Dosing & Uses
Dosage Forms & Strengths
capsules (Actigall)
- 300mg
tablets (Urso, Urso Forte)
- 250mg
- 500mg
Gallstone Dissolution (Actigall)
8-10 mg/kg/d PO divided q8-12hr PO; not to exceed 300 mg/dose
Maintenance: 250 mg PO HS x6 months
Gallstone prevention (Actigall)
300 mg PO BID
Primary Biliary Cirrhosis (Urso, Urso Forte)
13-15 mg/kg/d PO divided q6-12hr with food
Cystic Fibrosis Liver Disease (Orphan)
Orphan designation for treatment of cystic fibrosis liver disease
Sponsor
- Asklepion Pharmaceuticals, LLC; 5200 Maryland Way; Brentwood, TN 37027
Niemann-Pick Disease (Orphan)
Orphan designation for treatment of Niemann-Pick disease type C
Sponsor
- IntraBio Inc; 270 Devon Road; Tenafly, New Jersey 07670
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Contraindicated (0)
Serious - Use Alternative (0)
Monitor Closely (7)
- aluminum hydroxide
aluminum hydroxide decreases effects of ursodiol by pharmacodynamic antagonism. Use Caution/Monitor.
- calcium carbonate
calcium carbonate decreases effects of ursodiol by pharmacodynamic antagonism. Use Caution/Monitor.
- crofelemer
crofelemer increases levels of ursodiol by Other (see comment). Use Caution/Monitor. Comment: Crofelemer has the potential to inhibit transporters MRP2 and OATP1A2 at concentrations expected in the gut; unlikely to inhibit systemically because minimally absorbed.
- eluxadoline
eluxadoline increases levels of ursodiol by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 substrates.
- ethinylestradiol
ethinylestradiol decreases effects of ursodiol by pharmacodynamic antagonism. Use Caution/Monitor.
- sodium bicarbonate
sodium bicarbonate decreases effects of ursodiol by pharmacodynamic antagonism. Use Caution/Monitor.
- sodium citrate/citric acid
sodium citrate/citric acid decreases effects of ursodiol by pharmacodynamic antagonism. Use Caution/Monitor.
Minor (4)
- cholestyramine
cholestyramine decreases effects of ursodiol by pharmacodynamic antagonism. Minor/Significance Unknown.
- colesevelam
colesevelam decreases effects of ursodiol by pharmacodynamic antagonism. Minor/Significance Unknown.
- colestipol
colestipol decreases effects of ursodiol by pharmacodynamic antagonism. Minor/Significance Unknown.
- mestranol
mestranol decreases effects of ursodiol by pharmacodynamic antagonism. Minor/Significance Unknown.
Adverse Effects
>10%
Headache
Dizziness
Diarrhea
Dyspepsia
Nausea/vomiting
Back pain
Upper respiratory tract infection
1-10%
Alopecia
Rash
Hyperglycemia
Flatulence
Peptic ulcer
Urinary tract infection
Leukopenia
Thrombocytopenia
Cholecystitis
>1%
Fatigue
Abdominal pain
Thrombocytopenia
Pruritus
Angioedema
Peripheral edema
Biliary pain
Postmarketing Reports
Hepatobiliary disorders: Jaundice (or aggravation of pre-existing jaundice)
Abnormal laboratory tests: Increased ALT, AST, alkaline phosphatase, bilirubin, gamma-GT
Gastrointestinal disorders: Abdominal discomfort, enteroliths (bezoars), constipation
Warnings
Contraindications
Hypersensitivity
Gallstone complication requiring surgery
Known hepatocyte or bile ductal abnormalities, inflammatory bowel disease
Calcified gallstones, bile acid allergy, chronic hepatic disease
Billiary gastrointestinal fistula
Patients requiring cholecystectomy
Cautions
Only use in radiolucent, non calcified, high cholesterol content gallstone
Use caution in chronic liver disease
In nonvisualizing gallbladders use caution and discontinue therapy if gallbladder nonvisualization occurs during treatment
Liver function tests (gamma-GT, alkaline phosphatase, AST, ALT) and bilirubin levels should be monitored q3mo x3 months after start of therapy, and q6mo thereafter; consider treatment discontinuation if parameters increase to a level considered clinically significant in patients with history of stable liver function test levels
