ursodiol (Rx)

Brand and Other Names:Actigall, Urso Forte
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsules (Actigall)

  • 300mg

tablets (Urso, Urso Forte)

  • 250mg
  • 500mg

Gallstone Dissolution (Actigall)

8-10 mg/kg/d PO divided q8-12hr PO; not to exceed 300 mg/dose  

Maintenance: 250 mg PO HS x6 months

Gallstone prevention (Actigall)

300 mg PO BID

Primary Biliary Cirrhosis (Urso, Urso Forte)

13-15 mg/kg/d PO divided q6-12hr with food  

Cystic Fibrosis Liver Disease (Orphan)

Orphan designation for treatment of cystic fibrosis liver disease

Sponsor

  • Asklepion Pharmaceuticals, LLC; 5200 Maryland Way; Brentwood, TN 37027

Niemann-Pick Disease (Orphan)

Orphan designation for treatment of Niemann-Pick disease type C

Sponsor

  • IntraBio Inc; 270 Devon Road; Tenafly, New Jersey 07670

Dosage Forms & Strengths

capsules

  • 300mg

tablets

  • 250mg
  • 500mg

Biliary Atresia (Off-Label)

Post-Kasai procedure: 10-20 mg/kg/day PO divided q8-12hr  

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Interactions

Interaction Checker

and ursodiol

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 

            Contraindicated (0)

              Serious - Use Alternative (0)

                Monitor Closely (7)

                • aluminum hydroxide

                  aluminum hydroxide decreases effects of ursodiol by pharmacodynamic antagonism. Use Caution/Monitor.

                • calcium carbonate

                  calcium carbonate decreases effects of ursodiol by pharmacodynamic antagonism. Use Caution/Monitor.

                • crofelemer

                  crofelemer increases levels of ursodiol by Other (see comment). Use Caution/Monitor. Comment: Crofelemer has the potential to inhibit transporters MRP2 and OATP1A2 at concentrations expected in the gut; unlikely to inhibit systemically because minimally absorbed.

                • eluxadoline

                  eluxadoline increases levels of ursodiol by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 substrates.

                • ethinylestradiol

                  ethinylestradiol decreases effects of ursodiol by pharmacodynamic antagonism. Use Caution/Monitor.

                • sodium bicarbonate

                  sodium bicarbonate decreases effects of ursodiol by pharmacodynamic antagonism. Use Caution/Monitor.

                • sodium citrate/citric acid

                  sodium citrate/citric acid decreases effects of ursodiol by pharmacodynamic antagonism. Use Caution/Monitor.

                Minor (4)

                • cholestyramine

                  cholestyramine decreases effects of ursodiol by pharmacodynamic antagonism. Minor/Significance Unknown.

                • colesevelam

                  colesevelam decreases effects of ursodiol by pharmacodynamic antagonism. Minor/Significance Unknown.

                • colestipol

                  colestipol decreases effects of ursodiol by pharmacodynamic antagonism. Minor/Significance Unknown.

                • mestranol

                  mestranol decreases effects of ursodiol by pharmacodynamic antagonism. Minor/Significance Unknown.

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                Adverse Effects

                >10%

                Headache

                Dizziness

                Diarrhea

                Dyspepsia

                Nausea/vomiting

                Back pain

                Upper respiratory tract infection

                1-10%

                Alopecia

                Rash

                Hyperglycemia

                Flatulence

                Peptic ulcer

                Urinary tract infection

                Leukopenia

                Thrombocytopenia

                Cholecystitis

                >1%

                Fatigue

                Abdominal pain

                Thrombocytopenia

                Pruritus

                Angioedema

                Peripheral edema

                Biliary pain

                Postmarketing Reports

                Hepatobiliary disorders: Jaundice (or aggravation of pre-existing jaundice)

                Abnormal laboratory tests: Increased ALT, AST, alkaline phosphatase, bilirubin, gamma-GT

                Gastrointestinal disorders: Abdominal discomfort, enteroliths (bezoars), constipation

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                Warnings

                Contraindications

                Hypersensitivity

                Gallstone complication requiring surgery

                Known hepatocyte or bile ductal abnormalities, inflammatory bowel disease

                Calcified gallstones, bile acid allergy, chronic hepatic disease

                Billiary gastrointestinal fistula

                Patients requiring cholecystectomy

                Cautions

                Only use in radiolucent, non calcified, high cholesterol content gallstone

                Use caution in chronic liver disease

                In nonvisualizing gallbladders use caution and discontinue therapy if gallbladder nonvisualization occurs during treatment

