ursodiol

REMS

Gallbladder stone dissolution and prevention.
Primary biliary cirrhosis.

Unlabeled Use:

Biliary atresia.
TPN-induced cholestasis.

Action ⬆ ⬇

↓cholesterol content of bile and bile stones by suppressing cholesterol synthesis and secretion from the liver and inhibits intestinal absorption of cholesterol.

Therapeutic effects:

Gallstone dissolution and reduction in gallstone formation.
↓progression of liver disease and improvement in liver function tests.

Pharmacokinetics ⬆ ⬇

Absorption: 90% absorbed following oral administration.

Distribution: Only small quantities are found in the systemic circulation; sites of action include the liver, bile, and gut lumen.

Metabolism/Excretion: Undergoes extensive enterohepatic recycling; excreted in feces via bile.

Half-Life: 100 hr.

Time/Action Profile ⬆ ⬇

ROUTE	ONSET	PEAK	DURATION
PO	unknown	unknown	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Patients requiring cholecystectomy;
Calcified cholesterol stones, radiopaque stones, bile pigment stones, or stones >20 mm;
Complete biliary obstruction.

Use Cautiously in:

Chronic liver disease;
Surgical enteroanastomoses or Crohn's disease (↑ risk of bezoar formation).

Adv. Reactions/Side Effects ⬆ ⬇

Derm: hair thinning, pruritus, rash

EENT: rhinitis

GI: abdominal/biliary pain, bezoar formation, constipation, diarrhea, flatulence, ↑liver enzymes, jaundice, nausea, stomatitis, vomiting

MS: arthralgia, myalgia

Neuro: anxiety, depression, fatigue, headache, sleep disorder

Resp: cough

Interactions ⬆ ⬇

Drug-drug:

Cholestyramine, colestipol, and aluminum-containing antacids may ↓ absorption.
Estrogens may ↓ its effectiveness.

Route/Dosage ⬆ ⬇

PO (Adults ): Gallstone dissolution: Initial 8–10 mg/kg/day in 2–3 divided doses; maintenance: 250 mg/day at bedtime for 6 mo–1 yr; Gallstone prevention: 300 mg twice daily; Primary biliary cirrhosis: 13–15 mg/kg/day in 2–4 divided doses.
PO (Children and Infants): TPN-induced cholestasis: 30 mg/kg/day in 2–3 divided doses.
PO (Infants ): Biliary atresia: 10–15 mg/kg/day.

Availability ⬆ ⬇

(Generic available)

Capsules: 200 mg; 300 mg; 400 mg
Tablets: 250 mg; 500 mg

Assessment ⬆ ⬇

Monitor abdominal pain prior to and periodically during therapy. If GI obstructive symptoms present, hold therapy until clinical evaluation complete.
Monitor ultrasonograms at 6 mo intervals during the first yr of therapy.

Lab Test Considerations:

Monitor liver function tests (GGT, alkaline phosphatase, AST, ALT) and bilirubin levels every mo for 3 mo and every 6 mo thereafter. If increase to clinically significant levels, consider discontinuation of therapy.

Implementation ⬆ ⬇

Administer with food. Tablets may be broken in half and swallowed with water. To minimize the bitter taste, advise patient to swallow the half-tablet quickly without chewing. Half-tablets should be stored separately for up to 28 days.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take ursodiol as directed.
Advise patient to avoid aluminum-containing antacids during therapy; may impair absorption.

Evaluation/Desired Outcomes ⬆ ⬇

Dissolution and reduction in formation of gallstones. May take several mo of therapy and complete dissolution may not occur. Stone recurrence may occur after dissolution.
↓progression of liver disease and improvement in liver function tests.

section name header

Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