budesonide (inhalation)

Absorption: Flexhaler: 39%; Respules: 6%. Action is primarily local following inhalation.

Distribution: Crosses placenta; enters breast milk in small amounts.

Protein Binding: 85–90%.

Metabolism/Excretion: Metabolized by the liver (primarily by CYP3A4) following absorption from lungs; 60% excreted in urine, 40% in feces.

Half-Life: Adults: 2–3.6 hr; Children 10–14 yrs: 1.5 hr; Children 4–6 yrs: 2.3 hr (after nebulization).

Time/Action Profile ⬆ ⬇

(improvement in symptoms)

ROUTE	ONSET	PEAK	DURATION
Inhaln	within 24 hr	1–4 wk‡	unknown
Nebulization	with 2–8 days	4–6 wk	unknown

‡Improvement in pulmonary function; decreased airway responsiveness may take longer.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Acute attack of asthma/status asthmaticus.

Use Cautiously in:

Active untreated infection;
Diabetes;
Glaucoma;
Underlying immunosuppression (from disease or concurrent therapy);
Systemic corticosteroid therapy (should not be abruptly discontinued when inhaled therapy is started; additional corticosteroids needed during stress or trauma);
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Higher than recommended doses in children can lead to suppression of hypothalamic-pituitary-adrenal (HPA) function and suppression of linear growth.

Adv. Reactions/Side Effects ⬆ ⬇

Derm: rash

EENT: otitis media, dysphonia, epistaxis, oropharyngeal fungal infections, pharyngitis, rhinitis, sinusitis

Endo: ↓growth (children), adrenal suppression (high dose, long-term therapy only), weight gain

GI: abdominal pain, diarrhea, dyspepsia, gastroenteritis, nausea, vomiting

MS: back pain

Neuro: headache

Resp: bronchospasm, cough

Misc: ANAPHYLAXIS, flu-like syndrome

Interactions ⬆ ⬇

Drug-drug:

Strong CYP3A4 inhibitors, including ritonavir, atazanavir, clarithromycin, , itraconazole, ketoconazole, nefazodone, and nelfinavir, may ↑ levels and risk of toxicity.

Route/Dosage ⬆ ⬇

Flexhaler

Inhaln (Adults ): —180–360 mcg twice daily (not to exceed 720 mcg twice daily).
Inhaln (Children ≥6 yr): —180–360 mcg twice daily (not to exceed 360 mcg twice daily).

Respules

Inhaln (Children 1–8 yr): Previously on bronchodilators alone–0.5 mg once daily or 0.25 mg twice daily (not to exceed 0.5 mg/day); Previously on other inhaled corticosteroids: 0.5 mg once daily or 0.25 mg twice daily (not to exceed 1 mg/day); Previously on oral corticosteroids: 1 mg once daily or 0.5 mg twice daily (not to exceed 1 mg/day).

Availability ⬆ ⬇

(Generic available)

Inhalation powder (Flexhaler): 90 mcg/metered inhalation (delivers 60 metered inhalations); 100 mcg/metered inhalation (delivers 200 metered inhalations); 180 mcg/metered inhalation (delivers 120 metered inhalations); 200 mcg/metered inhalation (delivers 200 metered inhalations); 400 mcg/metered inhalation (delivers 200 metered inhalations)
Inhalation suspension (Respules): 0.25 mg/2 mL in single dose ampules (5 ampules/envelope); 0.5 mg/2 mL in single dose ampules (5 ampules/envelope); 1 mg/2 mL in single dose ampules (5 ampules/envelope)
In combination with: albuterol (Airsupra); formoterol (Symbicort); formoterol and glycopyrrolate (Breztri Aerosphere); see Appendix [not included in this PDA edition].

