URSODEOXYCHOLIC ACID Tablet Ref.[7799] Active ingredients: Ursodeoxycholic acid

Dosage

The dosage should be calculated based on the patient’s body weight. The calculated dosage should be rounded to the nearest number of tablets.

Dissolving of cholesterol stones

Usual dosage: 8 to 10 mg/kg/day, corresponding to, for example, four to six 150 mg tablets, or two to three tablets of 300 mg, or two tablets of 450 mg. The daily dose can be administered two or three times after the meals: two tablets should always be taken after the evening meal.

Also a single evening dose can be selected (e.g. a patient of 60 kg, in the evening two tablets of 300 mg). Preferably, this single dose should be taken one hour before bedtime and ± two hours after the evening meal with a glass of milk or a small snack.

The duration of the treatment in order to obtain lysis of the gallstones depends on their size, but is usually not shorter than three to four months. To assess the result of the therapy properly, it is necessary to determine the size of the stones accurately at the start of the treatment and to check this further regularly, for example every six months, by means of a new contrast X-ray recording and/or sonographic recording.

In patients in whom, after six months of treatment with the indicated dosage, the stones are not reduced in size, it is recommended to determine the lithogenic index in the bile by means of a duodenum drainage. When the bile has an index of >1.0, it is unlikely that a favourable result can be obtained, and it is better to consider a different form of treatment for the gallstones.

Treatment should be continued for three to four months after it is established by means of ultrasound check that the gallstones are completely dissolved. An interruption of the treatment for three to four weeks results in a return to over-saturation of the bile and prolongs the overall duration of the therapy. The interruption of the treatment after the dissolving of the gallstones can be followed by a recurrence.

Primary Biliary Cholangitis

The dosage of ursodeoxycholic acid in primary biliary cholangitis (stages I-III), amounts to 12-15 mg/kg/day, which is equivalent to four to eight tablets of 150 mg, two to four tablets of 300 mg, to be taken in two to three portions during the day, or with two tablets of 450 mg, to be taken in two portions during the day.

The dosage of ursodeoxycholic acid in primary biliary cholangitis stage IV and an increase of the serum bilirubin contents (>40 μg/l), should be in the first instance, only a half of the normal dose (6 to 8 mg/kg/day). Thereafter, the liver function should be closely monitored for several weeks (once every two weeks for six weeks). If there is no deterioration of the liver function (AF, ALT (SGPT), AST (SGOT), γ-GT, bilirubin) and no increase in itching occurs, the dose may be further increased to the usual level. Moreover, the liver function must then again be closely monitored for several weeks. If again no deterioration of the liver function takes place, the patient may be held at the normal dosage for a long time.

In patients with primary biliary cholangitis stage IV without elevated serum bilirubin, the usual starting dose is allowed to be administered directly. Anyway, here too an accurate control of the liver function should be executed.

The treatment of the primary biliary cholangitis should be regularly assessed on the basis of liver values (laboratory) and clinical findings.

Paediatric population

Children with cystic fibrosis aged 6 years to 18 years

Treatment of hepatobiliary diseases as a result of cystic fibrosis 20 mg/kg/day divided in two to three divided doses. If necessary, increase to 30 mg/kg/day. This corresponds with four to ten tablets of 150mg, two to five tablets of 300 mg, or with two to three tablets of 450 mg, to be taken in one or two portions during the day.

Method of administration

If the patient has difficulty in swallowing because of the size of the tablet, the tablet can be halved if necessary on the dividing score, so that one half tablet can be taken twice directly in sequence.

In the case of overdose diarrhoea may occur. In general, other symptoms of overdose are unlikely, because the absorption of the ursodeoxycholic acid decreases with increasing dose and therefore more is excreted in the faeces.

If diarrhoea occurs, the dosage should be reduced, and treatment should be discontinued in case of persistent diarrhoea.

No specific measures are needed and the consequences of diarrhoea should be treated symptomatically with restoration of fluid and electrolyte balance.

Additional information or special populations

Long-term, high-dose UDCA therapy (28-30 mg/kg/day) by patients with primary sclerosing cholangitis (off-label use) was associated with a higher frequency of serious adverse events.

24 months.

Do not store above 25°C.

Clear PVC/PVDC – plain aluminium foil.

Pack size: 20, 30, 50, 60 and 100 tablets.

Not all pack sizes may be marketed.

No special requirements.