Ursodeoxycholic acid

Oral
Dissolution of cholesterol-rich gallstones
Adult: 8-12 mg/kg once daily at bedtime or in 2 divided doses. May continue for up to 2 years depending on stone size and composition. Treatment is continued for 3-4 months after radiological disappearance of gallstones. Dosage recommendations may vary among individual products and between countries (refer to specific product guidelines).

Oral
Primary biliary cirrhosis
Adult: 12-16 mg/kg daily in 2-4 divided doses for the 1st 3 months, then may be given as once daily in the evening thereafter. Dosage recommendations may vary among individual products and between countries (refer to specific product guidelines).

Oral
Prophylaxis of gallstones in patients undergoing rapid weight loss
Adult: As cap: 600 mg daily as a single or in 2 divided doses.

Oral
Hepatobiliary disorder associated with cystic fibrosis
Child: As oral susp: ≥1 month 20 mg/kg daily to be given in 2-3 divided doses, may increase up to 30 mg/kg daily as necessary. As cap or tab: ≥6 years 20 mg/kg daily to be given in 2-3 divided doses, may increase up to 30 mg/kg daily as necessary. Dosage recommendations may vary among individual products and between countries (refer to specific product guidelines).

Special Populations: Dissolution of cholesterol-rich gallstones: In obese patient: Up to 15 mg/kg daily may be needed.

Should be taken with food.

Acute inflammation of gallbladder or biliary tract, biliary tract occlusion (common bile duct or cystic duct), frequent episodes of biliary colic, radio-opaque calcified gallstones, impaired contractility of gallbladder, gallstone pancreatitis or biliary-gastrointestinal fistula, non-functioning gallbladder, inflammatory bowel disease; hepatic and intestinal conditions interfering with enterohepatic recirculation of bile acids (e.g. extrahepatic and intrahepatic cholestasis, ileal resection and stoma, regional ileitis); active duodenal and gastric ulcer; unsuccessful portoenterostomy or without recovery of normal bile flow in children with biliary atresia. Acute, chronic or severe hepatic impairment.

Patients with non-visualising gallbladder, variceal bleeding, hepatic encephalopathy, ascites. Obese patients. Children. Pregnancy and lactation. Monitoring Parameters Monitor liver function tests (e.g. AST, ALT, γ-GT) as clinically necessary. If used for the dissolution of gallstone, perform oral cholecystography and ultrasound periodically. Evaluate pregnancy status before initiation of therapy.

Significant: Biliary obstruction. Gastrointestinal disorders: Diarrhoea, pasty stools, nausea, vomiting, constipation, dyspepsia; rarely, severe right upper abdominal pain (if used for primary biliary cirrhosis). Hepatobiliary disorders: Rarely, calcification of gallstones, decompensation of liver cirrhosis. Musculoskeletal and connective tissue disorders: Back pain. Nervous system disorders: Headache, dizziness. Respiratory, thoracic and mediastinal disorders: Upper respiratory tract infection. Skin and subcutaneous tissue disorders: Urticaria, pruritus.

Symptoms: Diarrhoea. Management: Symptomatic treatment with fluid and electrolyte balance restoration, may use ion-exchange resins to bind bile acids in the intestines.

May reduce absorption and efficacy with bile acid-binding resins (e.g. colestyramine, colestipol), antacids (e.g. aluminium hydroxide, aluminium oxide), charcoal. May increase absorption and serum concentration of ciclosporin. May reduce absorption of ciprofloxacin, nitrendipine. Increased hepatic cholesterol secretion and reduced efficacy with estrogen hormones, oral contraceptives, blood cholesterol-lowering agents (e.g. clofibrate). May increase serum concentration of rosuvastatin.

Ursodeoxycholic acid is a naturally occurring bile acid. It reduces cholesterol secretion from the liver and fractional reabsorption of the cholesterol by the intestine resulting in decreased cholesterol content of the bile and bile stones. Synonym: UDCA, Ursodiol.
Absorption: Rapidly absorbed from the gastrointestinal tract.
Distribution: Enters breast milk. Plasma protein binding: Approx 70%.
Metabolism: Undergoes extensive enterohepatic recycling, partly conjugated in the liver prior to biliary excretion. Under the influence of intestinal bacteria, the free and conjugated forms undergo 7α-dehydroxylation to lithocholic acid; some of which are further conjugated and sulfated hepatically.
Excretion: Via faeces; urine (<1%). Elimination half-life: Approx 3.5-5.8 days.

Oral: Store below 30°C.

Cholagogues, Cholelitholytics & Hepatic Protectors

A05AA02 - ursodeoxycholic acid ; Belongs to the class of bile acids. Used in bile therapy.