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Budesonide (Systemic)

Pronunciation

Pronunciation

(byoo DES oh nide)

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule Delayed Release Particles, Oral:

Entocort EC: 3 mg

Generic: 3 mg

Tablet Extended Release 24 Hour, Oral:

Uceris: 9 mg

Brand Names: U.S.

  • Entocort EC
  • Uceris

Pharmacologic Category

  • Corticosteroid, Systemic

Pharmacology

Controls the rate of protein synthesis; depresses the migration of polymorphonuclear leukocytes, fibroblasts; reverses capillary permeability and lysosomal stabilization at the cellular level to prevent or control inflammation. Has potent glucocorticoid activity and weak mineralocorticoid activity.

Distribution

Children 9 to 14 years: IV: 2.2 ± 0.4 L/kg

Adults: 2.2 to 3.9 L/kg

Metabolism

Hepatic via CYP3A4 to two metabolites: 16 alpha-hydroxyprednisolone and 6 beta-hydroxybudesonide; both are <1% as active as parent

Excretion

Urine (60%) and feces as metabolites

Time to Peak

Capsule: 0.5 to 10 hours; Tablet (extended release): 13.3 ± 5.9 hours

Half-Life Elimination

IV:

Children 9 to 14 years: 1.9 hours

Adults: 2 to 3.6 hours

Protein Binding

85% to 90%

Special Populations: Hepatic Function Impairment

Increased systemic exposure (≥2.5 fold) has been reported in moderate hepatic impairment.

Special Populations: Children

Plasma IV half-life is shorter than in adults.

Use: Labeled Indications

Crohn disease (capsules): Treatment of active Crohn disease (mild to moderate) involving the ileum and/or the ascending colon in patients 8 years and older; maintenance of clinical remission (for up to 3 months) of Crohn disease (mild to moderate) involving the ileum and/or the ascending colon in adults.

Ulcerative colitis (tablets): Induction of remission in patients with active ulcerative colitis (mild to moderate).

Contraindications

Hypersensitivity to budesonide or any component of the formulation.

Documentation of allergenic cross-reactivity for corticosteroids is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty.

Canadian labeling: Additional contraindications (not in US labeling): Active tuberculosis; systemic or local bacterial, fungal or viral infections; hypersensitivity to soya or peanut (Cortiment)

Dosing: Adult

Crohn disease (active): Oral: Capsule: 9 mg once daily in the morning for up to 8 weeks; recurring episodes may be treated with a repeat 8-week course of treatment.

Maintenance of remission: Following treatment of active disease (control of symptoms with Crohn Disease Activity Index [CDAI] <150), treatment may be continued at a dosage of 6 mg once daily for up to 3 months. If symptom control is maintained for 3 months, tapering of the dosage to complete cessation is recommended. Continued dosing beyond 3 months has not been demonstrated to result in substantial benefit.

Ulcerative colitis (active): Oral: Tablet: 9 mg once daily in the morning for up to 8 weeks

Eosinophilic esophagitis (off-label use): Oral: 2 mg/day as an oral budesonide viscous liquid/suspension. Dose may be divided into 2 doses. Avoid ingesting any solid or liquid food for 30 minutes after budesonide administration. (Dellon 2013; Dohil 2010; Liacouras 2011; Rubinstein 2014). See Extemporaneously Prepared field.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Crohn disease (active): Children ≥8 years and Adolescents ≤17 years (weighing >25 kg): Oral: Capsule: 9 mg once daily in the morning for up to 8 weeks, then 6 mg once daily for 2 weeks.

Eosinophilic esophagitis (off-label use):

Children ≥10 years of age or ≥5 ft in height: 2 mg/day as an oral budesonide viscous liquid/suspension. Dose may be divided into 2 doses. Avoid ingesting any solid or liquid food for 30 minutes after budesonide administration. (Dellon, 2013; Dohil, 2010; Liacouras, 2011; Rubinstein 2014).

Children <10 years or <5 ft in height: 1 mg/day as an oral budesonide viscous liquid/suspension. Avoid ingesting any solid or liquid food for 30 minutes after budesonide administration. (Dellon, 2013; Dohil, 2010; Liacouras, 2011; Rubinstein, 2014).

