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DEMS exam 2 part 1 > Treatment of Diabetes - Oral Agents > Flashcards

Treatment of Diabetes - Oral Agents Flashcards

1
Q

what is the MOA of sulfonylureas

A

Increase pancreatic Beta-cell insulin secretion by: Closing ATP-sensitive potassium channels -> depolarizes the membrane, -> opening of voltage-gated calcium channels -> influx of calcium into the Beta-cell -> fusion of insulin-containing secretory granules with the cell membrane -> insulin secretion.

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2
Q

Name the 3 Sulfonylureas

A

glipizide (Glucotrol), glyburide (Diabeta, Micronase), and glimepiride (Amaryl).

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3
Q

The major side effects of sulfonylureas are ______

A

hypoglycemia and weight gain

nausea and gastrointestinal discomfort.

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4
Q

Sulfonylureas must be used with caution in patients with ________

A

moderate to severe renal insufficiency or liver disease

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5
Q

Sulfonylureas must not be used in patients with allergy to _____- drugs, and can cause ______ in individuals with glucose 6-phosphate dehydrogenase (G6PD) deficiency.

A

sulfa,

hemolytic anemia

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6
Q

what is the MOA of Metformin

A

acts mainly at the liver to potentiate the suppressive effects of insulin on hepatic glucose production

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7
Q

what are the side effects of Metformin

A

nausea, vomiting, bloating, and diarrhea

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8
Q

what are the Contraindications to metformin use:

A

1) congestive heart failure, especially unstable or acute
2) intravascular iodinated contrast media for radiologic studies
3) eGFR <30 mL/min/1.73 m2
4) metabolic acidosis, acute or chronic, including ketoacidosis

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9
Q

what is the “incretin effect”

A

when glucose is given orally there is a 2-3 fold increase in insulin secretion when compared to IV glucose

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10
Q

what are Two specific gut peptides that account for a substantial proportion of the incretin effect:

A

glucagon-like peptide-1 (GLP-1) and

glucose-dependent insulinotropic polypeptide or [gastric inhibitory peptide (GIP)]

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11
Q

The actions of GIP and GLP-1 are transduced via G protein-coupled receptors, coupled to _______

A

adenyl cyclase

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12
Q

GIP receptors are predominantly expressed in ______ cells, while GLP-1 receptors are also expressed in the ________, among other tissues.

A

pancreatic islet ,

brain and heart

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13
Q

Both GIP and GLP-1 are rapidly inactivated within minutes of appearing in the circulation by an enzyme called _______

A

dipeptidyl peptidase-4 (DPP-4).

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14
Q

GLP-1 is an incretin produced in enteroendocrine L cells located in the _____ and ______

A

distal ileum,

colon.

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15
Q

how does GLP-1 control blood glucose ?

A

mainly by amplifying glucose-stimulated insulin secretion, inhibiting glucagon secretion, and slowing gastric emptying.

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16
Q

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

A

duodenum

17
Q

GIP administration has not been shown to be effective for the treatment of type 2 diabetes. why?

A

beta-cells in individuals with type 2 diabetes are resistant to the insulin stimulatory action of GIP

18
Q

Name the GLP-1 agonists

A 
exenatide (Byetta), 
liraglutide (Victoza), 
exenatide Qwk (Bydureon), 
dulaglutide (Trulicity), 
lixisenatide (Lyxumia
19
Q

name the DPP-4 inhibitors

A

sitagliptin (Januvia),
saxagliptin (Onglyza),
linagliptin (Tradjenta),
alogliptin (Nesina)

20
Q

The use of GLP-1 agonists is not recommended in patients with _______

A

active pancreatitis, a history of pancreatitis, or pancreatic carcinoma

21
Q

what are the downsides to GLP-1 agonists

A

SC injections
Side effects
Expensive

22
Q

How do DPP-4 inhibitors work

A

They enhance pancreatic insulin secretion and suppress glucagon secretion, but do not alter gastric emptying or affect appetite

23
Q

what are the main adverse effects of DPP-4 inhibitors

A

nasopharyngitis and headache

24
Q

what are DPP-4 (dipeptidylpeptidase-4) inhibitors ?

A

they inhibit the enzyme that cleaves incretines

25
Q

how do Sodium Glucose Co-transporter-2 (SGLT-2) inhibitors work

A

By inhibiting reabsorption of glucose by the kidneys, increasing glucose excretion, and reduces circulating glucose levels.

26
Q

Name the 3 Sodium Glucose Co-transporter-2 (SGLT-2) inhibitors

A

canagliflozin (Invokana),
dapagliflozin (Farxiga),
empagliflozin (Jardiance)

27
Q

what are The main beneficial effects Sodium Glucose Co-transporter-2 (SGLT-2) inhibitors besides blood glucose lowering?

A

weight loss and blood pressure lowering.

28
Q

what are Key adverse effects of Sodium Glucose Co-transporter-2 (SGLT-2) inhibitors

A

Increased risk for genital and urinary tract infections, hypovolemia,
hypokalemia,
possible effects on bone metabolism (increased fracture risk),
euglycemic diabetic ketoacidosis,
and (for canagliflozin) amputation

29
Q

Sodium Glucose Co-transporter-2 (SGLT-2) inhibitors should not be used in patients with _______

A

severe renal disease, end stage renal disease, or patients on dialysis

30
Q

Thiazolidinediones should not be used in which patients?

A

individuals with active liver disease, moderate or severe congestive heart failure, or significant cardiovascular risk.

31
Q

how do Thiazolidinediones work

A

insulin sensitizers that enhance insulin action, mainly at the level of skeletal muscle and adipose tissue, with a lesser effect to reduce hepatic gluconeogenesis

32
Q

Name the 2 Thiazolidinediones

A

rosiglitazone (Avandia) and pioglitazone (Actos)

33
Q

which individuals should have a stringent a1c target of <6.5%

A

relatively recent onset of diabetes,
are motivated,
have few or mild complications and/or comorbidities ts.

34
Q

which individuals should have a less stringent a1c goal of <8%

A

1) patients with hypoglycemia unawareness,
2) limited life expectancy,
3) advanced microvascular or macrovascular complications,
4) extensive comorbid conditions,
5) those with longstanding diabetes

35
Q

how often should A1c be checked in diabetic patients

A

Hemoglobin A1c is drawn at least twice and up to 4 times per year to monitor effectiveness of glycemic control.

36
Q

when and how often should patients check their blood glucose

A

at least twice per day at specific time points: fasting, before lunch, before dinner, and at bedtime.

37
Q

which glucose lowering drugs are the cheapest

A

metformin and sulfonlyureas at $4/month

DEMS exam 2 part 1 (17 decks)

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