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budesonide (Rhinocort, Pulmicort, Turbuhaler, Flexhaler, Entocort EC, Uceris, Cortiment, Eohilia)

Tradenames: Rhinocort, Pulmicort, Turbuhaler, Flexhaler, Pulmicort Respules (solution for nebulizer), Entocort EC, Eohilia Indications: 1) atopy, allergic rhinintis 2) prophylaxis for asthma in adults & children > 6 years 3) COPD [8] 3) acute flares of Crohn's disease a) Entocort EC targets the ileum & ascending colon b) advantage over other steroids is reduced systemic effect 4) ulcerative colitis - Uceris targets the entire colon 5) budesonide oral suspension (Eohilia) first oral treatment for eosinophilic esophagitis [10] Contraindications: Caution: - inhaler 1) low systemic absorption 2) will NOT provide glucocorticoid coverage for adrenal insufficiency (i.e. systemic steroid withdrawal) Dosage: 1) nasal spray: 2 sprays BID or 4 sprays QD. 2) inhaler: a) 1-2 puffs BID, max: 4 puffs BID (2 puffs BID for children) 360 ug/day is adult dose b) Turbuhaler: 200 ug/actuation; 160 ug from the mouth piece. 200 doses/inhaler c) Flexhaler: 90 & 180 ug/actuation [5] {contains lactose} 3) nebulizer BID, 0.25 & 0.5 mg/mL amps 4) oral: 9 mg PO QAM - budesonide MMX (Cortiment, Uceris): once daily colonic delivery system for ulterative colitis; 9 mg PO QAM [9] 5) no intravenous formulation Capsules: 3 mg Pharmacokinetics: 1) nasal spray: effects measureable within 5 hours & persist > 12 hours [4] 2) metabolized by cyt P450 3A4 on 1st pass through liver 3) very little reaches systemic circulation Adverse effects: 1) common (> 10%) - GI irritation, bitter taste, upper respiratory tract infection, sinusitis, hoarseness, diaphoresis 2) less common (1-10%) - insomnia, psychic changes, asthenia, pain, dyspepsia, nausea, anorexia, increased appetite, dry mouth, dry throat, alteration in voice, oral candidiasis, increased cough, ecchymosis, pharyngitis 3) uncommon (< 1&) - bronchospasm 4) other - irritation of nasal mucosa - rarely nasal ulceration - oral candidiasis (thrush) Drug interactions: 1) agents that inhibit cyt P450 3A4 may inhibit metabolism of budesonide (clarithromycin & others) [5] 2) agents which induce cyt P450 3A4 may enhance metabolism of budesonide 3) avoid grapefruit juice Laboratory: - budesonide in serum/plasma - budesonide in urine Notes: - Uceris costs ~$1200/month vs ~$4 for prednisone

Interactions

drug interactions drug adverse effects (more general classes) monitor with drug (more general classes)

Related

Crohn's disease; terminal ileitis; regional enteritis; granulomatous enteritis; chronic cicatrizing enteritis

General

antiasthmatic agent glucocorticoid

Properties

MISC-INFO: elimination route LIVER pregnancy-category C safety in lactation -

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Mayo Internal Medicine Board Review, 1998-99, Prakash UBS (ed) Lippincott-Raven, Philadelphia, 1998, pg 743
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. Journal Watch 20(9):70, 2000 Day et al J Allergy Clin Immunol 105:489, 2000
  5. Prescriber's Letter 14(6): 2007 Pulmicort Flexhaler (Budesonide Inhalation Powder) Detail-Document#: 2306209 (subscription needed) http://www.prescribersletter.com
  6. Prescriber's Letter 17(7): 2010 Clarithromycin Interaction with Salmeterol and Inhaled Corticosteroids Detail-Document#: 260701 (subscription needed) http://www.prescribersletter.com
  7. Prescriber's Letter 20(3): 2013 Treatments for Ulcerative Colitis Detail-Document#: 290303 (subscription needed) http://www.prescribersletter.com
  8. Deprecated Reference
  9. Hoy SM. Budesonide MMX: a review of its use in patients with mild to moderate ulcerative colitis. Drugs. 2015 May;75(8):879-86. Review. PMID: 25920500
  10. Brooks M FDA OKs First Oral Agent for Eosinophilic Esophagitis. Medscape. Feb 12, 2024 https://www.medscape.com/viewarticle/fda-oks-first-oral-agent-eosinophilic-esophagitis-2024a100031d

Component-of

albuterol/budesonide (Airspura) budesonide/formoterol (Symbicort) budesonide/formoterol/glycopyrrolate (Breztri Aerosphere)