Insulin Glulisine (Apidra)
By William T. Elliott, MD, FACP, and James Chan, PharmD, PhD
The FDA has approved another rapid-acting insulin to cover mealtime blood sugar spikes. Insulin glulisine is a recombinant DNA human insulin analogue similar to insulin lispro. It will be marketed by Aventis as ApidraTM.
Insulin glulisine is indicated for the treatment of adult patients with diabetes mellitus for the control hyperglycemia.1
Insulin glulisine is given subcutaneously or by an external infusion pump and should be given within 15 minutes before a meal or within 20 minutes after starting a meal. It generally used with a long-acting insulin.1 Insulin glulisine is supplied as 10 mL vials (100 units/mL).
Like other rapid acting insulins, insulin glulisine has a more rapid onset of action and shorter duration of action than regular human insulin.
Potential systemic reactions were reported in 4.3% (79/1833) of participants in controlled clinical trials. This compares to 3.8% (58/1524) who received comparator short-acting insulins.1 The long-term effect of insulin analogs is not known as modifications may alter affinity for (insulin growth factor) IGF-1 receptor more than for insulin receptors.3 This may lead to enhanced mitogenic activity.
Insulin glulisine is the third rapid-acting insulin to market in this country. It is produced by recombinant DNA technology and differs from human insulin at position B3 of the B-chain where aspargine is replaced by lysine and at B29 where lysine is replaced by glutamate. Other marketed rapid-acting insulin are insulin lispro where the amino acids in positions B28 and B29 are switched and insulin aspart where proline (B28) is replaced by aspartate. The pharmacokinetic and pharmacodynamic profiles of insulin glulisine appear to be very similar to that of insulin lispro.2 In 26-week studies in type 1 diabetics (n = 672) and type 2 diabetics (n = 876) glycemic control (ie, HbA1c) and rates of hypoglycemia requiring intervention from a third party were also comparable.1 The cost of insulin glulisine was not available at the time of this review.
Insulin glulisine adds another rapid-acting insulin to the markets. Given the higher cost, comparable glycemic control, and yet to be determined long term safety due to potential altered receptor binding of rapid-acting insulins, regular human insulin should still be considered for initial therapy.
1. Apidra Product Information. Aventis Pharmaceuticals. April 2004.
2. Frick A, et al Diabetes. 2003;(52 suppl 1):A119.
3. Rakatzi I, et al. Diabetes. 2003;52:2227-3228.
Dr. Elliott is Chair, Formulary Committee, Northern California Kaiser Permanente, and Assistant Clinical Professor of Medicine, University of California, San Francisco. Dr. Chan is Pharmacy Quality and Outcomes Manager, Kaiser Permanente, Oakland, CA. Both are Associate Editors of Internal Medicine Alert.