Note: See Extemporaneously Prepared field.

Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer’s labeling; use with caution.

Dosing: Hepatic Impairment

Oral capsule:

Mild hepatic impairment (Child-Pugh class A): No dosage adjustment necessary.

Moderate hepatic impairment (Child-Pugh class B): Consider reduced dosage to 3 mg once daily and monitor for hypercorticism.

Severe hepatic impairment (Child-Pugh class C): Avoid use.

Oral tablet:

Mild hepatic impairment: There are no specific dosage adjustments provided in the manufacturer’s labeling; use with caution.

Moderate to severe hepatic impairment: There are no specific dosage adjustments provided in the manufacturer's labeling (has not been studied); monitor for hypercorticism; consider discontinuing use.

Extemporaneously Prepared

Oral budesonide viscous liquid/suspension: Prepare immediately prior to ingestion from aqueous budesonide solution (1 mg per 2 mL) or nebulized solution (0.5 mg per 2 mL [Pulmicort Respules]) mixed to slurry consistency with 10 packets of Splenda or 2.5 cm3 of Neocate Nutra per milligram of budesonide. (Dellon 2013; Dohil 2010; Rubinstein 2014)

Administration

Oral: Administer in the morning without regard to meals. Swallow whole; do not crush, chew, or break.

Dietary Considerations

Avoid grapefruit juice.

Storage

Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Protect from light and moisture.

Drug Interactions

Aldesleukin: Corticosteroids may diminish the antineoplastic effect of Aldesleukin. Avoid combination

Antacids: May decrease the bioavailability of Corticosteroids (Oral). Management: Consider separating doses by 2 or more hours. Budesonide enteric coated tablets could dissolve prematurely if given with drugs that lower gastric acid, with unknown impact on budesonide therapeutic effects. Consider therapy modification

BCG (Intravesical): Immunosuppressants may diminish the therapeutic effect of BCG (Intravesical). Avoid combination

Bile Acid Sequestrants: May decrease the absorption of Corticosteroids (Oral). Monitor therapy

Coccidioides immitis Skin Test: Immunosuppressants may diminish the diagnostic effect of Coccidioides immitis Skin Test. Monitor therapy

Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Avoid combination

Corticorelin: Corticosteroids may diminish the therapeutic effect of Corticorelin. Specifically, the plasma ACTH response to corticorelin may be blunted by recent or current corticosteroid therapy. Monitor therapy

CYP3A4 Inhibitors (Moderate): May increase the serum concentration of Budesonide (Systemic). Avoid combination

CYP3A4 Inhibitors (Strong): May increase the serum concentration of Budesonide (Systemic). Avoid combination

Dasatinib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Deferasirox: Corticosteroids may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased. Monitor therapy

Denosumab: May enhance the adverse/toxic effect of Immunosuppressants. Specifically, the risk for serious infections may be increased. Monitor therapy

Echinacea: May diminish the therapeutic effect of Immunosuppressants. Consider therapy modification

Fingolimod: Immunosuppressants may enhance the immunosuppressive effect of Fingolimod. Management: Avoid the concomitant use of fingolimod and other immunosuppressants when possible. If combined, monitor patients closely for additive immunosuppressant effects (eg, infections). Consider therapy modification

Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates. Avoid combination

Grapefruit Juice: May increase the serum concentration of Budesonide (Systemic). Avoid combination

Hyaluronidase: Corticosteroids may diminish the therapeutic effect of Hyaluronidase. Management: Patients receiving corticosteroids (particularly at larger doses) may not experience the desired clinical response to standard doses of hyaluronidase. Larger doses of hyaluronidase may be required. Consider therapy modification

Idelalisib: May increase the serum concentration of CYP3A4 Substrates. Avoid combination

Ivacaftor: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Leflunomide: Immunosuppressants may enhance the adverse/toxic effect of Leflunomide. Specifically, the risk for hematologic toxicity such as pancytopenia, agranulocytosis, and/or thrombocytopenia may be increased. Management: Consider not using a leflunomide loading dose in patients receiving other immunosuppressants. Patients receiving both leflunomide and another immunosuppressant should be monitored for bone marrow suppression at least monthly. Consider therapy modification

