Each film-coated tablet contains: Ursodeoxycholic Acid 300 mg.
Pharmacology: Pharmacokinetics: Ursodeoxycholic acid suppresses hepatic synthesis and secretion of cholesterol and also inhibits intestinal absorption of cholesterol.
Absorption: Rapidly and completely absorbed from the GI tract.
Distribution: Protein binding: 96-98%. Undergoes enterohepatic recycling.
Metabolism: Partly conjugated in the liver before being excreted into the bile. Free and conjugated forms undergo 7a-dehydroxylation to lithocholic acid under the influence of gut bacteria. Some are reabsorbed and then further conjugated and sulfated by the liver.
Excretion: Excreted through feces.
Ursodeoxycholic Acid tablet are indicated in the treatment of primary biliary cirrhosis (PBC) and for the dissolution of small to medium sized radiolucent, cholesterol-rich gallstones in patients with a functioning gall bladder.
Adults and elderly: 10-15 mg per kg per day in two to four divided doses or use as directed by physician.
Calcified and pigment gallstones, radio opaque gallstones.
Non-functioning gallbladders; chronic liver and peptic ulcer disease.
Inflammatory disease of colon and small intestine. Pregnancy.
Ursodeoxycholic acid film-coated tablet should be taken under medical supervision.
During the first 3 months treatment, liver function parameters AST (SGOT), ALT (SGPT) and γ-GT should be monitored by the physician every 4 weeks, thereafter every 3 months. Apart from allowing for identification of responders or non-responders in patients being treated for primary biliary cirrhosis, this monitoring would also enable early detection of potential hepatic deterioration, particularly in patients with advanced stage primary biliary cirrhosis.
Dissolution of Cholesterol Gallstones: In order to asses therapeutic progress and for timely detection on any calcification of the gallstones, depending on stone size, the gallbladder should be visualized (oral cholecystography) with overview and occlusion views in standing and supine positions (ultrasound control) 6-10 months after the beginning of treatment. If the gallbladder cannot be visualized on x-ray images or in cases of calcified gallstones, impaired contractility of the gallbladder or frequent episodes of biliary colic, ursodeoxycholic acid film-coated tablet should not be used.
Treatment of the Advanced Stages of Primary Biliary Cirrhosis: In very rare cases, decompensation of the hepatic cirrhosis has been observed; which partially regressed after the treatment discontinued. If diarrhea occurs, the dose must be reduced and in cases of persistent diarrhea, the therapy should be discontinued.
There are no adequate data on the use of ursodeoxycholic acid, particularly in the first trimester of pregnancy. Animal studies have provided evidence of a teratogenic effect during the early phase of gestation. Film-coated tablet must not be used during pregnancy unless clearly necessary. Women of childbearing potential should be treated only if they use reliable contraception.
Non-hormonal or low estrogen oral contraceptive measures are recommended. However, in patients taking ursodeoxycholic acid film-coated tablet for dissolution of gallstones, effective non-hormonal contraception should be used, since hormonal oral contraceptives may increase biliary lithiasis. The possibility of a pregnancy must be excluded before beginning treatment.
It is not known whether ursodeoxycholic acid passes into breast milk. Therefore, ursodeoxycholic acid film-coated tablet should not be taken during lactation.
The evaluation of undesirable effects is based on the following frequency data: Very common (greater than or equal to 1/10), common (greater than or equal to 1/100 to less than 1/10), uncommon (greater than or equal to 1/1,000 to greater than or equal to 1/100), rare (greater than or equal to 1/10,000 to less than 1/1,000), very rare (less than 1/10,000).
Gastrointestinal Disorders: In clinical trials, reports of pasty stools or diarrhea during ursodeoxycholic acid therapy were common. Very rarely, severe right upper biliary cirrhosis.
Hepatobiliary Disorders: During treatment with ursodeoxycholic acid, calcification of gallstones can occur in very rare cases. During therapy of advanced stages of primary biliary cirrhosis, in very rare cases, decomposition of hepatic cirrhosis has been observed, which partially regressed after the treatment was discontinued.
Skin and Subcutaneous Tissue Disorders: Very rarely, urticaria can occur.
Cholestyramine, charcoal and antacids may reduce effectiveness.
Aluminum-based antacids may reduce absorption. Estrogens and clofibrate may counteract effectiveness of ursodeoxycholic acid by increasing cholesterol elimination in bile. Possible increase in ciclosporin serum concentration. Decreased effectiveness of dapsone. Possible decrease in serum ciprofloxacin and nitrendipine.
Film-Coated Tablet: Ursodeoxycholic acid has been shown to reduce peak plasma concentration and area under the curve of the calcium antagonist nitrendipine. An interaction with a reduction of the therapeutic effects of dapsone was also reported. These observations, together with in vitro findings could indicate a potential for ursodeoxycholic acid to induce cytochrome P450 (CYP450) 3A enzymes. Controlled clinical studies have shown, however, that ursodeoxycholic acid does not have a relevant inductive effect on CYP450 3A enzymes. Estrogen hormones and blood cholesterol-lowering agents eg, clofibrate may increase biliary lithiasis, which is a counter-effect to ursodeoxycholic acid used for dissolution of gallstones.
Store at temperatures not exceeding 30ºC.
A05AA02 - ursodeoxycholic acid ; Belongs to the class of bile acids. Used in bile therapy.
Colimax FC tab 300 mg
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