Chemical formula: C₂₅₇H₃₈₉N₆₅O₇₇S₆ Molecular mass: 5,811.691 g/mol
The primary activity of insulin lispro is the regulation of glucose metabolism.
In addition, insulins have several anabolic and anti-catabolic actions on a variety of different tissues. Within muscle tissue this includes increasing glycogen, fatty acid, glycerol and protein synthesis and amino acid uptake, while decreasing glycogenolysis, gluconeogenesis, ketogenesis, lipolysis, protein catabolism and amino acid output.
Insulin lispro has a rapid onset of action (approximately 15 minutes), thus allowing it to be given closer to a meal (within zero to 15 minutes of the meal) when compared to soluble insulin (30 to 45 minutes before). Insulin lispro takes effect rapidly and has a shorter duration of activity (2 to 5 hours) when compared to soluble insulin.
The pharmacokinetics of insulin lispro reflect a compound that is rapidly absorbed, and achieves peak blood levels 30 to 70 minutes following subcutaneous injection.
The pharmacokinetics of insulin lispro protamine suspension are consistent with those of an intermediate acting insulin such as NPH. The pharmacokinetics of insulin lispro protamine suspension are representative of the individual pharmacokinetic properties of the two components.
When considering the clinical relevance of these kinetics, it is more appropriate to examine the glucose utilisation curves.
Insulin lispro maintains more rapid absorption when compared to soluble human insulin in patients with renal impairment. In patients with type 2 diabetes over a wide range of renal function the pharmacokinetic differences between insulin lispro and soluble human insulin were generally maintained and shown to be independent of renal function. Insulin lispro maintains more rapid absorption and elimination when compared to soluble human insulin in patients with hepatic impairment.
Insulin lispro 200 units/ml solution for injection was bioequivalent to insulin lispro 100 units/ml solution for injection after subcutaneous administration of a single 20 unit dose in healthy subjects. Time to maximum concentration was also similar between formulations.
In in vitro tests, including binding to insulin receptor sites and effects on growing cells, insulin lispro behaved in a manner that closely resembled human insulin. Studies also demonstrate that the dissociation of binding to the insulin receptor of insulin lispro is equivalent to human insulin. Acute, one month and twelve month toxicology studies produced no significant toxicity findings.
Insulin lispro did not induce fertility impairment, embryotoxicity or teratogenicity in animal studies.
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