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Hydrocortisone

From Wikipedia, the free encyclopedia
Glucocorticoid and mineralocorticoid hormone Cortisol supplied as a medication

Pharmaceutical compound
Hydrocortisone
Clinical data
Trade namesCortef, others[1]
Other namesCortisol; 11β,17α,21-Trihydroxypregn-4-ene-3,20-dione; 11β,17α,21-Trihydroxyprogesterone
AHFS/Drugs.comMonograph
MedlinePlusa682206
License data
Pregnancy
category
Routes of
administration
By mouth,intravenous,topical,rectal
Drug classGlucocorticoid;Mineralocorticoid
ATC code
Legal status
Legal status
Pharmacokinetic data
BioavailabilityOral: 96 ± 20%[12][13]
Protein binding92 ± 2% (92–93%)[12][13]
Metabolism11β-HSDsTooltip 11β-Hydroxysteroid dehydrogenases, others[13]
MetabolitesCortisone, others[13]
Onset of actionOral: 1.2 ± 0.4 hours (Tmax)[12]
Eliminationhalf-life1.2–2.0 hours[12][13]
Duration of action8–12 hours[14]
Identifiers
  • (8S,9S,10R,11S,13S,14S,17R)-11,17-Dihydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-3-one
CAS Number
PubChemCID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
FormulaC21H30O5
Molar mass362.466 g·mol−1
3D model (JSmol)
  • O=C4\C=C2/[C@]([C@H]1[C@@H](O)C[C@@]3([C@@](O)(C(=O)CO)CC[C@H]3[C@@H]1CC2)C)(C)CC4
  • InChI=1S/C21H30O5/c1-19-7-5-13(23)9-12(19)3-4-14-15-6-8-21(26,17(25)11-22)20(15,2)10-16(24)18(14)19/h9,14-16,18,22,24,26H,3-8,10-11H2,1-2H3/t14-,15-,16-,18+,19-,20-,21-/m0/s1 checkY
  • Key:JYGXADMDTFJGBT-VWUMJDOOSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Hydrocortisone is the name for the hormonecortisol when supplied as a medication.[15] It is acorticosteroid and works as ananti-inflammatory and byimmune suppression.[1] Uses include conditions such asadrenocortical insufficiency,adrenogenital syndrome,high blood calcium,thyroiditis,rheumatoid arthritis,dermatitis,asthma, andCOPD.[1] It is the treatment of choice for adrenocortical insufficiency.[16] It can be givenby mouth,topically,rectally or byinjection.[1] Stopping treatment after long-term use should be done slowly.[1]

Common side effects may include mood changes,increased appetite,hyperglycemia,hypertension, andedema (swelling).[17] With long-term use, common side effects includeosteoporosis, adrenal insufficiency,upset stomach,physical weakness, easybruising, andcandidiasis (yeast infections).[1][17] It is unclear if it is safe for use duringpregnancy.[18]

Hydrocortisone was patented in 1936 and approved for medical use in 1941.[19][20] It is on theWorld Health Organization's List of Essential Medicines.[21] It is available as ageneric medication.[1] In 2023, it was the 182nd most commonly prescribed medication in the United States, with more than 2 million prescriptions.[22][23]

Medical uses

[edit]

Hydrocortisone is the pharmaceutical term for cortisol used inoral administration,intravenous injection, ortopical application. It is used as animmunosuppressive drug, given byinjection in the treatment of severeallergic reactions such asanaphylaxis andangioedema, in place ofprednisolone in patients needing steroid treatment but unable to take oral medication, and perioperatively in patients on long-term steroid treatment to prevent anadrenal crisis. It may also be injected into inflamed joints resulting from diseases such asgout.[citation needed]

It may be used topically for allergicrashes,eczema,psoriasis,itching, and otherinflammatory skin conditions.Topical hydrocortisone creams and ointments are available in most countries without prescription in strengths ranging from 0.05% to 2.5% (depending on local regulations) with stronger forms available by prescription only.[citation needed]

It may also be used rectally in suppositories to relieve theswelling,itch, andirritation inhemorrhoids.[7]

It may be used as an acetate form (hydrocortisone acetate), which has slightly different pharmacokinetics and pharmacodynamics.[7][24]

  • Cortisol for injection
    Cortisol for injection
  • A tube of hydrocortisone cream, purchased over-the-counter
    A tube of hydrocortisone cream, purchasedover-the-counter
  • Hydrocortisone 10 mg oral tablets (depicted a package for Russian market)
    Hydrocortisone 10 mg oral tablets (depicted a package for Russian market)

