Ursodiol

Ursodiol is a bile acid used to treat small gallstones in people who cannot have gallbladder surgery, and to prevent gallstones in overweight patients undergoing rapid weight loss. Ursodiol is also used to treat primary biliary cirrhosis (PBC).

Ursodiol is available under the following different brand names: Actigall, and Urso Forte.

Adult and Pediatric Dosage Forms and Strengths

Capsules

• 300 mg

Tablets

• 250 mg
• 500 mg

Dosage Considerations – Should be Given as Follows:

• 8-10 mg/kg/day orally divided every 8-12 hours orally; not to exceed 300 mg/dose
• Maintenance: 250 mg orally at bedtime for 6 months

Primary Biliary Cirrhosis

• 13-15 mg/kg/day orally divided orally with food

Biliary Atresia, Pediatric (Off-Label)

• 10-15 mg/kg orally once/day

Common side effects or health problems may include:

• Headache
• Dizziness
• Diarrhea
• Indigestion
• Nausea/vomiting
• Back pain
• Upper respiratory tract infection
• Hair loss
• Rash
• High blood sugar (hyperglycemia)
• Gas (flatulence)
• Peptic ulcer
• Urinary tract infection
• Low white blood cell counts (leukopenia)
• Low platelet counts (thrombocytopenia)
• Gallbladder inflammation
• Stomach upset or pain
• Constipation
• Tired feeling
• Fever
• Chills
• Body aches
• Flu symptoms
• Runny or stuffy nose
• Cough
• Cold symptoms

Serious side effects of ursodiol include:

• Weakness
• Swelling of the ankles or feet
• Increased thirst or urination
• Signs of infection (e.g., fever, persistent sore throat)
• Easy bleeding or bruising

Less common side effects of ursodiol include:

• Fatigue
• Abdominal pain
• Itching
• Skin swelling
• Biliary pain

Postmarketing side effects of ursodiol reported include:

• Hepatobiliary disorders: Yellowing of skin or eyes (jaundice) (or aggravation of pre-existing jaundice)
• Abnormal laboratory tests: Increased ALT, AST, alkaline phosphatase, bilirubin, gamma-GT

This is not a complete list of side effects and other serious side effects or health problems may occur as a result of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of this medicine or any drug before seeking medical advice from your doctor, healthcare provider or pharmacist first. To do so may result in serious consequences or side effects.

Ursodiol has no known severe interactions with other drugs.

Moderate interactions of ursodiol include:

• aluminum hydroxide
• calcium carbonate
• crofelemer
• eluxadoline
• ethinylestradiol
• sodium bicarbonate
• sodium citrate/citric acid

Mild interactions of ursodiol include:

• cholestyramine
• colesevelam
• colestipol
• mestranol

Ursodiol has mild interactions with at least 65 different drugs.
This document does not contain all possible interactions from the use of this medication. Therefore, before using this drug, tell your doctor or pharmacist of all the drugs you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist. Check with your physician if you have health questions or concerns.

Warnings

• This medication contains ursodiol. Do not take Actigall or Urso Forte if you are allergic to ursodiol or any ingredients contained in this drug.
• Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately.

Contraindications

• Hypersensitivity
• Gallstone complication requiring surgery
• Known hepatocyte or bile ductal abnormalities, inflammatory bowel disease
• Calcified gallstones, bile acid allergy, chronic hepatic disease
• Billiary gastrointestinal fistula
• Patients requiring cholecystectomy

Effects of Drug Abuse

• No information provided

Short-Term Effects

• See "What Are Side Effects Associated with Using Ursodiol?"

Long-Term Effects

• See "What Are Side Effects Associated with Using Ursodiol?"

Cautions

• Only use in radiolucent, non-calcified, high cholesterol content gallstone.
• Chronic liver disease.
• Liver function tests (gamma-GT, alkaline phosphatase, AST, ALT) and bilirubin levels should be monitored every 3 months for 3 months after start of therapy, and every 6 months thereafter.
• Gallbladder stone dissolution may take several months.
• 50% of cases have stone recurrence in 5 years.

Pregnancy and Lactation

• Ursodiol may be acceptable for use during pregnancy. Either animal studies show no risk but human studies are not available or animal studies showed minor risks and human studies were done and showed no risk.
• It is unknown if ursodiol is excreted in breast milk; use caution if breastfeeding.