ursodiol

General

Pronunciation
ER-soe-dye-ole

Trade Name(s)

• Actigall

• Urso 250

• Urso Forte

Pregnancy Category
Category B

Ther. class.
gallstone dissolution agents

Indications

• Gallbladder stone dissolution and prevention.

• Primary biliary cirrhosis.

Unlabelled Use(s):

• 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 Effect(s):

• Gallstone dissolution and reduction in gallstone formation.

• ↓ progression of liver disease and improvement in liver function tests.

Pharmacokinetics

Absorption: 90%.

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

Protein Binding: 70%.

Metabolism and 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

Contraindication/Precautions

Contraindicated in:

• Patients requiring cholecystectomy;

• Calcified cholesterol stones, radiopaque stones, bile pigment stones, or stones >20 mm.

Use Cautiously in:
Chronic liver disease.

Adverse Reactions/Side Effects

CNS: anxiety, depression, fatigue, headache, sleep disorder.

Derm: hair thinning, pruritus, rash.

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

Neuro: arthralgias, myalgia.

Resp: cough, rhinitis.

*CAPITALS indicates life-threatening.
*italic indicates most frequent.

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

• Capsules: 300 mg

• Tablets: 250 mg, 500 mg

Assessment

• Monitor abdominal pain prior to and periodically during therapy.

• Monitor ultrasonograms at 6 mo intervals during the first year of therapy.

Lab Test Considerations

• Monitor liver enzymes before and periodically during therapy.

Potential Nursing Diagnoses

• Acute pain (Indications)

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 months of therapy and complete dissolution may not occur. Stone recurrence may occur after dissolution.

• ↓ progression of liver disease and improvement in liver function tests.