Luliconazole: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Natalizumab: Immunosuppressants may enhance the adverse/toxic effect of Natalizumab. Specifically, the risk of concurrent infection may be increased. Avoid combination

Nivolumab: Immunosuppressants may diminish the therapeutic effect of Nivolumab. Consider therapy modification

Palbociclib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Pimecrolimus: May enhance the adverse/toxic effect of Immunosuppressants. Avoid combination

Roflumilast: May enhance the immunosuppressive effect of Immunosuppressants. Consider therapy modification

Simeprevir: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Sipuleucel-T: Immunosuppressants may diminish the therapeutic effect of Sipuleucel-T. Monitor therapy

Stiripentol: May increase the serum concentration of CYP3A4 Substrates. Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. Consider therapy modification

Tacrolimus (Topical): May enhance the adverse/toxic effect of Immunosuppressants. Avoid combination

Tofacitinib: Immunosuppressants may enhance the immunosuppressive effect of Tofacitinib. Management: Concurrent use with antirheumatic doses of methotrexate or nonbiologic disease modifying antirheumatic drugs (DMARDs) is permitted, and this warning seems particularly focused on more potent immunosuppressants. Avoid combination

Trastuzumab: May enhance the neutropenic effect of Immunosuppressants. Monitor therapy

Vaccines (Inactivated): Immunosuppressants may diminish the therapeutic effect of Vaccines (Inactivated). Management: Vaccine efficacy may be reduced. Complete all age-appropriate vaccinations at least 2 weeks prior to starting an immunosuppressant. If vaccinated during immunosuppressant therapy, revaccinate at least 3 months after immunosuppressant discontinuation. Consider therapy modification

Adverse Reactions

>10%:

Central nervous system: Headache (15% to 21%)

Dermatologic: Acne vulgaris (15%)

Endocrine & metabolic: Decreased cortisol (foam 17%; tablets 2% to 4%), bruise (15%), moon face (11%)

Gastrointestinal: Nausea (2% to 11%)

Respiratory: Respiratory tract infection (11%)

1% to 10%:

Cardiovascular: Chest pain (<5%), edema (<5%), facial edema (<5%), flushing (<5%), hypertension (<5%), palpitations (<5%), tachycardia (<5%)

Central nervous system: Dizziness (<5% to 7%), fatigue (3% to 5%), agitation (<5%), amnesia (<5%), confusion (<5%), drowsiness (<5%), insomnia (<5%), malaise (<5%), nervousness (<5%), paresthesia (<5%), sleep disorder (<5%), vertigo (<5%)

Dermatologic: Alopecia (<5%), dermatitis (<5%), dermatological disease (<5%), diaphoresis (<5%), eczema (<5%)

Endocrine & metabolic: Hirsutism (≤5%), hypokalemia (1% to <5%), intermenstrual bleeding (<5%), menstrual disease (<5%), weight gain (<5%), adrenocortical insufficiency (foam 4%; capsules >1%), redistribution of body fat (1%)

Gastrointestinal: Diarrhea (10%), dyspepsia (6%), anal disease (<5%), enteritis (<5%), epigastric pain (<5%), exacerbation of Crohn's disease (<5%), gastrointestinal fistula (<5%), glossitis (<5%), hemorrhoids (<5%), increased appetite (<5%), intestinal obstruction (<5%), oral candidiasis (<5%), upper abdominal pain (3% to 4%), flatulence (3%), abdominal distention (2%), constipation (2%)

Genitourinary: Urinary tract infection (2% to <5%), dysuria (<5%), nocturia (<5%), urinary frequency (<5%), hematuria (≥1%), pyuria (≥1%)

Hematologic & oncologic: C-reactive protein increased (1% to <5%), leukocytosis (1% to <5%), purpura (<5%), abnormal neutrophils (≥1%), anemia (≥1%), increased erythrocyte sedimentation rate (≥1%)

