Buy Generic Cytotec (Misoprostol) 100, 200 mcg online

Last Updated on February 19, 2017 by Dr.Derek Fhisher

Most popular brand: Cytotec
Active ingredient: Misoprostol
Available dosage forms: 100, 200 mcg

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Misoprostol general information

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Misoprostol (Misoprostol): instruction, and the use of a formula

Code CAS

Feature substance Misoprostol

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

The powder forming upon dilution with water, viscous liquid. Molecular weight 382,54.

Pharmacology

Mode of action – gastroprotective, antiulcer, uterotoniziruyuschee stimulating generic activities.

It has antisecretory activity. Bind to receptors of PGE gastric parietal cells, inhibits basal, stimulated and nocturnal gastric acid secretion and hydrochloric acid, enhances the formation of bicarbonate and mucus, improves blood flow and exhibits cytoprotective action. It reduces basal (but not stimulated by histamine) production of pepsin. It improves the stability of the gastric mucosa and prevents the development of erosive – ulcerative lesions, promotes healing of peptic ulcers. In patients taking NSAIDs. reduces the incidence of gastric and duodenal ulcers, reduces the risk of ulcer bleeding. The action begins in 30 minutes and lasts for at least 3 – 6 h At a dose of 50 mcg effect is moderate and short, 200 mcg .; expressed.

Misoprostol has a weak stimulating effect on the smooth muscles of the gastrointestinal tract. It induces a contraction of smooth muscle fibers of the myometrium and cervical extension. The ability of misoprostol to encourage uterine contractions facilitates cervical ripening, increases the tone of the uterus and can cause miscarriage. Misoprostol has no clinically significant effect on prolactin levels of gonadotropins, thyrotropin, growth hormone, thyroxine, cortisol, creatinine, platelet aggregation, lung and heart function – vasculature.

Once inside quickly and completely absorbed. Simultaneous administration with food reduced the bioavailability (fatty foods significantly reduces the absorption without affecting its duration). The walls of the gastrointestinal tract and hepatic biotransformation to pharmacologically active metabolite of diester ; misoprostol acid. C _max is misoprostol (6,08 & plusmn; 1,64) pg / ml, misoprostol acid ; (499 & plusmn; 15) pg / ml. T _max ; (12 & plusmn; 3) minutes, the system circulates in the bloodstream related proteins form (approximately 90%). T _1/2 terminal is 20 – 40 min. Equilibrium concentration in plasma is achieved within 2 days, no accumulation is observed. 80% of the dose is excreted by the kidneys (64 – 73% in the first 24 hours) and the faeces (15%). If the kidney function can increase C _max (almost 2 times) and elongated T _1/2 .

In elderly patients (over 64 years) an increase in AUC.

After a single oral administration of misoprostol metabolite ; misoprostol acid ; found in human milk. C _max misoprostol acid in breast milk is reached in 1 hour and is 7.6 pg / mL when taking 200 mg of misoprostol and 20.9 pg / ml when taking 600 mg of misoprostol. misoprostol acid concentration in breast milk is reduced to 1 pg / ml in 5 hours after taking misoprostol.

Application of the substance Misoprostol

The erosion of the gastrointestinal tract. gastric ulcer and duodenal ulcer disease, erosive – ulcerative lesions of the gastrointestinal tract in the background drug therapy. including NSAID – gastropathy (prevention and treatment).

interrupt early pregnancy (up to 42 days of amenorrhea) ; only in combination with mifepristone.

Contraindications

Hypersensitivity, including to other prostaglandins and their analogs, breast-feeding, Children and Youth age (up to 18).

Restrictions on the use

Severe hepatic dysfunction, renal failure, hypotension, ischemic heart disease. cerebral blood flow, cerebral atherosclerosis, koronarokardioskleroz, epilepsy, enterocolitis, diarrhea, older age; endocrinopathies and endocrine diseases, including diabetes, adrenal dysfunction; hormone – dependent tumors; anemia; when applying for abortion ; the use of intrauterine contraceptive (before application is necessary to remove IUDs), the suspicion of an ectopic pregnancy.

