Misoprostol (Tablets) Instructions for Use

ATC Code

G02AD06 (Misoprostol)

Active Substance

Misoprostol (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Prostaglandin E₁ preparation that increases the tone and contractile activity of the myometrium

Pharmacotherapeutic Group

Other agents used in gynecology; uterotonic agents; prostaglandins

Pharmacological Action

A synthetic analogue of prostaglandin E₁. It has a cytoprotective effect associated with an increase in mucus formation in the stomach and an increase in bicarbonate secretion by the gastric mucosa. By directly affecting the parietal cells of the stomach, Misoprostol suppresses basal, nocturnal, and stimulated (by food, histamine, pentagastrin) secretion. It reduces basal (but not histamine-stimulated) pepsin production.

It induces contraction of the smooth muscles of the myometrium and dilates the cervix. It increases the frequency and strength of myometrial contractions, having a weak stimulating effect on the smooth muscles of the gastrointestinal tract.

The action begins within 30 minutes and lasts for at least 3-6 hours. At a dose of 50 mcg, the effect is moderate and short; at 200 mcg, it is pronounced.

Pharmacokinetics

When taken orally, it is rapidly and completely absorbed (food delays absorption). Plasma protein binding is 85%. It is metabolized in the walls of the gastrointestinal tract and the liver to the pharmacologically active misoprostol acid. C_max is reached in 12 minutes. C_ss is reached in 2 days. It does not accumulate with repeated administration. T_1/2 is 20-40 minutes. It is excreted by the kidneys (80%) and with bile (15%). In case of renal impairment, an almost twofold increase in C_max and an increase in T_1/2 are possible.

Indications

Prevention of the development of gastric ulcers associated with the use of NSAIDs in patients with an increased risk of ulcer formation; treatment of exacerbation of duodenal ulcer; gastric ulcer.

In combination with mifepristone: termination of pregnancy in the early stages (up to 42 days of amenorrhea).

ICD codes

Dosage Regimen

Take tablets orally with water.

For ulcer prevention with NSAID use, the typical adult dose is 100-200 mcg four times daily with meals and at bedtime.

For active duodenal or gastric ulcer treatment, the typical adult dose is 200 mcg four times daily with meals and at bedtime; continue for at least 4 weeks for duodenal ulcer and 8 weeks for gastric ulcer.

For medical abortion, use only in combination with mifepristone under direct medical supervision; administer 800 mcg (four 200 mcg tablets) as a single dose buccally or vaginally 24-48 hours after mifepristone.

In patients with renal impairment, reduce the single dose to 100 mcg and/or extend the dosing interval.

For all indications, the maximum total daily dose should not exceed 800 mcg.

If a dose is missed, take it as soon as remembered unless it is almost time for the next dose; do not double the dose.

Discontinue use and consult a physician if severe or persistent diarrhea, abdominal pain, or vaginal bleeding occurs.

Adverse Reactions

From the digestive system: abdominal pain, flatulence, nausea, vomiting, diarrhea, constipation.

From the reproductive system: lower abdominal pain associated with myometrial contractions, dysmenorrhea, polymenorrhea, menorrhagia, metrorrhagia.

Allergic reactions: skin rash, itching, angioedema.

Other: change in body weight, asthenia, increased fatigue; very rarely – convulsions (in pre- or postmenopausal women).

Contraindications

Severe liver dysfunction, inflammatory bowel diseases, pregnancy, lactation period, severe renal failure, enteritis, childhood and adolescence under 18 years of age, hypersensitivity to misoprostol.

Use in Pregnancy and Lactation

Use is contraindicated during pregnancy and lactation (breastfeeding).

It must be taken into account that Misoprostol increases uterine tone and can provoke a miscarriage when used as a gastroprotective agent.

If use in women of childbearing age is necessary, a serum pregnancy test should be performed beforehand, which must remain negative for 2 weeks before starting misoprostol therapy. Treatment can only be started on the 2nd-3rd day of a normal menstrual period. Reliable methods of contraception should be used throughout the entire course of treatment.

Use in Hepatic Impairment

Contraindicated in severe liver dysfunction.

Use in Renal Impairment

Contraindicated in severe renal failure.

Pediatric Use

Contraindicated in childhood and adolescence under 18 years of age.

Special Precautions

Use with caution in patients with arterial hypotension, coronary artery disease, cerebrovascular accident, coronary cardiosclerosis, epilepsy, enterocolitis, diarrhea, hypersensitivity to prostaglandins or their analogues.

Use for termination of pregnancy is carried out only in combination with mifepristone and only in specialized medical institutions with appropriately trained medical personnel and equipped to provide emergency surgical gynecological and blood transfusion care.

Acetylsalicylic acid and other NSAIDs should not be prescribed within 1 week after taking misoprostol.

Drug Interactions

With simultaneous use with antacids, the concentration of misoprostol in the blood plasma decreases.

With simultaneous use with magnesium-containing antacids, diarrhea may increase.

A case of decreased anticoagulant effect of acenocoumarol with simultaneous use has been described.

With simultaneous use with diclofenac, indomethacin, the side effects of diclofenac and indomethacin are enhanced.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.