Hydrocortisone

Source: Wikipedia, the free encyclopedia.

Hydrocortisone
Clinical data
Trade namesA-hydrocort, Cortef, Solu-cortef, 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
intravenous, topical, rectal
Drug classCorticosteroid; Glucocorticoid; Mineralocorticoid
ATC code
Legal status
Legal status
Tmax)[11]
Elimination half-life1.2–2.0 hours[11][12]
Duration of action8–12 hours[13]
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
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 hormone

COPD.[1] It is the treatment of choice for adrenocortical insufficiency.[15] It can be given by mouth, topically, or by injection.[1] Stopping treatment after long-term use should be done slowly.[1]

Side effects may include mood changes, increased risk of

immune suppression.[1]

Hydrocortisone was patented in 1936 and approved for medical use in 1941.

generic medication.[1] In 2021, it was the 192nd most commonly prescribed medication in the United States, with more than 2 million prescriptions.[20][21]

Medical uses

Hydrocortisone is the pharmaceutical term for cortisol used in oral administration, intravenous injection, or topical application. It is used as an immunosuppressive drug, given by injection in the treatment of severe allergic reactions such as anaphylaxis and angioedema, in place of prednisolone in patients needing steroid treatment but unable to take oral medication, and perioperatively in patients on long-term steroid treatment to prevent an adrenal crisis. It may also be injected into inflamed joints resulting from diseases such as gout.

It may be used topically for allergic rashes,

itching and other inflammatory 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 the swelling, itch, and irritation in

haemorrhoids.[7]

It may be used as an acetate form (hydrocortisone acetate), which has slightly different pharmacokinetics and pharmacodynamics.[7][22]

  • Cortisol for injection
    Cortisol for injection
  • A tube of hydrocortisone cream, purchased over the counter
    A tube of hydrocortisone cream, purchased
    over 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

Pharmacodynamics

Hydrocortisone is a corticosteroid, acting specifically as both a glucocorticoid and as a mineralocorticoid. That is, it is an agonist of the glucocorticoid and mineralocorticoid receptors.

Hydrocortisone has low

synthetic corticosteroids.[13] Compared to hydrocortisone, prednisolone is about 4 times as potent and dexamethasone about 40 times as potent in terms of anti-inflammatory effect.[23] 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.[24] The equivalent doses and relative potencies of hydrocortisone compared to various other synthetic corticosteroids have also been reviewed and summarized.[13]

The

production 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).[25][26] 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 severe stress (e.g., surgery).[11]

The total and/or free concentrations of cortisol/hydrocortisone required for various glucocorticoid effects have been determined.[11]

Pharmacokinetics

Absorption

The

time to peak concentrations of oral hydrocortisone is 1.2 ± 0.4 (SD) hours.[11]

The

absorption of hydrocortisone varies widely depending on experimental circumstances and has been reported to range from 0.5 to 14.9% in different studies.[27] Some skin application sites, like the scrotum and vulva, absorb hydrocortisone much more efficiently than other application sites, like the forearm.[27][28][29] 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.[29] 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.[29][30][31]

Distribution

Most cortisol in the blood (all but about 4%) is bound to proteins, including corticosteroid binding globulin (CBG) and serum albumin. A pharmacokinetic review stated that 92% ± 2% (SD) (92–93%) of hydrocortisone is plasma protein-bound.[11] Free cortisol passes easily through cellular membranes.[32] Inside cells it interacts with corticosteroid receptors.[33]

Metabolism

Hydrocortisone is

dihydrocortisols, dihydrocortisones, tetrahydrocortisols, and tetrahydrocortisones.[34][11][12]

Elimination

The

duration of action of systemic hydrocortisone has been listed as 8 to 12 hours.[13]

Chemistry

See also: List of corticosteroids and List of corticosteroid esters § Hydrocortisone esters

Hydrocortisone, also known as 11β,17α,21-trihydroxypregn-4-ene-3,20-dione, is a

hydrocortisone esters exist and have been marketed for medical use.[35][36]

Society and culture

Legal status

In March 2021, the Committee for Medicinal Products for Human Use (CHMP) of the European 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.[37] The applicant for this medicinal product is Diurnal Europe BV.[37] Hydrocortisone (Efmody) was approved for medical use in the European Union, in May 2021, for the treatment of congenital adrenal hyperplasia (CAH) in people aged twelve years and older.[9]

