Pharmacodynamic aspects of glucocorticoid use in emergencies
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BACHINSKY, N.G., GHICAVÎI, Victor, GAVRILUŢA, Vadim. Pharmacodynamic aspects of glucocorticoid use in emergencies. In: Archives of the Balkan Medical Union Supliment, 2013, nr. S3(48), pp. 107-108. ISSN 0041-6940.
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Archives of the Balkan Medical Union Supliment
Numărul S3(48) / 2013 / ISSN 0041-6940

Pharmacodynamic aspects of glucocorticoid use in emergencies


Pag. 107-108

Bachinsky N.G., Ghicavîi Victor, Gavriluţa Vadim
 
”Nicolae Testemițanu” State University of Medicine and Pharmacy
 
 
Disponibil în IBN: 2 noiembrie 2022


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Introduction: Glucocorticoids is one of the most common groups of remedies used in emergencies due to their multiple effects which confirm their use as pathogenetic and symptomatic therapy. Recent researches have demonstrated new aspects presented in corticosteroids pharmacodynamics of the genomic and non- genomic effects which allowed to explain the doses and dosage regimens used in emergencies. Genomic mechanism consists in glucocorticoids cell penetration, interaction with cytoplasmatic receptors, nucleus penetration, which modifies gene expression and protein and enzyme synthesis which lays at the base of the corticosteroid classical effects and their use in small and medium doses . Non - genomic mechanisms of action are due to non-specific interaction with plasmatic and mitochondrial membrane (changing the transport of protons and cations) and/or by conncting to a specific membrane receptor, followed by increasing of the messengers concentration, as well as inhibiting the production of arachidonic acid and prostaglandins by co- chaperoans, which have disconnected from protein complex after the hormons connect to the cytosolic receptors. Prevalence of the genomic and non- genomic effects is dependent of the dosage and the remedies properties. It means that the genomic effects grow at low doses up to 100 mg then they become stable (up to 30 mg effects are almost just genomic) not earlier than in 30 min . Effects have a fast-growing development, their manifestations start at 30 mg and increase rapidly with the dosage increasing (at 100 mg are equal to the genomic efects) and at 250 mg are prevalent. Ratio of prednisolones genomic and non- genomic effects is 4/4, metiprednisolon-5/13,3, dexamethasone 25/20 and the betamethasone 25/2,7. Therefore methylprednisolone and dexamethasone in high doses at intensive-care regimen and pulse therapy (dependind on the clinical situation) take priority in emergencies. Pulse therapy is indicated in cases of resistance to the usual doses of glucocorticoids, aggressive forms of autoimmune processes that require high doses of corticosteroids, the need to obtain a curative effect rapidly, in high activity of the pathological process, in the diseases evolution with vasculitis symptoms. To perform pulse therapy are used high or very high doses, as ussually, within 3 days (there may be other variations) after which go back to use the pre-puls therapy dosage regimen. Conclusions and Discussion: Intensive therapy is performed in cases of acute rapidly evoluating pathological processes (shock, allergic diseases, intoxications, exacerbation of immune processes, etc) and it is limited up to few hours or days after what the corticosteroids may be suspended or treatment may be continued in dependence of clinical situation. The corticosteroid dosage can range from moderate to high.

Cuvinte-cheie
Glucocorticoids, genomic and non-genomic effects