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

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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 q3months x3 months after start of therapy, and q6months 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

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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
                -
                300 mg capsule
                ursodiol oral
                -
                300 mg capsule
                ursodiol oral
                -
                300 mg capsule
                ursodiol oral
                -
                250 mg tablet
                ursodiol oral
                -
                250 mg tablet
                ursodiol oral
                -
                250 mg tablet
                ursodiol oral
                -
                250 mg tablet
                ursodiol oral
                -
                500 mg tablet
                ursodiol oral
                -
                500 mg tablet
                ursodiol oral
                -
                300 mg capsule
                ursodiol oral
                -
                500 mg tablet
                ursodiol oral
                -
                250 mg tablet
                ursodiol oral
                -
                500 mg tablet
                ursodiol oral
                -
                300 mg capsule
                ursodiol oral
                -
                500 mg tablet
                ursodiol oral
                -
                250 mg tablet
                ursodiol oral
                -
                250 mg tablet
                ursodiol oral
                -
                400 mg capsule
                ursodiol oral
                -
                200 mg capsule
                URSO 250 oral
                -
                250 mg tablet
                URSO Forte oral
                -
                500 mg tablet
                Reltone oral
                -
                400 mg capsule
                Reltone oral
                -
                200 mg capsule

                Copyright © 2010 First DataBank, Inc.

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                Patient Handout

                Patient Education
                ursodiol oral

                URSODIOL - ORAL

                (UR-soe-DYE-ol)

                COMMON BRAND NAME(S): Actigall, Urso

                USES: Ursodiol is used to dissolve certain types of gallstones, to prevent gallstones from forming in obese patients who are losing weight rapidly, and to treat a certain type of liver disease (primary biliary cholangitis). Ursodiol is a bile acid.

                HOW TO USE: Take this medication exactly as directed by your doctor.Dosage is based on your medical condition and response to therapy.Do not increase your dose or take this medication more often without your doctor's approval. Your condition will not improve any faster, and the risk of serious side effects may be increased.Use this medication regularly to get the most benefit from it. To help you remember, take it at the same times each day.

                SIDE EFFECTS: Stomach upset, nausea, diarrhea, dizziness, back pain, hair loss, or cough may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if any of these unlikely but serious side effects occur: weakness, swelling of the ankles/feet, increased thirst/urination, signs of infection (e.g., fever, persistent sore throat), easy bleeding/bruising.A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

                PRECAUTIONS: Before taking ursodiol, tell your doctor or pharmacist if you are allergic to it; or to other bile acids; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: certain gallbladder/bile duct problems (e.g., acute cholecystitis, cholangitis, biliary obstruction, gallstone pancreatitis, biliary-gastrointestinal fistula).Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease (e.g., ascites, variceal bleeding, hepatic encephalopathy).This drug may make you dizzy. Alcohol or marijuana (cannabis) can make you more dizzy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.This medication passes into breast milk. Consult your doctor before breast-feeding.

                DRUG INTERACTIONS: Your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor or pharmacist first.Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use, especially of: aluminum-containing antacids, birth control pills, cholesterol medications (e.g., cholestyramine, clofibrate, colestipol), estrogen.This document does not contain all possible interactions. Before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

                OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: severe diarrhea.

                NOTES: Do not share this medication with others.Laboratory and/or medical tests (e.g., liver function tests, bilirubin level) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

                MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

                STORAGE: Store at room temperature away from light and moisture. Different brands/strengths of this medication may have different storage requirements. Read the package labeling or ask your pharmacist for the storage requirements for the product you are using. Do not store in the bathroom. Keep all medicines away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

                Information last revised August 2021. Copyright(c) 2021 First Databank, Inc.

                IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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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.