Drug Guide
Ursodiol
Classification
Therapeutic: Bile Acid Agent
Pharmacological: Choleretic, Bile Acid
FDA Approved Indications
- Dissolution of gallstones in patients who are suitable candidates, including those with radiolucent stones; treatment of primary biliary cirrhosis (PBC) to improve liver function tests
Mechanism of Action
Ursodiol decreases cholesterol absorption and synthesis, dissolves cholesterol gallstones by reducing cholesterol saturation in bile, and protects cholangiocytes from toxic bile acids in PBC by replacing more toxic bile acids.
Dosage and Administration
Adult: Typically 8-10 mg/kg/day divided into 2-3 doses; dose adjustment based on response and tolerability.
Pediatric: Use is less common; dose determined by weight and clinical judgment; consult specialist.
Geriatric: Adjust dose based on hepatic function and tolerability; monitor liver tests.
Renal Impairment: Use with caution; renal function should be monitored.
Hepatic Impairment: Adjust dose for hepatic impairment, particularly in PBC patients.
Pharmacokinetics
Absorption: Well absorbed from gastrointestinal tract.
Distribution: Wide distribution; bound to plasma proteins.
Metabolism: Metabolized hepatically.
Excretion: Excreted in bile and feces.
Half Life: Approximately 3 weeks; long half-life reflects enterohepatic recirculation.
Contraindications
- Obstruction of bile ducts
- Allergy to ursodiol or any component of the formulation
Precautions
- Monitor liver function during therapy for PBC; use cautiously in patients with liver impairment or biliary obstruction. Use in pregnancy only if clearly needed; safety not established in pregnancy/lactation.
Adverse Reactions - Common
- Diarrhea (Common)
- Upset stomach/nausea (Common)
- headache (Less common)
Adverse Reactions - Serious
- Cholelithiasis exacerbation (Rare)
- Allergic reactions such as rash or pruritus (Rare)
Drug-Drug Interactions
- Cholestyramine and colestipol (can reduce ursodiol absorption)
Drug-Food Interactions
- High-fat meals may enhance absorption or cause gastrointestinal upset
Drug-Herb Interactions
N/ANursing Implications
Assessment: Monitor liver function tests and symptom improvement during therapy. Assess for gallstone dissolution via imaging.
Diagnoses:
- Ineffective tissue perfusion related to gallstone presence
- Altered nutrition: less than body requirements related to gastrointestinal upset.
Implementation: Administer with meals to enhance absorption and reduce gastrointestinal irritation.
Evaluation: Assess symptom resolution, gallstone dissolution via imaging, and liver function tests periodically.
Patient/Family Teaching
- Take medication with food to improve absorption.
- Report persistent or severe side effects such as diarrhea or abdominal pain.
- Maintain regular follow-up appointments for monitoring.
- Explain purpose of medication and importance of adherence.
Special Considerations
Black Box Warnings: N/A
Genetic Factors: No known significant genetic factors affecting ursodiol efficacy.
Lab Test Interference: May alter liver function tests; interpret tests accordingly.
Overdose Management
Signs/Symptoms: Nausea, diarrhea, abdominal pain, and in severe cases, hepatotoxicity.
Treatment: Supportive care; no specific antidote. Dialysis may not be effective due to enterohepatic recirculation.
Storage and Handling
Storage: Store at room temperature away from moisture, heat, and light.
Stability: Stable for labeled duration when stored properly.