Budesonide

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Contents 1 Introduction 2 Indications 3 Contraindications 4 Dosage 5 Pharmacokinetics 6 Adverse-effects 7 Drug-interactions 8 More General Terms 9 Additional Terms 10 Internet Database 11 References

Introduction

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

Indications

• allergic rhinintis
• prophylaxis for asthma in adults & children > 6 years
• acute flares of Crohn's disease ( ileum & ascending colon) (advantage over other steroids is reduced systemic effect)

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 [5] {contains lactose}

• nebulizer BID, 0.25 & 0.5 mg/mL amps
• systemic: 9 mg QAM

• Capsules: 3 mg

Pharmacokinetics

• nasal spray: effects measureable within 5 hours & persist > 12 hours [4]
• 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) [5]
• agents which induce cyt P450 3A4 may enhance metabolism of budesonide
• avoid grapefruit juice
  
• drug interaction(s) of glucocorticoids with warfarin

More General Terms

• glucocorticoid
• antiasthmatic agent

Additional Terms

• Crohn's disease (terminal ileitis, regional enteritis, granulomatous enteritis, chronic cicatrizing enteritis)

Internet Database

PubChem: 5281004
PubChem: 3033890
PubChem: 2462
PubChem: 657195
PubChem: 470826
PubChem: 63006
PubChem: 40000

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#: [1] (subscription needed) [2]
6. Prescriber's Letter 17(7): 2010 Clarithromycin Interaction with Salmeterol and Inhaled Corticosteroids Detail-Document#: [3] (subscription needed) [4]

budesonide (Rhinocort, Pulmicort, Turbuhaler, Flexhaler, Entocort EC)