Ursofalk

Each capsule of Ursofalk contains the following active ingredient:

Ursodeoxycholic Acid 250mg

White, opaque, hard gelatine capsule

Ursofalk is indicated in the treatment of primary biliary cirrhosis (PBC) and for the dissolution of radiolucent gallstones in patients with a functioning gall bladder.

Method of administration: Oral

Primary Biliary Cirrhosis

Adults and the Elderly: 10-15mg ursodeoxycholic acid (UDCA) per kg per day in two to four divided doses. The following dosage regimen is recommended:

Children: Dosage should be related to bodyweight.

Dissolution of gallstones

Adults: 8-12mg ursodeoxycholic acid (UDCA) per kg per day in two divided doses. The following dosage regimen is recommended:

If doses are unequal the larger dose should be taken in late evening to counteract the rise in biliary cholesterol saturation which occurs in the early morning. The late evening dose may usefully be taken with food to help maintain bile flow overnight.

The time required for dissolution of gallstones is likely to range from 6 to 24 months depending on stone size and composition. Follow-up cholecystograms or ultrasound investigation may be useful at 6 month intervals until the gallstones have disappeared.

Treatment should be continued until 2 successive cholecystograms and/or ultrasound investigations 4-12 weeks apart have failed to demonstrate gallstones. This is because these techniques do not permit reliable visualisation of stones less than 2mm in diameter.

The likelihood of recurrence of gallstones after dissolution by bile acid treatment has been estimated as up to 50% at 5 years.

The efficiency of Ursofalk in treating radio-opaque or partially radio opaque gallstones has not been tested but these are generally thought to be less soluble than radiolucent stones.

Non-cholesterol stones account for 10-15% radiolucent stones and may not be dissolved by bile acids.

Elderly: There is no evidence to suggest that any alteration in the adult dose is needed but the relevant precautions should be taken into account.

Children: Cholesterol rich gallstones are rare in children but when they occur, dosage should be related to bodyweight.

Ursofalk is not suitable for the dissolution of radio-opaque gallstones and should not be used in patients with a non-functioning gall bladder.

A product of this class has been found to be carcinogenic in animals. The relevance of these findings to the clinical use of Ursofalk has not been established.

Some drugs, such as cholestyramine, charcoal, colestipol and certain antacids (e.g. aluminium hydroxide) bind bile acids in vitro. They could therefore have a similar effect in vivo and may interfere with the absorption of Ursofalk.

Drugs which increase cholesterol elimination in bile, such as oestrogenic hormones, oestrogen-rich contraceptive agents and certain blood cholesterol lowering agents, such as Clofibrate, should not be taken with Ursofalk.

UDCA may increase the absorption of cyclosporin in transplantation patients.

Ursofalk should not be used in pregnancy. When treating women of childbearing potential, non-hormonal or low oestrogen oral contraceptive measures are recommended.

Ursofalk is not expected to affect ability to drive and use machines.

Diarrhoea may occur rarely.

Serious adverse effects are unlikely to occur in overdosage. However, liver function should be monitored. If necessary, ion-exchange resins may be used to bind bile acids in the intestines.

UDCA is a bile acid which effects a reduction in cholesterol in biliary fluid primarily by dispersing the cholesterol and forming a liquid-crystal phase.

Ursodeoxycholic acid occurs naturally in the body. When given orally it is rapidly and completely absorbed. It is 96-98% bound to plasma proteins and efficiently extracted by the liver and excreted in the bile as glycine and taurine conjugates. In the intestine some of the conjugates are deconjugated and reabsorbed. The conjugates may also be dehydroxylated to lithocholic acid, part of which is absorbed, sulphated by the liver and excreted via the biliary tract.

Not applicable.

Ursofalk contains the following excipients:

Maize starch, colloidal anhydrous silica, magnesium stearate, gelatin, titanium dioxide.

None known.

36 months.

None.

Clear PVC blister strips with aluminium foil backing packed in cardboard cartons. Available in cartons containing 60 capsules packaged in six blister strips of 10 capsules or 100 capsules packaged in 4 blister strips of 25 capsules.

None.

Dr Falk Pharma UK Ltd

Unit K

Bourne End Business Park

Cores End Road

Bourne End

Bucks

SL8 5AS

United Kingdom

PL 10341/0006

31^st December 2004