Pharmacology

[edit]

Pharmacodynamics

[edit]

Hydrocortisone is acorticosteroid, acting specifically as both aglucocorticoid and as amineralocorticoid. That is, it is anagonist of theglucocorticoid andmineralocorticoid receptors.[citation needed]

Hydrocortisone has lowpotency relative tosynthetic corticosteroids.[14] Compared to hydrocortisone,prednisolone is about 4 times aspotent anddexamethasone about 40 times as potent in terms ofanti-inflammatory effect.[25] Prednisolone can also be used as cortisol replacement, and at replacement dose levels (rather than anti-inflammatory levels), prednisolone is about 8 times more potent than cortisol.[26] The equivalent doses and relative potencies of hydrocortisone compared to various other synthetic corticosteroids have also been reviewed and summarized.[14]

Theendogenousproduction rate of cortisol is approximately 5.7 to 9.9 mg/m2 per day, which corresponds to an oral hydrocortisone dose of approximately 15 to 20 mg/day (for a 70-kg person).[27][28] One review described daily cortisol production of 10 mg in healthy volunteers and reported that daily cortisol production could increase up to 400 mg in conditions of severestress (e.g.,surgery).[12]

The total and/or free concentrations of cortisol/hydrocortisone required for various glucocorticoid effects have been determined.[12]

Pharmacokinetics

[edit]

Absorption

[edit]

Thebioavailability oforal hydrocortisone is about 96% ± 20% (SD).[12][13] The pharmacokinetics of hydrocortisone are non-linear.[12] Thepeak level of oral hydrocortisone is 15.3 ± 2.9 (SD) μg/L per 1 mg dose.[12] Thetime to peak concentrations of oral hydrocortisone is 1.2 ± 0.4 (SD) hours.[12]

Thetopicalpercutaneousabsorption of hydrocortisone varies widely depending on experimental circumstances and has been reported to range from 0.5 to 14.9% in different studies.[29] Some skin application sites, like thescrotum andvulva, absorb hydrocortisone much more efficiently than other application sites, like theforearm.[29][30][31] In one study, the amount of hydrocortisone absorbed ranged from 0.2% to 36.2% depending on the application site, with the ball of the foot having the lowest absorption and the scrotum having the highest absorption.[31] The absorption of hydrocortisone by the vulva has ranged from 4.4 to 8.1%, relative to 1.3 to 2.8% for the arm, in different studies and subjects.[31][32][33]

Distribution

[edit]

Most cortisol in the blood (all but about 4%) isbound to proteins, includingcorticosteroid binding globulin (CBG) andserum albumin. A pharmacokinetic review stated that 92% ± 2% (SD) (92–93%) of hydrocortisone is plasma protein-bound.[12] Free cortisol passes easily through cellular membranes.[34] Inside cells it interacts withcorticosteroid receptors.[35]

Metabolism

[edit]

Hydrocortisone ismetabolized by11β-hydroxysteroid dehydrogenases (11β-HSDs) intocortisone, an inactivemetabolite.[13][12] It is additionally5α-,5β-, and3α-reduced intodihydrocortisols,dihydrocortisones,tetrahydrocortisols, andtetrahydrocortisones.[36][12][13]

Elimination

[edit]

Theelimination half-life of hydrocortisone ranges from about 1.2 to 2.0 (SD) hours, with an average of around 1.5 hours, regardless oforal versusparenteral administration.[12][13] Theduration of action ofsystemic hydrocortisone has been listed as 8 to 12 hours.[14]

Chemistry

[edit]
See also:List of corticosteroids andList of corticosteroid esters § Hydrocortisone esters

Hydrocortisone, also known as 11β,17α,21-trihydroxypregn-4-ene-3,20-dione, is anaturally occurringpregnanesteroid.[37][38] A variety ofhydrocortisone esters exist and have been marketed for medical use.[37][38]

Society and culture

[edit]

Legal status

[edit]

In March 2021, theCommittee for Medicinal Products for Human Use (CHMP) of theEuropean Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Efmody, intended for the treatment of congenital adrenal hyperplasia (CAH) in people aged twelve years and older.[39] The applicant for this medicinal product is Diurnal Europe BV.[39] Hydrocortisone (Efmody) was approved for medical use in the European Union, in May 2021, for the treatment ofcongenital adrenal hyperplasia (CAH) in people aged twelve years and older.[10]

