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User:Benadryl Submarine/Budesonide

< User:Benadryl Submarine

Budesonide, sold under the brand name Pulmicort(,) among others, is a steroid medication.[1] It is available as an inhaler, nebulization solution, pill, nasal spray, and rectal forms.[1][2] The inhaled form is used in the long-term management of asthma and chronic obstructive pulmonary disease (COPD).[1][3][4] The nasal spray is used for allergic rhinitis and nasal polyps.[2][5] Modified-release pills or capsules and rectal forms may be used for inflammatory bowel disease including Crohn's disease, ulcerative colitis, and microscopic colitis.[6][7][8]

Contraindications edit

Budesonide is contraindicated in people with:

  • Known hypersensitivity to budesonide or any component of the formulation.[9][10]
  • Status asthmaticus or other acute episodes of asthma which would require intensive, immediate measures.[9][11]

In Canada, there are additional contraindications labeled for Budesonide for people with:

  • Systemic or local bacterial, fungal and viral infections.[9]
  • Active or quiescent pulmonary tuberculosis.[9]

Side effects edit

Nasal budesonide inhalers have been associated with a number of side effects.[12][13] 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.[14] 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 (mostly affecting children).[12]

Overdose edit

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 can cause systemic toxicity that manifests as hypercortisolism.[9] 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.[15][16]

Interactions edit

Budesonide is mainly metabolized in the liver by the enzyme CYP34A[9][17]. Drugs that are CYP3A4 inhibitors such as ketoconazole, clarithromycin, ritonavir, and nefazodone, among many others, may inhibit the metabolism of Budesonide, prolonging its elimination and leading to possible increased rates of corticosteroid adverse effects due to unwanted drug accumulation[9][18]. Grapefruit is also a potent inhibitor of CYP3A4, and its consumption is not recommended while on budesonide treatment[9][19].

___an aside___

*removing high-fat meal delays absorption from interactions. Slowing gastric emptying and therefore delaying absorption without impeding overall absorption is not an interaction specific to Budesonide nor irregular. However I'll add this part to the pharmacokinetics section.

*removing information regarding echinacea. Theoretically, it is thought to have immunostimulant properties that may antagonize the pharmacologic effects of immunosuppressants. However, I could not find any solid clinical cases of drug interactions that have been reported for Budesonide or corticosteroids, and Lexi-comp shows no interactions. Interactions Between Herbal Medicines and Prescribed Drugs states "the currently available evidence suggests that echinacea is unlikely to pose serious health threats for patients combining it with conventional drugs". Most information advocating for the possible interaction stem around 1990-2000 and state their recommendation is theoretical and not based on clinical cases. Drugs.com doesn't include the interaction either.

Society and culture edit

 
Dry powder Inhaler that contains a combination of budesonide and formoterol.

Brand names edit

Budesonide is a drug that is marketed under various brand and generic names internationally, some notable examples for each formulation are listed here;

Inhalation: Pulmicort; Pulmicort Flexhaler, Pulmicort Nebuamp, Pulmicort Turbuhaler, TARO-Budesonide, TEVA-Budesonide, Novolizer budesonid meda, Budenova.[17][20]

Systemic (oral pills): Tarpeyo, Uceris, Eohilia, Cortiment, Entocort Jorveza.[21][20]

Nasal: MYLAN-Budesonide AQ, Rhinocort Aqua, Formancis.[22][20]

Topical: Entocort, Uceris, Budenofalk.[23][20]

Economics edit

In 2019, generic budesonide was listed as being involved in Teva's price fixing scheme in the United States.[24]

Legal status edit

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.[25] The applicant for this medicinal product is Calliditas Therapeutics AB.[25] Kinpeygo is a hybrid medicine of Entocort which has been authorised in the EU since 2 April 1992.[25] Kinpeygo contains the same active substance as Entocort but has a different formulation and a different indication.[25] Kinpeygo was approved for medical use in the European Union in July 2022.[26][27]

