Budesonide (Oral Inhalation)

• Pulmicort
• Pulmicort Flexhaler

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 4 to 6 years: 3 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

Clearance: Children 4 to 6 years: 0.5 L/minute (~50% greater than healthy adults after weight adjustment); Adults: 0.9 to 1.8 L/minute

Refer to adult dosing.

Asthma: Titrate to lowest effective dose once patient is stable.

Oral inhalation:

Pulmicort Flexhaler: Children ≥6 years: Initial: 180 mcg twice daily (some patients may be initiated at 360 mcg twice daily); maximum: 360 mcg twice daily; Note: May increase dose after 1 to 2 weeks of therapy in patients who are not adequately controlled.

Pulmicort Turbuhaler [Canadian product]:

Children 6 to 11 years:

Initial (or during periods of severe asthma or when switching from oral corticosteroid therapy): 200 to 400 mcg daily in 2 divided doses

Maintenance: Individualized, lowest effective dose in 2 divided doses

Children ≥12 years: Refer to adult dosing.

Asthma guidelines:

National Asthma Education and Prevention Program guidelines (NAEPP 2007): Dry powder inhaler (refers to the Pulmicort Flexhaler available in US). Note: Administer in divided doses twice daily.

Children 5 to 11 years:

“Low” dose: 180 to 400 mcg/day

“Medium” dose: >400 to 800 mcg/day

“High” dose: >800 mcg/day

Children ≥12 years and Adolescents: Refer to adult dosing.

Global Initiative for Asthma guidelines (GINA 2016): Dry powder inhaler (refers to the Pulmicort Turbuhaler available in Canada):

Children 6 to 11 years:

“Low” dose: 100 to 200 mcg daily

“Medium” dose: >200 to 400 mcg daily

“High” dose: >400 mcg daily

Children ≥12 years and Adolescents: Refer to adult dosing.

Conversion: Conversion from oral systemic corticosteroid to orally inhaled corticosteroid: Initiation of oral inhalation therapy should begin in patients whose asthma is reasonably stabilized on oral corticosteroids (OCS). A gradual dose reduction of OCS should begin ~7 to 10 days after starting inhaled therapy. The manufacturer labeling recommends reducing prednisone dose by 2.5 mg/day (or equivalent of other OCS) on a weekly basis (patients using oral inhaler) or by ≤25% every 1 to 2 weeks (patients using respules). Note: When transitioning from systemic to inhaled corticosteroids, supplemental systemic corticosteroid therapy may be necessary during periods of stress or during severe asthma attacks.

Nebulization: Pulmicort Respules: Children 12 months to 8 years: Titrate to lowest effective dose once patient is stable; start at 0.25 mg/day or use as follows:

Previous therapy of bronchodilators alone: 0.5 mg/day administered as a single dose or divided twice daily (maximum daily dose: 0.5 mg)

Previous therapy of inhaled corticosteroids: 0.5 mg/day administered as a single dose or divided twice daily (maximum daily dose: 1 mg)

Previous therapy of oral corticosteroids: 1 mg/day administered as a single dose or divided twice daily (maximum daily dose: 1 mg)

Asthma guidelines:

National Asthma Education and Prevention Program guidelines (NAEPP 2007):

Children 0 to 4 years:

“Low” dose: 0.25 to 0.5 mg/day

“Medium” dose: >0.5 to 1 mg/day

“High” dose: >1 mg/day

Children 5 to 11 years:

“Low” dose: 0.5 mg/day

“Medium” dose: 1 mg/day

“High” dose: 2 mg/day

Global Initiative for Asthma guidelines (GINA 2016):

Children ≤5 years: “Low” dose: 0.5 mg daily

Children 6 to 11 years:

“Low” dose: 0.25 to 0.5 mg daily

“Medium” dose: >0.5 to 1 mg daily

“High” dose: >1 mg daily

Oral: 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.

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)

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

Amphotericin B: Corticosteroids (Orally Inhaled) may enhance the hypokalemic effect of Amphotericin B. Monitor therapy

Ceritinib: Corticosteroids may enhance the hyperglycemic effect of Ceritinib. Monitor therapy

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 (Strong): May increase the serum concentration of Budesonide (Oral Inhalation). 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

Desmopressin: Corticosteroids (Orally Inhaled) may enhance the hyponatremic effect of Desmopressin. 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

Loop Diuretics: Corticosteroids (Orally Inhaled) may enhance the hypokalemic effect of Loop Diuretics. Monitor therapy

Loxapine: Agents to Treat Airway Disease may enhance the adverse/toxic effect of Loxapine. More specifically, the use of Agents to Treat Airway Disease is likely a marker of patients who are likely at a greater risk for experiencing significant bronchospasm from use of inhaled loxapine. Management: This is specific to the Adasuve brand of loxapine, which is an inhaled formulation. This does not apply to non-inhaled formulations of loxapine. Avoid combination

Telaprevir: May increase the serum concentration of Budesonide (Oral Inhalation). Management: Concomitant use of these agents is not recommended, unless the risk for excessive systemic corticosteroid effects is outweighed by the potential benefits. If combined, monitor patients closely for signs and symptoms of corticosteroid excess/toxicity. Consider therapy modification

Thiazide and Thiazide-Like Diuretics: Corticosteroids (Orally Inhaled) may enhance the hypokalemic effect of Thiazide and Thiazide-Like Diuretics. Monitor therapy

• 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 nosebleed, common cold symptoms, rhinitis, rhinorrhea, or pharyngitis. 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 adrenal gland problems (severe nausea, vomiting, severe dizziness, passing out, muscle weakness, severe fatigue, mood changes, lack of appetite, or weight loss), signs of Cushing’s disease (weight gain in upper back or abdomen; moon face; severe headache; or slow healing), signs of infection, burning or numbness feeling, ankle edema, severe loss of strength and energy, bone pain, joint pain, vision changes, bruising, bleeding, signs of a severe pulmonary disorder (lung or breathing problems like difficulty breathing, shortness of breath, or a cough that is new or worse), or thrush (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.