Patients with variceal bleeding, hepatic encephalopathy, ascites or in need of an urgent liver transplant, should receive appropriate specific treatment
Gallbladder stone dissolution may take several months of therapy and complete dissolution may not occur; reocurrence of stones may happen within 5 years in up to 50% of patients receiving therapy
Enteroliths in patients with risk for intestinal stenosis or stasis
- There are rare postmarketing reports of URSO-treated patients who developed enteroliths (bezoars) resulting in obstructive symptoms that required surgical intervention; these patients had medical conditions that predisposed them to intestinal stenosis or stasis (eg, surgical enteroanastomoses, Crohn's disease); if a patient presents with obstructive gastrointestinal symptoms, hold URSO until a clinical evaluation conducted
Pregnancy & Lactation
Pregnancy
Available published data on use of ursodiol in pregnant women derived from randomized controlled trials, observational studies, and case series collected over several decades have not identified a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes; most reported exposures to ursodiol occurred in second and third trimester of pregnancy
Animal data
- In animal reproduction studies, ursodiol had no adverse effects on embryo-fetal development when administered at doses greater than human therapeutic doses
Lactation
Ursodiol is naturally present in human milk; there are no reports of adverse effects of ursodiol on breastfed child, but reports are extremely limited; there are no data on effects of ursodiol on milk production; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed child from drug or from underlying maternal condition
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Naturally-occurring bile acid; reduces cholesterol secretion from the liver; reduces the fractional reabsorption of cholesterol by the intestines.
Absorption
Bioavailability: 90%
Onset: Initial response for gallstone dissolution is 3-6 months
Distribution
Protein Bound: 70%
Metabolism
Taken up rapidly by the liver, conjugated with glycine or taurine, and excreted in the bile
Nonabsorbed ursodiol passes into the colon where it is 7-dehydroxylated to lithocholic acid (an intermediary compound, sometimes formed, is called chenodiol); chenodiol is then dehydroxylated to lithocholic acid
Metabolites: Glyco-ursodeoxycholic acid, tauro-ursodeoxycholic acid, 7-keto-lithocholic acid (inactive); lithocholic acid (inactive) is formed from the 7-hydroxylation of ursodiol and chenodiol; a small portion is metabolized to sulfated lithocholic acid conjugates which are excreted in bile & eliminated in feces
Elimination
Excretion: Mainly in feces
Images
BRAND | FORM. | UNIT PRICE | PILL IMAGE |
---|---|---|---|
ursodiol oral - | 300 mg capsule | ![]() | |
ursodiol oral - | 250 mg tablet | ![]() | |
ursodiol oral - | 500 mg tablet | ![]() | |
ursodiol oral - | 250 mg tablet | ![]() | |
ursodiol oral - | 500 mg tablet | ![]() | |
ursodiol oral - | 300 mg capsule | ![]() | |
ursodiol oral - | 300 mg capsule | ![]() | |
ursodiol oral - | 500 mg tablet | ![]() | |
ursodiol oral - | 500 mg tablet | ![]() | |
ursodiol oral - | 300 mg capsule | ![]() | |
ursodiol oral - | 250 mg tablet | ![]() | |
ursodiol oral - | 250 mg tablet | ![]() | |
ursodiol oral - | 300 mg capsule | ![]() | |
ursodiol oral - | 500 mg tablet | ![]() | |
ursodiol oral - | 250 mg tablet | ![]() | |
ursodiol oral - | 400 mg capsule | ![]() | |
ursodiol oral - | 200 mg capsule | ![]() | |
ursodiol oral - | 250 mg tablet | ![]() | |
ursodiol oral - | 300 mg capsule | ![]() | |
Reltone oral - | 400 mg capsule | ![]() | |
Reltone oral - | 200 mg capsule | ![]() | |
URSO 250 oral - | 250 mg tablet | ![]() | |
URSO Forte oral - | 500 mg tablet | ![]() |
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