Each tablet contains Ursodeoxycholic acid, BP 200 mg.
Pharmacology: Pharmacodynamics: Ursodeoxycholic acid is a gallstone dissolving agent which acts by reducing the content of cholesterol in bile. This may be due either to a reduction in hepatic cholesterol synthesis or reduced absorption of cholesterol or both.
Pharmacokinetics: Intestinal absorption after an oral dose of ursodeoxycholic acid is high, with a first-pass clearance of about 50 to 60%. Studies show that passive diffusion occurs, whereupon the drug enters the enterohepatic circulation and is subject to an efficient hepatic extraction mechanism. The 'spillover' into the systemic blood supply is therefore minimal. Plasma levels are not clinically important but may be useful in estimating patient compliance; they reach maximum concentrations at about 60 minutes after ingestion with another peak recorded at 3 hours.
Ursodeoxycholic acid is rapidly conjugated with glycine and taurine in the liver. Microbial biotransformation of the drug and its metabolites occurs when they leave the enterohepatic circulation and is responsible for high levels of faecal lithocholic and 7-ketolithocholic acids during ursodeoxycholic acid therapy. Intestinal flora also hydrolyse conjugated drug back to the parent compound and interconvert ursodeoxycholic and chenodeoxycholic acids.
Dissolution of Pure Cholesterol Gallstones.
Adults: 200-250 mg of ursodeoxycholic acid is orally administered three times a day.
Dosage may be adjusted depending on the patient's age or symptoms. Or as prescribed by the physician.
Diarrhoea may occur. In general, other symptoms of overdose are unlikely because the absorption of Ursodeoxycholic Acid decreases with increasing dose and therefore more is excreted with the faeces. No specific counter-measures are necessary and the consequences of diarrhoea should be treated symptomatically with restoration of fluid and electrolyte balance. However, ion-exchange resins may be useful to bind bile acids in the intestine. Liver function tests monitoring is recommended.
Patients with complete atresia of bile duct.
Patients with severe liver diseases.
Patients with radio-opaque calcified gallstones.
Patients with non-functioning gall bladder.
Patients with acute cholecystitis.
Patients with severe pancreatic diseases.
Patients with peptic ulcer.
Patients who have gallstones in bile duct.
Serum hepatic enzyme level should be monitored periodically during therapy. Although severe adverse reaction following overdosage is not likely to happen, hepatic function test should be performed if necessary.
Use in Children: Cholesterol-rich gallstones are rare in children but when they occur, dosage should be related to bodyweight.
Use in Elderly: There is no evidence to suggest that any alteration in the adult dose is needed but the relevant precautions should be taken into account.
Teratogenicity has been reported in animal experiments. Therefore, the drug should not be used in patients who are or may become pregnant.
Occasionally diarrhea, nausea, vomiting, and rarely abdominal pain, constipation, heartburn, and gastric discomfort may occur.
Occasionally pruritus, and rarely eruption may occur.
Rarely malaise, dizziness, calcified gall bladder, and increased GOT, GPT, and γ-GTP level may occur.
Caution should be exercised when concomitantly using oral antidiabetic drugs such as tolbutamide, since ursodeoxycholic acid may potentiate the action of oral antidiabetic drugs.
In vitro study has shown that cholestyramine, colestipol, charcoal, and certain antacids containing aluminum hydroxide decrease the absorption of the drug.
Drugs known to increase cholesterol elimination in bile, such as estrogen-containing oral contraceptives, and certain blood cholesterol lowering agents, such as clofibrate, should not be prescribed concomitantly.
Store at temperatures not exceeding 30°C.
A05AA02 - ursodeoxycholic acid ; Belongs to the class of bile acids. Used in bile therapy.
Tab 200 mg (white, round tablet, scored on one side engraved with "U" and "T", "200" on the other side) x 100's.