Ursodeoxycholic Acid (Ursodiol) - Drug Information - UpToDate

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Ursodeoxycholic acid (ursodiol): Drug information
Copyright 1978-2022 Lexicomp, Inc. All rights reserved.
Contributor Disclosures
(For additional information see "Ursodeoxycholic acid (ursodiol): Patient drug information" and see "Ursodeoxycholic
acid (ursodiol): Pediatric drug information")
For abbreviations, symbols, and age group definitions used in Lexicomp ( show table)
Brand Names: US
Actigall [DSC];
Reltone;
Urso 250;
Urso Forte
Brand Names: Canada

AG-Ursodiol;
GLN-Ursodiol;
JAMP-Ursodiol;
PMS-Ursodiol;
PMS-Ursodiol C;
Urso;
Urso DS
Pharmacologic Category
Gallstone Dissolution Agent
Dosing: Adult
Collapse All
Gallstone dissolution 
Gallstone dissolution (capsules): Oral: 8 to 10 mg/kg/day in 2 to 3 divided doses;

use beyond 24 months is not established.
Gallstone prevention 
Gallstone prevention (capsules): Oral: 600 mg/day in 1 or 2 divided doses.
Gallstone prevention post–bariatric surgery 
https://www.uptodate.com/contents/ursodeoxycholic-acid-ursodiol-drug-information/print?search=ursofalk&topicRef=670&source=see_link 1/15
Gallstone prevention post–bariatric surgery (off-label use): Oral: 500 to 600 mg

once daily or in 2 divided doses for 6 months. Note: Doses up to 1,200 mg/day were
effective but were associated with a higher incidence of nonadherence (Magouliotis
2017).
Hepatic sinusoidal obstruction syndrome associated with stem cell transplant, 

prevention
Hepatic sinusoidal obstruction syndrome associated with stem cell transplant,

prevention (off-label use): Oral: 12 mg/kg/day in 2 divided doses beginning 1 day
before the conditioning regimen and continuing for 90 days after transplantation
(Ruutu 2002; Ruutu 2013). Refer to institutional protocols for further information.
Intrahepatic cholestasis of pregnancy 
Intrahepatic cholestasis of pregnancy (off-label use): Oral: 10 to 15 mg/kg/day in 2

to 3 divided doses (ACG [Tran 2016]; SMFM [Lee 2021]) or 500 mg twice daily,
gradually increase in increments of 500 mg/day (range: 500 mg to 2,000 mg/day in
divided doses) (Chappell 2019); continue until delivery.
Primary biliary cholangitis 
Primary biliary cholangitis (tablets): Oral: 13 to 15 mg/kg/day in 2 to 4 divided

doses (with food). Note: May be given once daily (at bedtime) to improve compliance
(AASLD [Lindor 2019]).
Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.
Dosing: Hepatic Impairment: Adult

Dosing: Pediatric
(For additional information see "Ursodeoxycholic acid (ursodiol): Pediatric drug

information")
Note: Extemporaneously compounded oral suspensions are available in multiple
concentrations (eg, 20 mg/mL, 25 mg/mL, 50 mg/mL, 60 mg/mL); precautions should be
taken to verify and avoid confusion between the different concentrations; dose should be
clearly presented as mg of ursodiol (ie, not in mL or number of tablets).
Biliary atresia, status post-Kasai procedure: Limited data available: Infants and
Children: Oral: 10 to 20 mg/kg/day in 2 to 3 divided doses. Dosing based on small
prospective and retrospective trials that included ursodiol as part of a multidrug
regimen designed to reduce the risk of cholangitis (Kelly 2007; Meyers 2003; Nittono
1989; Stringer 2007; Yamashiro 1994). Some patients may require higher doses (Wong
2019); a range of 20 to 36 mg/kg/day (mean: 25 mg/kg/day) in divided doses was
reported in neonates and infants (n=16) following Kasai procedures at a median age of
54 days (range: 14 to 89 days) (Willot 2008).
Cystic fibrosis-related liver disease: Limited data available: Infants, Children, and
Adolescents: Oral: Initial: 20 mg/kg/day in 2 divided doses; reported range: 10 to 30
mg/kg/day in divided doses; individualize dose based on patient response (Columbo
1990; Debray 2011; Kappler 2012; Lepage 1997; Sokol 1999; Warner 2021).
Parenteral nutrition-induced cholestasis, treatment: Limited data available (ASPEN

