Description
Ursodeoxycholic acid is used to reduce the cholesterol saturation of bile and to promote the dissolution of gallstones. The cholesterol saturation of bile is reduced by Ursodeoxycholic acid, allowing gradual solubilization of cholesterol gallstones. Cholesterol of secretion into bile is reduced and bile acid secretion rate is increased during Ursodeoxycholic acid treatment without a reduction in phospholipids.
Indication
Ursodeoxycholic Acid is indicated for the treatment of Cholestasis (Jaundice), Viral Hepatitis, Alcoholic Fatty Liver, Primary Billiary Cirrhosis (PBC), Primary Sclerosing Cholangitis (PSC), Dissolution of Gallstones and Non-Alcoholic Steato Hepatitis (NASH).
Pharmacology
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.
Dosage
Dissolution of Gall stones: 8-12 mg/kg/day either as single night time dose or in divided dosesPBC: 10-15 mg/kg/day in 2-4 divided dosesAcute Viral Hepatitis: 600 mg/dayAlcoholic Fatty Liver: 300 mg/dayPSC: 25-30 mg/kg/dayNASH: 13-15 mg/kg/day
Interaction
Ursodeoxycholic Acid should not be used with drugs, such as oestrogenic hormones, that increase bile cholesterol. Concomitant administration with bile-acid binding drugs including antacids, charcoal and cholestyramine should be avoided, since this may reduce the effectiveness of therapy with Ursodeoxycholic acid.
Contradiction
Non-functioning gall-bladder calcified and pigmented gallstones, inflammatory bowel disease.
Side Effect
Commonly reported side effects are nausea, vomiting, diarrhoea, gallstone opacilication, pruritus.
Pregnancy
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
It should be used cautiously in those with liver disease.
Overdose
Storage
Store below 25?ø C. Protected from light and moisture. Keep the medicine out of the reach of children.