Indula

Misoprostol is extensively absorbed, and undergoes rapid de-esterification to its free acid, which is responsible for its clinical activity and, unlike the parent compound, is detectable in plasma. Maximum plasma concentrations of Misoprostol acid are diminished when the dose is taken with food and total availability of Misoprostol acid is reduced by use of concomitant antacid. Misoprostol has both antisecretory (inhibiting gastric acid secretion) and (in animals) mucosal protective properties. NSAIDs inhibit prostaglandin synthesis, and a deficiency of prostaglandins within the gastric mucosa may lead to diminishing bicarbonate and mucus secretion and may contribute to the mucosal damage caused by these agents. Misoprostol can increase bicarbonate and mucus production, but in man this has been shown at doses 200 meg and above that are also antisecretory. It is therefore not possible to tell whether the ability of Misoprostol to reduce the risk of gastric ulcer is the result of its antisecretory effect, its mucosal protective effect, or both.

There is no evidence of clinically significant interaction between Misoprostol and cardiac, pulmonary, CNS drugs and NSAID’s. The bioavailability of Misoprostol is decreased with high doses of antacid.

Generally, Misoprostol is well tolerated. The most frequent adverse effects associated with Misoprostol therapy involve the GI tract such as diarrhea, abdominal pain, dyspepsia, flatulence, nausea, vomiting, rashes and dizziness. The incidence of diarrhea may be minimized by administering the drug after meal and at bedtime and by avoiding concomitant administration with a magnesium-containing or other laxative antacid.

Because of the abortifacient property of the Misoprostol component, it is contraindicated in women who are pregnant. It should not be used in women of childbearing potential unless the patient requires nonsteroidal anti-inflammatory drug (NSAID) therapy and is at high risk of developing gastric or duodenal ulceration or for developing complications from gastric or duodenal ulcers associated with the use of the NSAID. In such patients, it may be prescribed if the patient:

• has had a negative serum pregnancy test within 2 weeks prior to beginning therapy.
• is capable of complying with effective contraceptive measures.
• has received both oral and written warnings of the hazards of Misoprostol, the risk of possible contraception failure, and the danger to other women of childbearing potential should the drug be taken by mistake.
• will begin it only on the second or third day of the next normal menstrual period.

Excretion of the active metabolite (Misoprostol acid) into milk is possible but has not been studied. Because of the potential for serious adverse reactions in nursing infants, it is not recommended for use by nursing mothers.

In case of prevention and treatment of NSAID induced gastric and duodenal ulcer: Misoprostol is contraindicated in women who are pregnant, and should not be used in women of child bearing potential unless the patient requires NSAID therapy. Women of child bearing potential should be told that they must not be pregnant when Misoprostol therapy is initiated and they must use an effective contraception method while taking misoprostol.

In case of induction of labor: The pregnancy should have completed 38 weeks gestation by reliable dating, or lung maturity as evidenced by a L/S >2.0 or a positive phosphotidyl glycerol test, or completed 36 weeks gestation with a maternal or fetal medical indication for induction of labor. Induction of labor is contraindicated in acute fetal distress, abruptio placenta, placenta previa or unexplained vaginal bleeding. The fetus should be in vertex presentation.

Use in children: Safety and effectiveness of Misoprostol in children below the age of 18 years have not been established.

Drugs acting on the Uterus, Prostaglandin analogues

The toxic dose of Misoprostol in human has not been determined. Clinical signs that may indicate an overdose are a sedation, tremor, convulsions, dyspnea, abdominal pain, diarrhea and fever. Symptoms should be treated with supportive therapy.

Store in a cool and dry place, protected from light and moisture. Keep out of the reach of the children.