[Wales 2014]): Infants and Children: Oral: 30 mg/kg/day in 3 divided doses (Chen 2004;
De Marco 2006; Spagnuolo 1996).
Pruritus secondary to cholestasis: Limited data available: Infants, Children, and

Adolescents: Oral: 15 to 20 mg/kg/day once daily or in divided doses twice daily; doses
up to 30 mg/kg/day may be necessary in some patients (Dinler 1999; Hassan 2020;
Narkewicz 1998). Dosing based on long-term (2.5 years), open-label, crossover trial of
13 patients (ages 2 to 27 years) with intrahepatic cholestasis; six of the 13 patients had
symptomatic improvement in pruritus (Narkewicz 1998). In another study of 24
pediatric patients (1.5 to 15 years) treated with ursodiol, all patients experienced
improvement in pruritus and 16.7% had complete resolution of pruritus (Dinler 1999).
Dosing: Kidney Impairment: Pediatric

Dosing: Hepatic Impairment: Pediatric

Dosing: Older Adult

Refer to adult dosing.
Dosage Forms: US
Excipient information presented when available (limited, particularly for generics); consult
specific product labeling. [DSC] = Discontinued product
Capsule, Oral:
Actigall: 300 mg [DSC]

Actigall: 300 mg [DSC] [contains corn starch]
Reltone: 200 mg [contains corn starch]
Reltone: 400 mg [contains corn starch, fd&c yellow #10 (quinoline yellow), fd&c
yellow #6 (sunset yellow)]
Generic: 200 mg, 300 mg, 400 mg
Tablet, Oral:
Urso 250: 250 mg
Urso Forte: 500 mg [scored]
Generic: 250 mg, 500 mg
Generic Equivalent Available: US

Yes
Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult
specific product labeling.
Tablet, Oral:
Urso: 250 mg
Urso DS: 500 mg
Generic: 250 mg, 500 mg
Administration: Adult
Oral: Do not administer with aluminum-based antacids or bile acid sequestrants. If
aluminum-based antacids are needed, administer 2 hours after ursodiol; some experts
recommend administering ursodiol 1 hour prior to or 4 to 5 hours after bile acid
sequestrants (AASLD [Lindor 2019]; Rust 2000). Urso Forte can be split into halves for
appropriate dosage; do not chew. Tablets should be taken with food.
Administration: Pediatric
Oral: Do not administer with aluminum-based antacids or bile acid sequestrants. If

aluminum-based antacids are needed, administer 2 hours after ursodiol; administer
ursodiol 5 hours or more after bile acid sequestrants (Rust 2000).
Tablets: Urso Forte can be split into halves for appropriate dosage; do not chew.
Urso and Urso Forte should be administered with food.
Use: Labeled Indications
Gallstones (capsules only):
Treatment of patients 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 caused by systemic disease, advanced
age, idiosyncratic reaction to general anesthesia, or for those patients who refuse
surgery. Safety for use of ursodiol beyond 24 months is not established.
Prevention of gallstone formation in obese patients experiencing rapid weight loss.
Primary biliary cholangitis (tablets only): Treatment of patients with primary biliary
cholangitis (PBC) (previously referred to as primary biliary cirrhosis).
Use: Off-Label: Adult
Gallstone prevention post–bariatric surgery; Hepatic sinusoidal obstruction syndrome

associated with stem cell transplant, prevention; Intrahepatic cholestasis of pregnancy
Medication Safety Issues

Sound-alike/look-alike issues:
Ursodiol may be confused with ulipristal
Adverse Reactions
The following adverse drug reactions and incidences are derived from product labeling
unless otherwise specified.
>10%:
Central nervous system: Headache (≤25%), dizziness (17%)
Gastrointestinal: Diarrhea (≤27%), constipation (≤26%), dyspepsia (≤17%), nausea