Anti-competitive practices

[edit]

In the UK, theCompetition and Markets Authority (CMA) concluded an investigation into the supply of hydrocortisone tablets, finding that from October 2008 onwards, drug suppliers Auden McKenzie andActavis plc had charged "excessive and unfair prices" for 10mg and 20mg tablets and entered into agreements with potential competitors, paying companies who agreed not to enter the hydrocortisone market and enabling Auden McKenzie and Actavis to supply the drugs as "generic" rather than branded products and thereby escape price controls until eventually other companies entered the market. Auden and Actavis overcharged the UK'sNational Health Service for over ten years. Fines totalling over £255m were levied against the companies involved in this breach ofcompetition law.[40]

Research

[edit]

Chronic fatigue syndrome

[edit]

Cortisol levels have been found to be altered in people withmyalgic encephalomyelitis/chronic fatigue syndrome (ME/CFS).[41][42][43] Hydrocortisone has been clinically studied in the treatment of ME/CFS.[44][45][46] A 2016systematic review found that it had been assessed for this purpose in six clinical studies.[44] Its clinical effectiveness was conflicting in the studies, ranging from not effective, to slightly or mildly effective, to moderately effective.[44] Four of the studies came from one research group.[44] The systematic review called for higher-quality trials.[44] A 2015 systematic review found that the clinical data on hydrocortisone for ME/CFS was inconclusive.[47]

COVID-19

[edit]

Hydrocortisone was found to be effective in reducing mortality rate of critically illCOVID-19 patients when compared to other usual care or a placebo.[48]

