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Pharmacology > Endocrine: Drugs for Diabetes > Flashcards

Endocrine: Drugs for Diabetes Flashcards

1
Q

Which cell receptor does insulin activate to cause cell growth, proliferation, and gene expression?

A

MAP kinase

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2
Q

Which cell receptor does insulin activate to cause increased GLUT4 expression and synthesis of lipids, proteins, and glycogen?

A

PI-3K

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3
Q

How does insulin decrease glucose in the blood? (5)

A

GLUT4 translocation in skeletal/cardiac muscle and adipocytes
Activation of glycolysis
Activation of glycogen synthesis

Inhibition of gluconeogenesis
Inhibition of glycogenolysis

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4
Q

What are the rapid acting insulins?

A

Lispro
Aspart
Glulisine

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5
Q

What are the short acting insulins?

A

Regular insulin

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6
Q

Which are the intermediate acting insulins?

A

NPH insulin

-not used much anymore

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7
Q

What are the longer acting insulins?

A

Detemir

Glargine
-longest acting

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8
Q

Clinical use of lispro, aspart, or glulisine?

A

Decrease the post prandial hyperglycemia seen after meals

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9
Q

Which insulin is used for IV?

A

Regular insulin

-can use in emergency situations like DKA, HHS, or hyperkalemia

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10
Q

So say you wanted to cover someone with diabetes both after meals and all day, which combo of insulins would be best?

A

A rapid acting + a long

So: lispro, aspart, or glulisine + detemir/glargine

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11
Q

What are some adverse effects of insulin?

A

Hypoglycemia, lipodystrophy
Weight gain
Resistance
Hypokalemia

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12
Q

MOA of pramlintide? (3)

A

Amylin analog

  • blocks glucagon secretion
  • slows gastric emptying
  • increases satiety
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13
Q

What type of DM does pramlintide treat?

A

Type 1 or 2

The rest, besides insulin, only treat type 2

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14
Q

What are the adverse effects of pramlintide?

A

Nausea, vomiting, diarrhea

Severe hypoglycemia if used with insulin

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15
Q

MOA of Exenatide or Liraglutide?

A

GLP-1 agonists

-activates Gs, increases cAMP and PKA, which causes exocytosis of insulin

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16
Q

Adverse effects of the GLP-1 agonists (exenatide and liraglutide)

A

N/V, diarrhea, anorexia

Hypoglycemia

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17
Q

What is the suffix of all the DPP-4 inhibitors

A

Gliptin!

Sitagliptin, linagliptin, saxagliptin, alogliptin

18
Q

MOA of the DPP-4 inhibitors (gliptins)

A

Decrease breakdown of GLP-1

-ultimately increases insulin release

19
Q

Adverse effects of the DPP-4 inhibitors?

A

Hypoglycemia

20
Q

What is the MOA of Sulfonylureas/meglitinides?

A

block K-ATPase channels (via SUR1), Ca++ rushes in and Insulin is released

21
Q

What are the first gen sulfonyureas

A

Amides

Chlorpropamide, tolbutamide, tolazamide

22
Q

What are the second generation sulfonylureas?

A

Glipizide
Glyburide
Glimepiride

23
Q

What are the meglitinides?

A

Nateglinide
Repaglinide

-glinides

24
Q

What are the adverse effects of the sulfonyureas/meglitinides?

A

Hypoglycemia
Weight gain
Secondary failure

25
Q

What drugs can enhance the effect of sulfonylureas?

A

sulfonamides, clofibrates, aspirin/NSAIDs

Ethanol

CYP inhibitors: azoles, gemfibrozil. cimetidine

26
Q

What drugs can decrease the glucose lowering effect of sulfonylureas?

A

Drugs that inhibit insulin secretion: B-blockers, CCBs

CYP inducers: phenytoin, griseofluvin, rifampin

27
Q

Clinical use for the meglitinides?

A

Control of postprandial hyperglycemia in T2DM

-shorter acting than the sulfonylureas

28
Q

MOA of metformin?

A

activation of AMP kinase

-decreases gluconeogenesis, increases insulin sensitivity

29
Q

Which diabetic agent is usually first line in those w T2DM?

A

Metformin

  • no real issue w hypoglycemia
  • promotes weight loss
  • taken orally (instead of injection)
  • Can be combined
30
Q

How is metformin excreted?

A

Unmetabolized

-watch in those w renal failure!!

31
Q

Adverse effects of metformin?

A

GI upset

Lactic acidosis

32
Q

What conditions is metformin contraindicated in?

A

Renal or liver issues

33
Q

What are the thiazolidinediones (TZDs)?

A

-glitazones

Pioglitazone
Rosiglitazone

34
Q

MOA of the TZDs?

A

ligands for PPARy

-increase adiponectin and GLUT4

35
Q

Whare TZDs safe for those with renal issues?

A

Yes

36
Q

Adverse effects of TZDs?

A

Weight gain

Edema
-increases ENaC channels

Exacerbate HF
-increased water retention

Osteoporosis
-suppress osteoblasts

37
Q

MOA of canagliflozin, dapagliflozin, empagliflozin?

A

SGLT2 inhibitors

-work at PCT to block reabsorption of glucose

38
Q

Adverse effects of the SGLT2 inhibitors (flozins)

A

Osmotic Diuresis and Orthostatics

Genital and UTIs (candidiasis)

39
Q

Benefitial effects of SGLT2 inhibitors?

A

Reduces plasma uric acid levels
Weight loss

improves overall cardiovascular and renal outcomes

40
Q

MOA of acarbose and Miglitol?

A

competitive inhibition of a-glycosidases

-block resorption of disaccharides in intestines

41
Q

Effect of acarbose and miglitol on glucose levels?

A

Lower postprandial hyperglycemia to create insulin sparing effect

42
Q

Adverse effects of acarbose and miglitol?

A

GI Upset: malabsorption and flatulence

Pharmacology (50 decks)

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