ursodeoxycholic acid; ursodiol (Actigall)
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Introduction
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
- 90% absorbed in the small bowel
- only small amounts are found in the plasma
elimination via bile
Adverse effects
- not common (1-10%)
- uncommon (< 1%)
- fatigue, headache, pruritus, nausea/vomiting, dyspepsia, metallic taste, abdominal pain, biliary pibitsain, constipation
- other
Drug interactions
- antacids, fiber, bile acid sequestrants: decrease absorption of ursodiol
- estrogens, contraceptives:
- increase hepatic cholesterol secretion
- decrease effectiveness of ursodiol
Mechanism of action
- suppresses hepatic synthesis & secretion of cholesterol
- inhibits intestinal cholesterol absorption
- binds to & inhibits the farnesyl X receptor (FXR)
More general terms
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Mayo Internal Medicine Board Review, 1998-99, Prakash UBS (ed) Lippincott-Raven, Philadelphia, 1998, pg 329
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ 5.0 5.1 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: https://www.ncbi.nlm.nih.gov/pubmed/16729326
- ↑ Medical Knowledge Self Assessment Program (MKSAP) 11, American College of Physicians, Philadelphia 1998
- ↑ 7.0 7.1 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: https://www.ncbi.nlm.nih.gov/pubmed/36470304 https://www.nature.com/articles/s41586-022-05594-0
Database
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=31401
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5645
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5315136
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=388708
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=376832
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=465690