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

Introduction

Tradenames: Rhinocort, Pulmicort, Turbuhaler, Flexhaler, Pulmicort Respules (solution for nebulizer), Entocort EC, Eohilia

Indications

• atopy, allergic rhinintis
• prophylaxis for asthma in adults & children > 6 years
• COPD
• acute flares of Crohn's disease
  • Entocort EC targets the ileum & ascending colon
  • advantage over other steroids is reduced systemic effect
• ulcerative colitis
  • Uceris targets the entire colon
• budesonide oral suspension (Eohilia) first oral treatment for eosinophilic esophagitis

Contraindications

Caution:

• inhaler
• low systemic absorption
• will NOT provide glucocorticoid coverage for adrenal insufficiency (i.e. systemic steroid withdrawal)

pregnancy category = c

safety in lactation = -

Dosage

• nasal spray: 2 sprays BID or 4 sprays QD.
• inhaler:
  • 1-2 puffs BID, max: 4 puffs BID (2 puffs BID for children) 360 ug/day is adult dose
  • Turbuhaler: 200 ug/actuation; 160 ug from the mouth piece. 200 doses/inhaler
  • Flexhaler: 90 & 180 ug/actuation {contains lactose}
• nebulizer BID, 0.25 & 0.5 mg/mL amps
• oral: 9 mg PO QAM
  • budesonide MMX (Cortiment, Uceris): once daily colonic delivery system for ulterative colitis; 9 mg PO QAM
• no intravenous formulation

Capsules: 3 mg

Pharmacokinetics

• nasal spray: effects measureable within 5 hours & persist > 12 hours
• metabolized by cyt P450 3A4 on 1st pass through liver
• very little reaches systemic circulation

elimination via liver

Adverse effects

• common (> 10%)
  • GI irritation, bitter taste, upper respiratory tract infection, sinusitis, hoarseness, diaphoresis
• 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
• uncommon (< 1&)
  • bronchospasm
• other
  • irritation of nasal mucosa
  • rarely nasal ulceration
  • oral candidiasis (thrush)

• drug adverse effects of glucocorticoids
• drug adverse effects of immunosuppressive agents

Drug interactions

• agents that inhibit cyt P450 3A4 may inhibit metabolism of budesonide (clarithromycin & others)
• agents which induce cyt P450 3A4 may enhance metabolism of budesonide
• avoid grapefruit juice

• drug interaction(s) of methotrexate with biological response modifier
• drug interaction(s) of glucocorticoids with warfarin
• drug interaction(s) of NSAIDs with glucocorticoid

Laboratory

• budesonide in serum/plasma
• budesonide in urine

Notes

• Uceris costs ~$1200/month vs ~$4 for prednisone

More general terms

• glucocorticoid
• antiasthmatic agent

Additional terms

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

Component of

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

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5281004
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3033890
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=2462
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=657195
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=470826
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=63006
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=40000