Methylprednisolone

Furman, Brian L.

doi:10.1016/b978-0-12-801238-3.97802-4

Cited by 2 publications

(3 citation statements)

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“…Further observation says that the spin–lattice relaxation time at each crystallographically distinct carbon nuclei sites of methylprednisolone is less than that of prednisolone. The bioactivity of methylprednisolone is more than that of prednisolone (it is observed by in silico analysis, which will be discussed in the next section), and methylprednisolone has greater anti-inflammatory potency than prednisolone . Hence, the attachment of a methyl group with the C6 carbon atom of the “B” ring of prednisolone increases the spin–lattice relaxation rate and also increases the potency of the glucocorticoid as an anti-inflammatory hormone.…”

Section: Resultsmentioning

confidence: 99%

“…The bioactivity of methylprednisolone is more than that of prednisolone (it is observed by in silico analysis, which will be discussed in the next section), and methylprednisolone has greater anti-inflammatory potency than prednisolone. 15 Hence, the attachment of a methyl group with the C6 carbon atom of the “B” ring of prednisolone increases the spin–lattice relaxation rate and also increases the potency of the glucocorticoid as an anti-inflammatory hormone. It is revealed by these comparative data that the dynamics of the glucocorticoids can be correlated with the potency of the anti-inflammatory hormone.…”

Section: Resultsmentioning

confidence: 99%

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Investigation of the Influence of Various Functional Groups on the Dynamics of Glucocorticoids

et al. 2022

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The basic configuration of glucocorticoid consists of four-fused rings associated with one cyclohexadienone ring, two cyclohexane rings, and one cyclopentane ring. The ways the structure and dynamics of five glucocorticoids (prednisone, prednisolone, prednisolone acetate, methylprednisolone, and methylprednisolone acetate) are altered because of the substitution of various functional groups with these four-fused rings are studied thoroughly by applying sophisticated solid-state nuclear magnetic resonance (NMR) methodologies. The biological activities of these glucocorticoids are also changed because of the attachment of various functional groups with these four-fused rings. The substitution of the hydroxyl group (with the C11 atom of the cyclohexane ring) in place of the keto group enhances the potential of the glucocorticoid to cross the cellular membrane. As a result, the bioavailability of prednisolone (the hydroxyl group is attached with the C11 atom of the cyclohexane ring) is increased compared to prednisone (the keto group is attached with the C11 atom of cyclohexane rings). Another notable point is that the spin–lattice relaxation rate at crystallographically distinct carbon nuclei sites of prednisolone is increased compared to that of the prednisone, which implies that the motional degrees of freedom of glucocorticoid is increased because of the substitution of the hydroxyl group in place of the keto group of the cyclohexane ring. The attachment of the methyl group with the C6 atom of cyclohexane rings further reduces the spin–lattice relaxation time at crystallographically distinct carbon nuclei sites of glucocorticoid and its bioactivity is also increased. By comparing the spin–lattice relaxation time and the local correlation time at crystallographically different carbon nuclei sites of three steroids prednisone, prednisolone, and methylprednisolone, it is observed that both the spin–lattice relaxation time and the local correlation time gradually decrease at each crystallographically distinct carbon nuclei sites when we move from prednisone to prednisolone to methyl-prednisolone. On the other hand, if we compare the same for prednisolone, prednisolone acetate, and methylprednisolone acetate, then we also observe that both the spin–lattice relaxation time and the local-correlation time gradually decrease from prednisolone to prednisolone acetate to methylprednisolone acetate for all chemically different carbon nuclei. It is also noticeable that both the spin–lattice relaxation time and the local-correlation time gradually decrease from prednisone to prednisolone to prednisolone acetate to methylprednisolone to methylprednisolone acetate for most of the carbon nuclei sites. From in silico analysis, it is also revealed that the bioavailability and efficacy of the glucocorticoid increase from prednisone to prednisolone to prednisolone acetate to methylprednisolone to methylprednisolone acetate. Hence, it can be concluded that the biological activity and the motional degrees of freedom of the glu...

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Investigation of the Influence of Various Functional Groups on the Dynamics of Glucocorticoids

et al. 2022

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“…Medrol® (metilprednisolona) (Furman, 2019) (Fig. 6) y los corticosteroides en general, se consideran como adyuvantes en el tratamiento del COVID-19, puesto que se han utilizado ampliamente para tratar la neumonía grave y prevenir el daño pulmonar debido a su capacidad para suprimir la inflamación sistémica grave (Meduri et al, 2007).…”

Section: Azitromicina Corticosteroides Y Otros Agentes Coadyuvantes unclassified

COVID-2019: Una revisión de la nueva crisis pandémica

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2020

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La pandemia del COVID-19, causada por el nuevo coronavirus 2019-nCoV y responsable del síndrome respiratorio agudo severo por coronavirus 2 (SARS-CoV-2), constituye un punto de inflexión en la historia humana. La patogenicidad del virus y su capacidad para crear rápidamente una infección generalizada con graves consecuencias y alta mortalidad, justifican la adopción de medidas extraordinarias de prevención y control. Las tasas de infección por COVID-19 están en constante evolución, y es muy difícil predecir el comportamiento de la enfermedad, en consecuencia, se requiere el desarrollo urgente de nuevos fármacos o la reutilización de medicamentos conocidos. A pesar de que es un proceso complejo y que las pruebas clínicas tienen graves implicaciones bioéticas, la investigación sigue avanzando, el sector científico está produciendo resultados de calidad, entre ellos el primer antiviral aprobado contra el SARS-CoV-2, el Veklury® o remdesivir. Existen muchos otros agentes terapéuticos en investigación, y se hacen grandes esfuerzos por obtener una posible vacuna. En este artículo se hace una revisión sistemática acerca de algunos aspectos resaltantes del COVID-19, comenzando por ofrecer información acerca de las pandemias a lo largo de la historia, la descripción del nuevo coronavirus 2019-nCoV, los mecanismos de trasmisión y las pruebas de diagnóstico, algunos de los fármacos que se están probando (cloroquina, lopinavir/ritonavir, ribavirina, favipiravir, oseltamivir), así como agentes inmunomoduladores (tocilizumab, anakinra interferones, transfusiones de plasma), agentes coadyuvantes (azitromicina, corticosteroides, mesilato de camostat) y, finalmente, la situación en que se encuentra el desarrollo de una posible vacuna.

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Methylprednisolone

Cited by 2 publications

References 32 publications

Investigation of the Influence of Various Functional Groups on the Dynamics of Glucocorticoids

Investigation of the Influence of Various Functional Groups on the Dynamics of Glucocorticoids

COVID-2019: Una revisión de la nueva crisis pandémica

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