(≤17%)
Neuromuscular & skeletal: Back pain (≤12%)
Respiratory: Upper respiratory tract infection (≤16%)
1% to 10%:
Dermatologic: Alopecia (5%), skin rash (3%)
Endocrine & metabolic: Hyperglycemia (1%)
Gastrointestinal: Vomiting (≤10%), peptic ulcer (1%)
Genitourinary: Urinary tract infection (7%)
Hematologic & oncologic: Leukopenia (3%), thrombocytopenia (1%)
Hepatic: Cholecystitis (5%)
Hypersensitivity: Hypersensitivity reaction (5%)
Infection: Viral infection (9%)
Neuromuscular & skeletal: Arthritis (6%), musculoskeletal pain (6%)
Renal: Increased serum creatinine (1%)
Respiratory: Pharyngitis (≤8%), bronchitis (7%), cough (7%), flu-like symptoms (7%)
<1%, postmarketing, and/or case reports: Abdominal distress, abdominal pain,

abnormal hepatic function tests, angioedema, anorexia, biliary colic, esophagitis, facial
edema, fever, hepatobiliary disease, increased gamma-glutamyl transferase, increased
liver enzymes, increased serum alkaline phosphatase, increased serum ALT, increased
serum AST, increased serum bilirubin, jaundice, laryngeal edema, malaise, metallic
taste, myalgia, peripheral edema, pruritus, transaminases increased, urticaria,
weakness
Contraindications
Hypersensitivity to ursodiol or any component of the formulation (tablet); not to be

used with calcified cholesterol stones, radiopaque stones, or radiolucent bile pigment
stones; patients with unremitting acute cholecystitis, cholangitis, biliary obstruction,
gallstone pancreatitis, or biliary-gastrointestinal fistula; allergy to bile acids
Canadian labeling: Additional contraindications (not in US labeling): Complete biliary

obstruction of extrahepatic origin; widespread intrahepatic obstruction
Warnings/Precautions
Concerns related to adverse effects:
• Biliary obstruction: Maintain bile flow during therapy to prevent biliary

obstruction.
Disease-related concerns:
• Hepatic effects: Use with caution in patients with chronic liver disease. Monitor
LFTs; consider discontinuing therapy in patients with significant elevations in LFTs.
Other warnings/precautions:
• Appropriate use: Gallbladder stone dissolution may take several months of

therapy; complete dissolution may not occur and recurrence of stones within 5
years has been observed in up to 50% of patients. Patients should be cautiously
selected for therapy, consider alternative treatments. Specific treatments should
be initiated in patients with ascites, hepatic encephalopathy, variceal bleeding, or if
an urgent liver transplant is necessary.
• Nonvisualizing gallbladder: Use with caution in patients with a nonvisualizing

gallbladder; therapy should be discontinued if gallbladder nonvisualization occurs
during treatment.
Metabolism/Transport Effects
None known.
Drug Interactions
(For additional information: Launch drug interactions program)
Note: Interacting drugs may not be individually listed below if they are part of a group
interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a
complete list of drug interactions by individual drug name and detailed management
recommendations, use the Lexicomp drug interactions program by clicking on the “Launch
drug interactions program” link above.
Aluminum Hydroxide: May decrease the serum concentration of Ursodiol.

Management: Separate administration of ursodiol and aluminum-containing antacid
products to prevent adsorption in the gastrointestinal tract. Risk D: Consider therapy
modification
Bile Acid Sequestrants: May decrease the serum concentration of Ursodiol.

Management: Administer ursodiol 1 hour before or at least 4 to 5 hours after bile acid
sequestrants to minimize the potential for any significant interaction. Monitor for
decreased therapeutic effects of ursodiol in patients receiving bile acid sequestrants.
Risk D: Consider therapy modification
Estrogen Derivatives: May diminish the therapeutic effect of Ursodiol. Risk C: Monitor
therapy
Nitrendipine: Ursodiol may decrease the absorption of Nitrendipine. Risk C: Monitor

