Diabetes mellitus and SLE (Drugs) Flashcards
How can type I diabetes be treated?
Insulin
What are the types of insulin available?
- Fast-acting insulin
- Short-acting insulin
- Intermediate-acting insulin
- Long-acting insulin
What is an example of fast-acting insulin?
Insulin lispro
What is the mechanism of action of insulin lispro?
- Swapping of Lys/Pro residue in C-terminus
- Prevents oligomerisation of free insulin particles that causes deactivation
What is an example of short-acting insulin?
Unmodified insulin
What is an example of an intermdiate-acting insulin?
Neutral protamine hagedorn (NPH) insulin
What is the mechanism of action of NPH insulin?
- Suspension of protamine and insulin
- Causes formation of insoluble crystals of insulin and protamine that causes slow release of insulin
What are examples of long-acting insulin?
- Ultratard
- Glargine
What is the mechansm of action of ultratard?
- Suspension of Zn2+ and insulin
- Causes formation of insoluble Zn2+ and insulin crystals that release insulin slowly
What is the mechanism of action of glargine?
- Amino acid changes to the α/β chain causes shift in isoelectric point
- Causes aggregation of insulin particles once injected, reducing rate of absorption
How can type II diabetes be treated?
- Exercise and diet
- Metformin
- Sulphonylureas
- Meglitinides
- Thazolidinediones
- α-glucosidase inhibitors
- Incretin-related drugs
What is the mechanism of action of metformin?
Activation of AMPK receptors resulting in number of genetic changes leading to:
- ↓ Hepatic gluconeogenesis
- ↑ Glucose uptake by skeletal muscles
- ↓ Intestinal carbohydrate reabsorption
- ↓ Circulating levels of LDLs
- ↓ Appetite
What are the side effects of metformin?
- GI disturbalces
- Lactate acidosis
What is the mechanism of action of sulphonylureas?
Binds to SUR1 subunit of KATP in β-islet cells and causes closure, leading to increased release of insulin.
What are examples of sulphonylureas?
- Glibenclamide
- Glipizide
What are the side effects of sulphonylureas?
- Hypoglycaemia
- Increased appetite
- Cardiovascular risk (due to inhibition of cardiac KATP)
What is the mechanism of action of meglitinides?
Binds to SUR1 subunit of KATP in β-islet cells and causes closure, leading to increased release of insulin, but is much faster acting compared to sulphonylureas.
What is an example of meglitinides?
Repaglinide
What are the clinical uses of meglitinides and why?
- Taken before meals
- Fast-acting
What is the mechanism of action of thiazolidinediones?
Activation of PPARγ and induction of changes that including:
- ↑ Lipogenesis
- ↑ Glucose/fatty acid uptake
- ↑ Expression of transporters including GLUT4
What is an example of thazolidinediones?
Pioglitazone
What are the side effects of thiazolidinediones?
- Weight gain
- Fluid retention (enhancement of amiloride-sensitive Na+ absorption)
What are the clinical uses of thiazolidinediones and why?
- GIven as an add-on to other drugs
- Slow acting
What is the mechanism of action of α-glucosidase inhibitors?
Inhibits breakdown of starch/disaccharides into glucose in the GI tract and reduces amount of glucose absorption.
