Data from FDA - Curated by Toby Galbraith - Last updated 09 September 2017

Indication(s)

1 INDICATIONS AND USAGE URSO 250® and URSO Forte® (ursodiol) tablets are indicated for the treatment of patients with primary biliary cirrhosis (PBC). URSO 250 and URSO Forte (ursodiol) tablets are bile acids indicated for the treatment of patients with primary biliary cirrhosis (1)

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Advisory information

contraindications
4 CONTRAINDICATIONS Patients with complete biliary obstruction and known hypersensitivity or intolerance to ursodiol or any of the components of the formulation. Patients with complete biliary obstruction and known hypersensitivity or intolerance to ursodiol or any of the components of the formulation (4)
Adverse reactions
6 ADVERSE REACTIONS Most common adverse reactions reported with the use of ursodiol during worldwide postmarketing and clinical experience (≥1%) are, in alphabetical order: abdominal discomfort, abdominal pain, alopecia, diarrhea, nausea, pruritus, and rash (6) To report SUSPECTED ADVERSE REACTIONS, contact Allergan at 1-800-678-1605 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Studies Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. The following table summarizes the adverse reactions observed in two placebo-controlled clinical trials. ADVERSE REACTIONS VISIT AT 12 MONTHS VISIT AT 24 MONTHS UDCA n (%) Placebo n (%) UDCA n (%) Placebo n (%) Diarrhea --- --- 1 (1.32) --- Elevated creatinine --- --- 1 (1.32) --- Elevated blood glucose 1 (1.18) --- 1 (1.32) --- Leukopenia --- --- 2 (2.63) --- Peptic ulcer --- --- 1 (1.32) --- Skin rash --- --- 2 (2.63) --- Thrombocytopenia --- --- 1 (1.32) --- Note: Those adverse reactions occurring at the same or higher incidence in the placebo as in the UDCA group have been deleted from this table (this includes diarrhea and thrombocytopenia at 12 months, nausea/vomiting, fever and other toxicity). UDCA = Ursodeoxycholic acid = Ursodiol In a randomized, cross-over study in sixty PBC patients, seven patients (11.6%) reported nine adverse reactions: abdominal pain and asthenia (1 patient), nausea (3 patients), dyspepsia (2 patients) and anorexia and esophagitis (1 patient each). One patient on the twice a day regimen (total dose 1000 mg) withdrew due to nausea. All of these nine adverse reactions except esophagitis were observed with the twice a day regimen at a total daily dose of 1000 mg or greater. However, an adverse reaction may occur at any dose. 6.2 Postmarketing Experience The following adverse reactions, presented by system organ class in alphabetical order, have been identified during postapproval use of ursodiol. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Gastrointestinal disorders: abdominal discomfort, abdominal pain, constipation, diarrhea, dyspepsia, nausea, vomiting. General disorders and administration site conditions: malaise, peripheral edema, pyrexia. Hepatobiliary disorders: jaundice (or aggravation of pre-existing jaundice). Immune System Disorders: Drug hypersensitivity to include facial edema, urticaria, angioedema and laryngeal edema. Abnormal Laboratory Tests: ALT increased, AST increased, blood alkaline phosphatase increased, blood bilirubin increased, γ-GT increased, hepatic enzyme increased, liver function test abnormal, transaminases increased. Musculoskeletal and connective tissue disorders: myalgia. Nervous system disorders: dizziness, headache. Respiratory, thoracic and mediastinal disorders: cough. Skin and subcutaneous tissue disorder: alopecia, pruritus, rash.

Usage information

Dosing and administration
2 DOSAGE AND ADMINISTRATION Recommended adult dosage: 13-15 mg/kg/day administered in two to four divided doses with food (2.1) Scored URSO Forte tablet: scored tablet can be broken in halves to provide recommended dosage (2.2, 16.2) 2.1 General Dosing Information The recommended adult dosage for URSO 250® and URSO 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. 2.2 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 [ see Warnings and Precautions (5.1) ]. 2.3 Scoring the URSO Forte Tablet The URSO Forte scored tablet can be broken in halves to provide recommended dosage. To break URSO 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. [see How Supplied/Storage and Handling (16.2)].
Use in special populations
8 USE IN SPECIFIC POPULATIONS 8.1 Pregnancy Pregnancy Category B. Reproduction studies have been performed in pregnant rats at oral doses up to 22 times the recommended maximum human dose (based on body surface area) and in pregnant rabbits at oral doses up to 7 times the recommended maximum human dose (based on body surface area) and have revealed no evidence of impaired fertility or harm to the fetus due to ursodiol. There are no adequate or well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed. 8.3 Nursing Mothers It is not known whether ursodiol is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when URSO 250 and URSO Forte are administered to a nursing mother. 8.4 Pediatric Use The safety and effectiveness of URSO 250 and URSO Forte in pediatric patients have not been established.
Pregnancy and lactation
8.3 Nursing Mothers It is not known whether ursodiol is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when URSO 250 and URSO Forte are administered to a nursing mother.

Interactions

7 DRUG INTERACTIONS Bile Acid Sequestering Agents: May interfere with the action of URSO 250 and URSO Forte by reducing its absorption (7.1) Aluminum-based Antacids: May interfere with the action of URSO 250 and URSO Forte by reducing its absorption (7.2) Drugs that alter the metabolism of lipids or induce cholestasis may interfere with the action of URSO 250 and URSO Forte (7.3) 7.1 Bile Acid Sequestering Agents Bile acid sequestering agents such as cholestyramine and colestipol may interfere with the action of URSO 250 and URSO Forte by reducing its absorption. 7.2 Aluminum-based Antacids Aluminum-based antacids have been shown to adsorb bile acids in vitro and may be expected to interfere with URSO 250 and URSO Forte in the same manner as the bile acid sequestering agents. 7.3 Drugs Affecting Lipid Metabolism Estrogens, oral contraceptives, and clofibrate (and perhaps other lipid-lowering drugs) increase hepatic cholesterol secretion and encourage cholesterol gallstone formation and hence may counteract the effectiveness of URSO 250 and URSO Forte.

More information

Category Value
Authorisation number NDA020675
Agency product number 724L30Y2QR
Orphan designation No
Product NDC 58914-790,58914-785
Date Last Revised 28-02-2017
Type HUMAN PRESCRIPTION DRUG
RXCUI 858733
Marketing authorisation holder Allergan, Inc.