Ursocol 300

Ursocol 300 is a bile acid which is physiologically synthesized in the human liver and is also formed by bacteria in the large intestine. It is present in human bile making up 1.4-4% of the biliary bile acids. Ursocol 300 is an epimer of chenodeoxycholic acid; it differs from this bile acid only in the configuration of the hydroxyl group in the C7-position.

Ursocol 300 250® and Ursocol 300 Forte® (Ursodiol) tablets are indicated for the treatment of patients with primary biliary cirrhosis (PBC).

Treating and preventing gallstones. It may also be used for other conditions as determined by your doctor.

Ursocol 300 is a bile acid naturally found in the body. It works by dissolving the cholesterol that makes gallstones and inhibiting production of cholesterol in the liver and absorption in the intestines, which helps to decrease the formation of gallstones. It can also reduce the amount of other bile acids that can be harmful to liver cells when levels are elevated.

General Dosing Information

The recommended adult dosage for Ursocol 300 250® and Ursocol 300 Forte® in the treatment of PBC is 13-15 mg/kg/day administered in two to four divided doses with food. Dosing regimen should be adjusted according to each patient's need at the discretion of the physician.

Liver Function Tests

Liver function tests (γ-GT, alkaline phosphatase, AST, ALT) and bilirubin levels should be monitored every month for three months after start of therapy, and every six months thereafter.

Scoring the Ursocol 300 Forte Tablet

The Ursocol 300 Forte scored tablet can be broken in halves to provide recommended dosage.

To break Ursocol 300 Forte scored tablet easily, place the tablet on a flat surface with the scored section on top. Hold the tablet with your thumbs placed close to the scored part of the tablet (groove). Then apply gentle pressure and snap the tablet segments apart (segments breaking incorrectly should not be used). The segments should be washed down unchewed, with water, keeping the segments in the mouth can reveal a bitter taste. Due to the bitter taste, segments should be stored separately from whole tablets..

How supplied

Dosage Forms And Strengths

• Ursocol 300 250: 250 mg tablet
• Ursocol 300 Forte: 500 mg scored tablet

Storage And Handling

Ursocol 300 250

Each Ursocol 300 250 elliptical, biconvex, film-coated tablet, white, engraved with "URS785", contains 250 mg of ursodiol. Available in bottles of 100 tablets (NDC 58914-785-10).

Ursocol 300 Forte

Each Ursocol 300 Forte elliptical, biconvex, scored, film-coated tablet, white, engraved with "URS790", contains 500 mg of ursodiol. Available in bottles of 100 tablets (NDC 58914-790-10). Store at 20°C to 25°C (68°F to 77°F). Dispense in a tight container.

Half-tablets (scored Ursocol 300 Forte 500 mg tablets broken in half) maintain acceptable quality for up to 28 days when stored in the current packaging (bottles) at 20°C to 25°C (68°F to 77°F). Due to the bitter taste, the halved segments should be stored separately from the whole tablets.

Manufactured in Canada for: Aptalis Pharma US, Inc. 100 Somerset Corporate Boulevard Bridgewater, NJ 08807, USA. Revised: 6/2013

See also:
What is the most important information I should know about Ursocol 300?

Hypersensitivity to Ursocol 300 or to any of the excipients of Ursocol 300.

Patients with complete obstruction of biliary tract (choleretic actions may aggravate the symptoms), fulminant hepatitis, radiopaque calcifying cholelith, nonfunctioning cholecyst or acute cholecystitis, renal disease, gastric ulcers (acute gastroduodenal ulcers), colitis or enteritis eg, Crohn's disease.

Use in pregnancy: Do not administer to pregnant women or women suspected of being pregnant.

Use in children: Do not administer to pediatric patients.

Use Ursocol 300 as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Take Ursocol 300 by mouth with food or milk.
• Do not take an antacid that has aluminum in it or a bile acid sequestrant (eg, cholestyramine, colestipol) within 1 hour before or 2 hours after you take Ursocol 300.
• If you miss a dose of Ursocol 300, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.

Ask your health care provider any questions you may have about how to use Ursocol 300.

Ursodiol is a bile acid used to dissolve gallstones in patients who do not want surgery or cannot have surgery to remove gallstones. Ursodiol is also used to prevent the formation of gallstones in overweight patients who are undergoing rapid weight loss.

See also:
What other drugs will affect Ursocol 300?

Ursocol 300 should not be administered concomitantly with cholestyramine, colestipol or antacids containing aluminum hydroxide and/or smectite (aluminum oxide), because these preparations bind Ursocol 300 in the intestine and thereby inhibits its absorption and efficacy. Should the use of a preparation containing one of these active ingredients concomitantly be necessary, it must be taken at least 2 hrs before or after Ursocol 300.

Ursocol 300 can increase the absorption of ciclosporin from the intestine. In patients receiving ciclosporin treatment, blood concentrations of this substance should therefore be checked by physician and the ciclosporin dose adjusted if necessary.

In isolated cases, Ursocol 300 can reduce the absorption of ciprofloxacin.

Film-Coated Tablet: Ursocol 300 has been shown to reduce peak plasma concentrations (C_max) and area under the curve (AUC) 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 Ursocol 300 to induce cytochrome P450 (CYP450) 3A enzymes. Controlled clinical studies have shown, however, that Ursocol 300 does not have a relevant inductive effect on CYP450 3A enzymes.

Estrogenic hormones and blood cholesterol-lowering agents eg, clofibrate may increase biliary lithiasis, which is a counter-effect to Ursocol 300 used for dissolution of gallstones.

See also:
What are the possible side effects of Ursocol 300?

Applies to ursodiol: oral capsule, oral tablet

As well as its needed effects, ursodiol (the active ingredient contained in Ursocol 300) may cause unwanted side effects that require medical attention.

Major Side Effects

If any of the following side effects occur while taking ursodiol, check with your doctor immediately:

More common:

• Bladder pain
• bloody or cloudy urine
• difficult, burning, or painful urination
• dizziness
• fast heartbeat
• frequent urge to urinate
• indigestion
• lower back or side pain
• severe nausea
• skin rash or itching over the entire body
• stomach pain
• vomiting
• weakness

• Black, tarry stools
• chest pain
• chills or fever
• cough
• pinpoint red spots on the skin
• severe or continuing stomach pain
• sore throat or swollen glands
• sores, ulcers, or white spots on the lips or in the mouth
• unusual bleeding or bruising
• unusual tiredness or weakness

• Clay-colored stools
• dark urine
• difficulty with swallowing
• headache
• hives or welts
• hoarseness
• large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs
• loss of appetite
• nausea
• redness of the skin
• slow or irregular breathing
• tightness in the chest
• unpleasant breath odor
• yellow eyes or skin

Minor Side Effects

Some ursodiol side effects may not need any medical attention. As your body gets used to the medicine these side effects may disappear. Your health care professional may be able to help you prevent or reduce these side effects, but do check with them if any of the following side effects continue, or if you are concerned about them:

More common:

• Back pain
• body aches or pain
• congestion
• constipation
• general feeling of discomfort or illness
• heartburn
• loss of voice
• muscle aches
• muscle or bone pain
• pain, swelling, or redness in the joints
• runny nose
• sweating
• trouble sleeping

• Diarrhea

• Worsening psoriasis

• Acid or sour stomach
• belching bloating or swelling of face, arms, hands, lower legs, or feet
• difficulty with moving
• rapid weight gain
• stomach discomfort or upset
• tingling of the hands or feet
• unusual weight gain or loss