Insulin analogs: Glimpse on contemporary facts and future prospective (original) (raw)
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International Journal of General Medicine, 2011
The goal of insulin therapy in patients with either type 1 diabetes mellitus (T1DM) or type 2 diabetes mellitus (T2DM) is to match as closely as possible normal physiologic insulin secretion to control fasting and postprandial plasma glucose. Modifications of the insulin molecule have resulted in two long-acting insulin analogs (glargine and detemir) and three rapid-acting insulins (aspart, lispro, and glulisine) with improved pharmacokinetic/ pharmacodynamic (PK/PD) profiles. These agents can be used together in basal-bolus therapy to more closely mimic physiologic insulin secretion patterns. Methods: This study reviews effects of the multiple demographic and clinical parameters in the insulin analogs glargine, detemir, lispro, aspart, and glulisine in patients with T2DM. A search was conducted on PubMed for each major topic considered (effects of injection site, age, race/ ethnicity, obesity, renal or hepatic dysfunction, pregnancy, exercise, drug interactions) using the topic words and name of each type of insulin analog. Information was also obtained from the prescribing information for each insulin analog. Results: The PK/PD profiles for insulin analogs may be influenced by many variables including age, weight, and hepatic and renal function. However, these variables do not have equivalent effects on all long-acting or rapid-acting insulin analogs. Conclusion: Rapid-acting and long-acting insulin analogs represent major advances in treatment for patients with T2DM who require insulin therapy. However, there are potentially important PK and PD differences between the two long-acting agents and among the three rapid-acting insulin analogs, which should be considered when designing treatment regimens for special patient groups.
PHARMACOKINETIC AND PHARMACODYNAMIC MODELLING OF BASE INSULINS AND ANALOGS
Pharmacokinetic modeling implies establishing the medicine dosage regime based on the anticipated course of the effect, depending on the given time. It is based on measuring possible pharmacodynamic parameters that correlate with pharmacokinetic data. Taking into consideration the latest discoveries on the pharmacokinetics of the base insulins and analogs, the primary aim of this paper was to compare the variability of their pharmacokinetic profile by using therapy monitoring in the patients suffering from the secondary insulin-dependent diabetes mellitus, type II. The secondary aims were: examining the influence of obesity, age and sex onto the pharmacokinetics (PK) of the applied insulins, and comparing therapeutic efficiency of the examined insulin analogs with NPH insulin. The research was performed at the Endocrinology Clinic, Clinical Center Nis, and it involved 60 patients suffering from the secondary insulin-dependent diabetes mellitus, type II. The patients were on therapy ...
Characterisation of insulin analogues therapeutically available to patients
PloS one, 2018
The structure and function of clinical dosage insulin and its analogues were assessed. This included 'native insulins' (human recombinant, bovine, porcine), 'fast-acting analogues' (aspart, glulisine, lispro) and 'slow-acting analogues' (glargine, detemir, degludec). Analytical ultracentrifugation, both sedimentation velocity and equilibrium experiments, were employed to yield distributions of both molar mass and sedimentation coefficient of all nine insulins. Size exclusion chromatography, coupled to multi-angle light scattering, was also used to explore the function of these analogues. On ultracentrifugation analysis, the insulins under investigation were found to be in numerous conformational states, however the majority of insulins were present in a primarily hexameric conformation. This was true for all native insulins and two fast-acting analogues. However, glargine was present as a dimer, detemir was a multi-hexameric system, degludec was a dodecamer (...
In order to provide comprehensive information on the differences in bioactivity between human insulin and insulin analogues, published in vitro comparisons of human insulin and the rapid acting analogues insulin lispro (Humalog ® ), insulin aspart ( NovoRapid ® ), insulin glulisine (Apidra ® ), and the slow acting analogues insulin glargine (Lantus ® ), and insulin detemir (Levemir ® ) were gathered from the past 20 years (except for receptor binding studies). A total of 50 reports were retrieved, with great heterogeneity among study methodology. However, various differences in bioactivity compared to human insulin were obvious (e.g. differences in effects on metabolism, mitogenesis, apoptosis, intracellular signalling, thrombocyte function, protein degradation). Whether or not these differences have clinical bearings (and among which patient populations) remains to be determined.
Turkish Journal of Endocrinology and Metabolism, 2015
Yazarlar bu makale ile ilgili olarak herhangi bir çıkar çatışması bildirmemiştir. Diabetes mellitus (DM), yüksek prevalansı ve komplikasyonlarına bağlı morbidite ve mortalite nedeniyle iyi tedavi edilmesi gereken önemli bir sağlık sorunudur. DM hastalarında, sağlıklı bireylerdeki insülinin fizyolojik salınımına yakın bir tedavi uygulaması diyabet komplikasyonlarının önlenebilmesiyle doğrudan bağlantılıdır. Son yıllarda geliştirilen ve insan insülinine farmakokinetik ve farmakodinamik üstünlüğü gösterilen analog insülinler ile vücutta doğal insülin seyrinin elde edilebilmesi mümkün hale gelmiştir. Analog insülinlerin geliştirilmesi yanında en fizyolojik insülin uygulama yöntemi olan devamlı subkütan insülin infüzyonunun ("continuous subcutaneous insülin infusion", pompa insülin), insülin uygulama şekli olarak kullanılması DM tedavisinde yeni bir dönem açmıştır. Bu derlemede, tip 1 ve 2 DM hastalarında pompa ile insülin analoglarının, ağırlıkla insülin aspartın, uygulaması güncel literatür eşliğinde tartışılmıştır.
HUMAN INSULIN AND INSULIN ANALOGUES IN MANAGEMENT OF DIABETES MELLITUS
The aim of the study was to determine the outcomes of human insulin and insulin analogues in the management of diabetes mellitus. Since good glycemic control is needed for diabetic insulin analogues are having faster onset and shorter duration of action when compared to human insulin. Insulin analogues show improvements in clinical outcomes, medication adherence and patient satisfaction. When compared with human insulin, insulin analogues are having lesser episodes of hypoglycemia. Premixed insulin analogues show little benefits than Rapid and long acting insulin patients, Insulins are used widely for the treatment of diabetes mellitus. Most of the articles show analogues. This review indicates that the introduction of insulin analogues could be safe and effective approach for better glycemic control and to prevent long term complications in diabetes mellitus.