Bile Acid

Ursodiol

Approved 14 Feb 2013OralTablet

The FDA lists this product in 31 strengths and forms.

Indications

Ursodiol tablets are indicated for the treatment of patients with primary biliary cholangitis (PBC). Ursodiol tablets are bile acids indicated for the treatment of patients with primary biliary cholangitis. ( 1 )

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 )

Warnings and precautions

Abnormal Liver Function Tests : Liver function tests (γ-GT, alkaline phosphatase, AST, ALT) and bilirubin level should be monitored. Treatment discontinuation should be considered if parameters increase to a level considered clinically significant in patients with stable historical liver function test levels. Caution should be exercised to maintain patients’ bile flow. (5.1) Enteroliths in Patients with Risk for Intestinal Stenosis or Stasis: Monitor for obstructive gastrointestinal symptoms; if symptoms occur, hold ursodiol until a clinical evaluation has been conducted.

( 5.2 )

5.1Abnormal Liver Function Tests

Liver function tests ( y -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. This monitoring will allow the early detection of a possible deterioration of the hepatic function. Treatment discontinuation should be considered if the above parameters increase to a level considered clinically significant in patients with stable historical liver function test levels.

Caution has to be exercised to maintain the bile flow of the patients taking ursodiol.

5.2Enteroliths in Patients with Risk for Intestinal Stenosis or Stasis

There have been rare postmarketing reports of Ursodiol tablets-treated patients who developed enteroliths (bezoars) resulting in obstructive symptoms that required surgical intervention. These patients had medical conditions that predisposed them to intestinal stenosis or stasis (e.g., surgical enteroanastomoses, Crohn's disease). If a patient presents with obstructive gastrointestinal symptoms, hold Ursodiol tablets until a clinical evaluation has been conducted.

At a glance

Brand name: Ursodiol
Pharmacologic class: Bile Acid
Route: Oral
Dosage form: Tablet
Applicant: PH Health
Status: Prescription
FDA approval: 14 Feb 2013
Application: ANDA202540-002

Warnings and precautions

( 5.2 )

5.1Abnormal Liver Function Tests

Caution has to be exercised to maintain the bile flow of the patients taking ursodiol.

5.2Enteroliths in Patients with Risk for Intestinal Stenosis or Stasis

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 Endo at 1-800-828-9393 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

6.1Clinical 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 1,000 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 1,000 mg or greater.

However, an adverse reaction may occur at any dose.

6.2Postmarketing Experience

The following adverse reactions, presented by system organ class in alphabetical order, have been identified during post approval 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, enteroliths (bezoars), 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.

Ursodiol

Indications

Contraindications

Warnings and precautions

5.1Abnormal Liver Function Tests

5.2Enteroliths in Patients with Risk for Intestinal Stenosis or Stasis

At a glance

Two medicines in one question?

Ursodiol

Indications

Contraindications

Warnings and precautions

5.1Abnormal Liver Function Tests

5.2Enteroliths in Patients with Risk for Intestinal Stenosis or Stasis

At a glance

Two medicines in one question?

Interactions

7.1Bile Acid Sequestering Agents

7.2Aluminum-based Antacids

7.3Drugs Affecting Lipid Metabolism

Pregnancy and breastfeeding

8.1Pregnancy Risk Summary

Adverse reactions

6.1Clinical Studies Experience

6.2Postmarketing Experience

Composition

Strengths and forms

Official product information