside in a dose of 600 mg the maximum concentration — 1,98 mg/l are reached in 1,5 hours. Absolute bioavailability makes 69%. In a blood plasma mifepristone for 98% contacts proteins: albumine and acid alpha 1 - a glycoprotein. After a distribution phase, removal at first happens slowly, concentration decreases twice between 12–72 hours, then more quickly. The elimination half-life makes 18 hours.

Indications to use:

— medicamentous interruption of a uterine pregnancy on early terms (up to 42 days of an amenorrhea)

— preparation for childbirth and induction of childbirth at the full-term pregnancy

Route of administration and doses:

Drug has to be used in medical institutions which have appropriately prepared medical shots and the necessary equipment.

For medicamentous abortion of early terms.

600 mg of Penkroftona® (3 tablets on 200 mg) accept inside once in the presence of the doctor. The patient has to be under observation of medical personnel, at least, within 2 hours after use.

In 36–48 hours after reception of Penkroftona® the patient needs to conduct ultrasonography (ultrasonography). In 8–14 days repeatedly conduct clinical examination and ultrasonography, and also determine the level of beta and chorionic hormone for confirmation that the abortion occurred. In the absence of effect of use of drug for the 14th day (incomplete abortion or the continuing pregnancy) carry out vacuum aspiration with the subsequent histologic research of aspirate.

For preparation and induction of childbirth at the full-term pregnancy: once 200 mg of Penkroftona® (1 tablet) in the presence of the doctor. In 24 hours repeated reception of 200 mg.

In 48–72 hours assessment of a condition of patrimonial ways is carried out, and, as necessary, prostaglandins or oxytocin are appointed.

Features of use:

Patients have to be surely informed that in the absence of effect by 10–14 day of drug use (incomplete abortion or the continuing pregnancy), pregnancy should be interrupted with a different way because of high risk of formation, inborn malformations at a fruit.

Use of drug demands the prevention a Rhesus factor-alloimmunizatsii and holding other general actions accompanying abortion.

Patients with artificial heart valves or an infectious endocarditis at use of mifepristone should carry out preventive treatment by antibiotics.

Drug does not protect from diseases, sexually transmitted and AIDS, and is not recommended as planned continuous contraception.

Information on a possibility of negative influence of drug on performance of potentially dangerous types of activity requiring special attention and bystry reactions (driving and other vehicles, work with moving mechanisms, work of the dispatcher and operator, etc.) is absent.

Side effects:

Disturbance of a menstrual cycle, amenorrhea, metrorrhagia, lohia serosa, uterus subinvolution, discomfort and pain in the bottom of a stomach; aggravation of inflammatory processes of a uterus, appendages, urinary tract; weakness, headache, nausea, vomiting, diarrhea, dizziness, hyperthermia, fever, small tortoiseshell; bloody allocations from a genital tract, a nagrubaniye of mammary glands.

Interaction with other medicines:

It is necessary to avoid simultaneous use of non-steroidal anti-inflammatory drugs (NPVS), and also reception of NPVS within 8–12 days after mifepristone use.

Contraindications:

Hypersensitivity to mifepristone, adrenal insufficiency, long reception of glucocorticosteroids, an acute or chronic renal and/or liver failure, anemia, a porphyria, a hysteromyoma, existence of a hem on a uterus, disturbances of a hemostasis (including the previous treatment by anticoagulants), inflammatory diseases of generative organs, existence of heavy extragenital pathology.

The smoking women cannot apply 35 years without preliminary consultation of the therapist are more senior.

At medicamentous abortion: suspicion on an extrauterine pregnancy; the pregnancy which is not confirmed with clinical trials; the pregnancy exceeding 42 days of an amenorrhea on term; the pregnancy which occurred against the background of use of intrauterine contraception or after cancellation of hormonal contraception.

By preparation for childbirth and to induction of childbirth: a gestosis of heavy degree, a preeclampsia, an eclampsia, premature or postmature pregnancy, placental presentation, discrepancy of the sizes of a head of a fruit and the woman's basin, the abnormal provision of a fruit, bloody allocations from a genital tract of not clear etiology.

With care appoint at chronic obstructive diseases of lungs (including bronchial asthma), heavy arterial hypertension, disturbances of a heart rhythm and heart failure.

Overdose:

Reception of mifepristone in doses to 2 g does not cause undesirable reactions. In cases of overdose of drug emergence of symptoms of adrenal insufficiency is possible.

Storage conditions:

To store in the place protected from light at a temperature not above 25 °C. 

To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets of 200 mg, on 3 tablets in bank from light-protective glass or bank of polymeric; or in a blister strip packaging. Each can or a blister strip packaging are placed in a pack cardboard together with the instruction on a medical use.