Ursodeoxycholic Acid

Registered South African indications: 

• Primary biliary cirrhosis 
• Gallstones

Contraindications

Capsules

• Hypersensitivity to the active ingredient or any of its excipients
• Acute inflammation of the gall bladder or biliary tract
• Occlusion of the biliary tract (occlusion of the common bile duct or cystic duct)
• Peptic ulcer disease
• Frequent episodes of biliary colic
• Non-functional gall bladder
• Radio-opaque/calcified gallstones

Tablets

• Hypersensitivity to the active ingredient or any of its excipients
• Hypersensitivity to allergy to bile acids
• Peptic ulcer disease
• Chronic liver disease
• Inflammatory diseases of the small intestine and colon
• Bile duct obstruction, including:
  • Radio-opaque, calcified, or bile pigment stones
  • Non-functioning gallbladders
• Other gallstone complications, such as:
  • Biliary-gastrointestinal fistula
  • Biliary obstruction
  • Cholangitis
  • Cholecystitis
  • Pancreatitis
• Pregnancy or potential pregnancy

Cautions

• Pregnancy (cap)
• Breastfeeding
• Galactose intolerance
• Lapp lactase deficiency
• Glucose-galactose malabsorption
• Use of hormonal contraceptives
• Chronic diarrhoea
• Known (E110) colouring (Aluminium-based) agent

Forms avail. in SA and covered in this monograph: cap, tab 

Primary biliary cirrhosis
- Provided there is no decompensated hepatic cirrhosis

• Oral (cap, tab): 10-15mg/kg/day, in 2-4 divided doses

Dissolution of radiolucent cholesterol gallstones in a functioning gallbladder

• Oral (cap, tab): 8-12mg/kg/day, in divided doses after meals

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Treatment should be continued until 2 successive cholecystograms and/or ultrasound investigations 4-12 weeks apart have failed to demonstrate gallstones

Paed. forms avail. in SA and covered in this monograph: cap, tab

Biliary atresia
Progressive familial intrahepatic cholestasis

• Oral (cap, tab): 10-30mg/kg/day, in 3 divided doses

Gallstones

• Oral (cap, tab): 8-10mg/kg/day; Treatment duration: 6-24 months

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Initiate treatment in consultation with a paediatric gastroenterologist

Pregnancy

Capsules

• Caution; not recommended

Tablets

• Contraindicated

Breastfeeding 

• Caution; not recommended
• There are no clinical data available on the safety of ursodeoxycholic acid in women who are breastfeeding. Therefore, ursodeoxycholic acid is not recommended for breastfeeding women

Fertility

• Animal studies did not show and influence of ursodeoxycholic acid on fertility. Human data on fertility effects following treatment with ursodeoxycholic acid are not available

Renal Impairment

• No dose adjustment recommended 

Hepatic Impairment

Capsules

• Caution; no dose adjustment recommended

Tablets

• Chronic liver disease: Contraindicated

Elderly 

• No dose adjustment recommended 

Porphyria Information

• Not porphyrinogenic (NP)

Drugs in Sport

• Permitted - No warnings

Gastrointestinal Disorders

• Pale stools
• Diarrhoea
• Upper abdominal pain
• Nausea and vomiting

Hepatobiliary Disorders

• Calcification of gallstones
• Decompensation of hepatic cirrhosis

Skin and Subcutaneous Tissue Disorders

• Urticaria
• Pruritus

• Colestyramine
• Colestipol
• Aluminium hydroxide
• Aluminium oxide
• Charcoal
• Ciclosporin
• Ciprofloxacin
• Nitrendipine
• Dapsone
• Oestrogenic hormones
• Oral contraceptives
• Cholesterol lowering agents

• Hepatic function
• Ultrasound

Pharmacokinetic properties

• The half-life of ursodeoxycholic acid is 3.5 to 5.8 days

Ursodeoxycholic acid decreases the cholesterol content of bile and bile stones by reducing the secretion of cholesterol from the liver and the fractional reabsorption of cholesterol by the intestines. The mechanism of action in primary biliary cirrhosis is not clearly defined.

Tablet 100mg

• Ursotan (Sanofi) originator

Capsule 250mg

• Ursofalk (Orphan) originator