Dissolution of radiolucent, noncalcified cholesterol gallbladder stones < 20 mm in greatest diameter in patients at increased surgical risk; prevention of gallstone formation in obese patients experiencing rapid weight loss.
Also known as: Ursodiol, Urso, ursodeoxycholic acid, ácido ursodeoxicólico
DailyMed approved label (Ursodiol Capsule, Strides Pharma; setID 9a6c1928-2d52-4d9a-8e83-f71892a7e98d).
DailyMed approved label (Ursodiol Capsule, Strides Pharma; setID 9a6c1928-2d52-4d9a-8e83-f71892a7e98d).
Ursodeoxycholic acid + cholestyramine: cholestyramine reduces ursodiol absorption — separate doses by 4-6 hours.
The FDA ursodiol label documents in the interactions section that bile acid sequestering agents may interfere with the action of ursodiol by reducing its absorption ("Bile Acid Sequestering Agents: May interfere with the action of ursodiol tablets by reducing its absorption", 7.1). Cholestyramine binds bile acids and other molecules in the gut lumen, reducing the oral bioavailability of ursodeoxycholic acid given simultaneously. The clinical consequence is loss of efficacy in gallstone disease and primary biliary cholangitis — the patient may not respond to the usual dose. The practical guidance is to separate the doses: give ursodiol at least 1 hour before or 4-6 hours after cholestyramine, and assess clinical response. The same precaution applies to other sequestrants (colestipol, colesevelam).
Ursodeoxycholic acid + cholestyramine: cholestyramine reduces ursodiol absorption — separate doses by 4-6 hours.
The FDA ursodiol label documents: "Bile Acid Sequestering Agents: May interfere with the action of ursodiol tablets by reducing its absorption" (7.1). Cholestyramine binds bile acids in the gut lumen and reduces the absorption of orally administered ursodiol, compromising its effect in gallstone disease.
Assess clinical response (biliary symptoms, ultrasound follow-up when applicable) during the combination.
Lack of response in gallstone treatment with simultaneous intake.
Give ursodeoxycholic acid at least 1 hour before or 4-6 hours after cholestyramine; ideally space by 4-6 hours.
DailyMed/FDA (NIH/NLM) — approved Ursodiol label (BLUEPOINT LABORATORIES), section 7.1: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=a3c98080-0a4d-4a93-8dcb-02ab8533050b ; approved Cholestyramine label (ASCEND LABORATORIES): https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=430ac07e-8524-4dec-a599-b7ebc56d9563
Ursodeoxycholic acid + antacids: aluminium-containing antacids reduce ursodiol absorption — separate doses.
The FDA ursodiol label documents that aluminium-based antacids may interfere with the action of ursodiol by reducing its absorption ("Aluminum-based Antacids: May interfere with the action of ursodiol tablets by reducing its absorption", 7.2), and the Prontuário Terapêutico records the interaction with aluminium hydroxide in the ursodeoxycholic acid monograph (6.9.1). Adsorption to aluminium cations in the gut lumen reduces the oral bioavailability of ursodiol, compromising its effect in gallstone disease. The practical guidance is to separate administration by at least 2 hours and assess clinical response during the combination. In the gallstone patient, frequent simultaneous intake may translate into apparent lack of response.
Ursodeoxycholic acid + antacids: aluminium-containing antacids reduce ursodiol absorption — separate doses.
The FDA ursodiol label documents: "Aluminum-based Antacids: May interfere with the action of ursodiol tablets by reducing its absorption" (7.2), and the Prontuário Terapêutico records the interaction with aluminium hydroxide in the ursodeoxycholic acid monograph (6.9.1). Adsorption to aluminium cations reduces the oral bioavailability of ursodiol.
Assess clinical response during the combination.
Lack of response with simultaneous antacid intake.
Separate ursodeoxycholic acid from antacids by at least 2 hours.
DailyMed/FDA (NIH/NLM) — approved Ursodiol label (BLUEPOINT LABORATORIES), section 7.2: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=a3c98080-0a4d-4a93-8dcb-02ab8533050b ; Prontuário Terapêutico do INFARMED (11th ed., 2012) — Ursodeoxycholic acid, 6.9.1
Taking ursodeoxycholic acid with food optimises its dissolution and absorption.
Take with meals.
EMC-UK (MHRA) — approved Ursodeoxycholic acid SmPC: https://www.medicines.org.uk/emc/product/101999/smpc
Ursodeoxycholic acid is contraindicated in biliary obstruction and in patients with undrained cholangitis.
Do not use in patients with biliary obstruction.
EMC-UK (MHRA) — approved Ursodeoxycholic acid SmPC: https://www.medicines.org.uk/emc/product/101999/smpc
Ursodeoxycholic acid is used in intrahepatic cholestasis of pregnancy; it may be used when indicated.
Use under medical guidance, usually in the 2nd/3rd trimester for cholestasis of pregnancy.
Excreted into breast milk in small amounts; probably compatible.
No specific additional contraception.
EMC-UK (MHRA) — approved Ursodeoxycholic acid SmPC: https://www.medicines.org.uk/emc/product/101999/smpc
Clinical and educational support tool. The information does not replace a medical prescription or the opinion of a qualified healthcare professional.
Hydrophilic bile acid that reduces biliary cholesterol saturation: decreases hepatic cholesterol secretion and intestinal absorption, forming a liquid-crystalline phase that slowly dissolves cholesterol gallstones. It also exerts cytoprotective and immunomodulatory effects in primary biliary cholangitis.
Reduces biliary cholesterol saturation by decreasing hepatic cholesterol secretion and intestinal absorption, promoting progressive dissolution of cholesterol gallstones; the action takes place in the liver, bile and gut lumen.
Well absorbed in the small bowel (~90%); small quantities appear in the systemic circulation and very small amounts are excreted in urine.
About 90% of an oral dose is absorbed in the small bowel; after absorption it is efficiently extracted from portal blood by the liver (large first-pass effect), conjugated with glycine or taurine and secreted into the hepatic bile ducts. Undergoes enterohepatic circulation; a small proportion is degraded by intestinal bacteria.
Owing to enterohepatic circulation, the drug remains in the biliary compartment during the digestive cycle; the systemic half-life is short, but hepatic and biliary exposure is prolonged.
Medicines from the same therapeutic group (ATC classification) or the same pharmacological class.
