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Pharmacokinetic and pharmacodynamic advantages of insulin analogues and premixed insulin analogues over human insulins: impact on efficacy and safety.
Am J Med 2008; 121(6 Suppl):S9-S19AJ

Abstract

Human insulin preparations administered to patients with diabetes mellitus fail to reproduce the normal physiologic pattern of insulin secretion. Modifications have been made in the amino acid sequence of the insulin molecule with the aim of overcoming the pharmacokinetic shortcomings of human insulins. Such modifications have produced long-acting analogues, with relatively flat time-action profiles, for controlling glycemic levels between meals; and rapid-acting analogues with a fast onset and short duration of action, for controlling postprandial hyperglycemia. Premixed formulations of the rapid-acting analogues, containing both rapid-acting soluble and intermediate-acting protaminated forms, are also available. Trials of long-acting insulin analogues have consistently shown efficacy in controlling fasting plasma glucose and glycosylated hemoglobin (HbA1c), as well as a markedly reduced risk of hypoglycemia compared with neutral protamine Hagedorn insulin. The rapid-acting and premixed analogues offer better control of postprandial glucose excursions than do regular human insulin, resulting in similar or lower HbA1c levels. Furthermore, the analogues can offer patients greater flexibility and more convenience in administration compared with human insulins. This review provides an overview of the insulin analogues available today and describes their structure, pharmacokinetics, pharmacodynamics, efficacy, and safety.

Authors+Show Affiliations

Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, Massachusetts 02215, USA. arolla@caregroup.harvard.edu

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

18514090

Citation

Rolla, Arturo. "Pharmacokinetic and Pharmacodynamic Advantages of Insulin Analogues and Premixed Insulin Analogues Over Human Insulins: Impact On Efficacy and Safety." The American Journal of Medicine, vol. 121, no. 6 Suppl, 2008, pp. S9-S19.
Rolla A. Pharmacokinetic and pharmacodynamic advantages of insulin analogues and premixed insulin analogues over human insulins: impact on efficacy and safety. Am J Med. 2008;121(6 Suppl):S9-S19.
Rolla, A. (2008). Pharmacokinetic and pharmacodynamic advantages of insulin analogues and premixed insulin analogues over human insulins: impact on efficacy and safety. The American Journal of Medicine, 121(6 Suppl), pp. S9-S19. doi:10.1016/j.amjmed.2008.03.022.
Rolla A. Pharmacokinetic and Pharmacodynamic Advantages of Insulin Analogues and Premixed Insulin Analogues Over Human Insulins: Impact On Efficacy and Safety. Am J Med. 2008;121(6 Suppl):S9-S19. PubMed PMID: 18514090.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Pharmacokinetic and pharmacodynamic advantages of insulin analogues and premixed insulin analogues over human insulins: impact on efficacy and safety. A1 - Rolla,Arturo, PY - 2008/6/27/pubmed PY - 2008/7/22/medline PY - 2008/6/27/entrez SP - S9 EP - S19 JF - The American journal of medicine JO - Am. J. Med. VL - 121 IS - 6 Suppl N2 - Human insulin preparations administered to patients with diabetes mellitus fail to reproduce the normal physiologic pattern of insulin secretion. Modifications have been made in the amino acid sequence of the insulin molecule with the aim of overcoming the pharmacokinetic shortcomings of human insulins. Such modifications have produced long-acting analogues, with relatively flat time-action profiles, for controlling glycemic levels between meals; and rapid-acting analogues with a fast onset and short duration of action, for controlling postprandial hyperglycemia. Premixed formulations of the rapid-acting analogues, containing both rapid-acting soluble and intermediate-acting protaminated forms, are also available. Trials of long-acting insulin analogues have consistently shown efficacy in controlling fasting plasma glucose and glycosylated hemoglobin (HbA1c), as well as a markedly reduced risk of hypoglycemia compared with neutral protamine Hagedorn insulin. The rapid-acting and premixed analogues offer better control of postprandial glucose excursions than do regular human insulin, resulting in similar or lower HbA1c levels. Furthermore, the analogues can offer patients greater flexibility and more convenience in administration compared with human insulins. This review provides an overview of the insulin analogues available today and describes their structure, pharmacokinetics, pharmacodynamics, efficacy, and safety. SN - 1555-7162 UR - https://www.unboundmedicine.com/medline/citation/18514090/Pharmacokinetic_and_pharmacodynamic_advantages_of_insulin_analogues_and_premixed_insulin_analogues_over_human_insulins:_impact_on_efficacy_and_safety_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0002-9343(08)00309-4 DB - PRIME DP - Unbound Medicine ER -