Hepatic: Increased serum alkaline phosphatase (≥1%)

Hypersensitivity: Tongue edema (<5%)

Infection: Viral infection (6%), abscess (<5%)

Neuromuscular & skeletal: Ankle edema (7%), arthralgia (5%), arthritis (≤5%), hyperkinesia (<5%), muscle cramps (<5%), myalgia (<5%), tremor (<5%), weakness (<5%)

Ophthalmic: Eye disease (<5%), visual disturbance (<5%)

Otic: Otic infection (<5%)

Respiratory: Sinusitis (8%), bronchitis (<5%), dyspnea (<5%), flu-like symptoms (<5%), pharyngeal disease (<5%), rhinitis (<5%)

Miscellaneous: Fever (<5%)

<1% (Limited to important or life-threatening): Allergic dermatitis, anaphylaxis, emotional lability, hyperglycemia, maculopapular rash, pancreatitis, peripheral edema, pruritus, pseudotumor cerebri, rectal bleeding

Warnings/Precautions

Concerns related to adverse effects:

• Adrenal suppression: May cause hypercorticism or suppression of hypothalamic-pituitary-adrenal (HPA) axis, particularly in younger children or in patients receiving high doses for prolonged periods. HPA axis suppression may lead to adrenal crisis. Withdrawal and discontinuation of a corticosteroid should be done slowly and carefully. Particular care is required when patients are transferred from systemic corticosteroids to inhaled products or corticosteroids with lower systemic effect due to possible adrenal insufficiency or withdrawal from steroids, including an increase in allergic symptoms. Patients receiving >20 mg per day of prednisone (or equivalent) may be most susceptible. Fatalities have occurred due to adrenal insufficiency in asthmatic patients during and after transfer from systemic corticosteroids to aerosol steroids; aerosol steroids do not provide the systemic steroid needed to treat patients having trauma, surgery, or infections.

• Anaphylactoid reactions: Rare cases of anaphylactoid reactions have been observed in patients receiving corticosteroids.

• Immunosuppression: Prolonged use of corticosteroids may increase the incidence of secondary infection, mask acute infection (including fungal infections), prolong or exacerbate viral infections, or limit response to killed or inactivated vaccines. Exposure to chickenpox or measles should be avoided; corticosteroids should not be used to treat ocular herpes simplex. Corticosteroids should not be used for cerebral malaria, fungal infections, viral hepatitis. Close observation is required in patients with latent tuberculosis and/or TB reactivity; restrict use in active TB (only fulminating or disseminated TB in conjunction with antituberculosis treatment). Amebiasis should be ruled out in any patient with recent travel to tropic climates or unexplained diarrhea prior to initiation of corticosteroids. Use with extreme caution in patients with Strongyloides infections; hyperinfection, dissemination and fatalities have occurred.

• Kaposi sarcoma: Prolonged treatment with corticosteroids has been associated with the development of Kaposi sarcoma (case reports); if noted, discontinuation of therapy should be considered (Goedert 2002).

• Myopathy: Acute myopathy has been reported with high-dose corticosteroids, usually in patients with neuromuscular transmission disorders; may involve ocular and/or respiratory muscles; monitor creatine kinase; recovery may be delayed.

• Psychiatric disturbances: Corticosteroid use may cause psychiatric disturbances, including euphoria, insomnia, mood swings, personality changes, severe depression or psychotic manifestations. Preexisting psychiatric conditions may be exacerbated by corticosteroid use.

Disease-related concerns:

• Cardiovascular disease: Use with caution in patients with HF and/or hypertension; use has been associated with fluid retention, electrolyte disturbances, and hypertension. Use with caution following acute MI; corticosteroids have been associated with myocardial rupture.

• Diabetes: Use corticosteroids with caution in patients with diabetes mellitus; may alter glucose production/regulation leading to hyperglycemia.

• Gastrointestinal disease: Use with caution in patients with GI diseases (diverticulitis, fresh intestinal anastomoses, active or latent peptic ulcer, ulcerative colitis, abscess or other pyogenic infection) due to perforation risk.