Pharmacology edit

Main article: Glucocorticoid § Pharmacology

Mechanism of action edit

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

Pharmacokinetics edit

Different pharmacokinetic proprieties can be seen in the absorption of budesonide depending on how it is formulated. When taken as an extended-release oral capsule, budesonide has an oral bioavailability of 9–21% and reaches peak plasma concentrations (Cmax) within 2–8 hours.[21] A high fat meal when taken with the capsule can lengthen the time it takes to reach Cmax by another 2.3 hours, but will not have any other affects on the the pharmacokinetics properties of budesonide.[20] When inhaled through an metered dose inhaler, 34% of budesonide is deposited in the lung with a bioavailability of 39% and reaches Cmax within 10 minutes.[20][17] When nebulized, budesonide has an bioavailability of 6% and reaches Cmax within 1–3 hours.[17][20] When formulated as a rectal foam, budesonide has an bioavailability of 3% to 27% and reaches Cmax around 1.5 hours.[23]

The plasma protein binding of budesonide is around 85-90%, with an apparent volume of distribution of 2.2-3.9L/kg.[20][21] Budesonide is 80-90% metabolized at first pass in the liver by the hepatocytic cytochrome P450 isoenzyme 3A4 (CYP3A4) 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.[20] 60% of budesonide is excreted is through the urine as its metabolites, no unchanged budesonide is detectable in urine.[20] The average elimination half-life in plasma is between 2-3.6 hours.[20]

