Anti-diabetics Flashcards
Which are the rapid onset insulins?
Glulisine, Aspart, Lispro
Neutral Protamine Hagedorn (NPH)/isophane insulin belongs to slow onset or intermediate onset insulin?
Intermediate
What is the relative time to peak for regular insulin?
2-4 h
What is the relative time to peak for NPH?
4-8 h
Does glargine have peak in its action?
No peak (neither does detemir and degludec)
What is the best strategy to prevent microvascular complications of diabetes?
Tight glycemic control (HBA1c <7%)
Diabetic microvascular complications includes…?
Retinopathy, nephropathy, and neuropathy
Does intensive glycemic control prevent coronary heart disease?
No, control of diabetic dyslipidemia prevents macrovascular disease.
What is the most common side effect of intensive glycemic control?
Severe hypoglycemia
What is the mechanism of insulin secretion?
The pancreatic β cell in a resting state (fasting blood glucose) is hyperpolarized. Glucose, entering via GLUT 1 transporters is metabolized and elevates cellular ATP, which inhibits. K+ efflux through the KATP channel; the decreased K+ conductance (decreased efflux) results in depolarization, leading to Ca2+- dependent exocytosis of stored insulin.
What is the mechanism of action of sulfonylurea?
Bind to the sulfonylurea receptor (SUR1)→ Inhibit ATP-sensitive potassium channel → Inhibition of potassium efflux → depolarization → opening of calcium channels → release of stored insulin via calcium mediated exocytosis
What is the most important side effects of sulfonylurea?
Hypoglycemia and weight gain
Which sulfonylurea causes SIADH and disulfiram-like action?
Chlorpropamide (first generation)
What is the mechanism of action of metformin?
- Inhibits mitochondrial synthesis of ATP required for energy- intensive gluconeogenesis process in liver resulting in the main glucose lowering effect of reduced hepatic gluconeogenesis.
- Activates GLUT4 receptor in skeletal muscle which increases the basal glucose uptake in skeletal muscle cells. This is known as peripheral insulin sensitizing action.
What are the contraindications for metformin use?
Renal or liver disease, Cardiac failure, Chronic hypoxic lung disease (precipitates acidosis), Pregnancy, Radiologic procedure using IV iodinated contrast medium (due to potential for acute renal failure induced by contrast medium)