Budesonide

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Budesonide
Clinical data
Trade namesPulmicort, Rhinocort, Entocort, others
Other namesBUD
AHFS/Drugs.comMonograph
MedlinePlusa608007
License data
Pregnancy
category
  • AU: A/ B3
Routes of
administration		By mouth, nasal, tracheal, rectal, inhalation
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability10-20% (first pass effect)
Protein binding85-90%
MetabolismLiver CYP3A4
Elimination half-life2.0-3.6 hours
ExcretionUrine, feces
Identifiers
  • 11β,21-Dihydroxy-16α,17α-[butane-1,1-diylbis(oxy)]pregna-1,4-diene-3,20-dione
JSmol)
  • CCCC1O[C@@H]2C[C@H]3[C@@H]4CCC5=CC(=O)C=C[C@@]5([C@H]4[C@H](C[C@@]3([C@@]2(O1)C(=O)CO)C)O)C
  • InChI=1S/C25H34O6/c1-4-5-21-30-20-11-17-16-7-6-14-10-15(27)8-9-23(14,2)22(16)18(28)12-24(17,3)25(20,31-21)19(29)13-26/h8-10,16-18,20-22,26,28H,4-7,11-13H2,1-3H3/t16-,17-,18-,20+,21?,22+,23-,24-,25+/m0/s1 ☒N
  • Key:VOVIALXJUBGFJZ-KWVAZRHASA ☒N
 ☒NcheckY (what is this?)  (verify)

Budesonide, sold under the brand name Pulmicort among others, is a medication of the corticosteroid type.[8] It is available as an inhaler, nebulization solution, pill, nasal spray, and rectal forms.[8][9] The inhaled form is used in the long-term management of asthma and chronic obstructive pulmonary disease (COPD).[8][10][11] The nasal spray is used for allergic rhinitis and nasal polyps.[9][12] The pills in a delayed release form and rectal forms may be used for inflammatory bowel disease including Crohn's disease, ulcerative colitis, and microscopic colitis.[13][14][15]

Common

cataracts.[8] Long-term use of the pill form may cause adrenal insufficiency.[8] Stopping the pills suddenly following long-term use may therefore be dangerous.[8] The inhaled form is generally safe in pregnancy.[8] Budesonide chiefly acts as a glucocorticoid.[8]

Budesonide was initially patented in 1973.

generic medication.[19][20] In 2021, it was the 185th most commonly prescribed medication in the United States, with more than 2 million prescriptions.[21][22]

Medical uses

Asthma

Budesonide is given by

corticosteroids and those who may benefit from a systemic dose reduction.[23]

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.[24] A Cochrane review found evidence for up to three months (but not longer) of maintenance of remission in Crohn's disease.[25]

Budesonide assists in the induction of remission in people with active ulcerative colitis.[26]

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.[14][27]

Allergic rhinitis

Budesonide in the form of nasal sprays is a treatment for allergic rhinitis.[28]

Eosinophilic esophagitis

Topical budesonide has considerable effects in eosinophilic esophagitis.[29] For this use, it is formulated as a tablet that disperses in the mouth, and sold under the brand name Jorveza.[30]

Berger's disease

Budesonide (Tarpeyo (US); Kinpeygo (EU, UK)) is indicated to reduce proteinuria (increased protein levels in the urine) in adults with primary immunoglobulin A (IgA) nephropathy (Berger's disease) at risk of rapid disease progression.[3][31][7]

Side effects

Nasal budesonide inhalers have been associated with a number of side effects.

menstrual periods, severe acne, and on rare occasions, behavioral changes (mostly affecting children).[32]

Contraindications

Budesonide is contraindicated as a primary treatment of

status asthmaticus or other acute episode of asthma where intensive measures are required.[35] It is also contraindicated for patients who have hypersensitivity to budesonide.[36]

Interactions

Those taking tablets or capsules orally should avoid grapefruit and grapefruit juice[37][38] and echinacea.[39]: 160 

Also, high-fat meals delay absorption but do not impede absorption.[40]

Pharmacology

Budesonide is an agonist of glucocorticoid receptors. Among its effects are:

