In patients with primary biliary cirrhosis
Primary biliary cholangitis
An auto-immune disease that causes progressive destruction of the bile ducts.
How is Ursodiol used to treat primary biliary cirrhosis (PBC)?
Ursodiol Tablets, USP are indicated for the treatment of patients with primary biliary cirrhosis (PBC). The recommended adult dosage for Ursodiol in the treatment of PBC is 13 to 15 mg/kg/day administered in two to four divided doses with food. Dosing regimen should be adjusted according to each patient’s need at the discretion of the physician.
What is Ursodiol used to treat?
It is also used to prevent gallstones from forming in overweight patients. Later, it was learned ursodiol could help slow the progression of primary biliary cholangitis (PBC) patients. Ursodiol and new medication Ocaliva are the only treatments to help slow the progression of PBC.
Can Ursodiol improve liver function tests?
In a pilot study, ursodiol produced sustained improvement in liver-function tests22. We then conducted a two-year multicenter, double-blind, controlled trial in which patients with primary biliary cirrhosis were randomly assigned to receive either ursodiol or placebo23.
How much Ursodiol should I take for PBC?
The recommended adult dosage for Ursodiol tablets USP, 250 mg and 500 mg in the treatment of PBC is 13-15 mg/kg/day administered in two to four divided doses with food. Dosing regimen should be adjusted according to each patient’s need at the discretion of the physician.
How does ursodiol work in PBC?
Ursodeoxycholic acid (UDCA). This medication, also known as ursodiol (Actigall, Urso), is commonly used first. It helps move bile through your liver. UDCA doesn't cure primary biliary cholangitis, but it seems to improve liver function and reduce liver scarring. It's less likely to help with itching and fatigue.
What does ursodiol do for the liver?
Ursodiol is in a class of medications called gallstone dissolution agentss. It works by decreasing the production of cholesterol and by dissolving the cholesterol in bile to prevent stone formation and by decreasing toxic levels of bile acids that accumulate in primary biliary cirrhosis.
Does ursodiol help liver enzymes?
Ursodeoxycholic acid (UDCA or ursodiol) administration has been associated with a reduction of serum liver enzymes in patients with chronic liver disease and with improvement of liver histology in patients with primary biliary cirrhosis.
Does ursodiol reduce bile acids?
Ursodeoxycholic acid (ursodiol) is a naturally occurring hydrophilic bile acid which has been demonstrated to decrease cholestasis. Ursodiol has been postulated to reduce the hydrophobic bile acids in the hepatobiliary system to lessen the potential for hepatotoxicity.
Is ursodiol effective for PBC?
We found that ursodiol slows the progression of primary biliary cirrhosis and reduces the need for liver transplantation. After two years, the risk of hyperbilirubinemia or clinical complications was approximately three times higher in the placebo group than in the ursodiol group.
How long can you take ursodiol for?
You may need to take ursodiol for up to two years for the treatment of gallstones. Once the gallstones have dissolved, your physician may continue your treatment for three to four months to ensure that they have completely cleared up.
How do I know if ursodiol is working?
It is important that your doctor check your progress at regular visits. Blood tests will have to be done every few months while you are taking this medicine to make sure that the gallstones are dissolving and your liver is working properly.
How long does it take for ursodiol to lower liver enzymes?
UDCA significantly improved the liver function scores after 4 weeks of treatment and effectively reduced hepatic deoxycholic acid and serum microRNA-122 levels.
How long does it take for ursodiol to work?
This medication should take effect within 1 to 2 days; however, effects may not be visibly obvious and therefore laboratory tests may need to be done to evaluate this medication's effectiveness.
Does ursodiol make you tired?
Ursodiol may cause serious side effects. Call your doctor at once if you have: pain or burning when you urinate; liver problems--nausea, upper stomach pain, itching, tired feeling, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes); or.
Does ursodiol cause weight gain?
Ursodiol is generally well-received by patients. Uncommon side effects do, however, include nausea, fatigue, depression, even weight gain.
What can you not take with ursodiol?
