Insulin rapid-acting

Currently, the most advanced form of insulin therapy is the insulin pump, also referred to as continuous subcutaneous insulin infusion (CSII). Using the short- or rapid-acting insulins only, these pumps are programmed to provide a slow release of small amounts of insulin as the basal portion of therapy, and then larger bolus doses are injected by the patient to account for the consumption of food. 

Three rapid-acting insulins have been approved in the United States lispro, aspart, and glulisine. Substitution of one or two amino acids in regular insulin results in the unique pharmacokinetic properties characteristic of these agents. Onset of action of rapid-acting insulins varies from 15 to 30 minutes, with peak effects occurring 1 to 2 hours following administration. 

Rapid-Acting Insulin Lispro Humalog Eli Lilly U-100 15-30 0.5-2.5 3-4 1 0 mL vial, 3 mL cartridge and... 

Rapid-acting insulins Humalog (insulin lispro) Yes Insulin pen 3-mL, vial, and 3-mL pen cartridge... 

Reduction in postprandial glucose concentrations Pramlintide administered subcutaneously immediately prior to a meal reduced plasma glucose concentrations after the meal when used with regular insulin or rapid-acting insulin analogs. 

Rapid-acting insulin analogues (lispro, insulin aspart [Humalog, Novo log]) have been engineered to contain amino acid modifications that promote rapid entry into the circulation from subcutaneous tissue. They begin to exert their effects as early as 5 to 10 minutes after administration. Lispro insulin, the first insulin analogue to be approved in Europe and the United States, is produced by switching the positions of lysine-proline amino acid residues 28 and 29 of the carboxy terminus of the p-chain. Lispro insulin displays very similar actions to insulin and has a similar affinity for the insulin receptor, but it cannot form stable hexamers or dimers in subcutaneous tissue, which promotes its rapid uptake and absorption. 

Very rapid acting insulin aspart insulin lispro... 

Zinman B. Insulin pump therapy and rapid acting insulin what have we learned Int J Clin Pract Suppl 2001 (123) 47-50. 

Aspart insulin and biphasic insulin aspart (30% soluble rapid-acting insulin and 70% protamine-bound aspart insulin) have been reviewed (4). 

Heinemann L, Weyer C, Rauhaus M, Heinrichs S, Heise T. Variability of the metabohc effect of soluble insulin and the rapid-acting insulin analogue insulin aspart. Diabetes Care 1998 21(ll) 1910-4. 

In contrast to most medium- and long-acting formulations, insulin glargine is a clear solution. In two cases, patients gave themselves rapid-acting insulin instead of glargine. 

Finally, several commercial preparations are now available that combine two forms of insulin in the same product. Some common examples include preparations that contain a mixture of intermediateacting insulin (e.g., isophane human insulin) and rapid-acting insulin (e.g., regular human insulin, aspart, or lispro). These insulins can be combined in specific amounts such as 50 50, 70 30, or 75 25 ratio of intermediate- to rapid-acting form, depending on the preparation. Products that combine two different forms of insulin can help provide optimal control of blood glucose levels while minimizing the number of injections needed to achieve this control. 

Ristic S, Bates PC. Effects of rapid-acting insulin analogs on overall glycemic control in type 1 and type 2 diabetes mellitus. Diabetes Technol Ther. 2003 5 57-66. 

---