Anti-diabetic drugs Flashcards
Which are the rapid onset insulins?
Lispro, aspart, glulisine
NPH belongs to slow onset or intermediate onset insulin?
Intermediate onset
What is the relative time to peak for regular insulin?
2-4 hr
What is the relative time to peak for NPH?
4-8 hr
Does glargine have peak in its action?
No peak
What is the best strategy to prevent microvascular complications of diabetes?
Tight glycemic control
Diabetic microvascular complications includes…?
Retinopathy, nephropathy, neuropathy
Does intensive glycemic control prevent coronary heart disease?
Yes
What is the mechanism of insulin secretion?
GLUT1 allows entry of glucose inside beta cell, it is broken down and increases ATP which inhibits K efflux, depolarization occurs and insulin is released by Ca dependent exocytosis. Insulin binds cell membrane tyrosine kinase and does not enter nucleus.
What is the mechanism of action of sulfonylurea?
Insulin secretagogues (K channel modulators). Bind SUR1 inhibit K efflux leading to depolarization and insulin release.
What is the most important side effect of sulfonylurea?
Hypoglycemia, weight gain, not given in pregnancy.
Which sulfonylurea causes SIADH and disulfiram-like action?
Chlorpropamide
What is the mechanism of action of metformin?
Biguanide- insulin sensitizer. Reduces hepatic gluconeogenesis and activates GLUT4 receptors in skeletal muscles.
What are the contraindications for metformin use?
Renal or liver disease, cardiac failure, chronic hypoxic lung disease and radiologic procedure using IV iodinated contrast medium.
What is most important side effect of metformin?
Lactic acidosis and decreased absorption of Vit B12.
What is the mechanism of action of repaglinide?
Meglitinides (K channel modulators) also nateglinide. Closes K channel similar to sulfonylurea.
What is the MoA of pioglitazone? How about rosiglitazone?
Thiazolidinediones. Pioglitazone- binds and activates PPAR-y (primarily on adipocytes- increases tissue sensitivity to insulin) and PPAR-a (decreases triglycerides).
Rosiglitazone- binds PPAR-y
What are the side effects of thiazolidinediones?
Pioglitazone- bladder cancer, weight gain and edema
Rosiglitazone- increased risk of heart failure
CI- HF, pregnancy and liver dysfunction
What is the MoA of pramlintide?
Amylin analog, binds to its receptor in hindbrain causes decrease in glucagon release, delays gastric emptying- feeling of satiety.
Which are the incretins? What is its function?
Glucagon-like polypeptide-1 (GLP-1) and glucose dependent insulinotropic polypeptide (GIP). They increase glucose- induced insulin secretion cause less hypoglycemia.
What is the MoA of exenatide?
GLP-1 agonist same as liraglutide
What is function of DPP-4?
Inactivates GLP-1
What is the MoA of Sitagliptin?
DPP-4 inhibitor, increases levels of GLP-1, increase insulin secretion decreases glucagon secretion less hypoglycemia.
In the setting of diabetes + hypertension, which drug is the first choice to treat hypertension?
ACEI