Topogin (Tablets) Instructions for Use

Marketing Authorization Holder

Exelgyn (France)

Manufactured By

Delpharm Lille, SAS (France)

ATC Code

G02AD06 (Misoprostol)

Active Substance

Misoprostol (Rec.INN registered by WHO)

Dosage Form

Topogin

Tablets 200 mcg: 4 pcs.

Dosage Form, Packaging, and Composition

Tablets are white or almost white, round, flat-cylindrical in shape, with a score on one side and a bevel on both sides; above the score, the letter “M” is imprinted as a depressed print, and below the score is the number “200”.

Excipients: microcrystalline cellulose – 175.8 mg, hypromellose – 20 mg, sodium carboxymethyl starch (type A) – 3 mg, hydrogenated castor oil – 1 mg.

4 pcs. – PVC/PVdC/Al blisters (1) – cardboard packs.
4 pcs. – Al/Al blisters (1) – cardboard packs.

Clinical-Pharmacological Group

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

Pharmacotherapeutic Group

Labor stimulant – synthetic PGE1 analogue

Pharmacological Action

It is a synthetic analogue of prostaglandin E₁. It has a cytoprotective effect associated with an increase in mucus production 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-lived; 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 impaired renal function, 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 disease, gastric ulcer disease.

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

ICD codes

Dosage Regimen

Take orally. For ulcer prevention during NSAID therapy, administer 200 mcg two to four times daily with meals and at bedtime.

For active duodenal or gastric ulcer treatment, the usual dose is 200 mcg four times daily with meals and at bedtime. Continue therapy for at least 4 weeks for duodenal ulcer and 8 weeks for gastric ulcer, or until complete healing is confirmed.

For medical termination of pregnancy, use only in combination with mifepristone and under direct medical supervision in a qualified facility. A single dose of 400 mcg is administered buccally or vaginally, 36 to 48 hours after taking mifepristone.

In patients with increased sensitivity or moderate renal impairment, initiate therapy with a reduced dose of 100 mcg. The total daily dose should not exceed 600 mcg in these patients.

For all indications, the maximum single dose is 400 mcg. The maximum total daily dose is 800 mcg.

Administer the final daily dose at bedtime to suppress nocturnal acid secretion. If significant diarrhea occurs, reduce the dose or temporarily discontinue use.

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 – seizures (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 during pregnancy and during the lactation (breastfeeding) period is contraindicated.

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

If it is necessary to use it in women of childbearing age, a serum pregnancy test should be performed beforehand, which must remain negative for 2 weeks before starting misoprostol therapy. Treatment can be started only 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 children and adolescents 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 that have appropriately trained medical personnel and have the capacity 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 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.