Pharmacokinetics

Chemistry

See also: List of corticosteroids and List of corticosteroid cyclic ketals

Budesonide, also known as 11β,21-dihydroxy-16α,17α-(butylidenebis(oxy))pregna-1,4-diene-3,20-dione, is a

derivative of prednisolone (11β,17α,21-trihydroxypregna-1,4-diene-3,20-dione).[44][45]

Stereoisomerism

Budesonide
(2 stereoisomers)
(R)-Budesonid
(22R)-configuration 		(S)-Budesonid
(22S)-configuration

Society and culture

Economics

In 2019, generic budesonide was listed as being involved in Teva's price fixing scheme in the United States.[46]

Legal status

In May 2022, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a conditional marketing authorization for the medicinal product Kinpeygo, intended for the treatment of primary immunoglobulin A nephropathy.[47] The applicant for this medicinal product is Calliditas Therapeutics AB.[47] Kinpeygo is a hybrid medicine of Entocort which has been authorised in the EU since 2 April 1992.[47] Kinpeygo contains the same active substance as Entocort but has a different formulation and a different indication.[47] Kinpeygo was approved for medical use in the European Union in July 2022.[7][48]

Brand names

Inhaler for a powder based on budesonide and formoterol

Aeronide (TH); Aquacort (DE); B Cort (CO); Bronex (PH); Budair (MY); Budecort DP (MY); Budenofalk (DE, GB, HK, KP, PH, SG); Budeson (AR); Budeson Aqua (AR); BudeSpray (TH); Budiair (KP); Budicort Respules (IL); Budinide (KSA); Bunase (TH); Busonid (BR); Clebudan (CN); Cortiment (CA, GB, AU); Cycortide (HK); Denecort (PH); Duasma (TW); Eltair (MY); Entocort (AR, AT, BE, BR, CH, CZ, DK, FI, FR, GB, HK, IE, IL, IT, KP, NL, NO, PL, PT, SE, TR);[39]: 13  Giona Easyhaler (MY, SG, TH); Inflammide (PE); Miflonid (CZ); Miflonide (BE, DE, IL, IT, NZ, PT); Neumocort (PY); Novopulmon (DE, FR); Pulmicon Susp for Nebulizer (KP); Pulmicort (AT, BE, BG, BR, CH, CL, CN, CO, CR, CZ, DE, DK, DO, EE, FI, FR, GB, GR, GT, HN, HR, ID, IN, NI, NL, NO, PA, PK, PL, PT, RU, SE, SV, TR, TW, UY, VE, ZA);[39]: 13  Pulmicort Nasal Turbohaler (CL, KE, MU, NG); Pulmicort Turbuhaler (KE, MU, NG); Rafton (FR); Rhinocort (AU); Rhinocort Aqua (HK);[49] Rhinoside (GR); Symbicort (DE, FR, UK, US, ZA) Uceris (US).

Research

COVID-19

Budesonide was recommended in April 2021 by the UK's NHS to treat COVID-19 on a case-by-case basis for those aged 50 years of age and older.[50] After a University of Oxford research team found in a trial with 1,700 patients that budesonide could benefit many people over 50 with COVID-19 symptoms, it was recommended from 12 April 2021, by the National Health Service in the UK for general practitioners (GPs) to treat COVID-19 on a case-by-case basis.[51][52] Results of a large-scale trial published in August 2021 suggest that inhaled budesonide improves the time of recovery and people's well-being during the recovery process.[53][54] Inhalational budesonide was added to the recommended treatment for cases of COVID-19 in India in April 2021.[55][56] The NIH recommendation was withdrawn in December 2021 citing the need for more research.[57][58]

References

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  4. ^ "Pulmicort Flexhaler- budesonide aerosol, powder". DailyMed. Archived from the original on 19 September 2021. Retrieved 24 December 2021.
  5. ^ "Eohilia- budesonide suspension". DailyMed. 9 February 2024. Archived from the original on 26 February 2024. Retrieved 26 February 2024.
  6. ^ "Jorveza EPAR". European Medicines Agency (EMA). 17 September 2018. Archived from the original on 4 March 2023. Retrieved 3 March 2023.
  7. ^ a b c "Kinpeygo EPAR". European Medicines Agency (EMA). 17 May 2022. Archived from the original on 4 March 2023. Retrieved 3 March 2023.
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External links

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