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Product
Anti-asthmatic Products (Aerocort Inhaler)
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Misoprost(Misoprostol)
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Misoprost
Misoprostol
COMPOSITION
MISOPROST -100 mcg
Each uncoated tablet contains
Misoprostol ............. 100 mcg
MISOPROST -200 mcg
Each uncoated tablet contains
Misoprostol ............. 200 mcg
DOSAGE FORM
100 mcg / 200mcg oral tablets
PHARMACOLOGY
Pharmacodynamics
Misoprost is an analogue of naturally occurring prostaglandin E 1 which promotes peptic ulcer healing and symptomatic relief.
Misoprost protects the gastroduodenal mucosa by inhibiting basal, stimulated and nocturnal acid secretion and by reducing the volume of gastric secretions, the proteolytic activity of the gastric fluid, and increasing bicarbonate and mucus secretion. |
Pharmacokinetics
Misoprostol is rapidly absorbed following oral administration, with peak plasma levels of the active metabolite (misoprostol acid) occurring after about 30 minutes. The plasma elimination half-life of misoprostol acid is 20-40 minutes. No accumulation of misoprostol acid in plasma occurs after repeated dosing of 400 micrograms twice daily.
INDICATIONS
Gastro-Intestinal Use
MISOPROST is indicated for reducing the risk of NSAID-induced gastric ulcers in patients at high risk of complications from gastric ulcer, e.g. the elderly and patients with concomitant debilitating disease, as well as patients at high risk of developing gastric ulceration, such as patients with a history of ulcer.
DOSAGE AND ADMINISTRATION
For Gastro-Intestinal Use
Adult
The recommended adult oral dose for reducing the risk of NSAID induced ulceration is 200 mcg four times daily with food. If this dose is not tolerated, a dose of 100 mcg can be used. MISOPROST should be taken for the duration of NSAID therapy. It should be taken with meals and the last dose of the day should be at bedtime.
Elderly
The usual dosage may be used.
Renal impairment
Available evidence indicates that no adjustment of dosage is necessary in patients with renal impairment.
Hepatic impairment
Misoprostol is metabolised by fatty acid oxidising systems present in organs throughout the body. Its metabolism and plasma levels are therefore unlikely to be affected markedly in patients with hepatic impairment.
Children
Use of Misoprostol in children has not yet been evaluated in the treatment of peptic ulceration or NSAID-induced peptic ulcer disease.
CONTRAINDICATIONS
It is also contraindicated in patients with a known allergy to prostaglandins.
WARNINGS AND PRECAUTIONS
Use in pre-menopausal women : Misoprostol should not be used in pre-menopausal women unless the patient requires nonsteroidal anti-inflammatory (NSAID) therapy and is at high risk of complications from NSAID-induced ulceration.
In such patients it is advised that Misoprostol should only be used if the patient:
• takes effective contraceptive measures
• has been advised of the risks of taking Misoprostol if pregnant.
If pregnancy is suspected the product should be discontinued.
The results of clinical studies indicate that Misoprostol does not produce hypotension at dosages effective in promoting the healing of gastric and duodenal ulcers. Nevertheless, Misoprostol should be used with caution in the presence of disease states where hypotension might precipitate severe complications, e.g., cerebrovascular disease, coronary artery disease or severe peripheral vascular disease including hypertension.
There is no evidence that Misoprost has adverse effects on glucose metabolism in human volunteers or patients with diabetes mellitus.
Drug Interactions
Misoprostol is predominantly metabolised via fatty acid oxidising systems and has shown no adverse effect on the hepatic microsomal mixed function oxidase (P450) enzyme system. In specific studies no clinically significant pharmacokinetic interaction has been demonstrated with antipyrine, diazepam and propranolol. In extensive clinical studies no drug interactions have been attributed to Misoprostol. Additional evidence shows no clinically important pharmacokinetic or pharmacodynamic interaction with nonsteroidal anti-inflammatory drugs including aspirin, diclofenac and ibuprofen.
Use in pregnancy
Misoprostol is contraindicated in pregnant women and in women planning a pregnancy as it increases uterine tone and contractions in pregnancy which may cause partial or complete expulsion of the products of conception. Use in pregnancy has been associated with birth defects
Use in lactation
It is not known if the active metabolite of Misoprostol is excreted in breast milk; therefore Misoprostol should not be administered during breast feeding.
UNDESIRABLE EFFECTS
Gastrointestinal system: Diarrhoea has been reported and is occasionally severe and prolonged and may require withdrawal of the drug. It can be minimised by using single doses not exceeding 200 micrograms with food and by avoiding the use of predominantly magnesium containing antacids when an antacid is required.
Abdominal pain with or without associated dyspepsia or diarrhoea can follow misoprostol therapy.
Other gastrointestinal adverse effects reported include dyspepsia, flatulence, nausea and vomiting.
Female reproductive system: Menorrhagia, vaginal bleeding and intermenstrual bleeding have been reported in pre-and post-menopausal women.
Other adverse events: Skin rashes have been reported. Dizziness has been infrequently reported.
The pattern of adverse events associated with Misoprostol is similar when an NSAID is given concomitantly.
A number of side effects have been reported in clinical studies or in the literature following use of misoprostol for non-approved indications. These include abnormal uterine contractions, uterine haemorrhage, retained placenta, amniotic fluid embolism, incomplete abortion and premature birth.
OVERDOSAGE
Intensification of pharmacological effects may occur with overdose. In the event of overdosage symptomatic and supportive therapy should be given as appropriate. In clinical trials patients have tolerated 1200 micrograms daily for three months without significant adverse effects.
SHELF-LIFE
18 Months
STORAGE AND HANDLING INSTRUCTIONS
Store in a cool dry place
PACKAGING INFORMATION
MISOPROST -100 ..................... Pack 4 tablets
MISOPROST -200 ..................... Pack 4 tablets
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