Budesonide
Budesonide, sold under the brand name Pulmicort, among others, is a steroid medication. It is available as an inhaler, nebulization solution, pill, nasal spray, and rectal foam. The inhaled form is used in the long-term management of asthma and chronic obstructive pulmonary disease. The nasal spray is used for allergic rhinitis and nasal polyps. Modified-release pills or capsules and rectal forms may be used for inflammatory bowel disease including Crohn's disease, ulcerative colitis, and microscopic colitis.
Common side effects with the inhaled form include respiratory infections, cough, and headaches. Common side effects with the pills include feeling tired, vomiting, and joint pains. Serious side effects include an increased risk of infection, loss of bone strength, and cataracts. Long-term use of the pill form may cause adrenal insufficiency. Stopping the pills suddenly following long-term use may therefore be dangerous. The inhaled form is generally safe in pregnancy. Budesonide chiefly acts as a glucocorticoid.
Budesonide was initially patented in 1973. Commercial use as an asthma medication began in 1981. It is on the World Health Organization's List of Essential Medicines. Some forms are available as a generic medication. In 2023, it was the 162nd most commonly prescribed medication in the United States, with more than 3million prescriptions.
Medical uses
Asthma
Budesonide is given by metered-dose inhaler or nebulizer for maintenance and prophylactic treatment of asthma, including patients who require oral corticosteroids and those who may benefit from a systemic dose reduction.Inflammatory bowel disease
Formulations of delayed-release budesonide are an effective treatment for mild-to-moderately active Crohn's disease involving the ileum and/or ascending colon. A Cochrane review found evidence for up to three months of maintenance of remission in Crohn's disease, concluding that budesonide is not effective for maintenance of remission in CD.Budesonide assists in the induction of remission in people with active ulcerative colitis.
Budesonide is highly effective and recommended as the drug of choice in microscopic colitis, for induction and maintenance of remission, and for both the lymphocytic colitis and collagenous colitis forms.
Allergic rhinitis
Budesonide in the form of nasal sprays is a treatment for allergic rhinitis.Eosinophilic esophagitis
Topical budesonide has considerable effects in eosinophilic esophagitis. For this use, it is formulated as a tablet that disperses in the mouth, and sold under the brand name Jorveza.Berger's disease
Budesonide ; Kinpeygo ) is indicated to reduce proteinuria in adults with primary immunoglobulin A nephropathy at risk of rapid disease progression.Side effects
Nasal budesonide inhalers have been associated with a number of side effects. These include nose irritation or burning, bleeding or sores in the nose, lightheadedness, upset stomach, cough, hoarseness, dry mouth, rash, sore throat, bad taste in mouth, change in mucus, and blurred vision. Other symptoms which should be reported immediately include difficulty in breathing, swelling of the face, white patches in the throat, mouth, or nose, irregular menstrual periods, severe acne, and on rare occasions, behavioral changes.Overdose
Acute toxicity from an overdose of budesonide is significantly more rare than an overdosing of budesonide over a prolonged period of therapy, however both can cause systemic toxicity that manifests as hypercortisolism. Symptoms of an overdose include more specific symptoms such as darkening and thinning of the skin, changes in body fat around the face, neck, back, and waist, increased acne or facial hair, menstrual problems, impotence, or loss of interest in sex, as well as some less specific symptoms such as diarrhea, dizziness, loss of appetite, mental depression, nausea, skin rash, unusual tiredness or weakness, or vomiting.Contraindications
Budesonide is contraindicated in people with:- Known hypersensitivity to budesonide or any component of the formulation.
- Status asthmaticus or other acute episodes of asthma which would require intensive, immediate measures.
- Systemic or local bacterial, fungal and viral infections.
- Active or quiescent pulmonary tuberculosis.
Interactions
Pharmacology
Mechanism of action
Budesonide is an agonist of glucocorticoid receptors. Among its effects are:- Controls the rate of protein synthesis.
- Depresses the migration of polymorphonuclear leukocytes and fibroblasts.
- Reverses capillary permeability and lysosomal stabilization at the cellular level to prevent or control inflammation.
- Has a potent glucocorticoid activity and weak mineralocorticoid activity.
Pharmacokinetics
The plasma protein binding of budesonide is around 85-90%, with an apparent volume of distribution of 2.2-3.9L/kg. Budesonide is 80-90% metabolized at first pass in the liver by the hepatocytic cytochrome P450 isoenzyme 3A4 into two metabolites: 16 alpha-hydroxyprednisolone and 6 beta-hydroxybudesonide. Both of these metabolites have a negligible glucocorticoid activity of less than 1% compared to the parent compound budesonide. 60% of budesonide is excreted through urine as its metabolites, no unchanged budesonide is detectable in urine. The average elimination half-life in plasma is between 2–3.6 hours.
Chemistry
Budesonide, also known as 11β,21-dihydroxy-16α,17α-pregna-1,4-diene-3,20-dione, is a synthetic pregnane steroid and non-halogenated cyclic ketal corticosteroid. It is the C16α hydroxyl, C16α,17α cyclic ketal with butyraldehyde derivative of prednisolone.Stereoisomerism
Society and culture
Brand names
Budesonide is marketed under various brand and generic names internationally. Notable examples for each formulation include:Inhalation: Pulmicort, Pulmicort Flexhaler, Pulmicort Nebuamp, Pulmicort Turbuhaler, TARO-Budesonide, TEVA-Budesonide, Novolizer budesonid meda, Budenova.
Systemic : Tarpeyo, Uceris, Eohilia, Cortiment, Entocort Jorveza.
Nasal: MYLAN-Budesonide AQ, Rhinocort Aqua, Formancis.
Topical: Entocort, Uceris, Budenofalk.
Economics
In 2019, 44 US states filed a lawsuit claiming that leading drug companies including Teva, Pfizer, Novartis and Mylan conspired to inflate the prices of over a hundred generic drugs, including budesonide, as much as tenfold.Legal status
Kinpeygo, a hybrid medicine of Entocort that contains the same active substance as Entocort but has a different formulation and a different indication, was approved for medical use in the European Union in July 2022.The FDA granted the application breakthrough therapy designation.