Diabetes drugs Flashcards
Insulin, rapid acting
Lispro, Aspart, Glulisine
Action:
Binds insulin receptor (tyrosine kinase activity) rapidly
“no LAG”
Liver: increase glucose stored as glycogen
Muscle: increase glycogen , protein synthesis; increase K+ uptake
Fat: increase TG storage
Use:
Type I DM
Type II DM
GDM (postprandial glucose control)
Risks/concerns:
Hypoglycemia
Lipodystrophy
Rare hypersensitivity rxns
Insulin, short acting
regular
Use: Type I DM Type II DM GDM DKA Hyperkalemia (+ glucose) Stress hyperglycemia
Risks/concerns:
Hypoglycemia
Lipodystrophy
Rare hypersensitivity rxns
Insulin, intermediate acting
NPH
Use:
Type I DM
Type II DM
GDM
Risks/concerns:
Hypoglycemia
Lipodystrophy
Rare hypersensitivity rxns
Insulin, long acting
Detemir, Glargine
Use:
Type I DM
Type II DM
GDM (basal glucose control)
Risks/concerns:
Hypoglycemia
Lipodystrophy
Rare hypersensitivity rxns
Metformin
Action:
Decrease gluconeogenesis
Increase glycolysis
Increase peripheral glucose uptake (increase insulin sensitivity)
Use:
Oral
First line therapy in Type 2 DM (causes modest weight loss)
Can be used in patients w/o islet function
Risks/Concerns:
GI upset
most serious adverse effect is lactic acidosis (thus contraindicated in renal insufficiency)
Sulfonylureas
Action:
Close K+ channel in beta cell membrane –> cell depolarizes –> insulin release via increase Ca2+ influx
Use:
Stimulate release of endogenous insulin in type 2 DM
Require some islet function, so unless in type 1 DM
Risks/Concerns:
Risk of hypoglycemia increases in renal failure, weight gain.
First gen: disulfiram-like effects
Second gen: hypoglycemia
Glitazones/thiazolidinediones
Pioglitazone, Rosiglitazone
Action:
Increase in insulin sensitivity in peripheral tissue
Binds to PPAR-y nuclear transcription regulator
Used as monotherapy in type 2 dM or combined with above agents
Safe to use in renal impairment
Risks/Concerns: Weight gain Edema Hepatotoxicity HF Increase risk of fractures
Meglitinides
Nateglinide, Repaglinide
Action:
Stimulate postprandial insulin release by binding to K+ channels on beta-cell membranes (site differs from sulfonylureas)
Use:
monotherapy in type 2 DM or combined with metformin
Risks/Concerns:
Hypoglycemia (increase risk with renal failure)
Weight gain
GLP-1 analogs
Exenatide, Liraglutide-sc injection
Actions: Increase glucose-dependent insulin release Decrease glucagon release Decrease gastric emptying Increase satiety
Use:
Type 2 DM
Risks/Concerns:
Nausea, vomiting, pancreatitis
modest weight loss
DPP-4 inhibitors
Linagliptin, Saxagliptin, Sitagliptin
Actions:
Inhibits DPP-4 enzyme that deactivates GLP-1
—>Increase glucose-dependent insulin release
Decrease glucagon release
Decrease gastric emptying
Increase satiety
Use:
Type 2 DM
Risks/Concerns:
Mild urinary or respiratory infections
Weight neutral
Amylin analogs
Pramlintide-sc injection
Actions:
Decrease gastric emptying
Decrease glucagon
Use:
Type 1 DM
Type 2 DM
Risks/Concerns:
Hypoglycemia, nausea
Sodium-glucose co-transporter 2 (SGLT-2) inhibitors
Canagliflozin, Dapagliflozin, Empagliflozin
Actions:
Block reabsorption of glucose in PCT
Use:
Type 2 DM
Risks/Concerns:
Glucosuria, UTIs, vaginal yeast infections, hyperkalemia, dehydration (orthostatic hypotension)
a-glucosidase inhibitors
Acarbose, miglitol
Actions:
Inhibit intestinal brush-border a-glucosidases
Delayed carbohydrate hydrolysis and glucose absorption
—> decrease in postprandial hyperglycemia
Use:
Type 2 DM
Risks/Concerns:
GI disturbances
