Ursodiol

Administration

• Type: Hepatobiliary
• Dosage Forms: Cap: 300mg; Tab: 250mg, 500mg
• Routes of Administration: Oral
• Common Trade Names: Actigall, Urso 250, Urso Forte

Adult Dosing

Gallstone dissolution

• 8-10 mg/kg/day PO divided qd-tid

Primary biliary cirrhosis

• 13-15 mg/kg/day PO divided BID-TID

Primary sclerosing cholangitis

• 25-30 mg/kg/day PO divided qd-qid

Steatohepatitis, non-alcoholic

• 10-15 mg/kg/day PO divided qd-qid

Pediatric Dosing

Biliary atresia

• < 1mo
  • 20-30 mg/kg/day PO divided bid
• > 1mo
  • 10-30 mg/kg/day PO divided bid

Pruritus, cholestasis-associated

• > 1mo
  • 15-30 mg/kg/day

Special Populations

Pregnancy Rating

• Category B: may use during pregnancy

Lactation risk

• May use while breastfeeding

Renal Dosing

• Adult: Not defined
• Pediatric: Dose adjustment may be required, but specific guidelines not defined

Hepatic Dosing

• Adult: Not defined
• Pediatric: Dose adjustment may be required, but specific guidelines not defined

Contraindications

• Allergy to class/drug
• Unremitting acute cholecystitis
• Cholangitis, acute
• Biliary obstruction
• Gallstone pancreatitis
• Biliary-GI fistula
• Gallstones, calcified cholesterol
• Gallstones, radiopaque
• Gallstones, radiolucent bile pigment

Adverse Reactions

Serious

• Leukopenia, thrombocytopenia
• Hypersensitivity reaction
• Anaphylaxis
• Jaundice, LFTs elevated

Common

• Diarrhea, constipation
• Headache, dizziness
• nausea, dyspepsia, vomiting, flatulence
• Back pain, MSK pain
• Alopecia, rash, pruritus

Pharmacology

• Half-life: Unknown
• Metabolism: Liver, GI tract
• Excretion: Feces primarily, urine

Mechanism of Action

• Decreases cholesterol synthesis, secretion, and absorption
• Alters bile cholesterol composition