Insulin glargine: pharmacokinetic and pharmacodynamic basis of clinical effect

Glargine became the first long-acting insulin analogue. Glargine was designed to meet basal insulin requirements throughout the day with a single injection. Pharmacokinetics of insulin glargine is characterized by biotransformation into metabolites M1 and M2 that transforms the B chain of glargine s...

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Autores principales:	Vadim Valer'evich Klimontov, Natalya Evgen'evna Myakina
Formato:	article
Lenguaje:	EN RU
Publicado:	Endocrinology Research Centre 2014
Materias:	diabetes insulin glargine metabolite m1 metabolite m2 pharmacokinetics pharmacodynamics variability of insulin action hypoglycemia mitogenic effects Nutritional diseases. Deficiency diseases RC620-627
Acceso en línea:	https://doaj.org/article/68134155cb3a4de7b6012ca1ba4f09a4
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spelling	oai:doaj.org-article:68134155cb3a4de7b6012ca1ba4f09a42021-11-14T09:00:19ZInsulin glargine: pharmacokinetic and pharmacodynamic basis of clinical effect2072-03512072-037810.14341/DM2014499-107https://doaj.org/article/68134155cb3a4de7b6012ca1ba4f09a42014-12-01T00:00:00Zhttps://www.dia-endojournals.ru/jour/article/view/6691https://doaj.org/toc/2072-0351https://doaj.org/toc/2072-0378Glargine became the first long-acting insulin analogue. Glargine was designed to meet basal insulin requirements throughout the day with a single injection. Pharmacokinetics of insulin glargine is characterized by biotransformation into metabolites M1 and M2 that transforms the B chain of glargine so it is similar to the B chain of human insulin. Plasma concentrations of active M1 and M2 metabolites have no pronounced peaks during the day, resulting in lower glucose variability and hypoglycaemia risk when compared with NPH insulin. The metabolic activities of M1 and M2 metabolites are similar to the effect of glargine, whereas the mitogenic effects of these metabolites do not exceed the effect of human insulin. Insulin glargine shows a higher affinity for the insulin-like growth factor-1 (IGF-1) receptor when compared with human insulin. Glargine has no proliferative effect in vivo owing to its rapid conversion into metabolites. Pharmacokinetic and pharmacodynamic variability of glargine is comparable to other insulins. These characteristics are important for the clinical efficacy and safety of glargine.Vadim Valer'evich KlimontovNatalya Evgen'evna MyakinaEndocrinology Research Centrearticlediabetesinsulin glarginemetabolite m1metabolite m2pharmacokineticspharmacodynamicsvariability of insulin actionhypoglycemiamitogenic effectsNutritional diseases. Deficiency diseasesRC620-627ENRUСахарный диабет, Vol 17, Iss 4, Pp 99-107 (2014)
institution	DOAJ
collection	DOAJ
language	EN RU
topic	diabetes insulin glargine metabolite m1 metabolite m2 pharmacokinetics pharmacodynamics variability of insulin action hypoglycemia mitogenic effects Nutritional diseases. Deficiency diseases RC620-627
spellingShingle	diabetes insulin glargine metabolite m1 metabolite m2 pharmacokinetics pharmacodynamics variability of insulin action hypoglycemia mitogenic effects Nutritional diseases. Deficiency diseases RC620-627 Vadim Valer'evich Klimontov Natalya Evgen'evna Myakina Insulin glargine: pharmacokinetic and pharmacodynamic basis of clinical effect
description	Glargine became the first long-acting insulin analogue. Glargine was designed to meet basal insulin requirements throughout the day with a single injection. Pharmacokinetics of insulin glargine is characterized by biotransformation into metabolites M1 and M2 that transforms the B chain of glargine so it is similar to the B chain of human insulin. Plasma concentrations of active M1 and M2 metabolites have no pronounced peaks during the day, resulting in lower glucose variability and hypoglycaemia risk when compared with NPH insulin. The metabolic activities of M1 and M2 metabolites are similar to the effect of glargine, whereas the mitogenic effects of these metabolites do not exceed the effect of human insulin. Insulin glargine shows a higher affinity for the insulin-like growth factor-1 (IGF-1) receptor when compared with human insulin. Glargine has no proliferative effect in vivo owing to its rapid conversion into metabolites. Pharmacokinetic and pharmacodynamic variability of glargine is comparable to other insulins. These characteristics are important for the clinical efficacy and safety of glargine.
format	article
author	Vadim Valer'evich Klimontov Natalya Evgen'evna Myakina
author_facet	Vadim Valer'evich Klimontov Natalya Evgen'evna Myakina
author_sort	Vadim Valer'evich Klimontov
title	Insulin glargine: pharmacokinetic and pharmacodynamic basis of clinical effect
title_short	Insulin glargine: pharmacokinetic and pharmacodynamic basis of clinical effect
title_full	Insulin glargine: pharmacokinetic and pharmacodynamic basis of clinical effect
title_fullStr	Insulin glargine: pharmacokinetic and pharmacodynamic basis of clinical effect
title_full_unstemmed	Insulin glargine: pharmacokinetic and pharmacodynamic basis of clinical effect
title_sort	insulin glargine: pharmacokinetic and pharmacodynamic basis of clinical effect
publisher	Endocrinology Research Centre
publishDate	2014
url	https://doaj.org/article/68134155cb3a4de7b6012ca1ba4f09a4
work_keys_str_mv	AT vadimvalerevichklimontov insulinglarginepharmacokineticandpharmacodynamicbasisofclinicaleffect AT natalyaevgenevnamyakina insulinglarginepharmacokineticandpharmacodynamicbasisofclinicaleffect
_version_	1718429534060019712

Insulin glargine: pharmacokinetic and pharmacodynamic basis of clinical effect

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