Budesonide
- Atc Codes:A07EA06#D07AC09#R01AD05#R03BA02
- CAS Codes:51333-22-3#51372-29-3#51372-28-2
- PHARMGKB ID:51333-22-3#51372-29-3#51372-28-2
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Induces
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Belgium: Budenofalk, Budesonide Easyhaler, Docbudeso, Entocort, Miflonide, Novolizer Budesonide, Pulmicort, Rhinobudesonide, Rhinocort; Bulgaria: Budenofalk, Budiair, Neo-Rinactive, Pulmicort; Cyprus: Entocort, Novopulmon, Rhinocort; Czech Republic: Budenofalk, Budesonide, Budiair, Entocort, Giona Easyhaler, Miflonid, Pulmicort, Rhinocort, Ribuspir, Tafen Aqua, Tinkair; Denmark: Budenofalk, Budesonid, Entocord, Entocort, Giona Easyhaler, Miflonide, Pulmicort, Rhinocort, Spirocort; Estonia: Budesonid, Budiair, Miflonide, Neplit Easyhaler, Pulmax, Pulmicort, Rhinocort Aqua, Ribuspir; Finland: Budenofalk, Budesonid Easyhaler, Entocort, Novopulmon, Pulmicort, Rhinocort; France: Budesonide, Entocort, Miflonil, Novopulmon, Pulmicort, Rafton, Rhinocort; Germany: Aquacort, Budapp nasal, Budecort, Budehaler, Budenobronch, Budenofalk, Budes, Budesonid, Budiair, Entocort, Miflonide, Novopulmon, Pulmax, Pulmicort, Rhinocort; Greece: Abelitan, Aldesonit, Arsicort, Astrocast, Aurid, Axelovert, Beysonit, Biosonide, Budecol, Budemar, Budenite, Budenofalk, Budeprol, Buderen, Budesan, Budesoderm, Budesonal, Budesonide, Budiair, Busonal, Butekont, Buyamin, Dedostryl, Dexalocal, Eolan, Esonide, Etrafonil, Farlidone, Labetosol, Lisobron, Lydenal, Miflonide, Minalerg, Murapol, Nalator, Obecirol, Obusonid, Olpho Haler, Olfodil, Olfosonide, Pimoftal, Pulmicort, Pulmison, Pulmiver, Pulmovance, Resata, Rhinobros, Rhinoside, Rinoster, Serbo, Sonidal, Talgan; Hungary: Aerox, Budenofalk, Budesogen, Entocort, Miflonide, Neplit Easyhaler, Pulmicort, Rhinocort, Ribuspir; Ireland: Budenofalk, Budesitan, Entocort, Novolizer Budesonide, Pulmicort, Rhinocort; Italy: Aircort, Bidien, Bodinet, Bodix, Budesonide, Budexan, Budiair, Budineb, Busoded, Desonax, Eltair, Entocir, Kesol, Miflo, Miflonide, Pulmaxan, Rafton, Rhinocort, Xavin; Luxembourg: Entocort Enema, Preferid, Pulmicort, Rhinocort; Lithuania: Budesonid; Netherlands: Budenofalk, Budesonide, Entocort, Pulmicort, Rhinocort, Ribuspir; Poland: Budenofalk, Buderhin, Budesonid, Entocort, Horacort, Miflonide, Pulmicort, Rhinocort; Portugal: Aeromax Nasal, Budesonida, Budesonido, Budo San, Entocort, Miflonide, Neo Rinactive, Pulmicort; Romania: Budenofalk, Budiair, Frenolyn, Pulmocort, Rhinocort, Tafen Nasal; Slovakia: Budenofalk, Budiair, Entocort, Giona Easyhaler, Miflonid, Pulmicort, Rhinocort, Rhinogen, Tafen Nasal; Slovenia: Budenofalk, Budiair, Neplit Easyhaler, Pulmicort, Pulmovent, Tafen; Spain: Budesonida, Demotest, Entocord, Miflonide, Neo Rinactive, Novopulm Novolizer, Olfex, Pulmicort, Pulmictán, Rhinocort, Ribujet; Sweden: Budenofalk, Budesonid, Desonix, Entocord, Enyocort, Giona Easyhaler, Novopulmon, Pulmicort, Rhinocort; UK: Budelin, Budenofalk, Budesonide Easyhaler, Entocort, Novolizer Budesonide, Pulmicort, Rhinocort.
North America
Canada: Budesonide AQ, Entocort, Pulmicort, Rhinocort; USA: Entocort EC, Pulmicort, Rhinocort.
Latin America
Argentina: Aerovent, Budesón, Budesonida, Budesonide, Budezonil, Cuteral, Entocort, Hypersol B, Neumocort, Neumotex, Proetzonide, Pulmo Lisoflam, Rino-B; Brazil: Budecort, Budiair, Busonid, Entocort, Miflonide, Noex, Pulmicort; Mexico: Entocort, Miflonide, Numark, Pulmicort, Rhinocort.
Asia
Japan: Pulmicort.
Drug combinations
Budesonide and Formoterol
Chemistry
Budesonide: C~25~H~34~O~6~. Mw: 430.53. Mixture of two isomers; [11β,16α(S)] content between 40-51%. (1) Pregna-1,4-diene-3,20-dione, 16,17-butylidenebis(oxy)-11,21-dihydroxy-, [11β,16α(R)], and 16α,17-[(S)-Butylidenebis(oxy)]-11β,21-dihydroxypregna-1,4-diene-3,20-dione; (2)(R,S)-11β,16α,17,21-Tetrahydroxypregna-1,4-diene-3,20-dione cyclic 16,17-acetal with butyraldehyde. CAS-51333-22-3 (11 β,16α); CAS-51372-29-3 ((11β,16α[R])); CAS-51372-28-2 ((11 β,16α[S]))(1979).