Some products that may interact with this drug are: aluminum-containing antacids, birth control pills, cholesterol medications (such as cholestyramine, clofibrate, colestipol), estrogen.
Before Taking This Medicine
You should not use ursodiol if you are allergic to it, or if you have an obstruction in your liver or gallbladder.To make sure ursodiol is safe for...
How Should I Take Ursodiol?
Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended.Take the ur...
What Happens If I Miss A Dose?
Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to...
What Should I Avoid While Taking Ursodiol?
Ask your doctor before using an antacid, and use only the type your doctor recommends. Some antacids can make it harder for your body to absorb urs...
What Other Drugs Will Affect Ursodiol?
Other drugs may interact with ursodiol, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your hea...
How to take ursodiol?
Take the ursodiol tablet with food. You may need to break a tablet in half to get your correct dose. Each tablet is scored in the middle and should break apart easily. Swallow the tablet piece whole with a glass of water. A broken tablet can have a bitter taste. Use ursodiol regularly to get the most benefit.
What is ursodiol in the liver?
What is ursodiol? Ursodiol is a bile acid that decreases the amount of cholesterol produced by the liver and absorbed by the intestines. Ursodiol helps break down cholesterol that has formed into stones in the gallbladder. Ursodiol also increases bile flow in patients with primary biliary cirrhosis.
How long can you keep Ursodiol tablets at room temperature?
Store at room temperature away from moisture and heat. Tablets that are broken in half can be kept at room temperature for up to 28 days. If you split your tablets, keep them separate from any whole tablets.
Can ursodiol harm a baby?
FDA pregnancy category B. Ursodiol is not expected to harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment. It is not known whether ursodiol passes into breast milk or if it could harm a nursing baby. Tell your doctor if you are breast-feeding a baby.
Can you take Ursodiol if you are allergic to it?
You should not use ursodiol if you are allergic to it, or if you have an obstruction in your liver or gallbladder. To make sure ursodiol is safe for you, tell your doctor if: you have been coughing up blood; or. you have gained weight rapidly, especially in your face and midsection.
Does ursodiol increase bile flow?
Ursodiol also increases bile flow in patients with primary biliary cirrhosis. Ursodiol is used to treat primary biliary cirrhosis. Ursodiol capsules are used to treat small gallstones in people who cannot have gallbladder surgery, and to prevent gallstones in overweight patients undergoing rapid weight loss.
How long did it take for Ursodiol to stop?
Two of the four patients assigned to ursodiol who underwent liver transplantation stopped taking the drug at least six months before the decision was made to perform transplantation. The indication for liver transplantation in the third patient (histologic evidence of cirrhosis) was unconventional.
What are the criteria for entry into the biliary cirrhosis trial?
The criteria for entry were biopsy-proved primary biliary cirrhosis, serum alkaline phosphatase activity more than twice the upper limit of normal , and a positive test for antimitochondrial antibodies. Patients were admitted to the trial regardless of the duration of the disease or the histologic stage.
What is the treatment for cirrhosis of the liver?
Orthotopic liver transplantation is now considered the treatment of choice. Medications to treat primary biliary cirrhosis that have been assessed in controlled trials include immunosuppressive agents, penicillamine, and colchicine2-21. None of these medications, however, have proved totally effective or safe.
What is primary biliary cirrhosis?
Primary biliary cirrhosis is a chronic cholestatic liver disease that progresses slowly toward a terminal phase characterized by hyperbilirubinemia, signs of decompensated cirrhosis, ascites, and variceal bleeding. The survival of patients with end-stage primary biliary cirrhosis is usually very short1.
Does Ursodiol cause hepatotoxicity?
Given that ursodiol (ursodeoxycholic acid) has no apparent hepatotoxicity in humans, we postulated that long-term treatment with this drug might displace endogenous bile acids and thus reverse their suspected cytotoxicity in primary biliary cirrhosis.
How is ursodiol absorbed?