References

[edit]
  1. ^abcdefg"Hydrocortisone".Drugs.com. American Society of Health-System Pharmacists. 9 February 2015.Archived from the original on 20 September 2016. Retrieved30 August 2016.
  2. ^"Prescribing medicines in pregnancy database".Therapeutic Goods Administration (TGA).Archived from the original on 20 December 2016. Retrieved21 February 2021.
  3. ^"Hydrocortisone Notice of enforcement policy"(PDF). FDA.Archived(PDF) from the original on 12 March 2023. Retrieved31 December 2022.
  4. ^"Ala-cort- hydrocortisone cream".DailyMed.Archived from the original on 27 October 2020. Retrieved21 February 2021.
  5. ^"Ala-scalp- hydrocortisone lotion".DailyMed.Archived from the original on 21 April 2021. Retrieved21 February 2021.
  6. ^"Alkindi Sprinkle- hydrocortisone granule".DailyMed.Archived from the original on 10 February 2022. Retrieved21 February 2021.
  7. ^abc"Anusol HC- hydrocortisone acetate suppository".DailyMed.Archived from the original on 10 February 2022. Retrieved21 February 2021.
  8. ^"Cortef- hydrocortisone tablet".DailyMed.Archived from the original on 17 April 2021. Retrieved21 February 2021.
  9. ^"Khindivi- hydrocortisone solution".DailyMed. 2 July 2025. Retrieved6 July 2025.
  10. ^ab"Efmody EPAR".European Medicines Agency (EMA). 24 March 2021.Archived from the original on 14 June 2021. Retrieved14 June 2021. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  11. ^"Efmody Product information".Union Register of medicinal products.Archived from the original on 5 March 2023. Retrieved3 March 2023.
  12. ^abcdefghijklmnCzock D, Keller F, Rasche FM, Häussler U (2005). "Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids".Clinical Pharmacokinetics.44 (1):61–98.doi:10.2165/00003088-200544010-00003.PMID 15634032.S2CID 24458998.
  13. ^abcdefghiLennernäs H, Skrtic S, Johannsson G (June 2008). "Replacement therapy of oral hydrocortisone in adrenal insufficiency: the influence of gastrointestinal factors".Expert Opinion on Drug Metabolism & Toxicology.4 (6):749–758.doi:10.1517/17425255.4.6.749.PMID 18611115.S2CID 73248541.
  14. ^abcdLiu D, Ahmet A, Ward L, Krishnamoorthy P, Mandelcorn ED, Leigh R, et al. (August 2013)."A practical guide to the monitoring and management of the complications of systemic corticosteroid therapy".Allergy Asthma Clin Immunol.9 (1) 30.doi:10.1186/1710-1492-9-30.PMC 3765115.PMID 23947590.
  15. ^Becker KL (2001).Principles and Practice of Endocrinology and Metabolism. Lippincott Williams & Wilkins. p. 762.ISBN 978-0-7817-1750-2.Archived from the original on 14 September 2016.
  16. ^Hamilton R (2015).Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 202.ISBN 978-1-284-05756-0.
  17. ^ab"Hydrocortisone: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing - WebMD".www.webmd.com. Retrieved10 June 2025.
  18. ^"Hydrocortisone Pregnancy and Breastfeeding Warnings".Drugs.com.Archived from the original on 20 September 2016. Retrieved1 September 2016.
  19. ^U.S. patent 2,183,589
  20. ^Fischer J, Ganellin CR (2006).Analogue-based Drug Discovery. John Wiley & Sons. p. 484.ISBN 978-3-527-60749-5.Archived from the original on 10 January 2023. Retrieved7 September 2020.
  21. ^World Health Organization (2019).World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization.hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
  22. ^"Top 300 of 2023".ClinCalc.Archived from the original on 12 August 2025. Retrieved12 August 2025.
  23. ^"Hydrocortisone Drug Usage Statistics, United States, 2013 - 2023".ClinCalc. Retrieved19 August 2025.
  24. ^Leite FM, Longui CA, Kochi C, Faria CD, Borghi M, Calliari LE, et al. (February 2008)."[Comparative study of prednisolone versus hydrocortisone acetate for treatment of patients with the classic congenital adrenal hyperplasia due to 21-hydroxylase deficiency]".Arq Bras Endocrinol Metabol (in Portuguese).52 (1):101–8.doi:10.1590/s0004-27302008000100014.PMID 18345402.
  25. ^"Dexamethasone". drugs.com.Archived from the original on 21 June 2013. Retrieved14 June 2013.
  26. ^Caldato MC, Fernandes VT, Kater CE (October 2004)."One-year clinical evaluation of single morning dose prednisolone therapy for 21-hydroxylase deficiency".Arquivos Brasileiros de Endocrinologia e Metabologia.48 (5):705–712.doi:10.1590/S0004-27302004000500017.PMID 15761542.S2CID 13986916.
  27. ^Arvat E, Falorni A (2016).Cortisol Excess and Insufficiency. Frontiers of Hormone Research. S. Karger AG. p. 1-PA61.ISBN 978-3-318-05840-6.Archived from the original on 27 April 2023. Retrieved10 April 2023.
  28. ^Ghizzoni L, Cappa M, Chrousos GP, Loche S, Maghnie M, eds. (2011).Pediatric Adrenal Diseases: Workshop, May 16-18, 2010, Turin (Italy). Karger Medical and Scientific Publishers. pp. 174–.ISBN 978-3-8055-9643-5.OCLC 1020003143.Archived from the original on 10 April 2023. Retrieved10 April 2023.
  29. ^abWester RC, Maibach HI (1993). "Percutaneous absorption of topical corticosteroids".Current Problems in Dermatology.21:45–60.doi:10.1159/000422362.ISBN 978-3-8055-5712-2.PMID 8299376.
