Endo - Pharm (Part 1: Diabetes Drugs) Flashcards
Pg. 330-331 in First Aid 2014 Sections include: -Diabetes drugs
What are the treatment strategies for DM1?
DM1 - low-sugar diet, insulin replacement
What are the treatment strategies for DM2?
DM2 - dietary modification and exercise for weight loss; oral agents, non-insulin injectables, insulin replacement
What are the treatment strategies for Gestational DM (GDM)?
Gestational DM (GDM) - dietary modifications, exercise, insulin replacement if lifestyle modification fails
Name 11 drug classes of diabetes drugs.
(1) Insulin, rapid acting (2) Insulin, short acting (3) Insulin, intermediate acting (4) Insulin, long acting (5) Biguanides (6) Sulfonylureas (7) Glitazones/Thiazolidinediones (8) Alpha-glucosidase inhibitors (9) Amylin analogs (10) GLP-1 analogs (11) DPP-4 inhibitors
What are 3 examples of rapid-acting insulin?
(1) Lispro (2) Aspart (3) Glulisine
What is the overall mechanism of insulin? What 3 organs does it effect, and how?
Bind insulin receptor (tyrosine kinase activity); (1) Liver: Increase glucose stored as glycogen (2) Muscle: Increase glycogen, protein synthesis; Increase K+ uptake (3) Fat: Increase TG storage
What are 3 clinical uses for rapid acting insulin, and in what context?
(1) DM1 (2) DM2 (3) GDM (postprandial glucose control)
What are 2 toxicities associated with insulin, and which is rare?
(1) Hypoglycemia (2) Rare hypersensitivity reactions
What is an example of short acting insulin?
Regular
What are 6 clinical uses for short acting insulin?
(1) DM1 (2) DM2 (3) GDM (4) DKA (IV) (5) hyperkalemia (+ glucose) (6) stress hyperglycemia
How is short acting insulin administered in DKA versus hyperkalemia?
DKA (IV); Hyperkalemia (+ glucose)
What is an example of intermediate acting insulin?
NPH
What are 3 clinical uses for intermediate acting insulin?
(1) DM1 (2) DM2 (3) GDM
What are 2 examples of long acting insulin?
(1) Glargine (2) Detemir
What are 3 clinical uses for long acting insulin?
(1) DM1 (2) DM2 (3) GDM (basal glucose control)
What is an example of Biguanides?
Metformin
What is the mechanism of Biguanides? What are 3 effects of this?
Exact mechanism is unknown; (1) Decrease gluconeogenesis, (2) Increase glycolysis, (3) Increase peripheral glucose uptake (insulin sensitivity).
What is the first line therapy for type 2 DM? How is it administered?
Metformin. First line therapy in type 2 DM. Oral.
How does islet function relate to the use of Biguanides?
Can be used in patients without islet function.
What are 2 toxicities associated with Biguanides? In what condition are Biguanides contraindicated?
(1) GI upset; (2) Most serious adverse effect is lactic acidosis (thus contraindicated in renal failure).
What are the 2 major groups of Sulfonylureas? Give at least 2 examples in each group.
FIRST GENERATION: (1) Tolbutamide (2) Chlorpropamide; SECOND GENERATION: (1) Glyburide (2) Glimepiride (3) Glipizide
What is the mechanism of Sulfonylureas, and what effect does this have?
Close K+ channel in Beta-cell membrane, so cell depolarizes => triggering of insulin release via increased Ca2+ influx
What is the clinical use and limitation of Sulfonylureas?
Stimulate release of endogenous insulin in type 2 DM. Require some islet function, so useless in type 1 DM.
What is a toxicity of all sufonlyureas? What are toxicities specific to first generation versus second generation sulfonylureas?
Risk of hypoglycemia increase in renal failure; FIRST GENERATION: disulfiram-like effects; SECOND GENERATION: hypoglycemia
What is another name for Glitazones? What are 2 examples of such drugs?
Glitazones/Thiazolidinediones - (1) Pioglitazone (2) Rosiglitazone
What is the mechanism/action of Glitazones/Thiazolidinediones? Explain this.
Increase insulin sensitivity in peripheral tissue. Binds to PPAR-gamma nuclear transcription regulator. Genes activated by PPAR-gamma regulate fatty acid storage and glucose metabolism. Activation of PPAR-gamma increases insulin sensitivity and levels of adiponectin.
What is the clinical use of Glitazones/Thiazolidinediones?
Used as monotherapy in type 2 DM or combined with above agents (i.e., insulin, biguanides, sulfonylureas).
What are 4 toxicities of Glitazones/Thiazolidinediones?
(1) Weight gain (2) Edema (3) Hepatotoxicity (4) Heart failure
What are 2 examples of alpha-glucosidase inhibitors?
(1) Acarbose (2) Miglitol
What is the mechanism/action of alpha-glucosidase inhibitors?
Inhibit intestinal brush-border alpha-glucosidases. Delayed sugar hydrolysis and glucose absorption => decreased postprandial hyperglycemia.
What is a clinical use of alpha-glucosidase inhibitors?
Used as monotherapy in type 2 DM or in combination with above agents (i.e., insulin, biguanides, sulfonylureas, glitazones/thiazolidinediones).
What is a toxicity of alpha-glucosidase inhibitors?
GI disturbances
What is an example of amylin analogs?
Pramlintide
What is the mechanism/action of amylin analogs?
Decrease gastric emptying, Decrease glucagon
What are 2 clinical uses for Amylin analogs?
Type 1 and Type 2 DM
What are 3 toxicities associated with Amylin analogs?
(1) Hypoglycemia (2) Nausea (3) Diarrhea
What are 2 examples of GLP-1 analogs?
(1) Exenatide (2) Liraglutide
What is the mechanism/action of GLP-1 analogs?
Increase insulin, Decrease glucagon release
What is the clinical use for GLP-1 analogs?
Type 2 DM
What are 3 toxicities of GLP-1 analogs?
(1) Nausea (2) Vomiting; (3) Pancreatitis
What are 3 examples of DPP-4 inhibitors?
(1) Linagliptin (2) Saxagliptin (3) Sitagliptin
What is the mechanism/action of DPP-4 inhibitors?
Increase insulin, Decrease glucagon release
What is the clinical use for DPP-4 inhibitors?
Type 2 DM
What are 2 toxicities associated with DPP-4 inhibitors?
Mild urinary or respiratory infections
