Actigall

Name: Actigall

What is Actigall (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.

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. Ursodiol capsules are not for treating gallstones that are calcified

Ursodiol may also be used for purposes not listed in this medication guide.

How should I take Actigall (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 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. Get your prescription refilled before you run out of medicine completely.

To treat gallstones, you may have to take ursodiol for several months before your gallstones dissolve. Keep using the medication as directed and tell your doctor if your symptoms do not improve.

Not all gallstones completely dissolve with ursodiol treatment, and you may develop new gallstones within 5 years after treatment. Talk to your doctor about your specific risks.

While using ursodiol, you may need gallbladder ultrasound exams, or frequent blood tests to check your liver function. Your doctor may also want to check your liver function every 6 months after you stop using ursodiol.

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.

Uses For Actigall

Ursodiol is used to dissolve gallstones in patients who do not need to have their gallbladders removed or in those in whom surgery should be avoided because of other medical problems. However, ursodiol works only in those patients whose gallstones are made of cholesterol and works best when these stones are small and of the “floating” type. It is also used to help prevent gallstones in patients who are on rapid weight-loss programs.

Ursodiol is also used to treat primary biliary cirrhosis (PBC). PBC is an autoimmune disorder that causes a patient's liver to have problems and not work properly.

This medicine is available only with your doctor's prescription.

Uses of Actigall

  • It is used to treat or prevent gallstones.
  • 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.

Indications and Usage for Actigall

  1. Actigall is indicated for patients with radiolucent, noncalcified gallbladder stones < 20 mm in greatest diameter in whom elective cholecystectomy would be undertaken except for the presence of increased surgical risk due to systemic disease, advanced age, idiosyncratic reaction to general anesthesia, or for those patients who refuse surgery. Safety of use of Actigall beyond 24 months is not established.
  2. Actigall is indicated for the prevention of gallstone formation in obese patients experiencing rapid weight loss.

Precautions

Liver Tests

Ursodiol therapy has not been associated with liver damage. Lithocholic acid, a naturally occurring bile acid, is known to be a liver-toxic metabolite. This bile acid is formed in the gut from ursodiol less efficiently and in smaller amounts than that seen from chenodiol. Lithocholic acid is detoxified in the liver by sulfation and, although man appears to be an efficient sulfater, it is possible that some patients may have a congenital or acquired deficiency in sulfation, thereby predisposing them to lithocholate-induced liver damage.

Abnormalities in liver enzymes have not been associated with Actigall therapy and, in fact, Actigall has been shown to decrease liver enzyme levels in liver disease. However, patients given Actigall should have SGOT (AST) and SGPT (ALT) measured at the initiation of therapy and thereafter as indicated by the particular clinical circumstances.

Drug Interactions

Bile acid sequestering agents such as cholestyramine and colestipol may interfere with the action of Actigall by reducing its absorption. Aluminum-based antacids have been shown to adsorb bile acids in vitro and may be expected to interfere with Actigall in the same manner as the bile acid sequestering agents. Estrogens, oral contraceptives, and clofibrate (and perhaps other lipid-lowering drugs) increase hepatic cholesterol secretion, and encourage cholesterol gallstone formation and hence may counteract the effectiveness of Actigall.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Ursodeoxycholic acid was tested in 2-year oral carcinogenicity studies in CD-1 mice and Sprague-Dawley rats at daily doses of 50, 250, and 1000 mg/kg/day. It was not tumorigenic in mice. In the rat study, it produced statistically significant dose-related increased incidences of pheochromocytomas of adrenal medulla in males (p = 0.014, Peto trend test) and females (p = 0.004, Peto trend test). A 78-week rat study employing intrarectal instillation of lithocholic acid and tauro-deoxycholic acid, metabolites of ursodiol and chenodiol, has been conducted. These bile acids alone did not produce any tumors. A tumor-promoting effect of both metabolites was observed when they were co-administered with a carcinogenic agent. Results of epidemiologic studies suggest that bile acids might be involved in the pathogenesis of human colon cancer in patients who had undergone a cholecystectomy, but direct evidence is lacking. Ursodiol is not mutagenic in the Ames test. Dietary administration of lithocholic acid to chickens is reported to cause hepatic adenomatous hyperplasia.

Pregnancy Category B

Reproduction studies have been performed in rats and rabbits with ursodiol doses up to 200-fold the therapeutic dose and have revealed no evidence of impaired fertility or harm to the fetus at doses of 20- to 100-fold the human dose in rats and at 5-fold the human dose (highest dose tested) in rabbits. Studies employing 100- to 200-fold the human dose in rats have shown some reduction in fertility rate and litter size. There have been no adequate and well-controlled studies of the use of ursodiol in pregnant women, but inadvertent exposure of 4 women to therapeutic doses of the drug in the first trimester of pregnancy during the Actigall trials led to no evidence of effects on the fetus or newborn baby. Although it seems unlikely, the possibility that ursodiol can cause fetal harm cannot be ruled out; hence, the drug is not recommended for use during pregnancy.

Nursing Mothers

It is not known whether ursodiol is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Actigall is administered to a nursing mother.

Pediatric Use

The safety and effectiveness of Actigall in pediatric patients have not been established.

Geriatric Use

In worldwide clinical studies of Actigall, approximately 14% of subjects were over 65 years of age (approximately 3% were over 75 years old). In a subgroup analysis of existing clinical trials, patients greater than 56 years of age did not exhibit statistically significantly different complete dissolution rates from the younger population. No age-related differences in safety and effectiveness were found. Other reported clinical experience has not identified differences in response in elderly and younger patients. However, small differences in efficacy and greater sensitivity of some elderly individuals taking Actigall cannot be ruled out. Therefore, it is recommended that dosing proceed with caution in this population.

Actigall Overview

Actigall is a prescription medication used to non-surgically treat and prevent gallstones. Actigall is a bile acid, a natural substance produced by the liver. It helps to decrease the formation of gallstones by dissolving the cholesterol necessary to make gallstones and suppressing production of cholesterol in the liver and absorption in the intestines. 

Actigall comes in capsule form. It is taken 2 or 3 times daily, with food.

Common side effects include stomach pain, diarrhea, and headache. 

Actigall can cause dizziness. Do not drive or operate heavy machinery until you know how it affects you.

Side Effects of Actigall

Common side effects include:

  • stomach pain
  • diarrhea
  • constipation
  • nausea
  • headache
  • indigestion
  • dizziness
  • vomiting
  • cough
  • sore throat
  • runny nose
  • back pain
  • muscle and joint pain
  • hair loss
  • viral infection

This is not a complete list of Actigall side effects. Ask your doctor or pharmacist for more information.

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Ursodiol Pregnancy Warnings

FDA pregnancy category: B Ursodiol should be used during pregnancy only if clearly needed.

Animal studies have failed to reveal evidence of fetal harm. There are no controlled data in human pregnancy.

Ursodiol Breastfeeding Warnings

Caution is recommended. Excreted into human milk: Unknown Excreted into animal milk: Unknown The effects in the nursing infant are unknown.

Administrative Information

LactMed Record Number

510

Last Revision Date

20130907

Disclaimer

Information presented in this database is not meant as a substitute for professional judgment. You should consult your healthcare provider for breastfeeding advice related to your particular situation. The U.S. government does not warrant or assume any liability or responsibility for the accuracy or completeness of the information on this Site.

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