  30. ^Bormann JL, Maibach HI (September 2020). "Effects of anatomical location onin vivo percutaneous penetration in man".Cutaneous and Ocular Toxicology.39 (3):213–222.doi:10.1080/15569527.2020.1787434.PMID 32643443.S2CID 220439810.
  31. ^abcWester RC, Maibach HI (8 June 2021). "Regional Variation in Percutaneous Absorption".Percutaneous Absorption. CRC Press. pp. 165–174.doi:10.1201/9780429202971-11.ISBN 978-0-429-20297-1.S2CID 132864025.
  32. ^Britz MB, Maibach HI, Anjo DM (1980). "Human percutaneous penetration of hydrocortisone: the vulva".Archives of Dermatological Research.267 (3):313–316.doi:10.1007/BF00403852.PMID 7406539.S2CID 33367289.
  33. ^Oriba HA, Bucks DA, Maibach HI (February 1996). "Percutaneous absorption of hydrocortisone and testosterone on the vulva and forearm: effect of the menopause and site".The British Journal of Dermatology.134 (2):229–233.doi:10.1111/j.1365-2133.1996.tb07606.x.PMID 8746334.S2CID 30076779.
  34. ^Charmandari E, Johnston A, Brook CG, Hindmarsh PC (April 2001)."Bioavailability of oral hydrocortisone in patients with congenital adrenal hyperplasia due to 21-hydroxylase deficiency".The Journal of Endocrinology.169 (1):65–70.doi:10.1677/joe.0.1690065.PMID 11250647.
  35. ^Boron WF, Boulpaep EL (2011).Medical Physiology (2nd ed.). Philadelphia: Saunders.ISBN 978-1-4377-1753-2.
  36. ^Nikolaou N, Hodson L, Tomlinson JW (March 2021). "The role of 5-reduction in physiology and metabolic disease: evidence from cellular, pre-clinical and human studies".The Journal of Steroid Biochemistry and Molecular Biology.207 105808.doi:10.1016/j.jsbmb.2021.105808.PMID 33418075.S2CID 230716310.
  37. ^abElks J (14 November 2014).The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. p. 316.ISBN 978-1-4757-2085-3.Archived from the original on 8 September 2017.
  38. ^abIndex Nominum 2000: International Drug Directory. Taylor & Francis. 2000. pp. 524–.ISBN 978-3-88763-075-1.Archived from the original on 10 January 2023. Retrieved19 June 2020.
  39. ^ab"Efmody: Pending EC decision".European Medicines Agency (EMA). 25 March 2021. Archived fromthe original on 4 May 2021. Retrieved27 March 2021. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  40. ^This article contains OGL licensed text This article incorporates text published under the BritishOpen Government Licence: Competition and Markets Authority,Decision: Hydrocortisone tablets. Excessive and unfair pricing and Anti-competitive agreements, published 31 March 2022, accessed 1 June 2023
  41. ^Taccori A, Maksoud R, Eaton-Fitch N, Patel M, Marshall-Gradisnik S (July 2023)."A systematic review and meta-analysis of urinary biomarkers in myalgic encephalomyelitis/chronic fatigue syndrome (ME/CFS)".J Transl Med.21 (1) 440.doi:10.1186/s12967-023-04295-0.PMC 10320942.PMID 37408028.
  42. ^Tak LM, Cleare AJ, Ormel J, Manoharan A, Kok IC, Wessely S, et al. (May 2011). "Meta-analysis and meta-regression of hypothalamic-pituitary-adrenal axis activity in functional somatic disorders".Biol Psychol.87 (2):183–194.doi:10.1016/j.biopsycho.2011.02.002.PMID 21315796.
  43. ^Powell DJ, Liossi C, Moss-Morris R, Schlotz W (November 2013)."Unstimulated cortisol secretory activity in everyday life and its relationship with fatigue and chronic fatigue syndrome: a systematic review and subset meta-analysis".Psychoneuroendocrinology.38 (11):2405–2422.doi:10.1016/j.psyneuen.2013.07.004.PMID 23916911.
  44. ^abcdeCollatz A, Johnston SC, Staines DR, Marshall-Gradisnik SM (June 2016). "A Systematic Review of Drug Therapies for Chronic Fatigue Syndrome/Myalgic Encephalomyelitis".Clin Ther.38 (6): 1263–1271.e9.doi:10.1016/j.clinthera.2016.04.038.PMID 27229907.
  45. ^Cleare AJ, Heap E, Malhi GS, Wessely S, O'Keane V, Miell J (February 1999). "Low-dose hydrocortisone in chronic fatigue syndrome: a randomised crossover trial".Lancet.353 (9151):455–458.doi:10.1016/S0140-6736(98)04074-4.PMID 9989716.
  46. ^McKenzie R, O'Fallon A, Dale J, Demitrack M, Sharma G, Deloria M, et al. (1998). "Low-dose hydrocortisone for treatment of chronic fatigue syndrome: a randomized controlled trial".JAMA.280 (12):1061–1066.doi:10.1001/jama.280.12.1061.PMID 9757853.
  47. ^Smith ME, Haney E, McDonagh M, Pappas M, Daeges M, Wasson N, et al. (June 2015). "Treatment of Myalgic Encephalomyelitis/Chronic Fatigue Syndrome: A Systematic Review for a National Institutes of Health Pathways to Prevention Workshop".Ann Intern Med.162 (12):841–850.doi:10.7326/M15-0114.PMID 26075755.
  48. ^Sterne JA, Murthy S, Diaz JV, Slutsky AS, Villar J, Angus DC, et al. (October 2020)."Association Between Administration of Systemic Corticosteroids and Mortality Among Critically Ill Patients With COVID-19: A Meta-analysis".JAMA.324 (13):1330–1341.doi:10.1001/jama.2020.17023.PMC 7489434.PMID 32876694.
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