Following oral administration, the majority of Ursodiol is absorbed by passive diffusion and its absorption is incomplete. Once absorbed, Ursodiol undergoes hepatic extraction to the extent of about 50% in the absence of liver disease. As the severity of liver disease increases, the extent of extraction decreases. In the liver, Ursodiol is conjugated with glycine or taurine, then secreted into bile. These conjugates of Ursodiol are absorbed in the small intestine by passive and active mechanisms. The conjugates can also be deconjugated in the ileum by intestinal enzymes, leading to the formation of free Ursodiol that can be reabsorbed and reconjugated in the liver. Nonabsorbed Ursodiol passes into the colon where it is mostly 7-dehydroxylated to lithocholic acid. Some Ursodiol is epimerized to chenodiol (CDCA) via a 7-oxo intermediate. Chenodiol also undergoes 7-dehydroxylation to form lithocholic acid. These metabolites are poorly soluble and excreted in the feces. A small portion of lithocholic acid is reabsorbed, conjugated in the liver with glycine, or taurine and sulfated at the 3 position. The resulting sulfated lithocholic acid conjugates are excreted in bile and then lost in feces.
How many mg of ursodiol is in a USP?
Each Ursodiol tablet USP, 250 mg white to off white, elliptical shaped, biconvex film-coated tablet, debossed with "250" on one side and plain on the other side, contains 250 mg of Ursodiol. Available in bottles of 100 tablets (NDC 64380-918-06).
How many times a day can you take UDCA?
This study demonstrated that UDCA (13 to 15 mg/kg/day) given twice a day is equally effective to UDCA given four times a day. In addition, Ursodiol tablets, 250 mg was given as a single versus three times a day dosing schedules in 10 patients.
Where is ursodiol excreted?
Ursodiol is excreted primarily in the feces.
Where is lithocholic acid reabsorbed?
A small portion of lithocholic acid is reabsorbed, conjugated in the liver with glycine, or taurine and sulfated at the 3 position. The resulting sulfated lithocholic acid conjugates are excreted in bile and then lost in feces. In healthy subjects, at least 70% of Ursodiol (unconjugated) is bound to plasma protein.
Can ursodiol cause liver failure?
Lithocholic acid, when administered chronically to animals, causes cholestatic liver injury that may lead to death from liver failure in certain species unable to form sulfate conjugates. Ursodiol is 7-dehydroxylated more slowly than chenodiol. For equimolar doses of Ursodiol and chenodiol, steady state levels of lithocholic acid in biliary bile acids are lower during Ursodiol administration than with chenodiol administration. Humans and chimpanzees can sulfate lithocholic acid. Although liver injury has not been associated with Ursodiol therapy, a reduced capacity to sulfate may exist in some individuals.
Is ursodiol a hydrophilic bile acid?
Ursodiol, a naturally occurring hydrophilic bile acid, derived from cholesterol, is present as a minor fraction of the total human bile acid pool. Oral administration of Ursodiol increases this fraction in a dose related manner, to become the major biliary acid, replacing/displacing toxic concentrations of endogenous hydrophobic bile acids that tend to accumulate in cholestatic liver disease.
What to do if you don't respond to Ursodiol?
If you do not respond to ursodiol, your doctor may prescribe obeticholic acid. NIH external link. . Although obeticholic acid may improve blood test results, it may worsen symptoms. Obeticholic acid has not been shown to improve the course of illness or prevent cirrhosis.
Does Ursodiol cure biliary cholangitis?
NIH external link. . Although ursodiol does not cure primary biliary cholangitis, it can slow the progression of liver damage. People who respond to ursodiol early in the course of primary biliary cholangitis can live longer without needing a liver transplant. If you do not respond to ursodiol, your doctor may prescribe obeticholic acid.
How to treat PBC?
Because doctors do not know the cause of PBC, it cannot be prevented. However, you can take steps to lessen liver damage, including: 1 Quit smoking, stop drinking alcohol and stop using illegal drugs 2 Take all medicines as directed by your doctor. 3 Eat a healthy, well balanced diet. 4 Get regular exercise, such as walking.
Why do doctors believe PBC is caused by the immune system?
In PBC, doctors believe the immune system damages the bile ducts.
What is the function of the bile ducts?
