Ursodiol 300mg Capsules
It is used to treat or prevent gallstones.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Gallstone solubilizing agent; Bile acid
Pharmacologic Class
Bile acid derivative
Pregnancy Category
Category B
FDA Approved
Dec 1987
DEA Schedule
Not Controlled
Overview
What is this medicine?
Ursodiol is a medicine that helps dissolve certain types of gallstones and can also help treat a liver disease called primary biliary cholangitis (PBC). It works by changing the makeup of your bile, which is a digestive fluid made by your liver.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, it's essential to follow your doctor's instructions carefully. Read all the information provided with your medication 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're taking other medications like cholestyramine, colesevelam, colestipol, or antacids containing aluminum, you may need to take them at a different time than your prescribed medication. Be sure to discuss this with your doctor or pharmacist to determine the best schedule for your medications.
Storing and Disposing of Your Medication
To maintain the effectiveness and safety of your medication, store it at room temperature in a dry place, avoiding the bathroom. Keep all medications in a secure location, out of the reach of children and pets. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless instructed to do so by your pharmacist. Instead, check with your pharmacist for guidance on the proper disposal method or explore drug take-back programs in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Avoid taking two doses at the same time or taking extra doses, as this can increase the risk of side effects.
To get the most benefit from your medication, it's essential to follow your doctor's instructions carefully. Read all the information provided with your medication 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're taking other medications like cholestyramine, colesevelam, colestipol, or antacids containing aluminum, you may need to take them at a different time than your prescribed medication. Be sure to discuss this with your doctor or pharmacist to determine the best schedule for your medications.
Storing and Disposing of Your Medication
To maintain the effectiveness and safety of your medication, store it at room temperature in a dry place, avoiding the bathroom. Keep all medications in a secure location, out of the reach of children and pets. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless instructed to do so by your pharmacist. Instead, check with your pharmacist for guidance on the proper disposal method or explore drug take-back programs in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Avoid taking two doses at the same time or taking extra doses, as this can increase the risk of side effects.
Lifestyle & Tips
- Maintain a healthy diet and weight, as obesity can contribute to gallstone formation.
- Avoid rapid weight loss, which can also promote gallstone formation.
- For gallstone dissolution, treatment can take many months to years, and gallstones may recur after treatment stops.
- Take with food to improve absorption and reduce gastrointestinal upset.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
For gallstone dissolution: 8-10 mg/kg/day orally in 2-3 divided doses. For 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 (e.g., 300 mg BID or TID)
primaryBiliaryCholangitis:
13-15 mg/kg/day orally in 2-4 divided doses (e.g., 250 mg to 500 mg TID or QID)
Pediatric Dosing
Neonatal:
Not established for gallstones/PBC. Used off-label for cholestasis in neonates/infants (e.g., 10-30 mg/kg/day).
Infant:
Not established for gallstones/PBC. Used off-label for cholestasis in neonates/infants (e.g., 10-30 mg/kg/day).
Child:
Not established for gallstones/PBC. Used off-label for cystic fibrosis-associated liver disease (e.g., 15-30 mg/kg/day).
Adolescent:
Not established for gallstones/PBC. Used off-label for cystic fibrosis-associated liver disease (e.g., 15-30 mg/kg/day).
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment needed.
Moderate:
No specific adjustment needed.
Severe:
No specific adjustment needed.
Dialysis:
Not significantly dialyzable; no specific adjustment needed.
Hepatic Impairment:
Mild:
No specific adjustment needed, as it is a naturally occurring bile acid.
Moderate:
No specific adjustment needed, as it is a naturally occurring bile acid.
Severe:
No specific adjustment needed, as it is a naturally occurring bile acid. However, use with caution in patients with decompensated cirrhosis.
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 desaturation of bile, allowing for the dissolution of cholesterol gallstones. In primary biliary cholangitis (PBC), UDCA is thought to protect cholangiocytes from toxic bile acids, improve bile flow, and exert immunomodulatory effects.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 90%
Tmax:
1-3 hours
FoodEffect:
Food enhances absorption.
Distribution:
Vd:
Not readily available, but distributes into bile and liver.
ProteinBinding:
>90%
CnssPenetration:
Limited
Elimination:
HalfLife:
3-6 days (due to enterohepatic recirculation)
Clearance:
Not readily available, primarily eliminated via feces.
ExcretionRoute:
Fecal (primarily), small amounts in urine.
Unchanged:
<1%
Pharmacodynamics
OnsetOfAction:
Gallstone dissolution: Months to years. PBC: Clinical improvement may take weeks to months.
PeakEffect:
Gallstone dissolution: Not applicable (long-term effect). PBC: Not applicable (long-term effect).
DurationOfAction:
Effects persist as long as therapy is continued.
