Ursodeoxycholic acid


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Dissolution of cholesterol-rich gallstones 8-12 mg/kg once daily at bedtime or in 2 divided doses continued for 3-4 mth after radiological disappearance of gallstones. Duration: Up to 2 yr. Primary biliary cirrhosis 10-16 mg/kg/day in 2-4 divided doses, may be taken once daily in the evening after the 1st 3 mth. Prophylaxis of gallstones in patients undergoing rapid wt loss 300 mg bid.
Dosage Details
Oral
Dissolution of cholesterol-rich gallstones
Adult: 8-12 mg/kg once daily at bedtime or in 2 divided doses continued for 3-4 mth after radiological disappearance of gallstones. Duration of treatment: Up to 2 yr. Obese patients: Up to 15 mg/kg daily.

Oral
Prophylaxis of gallstones in patients undergoing rapid weight loss
Adult: 300 mg bid.

Oral
Primary biliary cirrhosis
Adult: 10-16 mg/kg daily in 2-4 divided doses, may be taken once daily in the evening after the 1st 3 mth.
Administration
Should be taken with food.
Contraindications
Acute inflammation of gallbladder or biliary tract, occlusion of biliary tract, frequent episodes of biliary colic, radio-opaque calcified gallstones, impaired contractility of gallbladder, non-functioning gallbladder, inflammatory bowel disease, hepatic and intestinal conditions interfering w/ enterohepatic recirculation of bile acids, extrahepatic and intrahepatic cholestasis, ileal resection and stoma, regional ileitis, active duodenal and gastric ulcer; acute, chronic or severe hepatic disease.
Special Precautions
Pregnancy and lactation.
Adverse Reactions
Nausea, vomiting, diarrhoea, other GI disturbances, pruritus, viral infection, headache, upper resp tract infection, sinusitis, pharyngitis, arthralgia, back pain, cough, bronchitis, UTI, arthritis, myalgia, cholecystitis, rhinitis, fatigue, dysmenorrhoea, musculoskeletal pain, asthenia, peripheral oedema, HTN. Rarely, gallstone calcification, liver function deterioration.
MonitoringParameters
Monitor LFTs mthly for the 1st 3 mth and every 6 mth thereafter.
Overdosage
Symptoms: Diarrhoea. Management: Symptomatic treatment w/ fluid and electrolyte balance restoration.
Drug Interactions
Reduced absorption w/ Al-containing antacids, bile acid sequestrants (e.g. cholestyramine, colestipol), charcoal. Possibly reduced efficacy w/ clofibrate, oestrogens and OCs. May increase the absorption of ciclosporin.
Action
Description: Ursodeoxycholic acid suppresses hepatic synthesis and secretion of cholesterol and also inhibits intestinal absorption of cholesterol.
Pharmacokinetics:
Absorption: Absorbed from the GI tract.
Distribution: Plasma protein binding: Approx 70%.
Metabolism: Undergoes extensive enterohepatic recycling. Free and conjugated forms undergo 7α-dehydroxylation to lithocholic acid under the influence of intestinal bacteria; some of which are further conjugated and sulfated hepatically.
Excretion: Via faeces; urine (<1%). Half-life: Approx 4-6 days.
Chemical Structure

Chemical Structure Image
Ursodeoxycholic acid

Source: National Center for Biotechnology Information. PubChem Database. Ursodeoxycholic acid, CID=31401, https://pubchem.ncbi.nlm.nih.gov/compound/Ursodeoxycholic-acid (accessed on Jan. 23, 2020)

Storage
Store between 20-25°C.
ATC Classification
A05AA02 - ursodeoxycholic acid ; Belongs to the class of bile acids. Used in bile therapy.
References
Anon. Ursodiol. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 05/02/2016.

Buckingham R (ed). Ursodeoxycholic acid. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/02/2016.

Joint Formulary Committee. Ursodeoxycholic acid. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/02/2016.

McEvoy GK, Snow EK, Miller J et al (eds). Ursodiol. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 05/02/2016.

Ursodiol Capsule (Actavis Pharma, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/02/2016.

Disclaimer: This information is independently developed by MIMS based on Ursodeoxycholic acid from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
Register or sign in to continue
Asia's one-stop resource for medical news, clinical reference and education
Sign up for free
Already a member? Sign in