Uses of Ursocol 150: - Primary biliary cirrhosis - Gallbladder stones Dissolution of cholesterol-rich gallstones, Primary biliary cirrhosis, Prevention of gallstone formation in obese patients experiencing rapid weight loss, Acute inflammation of gallbladder or biliary tract, occlusion of biliary tract, frequent episodes of biliary colic, radio-opaque calcified gallstones, impaired contractility of gallbladder, non-functioning gallbladder, inflammatory bowel disease, hepatic and intestinal conditions interfering w/ enterohepatic recirculation of bile acids, extrahepatic and intrahepatic cholestasis, ileal resection and stoma, regional ileitis, active duodenal and gastric ulcer; acute, chronic or severe hepatic disease.

Anti-gallstones drugs: Bile Acids

Ursodeoxycholic Acid is a naturally occurring bile acid used to treat different hepatobilliary disorders. The activity of Ursodeoxycholic Acid is achieved through a decrease in secretion of cholesterol in bile. Ursodeoxycholic Acid achieves this through a few mechanisms: it reduces cholesterol absorption, suppresses liver cholesterol synthesis and it does not inhibit bile acid synthesis.Therefore, alters bile composition from supersaturated to unsaturated. Ursodeoxycholic Acid also promotes the formation of liquid cholesterol crystal complexes which enhance removal of the cholesterol from the gallbladder into the intestine to be expelled. Ursodeoxycholic Acid improves cholestatic liver diseases by- Protecting cholangiocytes against cytotoxicity of hydrophobic bile acids Stimulating hepatobilliary secretion Protecting hepatocytes against bile acid-induced apoptosis Ursodeoxycholic Acid is completely absorbed in the upper intestine. Time to peak serum concentration varies from 30 to 150 minutes. The rate of absorption ranges from 60-80%. After absorption Ursodeoxycholic Acid enters the portal vein and undergoes extraction from portal blood by liver where it is conjugated with amino acid & that may be either glycine or taurine and then secreted into the hepatic bile ducts. Small quantities of Ursodeoxycholic Acid appear in the circulation and very small amounts are excreted into urine. The biologic half life of Ursodeoxycholic Acid ranges from 3.5-5.8 days.

How to use Ursodeoxycholic Acid: Take this medicine in the dose and duration as advised by your doctor. Swallow it as a whole. Do not chew, crush or break it. Ursodeoxycholic Acid is to be taken with food. Administration: Should be taken with food. Adult Dose: Oral Dissolution of cholesterol-rich gallstones Adult: 8-12 mg/kg once daily at bedtime or in 2 divided doses continued for 3-4 mth after radiological disappearance of gallstones. Duration of treatment: Up to 2 yr. Obese patients: Up to 15 mg/kg daily. Primary biliary cirrhosis Adult: 10-16 mg/kg daily in 2-4 divided doses, may be taken once daily in the evening after the 1st 3 mth. Prophylaxis of gallstones in patients undergoing rapid weight loss Adult: 300 mg bid. Non-alcoholic fatty liver disease: 13-15 mg/kg/day;

Cholestyramine, charcoal and antacids may reduce effectiveness. Aluminum-based antacids may reduce absorption. Oestrogens and clofibrate may counteract effectiveness of ursodeoxycholic acid by increasing cholesterol elimination in bile. Possible increase in ciclosporin serum concentration. Decreased effectiveness of dapsone. Possible decrease in serum ciprofloxacin and nitrendipine.

Acute inflammation of gallbladder or biliary tract, occlusion of biliary tract, frequent episodes of biliary colic, radio-opaque calcified gallstones, impaired contractility of gallbladder, non-functioning gallbladder, inflammatory bowel disease, hepatic and intestinal conditions interfering w/ enterohepatic recirculation of bile acids, extrahepatic and intrahepatic cholestasis, ileal resection and stoma, regional ileitis, active duodenal and gastric ulcer; acute, chronic or severe hepatic disease.

Common - Abdominal pain - Diarrhea - Hair loss - Itching - Nausea - Rash >10% Headache,Dizziness,Diarrhea,Dyspepsia,Nausea/vomiting,Back pain,Upper respiratory tract infection 1-10% Alopecia,Rash,Hyperglycemia,Flatulence,Peptic ulcer,Urinary tract infection,Leukopenia,Thrombocytopenia,Cholecystitis >1% Fatigue,Abdominal pain,Thrombocytopenia,Pruritus,Angioedema,Peripheral edema,Biliary pain

Pregnancy category B. No evidence of harm has been reported in pregnancy. It has been effectively used for the treatment of cholestasis of pregnancy during the last trimester without any side effects. Problems have not been documented in humans regarding breast feeding.

Precaution: Excessive diatery intake of calories and cholesterol should be avoided. Liver function tests and bilirubin levels should be monitored every month for three months after start of therapy. 50% of successfully treated patients will develop further gallstones within 10 yr. Pregnancy and lactation. Monitoring Parameters Monitor LFTs mthly for the 1st 3 mth and every 6 mth thereafter. Lactation: unknown if excreted in breast milk; use caution

Store below 25° C. Protected from light and moisture. Keep the medicine out of the reach of children.

Ursodeoxycholic acid suppresses hepatic synthesis and secretion of cholesterol and also inhibits intestinal absorption of cholesterol.