Ursodiol

INTRODUCTION

Indications

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.

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.

PHYSICAL THERAPY IMPLICATIONS

Examination and Evaluation

• Watch for changes in mood and behavior, including anxiety and depression. Notify physician if these changes become problematic.

• Assess any muscle or joint pain to rule out musculoskeletal pathology; that is, try to determine if pain is drug induced rather than caused by anatomic or biomechanical problems.

Patient/Client-Related Instruction

• Advise patient about the likelihood of GI problems, including nausea, vomiting, diarrhea, constipation, abdominal pain, flatulence, and irritation in or around the mouth. Instruct patient to report severe or prolonged GI reactions.

• Instruct patient and family/caregivers to report other troublesome side effects such as severe or prolonged headache, cough, nasal irritation, or skin reactions (rash, itching, thinning hair).

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.

Contraindications/Precautions

Contraindicated in: Patients requiring cholecystectomy; Calcified cholesterol stones, radiopaque stones, bile pigment stones, or stones >20 mm.

Use Cautiously in: Chronic liver disease.

Interactions

Drug-Drug: Bile acid sequestering agents (cholestyramine, colestipol) and aluminum based anatacids may decrease effects by reducing absorption. Estrogens, oral. contraceptives, and clofibrate (and perhaps other lipid-lowering drugs) may counteract effectiveness by increasing hepatic cholesterol secretion and encouraging cholesterol gallstone formation.

Route/Dosage

PO (Adults): Gallstone dissolution—Initial 8–10 mg/kg/day in 2–3 divided doses; maintenance: 250 mg/day hs for 6 mo–1 yr; Gallstone prevention—300 mg bid; 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 ...