budesonide (Rx)

Brand and Other Names:Entocort EC, Uceris
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule, extended-release (Entocort EC)

  • 3mg

tablet, extended-release (Uceris)

  • 9mg

Ulcerative Colitis

Uceris only

Indicated for the induction of remission of active, mild-to-moderate ulcerative colitis

9 mg PO qAM for up to 8 weeks

Crohn Disease

Entocort EC only

Indicated for treatment of mild-to-moderate active Crohn disease involving the ileum and/or ascending colon

Induction

  • 9 mg PO qAM for up to 8 weeks; for recurring episodes of active disease, 8-week courses may be repeated
  • Once symptoms are controlled, may be tapered to 6 mg PO qAM for maintenance

Maintenance

  • 6 mg PO qAM for up to 3 months
  • If symptom control is maintained at 3 months, tapering to complete cessation may be attempted (recommended)

Dosage Modifications

Hepatic impairment

  • Mild: No dosage modification recommended
  • Moderate-to-severe: Consider discontinuing budesonide

Renal impairment

  • Not studied; intact budesonide is not renally excreted, but metabolites are renally excreted to a large extent; metabolites have negligible corticosteroid activity compared with budesonide

Immunoglobulin A Nephropathy (Orphan)

Orphan designation to slow progression of immunoglobulin A nephropathy, and therefore, delaying of onset of kidney failure in patients affected by this disease

Orphan sponsor

  • Pharmalink AB; Engelbrekts kyrkogata 7b; Stockholm, Sweden

Cholangitis (Orphan)

Orphan designation for treatment of primary biliary cholangitis

Orphan sponsor

  • Calliditas Therapeutics AB; 26B Wallingatan; Norrmalm,Sweden

Eosinophilic Esophagitis (Orphan)

Orphan designation for treatment of eosinophilic esophagitis

Orphan sponsor

  • Salix Pharmaceuticals, Inc., division of Valeant Pharmaceuticals North America; 400 Somerset Corporate Boulevard; Bridgewater, NJ 08807

Dosage Forms & Strengths

capsule, extended-release (Entocort EC)

  • 3mg

Crohn Disease

Entocort EC only

Indicated for mild-to-moderate active Crohn disease involving the ileum and/or the ascending colon in patients aged ≥8 years

<8 years: Safety and efficacy not established

≥8 years and weight >25 kg: 9 mg PO qAm for up to 8 weeks, followed by 6 mg qAM for 2 weeks

Ulcerative Colitis (Orphan)

Orphan designation (budesonide [Uceris]) for treatment ulcerative colitis in pediatric patients aged 0 through 16 years

Orphan sponsor

  • Santarus, Inc.; 3611 Valley Centre Drive, Suite 400; San Diego, CA 92130
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Interactions

Interaction Checker

and budesonide

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Headache (21%)

            Acne (<5-15%)

            Nausea (11%)

            Respiratory infection (11%)

            1-10%

            Back pain (7%)

            Dizziness (7%)

            Abdominal pain (6%)

            Dyspepsia (6%)

            Vomiting (6%)

            Fatigue (5%)

            Frequency Not Defined

            Adrenal suppression

            Amnesia

            Anaphylactic reactions

            Benign intracranial hypertension

            Diarrhea

            Facial edema

            Fever

            Flu syndrome

            GI irritation

            Hypokalemia

            Increased appetite

            Insomnia

            Migraine

            Nervousness

            Pharyngitis

            Rash

            Xerostomia

            Weight gain

            Postmarketing Reports

            Rectal bleeding

            Peripheral edema

            Muscle cramps/spasms

            Mood swings

            Increased blood pressure

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            Warnings

            Contraindications

            Documented hypersensitivity

            Cautions

            When used chronically, systemic effects (eg, hypercorticism, adrenal suppression) may occur; glucocorticosteroids can reduce the response of the hypothalamus-pituitary-adrenal (HPA) axis to stress; if patients are subject to surgery or other stress situations, supplement with a systemic glucocorticosteroid

            Caution in patients who are transferred from glucocorticosteroid treatment with higher systemic effects to those with lower systemic effects (eg, budesonide); monitor for symptoms of steroid withdrawal, including those of acute adrenal suppression or benign intracranial hypertension

            Drugs that suppress the immune system, including budesonide, may increase risk for infection; patients who have not had certain infections (eg, chicken pox, measles) can have more serious infections, including fatalities