                Liver function tests (gamma-GT, alkaline phosphatase, AST, ALT) and bilirubin levels should be monitored q3mo x3 months after start of therapy, and q6mo thereafter; consider treatment discontinuation if parameters increase to a level considered clinically significant in patients with history of stable liver function test levels

                Patients with variceal bleeding, hepatic encephalopathy, ascites or in need of an urgent liver transplant, should receive appropriate specific treatment

                Gallbladder stone dissolution may take several months of therapy and complete dissolution may not occur; reocurrence of stones may happen within 5 years in up to 50% of patients receiving therapy

                Enteroliths in patients with risk for intestinal stenosis or stasis

                • There are rare postmarketing reports of URSO-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 (eg, surgical enteroanastomoses, Crohn's disease); if a patient presents with obstructive gastrointestinal symptoms, hold URSO until a clinical evaluation conducted
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                Pregnancy & Lactation

                Pregnancy

                Available published data on use of ursodiol in pregnant women derived from randomized controlled trials, observational studies, and case series collected over several decades have not identified a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes; most reported exposures to ursodiol occurred in second and third trimester of pregnancy

                Animal data

                • In animal reproduction studies, ursodiol had no adverse effects on embryo-fetal development when administered at doses greater than human therapeutic doses

                Lactation

                Ursodiol is naturally present in human milk; there are no reports of adverse effects of ursodiol on breastfed child, but reports are extremely limited; there are no data on effects of ursodiol on milk production; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed child from drug or from underlying maternal condition

                Pregnancy Categories

                A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

                B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

                C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

                D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

                X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

                NA: Information not available.

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                Pharmacology

                Mechanism of Action

                Naturally-occurring bile acid; reduces cholesterol secretion from the liver; reduces the fractional reabsorption of cholesterol by the intestines.

                Absorption

                Bioavailability: 90%

                Onset: Initial response for gallstone dissolution is 3-6 months

                Distribution

                Protein Bound: 70%

                Metabolism

                Taken up rapidly by the liver, conjugated with glycine or taurine, and excreted in the bile

                Nonabsorbed ursodiol passes into the colon where it is 7-dehydroxylated to lithocholic acid (an intermediary compound, sometimes formed, is called chenodiol); chenodiol is then dehydroxylated to lithocholic acid

                Metabolites: Glyco-ursodeoxycholic acid, tauro-ursodeoxycholic acid, 7-keto-lithocholic acid (inactive); lithocholic acid (inactive) is formed from the 7-hydroxylation of ursodiol and chenodiol; a small portion is metabolized to sulfated lithocholic acid conjugates which are excreted in bile & eliminated in feces

                Elimination

                Excretion: Mainly in feces

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                Images

                BRAND FORM. UNIT PRICE PILL IMAGE
                ursodiol oral
                -
                300 mg capsule
                ursodiol oral
                -
                250 mg tablet
                ursodiol oral
                -
                500 mg tablet
                ursodiol oral
                -
                250 mg tablet
                ursodiol oral
                -
                500 mg tablet
                ursodiol oral
                -
                300 mg capsule
                ursodiol oral
                -
                300 mg capsule
                ursodiol oral
                -
                500 mg tablet
                ursodiol oral
                -
                500 mg tablet
                ursodiol oral
                -
                300 mg capsule
                ursodiol oral
                -
                250 mg tablet
                ursodiol oral
                -
                250 mg tablet
                ursodiol oral
                -
                300 mg capsule
                ursodiol oral
                -
                500 mg tablet
                ursodiol oral
                -
                250 mg tablet
                ursodiol oral
                -
                400 mg capsule
                ursodiol oral
                -
                200 mg capsule
                ursodiol oral
                -
                250 mg tablet
                ursodiol oral
                -
                300 mg capsule
                Reltone oral
                -
                400 mg capsule
                Reltone oral
                -
                200 mg capsule
                URSO 250 oral
                -
                250 mg tablet
                URSO Forte oral
                -
                500 mg tablet

                Copyright © 2010 First DataBank, Inc.

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                Patient Handout

                A Patient Handout is not currently available for this monograph.
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                Formulary

                FormularyPatient Discounts

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                The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                Tier Description
                1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                NC NOT COVERED – Drugs that are not covered by the plan.
                Code Definition
                PA Prior Authorization
                Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                QL Quantity Limits
                Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
                ST Step Therapy
                Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
                OR Other Restrictions
                Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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                Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.