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ursodeoxycholic acid; ursodiol (Actigall)

Tradename: Actigall. Indications: - small (< 20 mm) CT radiolucent, non-calcified gallstones in patients with high surgical risk - prevention of gallstone formation in patients on rapid weight-loss programs - primary biliary cirrhosis - post-exposure prophylaxis for Covid-19? * ursodiol inhibits expression of ACE2 (receptor for SARS-Cov2) in lung via binding to & inhibiting FXR [7] Contraindications: - delaying cholecystecomy in patients with symptomatic gallstones [5] Dosage: 8-10 mg/kg/day PO divided BID/TID for 6-24 months Tabs: 300 mg. Pharmacokinetics: 1) 90% absorbed in the small bowel 2) only small amounts are found in the plasma Adverse effects: 1) not common (1-10%) - diarrhea 2) uncommon (< 1%) - fatigue, headache, pruritus, nausea/vomiting, dyspepsia, metallic taste, abdominal pain, biliary pibitsain, constipation 3) other - stomatitis Drug interactions: 1) antacids, fiber, bile acid sequestrants: decrease absorption of ursodiol 2) estrogens, contraceptives: a) increase hepatic cholesterol secretion b) decrease effectiveness of ursodiol Mechanism of action: 1) suppresses hepatic synthesis & secretion of cholesterol 2) inhibits intestinal cholesterol absorption 3) binds to & inhibits the farnesyl X receptor (FXR)

General

gastrointestinal agent

Properties

MISC-INFO: elimination route BILE pregnancy-category B safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Mayo Internal Medicine Board Review, 1998-99, Prakash UBS (ed) Lippincott-Raven, Philadelphia, 1998, pg 329
  3. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  4. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  5. Venneman NG, Besselink MG, Keulemans YC, Vanberge-Henegouwen GP, Boermeester MA, Broeders IA, Go PM, van Erpecum KJ. Ursodeoxycholic acid exerts no beneficial effect in patients with symptomatic gallstones awaiting cholecystectomy. Hepatology. 2006 Jun;43(6):1276-83. PMID: 16729326
  6. Medical Knowledge Self Assessment Program (MKSAP) 11, American College of Physicians, Philadelphia 1998
  7. Brevini T, Maes M, Webb GJ et al FXR inhibition may protect from SARS-CoV-2 infection by reducing ACE2. Nature 2022. Dec 5. PMID: 36470304 https://www.nature.com/articles/s41586-022-05594-0