therapy
Sincalide: Drugs that Affect Gallbladder Function may diminish the therapeutic effect of
Sincalide. Management: Consider discontinuing drugs that may affect gallbladder
motility prior to the use of sincalide to stimulate gallbladder contraction. Risk D:
Consider therapy modification
Pregnancy Considerations
Ursodiol has been evaluated for treating intrahepatic cholestasis of pregnancy (ICP).
Maternal symptoms (eg, itching, increased bile acid concentrations) generally occur during
the second and third trimester. Fetal distress, preterm birth, and intrauterine death are also
associated with ICP. Although some studies have shown a decrease in maternal symptoms
(primarily itching) with ursodiol treatment, data is inconclusive regarding improvement of
fetal/neonatal outcomes (ACG [Tran 2016]; Chappell 2019; Kong 2016; Ovadia 2021; Parízek
2016; Sepúlveda Marín 2016; Shen 2019; SMFM [Lee 2021]; Walker 2020; Zhang 2016).
The American College of Gastroenterology guideline for liver disease in pregnancy and the
Society for Maternal-Fetal Medicine intrahepatic cholestasis of pregnancy consult series
consider ursodiol a first-line therapy for the treatment of ICP during the second and third
trimesters of pregnancy (ACG [Tran 2016]; SMFM [Lee 2021]).
Breastfeeding Considerations
Ursodiol may be present in breast milk (Brites 1998).
Total bile acid concentrations are increased in the colostrum of patients with
intrahepatic cholestasis of pregnancy (ICP). Ursodiol treatment for ICP until delivery
decreased the concentrations of total bile acid in the colostrum of 7 women compared
to nontreated patients. Ursodeoxycholic acid concentrations were insignificantly
elevated in the colostrum and were lower than the maternal serum (Brites 1998).
Based on limited case reports, adverse events have not been observed in breastfed
infants (Brites 1998; Erol-Coskun 2018; Vítek 2010).
According to the manufacturer, the decision to breastfeed during therapy should

consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the
benefits of treatment to the mother.
Dietary Considerations
Urso and Urso Forte should be taken with food.
Monitoring Parameters
Gallstone disease: ALT, AST, ultrasound every 6 months for the first year.
Intrahepatic cholestasis of pregnancy: Serum bile acid and liver transaminase prior to
therapy (SMFM [Lee 2021]).
Primary biliary cholangitis: Monitor LFTs (GGT, AST, ALT, bilirubin, and alkaline
phosphatase) monthly for the first 3 months and every 6 months thereafter or as
clinically necessary (90% of the improvement usually occurs within 6 to 9 months)
(AASLD [Lindor 2019]); baseline vitamin D level (Guo 2015).
Mechanism of Action
Ursodiol decreases the cholesterol content of bile and bile stones by reducing the secretion
of cholesterol from the liver and the fractional reabsorption of cholesterol by the intestines.
Mechanism of action in primary biliary cholangitis is not clearly defined. Ursodiol reduces
hydrophobic bile acids; hydrophobic bile acids may be toxic to hepatic parenchymal cells in
patients receiving hematopoietic stem cell transplantation (BCSH/BSBMT [Dignan 2013];
Ruutu 2002).
Pharmacokinetics
Absorption: 90%
Protein binding: ~70%
Metabolism: Undergoes extensive enterohepatic recycling; following hepatic

conjugation and biliary secretion, the drug is hydrolyzed to active ursodiol, where it is
recycled or transformed to lithocholic acid by colonic microbial flora; during chronic
administration, ursodiol becomes a major biliary and plasma bile acid constituting 30%
to 50% of biliary and plasma bile acids
Excretion: Feces; urine (<1%)
Pricing: US
Capsules (Reltone Oral)
200 mg (per each): $23.94
400 mg (per each): $35.28
Capsules (Ursodiol Oral)
200 mg (per each): $50.00
300 mg (per each): $1.50 - $13.94
400 mg (per each): $70.00
Tablets (Urso 250 Oral)
250 mg (per each): $6.61
Tablets (Urso Forte Oral)
500 mg (per each): $11.71
Tablets (Ursodiol Oral)
250 mg (per each): $2.68
500 mg (per each): $4.75
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is

provided as reference price only. A range is provided when more than one manufacturer's
AWP price is available and uses the low and high price reported by the manufacturers to
determine the range. The pricing data should be used for benchmarking purposes only,
and as such should not be used alone to set or adjudicate any prices for reimbursement or
purchasing functions or considered to be an exact price for a single product and/or
manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether
express or implied, and assumes no liability with respect to accuracy of price or price range
data published in its solutions. In no event shall Medi-Span be liable for special, indirect,
incidental, or consequential damages arising from use of price or price range data. Pricing
data is updated monthly.
Brand Names: International