Anti-competitive practices

In the UK, the

Actavis 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's National Health Service for over ten years. Fines totalling over £255m were levied against the companies involved in this breach of competition law.[38]

Research

COVID-19

Hydrocortisone was found to be effective in reducing mortality rate of critically ill COVID-19 patients when compared to other usual care or a placebo.[39]

References

  1. ^ a b c d e f g h "Hydrocortisone". Drugs.com. American Society of Health-System Pharmacists. 9 February 2015. Archived from the original on 20 September 2016. Retrieved 30 August 2016.
  2. ^ "Prescribing medicines in pregnancy database". Therapeutic Goods Administration (TGA). Archived from the original on 20 December 2016. Retrieved 21 February 2021.
  3. ^ "Hydrocortisone Notice of enforcement policy" (PDF). FDA. Archived (PDF) from the original on 12 March 2023. Retrieved 31 December 2022.
  4. ^ "Ala-cort- hydrocortisone cream". DailyMed. Archived from the original on 27 October 2020. Retrieved 21 February 2021.
  5. ^ "Ala-scalp- hydrocortisone lotion". DailyMed. Archived from the original on 21 April 2021. Retrieved 21 February 2021.
  6. ^ "Alkindi Sprinkle- hydrocortisone granule". DailyMed. Archived from the original on 10 February 2022. Retrieved 21 February 2021.
  7. ^ a b c "Anusol HC- hydrocortisone acetate suppository". DailyMed. Archived from the original on 10 February 2022. Retrieved 21 February 2021.
  8. ^ "Cortef- hydrocortisone tablet". DailyMed. Archived from the original on 17 April 2021. Retrieved 21 February 2021.
  9. ^ a b "Efmody EPAR". European Medicines Agency (EMA). 24 March 2021. Archived from the original on 14 June 2021. Retrieved 14 June 2021. Text was copied from this source which is © European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  10. ^ "Efmody Product information". Union Register of medicinal products. Archived from the original on 5 March 2023. Retrieved 3 March 2023.
  11. ^
    S2CID 24458998
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  12. ^
    S2CID 73248541
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  13. ^
    PMID 23947590
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  14. ISBN 978-0-7817-1750-2. Archived
    from the original on 14 September 2016.
  15. ISBN 978-1-284-05756-0
    .
  16. ^ "Hydrocortisone Pregnancy and Breastfeeding Warnings". Drugs.com. Archived from the original on 20 September 2016. Retrieved 1 September 2016.
  17. ^ U.S. patent 2,183,589
  18. ISBN 978-3-527-60749-5. Archived
    from the original on 10 January 2023. Retrieved 7 September 2020.
  19. hdl:10665/325771
    . WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
  20. ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
  21. ^ "Hydrocortisone - Drug Usage Statistics". ClinCalc. Archived from the original on 12 April 2020. Retrieved 14 January 2024.
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  23. ^ "Dexamethasone". drugs.com. Archived from the original on 21 June 2013. Retrieved 14 June 2013.
  24. S2CID 13986916
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  25. ISBN 978-3-318-05840-6. Archived
    from the original on 27 April 2023. Retrieved 10 April 2023.
  26. OCLC 1020003143. Archived
    from the original on 10 April 2023. Retrieved 10 April 2023.
  27. ^
    PMID 8299376
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    S2CID 132864025
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  31. S2CID 30076779
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  32. PMID 11250647
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  33. ISBN 978-1-4377-1753-2
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  34. S2CID 230716310
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  35. ^
    ISBN 978-1-4757-2085-3. Archived
    from the original on 8 September 2017.
  36. ^
    ISBN 978-3-88763-075-1. Archived
    from the original on 10 January 2023. Retrieved 19 June 2020.
  37. ^ a b "Efmody: Pending EC decision". European Medicines Agency (EMA). 25 March 2021. Archived from the original on 4 May 2021. Retrieved 27 March 2021. Text was copied from this source which is © European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  38. ^ This article contains OGL licensed text This article incorporates text published under the British Open 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
  39. PMID 32876694
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