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Pharm II Final Annie & Lauren > Antidiabetics (wait is this pharm or clin med?? 🤔) > Flashcards

Antidiabetics (wait is this pharm or clin med?? 🤔) Flashcards

1
Q

What are the 2 agents that are used to INCREASE blood sugar?

A

Glucagon

Diazoxide (Proglycem)

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2
Q

What happens to levels when you inject insulin (in anyone)

Blood glucose:

Pyruvate and lactate:

Inorganic phosphate:

Plasma potassium:

A

Glucose decreases

Pyruvate and Lactate: increase (metabolism)

Phosphate: decrease (metabolism)

Potassium- decreases. Glucose in cells makes Na-K pumps work more

(PROBABLY not on test)

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3
Q

Do we use insulin for Type 1 or Type 2

A

Both

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4
Q

What are the adverse reactions of insulin?

A

HYPOGLYCEMIA**

Weight gain***

Cough (inhaled only)

Local reactions (allergy)

Lipodystrophy and lipohypertrophy

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5
Q

What kinds of things can cause hypoglycemia in a patient who uses insulin?

A

Taking too much insulin

Change in insulin type preparation

Too many insulin secreting drugs

Spontaneous decreases in insulin requirements (no longer pregnant or stressed out)

Vigorous exercise ⛹️‍♂️

Failure to eat

Overindulgence in alchol🍻🍸🥃🍾🍷🥂🍺🍹

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6
Q

How do you treat hypoglycemia in someone who is unconscious?

A

Give 50% glucose solution IV until they wake up

Could also theoretically give glucagon but no one does that

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7
Q

What kinds of things increase insulin requirement?

A

ANYTHING that increases stress**
….Like SURGERY, preganncy, thyrotoxicosis, infection

Acromegaly and Cushings

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8
Q

If your patient is having surgery, what do you need to do to their insulin dose?

A

Increase it! (Surgery is stressful)

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9
Q

What are the 4 preparation types of insulin?

A

Rapid

Short (Regular)

Intermediate

Long acting

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10
Q

What are the 4 types of rapid acting insulin available

A

Lispro

Aspart

Glulisine

Inhaled*

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11
Q

What kind of insulin is used first in type II DM?

A

Long-acting (basal)

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12
Q

What is necessary for glucagon to work to increase blood glucose?

A

You must have glycogen stores!**

NOT EVERYONE DOES

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13
Q

What is Diazoxide (Proglycem)?

A

It’s used to INHIBIT insulin secretion.

Does so by acting on K+ channels so no insulin can be released.

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14
Q

Who do we give Diazoxide (Proglycem) to?

A

Patients with insulinoma (insulin secreting tumor)

Diazoxide inhibits insulin secreting and raises blood sugar

NOT patients with diabetes

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15
Q

What are the 4 rapid acting insulins?

A

Insulin lispro (Humalog)

Insulin aspart (NovoLog)

Insulin glulisine (Apidra)

Insulin, inhaled (Afrezza)

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16
Q

What are the short acting insulin’s

A

Regular Insulin (Novolin R, Humulin R)

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17
Q

What are the intermediate acting insulins?

A

NPH or Isophane Insulin (Humulin N, Novolin N)

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18
Q

What are the long acting insulins?

A

Insulin glargine (Lantus)

Insulin detemir (Levemir)

Insulin degludec (Tresiba)

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19
Q

What is the #1 killer of diabetics

A

cardiovascular disease

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20
Q

What is the initial drug of choice for Type 2 diabetics, as long as their A1C is under 10%?

A

Metformin

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21
Q

What is the MOA of Metformin?

A

Decreases glucose in an insulin-INDEPENDENT matter:

Removes glucose from blood (AMPK)

Secretion of GLP-1

Decrease glucose absorption from GI

Decrease glucagon levels

Decreased gluconeogenesis (mitochondrial enzyme inhibition)

notice that not one of these says that it INCREASES insulin***

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22
Q

What glycemic effects does metformin have?

