Each capsule contains: Ursodeoxycholic acid 250 mg.
Excipients/Inactive Ingredients: Corn starch, starch 1500, aerosil200, magnesium stearate, gelatin, purified water.
Pharmacology: Pharmacodynamics: The mechanism of ursodeoxycholic acid is anticholelithic action is not completely understood, it is known that when administered orally ursodeoxycholic acid is concentrated in bile and decreases biliary cholesterol saturation by inhibiting its intestinal absorption. The reduced cholesterol saturation permits the gradual solubilization of cholesterol from gallstones, resulting in their eventual dissolution.
Ursodeoxycholic acid increases bile flow. In chronic cholestatic liver disease, ursodeoxycholic acid appears to reduce the detergent properties of the bile salts, thus reducing their cytotoxicity. Also, ursodeoxycholic acid may protect liver cells from the damaging activity of toxic bile acids (e.g., lithocholate, deoxycholate, and chenodeoxycholate), which increase in concentration in patients with chronic liver disease.
Pharmacokinetics: Ursodeoxycholic acid is absorbed from the small bowel (about 90% of dose).
Ursodeoxycholic acid is extensively bound to plasma proteins.
Hepatic (first-pass hepatic clearance). Exogenous ursodeoxycholic acid is metabolized in the liver to its taurine and glycine conjugates. The resulting conjugates are secreted into bile.
Time to peak concentration is 1 to 3 hour.
The half life of administered ursodeoxycholic acid is 3.5-5.8 days.
The excretion of ursodeoxycholic acid is primarily fecal; very small amounts are excreted into urine. Small amount of unabsorbed ursodeoxycholic acid passes into the colon where it undergoes bacterial degradation (7-dehydroxylation); resulting lithocholic acid is partly absorbed from the colon but is sulfated in the liver and rapidly eliminated in the feces as the sulfolithocholyl glycine or sulfolithocholyl taurine conjugate.
Dissolution of gallstones in patients with radiolucent, noncalcified, gallbladder stones less than 20 mm diameter in whom elective cholecystectomy would be undertaken except for the presence of increased surgical risk due to systemic disease, advanced age, idiosyncratic reaction to general anesthesia, or for patients who refuse surgery.
Prevention of gallstone formation in obese patients experiencing rapid weight loss.
Compensated primary biliary cirrhosis.
Chronic cholestatic syndrome various liver lesions.
The recommended oral dose for treatment of gallstone disease is 8-10 mg/kg/day given in 2 or 3 divided doses with meals.
Duration of therapy 6-12 months. After complete dissolution, it is recommended that Ursomax be continued for at least 3 months to promote dissolution of particles that are too small to image.
To prevent gall stone formation in obese patient experiencing rapid weight loss the recommended dose is 800 mg twice a day with meals.
Cholestatic liver diseases:
The recommended oral dose for treatment of cholestatic liver diseases is 13-15 mg/kg/day given in 2 divided doses with meals.
Primary biliary cirrhosis:
The daily dose of 10-15 mg/kg/day in divided dose. (See table.)
Click on icon to see table/diagram/image
No cases of ursodeoxycholic acid overdose have been reported.
The most likely manifestation of severe overdose with ursodeoxycholic acid would probably be diarrhea, which should be treated symptomatically.
Ursomax must not be used in the presence of: Allergy to bile acids; Patients with gallstone complications such as biliary-gastrointestinal fistula, biliary obstruction, cholangitis, cholecystitis, pancreatitis or frequent biliary colic.
Ursomax is ineffective for the dissolution of calcified and pigment gallstones and is of no value in patients without a patent and functioning gallbladder.
Liver tests: Patients given ursodeoxycholic acid should have SGPT (ALT), SGOT(AST), GGT, ALP and bilirubin measured at the initiation of therapy and thereafter as indicated by the particular clinical circumstances. Monitoring of serum values is recommended upon initiation of treatment, every 1 to 3 months for the first 3 months of treatment (depending on the indication for use), and then every 6 months during treatment; ursodeoxycholic acid must be discontinued if increased values persist.
Use in Pregnancy & Lactation: Should not be used during pregnancy and lactation without medical advice.
Use in Children: Safety and efficacy have not been established.
Should not be used during pregnancy and lactation without medical advice.
May cause allergy, cholecystitis, leucopenia, peptic ulcer and urinary tract infection.
Should not be taken at the same time as antacids containing aluminium, cholestyramine, colestipol, antihyperlipidemics, especially clofibrate, estrogens, neomycin, oral contraceptives or progestins as these preparations bind ursodeoxycholic acid in the intestine, thus impairing absorption and efficacy.
Note: Do not use the product if there are any significant changes in appearance of the capsules.
Store below 25°C in a dry place, away from direct sunlight.
Shelf Life: Two years from manufacturing date.
A05AA02 - ursodeoxycholic acid ; Belongs to the class of bile acids. Used in bile therapy.