Adult Dosing

Gallstone dissolution

• 8-10 mg/kg/day PO divided bid-tid

Gallstone prevention in obese patients undergoing rapid weight loss

• 300 mg PO bid. Max: 600 mg/day

Primary Biliary Cirrhosis

• 13-15 mg/kg/day PO divided bid-qid given with food

Pediatric Dosing

• Safety and effectiveness in pediatric patients have not been established

[Outline]

• Adult Dosing
• Pediatric Dosing

• Dissolution of gall stones with radiolucent, noncalcified gallbladder stones <20 mm in greatest diameter in whom elective cholecystectomy would be undertaken except for the presence of increased surgical risk (capsules only)
• Prevention of gallstone formation in obese patients experiencing rapid weight loss (capsules only)
• Treatment of patients with primary biliary cirrhosis (tablets only)

• Hypersensitivity to any of the ingredients of the product
• Allergy to bile acids
• Patients with compelling reasons for cholecystectomy
• Acute cholecystitis
• Acute cholangitis
• Acute biliary obstruction
• Gallstones pancreatitis
• Calcified cholesterol gallstones
• Radiolucent bile pigment stones
• Biliary-GI fistula
• Radiopaque gallstones

• N/A

Renal Dose Adjustment

• Renal impairment: Dose adjustments not defined

Hepatic Dose Adjustment

• Hepatic impairment: Dose adjustments not defined

See Supplemental Patient Information

• Gallbladder stone dissolution requires months of therapy. Complete dissolution does not occur in all patients
• Gall stones may recur within 2 yrs in 30% of patients and within 5 yr in 50% of patients
• Patients with hepatic encephalopathy, variceal bleeding, ascites or in need of an urgent liver transplant should receive appropriate specific treatment
• Calcified cholesterol stones, radiopaque stones, or radiolucent bile pigment stones do not dissolve with ursodiol therapy
• Patients with acute cholecystitis, cholangitis, biliary obstruction, gallstone pancreatitis, or biliary gastrointestinal fistula should not be considered for ursodiol therapy
• Gallbladder nonvisualization developing during therapy predicts failure of complete stone dissolution. Treatment should be discontinued in such cases
• Bile acid sequestering agents and aluminum-based antacids may interfere with the action of ursodiol by reducing its absorption
• Safety beyond 24 months of treatment is not established
• Liver function tests (gamma-GT, alkaline phosphatase, AST, ALT) and bilirubin levels should be monitored every month for three months after initiation of therapy, and then after every 6 months
• Perform gallbladder ultrasound at 6-month intervals for first year of therapy to monitor gallstone response

Cautions: Use cautiously in

• Pregnancy
• Lactation

Supplemental Patient Information

• Should be taken with food

Pregnancy Category:B

Breastfeeding: Due to the low levels of ursodiol in breastmilk, amounts ingested by the infant would be small and would not be expected to cause any adverse effects in breastfed infants. This information is based upon LactMed database (available at http://toxnet.nlm.nih.gov/cgi-bin/sis/htmlgen?LACT last accessed 20 July 2010). Manufacturer advises caution.

• GI: Diarrhea, peptic ulcer, dyspepsia, abdominal pain, nausea, vomiting, constipation
• CV: Hypertension
• RESP: URI symptoms
• EENT: Bronchitis, pharyngitis
• CNS: Dizziness
• ENDO: Diabetes
• ONCO: Breast neoplasm
• HEMA: Leukopenia, thrombocytopenia
• DERM: Alopecia, skin rash, pruritis
• MISC: Anaphylaxis, asthenia, peripheral edema, chest pain

• Inhibits intestinal absorption of cholesterol; decreases cholesterol synthesis and secretion; alters bile cholesterol composition
• Metabolized in liver and GI tract; CYP450: Unknown
• Primarily excreted in feces, minimally in urine
• Half-life: Unknown

US Trade Name(s)

• Actigall
• Urso 250
• Urso Forte

US Availability

ursodiol (generic)

• TABS: 250, 500 mg
• CAPS: 300 mg

Actigall

• CAPS: 300 mg

Urso 250

• TABS: 250 mg

Urso Forte

• TABS: 500 mg

Canadian Trade Name(s)

• Urso
• Urso Ds

Canadian Availability

ursodiol (generic)

• TABS: 250, 500 mg

Urso

• TABS: 250 mg

Urso DS

• TABS: 500 mg

UK Trade Name(s)

• Destolit
• Urdox
• Ursofalk
• Ursogal

UK Availability

ursodeoxycholic acid (generic)

• TABS: 150 mg
• CAPS: 250 mg

Destolit

• TABS: 150 mg

Urdox

• TABS: 300 mg

Ursofalk

• CAPS: 250 mg
• SUSP: 250 mg/5 mL (250 mL)

Ursogal

• TABS: 150 mg
• CAPS: 250 mg

Australian Trade Name(s)

• Ursofalk

Australian Availability

Ursofalk

• CAPS: 250 mg
• SUSP: 50 mg/mL (250 mL)

[Outline]

Gastrointestinal

Gallstone Solubilizing Agents

Pricing data from www.DrugStore.com in U.S.A.

• Ursodiol 250 MG TABS [Bottle] (TEVA PHARMACEUTICALS USA)
  100 mg = $214
  300 mg = $541.98
• Ursodiol 300 MG CAPS [Bottle] (TEVA PHARMACEUTICALS USA)
  30 mg = $71.99
  90 mg = $201.98
• Actigall 300 MG CAPS [Bottle] (WATSON LABS)
  30 mg = $198.98
  90 mg = $551
• Ursodiol 500 MG TABS [Bottle] (TEVA PHARMACEUTICALS USA)
  100 mg = $404.99
  300 mg = $1114.01
• Urso Forte 500 MG TABS [Bottle] (AXCAN PHARMA US)
  30 mg = $185.99
  90 mg = $526
• Urso 250 250 MG TABS [Bottle] (AXCAN PHARMA US)
  30 mg = $106.46
  90 mg = $297.01

Warning: This pricing information is subject to change at the sole discretion of DS Pharmacy. For the most current and up-to-date pricing information, please visit drugstore.com.

• Actigall 300 MG Oral Capsule (Watson Pharma, Inc.)
• URSODIOL 300 mg (STAT RX USA LLC)
• Urso 250 MG Oral Tablet (Axcan Scandipharm Inc. )
• Urso Forte 500 MG Oral Tablet (Axcan Scandipharm Inc. )
• Ursodiol 250 MG Oral Tablet (PRASCO Laboratories)
• Ursodiol 250 MG Oral Tablet (TEVA Pharmaceuticals USA)
• Ursodiol 300 MG Oral Capsule (American Health Packaging)
• Ursodiol 300 MG Oral Capsule (Lannett Company, Inc.)
• Ursodiol 300 MG Oral Capsule (Mylan Pharmaceuticals Inc.)
• Ursodiol 300 MG Oral Capsule (NCS HealthCare of KY, Inc dba Vangard Labs)
• Ursodiol 300 MG Oral Capsule (Rising Pharmaceuticals Inc)
• Ursodiol 300 MG Oral Capsule (TEVA Pharmaceuticals USA Inc)
• Ursodiol 300 MG Oral Capsule (UDL Laboratories, Inc.)
• Ursodiol 300 MG Oral Capsule (Watson Laboratories, Inc.)
• Ursodiol 500 MG Oral Tablet (PRASCO Laboratories)
• Ursodiol 500 MG Oral Tablet (TEVA Pharmaceuticals USA)