Misoprostol

When ATH:
A02BB01

Characteristic.

A synthetic analog of PGE₁. It consists of two diastereoisomers in a ratio 1:1.

Powder, when diluted with water forming a viscous liquid. Molecular weight 382,54.

Pharmacological action.
Gastroprotective, protivoyazvennoe, uterotoniziruyuschee, stimulating generic activities.

Application.

Erosion of the gastrointestinal tract, gastric ulcer and duodenal ulcer, erosive and ulcerative lesions of the gastrointestinal tract during therapy with drugs, incl. NSAID-gastropathy (Prevention and treatment). Termination of pregnancy of early terms (to 42 days of amenorrhea) only in combination with mifepristone.

Contraindications.

Hypersensitivity, incl. to other prostaglandins and their analogues, lactation, Children and Youth age (to 18 years).

Restrictions apply.

Expressions of the liver, renal failure, hypotension, CHD, cerebrovascular accident, cerebral atherosclerosis, koronarokardioskleroz, epilepsy, enterocolitis, diarrhea, advanced age; endocrinopathies and endocrine diseases, incl. diabetes, adrenal dysfunction; hormone-dependent tumors; anemia; When applying for termination of pregnancy — the use of intrauterine contraceptive (Before use, remove the IUD), Suspected ectopic pregnancy.

Pregnancy and breast-feeding.

When used as a gastroprotective agent: contraindicated in pregnancy (incl. when planning pregnancy). In order to avoid pregnancy in women of reproductive age before treatment, you must first spend serum pregnancy test, which should be negative for 2 weeks before receiving the drug. Treatment should begin no earlier than 2-3 days after the onset of menstruation. During the period of administration of misoprostol should use reliable methods of contraception (upon the occurrence of pregnant women are informed about the potential threat to the fetus).

When used as a means of uterotoniziruyuschego It can only be used to terminate pregnancy, otherwise contraindicated in pregnancy.

Category actions result in FDA - X. (Animal tests or clinical trials revealed a violation of the fetus and / or there is evidence of the risk of adverse effects on the human fetus, obtained in research or practice; risk, associated with the use of drugs in pregnancy, greater than the potential benefits.)

Unlikely, misoprostol passes into breast milk, tk. it is rapidly metabolized in the body. However, information about its active metabolite concentrations of misoprostol acid-is missing, therefore not recommended for nursing women misoprostol because the potential penetration of misoprostol acid in mother's milk, which can cause severe diarrhea in a child.

Side effects.

From the digestive tract: abdominal pain, dyspepsia, flatulence (2,9%), nausea and / or vomiting, diarrhea (11–40%) or constipation (1,1%).

With the genitourinary system: menstrual disorders, dysmenorrhoea, hypermenorrhea, postmenopausal vaginal bleeding, menorragija, metrorragija, lower abdominal pain, related to the reduction of the myometrium.

Allergic reactions: skin rash, itch, angioedema.

Other: weight change, dizziness, headache (2,4%), asthenia, fatigue, hyperthermia; extremely rare in women before- and post-menopausal stages-convulsions.

Cooperation.

Eating, antacids accompanied by decrease in the concentration of misoprostol acid in plasma (clinically insignificant). When combined with a magnesium-containing antacids may increase diarrhea caused by misoprostol. Admission for a long time rifampicin, izoniazida, anticonvulsants, Antidepressants, cimetidine, acetylsalicylic acid, indomethacin and drugs group phenobarbital, smoking more 10 cigarettes per day — stimulate the metabolism of misoprostol, reducing the level of serum.

During 1 weeks after misoprostol should abandon admission of acetylsalicylic acid and other NSAIDs.

Overdose.

Manifestations of overdose in humans has not been described. Proceeding from the results of animal studies tioksichnosti, clinical signs, ukazыvayushtimi of misoprostol peredozirovku, be sleepy, lethargy, tremor, convulsions, breathlessness, abdominal pain, diarrhea, fever, heartbeat, decrease in blood pressure, bradycardia.

Treatment: simptomaticheskaya therapy. Hemodialysis nyeeffyektivyen.

Dosing and Administration.

Inside. The dosage regimen is determined individually, depending on the evidence.

For the prevention of gastric ulcers, caused by NSAIDs, and the treatment of erosive gastritis and gastric ulcer and duodenal ulcer: by 200 UG 2-4 times a day (Last admission is at bedtime); daily dose-400-800 mcg. When poor tolerability of a single dose may be reduced to 100 mg. In renal insufficiency the daily dose reduced by 50%.

Abortion (in combination with mifepristone): 36-48 hours after mifepristone administered 400 mg of misoprostol.

Precautions.

In the application for the termination of early pregnancy Misoprostol should only be used in combination with mifepristone. In combination with mifepristone medication should be used only by prescription and under medical supervision and only in specialized hospitals, with capacity to provide emergency surgical and gynecological transfusion assistance, and having appropriately trained medical staff.

Use of the drug requires prevention of Rh-conflict and other general activities, concomitant abortion. Before the appointment of misoprostol patient should be informed in detail about the effects and possible side effects of the drug. The patient should be observed in a hospital for 4-6 hours before dosing. During and after treatment the patient must be given timely medical assistance in the event of massive bleeding or other complications. After taking the drug for patients, usually, there is a slight vaginal bleeding, some of the women is very long. In very early pregnancy abortion is possible after mifepristone, but in this case also need pills of misoprostol to optimize the results of medical abortion. After administration of misoprostol in approximately 80% Women abortion occurs within 6 h and approximately 10% women within 1 Sun. The patient must be retested in the same hospital after 8-15 days after dosing. If necessary, it should be carried out or ultrasound to determine the level of human chorionic gonadotropin in serum. If you suspect an incomplete abortion or continuation of the pregnancy must be timely to conduct a comprehensive medical examination. With incomplete abortion or ongoing pregnancy, estimated at 10-14 days after mifepristone, ALWAYS vacuum aspiration with subsequent histological examination of aspirate.

Taking the drug as gastroprotectives should stop when diarrhea occurs (mild diarrhea is not considered grounds for cancellation of the treatment, medication overturned when severe diarrhea is approximately 2% cases), pruritus, bleeding from the vagina, lowering blood pressure and increasing the activity of transaminases.

Cooperation