Assessment ⬆ ⬇

Monitor respiratory status and lung sounds. Assess pulmonary function tests periodically during and for several mo following a transfer from systemic to inhalation corticosteroids.
Assess patients changing from systemic corticosteroids to inhalation corticosteroids for signs of adrenal insufficiency (anorexia, nausea, weakness, fatigue, hypotension, hypoglycemia) during initial therapy and periods of stress. If these signs appear, notify health care professional immediately; condition may be life-threatening.
Monitor for withdrawal symptoms (fatigue, weakness, nausea, vomiting, hypotension, joint or muscular pain, lassitude, depression) during withdrawal from oral corticosteroids.
Monitor growth rates in children receiving chronic therapy; lowest possible dose should be used.

Lab Test Considerations:

Periodic adrenal function tests may be ordered to assess degree of hypothalamic-pituitary-adrenal (HPA) axis suppression in chronic therapy. Children and patients using higher than recommended doses are at highest risk for HPA suppression.
- May cause ↑ serum and urine glucose concentrations if significant absorption occurs.

Implementation ⬆ ⬇

After the desired clinical effect has been obtained, attempts should be made to decrease dose to lowest amount required to control symptoms. Gradually decrease dose every 2–4 wk as long as desired effect is maintained. If symptoms return, dose may briefly return to starting dose.
Inhaln: Allow at least 1 min between inhalations of Flexhaler. Do not shake inhaler or use with spacer.
Clear nasal passage by blowing nose prior to use, shake canister gently before use.

Patient/Family Teaching ⬆ ⬇

Advise patient to take medication as directed. Take missed doses as soon as remembered unless almost time for next dose. Advise patient not to discontinue medication without consulting health care professional; gradual decrease is required. Instruct patient to read the Patient Information and Instructions for Use before using and with each Rx refill, in case of new information.
Advise patients using inhalation corticosteroids and bronchodilator to use bronchodilator first and to allow 5 min to elapse before administering the corticosteroid, unless otherwise directed by health care professional.
Advise patient that inhalation corticosteroids should not be used to treat an acute asthma attack but should be continued even if other inhalation agents are used.
Patients using inhalation corticosteroids to control asthma may require systemic corticosteroids for acute attacks. Advise patient to use regular peak flow monitoring to determine respiratory status.
Advise patient to rinse mouth with water after treatment to decrease risk of developing local candidiasis.
Caution patient to avoid smoking, known allergens, and other respiratory irritants.
Advise patient to notify health care professional if sore throat or mouth or symptoms of anaphylaxis (rash, severe itching, swelling of the face, mouth, and tongue, trouble breathing or swallowing, chest pain, anxiety or feeling of doom) occur.
Instruct patient whose systemic corticosteroids have been recently reduced or withdrawn to carry a warning card indicating the need for supplemental systemic corticosteroids in the event of stress or severe asthma attack unresponsive to bronchodilators.
Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.
Pulmicort Flexhaler: Advise patient to follow instructions supplied. Before first-time use, prime unit by turning cover and lifting off; hold upright with mouthpiece up and twist brown grip fully to right, then fully to left until it clicks. To administer dose, hold upright, twist brown grip fully to right, then fully to left, until it clicks. Turn head away from inhaler and exhale (do not blow into inhaler). Do not shake inhaler. Place mouthpiece between lips and inhale deeply and forcefully. Remove inhaler from mouth and exhale (do not exhale into mouthpiece). Repeat procedure if 2nd dose required. Replace cover.
Pulmicort Respules: Administer with a jet nebulizer connected to adequate air flow, equipped with a mouthpiece or face mask. Adjust face mask to avoid exposing eyes to nebulized medication. Wash face after use of face mask. Ultrasonic nebulizers are not adequate for administration and not recommended.
- Instruct parent to read and follow the Patients Instructions for Use included in each package. Do not mix with other medications in the nebulizer.
- Store respules upright, away from heat and protected from light. Do not refrigerate or freeze. Respules are stable for 2 wk at room temperature after opening aluminum foil envelope. Open respules must be used promptly. Unused respules should be returned to aluminum foil envelope.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