Adursal (FI);
Axialith (PH);
Canlin (TW);
Cholemax (TH);
Destolit (MT);
Deursil (IT);
Dexo (PY);
Dozurso (BE);
Estazor (ID);
Galcholic (VN);
Homan (VN);
Lupible (PH);
Taurolite (CN);
Triptor
(LK);
Udihep (LK, TH);
Uldeso (HK);
Urdafalk (ID);
Urdek (ID);
Urosan (BE, JP);
Ursa (JO, PH);
Ursacol (BR, CO, IT);
Ursilon (VN);
Ursimex (VN);
Urso (IN, LK);
Ursobilane (ES);
Ursocel (EC);
Ursochol (BE, CH, EG, ES, ID, IS, LU, NL, NO, UA);
Ursodox (LK, PH);
Ursofalk (AE, AR, AT, AU,
BE, BG, CL, CN, CO, CR, CY, CZ, DE, EE, GR, GT, HK, HN, HR, HU, IE, IL, KR, KW, LB, LU, MT, MX,
MY, NI, NZ, PA, PE, PH, PK, PT, RO, SA, SE, SI, SK, SV, TH, TR, UA, UY);
Ursolic (TW);
Ursolin (TH);
Ursolit (IL);
Ursoliv (PH);
Ursolvan (FR);
Ursopol (PL);
Ursosan (JP, RU, UA)
For country abbreviations used in Lexicomp ( show table)
Use of UpToDate is subject to the Terms of Use.
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9/26/22, 8:17 PM Ursodeoxycholic acid (ursodiol): Drug information - UpToDate

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Ursodeoxycholic acid (ursodiol): Drug information

Copyright 1978-2022 Lexicomp, Inc. All rights reserved.

Brand Names: Canada

Gallstone dissolution (capsules): Oral: 8 to 10 mg/kg/day in 2 to 3 divided doses;

Gallstone prevention (capsules): Oral: 600 mg/day in 1 or 2 divided doses.

Gallstone prevention post–bariatric surgery 

Gallstone prevention post–bariatric surgery (off-label use): Oral: 500 to 600 mg

Hepatic sinusoidal obstruction syndrome associated with stem cell transplant, 

Hepatic sinusoidal obstruction syndrome associated with stem cell transplant,

Intrahepatic cholestasis of pregnancy 

Intrahepatic cholestasis of pregnancy (off-label use): Oral: 10 to 15 mg/kg/day in 2

Primary biliary cholangitis 

Primary biliary cholangitis (tablets): Oral: 13 to 15 mg/kg/day in 2 to 4 divided

Dosing: Kidney Impairment: Adult

Dosing: Hepatic Impairment: Adult

(For additional information see "Ursodeoxycholic acid (ursodiol): Pediatric drug

Parenteral nutrition-induced cholestasis, treatment: Limited data available (ASPEN

Pruritus secondary to cholestasis: Limited data available: Infants, Children, and

Dosing: Kidney Impairment: Pediatric

Dosing: Hepatic Impairment: Pediatric

Dosing: Older Adult

Actigall: 300 mg [DSC]

Actigall: 300 mg [DSC] [contains corn starch]

Reltone: 200 mg [contains corn starch]

Generic: 200 mg, 300 mg, 400 mg

Urso 250: 250 mg

Urso Forte: 500 mg [scored]

Generic: 250 mg, 500 mg

Generic Equivalent Available: US

Dosage Forms: Canada

Urso DS: 500 mg

Generic: 250 mg, 500 mg

Oral: Do not administer with aluminum-based antacids or bile acid sequestrants. If

Use: Labeled Indications

Gallstones (capsules only):

Treatment of patients with radiolucent, noncalcified gallbladder stones <20 mm in

Prevention of gallstone formation in obese patients experiencing rapid weight loss.

Use: Off-Label: Adult

Gallstone prevention post–bariatric surgery; Hepatic sinusoidal obstruction syndrome

Medication Safety Issues

Ursodiol may be confused with ulipristal

Central nervous system: Headache (≤25%), dizziness (17%)

Gastrointestinal: Diarrhea (≤27%), constipation (≤26%), dyspepsia (≤17%), nausea

Neuromuscular & skeletal: Back pain (≤12%)

Respiratory: Upper respiratory tract infection (≤16%)

Dermatologic: Alopecia (5%), skin rash (3%)

Endocrine & metabolic: Hyperglycemia (1%)

Gastrointestinal: Vomiting (≤10%), peptic ulcer (1%)

Genitourinary: Urinary tract infection (7%)

Hematologic & oncologic: Leukopenia (3%), thrombocytopenia (1%)

Hepatic: Cholecystitis (5%)

Hypersensitivity: Hypersensitivity reaction (5%)

Infection: Viral infection (9%)

Neuromuscular & skeletal: Arthritis (6%), musculoskeletal pain (6%)

Renal: Increased serum creatinine (1%)

<1%, postmarketing, and/or case reports: Abdominal distress, abdominal pain,