Pharmacologic Category
Hormones and Synthetic Substitutes; Adrenals. EENT Preparations; Anti-inflammatory Agents; Corticosteroids. (ATC-Code: A07EA06; D07AC09; R01AD05; R03BA02).
Mechanism of action
Decreases inflammation by stabilizing leukocyte lysosomal membranes, preventing release of destructive acid hydrolases from leukocytes, or reducing leukocyte adhesion to capillary endothelium. Inhibits macrophage accumulation in inflamed areas. Reduces capillary wall permeability and edema formation. Antagonizes histamine activity and release of kinin from substrates. Reduces fibroblast proliferation, collagen deposition, and subsequent scar tissue formation. Stimulates erythroid cells of bone marrow, prolongs survival time of erythrocytes and platelets, and produces neutrophilia and eosinopenia. Potent glucocorticoid and weak mineralocorticoid activity. Promotes gluconeogenesis, redistribution of fat from peripheral to central areas of the body, and protein catabolism, which results in negative nitrogen balance. Reduces intestinal absorption and increases renal excretion of calcium. Suppresses the immune response by reducing activity and volume of the lymphatic system, producing lymphocytopenia. Decreases immunoglobulin and complement concentrations and passage of immune complexes through basement membranes. Depresses reactivity of tissue to antigen-antibody interactions. Appears to have immunosuppressant and substantial topical anti-inflammatory activity and lower systemic availability than conventional corticosteroids.
Therapeutic use
Management of symptoms of seasonal or perennial rhinitis. Prevention and treatment of nasal polyps. Maintenance and prophylactic treatment of asthma (not indicated for the relief of acute bronchospasm). Treatment of active Crohn’s disease (mild-to-moderate) involving the ileum and/or ascending colon. Maintenance of remission (for up to 3 months) of Crohn’s disease (mild-to-moderate) involving the ileum and/or ascending colon.
Pregnancy and lactiation implications
Adverse events observed in animal reproduction studies. Studies of pregnant women using inhaled budesonide have not demonstrated an increased risk of abnormalities. Some studies have shown an association between first trimester systemic corticosteroid use and oral clefts. Hypoadrenalism reported in infants. Budesonide is the preferred inhaled corticosteroid for the treatment of asthma in pregnant women. Use with caution during lactation.
Unlabeled use
Contraindications
Hypersensitivity to budesonide or any component of the formulation. Inhalation is contraindicated in primary treatment of status asthmaticus, acute episodes of asthma (not for relief of acute bronchospasm). Some institutions advise against its use in moderate-to-severe bronchiectasis, pulmonary tuberculosis (active or quiescent), untreated respiratory infection (bacterial, fungal, or viral), or in patients <6 years of age.
Warnings and precautions
May cause hypercorticism or suppression of hypothalamic-pituitary-adrenal axis, leading to adrenal crisis. Withdrawal and discontinuation of a corticosteroid should be done slowly and carefully. Caution when patients are transferred from systemic corticosteroids to inhaled products. Aerosol steroids do not provide the systemic steroid needed to treat patients having trauma, surgery, or infections. Bronchospasm may occur with wheezing after inhalation. Avoid nasal corticosteroid use in recent nasal septal ulcers, nasal surgery or nasal trauma until healing has occurred. Prolonged use of corticosteroids may increase the incidence of secondary infection, mask acute infection (including fungal infections), prolong or exacerbate viral infections, or limit response to vaccines. Exposure to chickenpox should be avoided. Corticosteroids should not be used to treat ocular herpes simplex, cerebral malaria, or viral hepatitis. Restrict use in active tuberculosis (only in conjunction with antituberculosis treatment). Prolonged treatment has been associated with Kaposi’s sarcoma. Acute myopathy reported with high-dose corticosteroids, usually in neuromuscular transmission disorders (may involve ocular and/or respiratory muscles). Corticosteroid use may cause psychiatric disturbances, including depression, euphoria, insomnia, mood swings, and personality changes. Pre-existing psychiatric conditions may be exacerbated by corticosteroid use. Use with caution in heart failure or hypertension (may cause fluid retention and hypertension), diabetes mellitus (may alter glucose production/regulation), gastrointestinal diseases due to perforation risk (diverticulitis, peptic ulcer, ulcerative colitis), hepatic impairment (may cause fluid retention), or myasthenia gravis (exacerbation of symptoms). Use with caution following acute myocardic infarct. May cause increased intraocular pressure, open-angle glaucoma, and cataracts. Use with caution in osteoporosis (risk of increased bone loss and osteoporotic fractures). Use with caution in renal impairment (fluid retention). Use with caution in history of seizure disorder (higher risk if adrenal crisis). Metabolic clearance of corticosteroids increases in hyperthyroidism and decreases in hypothyroidism. Orally-inhaled and intranasal corticosteroids may cause reduction in growth velocity in pediatric patients (~1 cm/year). Some forms contain lactose (risk of anaphylactic reactions in severe milk protein allergy). Oral capsule should be swallowed whole. May cause xerostomia, dry throat, abnormal taste, and herpes simplex. Rarely, immediate or delayed hypersensitivity reactions may occur. Wheezing reported very rarely.