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COMPOSITION

Each GROOVED TABLET contains :

Misoprostol .................................. 200,0 mcg

Excipients, c.s.p. .............................. 1 Tableta

PROPERTIES AND PHARMACOLOGICAL ACTION :

Misoprostol is an E1 Prostaglandin analogue.

MECHANISM OF ACTION / IMPACT :
Cytoprotective : Misoprostol increases natural defense mechanisms of the gastric mucus and promotes healing in disorders caused by heartburn, probably because of an increment in the production of gastric mucus and the secretion of bicarbonate in the mucus.

Antisecretory : Misoprostol inhibits basal and nocturnal gastric acid secretion by a direct action on the parietal cells, and also inhibits gastric acid secretion stimulated by food, coffee, histamine and pentagastrin. Decreases the secretion of pepsin in basal conditions, but not the stimulation of histamine.

Birth Inducer : Misoprostol may produce uterine contractions, bleeding and expulsion of the products of conception.

Absorption : Misoprostol is rapidly absorbed when taken orally. Plasma concentrations of misoprostol acid, which is the primary biologically active metabolite, decreases when the dose is taken with food. The availability of misoprostol acid is reduced by concomitant use of antacids, but this effect does not appear to be clinically important.

Plasma protein binding : It is approximately 85%.

Biotransformation : Rapidly de-esterifies to misoprostol acid. The de-esterified metabolite undergoes further metabolism by beta and omega oxidation; which is followed by reduction of the ketone to prostaglandin F analogs.

Duration of action: 3 to 6 hours.

Elimination :
Is renal and fecal.

Renal : 64-73% of the oral dose is excreted during the first 24 hours, 56% in the first 8 hours.

Fecal : 15% of the oral dose is excreted during the first 24 hours.


INDICATIONS :

• To reduce the risk of NSAID-(nonsteroidal anti-inflammatory drugs, including acetylsalicylic acid)–induced gastric ulcers in patients at high risk of complications from gastric ulcer, e.g., the elderly and/or patients with concomitant disease, as well as patients at high risk of developing gastric ulceration, such as patients with a history of ulcer.
• To treat duodenal ulcers for short periods.

CONTRAINDICATIONS :
Caution should be taken when administering in the following clinical situations :

• Cerebral and/or cardiovascular disease.
• Epilepsy : It is recommended that Misoprostol is used in epileptic patients only when their condition is properly controlled.
• Irritable Bowel Syndrome : This may exacerbate diarrhea symptoms leading to dehydration, so it should be monitored by your doctor.
• Sensitivity to prostaglandins or prostaglandin analogues.


CAUTION :
• Cross Sensitivity and Related Problems : Patients sensitive to other prostaglandins or prostaglandin analogues may also be sensitive to Misoprostol.

Carcinogenesis / Mutagenesis :
Animal studies have shown no evidence that Misoprostol is carcinogenic or mutagenic.

• Pregnancy / Reproduction : Misoprostol is contraindicated during pregnancy.
• Human studies have shown that Misoprostol increases the frequency and intensity of uterine contractions. In addition, administration of Misoprostol has been associated with an increased incidence of uterine bleeding and expulsion of uterine contents.
• Lactation : Misoprostol is rapidly metabolized in the body to the active metabolite (Misoprostol Acid), which is not known whether it is excreted in breast milk. Therefore, administration of Misoprostol is not recommended to nursing mothers because of the potential excretion of Misoprostol Acid in breast milk, which can cause severe diarrhea to the breast-feeding child.
• Pediatrics : No adequate studies have been conducted in relation to age and the effects of Misoprostol in patients under 18 years of age. Its safety and effectiveness have not been well established.
• Geriatrics : Studies in approximately 500 patients 65 years of age or older with ulcers have not shown specific problems that limit the use of Misoprostol in geriatric patients.

INCOMPATIBILITY :
None reported.

DRUG INTERACTIONS AND / OR RELATED PROBLEMS :
Antacids containing magnesium : Concurrent use with antacids containing magnesium can aggravate any Misoprostol-induced diarrhea.

ADVERSE REACTIONS :
Patient should seek medical attention only if they continue or are bothersome.

Frequent Incidences : Abdominal or stomach ache, mild diarrhea.
Less Frequent Incidence : Constipation, dyspepsia, flatulence, headache, nausea and/or vomiting, uterine stimulation (cramps in the lower abdomen or stomach area), vaginal bleeding.

DOSAGE AND ADMINISTRATION ROUTE :

Route of Administration : Oral.
Recommended Adult Dose : For the prevention of NSAID-induced gastric ulcers or for the treatment of duodenal ulcer : 200 mcg (0.2 mg) four times daily with food, or 400 mcg (0.4 mg) twice a day with food. The last dose of the day should be taken at bedtime. If this dose cannot be tolerated, it may be reduced to 100 mcg (0.1 mg). Dose adjustment n renally impaired patients is not routinely needed, but it is recommended to start with a dose of 100 mcg (0.1 mg).
Pediatric and Adolescent Dose : No dosage has been established.
Geriatric Dose : Same as the recommended adult dose.

WARNINGS :

• If you miss a dose, take it as soon as possible. Do not take it if is close to the next dose, do not double the dose.
• If you think you might be pregnant, immediately stop taking this medication and consult your doctor.
• Consult your doctor if diarrhea occurs and if it continues for more than a week.
• Keep away from children.

TREATMENT IN CASE OF OVERDOSE :


Clinical signs that may indicate overdose are : abdominal pain, bradycardia, diarrhea, dyspnea, fever, hypotension, palpitations, sedation, seizures, and tremor.

Treatment : There is no specific treatment for Misoprostol overdose. Treatment should be symptomatic and supportive care is indicated.
Elimination : Because Misoprostol is metabolized the same way as fatty acid, it is unlikely that dialysis is an adequate treatment in overdose cases.

If intentional overdose is suspected, patient should be referred for psychiatric consultation.


CONDITIONS OF CONSERVATION AND STORAGE :

Store below 15 to 30 °C, in airtight containers away from light and moisture.

PRESENTATION :

Box of 28 grooved tablets in 4-tablet aluminum blisters.
Box of 100 grooved tablets in 4-tablet aluminum blisters.

Sold under prescription.

MASTER FARMA S.A.

Address :
Calle Mariano Odicio 490,
Miraflores,
Lima 18 – Perú

Phone :
+51 (1) 446 1250
+51 (1) 242 5577

Fax :
+51 (1) 445 7701



Propiedad de MASTER FARMA S.A. ® - 2006