  1. ^ a b c "Budesonide". The American Society of Health-System Pharmacists. Archived from the original on 28 November 2015. Retrieved 2 December 2015.
  2. ^ a b "Budesonide eent". The American Society of Health-System Pharmacists. Archived from the original on 8 December 2015. Retrieved 2 December 2015.
  3. ^ De Coster DA, Jones M (2014). "Tailoring of corticosteroids in COPD management". Current Respiratory Care Reports. 3 (3): 121–132. doi:10.1007/s13665-014-0084-2. PMC 4113685. PMID 25089228.
  4. ^ Christophi GP, Rengarajan A, Ciorba MA (2016). "Rectal budesonide and mesalamine formulations in active ulcerative proctosigmoiditis: efficacy, tolerance, and treatment approach". Clinical and Experimental Gastroenterology. 9: 125–30. doi:10.2147/CEG.S80237. PMC 4876845. PMID 27274301.
  5. ^ Rudmik L, Schlosser RJ, Smith TL, Soler ZM (July 2012). "Impact of topical nasal steroid therapy on symptoms of nasal polyposis: a meta-analysis". The Laryngoscope. 122 (7): 1431–7. doi:10.1002/lary.23259. PMID 22410935. S2CID 25637461.
  6. ^ Silverman J, Otley A (July 2011). "Budesonide in the treatment of inflammatory bowel disease". Expert Review of Clinical Immunology. 7 (4): 419–28. doi:10.1586/eci.11.34. PMID 21790284. S2CID 32892611.
  7. ^ Pardi DS, Tremaine WJ, Carrasco-Labra A (January 2016). "American Gastroenterological Association Institute Technical Review on the Medical Management of Microscopic Colitis". Gastroenterology. 150 (1): 247–274.e11. doi:10.1053/j.gastro.2015.11.006. PMID 26584602.
  8. ^ British national formulary: BNF 58 (58 ed.). British Medical Association. 2009. pp. 56–57. ISBN 9780857111562.
  9. ^ a b c d e f g h Kalola, Urvashi K.; Ambati, Shashikanth (2024), "Budesonide", StatPearls, Treasure Island (FL): StatPearls Publishing, PMID 33085348, retrieved 2024-04-28
  10. ^ Todd, G R G (2002-12-01). "Survey of adrenal crisis associated with inhaled corticosteroids in the United Kingdom". Archives of Disease in Childhood. 87 (6): 457–461. doi:10.1136/adc.87.6.457.
  11. ^ Todd GR, Acerini CL, Buck JJ, Murphy NP, Ross-Russell R, Warner JT, McCance DR (2002). "Acute Adrenal Crisis in Asthmatics Treated With High-Dose Fluticasone Propionate". Eur Respir J. 19 (6): 1207–9. doi:10.1183/09031936.02.00274402. PMID 12108877.
  12. ^ a b "GENERIC NAME: BUDESONIDE - NASAL AEROSOL INHALER (byou-DESS-oh-nide)". eMedicineHealth. Archived from the original on 6 November 2008.
  13. ^ "What are the possible side effects of budesonide nasal (Childrens Rhinocort Allergy, Rhinocort Allergy, Rhinocort Aqua)?". eMedicineHealth. Archived from the original on 6 August 2020. Retrieved 25 August 2020.
  14. ^ "Budesonide: CMDh scientific conclusions and grounds for variation, amendments to the product information and timetable for the implementation - PSUSA/00000449/201604" (PDF). European Medicines Agency (EMA). 10 March 2017. Archived (PDF) from the original on 8 September 2017. Retrieved 19 May 2017.
  15. ^ "Budesonide (Oral Route) Precautions - Mayo Clinic". www.mayoclinic.org. Retrieved 2024-05-03.
  16. ^ "Budesonide inhalation Uses, Side Effects & Warnings". Drugs.com. Retrieved 2024-05-03.
  17. ^ a b c d "Budesonide (Oral Inhalation)". Lexi-Drugs. UpToDate Lexidrug. UpToDate Inc. April 28, 2024.
  18. ^ Ajimura, Chanelle M.; Jagan, Nikhil; Morrow, Lee E.; Malesker, Mark A. (December 2018). "Drug Interactions With Oral Inhaled Medications". Journal of Pharmacy Technology. 34 (6): 273–280. doi:10.1177/8755122518788809. ISSN 8755-1225. PMC 6231282. PMID 34861014.{{cite journal}}: CS1 maint: PMC format (link)
  19. ^ Baily DG (2010). "Grapefruit and Other Fruit Juices Interactions with Medicines". In Boullata JI, Armenti VT (eds.). Handbook of drug-nutrient interactions (2nd ed.). New York, NY: Humana Press. p. 282. ISBN 978-1-60327-362-6.
  20. ^ a b c d e f g h i j k "Budesonide". go.drugbank.com. Retrieved 2024-04-28.
  21. ^ a b c "Budesonide (Systemic)". Lexi-Drugs. UpToDate Lexidrug. UpToDate Inc. April 28, 2024.
  22. ^ "Budesonide (Nasal)". Lexi-Drugs. UpToDate Lexidrug. UpToDate Inc. April 28, 2024.
  23. ^ a b "Budesonide (Topical)". Lexi-Drugs. UpToDate Lexidrug. UpToDate Inc. April 28, 2024.
  24. ^ Murphy H (11 May 2019). "Teva and Other Generic Drugmakers Inflated Prices Up to 1,000%, State Prosecutors Say". The New York Times. Archived from the original on 30 May 2020. Retrieved 27 May 2020.
  25. ^ a b c d "Kinpeygo: Pending EC decision". European Medicines Agency (EMA). 20 May 2022. Archived from the original on 20 May 2022. Retrieved 20 May 2022. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  26. ^ "Kinpeygo EPAR". European Medicines Agency (EMA). 17 May 2022. Archived from the original on 4 March 2023. Retrieved 3 March 2023.
  27. ^ "Kinpeygo Product information". Union Register of medicinal products. Archived from the original on 4 March 2023. Retrieved 3 March 2023.
  28. ^ a b Kizior RJ, Hodgson BB (21 February 2018). Saunders Nursing Drug Handbook 2019 E-Book. Elsevier Health Sciences. p. 160. ISBN 978-0-323-61257-9. Archived from the original on 30 April 2024. Retrieved 5 October 2020.
  29. ^ Skidmore-Roth L, Richardson F (9 July 2020). Mosby's Canadian Nursing Drug Reference - E-Book. Elsevier Health Sciences. p. 187. ISBN 978-1-77172-084-7. Archived from the original on 11 March 2024. Retrieved 5 October 2020.
  30. ^ Gavins, Felicity; Flower, Roderick J. (2008-01-01), Enna, S. J.; Bylund, David B. (eds.), "Budesonide", xPharm: The Comprehensive Pharmacology Reference, New York: Elsevier, pp. 1–5, ISBN 978-0-08-055232-3, retrieved 2024-05-03
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