Ambisol-150/Ambisol-300

Ambisol-150/Ambisol-300

ursodeoxycholic acid

Manufacturer:

Sydler Remedies

Distributor:

Ambica
Full Prescribing Info
Contents
Ursodeoxycholic acid.
Description
Each uncoated tablet contains: Ursodiol (Ursodeoxycholic Acid) USP 150 or 300 mg, Excipients qs.
Action
Pharmacology: Pharmacodynamics: Mechanism of action: Ursodeoxycholic acid reduces the ratio of cholesterol to bile salts plus phospholipids in bile, causing desaturation of cholesterol saturated bile. The exact mechanism of action has not been fully elucidated.
Pharmacokinetics: Ursodeoxycholic acid is absorbed from the gastrointestinal tract and undergoes enterohepatic recycling. It is partly conjugated in the liver before being excreted into the bile. Under the influence of intestinal bacteria the free and conjugated forms undergo 7a-dehydroxylation to lithocholic acid, some of which is excreted directly in the faeces and the rest absorbed and mainly conjugated and sulfated by the liver before excretion in the faeces. However, in comparison with chenodeoxycholic acid, less ursodeoxycholic acid undergoes such bacterial degradation.
Indications/Uses
Ursodeoxycholic Acid tablets are indicated in the treatment of primary biliary cirrhosis (PBC) and for the dissolution of small to medium sized radiolucent, cholesterol-rich gall-stones in patients with a functioning gall bladder.
Dosage/Direction for Use
Ursodeoxycholic acid tablets are for oral administration.
To be taken with a drink of water.
Primary Biliary Cirrhosis: Adults and Elderly: 10-15 mg ursodeoxycholic acid (UDCA) per kg per day in two or four divided doses.
Children: Dosage should be related to bodyweight.
Dissolution of gallstones: Adults and Elderly: The usual dose is 6-12 mg/kg/day either as a single night time dose or in divided doses. This may be increased to 15 mg/kg/day in obese patients, if necessary.
The duration of treatment may be up to two years, depending on the size of the stone(s), and should be continued for three months after apparent dissolution of the stone(s).
Children: Dosage should be related to bodyweight. Or as prescribed by the physician.
Overdosage
Diarrhoea may occur in cases of overdose. In general, other symptoms of overdose are unlikely because the absorption of ursodeoxycholic acid decreases with increasing dose and therefore more is excreted with the faeces.
No specific counter-measures are necessary and the consequences of diarrhoea should be treated symptomatically with restoration of fluid and electrolyte balance.
Contraindications
Ursodeoxycholic acid should not be used in patients with: Radio-opaque calcified gall-stones, Acute inflammation of the gall bladder or biliary tract.
Occlusion of the biliary tract (occlusion of the common bile duct or a cystic duct).
Frequent episodes of biliary colic.
Impaired contractability of the gall bladder.
Hypersensitivity to bile acids or any excipients of the formulation.
Who are pregnant or breastfeeding, or in women who may become pregnant.
Chronic liver disease, peptic ulcers or in those with inflammatory disease of the small intestine and colon.
Special Precautions
Ursodeoxycholic acid should be taken under medical supervision.
During the first 3 months of treatment, the 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 and 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.
When used for the dissolution of cholesterol gallstones: In order to assess therapeutic progress and for timely detection of any calcification of the gallstones, depending on stone size, the gall bladder should be visualised (oral cholecystography) with overview and occlusion views in standing and supine positions (ultrasound control) 6-10 months after the beginning of treatment.
If the gall bladder cannot be visualised on X-ray images, or in cases of calcified gallstones, impaired contractility of the gall bladder or frequent episodes of biliary colic, ursodeoxycholic acid should not be used.
When used for treatment of advanced stage of primary biliary cirrhosis: In very rare cases decompensation of hepatic cirrhosis has been observed, which partially regressed after the treatment was discontinued.
If diarrhoea occurs, the dose must be reduced and in cases of persistent diarrhoea, the therapy should be discontinued.
Patients with rare hereditary problems of galactose intolerance, the Lapp lactose deficiency or glucose-galactose malabsorption should not take this medicine.
Adverse Reactions
The evaluation of undesirable effects is based on the following frequency data: Very common (≥ 1/10), Common (≥ 1/100 to < 1/10), Uncommon (≥ 1/1,000 to < 1/100), Rare (≥ 1/10,000 to < 1/1,000), Very rare/Not known (< 1/10,000/cannot be estimated from available data).
Gastrointestinal disorders: In clinical trials, reports of pasty stools or diarrhoea during ursodeoxycholic acid therapy were common.
Very rarely, severe right upper abdominal pain has occurred during the treatment of primary biliary cirrhosis.
Ursodeoxycholic acid may give rise to nausea and vomiting. The frequency of these effects are not known.
Hepatobiliary disorders: During treatment with ursodeoxycholic acid, calcification of gallstones can occur in very rare cases making them unable to be dissolved by bile acid therapy and resulting in surgery for some patients.
During therapy of the advanced stages of primary biliary cirrhosis, in very rare cases decompensation of hepatic cirrhosis has been observed, which partially regressed after the treatment was discontinued.
Skin and subcutaneous disorders: Very rarely, urticaria can occur.
Ursodeoxycholic acid may give rise to pruritus. The frequency of this effect is not known.
Drug Interactions
Ursodeoxycholic acid should not be administered concomitantly with charcoal, colestyramine, colestipol or antacids containing aluminium hydroxide and/or smectite (aluminium oxide), because these preparations bind ursodeoxycholic acid in the intestine and thereby inhibit its absorption and efficacy. Should the use of a preparation containing one of these substances be necessary, it must be taken at least 2 hours before or after ursodeoxycholic acid.
Ursodeoxycholic acid can increase the absorption of ciclosporin from the intestine. In patients receiving ciclosporin treatment, blood concentrations of this substance should therefore be checked by the physician and the ciclosporin dose adjusted if necessary.
In isolated cases ursodeoxycholic acid can reduce the absorption of ciprofloxacin.
Ursodeoxycholic acid has been shown to reduce the plasma peak concentrations (Cmax) and the area under the curve (AUC) of the calcium antagonist nitrendipine. An interaction with a reduction of the therapeutic effect of dapsone was also reported. These observations together with in vitro findings could indicate a potential for ursodeoxycholic acid to induce cytochrome P450 3A enzymes. Controlled clinical trials have shown, however, that ursodeoxycholic acid does not have a relevant inductive effect on cytochrome P450 3A enzymes.
Oral contraceptives, oestrogenic hormones and blood cholesterol lowering agents such as clofibrate may increase biliary lithiasis, which is a counter-effect to ursodeoxycholic acid used for dissolution of gallstones.
Storage
Store at temperatures not exceeding 25°C. Protect from light.
Shelf Life: 36 Months from the date of manufacturing.
ATC Classification
A05AA02 - ursodeoxycholic acid ; Belongs to the class of bile acids. Used in bile therapy.
Presentation/Packing
Ambisol-150: Tab 150 mg x 30's.
Ambisol-300: Tab 300 mg x 30's.
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