Anti-hyperglycemics Flashcards
Anti-hyperglycemics
Insulin replacements (Lispro, Regular, NPH, Glargine), Inhibitors of CHO absorption, Insulin secretagogues, Insulin sensitizers, Insulin releasers, Na-glucose cotransporter 2 inhibs
What are the rapid insulin preparations
Lispro, Aspart, Glulisine
What is the short acting insuline preparation?
Regular (human)
What is the intermediate insulin preparation?
NPH (neutral protamine hagadorn)
What are the long-acting insulin preparations?
Glargine, Detimir
What are the CHO absorption inhibitors?
Acarbose, Miglitol
Acarbose, Miglitol (CHO absorption) - MoA
alpha-glucosidase inhibitor prevents cleavage of disaccharides to monosaccharides
Acarbose, Miglitol (CHO absorption) - adverse effects
GI side effects include flatulence (80%), diarrhea (27%) and nausea (8%) . Titrating the dose of drug slowly reduces GI side effects.
What are the insulin secretagogues?
Sulfonylureas
Repaglinide
Nateglinide
Sulfonylureas - MoA
Blocks potassium channel. Cell becomes more positive and depolarizes. Calcium enters cell and causes a release of insulin granules
What are the sulfonylureas?
1st generation - chlorpropamide
2nd generation - Glyburide, Glimeperide, Glipizide
Sulfonylureas - adverse effects
Hypoglycemia and weight gain
Sulfonylureas - Contraindications
Type 1 Diabetes
Pregnancy
Lactation
Significant Renal and/or hepatic insufficiency
Insulin Secretagogues -Meglitinides (Repaglinide, Nateglinide)
Same mechanism of action as sulfonylureas but needs glucose to work.
Metabolized by liver, so watch out for liver failure
Insulin Sensitizers
Biguanides, Thiazolidinediones
Biguanides example
Metformin
Metformin (Biguanide) - MoA
Decr. Mitochondrial ATP production
Net: decr. hepatic glucose production and incr. glucose uptake in muscle and adipose
Incr. expression or activity of glycolytic enzymes and Glut-4
Can reduce plasma glucose by 25% and decrease Hb A1C by 1-2%. Also lowers TG levels
Metformin - adverse effect
metabolic acidosis with non-compliance
Metformin - contraindication
Not used if receiving contrast
Not used with acidosis
Not used with renal failure (>1.5 men and 1.4 women)
Thiazolidinediones (insulin sensitizers) example
Pioglitazone
Pioglitazone - MoA
Activate nuclear receptors - peroxisome proliferator-activator receptors (PPAR-y)
Stimulates fat synthesis and decreases free fatty acids.
Increases insulin sensitivity
Pioglitazone - adverse rxns
Can worsen or cause heart failure. Also causes edema and a decrease in hematocrit
New Classes - Amylin, Pramlintide - MoA
suppresses inappropriate postprandial
glucagon secretion
delays gastric emptying
suppress appetite.
New Classes - Incretin - Glucagon-like peptide (GLP) - MoA
- increases Beta cell number
- enhances insulin release
- Inhibits glucagon secretion
- delays gastric emptying
- suppress appetite, weight loss
GLP-1 agonists (2)
Exenatide, Liraglutide
DPP-4 inhibitors (4)
Sitagliptin, Linagliptin, Alogliptin, Saxagliptin
DPP-4 inhibitors - MoA
Blocks enzyme that degrades incretin (GLP-1) called dipeptidl peptidase-4
Sodium Glucose co-transporter inhibitors (2)
Canagliflozin
Dapagliflozin
Sodium-Glucose co-transporter inhibitor - MoA
Inhibits the sodium-glucose co-transporter 2 in the kidney leads to an increase in urine glucose and a decrease in blood glucose
Sodium-glucose co-transporter inhibitor - contraindication
Renal insufficiency
Hypotension
Hyperkalemia
Hyperglycemics
Glucagon Diazoxide (opens K channels in beta cells and prolongs open state, hyperpolarizes cell)