Safety & Warnings
Side Effects
Urgent 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 unusual symptoms, 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
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, consult 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 unusual symptoms, 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
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, consult 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 abdominal pain (especially in the upper right side)
- Yellowing of the skin or eyes (jaundice)
- Dark urine or pale stools
- Persistent nausea or vomiting
- Unusual tiredness or weakness
- Severe 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. Describe the allergic reaction you experienced, including the 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 your safety, provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter medications you are taking
Natural products and vitamins you are using
* Any health problems you have
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, given your specific health conditions and medications.
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. Describe the allergic reaction you experienced, including the 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 your safety, provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter medications you are taking
Natural products and vitamins you are using
* Any health problems you have
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, given your specific health conditions and medications.
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 (most common)
- Nausea
- Vomiting
What to Do:
In case of overdose, call your poison control center at 1-800-222-1222. Treatment is generally supportive and symptomatic. Severe diarrhea may require fluid and electrolyte replacement.
Drug Interactions
Moderate Interactions
- Bile acid sequestrants (e.g., cholestyramine, colestipol): May reduce ursodiol absorption. Administer ursodiol at least 2 hours before or 4-6 hours after these agents.
- Aluminum-based antacids: May reduce ursodiol absorption. Administer ursodiol at least 2 hours before or 4-6 hours after these agents.
- Estrogens, oral contraceptives, clofibrate: May increase hepatic cholesterol secretion, counteracting ursodiol's effect on gallstone dissolution.
Monitoring
Baseline Monitoring
Liver function tests (ALT, AST, ALP, total bilirubin)
Rationale: To assess baseline liver function and monitor for potential drug-induced liver injury or disease progression (especially in PBC).
Timing: Prior to initiation of therapy.
Serum cholesterol
Rationale: To monitor cholesterol levels, especially in patients with gallstones.
Timing: Prior to initiation of therapy.
Routine Monitoring
Liver function tests (ALT, AST, ALP, total bilirubin)
Frequency: Every 3-6 months for the first year, then annually, or as clinically indicated.
Target: Within normal limits or stable for patient's condition.
Action Threshold: Significant elevation (e.g., >3x ULN) may warrant dose reduction or discontinuation.
Abdominal ultrasound (for gallstones)
Frequency: Every 6-12 months for the first year, then annually, until gallstone dissolution is confirmed.
Target: Not applicable (visual assessment)
Action Threshold: Lack of gallstone dissolution after 12-18 months may indicate treatment failure.
Symptom Monitoring
- Abdominal pain
- Nausea
- Diarrhea
- Pruritus (itching)
- Jaundice (yellowing of skin/eyes)
- Dark urine
- Light-colored stools
- Fatigue
Special Patient Groups
Pregnancy
Pregnancy Category B. Animal studies have shown no evidence of impaired fertility or harm to the fetus. There are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if clearly needed and the potential benefits outweigh the potential risks.
Trimester-Specific Risks:
First Trimester:
No specific increased risk identified.
Second Trimester:
No specific increased risk identified.
Third Trimester:
No specific increased risk identified.
Lactation
Ursodiol is excreted in breast milk in very small amounts. The amount is considered clinically insignificant and unlikely to cause adverse effects in a breastfed infant. Generally considered compatible with breastfeeding (L3).
Infant Risk:
Low risk of adverse effects to the infant.
Pediatric Use
Safety and efficacy for gallstone dissolution or PBC in pediatric patients have not been established. However, it is used off-label for various cholestatic liver diseases in children, including cystic fibrosis-associated liver disease, often at doses of 15-30 mg/kg/day.
Geriatric Use
No specific dose adjustment is required based on age. However, elderly patients may have age-related decreases in renal or hepatic function, and comorbidities should be considered. Monitor for adverse effects as with younger adults.
Clinical Information
Clinical Pearls
- Ursodiol is the only FDA-approved medication for the dissolution of cholesterol gallstones and for the treatment of primary biliary cholangitis (PBC).
- Gallstone dissolution can take 6 months to 2 years, and only small, non-calcified, radiolucent gallstones are candidates for dissolution.
- Gallstones may recur in up to 50% of patients within 5 years after successful dissolution if predisposing factors persist.
- In PBC, ursodiol significantly improves liver biochemistry, delays disease progression, and improves transplant-free survival.
- Patients with PBC should be monitored for bone density due to increased risk of osteoporosis.
Alternative Therapies
- Cholecystectomy (surgical removal of gallbladder) for gallstones.
- Obeticholic acid (for PBC, often in combination with or as an alternative to ursodiol in non-responders).
- Liver transplantation (for advanced PBC).
Cost & Coverage
Average Cost:
$50 - $300+ per 30 capsules (300mg)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (generic)
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 details. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider for clarification. 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 information about the medication taken, the amount, and the time it occurred, as this will help healthcare professionals provide the best possible care.