Application of pregnancy and breastfeeding

When used as a gastroprotective agent . contraindicated in pregnancy (including the planning of pregnancy). In order to avoid pregnancy in women of reproductive age before treatment, you must first spend serum pregnancy test, which must be negative for 2 weeks before taking the drug. Treatment should be started no earlier than 2 – 3 days after the onset of menstruation. In should use reliable methods of contraception during the entire period of administration of misoprostol (if pregnancy occurs the woman informed of the potential threat to the fetus).

When used as a means of uterotoniziruyuschego can be used only for the purpose of termination of pregnancy, otherwise contraindicated in pregnancy.

Category effects on the fetus by FDA ; X.

The active metabolite of misoprostol ; misoprostol acid ; excreted into breast milk. Although reports about the development of public – any adverse side effects in children who are breastfed misoprostol is not registered, it is advisable to be careful in the appointment of misoprostol in this period.

Side effects of substance Misoprostol

From the digestive tract: abdominal pain, dyspepsia, flatulence (2.9%), nausea and / or vomiting, diarrhea (11 – 40%) and constipation (1.1%) .

With the genitourinary system: irregular menstruation, dysmenorrhea, hypermenorrhoea, postmenopausal vaginal bleeding, menorrhagia, metrorrhagia, pelvic pain associated with contractions of the myometrium.

Allergic reactions: skin rash, pruritus, anaphylactic reactions, angioedema.

Other: the change in body weight, dizziness, headache (2.4%), asthenia, fatigue, pyrexia, chills; It is extremely rare in women in pre – and postmenopausal ; cramps.

Interaction

Eating, antacids, misoprostol acid is accompanied by a decrease in plasma concentrations (clinically insignificant). When combined with a magnesium-containing antacids may increase diarrhea caused by misoprostol. Admission for a long time of rifampicin, isoniazid, anticonvulsants, antidepressants, cimetidine, aspirin, indomethacin and phenobarbital drug group, smoking more than 10 cigarettes a day ; misoprostol stimulate the metabolism, reducing its levels in the blood serum.

Within 1 week after misoprostol should stop taking aspirin and other NSAIDs.

Overdose

Phenomena overdose in humans has not been described. From tioksichnosti studies in animals, the clinical symptoms suggestive of an overdose of misoprostol may be drowsiness, confusion, tremors, convulsions, shortness of breath, abdominal pain, diarrhea, fever, palpitations, blood pressure reduction. bradycardia.

Treatment: symptomatic therapy. Hemodialysis is ineffective.

Dosing and Administration

Inside. Dosage is determined individually, depending on the evidence.

To prevent stomach ulcers caused by NSAIDs. and treatment of erosive gastritis and gastric ulcer and duodenal ulcer: 200 mg 2 – 4 times daily (last admission ; at bedtime); daily dose of ; 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%.

To abortion (in combination with mifepristone): 36 – 48 hours after receiving mifepristone 400 mg administered misoprostol.

Precautions substance Misoprostol

In the application for the termination of early pregnancy misoprostol should be used only 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 care, and have appropriately trained medical staff.

The use of the drug requires prevention of Rhesus – conflict and other general activities related to abortion. Before the appointment of misoprostol patient must be informed in detail about the action and the possible side effects of the drug. The patient should be observed in a hospital for 4 – 6 hours before dosing. During and after the administration of the drug to the patient timely medical assistance in the event of massive bleeding or other complications should be provided. After drug administration in patients, usually there is a slight vaginal bleeding in some women ; very long. At a very early stage of pregnancy can have an abortion after mifepristone, but in this case it is also necessary pills of misoprostol for medical abortion optimization results. After administration of misoprostol in approximately 80% of women have an abortion takes place for 6 hours and approximately 10% of women ; for 1 week. The patient need to be retested in the same hospital at 8 – 15 days after ingestion. If necessary, it should be carried out or ultrasound to determine the level of human chorionic gonadotropin in serum. If you suspect incomplete abortion or continuation of the pregnancy is necessary to conduct a comprehensive medical examination in a timely manner. With incomplete abortion or ongoing pregnancy, estimated at 10 – 14 days after mifepristone, carefully carried out the vacuum – aspiration followed by histological examination of aspirate.

The drug as gastroprotectives should be discontinued in the event of diarrhea (mild diarrhea is not considered grounds for cancellation of treatment, drug overturned in severe diarrhea ; about 2% of cases), skin itching, bleeding from the vagina, lowering blood pressure and increasing the activity of transaminases .

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