Ursodiol 500mg Tablets
It is used to treat a type of liver disease caused by bile duct problems in the liver (biliary cirrhosis).It may be given to you for other reasons. Talk with the doctor.
Drug Class
Gallstone solubilizing agent; Cholagogue and Choleretic
Pharmacologic Class
Bile acid
Pregnancy Category
Category B
FDA Approved
Mar 1997
DEA Schedule
Not Controlled
Overview
What is this medicine?
Ursodiol is a medication that helps dissolve certain types of gallstones and can improve liver function in people with specific liver diseases like Primary Biliary Cholangitis (PBC). It works by changing the composition of bile in your body.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel better.
If you are taking cholestyramine, colesevelam, colestipol, or an antacid that contains aluminum, you may need to take these medications at a different time than your prescribed medication. Consult with your doctor or pharmacist to determine the best schedule.
Take your medication with food to help your body absorb it properly. Some products may be broken in half, but check with your doctor first to confirm. If you do break a tablet in half, do not chew the half-tablet. Instead, swallow it whole with a glass of water to avoid a bitter taste. If you break a tablet in half, use the other half for your next dose as directed by your doctor. Discard any unused half-tablets after 28 days.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from the bathroom. If you break tablets in half, store the half-tablets separately from the whole tablets. Keep all medications in a safe place, out of the reach of children and pets.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it is close to the time for your next dose, skip the missed dose and resume your regular schedule. Do not take two doses at the same time or take extra doses to make up for a missed dose.
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel better.
If you are taking cholestyramine, colesevelam, colestipol, or an antacid that contains aluminum, you may need to take these medications at a different time than your prescribed medication. Consult with your doctor or pharmacist to determine the best schedule.
Take your medication with food to help your body absorb it properly. Some products may be broken in half, but check with your doctor first to confirm. If you do break a tablet in half, do not chew the half-tablet. Instead, swallow it whole with a glass of water to avoid a bitter taste. If you break a tablet in half, use the other half for your next dose as directed by your doctor. Discard any unused half-tablets after 28 days.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from the bathroom. If you break tablets in half, store the half-tablets separately from the whole tablets. Keep all medications in a safe place, out of the reach of children and pets.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it is close to the time for your next dose, skip the missed dose and resume your regular schedule. Do not take two doses at the same time or take extra doses to make up for a missed dose.
Lifestyle & Tips
- Maintain a healthy weight and avoid rapid weight loss, as this can promote gallstone formation.
- Follow a balanced diet as recommended by your healthcare provider.
- For gallstone dissolution, treatment can take many months (6-24 months) and gallstones may recur after stopping the medication.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
For gallstone dissolution: 8-10 mg/kg/day in 2-3 divided doses. For Primary Biliary Cholangitis (PBC): 13-15 mg/kg/day in 2-4 divided doses.
Dose Range:
8 - 15 mg
Condition-Specific Dosing:
gallstoneDissolution:
8-10 mg/kg/day in 2-3 divided doses
primaryBiliaryCholangitis:
13-15 mg/kg/day in 2-4 divided doses
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established for FDA-approved indications; off-label for cholestatic liver diseases: 10-15 mg/kg/day
Child:
Not established for FDA-approved indications; off-label for cholestatic liver diseases: 10-15 mg/kg/day (up to 30 mg/kg/day in some cases)
Adolescent:
Not established for FDA-approved indications; off-label for cholestatic liver diseases: 10-15 mg/kg/day (up to 30 mg/kg/day in some cases)
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment needed
Moderate:
No specific adjustment needed
Severe:
No specific adjustment needed
Dialysis:
No specific adjustment needed; not significantly dialyzable
Hepatic Impairment:
Mild:
No specific adjustment needed (used to treat hepatic impairment)
Moderate:
No specific adjustment needed (used to treat hepatic impairment)
Severe:
No specific adjustment needed (used to treat hepatic impairment)
Pharmacology
Mechanism of Action
Ursodiol (ursodeoxycholic acid, UDCA) is a naturally occurring bile acid. It suppresses hepatic synthesis and secretion of cholesterol, and inhibits intestinal absorption of cholesterol. This leads to a decrease in the cholesterol saturation of bile, promoting the dissolution of cholesterol gallstones. In cholestatic liver diseases, it replaces more toxic endogenous bile acids, protects hepatocytes from damage, and improves bile flow.