A

Decreases A1C a LOT! (1-1.5%)

Promotes a euglycemic state *!!! (as opposed to hypoglycemic)

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23
Q

Why is it ok to give metformin to women with PCOS that DONT have diabetes?

A

Because metformin promotes a euglycemic state and NOT a hypoglycemic state

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24
Q

What are the cardiovascular effects of metformin?

A

Lower triglycerides by 15-20%

Decrease Macrovascular events (aka heart attacks)*******

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25
Q

What are some “other” effects of metformin?

A

Weight neutral (does NOT increase insulin release, so it has no effect on weight!)***

Decrease all-cause mortality events

BEST pharmacologic therapy for diabetes prevention in prediabetics**

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26
Q

Will metformin cause weight gain

A

No*****

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27
Q

How is metformin excreted?

A

Through the kidneys

Remember the whole contrast and holding metformin thing?

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28
Q

What are the adverse effects of metformin?

A

Lactic Acidosis** LETHAL

Diarrhea*** (53% of patients!)

Hypoglycemia almost NEVER

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29
Q

What are the contraindications/precautions for metformin?

A

Anything that can cause lactic acidosis:

Kidney disease (contraindicated in renal failure or GFR <30)

Liver disease

Alcoholism

Diseases that predispose to tissue hypoxia: COPD, CHF

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30
Q

What are incretins?

A

GLP-1 and GIP that get released when you take glucose ORALLY

They increase insulin release and inhibit glucagon release (decreased hepatic gluconeogenesis)

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31
Q

What is the MOA of GLP-1 agonists?

A

They are GLP-1 agonists that are ~resistant~ to DPP-4 degradation

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32
Q

What are the 5 GLP-1 agonists?

A

Exenatide (Byetta, Bydureon)

Liraglutide (Victoza)

Dulaglutide (Trulicity)

Albiglutide (Tanzeum)

Lixisenatide (Adlyxin)

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33
Q

How are GLP-1 agonists administered?

A

SC injections 2x/day or 1x/week

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34
Q

What are the effects of GLP-1 agonists?

A

Increase the effects of insulin

Large A1C decrease (1-1.5%)

Liraglutide (Victoza) will decrease macrovascular events**

Lower BP (maybe)

Slows gastric emptying= eating less***

Weight loss**

Increased B cell number and function**

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35
Q

Which GLP-1 agonist is only approved for weight loss?

A

Liraglutide (Sandexa)

🏝👙 (take it before you hit the SAND)

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36
Q

What are the adverse effects of GLP-1 agonists?

A

ACUTE PANCREATITIS* ON TEST***!!

Hypoglycemia (low risk)

GI

Hypersensitivity

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37
Q

What are the contraindications/precautions of GLP-1 agonists?

A

Pancreatitis (now or ever)***

Thyroid Cancer BLACK BOX WARNING it is thought that it exacerbates thyroid cancer when it increases the # of B cells

38
Q

What are the 4 DPP-4 inhibitors?

A

Sitagliptin (Januvia)

Saxagliptin (Onglyza)

Linagliptin (Tradjenta)

Alogliptin (Nesina)

the gliptins

39
Q

What is the MOA of DPP-4 inhibitors?

A

Potentiates the effects of endogenous incretins by inhibiting their breakdown by DPP-4

40
Q

How are DPP-4 inhibitors administered?

A

Oral

41
Q

What are the therapeutic effects of DPP-4 inhibitors?

A

Decrease A1C a medium amount (0.5-1%)

Weight neutral

42
Q

What are the adverse effects of DPP-4 inhibitors?

A

Hypoglycemia (rare)

Acute pancreatitis***

Severe joint pain

43
Q

What are the contraindications/precautions of DPP-4 inhibitors?

A

Pancreatitis now or ever*

Slow GI

Renal impairment

44
Q

What are the 4 SGLT-2 inhibitors?

A

Canagliflozin (Invokana)

Dapagliflozin (Farxiga)

Empagliflozin (Jardiance)

Ertugliflozin (Steglatro)

“Gli” -> glucose

“Flozin” -> flowing (kidney)

45
Q

What is the MOA of SGLT-2 inhibitors?