• Hepatic impairment: Avoid use in patients with severe hepatic impairment (Child-Pugh class C). Consider reduced dosage in patients with moderate hepatic impairment (Child-Pugh Class B); monitor for hypercorticism. Long-term use of corticosteroids in patients with hepatic impairment, including cirrhosis, has been associated with fluid retention.

• Myasthenia gravis: Use with caution in patients with myasthenia gravis; exacerbation of symptoms has occurred especially during initial treatment with corticosteroids.

• Ocular disease: Use with caution in patients with cataracts and/or glaucoma; increased intraocular pressure, open-angle glaucoma, and cataracts have occurred with prolonged use. Consider routine eye exams in chronic users.

• Osteoporosis: Use with caution in patients with osteoporosis; high doses and/or long-term use of corticosteroids have been associated with increased bone loss and osteoporotic fractures.

• Renal impairment: Use with caution in patients with renal impairment; fluid retention may occur.

• Seizure disorders: Use corticosteroids with caution in patients with a history of seizure disorder; seizures have been reported with adrenal crisis.

• Thyroid disease: Changes in thyroid status may necessitate dosage adjustments; metabolic clearance of corticosteroids increases in hyperthyroid patients and decreases in hypothyroid ones.

Concurrent therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Dosage form specific issues:

• Polysorbate 80: Some dosage forms may contain polysorbate 80 (also known as Tweens). Hypersensitivity reactions, usually a delayed reaction, have been reported following exposure to pharmaceutical products containing polysorbate 80 in certain individuals (Isaksson 2002; Lucente 2000; Shelley 1995). Thrombocytopenia, ascites, pulmonary deterioration, and renal and hepatic failure have been reported in premature neonates after receiving parenteral products containing polysorbate 80 (Alade 1986; CDC 1984). See manufacturer’s labeling.

Monitoring Parameters

Serum glucose, electrolytes; blood pressure, weight, presence of infection; monitor IOP with therapy >6 weeks; bone mineral density; assess HPA axis suppression (eg, ACTH stimulation test, morning plasma cortisol test, urinary free cortisol test); growth in pediatric patients.

Pregnancy Risk Factor

C (tablet)

Pregnancy Considerations

Some studies have shown an association between first trimester systemic corticosteroid use and oral clefts (Park-Wyllie 2000; Pradat 2003). Systemic corticosteroids may also influence fetal growth (decreased birth weight); however, information is conflicting (Lunghi 2010). Hypoadrenalism may occur in newborns following maternal use of corticosteroids in pregnancy (monitor). When systemic corticosteroids are needed in pregnancy, it is generally recommended to use the lowest effective dose for the shortest duration of time, avoiding high doses during the first trimester (Leachman 2006; Lunghi 2010). Budesonide may be used for the induction of remission in pregnant women with inflammatory bowel disease (Habal 2012; Nguyen 2016).

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience nausea, insomnia, agitation, flatulence, constipation, bloating, or back pain. Have patient report immediately to prescriber signs of high blood sugar (confusion, fatigue, increased thirst, increased hunger, polyuria, flushing, fast breathing, or breath that smells like fruit), signs of skin changes (acne, stretch marks, slow healing, or hair growth), signs of bleeding (vomiting blood or vomit that looks like coffee grounds; coughing up blood; hematuria; black, red, or tarry stools; bleeding from the gums; abnormal vaginal bleeding; bruises without a reason or that get bigger; or any severe or persistent bleeding), signs of low potassium (muscle pain or weakness, muscle cramps, or an abnormal heartbeat); signs of infection; signs of adrenal gland problems (severe nausea, vomiting, severe dizziness, passing out, muscle weakness, severe fatigue, mood changes, lack of appetite, or weight loss), moon face, buffalo hump, severe loss of strength and energy, irritability, tremors, tachycardia, confusion, sweating a lot, dizziness, excessive weight gain, swelling of arms or legs, severe headache, abnormal heartbeat, angina, bone pain, joint pain, vision changes, mood changes, behavioral changes, depression, seizures, burning or numbness feeling, severe abdominal pain, or shortness of breath (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating, and advising patients.

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