Misoprostol, Cytotec: User and Application
The Latin name of the substance Misoprostol
Misoprostol
Pharmacotherapeutic group substances Misoprostol
Prostaglandins, thromboxanes, leukotrienes and their antagonists
Nosological classification (ICD-10)
K25 Gastric ulcer
K26 duodenal ulcer
K27 Peptic ulcer unspecified location
K29.1 Other acute gastritis
K63.3 Ulcer Bowel
O04 Medical abortion
Y45 adverse effects in therapeutic use of analgesics, antipyretics and anti-inflammatory drugs
Code CAS
59122-46-2
Characteristics of substance Misoprostol Cheap
Synthetic analogue of PGE1. Consists of two diastereomers in a 1:1 ratio.
Powder forming on dilution with water a viscous liquid. The molecular weight of 382.54.
Pharmacology
Pharmacological action - gastroprotective, antiulcer, uterotoniziruyuschee, stimulating labor. Has antisecretory activity. Binds to receptors of gastric parietal cells of PGE, inhibits basal, stimulated and nocturnal secretion of gastric juice and hydrochloric acid, enhances the formation of bicarbonate and mucus, improves blood flow and exerts cytoprotective action. Reduces the basal (but not stimulated by histamine) produce pepsin. Increases the resistance of the gastric mucosa and prevents the development of erosive and ulcerative lesions, promotes healing of peptic ulcers. In patients taking NSAIDs, reduces the incidence of gastric and duodenal ulcer reduces the risk of ulcer bleeding. The action begins in 30 minutes and lasts at least 3-6 hours at a dose 50 mcg effects are mild and short, 200 mg - expressed.
Misoprostol has a weak stimulating effect on smooth muscles of the digestive tract. It induces the contraction of smooth muscle fibers of the myometrium and the expansion of the cervix. The ability of misoprostol to stimulate uterine contractions facilitate the disclosure of the cervix increases the tone of the uterus and can provoke a miscarriage. Cytotec generic has no clinically significant effect on prolactin levels of gonadotropins, thyrotropin, growth hormone, thyroxine, cortisol, creatinine, on platelet aggregation, pulmonary function and cardio-vascular system.
Once inside quickly and completely absorbed. Simultaneous reception with food reduces bioavailability (fatty food reduces absorption, without affecting its duration). In the walls of the gastrointestinal tract and liver biotransformation to pharmacologically active metabolite diester - misoprostol acid. Cmax misoprostol is (6,08 ± 1,64) pg / ml misoprostol acid - (499 ± 15) pg / ml. Tmax - (12 ± 3) min, circulates in the systemic vascular bed in the protein-bound form (approximately 90%). T1 / 2 terminal is 20-40 minutes. Equilibrium concentration in plasma is reached within 2 days, cumulation is not observed. 80% of the dose is excreted by the kidneys (64-73% in the first 24 h) and faeces (15%). If the kidney function can increase Cmax (almost 2-fold) and lengthened T1 / 2.
In elderly patients (older than 64 years) an increase in the AUC.
After a single oral dose of misoprostol its metabolite - misoprostol acid - found in breast milk. Cmax misoprostol acid in human milk is reached after 1 h and was 7.6 pg / ml, while taking 200 mg of misoprostol and 20.9 pg / ml, while taking 600 mg of misoprostol. The concentration of misoprostol acid in human milk is reduced to 1 pg / ml 5 h after taking misoprostol.
Application of the substance Misoprostol Generic
Erosion of the gastrointestinal tract, stomach ulcer and duodenal ulcer, erosive and ulcerative lesions of the gastrointestinal tract during therapy with drugs, including NSAID-gastropathy (prevention and treatment).
Interruption of early pregnancy (up to 42 days of amenorrhea) - only in combination with mifepristone.
Contraindications (100mg-200mg)
Hypersensitivity, including to other prostaglandins and their analogues, lactation, childhood and adolescence (18 years).
Restrictions apply 100mg
Expressed in liver function, renal failure, hypotension, ischemic heart disease, stroke, atherosclerosis of brain vessels, koronarokardioskleroz, epilepsy, enterocolitis, diarrhea, advanced age, endocrinopathy, and disorders of the endocrine system, including diabetes mellitus, dysfunction of the adrenal hormone-dependent tumors, anemia, while applying for termination of pregnancy - the use of intrauterine contraceptive (before application to remove the IUD), the suspicion of an ectopic pregnancy.
Application of pregnancy and breastfeeding
When applying as a gastroprotective means: contraindicated in pregnancy (including the planning of pregnancy). In order to prevent pregnancies among women of reproductive age before the treatment, you must first spend serum pregnancy test, which should remain negative during the 2 weeks before taking the drug. Treatment should begin no earlier than 2-3 days after onset of menstruation. Throughout the period of administration of misoprostol should use reliable methods of contraception (if pregnancy occurs the woman informed of the potential threat to the fetus).
When applying as a uterotoniziruyuschego tools can be applied only to abortion, otherwise contraindicated in pregnancy.
Category effects on the fetus by FDA - X.
The active metabolite of cytotec - misoprostol acid - is excreted in breast milk. Although reports on the development of any adverse reactions in children who are breastfed mother, takes misoprostol is not registered, we recommend caution when assigning misoprostol during this period.
Side effects of substance Misoprostol 200mg
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, dysmenorrhea, hypermenorrhea, postmenopausal vaginal bleeding, menorrhagia, metrorrhagia, pelvic pain associated with contractions of the myometrium.
Allergic reactions: skin rash, itching, anaphylaxis, angioedema.
Other: weight change, dizziness, headache (2.4%), asthenia, fatigue, pyrexia, chills, very rarely in women with pre-and post-menopausal period - cramps.
