Ursodeoxycholic acid


Generic Medicine Info
Indications and Dosage
Oral
Dissolution of cholesterol-rich gallstones
Adult: 8-12 mg/kg once daily at bedtime or in 2 divided doses. May continue for up to 2 years depending on stone size and composition. Treatment is continued for 3-4 months after radiological disappearance of gallstones. Dosage recommendations may vary among individual products and between countries (refer to specific product guidelines).

Oral
Primary biliary cirrhosis
Adult: 12-16 mg/kg daily in 2-4 divided doses for the 1st 3 months, then may be given as once daily in the evening thereafter. Dosage recommendations may vary among individual products and between countries (refer to specific product guidelines).

Oral
Hepatobiliary disorder associated with cystic fibrosis
Child: As oral susp: ≥1 month 20 mg/kg daily to be given in 2-3 divided doses, may increase up to 30 mg/kg daily as necessary. As cap or tab: ≥6 years 20 mg/kg daily to be given in 2-3 divided doses, may increase up to 30 mg/kg daily as necessary. Dosage recommendations may vary among individual products and between countries (refer to specific product guidelines).

Oral
Prophylaxis of gallstones in patients undergoing rapid weight loss
Adult: As cap: 600 mg daily as a single or in 2 divided doses.
Special Patient Group
Dissolution of cholesterol-rich gallstones:
In obese patient: Up to 15 mg/kg daily may be needed.
Administration
Should be taken with food.
Contraindications
Acute inflammation of gallbladder or biliary tract, biliary tract occlusion (common bile duct or cystic duct), frequent episodes of biliary colic, radio-opaque calcified gallstones, impaired contractility of gallbladder, gallstone pancreatitis or biliary-gastrointestinal fistula, non-functioning gallbladder, inflammatory bowel disease; hepatic and intestinal conditions interfering with enterohepatic recirculation of bile acids (e.g. extrahepatic and intrahepatic cholestasis, ileal resection and stoma, regional ileitis); active duodenal and gastric ulcer; unsuccessful portoenterostomy or without recovery of normal bile flow in children with biliary atresia. Acute, chronic or severe hepatic impairment.
Special Precautions
Patients with non-visualising gallbladder, variceal bleeding, hepatic encephalopathy, ascites. Obese patients. Children. Pregnancy and lactation.
Adverse Reactions
Significant: Biliary obstruction.
Gastrointestinal disorders: Diarrhoea, pasty stools, nausea, vomiting, constipation, dyspepsia; rarely, severe right upper abdominal pain (if used for primary biliary cirrhosis).
Hepatobiliary disorders: Rarely, calcification of gallstones, decompensation of liver cirrhosis.
Musculoskeletal and connective tissue disorders: Back pain.
Nervous system disorders: Headache, dizziness.
Respiratory, thoracic and mediastinal disorders: Upper respiratory tract infection.
Skin and subcutaneous tissue disorders: Urticaria, pruritus.
Monitoring Parameters
Monitor liver function tests (e.g. AST, ALT, γ-GT) as clinically necessary. If used for the dissolution of gallstone, perform oral cholecystography and ultrasound periodically. Evaluate pregnancy status before initiation of therapy.
Overdosage
Symptoms: Diarrhoea. Management: Symptomatic treatment with fluid and electrolyte balance restoration, may use ion-exchange resins to bind bile acids in the intestines.
Drug Interactions
May reduce absorption and efficacy with bile acid-binding resins (e.g. colestyramine, colestipol), antacids (e.g. aluminium hydroxide, aluminium oxide), charcoal. May increase absorption and serum concentration of ciclosporin. May reduce absorption of ciprofloxacin, nitrendipine. Increased hepatic cholesterol secretion and reduced efficacy with estrogen hormones, oral contraceptives, blood cholesterol-lowering agents (e.g. clofibrate). May increase serum concentration of rosuvastatin.
Action
Description: Ursodeoxycholic acid is a naturally occurring bile acid. It reduces cholesterol secretion from the liver and fractional reabsorption of the cholesterol by the intestine resulting in decreased cholesterol content of the bile and bile stones.
Synonym: UDCA, Ursodiol.
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract.
Distribution: Enters breast milk. Plasma protein binding: Approx 70%.
Metabolism: Undergoes extensive enterohepatic recycling, partly conjugated in the liver prior to biliary excretion. Under the influence of intestinal bacteria, the free and conjugated forms undergo 7α-dehydroxylation to lithocholic acid; some of which are further conjugated and sulfated hepatically.
Excretion: Via faeces; urine (<1%). Elimination half-life: Approx 3.5-5.8 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 below 30°C.
MIMS Class
Cholagogues, Cholelitholytics & Hepatic Protectors
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 13/04/2021.

Buckingham R (ed). Ursodeoxycholic acid. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 13/04/2021.

Joint Formulary Committee. Ursodeoxycholic acid. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 13/04/2021.

Reltone 200 mg, 400 mg Capsule (Intra-Sana Laboratories). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 15/04/2021.

Ursodeoxycholic Acid 250 mg Capsules, Hard (AS Grindeks). MHRA. https://products.mhra.gov.uk. Accessed 13/04/2021.

Ursodeoxycholic Acid 500 mg Tablets (TEVA UK Limited). MHRA. https://products.mhra.gov.uk. Accessed 13/04/2021.

Ursodiol Tablet (BluePoint Laboratories). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 15/04/2021.

Ursofalk 250 mg/5 mL Suspension (Dr Falk Pharma UK Ltd). MHRA. https://products.mhra.gov.uk. Accessed 13/04/2021.

Ursosan 250 mg Hard Capsules (PharmEng Technology Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 13/04/2021.

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 © 2021 MIMS. All rights reserved. Powered by MIMS.com
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