MUPEg.com > Products > Gastroenterology > Ursochol

Composition:

Each capsule contains 250mg-ursodeoxycholic acid (UDCA) in micronized form.

Properties:

	Ursochol (ursodeoxycholic acid) is a naturally occurring bile acid found in small quantities in normal human bile (about 5% of total bile acids).
	Ursochol is an oral gallstone solubilizing agent intended for dissolution of cholesterol -radiolucent–gallstones. Ursochol is also approved for the prophylaxis against gallstone formation in obese patients who are rapidly losing weight. Ursochol is designated as an orphan drug for treating primary biliary cirrhosis.
	It is markedly more hydrophilic than other bile acids. Its high polarity correlates with its low potential of forming micelles -low surface activity and detergent effect -which may explain its safety profile

Clinical Pharmacology:

	Following oral administration, most of UDCA is absorbed by passive diffusion.
	In the liver UDCA is conjugated with glycine or taurine, then secreted into bile; these conjugates are absorbed in the small gut by both passive and active mechanisms.
	The conjugates are also deconjugated in the ileum by intestinal enzymes, leading to the formation of free UDCA that can be reabsorbed and reconjugated in the liver.
	unabsorbed UDCA passes into the colon where it is mostly dehydroxylated into lithocholic acid which is poorly soluble and is excreted in feces.
	In healthy individuals 70% of UDCA is bound to plasma protein. The drug is mostly distributed in bile and is mainly excreted in feces; urinary excretion is less than 1% (except in severe cholestatic liver disease).
	During chronic administration of 13-15mg/kg/day, Ursochol (UDCA) becomes a major biliary and plasma bile acid (constitutes up to 30 to 50 % of bile acids).

Indications:

Based on the above properties and effects, Ursochol is indicated in the following conditions
	Treatment of cholesterol radio translucent- non calcified - gallstones.
	Prophylaxis against gallstone formation in obese patients who are rapidly losing weight.
	Primary biliary cirrhosis and chronic cholestatic liver diseases.
	Chronic hepatitis.
	Dyspepsia due to biliary reflux gastritis, cholecystitis or gallstones.

Contraindications:

Hypersensitivity to ursodeoxycholic acid.

Precautions:

Patients with variceal bleeding, hepatic encephalopathy, ascitis or who are in need of urgent liver transplant should receive the appropriate specific treatment.

Interactions:

	Bile acid sequestering agents such as cholestyramin, or aluminum based antacids may interfere with the absorption of ursodeoxycholic acid.
	Estrogen, contraceptive pills and lipid lowering agents (such as clofibrate) increase hepatic cholesterol secretion and encourage cholesterol gallstone formation and hence may counteract the efficacy of Ursochol.

Pregnancy: (Pregnancy category B)

Studies in pregnant rats at oral doses up to 22 times the recommended maximum human dose and similar studies performed in pregnant rabbits have revealed no harm to the fetus due to UDCA.
However, since there are no adequate well-controlled studies in pregnant women and because animal reproduction studies are not always predictive of human response, UDCA should be used during pregnancy only if clearly needed and better be avoided in first trimester.

Adverse reactions:

UDCA is generally well tolerated, however steatorrhea due to unabsorbed fat may rarely occur; less frequently skin rash or leucopenia have also been reported.

Dosage & Administration:

To enhance its absorption Ursochol should be taken with meals since it dissolves more rapidly when bile and pancreatic juice are present in the intestinal chyme, the micronized form of UDCA in Ursochol enhances its rapid absorption
	Treatment of cholesterol gallstone: 8-10 mg/kg body weight, given in 2 divided doses, (Usual average adult dose is 1 capsule in the morning and 2 capsules in the evening usually taken with meals).
	Prophylaxis of gallstone formation in obese patients: 8-10 mg/kg body weight, (Usual average adult dose is 1 capsule in the morning and 1- 2 capsules in the evening usually taken with meals).
	In cholestatic liver diseases and chronic hepatitic conditions: 13-15 mg/kg body weight given in 2 divided doses; (Usual average adult dose is 1 capsule in the morning and 2-3 capsules in the evening usually taken with meals).
	In gastritis due to biliary reflux: 1 capsule daily.
Course of treatment:
	In cholesterol stone dissolution, cholestatic liver diseases and chronic hepatitic conditions: A long course of treatment is required, gallstones usually take 5 to 24 months to dissolve or as recommended by the physician. Treatment results and prognosis are assessed by performing periodic liver function tests, liver enzymes, ultrasonography and x-ray.
	In gastritis due to biliary reflux: usual treatment course is 2 weeks or as advised by the physician.

Package:

Each pack contains 20 capsules (in two strips)