Destone(ursodeoxycholic acid)


Ursodeoxycholic acid


Dissolution of cholesterol-rich gallstones in patients w/ functioning gallbladders. Treatment of primary biliary cirrhosis & sclerosing cholangitis

Dosage / Direction For Use

Dissolution of cholesterol gallstones Approx 10 mg/kg Body wt over 100 kg 5 cap, up to 100 kg 4 cap, up to 80 kg 3 cap, up to 60 kg 2 cap. Biliary reflux gastritis 1 cap daily at bedtime. Symptomatic treatment of primary biliary cirrhosis Daily doses depending on the body wt of the patient which lies between 2-6 cap (approx 10-15 mg of ursodeoxycholic acid/kg).




Special Precaution

Patients w/ severe pancreatic disease; cholelithiasis in bile duct; variceal bleeding, hepatic encephalopathy, ascites or in need of an urgent liver transplantation. Do not give to patients w/ peptic ulcer disease, inflammatory bowel disease, or chronic liver disease. Regularly check the level of liver enzyme (ALT, AST, γ-GT, ALP, total bilirubin). Avoid in pregnancy. Lactation. Elderly.

Adverse Reactions

Sometimes pasty stools, diarrhea, vomit, nausea. Sometimes, itch. Interstitial pneumonia (fever, cough, dyspnea, interstitial pneumonia accompanying chest x-ray abnormality).

Drug Interaction

May increase effect of tolbutamide in diabetics. Reduced absorption w/ cholestryramine, colestipol, charcoal, Al hydroxide & Mg-based antacid. Can affect the absorption of ciclosporin & ciprofloxacin. OCs containing estrogens or clofibrate. Drugs which induce liver injury.


Store at temperatures not exceeding 30°C.


Each capsule contains: Ursodeoxycholic acid 250 mg.


Pharmacology: Pharmacokinetics: Ursodeoxycholic acid is absorbed from the gastrointestinal tract and undergoes enterohepatic recycling. It is partly conjugated in the liver before being excreted into the bile. Under the influence of intestinal bacteria the free and conjugated forms undergo 7α-dehydroxylation to lithocholic acid, some of which is excreted directly in the faeces and the rest absorbed and mainly conjugated and sulfated by the liver before excretion in the faeces. However, in comparison with chenodeoxycholic acid, less ursodeoxycholic acid undergoes such bacterial degradation.Pharmacodynamics: After oral administration of unconjugated UDCA, 30-60% of the dose is passively absorbed in the small and large intestines and undergoes efficient hepatic uptake (>60% of the absorbed dose) and conjugation in the liver with glycine (to a lesser extent with taurine). Because colonic absorption may account for as much as 20% of an ingested dose, unconjugated UDCA is also absorbed in patients who have had ileal resections, as long as high oral doses (4 g/day) of UDCA are administered. Conjugated UDCA is then secreted into the biliary tree and intestine where it undergoes efficient enterohepatic circulation with active reabsorption in the terminal ileum. Under continuous oral treatment at pharmacological doses (10-15 mg/kg/day) UDCA becomes the predominant bile acid in the liver and the systematic circulation, comprising 40-60% of the circulating bile acid pool.