Endo - Pharm (Part 1: Diabetes Drugs) Flashcards

Pg. 330-331 in First Aid 2014 Sections include: -Diabetes drugs

1
Q

What are the treatment strategies for DM1?

A

DM1 - low-sugar diet, insulin replacement

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2
Q

What are the treatment strategies for DM2?

A

DM2 - dietary modification and exercise for weight loss; oral agents, non-insulin injectables, insulin replacement

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3
Q

What are the treatment strategies for Gestational DM (GDM)?

A

Gestational DM (GDM) - dietary modifications, exercise, insulin replacement if lifestyle modification fails

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4
Q

Name 11 drug classes of diabetes drugs.

A

(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

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5
Q

What are 3 examples of rapid-acting insulin?

A

(1) Lispro (2) Aspart (3) Glulisine

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6
Q

What is the overall mechanism of insulin? What 3 organs does it effect, and how?

A

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

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7
Q

What are 3 clinical uses for rapid acting insulin, and in what context?

A

(1) DM1 (2) DM2 (3) GDM (postprandial glucose control)

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8
Q

What are 2 toxicities associated with insulin, and which is rare?

A

(1) Hypoglycemia (2) Rare hypersensitivity reactions

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9
Q

What is an example of short acting insulin?

A

Regular

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10
Q

What are 6 clinical uses for short acting insulin?

A

(1) DM1 (2) DM2 (3) GDM (4) DKA (IV) (5) hyperkalemia (+ glucose) (6) stress hyperglycemia

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11
Q

How is short acting insulin administered in DKA versus hyperkalemia?

A

DKA (IV); Hyperkalemia (+ glucose)

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12
Q

What is an example of intermediate acting insulin?

A

NPH

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13
Q

What are 3 clinical uses for intermediate acting insulin?

A

(1) DM1 (2) DM2 (3) GDM

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14
Q

What are 2 examples of long acting insulin?

A

(1) Glargine (2) Detemir

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15
Q

What are 3 clinical uses for long acting insulin?

A

(1) DM1 (2) DM2 (3) GDM (basal glucose control)

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16
Q

What is an example of Biguanides?

A

Metformin

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17
Q

What is the mechanism of Biguanides? What are 3 effects of this?

A

Exact mechanism is unknown; (1) Decrease gluconeogenesis, (2) Increase glycolysis, (3) Increase peripheral glucose uptake (insulin sensitivity).

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18
Q

What is the first line therapy for type 2 DM? How is it administered?

A

Metformin. First line therapy in type 2 DM. Oral.

19
Q

How does islet function relate to the use of Biguanides?

A

Can be used in patients without islet function.

20
Q

What are 2 toxicities associated with Biguanides? In what condition are Biguanides contraindicated?

A

(1) GI upset; (2) Most serious adverse effect is lactic acidosis (thus contraindicated in renal failure).

21
Q

What are the 2 major groups of Sulfonylureas? Give at least 2 examples in each group.

A

FIRST GENERATION: (1) Tolbutamide (2) Chlorpropamide; SECOND GENERATION: (1) Glyburide (2) Glimepiride (3) Glipizide

22
Q

What is the mechanism of Sulfonylureas, and what effect does this have?

A

Close K+ channel in Beta-cell membrane, so cell depolarizes => triggering of insulin release via increased Ca2+ influx

23
Q

What is the clinical use and limitation of Sulfonylureas?

A

Stimulate release of endogenous insulin in type 2 DM. Require some islet function, so useless in type 1 DM.

24
Q

What is a toxicity of all sufonlyureas? What are toxicities specific to first generation versus second generation sulfonylureas?

A

Risk of hypoglycemia increase in renal failure; FIRST GENERATION: disulfiram-like effects; SECOND GENERATION: hypoglycemia

25
Q

What is another name for Glitazones? What are 2 examples of such drugs?

A

Glitazones/Thiazolidinediones - (1) Pioglitazone (2) Rosiglitazone

26
Q

What is the mechanism/action of Glitazones/Thiazolidinediones? Explain this.

A

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.

27
Q

What is the clinical use of Glitazones/Thiazolidinediones?

A

Used as monotherapy in type 2 DM or combined with above agents (i.e., insulin, biguanides, sulfonylureas).

28
Q

What are 4 toxicities of Glitazones/Thiazolidinediones?

A

(1) Weight gain (2) Edema (3) Hepatotoxicity (4) Heart failure

29
Q

What are 2 examples of alpha-glucosidase inhibitors?

A

(1) Acarbose (2) Miglitol

30
Q

What is the mechanism/action of alpha-glucosidase inhibitors?

A

Inhibit intestinal brush-border alpha-glucosidases. Delayed sugar hydrolysis and glucose absorption => decreased postprandial hyperglycemia.

31
Q

What is a clinical use of alpha-glucosidase inhibitors?

A

Used as monotherapy in type 2 DM or in combination with above agents (i.e., insulin, biguanides, sulfonylureas, glitazones/thiazolidinediones).

32
Q

What is a toxicity of alpha-glucosidase inhibitors?

A

GI disturbances

33
Q

What is an example of amylin analogs?

A

Pramlintide

34
Q

What is the mechanism/action of amylin analogs?

A

Decrease gastric emptying, Decrease glucagon

35
Q

What are 2 clinical uses for Amylin analogs?

A

Type 1 and Type 2 DM

36
Q

What are 3 toxicities associated with Amylin analogs?

A

(1) Hypoglycemia (2) Nausea (3) Diarrhea

37
Q

What are 2 examples of GLP-1 analogs?

A

(1) Exenatide (2) Liraglutide

38
Q

What is the mechanism/action of GLP-1 analogs?

A

Increase insulin, Decrease glucagon release

39
Q

What is the clinical use for GLP-1 analogs?

A

Type 2 DM

40
Q

What are 3 toxicities of GLP-1 analogs?

A

(1) Nausea (2) Vomiting; (3) Pancreatitis

41
Q

What are 3 examples of DPP-4 inhibitors?

A

(1) Linagliptin (2) Saxagliptin (3) Sitagliptin

42
Q

What is the mechanism/action of DPP-4 inhibitors?

A

Increase insulin, Decrease glucagon release

43
Q

What is the clinical use for DPP-4 inhibitors?

A

Type 2 DM

44
Q

What are 2 toxicities associated with DPP-4 inhibitors?

A

Mild urinary or respiratory infections