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CYTOTEC® Tablets

COMPOSITION:
Each CYTOTEC tablet contains 200 mcg
misoprostol.

PHARMACOLOGICAL ACTION:
CYTOTEC is a synthetic prostaglandin E
1 analogue which has gastric antisecretory and mucosal protective properties. The antisecretory activity is mediated by direct action on specific prostaglandin receptors on the surface of gastric parietal cells. The mucosal protective effect against various damaging agents has been demonstrated in humans with doses that inhibit, and doses which minimally affect acid secretion.
Antisecretory activity:
Effect on acid secretion: In healthy human subjects, CYTOTEC inhibits daytime and nocturnal basal gastric acid secretion and acid secretion stimulated by histamine, pentagastrin, food, tetragastrin, betazole and coffee.
Effect on pepsin secretion and gastric fluid volume: CYTOTEC decreases pepsin and gastric volume under basal conditions.
Effect on serum gastrin: CYTOTEC has no persistent effects on fasting levels of, or on postprandial increase in, serum gastrin.
Mucosal protective activity:
CYTOTEC has properties in animals and humans that strengthen the integrity of the gastroduodenal mucosal barrier against damaging agents. These include stimulation of duodenal bicarbonate secretion and gastric mucus production. In addition, CYTOTEC maintains mucosal haemodynamics.
Other pharmacological effects:
CYTOTEC has been shown to produce uterine contractions which may endanger pregnancy (see Contra-indications).
CYTOTEC does not produce clinically significant effects on serum prolactin, gonadotrophins, TSH, GH, thyroxine, cortisol, gastro-intestinal hormones (somatostatin, gastrin, vaso-active intestinal polypeptide and motilin), creatinine, or uric acid, gastric emptying, immunological competence, platelet aggregation, pulmonary function, or the cardiovascular system.

PHARMACOKINETICS:
CYTOTEC is rapidly absorbed following oral administration.
After an oral dose of radiolabelled CYTOTEC, about 73% of the administered radio-activity is excreted in the urine.
Pharmacokinetic studies in patients with mild to moderate renal impairment showed an increase in T
½, Cmax and AUC in renal impaired, compared to normal patients. In patients with total renal failure, there was an approximate two-fold increase in AUC in four of six patients.
CYTOTEC does not accumulate in red blood cells. The serum protein binding of misoprostol acid is less than 90% and is concentration-independent in the therapeutic range.
CYTOTEC is metabolized by fatty-acid oxidizing systems (beta and omega oxidation) which are present in organs throughout the body. It’s metabolism and plasma levels are therefore unlikely to be markedly affected in hepatically-impaired patients. CYTOTEC does not interfere with hepatic drug-metabolizing enzymes nor hepatic blood flow in animals. In multiple-dose human studies, CYTOTEC did not alter the pharmacokinetics or the bio-availability of propranolol, antipyrine or diazepam.
CYTOTEC bio-availability was reduced (by 16%) when it was co-administered with high doses of antacid. Administration of CYTOTEC with a high fat content meal did not alter the extent of misoprostol absorption but did reduce the rate of absorption resulting in lower C
max and higher Tmax values for misoprostol acid.
In healthy elderly subjects over 64 years of age, the AUC for misoprostol acid was slightly increased from that in younger subjects. This was attributed to the reduced clearance probably due partly to decreased volume of distribution and a slight prolongation of elimination T
½ of this metabolite in the elderly.

INDICATIONS:
CYTOTEC is indicated for co-administration with non-steroidal anti-inflammatory drugs (NSAIDs) for the prevention of gastric and duodenal ulcers, haemorrhagic lesions and erosions induced by NSAIDs.

CONTRA-INDICATIONS:
CYTOTEC should not be administered to anyone with a known hypersensitivity to misoprostol or other prostaglandins.
CYTOTEC SHOULD NOT BE USED IN PREGNANT WOMEN AS TERATOGENICITY IN ANIMALS HAS BEEN DEMONSTRATED AND IT INDUCES UTERINE CONTRACTIONS AND THEREFORE HAS ABORTIFACIENT POTENTIAL.
WOMEN OF CHILDBEARING POTENTIAL SHOULD NOT BE STARTED ON CYTOTEC UNTIL PREGNANCY IS EXCLUDED AND SHOULD BE FULLY COUNSELLED ON THE IMPORTANCE OF ADEQUATE CONTRACEPTION WHILE UNDERGOING TREATMENT.
Although it is not known whether CYTOTEC or misoprostol acid is excreted in human milk, CYTOTEC should not be administered to nursing mothers because the potential excretion of misoprostol acid could cause diarrhoea in nursing infants.
Moderate to severely impaired renal function.
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