Insulin Preparations - Exam 2 Hockerman Flashcards
Insulin Prep and their rate of onset, duration of action, and modifications of each
Ultra-rapid Insulins (Rate of Onset = 5-15 min)
Lispro (Humalog), Aspart (Novolog), Glulisine (Apidra), Afrezza (inhaled)
Rapid Insulin (Rate of Onset = 30-60 min
Regular insulin (Humulin, Novolin)
Intermediate Insulin (Rate of Onset = 60-90 min)
NPH
Slow Insulins
Glargine (Lantus), Detemir (Levemir), Degludec (Tresiba)
Glargine (Lantus) Rate of Onset
60-90 min
Detemir (Levemir) Rate of Onset
1-2 h
Degludec (Tresiba) Rate of Onset
1 h
Lispro (Humalog) Duration of Action
6-8 h
Aspart (Novolog), Glulisine (Apidra), and Afrezza (inhaled) Duration of Action
3-5 h
Regular Insulin (Humulin, Novolin) Duration of Action
8-12 h
NPH Duration of Action
24 h
Glargine (Lantus), Detemir (Levemir), and Degludec (Tresiba) Duration of Action
> 24 h
Lispro (Humalog) Modifications
Reversing proline-28 and lysine-29 (K29) on insulin B chain to decrease self-association/destabilize dimerization
Aspart (Novolog) Modifications
Proline-28 on insulin B chain is switched to Aspartate-28 (D28) to decrease self-association/destabilize dimerization
Glulisine (Apidra) Modifications
Asparagine-3 (N3) and Lysine-29 (K29) on insulin B chain are switched to Lysine-3 (K3) and Glutamic Acid-29 (E29)
Afrezza (inhaled) Modifications
Uses a technosphere particle that has insulin bound to a peptide. It is small but it has a lot of surface area
Regular Insulin Modifications
Nothing lol, forms a dimer/hexamer
NPH Modifications
Neutral Protamine Hagedorn, forms an insoluble insulin complex where insulin is bound to protamine and must be freed by proteases before absorption
Glargine (Lantus) Modifications
Asparagine-21 (N21) of the insulin A chain is changed to Gycine-21 (G21), which makes the insulin very soluble at a pH of 4 (but not at pH of 7 - blood), so it must precipitate and release slowly. Also, 2 Arginine residues are added to the end of the insulin B chain (R30 and R31)
Detemir (Levemir) Modifications
Threonine (T30) of the insulin B chain is deleted, and Lysine-29 (K29) is myristylated (aka added a fatty acid). This makes it easier to bind to serum albumin extensively.
Degludec (Tresiba) Modifications
Threonine-30 (T30) of insulin B chain is replaced by gamma-Glu/C16 fatty acid. This makes it easier to bind to serum albumin extensively.
