Ursodiol 250mg 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 dissolution agent; Bile acid
Pharmacologic Class
Bile acid
Pregnancy Category
Category B
FDA Approved
Dec 1988
DEA Schedule
Not Controlled
Overview
What is this medicine?
Ursodiol is a medicine that helps dissolve certain types of gallstones and can improve liver function in people with certain liver diseases like primary biliary cholangitis (PBC). It works by changing the makeup 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 to you and follow the instructions closely. Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel well.
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 can 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 to you and follow the instructions closely. Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel well.
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 can 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
- For gallstone dissolution, maintaining a healthy weight and avoiding rapid weight loss may help prevent new stone formation.
- Follow a balanced diet as recommended by your doctor.
- Take medication with food to improve absorption and reduce stomach upset.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
Gallstone dissolution: 8-10 mg/kg/day orally in 2-3 divided doses. Primary Biliary Cholangitis (PBC): 13-15 mg/kg/day orally in 2-4 divided doses.
Dose Range:
8 - 15 mg
Condition-Specific Dosing:
gallstoneDissolution:
8-10 mg/kg/day orally in 2-3 divided doses
primaryBiliaryCholangitis:
13-15 mg/kg/day orally in 2-4 divided doses
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Cystic Fibrosis-associated Liver Disease: 10-15 mg/kg/day orally in 2-3 divided doses (some sources suggest up to 20-30 mg/kg/day).
Adolescent:
Cystic Fibrosis-associated Liver Disease: 10-15 mg/kg/day orally in 2-3 divided doses (some sources suggest up to 20-30 mg/kg/day). Primary Biliary Cholangitis: 13-15 mg/kg/day orally in 2-4 divided doses.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment recommended.
Moderate:
No specific adjustment recommended.
Severe:
No specific adjustment recommended.
Dialysis:
Not significantly dialyzable; no specific supplemental dose needed.
Hepatic Impairment:
Mild:
No specific adjustment recommended; used to treat hepatic conditions.
Moderate:
No specific adjustment recommended; used to treat hepatic conditions.
Severe:
No specific adjustment recommended; used to treat hepatic conditions. Monitor liver function closely.
Pharmacology
Mechanism of Action
Ursodiol (ursodeoxycholic acid) is a naturally occurring bile acid. It suppresses hepatic synthesis and secretion of cholesterol and inhibits intestinal absorption of cholesterol. It also alters the composition of bile, making it less saturated with cholesterol, thereby promoting the dissolution of cholesterol gallstones. In chronic cholestatic liver diseases like PBC, ursodiol is thought to protect cholangiocytes from toxic bile acids, improve bile flow, and exert immunomodulatory effects.
Pharmacokinetics
Absorption:
Bioavailability:
Variable, approximately 90% (after deconjugation and reabsorption)
Tmax:
1-3 hours
FoodEffect:
Food increases absorption.
Distribution:
Vd:
Not available
ProteinBinding:
>90%
CnssPenetration:
Limited
Elimination:
HalfLife:
3.5-5.8 hours (terminal half-life of unconjugated ursodiol)
Clearance:
Not available
ExcretionRoute:
Primarily fecal (as unconjugated ursodiol and its metabolites), small amounts in urine.
Unchanged:
<1% in urine
Pharmacodynamics
OnsetOfAction:
Gallstone dissolution: Months (typically 6-24 months). PBC: Clinical improvement may take weeks to months.
PeakEffect:
Gallstone dissolution: Varies, depends on stone size and composition. PBC: Improvement in LFTs typically seen within 3-6 months.
DurationOfAction:
Effect on bile composition persists as long as therapy continues.
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Attention Immediately
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice 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 any other symptoms that bother you or do not go away, contact your doctor or seek medical help:
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
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, 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, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice 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 any other symptoms that bother you or do not go away, contact your doctor or seek medical help:
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
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, 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:
- Severe or persistent diarrhea
- New or worsening abdominal pain
- Yellowing of your skin or eyes (jaundice)
- Dark urine or pale stools
- Unusual tiredness or weakness
- Signs of an allergic reaction (rash, itching, swelling, severe dizziness, trouble breathing)
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 conditions to ensure safe treatment:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Describe the allergic reaction you experienced, including the symptoms that occurred.
If you have a blockage in the biliary tract.
If you have cholangitis, a specific type of bile duct problem.
If you have any of the following health conditions:
+ An abnormal opening 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 medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other treatments. Never start, stop, or change the dose of any medication without consulting your doctor first.