Pharmacokinetics
Absorption:
Bioavailability:
Variable (approx. 90% absorbed, but significant first-pass effect)
Tmax:
1-3 hours
FoodEffect:
Food increases absorption
Distribution:
Vd:
Not widely reported; distributes into bile
ProteinBinding:
>90%
CnssPenetration:
Limited
Elimination:
HalfLife:
3-6 days (due to enterohepatic recirculation)
Clearance:
Not readily quantifiable due to enterohepatic recirculation
ExcretionRoute:
Primarily fecal (as conjugated bile acids and metabolites)
Unchanged:
<1%
Pharmacodynamics
OnsetOfAction:
Gallstone dissolution: Months; Biochemical improvement in PBC: Weeks to months
PeakEffect:
Gallstone dissolution: 6-24 months; PBC: Varies, sustained with chronic use
DurationOfAction:
Sustained with chronic administration due to enterohepatic recirculation
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Attention Immediately
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of a urinary tract infection (UTI), including:
+ Blood in the urine
+ Burning or pain when passing urine
+ Frequent or urgent need to urinate
+ Fever
+ Lower stomach pain
+ Pelvic pain
Abdominal swelling
Stomach cramps
Loss of appetite
Rarely, stomach or bowel stones may occur, which may require surgery. If you have a history of Crohn's disease or bowel surgery, you may be at higher risk. Seek medical attention immediately if you experience:
+ Severe constipation
+ Abdominal pain
+ Bloating
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or if they persist or bother you, contact your doctor:
Dizziness or headache
Back pain
Constipation
Diarrhea
Stomach pain
Upset stomach
Nausea or vomiting
Heartburn
Gas
Muscle or joint pain
Signs of a common cold
Hair loss
This is not an exhaustive list of possible side effects. If you have questions or concerns, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of a urinary tract infection (UTI), including:
+ Blood in the urine
+ Burning or pain when passing urine
+ Frequent or urgent need to urinate
+ Fever
+ Lower stomach pain
+ Pelvic pain
Abdominal swelling
Stomach cramps
Loss of appetite
Rarely, stomach or bowel stones may occur, which may require surgery. If you have a history of Crohn's disease or bowel surgery, you may be at higher risk. Seek medical attention immediately if you experience:
+ Severe constipation
+ Abdominal pain
+ Bloating
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or if they persist or bother you, contact your doctor:
Dizziness or headache
Back pain
Constipation
Diarrhea
Stomach pain
Upset stomach
Nausea or vomiting
Heartburn
Gas
Muscle or joint pain
Signs of a common cold
Hair loss
This is not an exhaustive list of possible side effects. If you have questions or concerns, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Worsening jaundice (yellowing of skin or eyes)
- Severe or persistent abdominal pain
- Persistent nausea or vomiting
- Unusual fatigue or weakness
- Dark urine
- Pale or clay-colored stools
- New or worsening itching
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you have a blockage in your biliary tract or a specific bile duct condition known as cholangitis.
If you have any of the following health conditions:
+ An abnormal connection between the biliary and gastrointestinal tracts
+ Pancreatitis (inflammation of the pancreas)
+ Cholecystitis (swelling of the gallbladder)
This list is not exhaustive, and it is crucial to discuss all your health problems and medications with your doctor.
To ensure safe treatment, inform your doctor and pharmacist about:
All prescription and over-the-counter medications you are taking
Any natural products or vitamins you are using
* All your health problems
Before starting, stopping, or changing the dose of any medication, including this one, consult with your doctor to confirm it is safe for you to do so.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you have a blockage in your biliary tract or a specific bile duct condition known as cholangitis.
If you have any of the following health conditions:
+ An abnormal connection between the biliary and gastrointestinal tracts
+ Pancreatitis (inflammation of the pancreas)
+ Cholecystitis (swelling of the gallbladder)
This list is not exhaustive, and it is crucial to discuss all your health problems and medications with your doctor.
