Lecture 8: Insulin Therapy Flashcards
What does insulin bind to?
Binds to IGF-1 receptors and gets GLUT 4 to come to the membrane
Tyrosine kinase
Broken down in liver
What kind of hormone is insulin?
An ANABOLIC one
- adipose tissue build up
- muscle tissue build up
- glycogen build up and FA synthesis in the liver
What are the indications for insulin?
- Type 1 diabetes
- Inadequately controlled Type 2 diabetes
- Temporary use
- hospitalization/surgery
- surgery
- renal disease
- to initially attain glycemic control in patients with severe type 2 diabetes
- to overcome glucose toxicity and re-regulate decompensated patients
What are the types of insulin analogues?
Modification of synthetic insulin molecules allow for unique pharmacodynamics profiles
i. rapid-acting: lispro aspart, glulisine
ii. short-acting: regular
iii. intermediate: NPH
iv. long acting: glargine, detemir
What are examples of RAPIDLY acting human analogs of insulin?
- Aspart (aspartic acid for proline)
- lispro (lysine for proline)
- Glulisine (glutamic acid for lysine)
Homologous with regular human insulin
Single substitution
What is bolus insulin?
Used for coverage of food intake or correction of hyperglycemia
Comes in short acting and rapid acting forms
Short acting = regular insulin
Rapid acting = apart, lispro, glulisine
What types of insulin are used for bolus insulin?
Rapid acting Aspart (aspartic acid for proline) Lispro Glulisine Short acting Regular insulin
What is the structure of lispro?
Exchanged a lysine (lis) for a proline (pro) in the insulin structure
Otherwise all the same
Dirsupts monomer-monomer interactions and leads to more rapid absorption
When do you take aspart, lispro, glulisine?
Take them 5-15 minutes before meal
What is the difference between regular and rapid acting insulin?
Rapid = 2x faster absorption
2x higher peak concentration
10-20 minutes post injection
What is basal insulin?
Maintain euglycemia in the fasting state
Two types: intermediate and longacting
What is intermediate types of basal insulin?
NPH
Neutral protamine Hagedorn
What is NPH?
Intermediate type of insulin
Used for basal insulin
Insulin + protamine, a positively charged polypeptide
What is glargine and detemir?
Long acting insulin
Used for basal insulin
Several substitutions and addtions
Forms microprecipitate of insulin (Glargine) and is broken down slowly in body
Detemir binds to albumin and slowly dissociates (long-acting)
What are the long acting basal insulins?
Glargine
Detemir