Misoprostol - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Prostaglandins, thromboxanes, leukotrienes and their antagonists

Included in the formulation

Misoprostol

pills inwards

China Resource Zizhu Pharmaceutical Co., Ltd China

Mirolut®

pills inwards

NIZHFARM, JSC Russia

Topogin

pills inwards

Exceleljin France

Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

VED

АТХ:

G.02.A.D.06 Misoprostol

G.02.A.D. Prostaglandins

Pharmacodynamics:

The drug has a number of pharmacological effects:

- direct influence on parietal cells of the stomach, suppression of basal and stimulated (food, histamine, pentagastrin) secretion of hydrochloric acid;

- decrease in basal (but not histamine-stimulated) pepsin production;

- increase in the formation of protective mucus and bicarbonates;

- Increased blood flow in the mucous membrane of the stomach;

- increased frequency and strength of contractions of the myometrium, promotes the maturation of the cervix.

Pharmacokinetics:

Relationship with plasma proteins 85%. Biotransformation in the mucosa of the gastrointestinal tract and liver to active misoprostol acid, further metabolism in tissues (β- and ω-oxidation). Half-life 20-40 minutes. Elimination of metabolites by the kidneys (73%), with feces (15%).

Indications:

- erosive and ulcerative lesions of the gastrointestinal tract against the background of drug therapy (prevention and treatment of ulcerogenic effects of non-steroidal anti-inflammatory drugs);

- erosive gastroduodenitis, including ulcers of the stomach and duodenum;

- Stomach ulcer and duodenal ulcer.

ICD-10

XI.K20-K31.K25 Stomach ulcer

XI.K20-K31.K26 Duodenal ulcer

XI.K20-K31.K27 Peptic ulcer of unspecified site

XI.K20-K31.K29.1 Other acute gastritis

XI.K55-K63.K63.3 Ulcer of the intestine

XV.O00-O08.O04 Medical abortion

Contraindications:

- individual intolerance, including other prostaglandin preparations;

- pregnancy and the period of breastfeeding;

- children and adolescence (up to 18 years).

Carefully:

- inflammatory bowel diseases and other conditions predisposing to diarrhea;

- risk of dehydration;

- impaired cerebral circulation;

- cardiac ischemia;

- epilepsy.

Pregnancy and lactation:

Recommendations FDA category X (risk of spontaneous incomplete abortion). The drug is prohibited for use during pregnancy and breastfeeding.

Dosing and Administration:

Erosive-ulcerative lesions of the gastrointestinal tract against the background of drug therapy - 200 mcg 2-4 times a day during the entire period of treatment with nonsteroidal anti-inflammatory drugs (800 mg per day is more effective than 400 mg per day).

Erosive gastroduodenitis, including ulcers of the stomach and duodenum - 400 mcg per day.

Stomach ulcer and duodenal ulcer - 200 mcg 3-4 times a day or 400 mcg 2 times a day (the last intake before going to bed) - 4-8 weeks.

The drug is taken inwards while eating.

Side effects:

Diarrhea - 13-40% (dose-dependent, passes independently after 8 days, in 2% of patients requires withdrawal of the drug), pain in the abdomen or epigastrium - 13-40%, flatulence - 2.9%, nausea, vomiting, constipation - 1, 1 %.

Abdominal pain associated with uterine contractions, dysmenorrhea, polymenorrhea, menorrhagia, metrorrhagia.

Allergic reactions: skin rash, itching, angioedema.

Changes in body weight, asthenia, fatigue, headache - 2.4%, extremely rarely - convulsions (in women in the pre- or post-menopausal period).

Overdose:

When an overdose is observed drowsiness, inhibition, tremor, cramps, shortness of breath, abdominal pain, diarrhea, fever, palpitation, lowering blood pressure, bradycardia.

Treatment is symptomatic, hemodialysis is ineffective.

Interaction:

Magnesium-containing antacids - increased diarrhea.

Food intake, antacids - a decrease in the concentration of misoprostol acid in the blood plasma.

With simultaneous use with diclofenac, indomethacin, the side effects of the latter are intensified.

Special instructions:

For abortion, it is only used in combination with mifepristone and only in specialized medical institutions that have appropriately trained medical personnel and who have the capacity to provide emergency surgical gynecological and blood transfusion care. For one week after taking misoprostol, do not prescribe acetylsalicylic acid and other non-steroidal anti-inflammatory drugs.

Instructions

Misoprostol (Misoprostolum)