A

Inhibits the sodium-glucose cotransporter (SGLT-2) in the kidney= makes you pee out a lot of glucose

46
Q

What are the 2 antidiabetic drugs that are FDA approved too treat Cardiovascular Disease’?

A

Liraglutide (Victoza)

Empagliflozin (Jardiance)

This is probably due to their weight loss effect

47
Q

Do SGLT-2 inhibitors do anything to address the insulin resistance problem

A

No

48
Q

What are the therapeutic effects of SGLT-2 inhibitors?

A

Medium A1C decrease (0.5-1%)

Empagliflozin decreases CV events****

Lower BP*

Weight Loss** (you’re pissing out glucose)

49
Q

What are the adverse effects of SGLT-2 inhibitos?

A

Vaginal yeast infections, UTIs and increased urinary frequency**** You’re pissing out glucose 🧁🚽

Hyponatremia***Increased urinary Na+ excretion due to increased H2O in proximal tubule

Osmotic diuresis**

Hypotension, dizziness, syncope, dehydration due to diuresis**

Hypoglycemia rarely

50
Q

What are the contraindications/precautions for SGLT-2 inhibitos?

A

Contraindicated in severe kidney disease or on dialysis (these drugs wont work if your kidneys are shitty)

Prone to UTIs or other GU infections

51
Q

How would an SGLT-2 inhibitor affect someone with an overactive bladder?

A

It would be made WORSE due to the osmotic diuresis and increased need to pee

52
Q

What are the 2 thiazolidinediones (TZDs)?

A

Pioglitazone (Actos)

Rosiglitazone (Avandia)

the glitazones

53
Q

What is the MOA of thiazolidinediones (TZDs)?

A

They are “insulin sensitizers”= specifically target insulin resistance**

Bind to PPARγ receptor which causes post-receptor insulin-mimetic action*****

Increased expression of GLUT4 transporter

54
Q

What antilipid drug class are Thiazolidinediones (TZDs) similar to?

A

Fibrates (PPAα ligands)

55
Q

Do thiazolidinediones (TZDs) specifically target insulin resistance?

A

YES. They are “Insulin sensitizers”*****

56
Q

What are the therapeutic effects of thiazolidinediones?

A

High A1C decrease (1-1.5%)

Lower triglycerides in long-term use (insulin is getting glucose into cells, so there’s less FFA’s)

Increase HDL

Lower insulin resistance**

May help prediabetics prevent development of DM

57
Q

What are the adverse effects of thiazolidinediones?

A

Hypoglycemia **(sometimes)

Edema (can cause HF in patients with CHF!!)

Weight gain ** (maybe due to edema)

Bone fracture risk** (no one knows why)

58
Q

What are the contraindications/precautions for thiazolidinediones?

A

Contraindicated in heart failure ** due to edema***

Hepatic disease (1st TZD was taken off the market for this!)

59
Q

What are the 2 α-glucosidase inhibitors?

A

Acarbose (Precose)

Miglitol (Glyset)

60
Q

What is the only Class of antidiabetic agent that is used in type 1 and Type 2 diabetes?

A

α-glucosidase inhibitors

Used off-label in type 1 becasue if they eat too many carbs than the amount of insulin they took for their insulin profile, they can take this to prevent the absorption of the carbs)

61
Q

What is the MOA of α-glucosidase inhibitors?

A

Inhibit α-glucosideases in small intestine= delayed carb digestion and absorption

62
Q

How do you take α-glucosidase inhibitors?

A

Orally, pre-prandially

63
Q

What are the therapeutic effects of α-glucosidase inhibitors?

A

Decrease postprandial glucose (can lower A1C)

No effect on weight (?!?!)

64
Q

What are the adverse effects of α-glucosidase inhibitors?

A

GI effects- diarrhea and flatulence**** (all those undigested carbs make your gut bacteria very happy!)💩💨

65
Q

Do α-glucosidase inhibitors cause hypoglycemia?

A

NEVER**

66
Q

How do Sulfonylureas work?

