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Glucocorticosteroids
(or corticosteroids or corticoids)

Corticoids are synthetic derivatives of cortisol, the main glucocorticoid hormone secreted by the adrenal gland.

All corticoids have a common sterane (steroid) core but each derivative carries different chemical modifications designed to increase its anti-inflammatory effects and decrease its mineralocorticoid properties. The corticoids available on the market differ in their anti-inflammatory and mineralocorticoid strengths, and in the duration of their action.

Therapeutic indications

Corticoids are used as therapeutic agents owing primarily to their anti-inflammatory properties. However, they also have immunosuppressive and antiallergenic effects. In case of inflammation, corticoids may in addition act as antalgics (pain killers) and antipyretics (fever-reducing medication). Corticoids are therefore useful in many situations, including asthma management, a very common application.

Corticosteroids are widely used in sports medicine to treat tendon injuries, ligament lesions and overuse syndromes. Thus, corticoids exert their positive effects on performance indirectly thanks to their anti-inflammatory, antalgic and potentially euphorizing properties.

Side effects

The therapeutic effects of corticoids are accompanied by adverse side effects that are for the most part and by definition unavoidable whenever hormonal activity is present. These side effects can be effectively countered or even prevented by respecting the strict rules of corticoid use that take into account their pharmacological properties. In general terms, adverse effects are caused by an overdose or axis inhibition leading to hormonal insufficiency (in case of prolonged use).

Classical side-effect include digestive and neuropsychiatric complications, susceptibility to infections, problems with skin, locomotion and vision, endocrine complications and various other biological problems, as well as tendon rupture following corticoid infiltration. Long term corticoid use may have a negative effect on bones, leading to an increased risk of osteoporosis and fractures as well as osteonecrosis. The major risk is corticotropic insufficiency with the development in extreme cases of atrophic adrenal Cushing's syndrome. Corticoids are also addictive and habit-forming. Lowering dosage, interrupting a long term treatment or over-dosing all lead to withdrawal symptoms. These symptoms are brought about by partial functional hypothalamo-pituitary-adrenal inertia (kidney insufficiency).

Intensive sports practice leads to different overuse syndromes that can affect soft tissues (muscles and tendons), bones and periostum tissues, and specific joints. In addition, in certain disciplines, in collective sports in particular, there is a high prevalence of capsuloligamentary trauma (mainly knee and ankle sprains)

Laboratory analyses

Laboratory glucocorticosteroids testing is carried out on urine samples collected in-competition. The urine is first hydrolyzed to release free glucocorticosteroids which are initially in conjugated form. The sample is then subjected to liquid extraction to purify and extract the relevant compounds. To detect glucocorticosteroids the extract is analyzed by liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS).







Structure du cortisol

Chemical structure of cortisol












Métabolisme des corticostéroïdes - cliquer pour agrandir
Corticosteroids metabolism
 

Last Update on 07.10.2008

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