It is essential to inform your doctor about the following conditions to ensure safe treatment:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Describe the allergic reaction you experienced, including the symptoms that occurred.
If you have a blockage in the biliary tract.
If you have cholangitis, a specific type of bile duct problem.
If you have any of the following health conditions:
+ An abnormal opening 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 medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other treatments. Never start, stop, or change the dose of any medication without consulting your doctor first.
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 may not be effective for all patients. Additionally, some patients may experience the return of gallstones after treatment. If you have any questions or concerns regarding this information, be sure to discuss them with your doctor. If you are pregnant, planning to become pregnant, or are breastfeeding, you must consult with your doctor to weigh the benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- Diarrhea (most common symptom of overdose)
- Nausea
- Vomiting
- Abdominal pain
What to Do:
Treatment is symptomatic and supportive. In case of suspected overdose, contact a poison control center (e.g., 1-800-222-1222) or seek emergency medical attention immediately.
Drug Interactions
Moderate Interactions
- Bile acid sequestrants (e.g., cholestyramine, colestipol): May reduce ursodiol absorption. Administer ursodiol at least 1 hour before or 4-6 hours after sequestrants.
- Aluminum-containing antacids: May reduce ursodiol absorption. Administer ursodiol at least 1 hour before or 4-6 hours after antacids.
- Estrogens, oral contraceptives, clofibrate (and other lipid-lowering agents): May increase hepatic cholesterol secretion, counteracting ursodiol's effect on gallstone dissolution.
Monitoring
Baseline Monitoring
Liver Function Tests (LFTs): AST, ALT, ALP, GGT, total bilirubin
Rationale: To assess baseline liver function and monitor for potential drug-induced liver injury or disease progression.
Timing: Prior to initiation of therapy.
Abdominal Ultrasound (for gallstone dissolution)
Rationale: To confirm presence of cholesterol gallstones and assess their size and number.
Timing: Prior to initiation of therapy.
Routine Monitoring
Liver Function Tests (LFTs): AST, ALT, ALP, GGT, total bilirubin
Frequency: Every 1-3 months for the first 6 months, then every 6-12 months, or as clinically indicated.
Target: Within normal limits or stable, improved values for PBC.
Action Threshold: Significant elevation (e.g., >3x ULN) or worsening of LFTs may require dose adjustment or discontinuation.
Abdominal Ultrasound (for gallstone dissolution)
Frequency: Every 6-12 months.
Target: Reduction in gallstone size or complete dissolution.
Action Threshold: No change or increase in stone size after 12-18 months may indicate treatment failure.
Symptom Monitoring
- Persistent diarrhea (common side effect)
- Abdominal pain
- Nausea/vomiting
- Pruritus (itching)
- Jaundice (yellowing of skin/eyes)
- Dark urine
- Light-colored stools
Special Patient Groups
Pregnancy
Category B. Animal studies have shown no evidence of impaired fertility or harm to the fetus. Limited human data suggest no increased risk of major birth defects or miscarriage. Use only if clearly needed.
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 naturally present in breast milk. Levels in breast milk are generally low and unlikely to cause adverse effects in a breastfed infant. Monitor infant for diarrhea.
Infant Risk:
Low risk of adverse effects.
Pediatric Use
Approved for use in children for specific indications like cystic fibrosis-associated liver disease. Dosing is weight-based. Safety and efficacy for gallstone dissolution in children are not well-established.
Geriatric Use
No specific dose adjustment is generally required. However, elderly patients may have age-related decreases in renal or hepatic function, which should be considered. Monitor for adverse effects and liver function.
Clinical Information
Clinical Pearls
- Ursodiol is most effective for small, non-calcified, cholesterol gallstones in patients who are not candidates for surgery or prefer non-surgical options. It is not effective for calcified or pigment gallstones.
- Gallstone dissolution can take 6-24 months, and recurrence is common after discontinuation of therapy.
- For PBC, ursodiol is the first-line treatment and significantly improves liver biochemistry, delays disease progression, and improves transplant-free survival.
- Diarrhea is a common side effect, especially at higher doses. It can often be managed by reducing the dose temporarily or taking the medication with food.
- Patients should be advised to continue therapy even if they feel well, especially for chronic conditions like PBC.
Alternative Therapies
- Cholecystectomy (surgical removal of the gallbladder) for gallstones.
- Chenodiol (chenodeoxycholic acid) - another bile acid, less commonly used due to higher incidence of side effects.
- For PBC, liver transplantation is an option for advanced disease.
Cost & Coverage
Average Cost:
$50 - $200 per 30 tablets (250mg)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (preferred generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea 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.