            Reduced liver function affects the elimination of glucocorticosteroids; increased systemic availability of oral budesonide demonstrated with liver cirrhosis; consider discontinuing use in patients with moderate-to-severe liver disease

            Caution with hypertension, diabetes mellitus, osteoporosis, peptic ulcer, glaucoma or cataracts, or with other conditions where glucocorticosteroids may have unwanted effects

            Drug interaction overview

            • CYP3A4 inhibitors or inducers
              • Coadministration with potent CYP3A4 inhibitors may increase systemic exposure; oral ketoconazole (inhibits CYP3A4 in liver and intestine) caused an 8-fold increase of the systemic exposure to oral budesonide
              • If treatment with CYP3A4 inhibitors (eg, ketoconazole, itraconazole, ritonavir, indinavir, saquinavir, erythromycin) is indicated, consider discontinuing budesonide
              • Extensive intake of grapefruit juice (inhibits CYP3A4 activity predominantly in the intestine) increase oral budesonide systemic exposure ~2-fold; avoid coadministration
              • Conversely, CYP3A4 inducers may decrease budesonide systemic exposure
            • Drugs that inhibit gastric acid secretion
              • Uceris: Dissolution of the tablet coating is pH dependent; release properties and uptake of the compound may be altered when used after treatment with gastric acid reducing agents (eg, PPIs, H2-blockers, antacids)
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            Pregnancy & Lactation

            Pregnancy

            Limited published studies report in pregnant women; however, data insufficient to inform a drug-associated risk for major birth defects and miscarriage; there are clinical considerations; in animal reproduction studies with pregnant rats and rabbits, administration of subcutaneous budesonide during organogenesis at doses approximately 0.5 times or 0.05 times, respectively, the maximum recommended human dose, resulted in increased fetal loss, decreased pup weights, and skeletal abnormalities; maternal toxicity was observed in both rats and rabbits at these dose levels; based on animal data, advise pregnant women of potential risk to a fetus

            Some published epidemiological studies show an association of adverse pregnancy outcomes in women with Crohn disease, including preterm birth and low birth weight infants, during periods of increased disease activity (including increased stool frequency and abdominal pain); pregnant women with Crohn disease should be counseled regarding importance of controlling disease

            Hypoadrenalism may occur in infants born of mothers receiving corticosteroids during pregnancy; infants should be carefully observed for signs of hypoadrenalism, such as poor feeding, irritability, weakness, and vomiting, and managed accordingly

            Lactation

            Lactation studies conducted with oral budesonide, and no information is available on effects of drug on breastfed infant or effects of drug on milk production

            One published study reports that budesonide is present in human milk following maternal inhalation of budesonide; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed infant 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

            Anti-inflammatory corticosteroid; potent glucocorticoid activity but weak mineralocorticoid activity; controls rate of protein synthesis; decreases inflammation by suppressing migration of polymorphonuclear leukocytes (PMNs) and reducing capillary permeability; stabilizes cell and lysosomal membranes, increases surfactant synthesis, increases serum vitamin A concentration, and inhibits prostaglandin and proinflammatory cytokines; suppresses lymphocyte proliferation through direct cytolysis, inhibits mitosis, and breaks down granulocyte aggregates

            Absorption

            Bioavailability: Capsule, 9-21%

            Peak plasma time: Capsule, 5-10 hr

            Distribution

            Protein bound: 85-90%

            Vd: 2.2-3.9 L/kg

            Metabolism

            Extensive 1st-pass metabolism by CYP3A4 in liver

            Metabolites: 6-Beta-hydroxybudesonide, 16-alpha-hydroxyprednisolone (inactive)

            Elimination

            Half-life: 2-3.6 hr

            Excretion: Urine (60%), feces (minimal)

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            Administration

            Oral Administration

            May take with or without food

            Avoid consuming grapefruit juice for duration of treatment

            Uceris

            • Swallow tablet whole with water; do not chew, crush, or break

            Entocort EC

            • Swallow capsule whole; do not chew or crush
            • Unable to swallow capsule
              • If unable to swallow intact capsule, open capsule and empty granules onto 1 tablespoonful of applesauce
              • Mix and consume the entire contents within 30 minutes
              • Do not chew or crush
              • Follow with 8 ounces of water

            Storage

            Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F

            Keep container tightly closed

            Protect from light and moisture

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            Images

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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.
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            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.