Non-insulin diabetes pharm - Lowwang Flashcards

1
Q

What class of medication increases insulin secretion (secretagogues)?

What is the MOA?

A

Sulfonylureas.

Blockage of an ATP sensitive K+ channel on the B cell leading to depolarization, Ca influx, and vesicle fusion resulting in insulin release.

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2
Q

What are the side effects of the sulfonylureas?

A

hypoglycemia and weight gain.

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3
Q

glyburide

A

sulfonylureas

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4
Q

glimepiride

A

sulfonylureas

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5
Q

glipizide

A

sulfonylureas

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6
Q

What are some contraindications to the sulfonylureas?

A
Liver/kidney disease
G6PD deficiency (sulfa-containing drug--> hemolytic anemia)
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7
Q

What is the MOA of metformin?

A

Suppresses hepatic glucose production by potentiating the effects of insulin.

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8
Q

Contraindications to metformin use include:

A

1) congestive heart failure, especially unstable or acute
2) radiologic studies
3) renal impairment
4) metabolic acidosis, acute or chronic, including ketoacidosis

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9
Q

Metformin is the only drug in the class of _____.

A

Biguanines

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10
Q

Thiazolidinediones (TDZs) work in what fashion?

A

tl;dr Regulation of transcription factors by PPAR-gamma binding enhance insulin action.

Thiazolidinediones activate nuclear peroxisome proliferator-activated receptor (PPAR) gamma. They are true insulin sensitizers that enhance insulin action.

Binding of a thiazolidinedione (TZD) to a PPAR-γ receptor leads to ….regulation of the transcription of genes involved in adipocyte differentiation, and glucose and lipid metabolism.

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11
Q

What are the contraindications of TDZs?

A

HEART FAILURE, probably due to water retention (weight gain)
Femur fractures
Bladder cancer if taken >1yr
Liver disease

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12
Q

What is the incretin effect?

A

Oral glucose ingestion increases insulin release beyond IV administration of insulin.

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13
Q

What two hormones create the incretin effect?

How?

A

GLP-1, GIP

Act through G-protein receptors.

These peptides are important for the integrated control of gut motility, satiety and postprandial islet hormone responses. Rapidly inactivated by DPP-4.

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14
Q

GLP-1 controls blood glucose mainly by

A

Amplifying insulin secretion in response to po glucose
Inhibiting glucagon secretion
Decreasing gastric emptying
Signalling satiety to the brain.

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15
Q

GLP-1 is an incretin produced in the____ and ____.

A

Distal ileum and colon

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16
Q

GIP is an incretin produced in enteroendocrine K cells in the _____.

A

duodenum

17
Q

GIP is secreted after nutrient ingestion and enhances glucose-dependent insulin secretion. β-cells in individuals with type 2 diabetes are (resistant or sensitive) to the insulin stimulatory action of GIP.

A

resistant

18
Q

What is the prototypical GLP-1 agonist?

A

exenatide. It is resistant to cleavage by DPP-4, making it much more potent than endogenous GLP-1

19
Q

Pros of exenatide?

A

Lower A1c
BID administration
Weight loss

20
Q

Cons of exenatide?

A

subcutaneous injection
nausea
$$$$

21
Q

Name three GLP-1 agonists aside from exenatide?

A

Liraglutide (may be better than exenatide)
albiglutide
dulaglutide

22
Q

Name 4 DPP-4 (dipeptidylpeptidase-4) inhibitors

A

-gliptins

saxagliptin
sitagliptin
linagliptin
alogliptin

23
Q

What are pros of the DPP-4 inhibitors?

A

po administration (TID)
lower fasting glucose
weight neutral

24
Q

What is the MOA of DPP-4 inhibitors?

A

INhibit DPP-4, obviously. But they increase pancreatic secretion of insulin and decrease glucagon release.

25
Q

What are the cons/side effects of DPP-4 inhibitors?

A

Nasopharyngitis

Headache

26
Q

Name the Sodium Glucose Co-transporter-2 (SGLT-2) inhibitors.

A

Canagliflozin
dapagliflozin
empagliflozin

27
Q

How does Canagliflozin work?

A

Block glucose reuptake by the renal tubule.

28
Q

What are the pros of the SGLT-2 inhibitors?

A

po, BID
weight loss
lower BP

29
Q

What are the cons of the SGLT-2 inhibitors?

A

UIs
hypovolemia
hypokalemia

CONTRAINDICATED in RENAL DISEASE

30
Q

What are some pros of metformin?

A

Cheap

can be taken with other diabetes meds

31
Q

What are some cons of metformin?

A

must titrate up to dose

32
Q

GLP-1 is GLUCOSE DEPENDENT!

A

ok