Diabetes Drugs Flashcards
What is diabetes? What is the difference between Type 1 and Type 2 diabetes?
*Diabetes is characterized by elevated blood sugar levels due to absolute or relative lack of insulin
*Type 1 diabetes= B-cell failure and insulin dependent
*Type 2 diabetes= gradual B-cell deterioration; Early stages include diet modification and oral agents; Late stages include insulin therapy
What are the common symptoms related to diabetes?
Symptoms include increased thirst, slow healing cuts and sores, fatigue, blurred vision, frequent urination, unexplained weight loss
What type of hormone is insulin?
Insulin is a storage hormone as it promotes anabolisms and inhibits catabolism of carbohydrates, fatty acids, and protein
In the absense of insulin, most tissues cant use glucose so fats and proteins are broken down to provide energy
What is the MOA of insulin?
MOA: insulin binds to insulin receptors on the plasma membrane and activates tyrosine kinase primarily in adipose tissue, liver, and skeletal muscle
Nerves, RBCs, kidney, and the lens of the eye do not require insulin for glucose transport
What is the physiology of insulin at the liver?
Insulin increases the storage of glucose as glycogen in the liver and inhibits gluconeogenesis which significantly decreases glucose output by the liver. Protein catabolism also decreases.
What is the physiology of insulin at the muscle?
Insulin stimulates the glycogen synthesis and protein synthesis. Glucose transport into the cells is facilitated by GLUT-4 into the cell membrane. Insulin inhibits protein catabolism.
What is the physiology of insulin in adipose tissue?
Insulin facilitates the storage of triglycerides by activating plasma lipoprotein lipase and inhibiting intracellular lipolysis. Insulin increases the glucose uptake by GLUT-4 insertion into the cell membrane
What are common adverse effects of insulin?
Hypoglycemia, allergic reactions, lipodystrophy, seizures, coma
What is the MOA for oral antidiabetic drugs to reduce blood sugar?
*Stimulate pancreatic insulin release = sulfonylureas, meglitinide
*Reduce bio-synthesis of glucose in the liver= biguanides (Metformin)
*Increased sensitivity of target cells to insulin= thiazolidinediones
*Retard the absorption of sugars from the GI tract = acarbose, miglitol
List of first, second, and third generation sulfonylureas
*Ist gen:
Acetohexamide
Chlorpropamide
Tolbutamide
Tolazamide
*2nd generation:
Glipizide
Glyburide
*3rd generation:
* Glimepiride
What are common adverse effects of sulfonylureas?
*Hypoglycemia
*Cholestatic jaundice
*Weight gain
*Cross placenta – fetal hypoglycemia
Describe meglitinides
Repaglinide
Nateglinide
*MOA: More rapidly acting insulin enhancers and shorter duration than
sulfonylureas
*AE: Hypoglycemia
*Indications: minimal renal excretion and thus useful in patients with DM and
impaired renal function
MUST BE TAKEN WITH A MEAL
Describe biguanides (Metformin) MOA and AE
*decreases hepatic glucose production by Inhibiting gluconeogenesis
* Does NOT promote insulin secretion. It
increase the sensitivity of liver and muscle
to insulin. Does not cause hypoglycemia.
AE: modest weight loss,
drop in TG and LDL, and increase in HDL; GI Side effects and Lactic acidosis
Describe thiazolidinediones MOA, AE, and indications
Pioglitazone
Rosiglitazone
*MOA: Enhance glucose and lipid metabolism through action on PPAR–γ; Enhance sensitivity to insulin in muscle and fat by increasing the GLUT 4
glucose transporters
*Indications: Beneficial effects on serum lipid; decrease TG and increase HDL
*AE: Edema is an adverse effect
Describe alpha-glucosidase inhibitors MOA, indications, AE
Acarbose and Miglitol
*MOA: It inhibits alpha-glucosidase which converts dietary starch and complex carbohydrates into simple sugars
*Indications: reduces absorption of glucose after meals
*AE: flatulence and diarrhea
