PHARM Chapter 30 - Endocrine Pancreas and Glucose Homeostasis Flashcards

(53 cards)

1
Q

ME of
Acarbose
Miglitol
Voglibose

A

Alpha-Glucosidase Inhibitors - Carbohydrate analogues that bind avidly to intestinal brush border alpha-glucosidase enzymes - slowing breakdown and absorption of dietary carbohydrates (starch, dextrin, disaccharides)

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2
Q

Uses of
Acarbose
Miglitol
Voglibose

A

Type 2 diabetes mellitus

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3
Q

Continued use of alpha-glucosidase inhibitor associated with

A

diminishement of GI distress

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4
Q

Alpha-glucosidase inhibitors most useful for patients w

A

postrpandial hyperglycemia

new-onset patients w/ mild glycemia

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5
Q

Alpha-glucosidase ihibitors contraindicated in

A

Inflammatory bowel disease - delivery of undigested carbohydrates to distal bowel provides nutrients for colonic bacteria

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6
Q

ME of exogenous insulin

A

Classic anabolic hormone, promotes carbohydrate metabolism and facilitates glucose, amino acid, and triglyceride uptake and storage in liver, cardiac, and skeletal muscle, and adipose tissue

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7
Q

4 Prandial bolus exogenous insulins

A

Regular Insulin
Insulin lispro
Insulin aspart
Insulin glulisine

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8
Q

3 Basal “long-acting” exogenous insulins

A

NPH insulin
Insulin glargine
Insulin detemir

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9
Q

Uses of exogenous insulin

A

Diabetes mellitus

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10
Q

How are exogenous insulins delivered

A

parenternally, subcutanous is most commpon

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11
Q

Intermediate acting insulin that contains protamine which prolongs the time required for absorbtion

A

NPH insulin

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12
Q

Prandial bolus insulins

A

act rapidly, used to mimic B-cell release of insulin in response to nutreitn load

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13
Q

How is regular insulin stabilized for use and how long is it’s time of onset?

A

addition of zinc ions

30 minutes

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14
Q

NPH Insulin is formed how?

A

regular insulin suspended with zinc and protamine (arginine rich protien isolated from fish sperm) - peak activity occurs between 4-10 hours after administration, associated w/ increased hypoglycemia

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15
Q

Major SE of insulin therapy

A

in absence of carbs can result in hypoglycemia

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16
Q

What are the mainstay treatment for type 2 diabetics

A

sulfonylureas

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17
Q

4 first-generation sulfonylureas

A

acetohexamide
chlorpropamide
tolazamide
tolbutamide

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18
Q

5 second-generation sulfonylureas

A
glimepiride
glipizide
glibenclamide (glyburide)
glicclazide
gliquidone
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19
Q

ME of Sulfonylureas

A

inhibit B-cell K/ATP channel at SUR1 subunit - stimulates insulin release form pancreatic B cells and increase circulating insulin to lvels sufficient to overcome insulin resistance

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20
Q

Major adverse effect of SUlfonylureas

A

hypoglycemia from oversecretion of insulin

can cause weight gain secodnary to increased insulin activity in adipose tissue (better for nonobese)

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21
Q

Differences between first and second generation sulfonylureas in dosing

A

first generation bind w/ lower affinity to SUR1 so they must be administered at higher doses

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22
Q

ME of meglitinides

A

Inhibit B-cell K/ATP channel at SUR1 subunit - stimulate insulin release from pancreatic B-cells and increase circulating insulin to levels sufficient to overcome insulin resistance

23
Q

2 meglitidines

A

Nateglinide

Repaglinide

24
Q

Sulfonylureas may displace endogenous ___ which binds to SUR1 to activate the channel

25
How are sulfonylureas delivered
orally
26
ME of metformin
activates AMP-dependent protein kinase to block synthesis of fatty acids and to inhibit hepatic gluconeogenesis and glycogenolysis - increases insulin receptor activity and metabolic responsiveness in liver and skeletal muscle
27
Uses of Metformin
type 2 diabetes mellitus | polycystic ovarian syndrome
28
SE of metformin
lactic acidosis, GI distress
29
Biguanides (metformin) have what additional benefit?
lowering of serum lipids, decrease in weight
30
Why do Biguanides (metformin) cause lactic acidosis
decrease flux of metabolic acids through gluconeogenic pathways
31
ME of pramlintide
Co-released w/ insulin from B-cell acts on receptors in CNS to slow gastric emptying - reduces postrpandial glucagon and glucose release - promotes satiety (amylin analogue)
32
Uses of pramlintide
Type 1 and Type 2 diabetes
33
Why can both type 1 and 2 diabetics benefit from pramlintide
type 1 lack endogenous amylin | type 2 deficient in amylin
34
Added bonus of pramlintide
modest weight loss
35
SE of pramlintide
nausea
36
ME of GLP-1 analogues Exenatide Liraglutide
Act on GLP1 receptor to enhance glucose-dependent insulin secretion, inhibits glucagon secretion, delays gastric emptying and decreases appetite
37
ME of DDP-4 inhibitors Sitagliptin Saxagliptin
Prolongs GLP-1 activity to enhance glucose-dependent insulin secretion, inhbits glucagon secretion, delays gastric emptying and decreases appetite
38
Uses of Exenatide liraglutidde sitagliptin saxagliptin
Type 2 diabetes mellitus
39
SE of exenatide liraglutide sitagliptin saxagliptin
hypoglycemia
40
most common sideeffect of exenatide and liraglutide
nausea - acute pancreatitis is possible
41
2 Thiazolidinediones
Pioglitazone | Rosiglitazone
42
ME of pioglitazone and rosiglitazone
bind and stimulate the nuclear hormone receptor peroxisome proliferator-activated receptor-gamma (PPARy), increases insulin sensitivty in adipose tissue, liver, muscle
43
Uses of pioglitazone, rosiglitazone
type 2 diabetes mellitus
44
Why do TZDs not induce hypogycemia
do not increase insulin levels
45
What main role do TZDs play in treatment
sensitizers - enhance action of insulin at target tissues
46
SE of rosiglitazone
MI, heart failure, weight gain, edema, bone fractures
47
ME of diazoxide
Binds to SUR1 subunit of K/ATP channels in pancreatic B-cells and stabilizes ATP-bound (open) state of the channel so that B-cells remain hyperpolarized - decreases insulin secretion by cells
48
Uses of diazoxide
Hypoglycemia due to hyperinsulinism | malignant hypertension
49
By what mechanism is diazoxide used off label to treat elevated BP in hypertensive emergencies
hyperpolarizes SUR2 channels in cardiac and smooth muscle cells
50
Why is oral combination therapy beneficial
drugs have different MEs so lower doses can be used to have glycemic control
51
octreotide is a ___ analogue
somatostatin - blocks hormone release
52
What is used to treat severe hypoglycemia
glucagon via subcutaneous injection
53
What other purposes is glucagon used for
intestinal relaxant before radiographic or MRI