Budesonide
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Budesonide
Pulmicort (inhaled), Rhinocort (intranasal), Entocort EC and Uceris (enteric-coated oral for IBD), Symbicort (with formoterol)
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Summary
Common uses
Asthma controller0, COPD0, Allergic rhinitis (intranasal)0, Croup (nebulized)0, Crohn's disease (oral enteric-coated, ileal/right-colonic disease)0, Ulcerative colitis (Uceris)0
Pharmacy
Starting dose
ICS Pulmicort Flexhaler 180-360 mcg BID; intranasal Rhinocort 64 mcg/spray, 1-2 sprays/nostril daily; Entocort EC 9 mg PO daily for active Crohn's; Symbicort 80/4.5 or 160/4.5 mcg, 2 puffs BID
Preparations
Pulmicort Flexhaler DPI 90, 180 mcg/dose; Pulmicort Respules 0.25, 0.5, 1 mg/2 mL nebulized; Rhinocort intranasal 32 mcg/spray; Entocort EC 3 mg capsules; Uceris 9 mg ER tablets and rectal foam
US FDA Max
ICS ~1280 mcg/d; intranasal 256 mcg/d; Entocort 9 mg/d standard
Pharmacology
Routes
Inhaled, intranasal, oral (enteric-coated, rectal foam), nebulized
Onset
Inhaled: bronchial effect 1-2 weeks; oral GI effect 1-2 weeks
Duration
12-24 hours
Half-life
~2-3.6 hours (plasma)[1]
Bioavailability
~6-13% inhaled lung deposition; ~10% oral (Entocort EC; extensive first-pass via CYP3A4 — this is the basis of the favorable hepatic-targeted local-effect profile in IBD)[1]
Pregnancy
Long the preferred ICS in pregnancy (Pulmicort) due to the most pregnancy data among the class.[citation needed]
Legal status
OTC (intranasal Rhinocort Allergy) and Rx-only (other forms) in US
Purported mechanism
Budesonide is a high-potency glucocorticoid receptor agonist designed with high topical receptor affinity and extensive hepatic first-pass to minimize systemic glucocorticoid exposure.0 The first-pass property is the basis of enteric-coated oral formulations for IBD: drug is delivered locally to ileum/right colon (Entocort EC) or to colon (Uceris), then largely inactivated on first hepatic pass, sparing systemic steroid exposure. CYP3A4 substrate; strong CYP3A4 inhibitors (ritonavir, ketoconazole) can raise systemic levels enough to produce iatrogenic Cushing's[1].
References
- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Pulmicort Flexhaler (budesonide), AstraZeneca, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021949s041lbl.pdf