The bile ducts are small tubes in the liver that carry bile (a substance needed to digest food) from the liver to other parts of the digestive system. When the bile ducts don’t work, bile builds up in the liver. This buildup can cause scarring in the liver (cirrhosis).
What causes PBC in family?
In addition, infections, smoking and exposure to certain chemicals may play a role in triggering PBC. PBC also tends to occur more commonly among family members. If one member of a family has PBC, the other family members are at an increased risk. Cleveland Clinic is a non-profit academic medical center.
What test is used to check for PBC?
Blood work, specific for liver disease, will also be checked. If you do have PBC, your doctor may also use an ultrasound test, which provides images of the liver and the bile ducts. Ultrasound enables doctors to see any other abnormal findings in the liver.
Is there a cure for PBC?
There is no known cure for PBC. Doctors use medication to manage symptoms and slow the progression of PBC. Ursodiol (Actigall®) helps remove bile from the liver. This treatment improves liver function and prevents progression of the liver disease in many cases.
Can PBC cause autoimmune disease?
While there is not a known cause, some people with PBC also have other related autoimmune diseases. These conditions include autoimmune hepatitis, thyroid diseases, scleroderma, Raynaud’s diseases, Sjogren’s syndrome and celiac disease. Frequent urinary tract infections are also often seen in patients with PBC.
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Indications and Usage For Ursodiol
Ursodiol Dosage and Administration
- General Dosing Information
The recommended adult dosage for Ursodiol tablets, USP 250 mg and 500 mg in the treatment of PBC is 13-15 mg/kg/day administered in two to four divided doses with food. Dosing regimen should be adjusted according to each patient's need at the discretion of the physician. - Liver Function Tests
Liver function tests (γ-GT, alkaline phosphatase, AST, ALT) and bilirubin levels should be monitored every month for three months after start of therapy, and every six months thereafter [see Warnings and Precautions (5.1)].
Dosage Forms and Strengths
- Ursodiol: 250 mg tablet
- Ursodiol: 500 mg scored tablet
Contraindications
- Patients with complete biliary obstruction and known hypersensitivity or intolerance to Ursodiol or any of the components of the formulation.
Warnings and Precautions
- Patients with variceal bleeding, hepatic encephalopathy, ascites or in need of an urgent liver transplant, should receive appropriate specific treatment.
Adverse Reactions
- Clinical Studies Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. The following table sum… - Postmarketing Experience
The following adverse reactions, presented by system organ class in alphabetical order, have been identified during post approval use of Ursodiol. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their …
Drug Interactions
- Bile Acid Sequestering Agents
Bile acid sequestering agents such as cholestyramine and colestipol may interfere with the action of Ursodiol by reducing its absorption. - Aluminum-based Antacids
Aluminum-based antacids have been shown to adsorb bile acids in vitroand may be expected to interfere with Ursodiol in the same manner as the bile acid sequestering agents.
Use in Specific Populations
- Pregnancy
Risk Summary Available published data on the 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 a… - Lactation
Risk Summary Ursodiol is naturally present in human milk. There are no reports of adverse effects of Ursodiol on the breastfed child, but the reports are extremely limited. There are no data on the effects of Ursodiol on milk production. The developmental and health benefits of breastfeeding …
Overdosage
- There have been no reports of accidental or intentional overdosage with Ursodiol. Single oral doses of Ursodiol at 10 g/kg in mice and dogs, and 5 g/kg in rats were not lethal. A single oral dose of Ursodiol at 1.5 g/kg was lethal in hamsters. Symptoms of acute toxicity were salivation and vomiting in dogs, and ataxia, dyspnea, ptosis, agonal convulsions and coma in hamsters.
Ursodiol Description
- Ursodiol tablets, USP 250 mg is available as a film-coated tablet for oral administration. Ursodiol tablets, USP 500 mg is available as a scored film-coated tablet for oral administration. Ursodiol (ursodeoxycholic acid, UDCA) is a naturally occurring bile acid found in small quantities in normal human bile and in larger quantities in the biles of certain species of bears. It is a bitter-tasting w…