A

They float over to the β-cells and bind to a K+ channel, which depolarizes the membrane and increases Calcium influx into the cells= big fat insulin release

67
Q

What are the therapeutic effects of sulfonylureas?

A

Lower A1C a lot (1-1.5%)

Decrease risk of MI and microvascular disease

Decrease mortality

Decrease glucagon= lower hepatic glucose production

Potentiate action of insulin on target tissues

68
Q

What are the adverse effects of sulfonylureas?

A

HYPOGLYCEMIA** the worst drug for this

Weight gain*****

69
Q

What are the contraindications of sulfonylureas?

A

SULFA ALLERGY!!!!!*****

70
Q

Which diabetic drug class has the highest risk of causing hypoglycemia (other than insulin)

A

Sulfonylureas

71
Q

Why dont we use sulfonylureas very much anymore?

A

They have the highest risk of hypoglycemia

72
Q

A guy went on a trip to the Himalayan Mountains, and he got Acute mountain sickness. The doctor there gave him a drug to treat this and he had an allergy! What drug class can we not use to treat his Type II diabetes

A

Sulfonylureas, because they are SULFAS

He was treated with acetzolamide- a sulfa

73
Q

What are the 1st generation sulfonylureas, and what are the points you need to know about them? (Maybe???)

A

Tolbutamide- short acting (less hypoglycemia)

Chlorpropamide- long acting, disulfiram-like effect, WORST hypoglycemia

Tolazamide

74
Q

What are the 3 second generation sulfonylureas, and which ones has the highest risk of hypoglycemia?

A

Glyburide- most hypoglycemia

Glipizide-least hypoglycemia

Glimepiride

75
Q

Which sulfonylureas generation is the most potent: 1st or 2nd?

A

2nd

76
Q

What are meglitinides?

A

Almost the same thing as sulfonylureas, but they are NOT sulfonamides= can be used in a sulfa allergy***

77
Q

What are the 2 Meglitinides?

A

Repaglinide (Prandin)

Nateglinide (Starlix)

78
Q

What is Colesevelam (WelChol)?

A

A bile acid binding resin that has some hypoglycemic effect when combined with other antidiabetic agents

79
Q

What is Bromocriptine (Cycloset)?

A

It is a dopamine agonist that inhibits excessive SNS tone which suppresses hepatic glucose production

80
Q

What is Pramlintide (Symlin)?

A

An amylin-like peptide**

81
Q

How is Pramlintide (Symlin) administered?

A

It is injected because it is a PEPTIDE

82
Q

Can we give Pramlintide (Symlin) alone?

A

No, it is only an adjunct to insulin therapy in Type 1 AND Type 2 diabetes!!!!!***!!

83
Q

What is the MOA of Pramlintide (Symlin)?

A

It works with insulin to Lower post-prandial glucose by:

Slowing gastric emptying

Suppressing glucagon

Centrally-mediated appetite suppression

84
Q

What are the only two classes of diabetes drugs that can cause hypoglycemia?

A

Sulfonylureas

Meglitinides

(+ insulin of course)

85
Q

What are the only two classes of drugs that can cause hyperinsulinemia?

A

Sulfonylureas

Meglitinides

86
Q

Some guy rolls into the ER and you can tell right away he has way too much insulin flowing through his system. How can you tell if it’s from taking too much insulin or if he took too much of a sulfonylurea or Meglitinide?

A

C-peptide.

Sulfonylureas and Meglitinides will increase endogenous insulin production

87
Q

How long do short acting insulin take to kick in and how long does it last?

A

Starts in 1 hour

Lasts 4-5 hours

88
Q

How long does intermediate acting insulin take to reach peak effect and how long does it last?

A

Peaks in 4 hours and lasts 15 hours

89
Q

When do long acting insulins reach peak effect?

A

They don’t peak. They have a sustained effect for 24 hours or longer

90
Q

Which type of insulin is best to start type 2 diabetics on since it will fix their fasting glucose?

A

Basal/long acting

91
Q

How long does rapid acting insulin take to kick in and how long do they last?

A

Start in 30 min

Lasts 2-3 hrs

Pharm II Final Annie & Lauren (3 decks)

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