To ensure safe treatment, inform your doctor and pharmacist about:
All prescription and over-the-counter medications you are taking
Any natural products or vitamins you are using
* All your health problems
Before starting, stopping, or changing the dose of any medication, including this one, consult with your doctor to confirm it is safe for you to do so.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Regular blood work and laboratory tests should be conducted as directed by your doctor to monitor your condition. Please note that this medication may take several months to dissolve gallstones, and its effectiveness can vary from patient to patient. In some cases, gallstones may recur after treatment. If you have any questions or concerns about this information, be sure to discuss them with your doctor. Additionally, if you are pregnant, planning to become pregnant, or are breastfeeding, you should consult with your doctor to carefully weigh the benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- Diarrhea
What to Do:
In case of overdose, symptomatic and supportive treatment should be provided. Contact a poison control center (e.g., 1-800-222-1222) or seek emergency medical attention.
Drug Interactions
Major Interactions
- Cholestyramine
- Colestipol
- Aluminum-containing antacids
- Estrogens
- Oral contraceptives
- Clofibrate
Monitoring
Baseline Monitoring
Liver Function Tests (ALT, AST, ALP, GGT, Bilirubin)
Rationale: To assess baseline liver health and monitor for potential drug-induced liver injury or disease progression.
Timing: Prior to initiation of therapy
Abdominal Ultrasound
Rationale: To confirm presence and type of gallstones (for dissolution indication) or assess liver morphology (for PBC).
Timing: Prior to initiation of therapy
Routine Monitoring
Liver Function Tests (ALT, AST, ALP, GGT, Bilirubin)
Frequency: Every 1-3 months for the first 6 months, then every 6 months
Target: Within normal limits or stable for underlying condition
Action Threshold: Significant elevation (e.g., >3x ULN) or worsening of liver function tests may require dose adjustment or discontinuation.
Abdominal Ultrasound
Frequency: Every 6-12 months (for gallstone dissolution)
Target: Reduction in gallstone size or complete dissolution
Action Threshold: No change or increase in gallstone size after 12-18 months may indicate treatment failure.
Symptom Monitoring
- Pruritus (itching)
- Jaundice (yellowing of skin or eyes)
- Fatigue
- Abdominal pain (especially right upper quadrant)
- Dark urine
- Pale stools
- Nausea
- Vomiting
Special Patient Groups
Pregnancy
Category B. Studies in animals have shown no evidence of impaired fertility or harm to the fetus. Limited human data suggest no increased risk. Use only if clearly needed and the potential benefits outweigh the potential risks.
Trimester-Specific Risks:
First Trimester:
No increased risk observed in limited human data.
Second Trimester:
No increased risk observed in limited human data.
Third Trimester:
No increased risk observed in limited human data.
Lactation
L2 (Likely Compatible). Ursodiol is excreted in breast milk in very small amounts. No adverse effects have been reported in breastfed infants. Considered safe for use during breastfeeding.
Infant Risk:
Low risk
Pediatric Use
Not FDA-approved for pediatric use for gallstone dissolution or PBC. However, it is used off-label for various cholestatic liver diseases in children, with weight-based dosing. Efficacy and safety in pediatric populations for these off-label uses are supported by clinical experience.
Geriatric Use
No specific dose adjustments are typically needed for geriatric patients. However, use with caution in elderly patients with multiple comorbidities or impaired organ function, as they may be more susceptible to adverse effects.
Clinical Information
Clinical Pearls
- Ursodiol is effective only for cholesterol gallstones that are radiolucent (not visible on X-ray) and less than 20 mm in diameter. It is not effective for calcified gallstones or pigment stones.
- Gallstone dissolution can be a lengthy process, often requiring 6 to 24 months of continuous therapy. Gallstones may recur after discontinuation of treatment.
- For Primary Biliary Cholangitis (PBC), ursodiol is the first-line therapy and should be continued long-term as it slows disease progression and improves transplant-free survival.
- Patients should be advised to take ursodiol with food to enhance absorption and reduce gastrointestinal upset.
- Concurrent administration with bile acid sequestrants (e.g., cholestyramine) or aluminum-containing antacids should be avoided or separated by several hours to prevent reduced ursodiol absorption.
Alternative Therapies
- For gallstones: Cholecystectomy (surgical removal of gallbladder), Chenodiol (less commonly used due to higher incidence of side effects).
- For Primary Biliary Cholangitis (PBC): Obeticholic acid (for patients with inadequate response to ursodiol or who are intolerant), Fibrates (off-label for pruritus and cholestasis in some PBC patients), Liver transplantation (for end-stage liver disease).
Cost & Coverage
Average Cost:
Varies widely, typically $50-$200 per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (for generic formulations)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.