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 |
|---|---|---|---|
| Reltone oral - | 400 mg capsule |  | |
| Reltone oral - | 200 mg capsule |  | |
| URSO 250 oral - | 250 mg tablet |  | |
| URSO Forte oral - | 500 mg tablet |  | |
| ursodiol oral - | 300 mg capsule |  | |
| ursodiol oral - | 500 mg tablet |  | |
| ursodiol oral - | 250 mg tablet |  | |
| ursodiol oral - | 500 mg tablet |  | |
| ursodiol oral - | 250 mg tablet |  | |
| ursodiol oral - | 300 mg capsule |  | |
| 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 - | 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 |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
ursodiol oral
URSODIOL - ORAL
(UR-soe-DYE-ol)
COMMON BRAND NAME(S): Actigall, Urso
USES: Ursodiol is used to dissolve certain types of gallstones, to prevent gallstones from forming in obese patients who are losing weight rapidly, and to treat a certain type of liver disease (primary biliary cholangitis). Ursodiol is a bile acid.
HOW TO USE: Take this medication exactly as directed by your doctor.Dosage is based on your medical condition and response to therapy.Do not increase your dose or take this medication more often without your doctor's approval. Your condition will not improve any faster, and the risk of serious side effects may be increased.Use this medication regularly to get the most benefit from it. To help you remember, take it at the same times each day.
SIDE EFFECTS: Stomach upset, nausea, diarrhea, dizziness, back pain, hair loss, or cough may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: weakness, swelling of the ankles/feet, increased thirst/urination, signs of infection (such as sore throat that doesn't go away, fever), easy bleeding/bruising, symptoms of stomach/intestinal blockage (such as abdominal pain, loss of appetite, cramping, vomiting).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before taking ursodiol, tell your doctor or pharmacist if you are allergic to it; or to other bile acids; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: certain gallbladder/bile duct problems (such as acute cholecystitis, cholangitis, biliary obstruction, gallstone pancreatitis, biliary-gastrointestinal fistula), liver disease (such as ascites, variceal bleeding, hepatic encephalopathy).This drug may make you dizzy. Alcohol or marijuana (cannabis) can make you more dizzy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.This medication passes into breast milk. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: severe diarrhea.
NOTES: Do not share this medication with others.Lab and/or medical tests (such as liver function, bilirubin level) should be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.
MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.
STORAGE: Store at room temperature away from light and moisture. Different brands/strengths of this medication may have different storage requirements. Read the package labeling or ask your pharmacist for the storage requirements for the product you are using. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
Information last revised February 2023. Copyright(c) 2023 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
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