Budesonide

Budesonide
ATC Code A07EA06, D07AC09, R01AD05, R03BA02
Formula C25H34O6
Molar Mass (g·mol−1) 430,53
Physical State solid
Melting Point (°C) 226
CAS Number 51333-22-3
PUB Number 2462
Drugbank ID DB01222
Solubility practically insoluble in water, sparingly soluble in ethanol 96%, soluble in dichloromethane and acetone

Basics

Budesonide is a drug from the group of corticosteroids. It is available as an aerosol for inhalation, tablet, nasal spray and suppository. The inhaled form is used in the long-term treatment of asthma and chronic obstructive bronchitis (COPD). The nasal spray is used for allergic rhinitis and nasal polyps. The sustained-release tablets and the rectal form may be used for inflammatory bowel diseases such as Crohn's disease and ulcerative colitis. Budenoside is available by prescription only.

Pharmacology

Pharmacodynamics

Budesonide is an agonist of glucocorticoid receptors. It is used in the treatment of respiratory and digestive tract diseases by inhibiting inflammatory processes. For example, it inhibits the arachidonic acid cascade and the formation of inflammatory cytokines, which are critically involved in the development of inflammation.

Pharmacokinetics

Corticosteroids are generally bound to corticosteroid-binding globulin and serum albumin in plasma. Thus, overall plasma protein binding is approximately 85-90%. Budesonide is 80-90% metabolized at the first liver passage. Budesonide is metabolized by CYP3A4 to its 2 major metabolites, 6-beta-hydroxybudesonide and 16-alpha-hydroxyprednisolone. The activity of these metabolites is negligible (<1/100). Approximately 60% of a budesonide dose is excreted in the urine in the form of the major metabolites 6-beta-hydroxybudesonide and 16-alpha-hydroxyprednisolone. Budesonide has an elimination half-life of 2-4h.

Drug Interactions

With concomitant administration of digitalis glycosides, their effect may be enhanced. Saliuretics together with budesonide may lead to an increased excretion of calamine.

Particular care should be taken in combination with drugs which are also metabolised via the CYP3A4 enzyme. This can lead to increased plasma levels of the active substances and thus to increased side effects. Some drugs also increase the expression of CYP3A4, which may cause the plasma level of budenoside to fall below the effective concentration.

When taking steroid-binding resins such as colestyramine, plasma levels of budenoside may also fall below the effective concentration.

Toxicity

Side effects

Budesonide may cause the following side effects:

  • nasal irritation or burning
  • bleeding or sores in the nose
  • dizziness
  • stomach upset
  • cough
  • hoarseness
  • dry mouth
  • Rash
  • Sore throat
  • Bad taste in the mouth
  • change in mucus
  • blurred vision
  • Mouth sores (if used by inhalation).

Seek immediate medical attention if the following symptoms occur:

  • Difficulty breathing or swelling of the face
  • white patches in the throat, mouth, or nose
  • Irregular menstrual periods
  • severe acne
  • Behavioral changes (usually in children)

Toxicological data

LD50 (rat, oral): > 3200 mg-kg-1

Sources

Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter ist Autor zu pharmazeutischen Themen in der Medizin-Redaktion von Medikamio. Er befindet sich im letzten Semester seines Pharmaziestudiums an der Universität Wien und liebt das wissenschaftliche Arbeiten im Bereich der Naturwissenschaften.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer ist seit 2020 freie Autorin bei Medikamio und studierte Pharmazie an der Universität Wien. Sie arbeitet als Apothekerin in Wien und ihre Leidenschaft sind pflanzliche Arzneimittel und deren Wirkung.

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The contents shown do not replace the original package insert of the medicinal product, especially with regard to dosage and effect of the individual products. We cannot assume any liability for the correctness of the data, as the data was partly converted automatically. A doctor should always be consulted for diagnoses and other health questions. Further information on this topic can be found here.