Ursodiol

Trade Names:
Actigall
- Capsules 300 mg

Trade Names:
URSO 250
- Tablets 250 mg

Trade Names:
URSO Forte
- Tablets 500 mg

Pharmacology

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Suppresses hepatic synthesis and cholesterol secretion and inhibits intestinal absorption of cholesterol.

Pharmacokinetics

Absorption

About 90% absorbed in the small bowel.

Metabolism

Extracted from portal blood in the liver where it is conjugated with glycine or taurine and then secreted into the hepatic bile ducts. These conjugates are absorbed in the small intestine. The conjugates is deconjugated in the ileum, leading to formation of free ursodiol that can be reabsorbed and reconjugated in the liver. Some ursodiol is epimerized to chenodiol, which may undergo 7-hydroxylation to lithocholic acid.

Elimination

Various metabolites (including chenodiol, lithocholic acid, and sulfated lithocholic acid conjugates) are excreted in the feces.

Indications and Usage

Dissolution of gallstones in patients with radiolucent, noncalcified, gallbladder stones less than 20 mm in greatest diameter in whom elective cholecystectomy would be undertaken except for the presence of increased surgical risk due to systemic disease, advanced age, idiosyncratic reaction to general anesthesia, or for patients refusing surgery (capsules only); prevention of gallstone formation in obese patients experiencing rapid weight loss (capsules only); treatment of patients with primary biliary cirrhosis (tablets only).

Unlabeled Uses

Cholestasis-associated pruritus; primary sclerosing cholangitis.

Contraindications

Hypersensitivity to any component of product.

Presence of calcified cholesterol stones, radiopaque stones, or radiolucent bile pigment stones; patients with compelling reasons for cholecystectomy, including unremitting acute cholecystitis, cholangitis, biliary obstruction, gallstone pancreatitis, or biliary-GI fistula; allergy to bile acids.

Dosage and Administration

PO 8 to 10 mg/kg/day in 2 or 3 divided doses.

PO 300 mg twice daily.

PO 13 to 15 mg/kg/day in 2 to 4 divided doses with food.

Storage/Stability

Store tablets at controlled room temperature (68° to 77°F). Store capsules at controlled room temperature (59° to 86°F).

Drug Interactions

May decrease ursodiol absorption.

May decrease the efficacy of ursodiol by increasing hepatic cholesterol secretion and encouraging cholesterol gallstone formation.

Laboratory Test Interactions

None well documented.

Adverse Reactions

The following adverse reactions occurred at an incidence rate of 5% or more.

Cardiovascular

Hypertension.

CNS

Asthenia; dizziness; fatigue; headache; insomnia.

Dermatologic

Alopecia; pruritus.

EENT

Bronchitis; pharyngitis.

GI

Abdominal pain; cholecystitis; constipation; diarrhea; dyspepsia; flatulence; GI disorder; nausea; vomiting.

Genitourinary

Dysmenorrhea; UTI.

Musculoskeletal

Arthralgia; arthritis; back pain; musculoskeletal pain; myalgia.

Respiratory

Bronchitis; coughing; sinusitis; upper respiratory tract infection.

Miscellaneous

Allergy; chest pain; influenza-like symptoms; peripheral edema; viral infection.

Precautions

Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Carcinogenesis

Studies suggest bile acids might be involved in pathogenesis of human colon cancer in patients undergoing a cholecystectomy; however, direct evidence is lacking.

Gallbladder nonvisualization

Gallbladder nonvisualization developing during treatment predicts failure of complete stone dissolution and treatment should be discontinued.

Gallstone recurrence

May recur within 2 yr in 30% of patients and within 5 yr in 50% of patients.

Hepatic effects

The lithocholic acid metabolite of ursodiol is hepatotoxic; therefore, monitor AST and ALT.

Patient Information

• Emphasize to patient that effective treatment will require months of treatment.
• Advise patient to read patient information leaflet before starting therapy and with each refill.
• Advise patient taking tablets to take 2 to 4 times daily with food as prescribed. Advise patient to swallow tablets whole and not to chew, crush, or break because contents of tablet have a bitter taste.
• Advise patient taking capsules to take 2 or 3 times daily as prescribed. Advise patient to take without regard to meals but to take with food if stomach upset occurs. Advise patient to swallow capsules whole and not to chew, crush, or open because contents of capsule have a very bitter taste.
• Advise patient that if a dose is missed to skip that dose and take the next dose at the regularly scheduled time.
• Caution patient not to change the dose or stop taking unless advised by health care provider.

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