Lipid lowering drugs, Drugs to treat Diabetes Flashcards Preview

AU 15 - Pharmacology Exam 3 > Lipid lowering drugs, Drugs to treat Diabetes > Flashcards

Flashcards in Lipid lowering drugs, Drugs to treat Diabetes Deck (52):
1

What are the steps in plaque formation and growth?

1) Cholesterol particles infiltrate the wall of the artery at the site of the damaged inner lining of the artery
2) Plaque develops in the artery
3) As more cholesterol and materials are incorporated into the plaque, the plaque grows
4) The plaque may continue to grow blocking blood flow through the artery or
5) The plaque may rupture and blood clots may form, completely blocking blood flow through the artery

2

What are "bad cholesterols"?

LDL - stores cholesterol in the blood stream

3

What are "good cholesterols"?

HDL - regulates LDL storage and promotes excretion

4

What contributes to plaque buildup?

LDLs
Triglycerides
Inflammatory component

5

What are some mechanical procedures to treat plaque buildup in the circulatory system?

Balloon angioplasty to treat blocked coronary artery
Stent placement in carotid artery
High pressure jetting

6

Dyslipidemia

High cholesterol
An imbalance of lipids circulating in the blood stream

7

What are drugs used to treat dyslipidemia?

Derivatives of fibric acid
Nicotinic acid
Bile Acid sequestrants
Inhibitors oh HMG CoA Reductase
Cholesterol absorption inhibitors

8

What do fibric acids do?

Increase peripheral lipolysis
Decrease hepatic triglyceride production

9

What are side effects of fibric acid derivatives?

Abdominal discomfort
Diarrhea
Nausea
Blurred vision
Increased risk of gallstones
Prolonged prothrombin time
Liver studies may show increased function

10

What are the two mechanisms of action for Nicotinic acid?

1) Agonist for GPR 109A and 109B receptors
2) Inhibitor of diacylglycerol acyltransferase

11

What is the result of using Nicotinic acid?

Increase HDL-particles
Decrease Triglyceride

12

What are the side effects of nicotinic acid?

Flushing (due to histamine release)
Pruritis (itching)
GI distress

13

What happens to cholesterol in the liver?

It is converted to bile acid, which is excreted to the intestine through the action of C7H
By preventing bile acid resorption, the sequestrants increase cholesterol metabolism to bile acid

14

What are the major actions of bile acid sequestrants?

Reduce LDL-C 15-30%
Increase HDL-C 3-5%
May increase TG

15

What are the major side effects of Bile acid sequestrants?

GI distress/constipation
Decreased absorption of other drugs

16

Inhibitors of HMG CoA Reuctase

HMG-CoA reductase is an enzyme along the pathway of cholesterol synthesis
By inhibiting it, it prevents the synthesis of cholesterol

17

Statins (HMG-CoA Reductase inhibitor) lowers cholesterol, but do they help people live longer?

The current prevailing opinion is that they are helpful for people at risk of having a heart attack

18

NPC1L1

A transport protein moving cholesterol from the lumen into the enterocyte and ultimately back into the blood
Blocked by Ezetimbie (Cholesterol Absorption inhibitor)

19

What do Cholesterol Absorption inhibitors do?

Inhibit absorption of both dietary and biliary cholesterol
Lower LDL formation - increases expression of hepatic LDL receptors

20

What is the mechanism of Cholesterol Absorption inhibitors?

Inhibit LDL formation by increasing hepatic LDL receptors and taking it up to be secreted

21

What are adverse effects of Cholesterol Absorption inhibitors?

Mild abdominal pain and diarrhea

22

What is a major complication of diabetes that WE care about (hint, hint)

Dental disease

23

Glycogenesis

Process of glycogen synthesis, in which glucose molecules are added to chains of glycogen for storage
(glucose --> glycogen)

24

Glycogenolysis

The reverse process to glycogenesis
The breakdown of glycogen to Glucose-6-Phosphate and glycogen
(glycogen --> glucose)

25

Gluconeogenesis

Metabolic pathway that results in the generation of glucose from non-carbohydrate carbon substrates such as pyruvate
One of the two main mechanisms used to maintain blood-glucose levels
(Carbon substrates --> glucose)

26

What are the principal hormones regulating blood sugar levels?

Glucagon
Insulin

27

What cells secrete glucagon?

alpha cells

28

What cells secrete insulin?

beta cells

29

A1C test

Measures glycation of hemoglobin
It provides a window into the average blood sugar of an individual over a period of months

30

What are the ranges of A1c test scores

Excellent = 4-6
Good = 7-8
Action suggested = 9-14

31

What are the actions of insulin?

Glucose uptake
Glycolysis
Glycogen syntesis
Protein synthesis
Uptake of Ions
Stop gluconeogenesis
Stop glucogenolysis
Stop liposysis
Stop ketogenesis
Stop proteolysis

32

Type 1 diabetes

Not enough insulin, so cells can't absorb glucose

33

Type 2 diabetes

Cells do not respond to insulin, so cells can't absorb glucose

34

What drugs can be used to treat diabetes?

Insulin
Sulfonylureas
Meglitinides
Drugs working on GLP-1 receptors
Biguanides
Thiazolidinediones
a-glucosidase inhibitors

35

Secretagogues

A K+ channel that regulates insulin release from pancreatic B cells by sensing ATP/ADP

36

What happens to secretagogues when ATP/ADP is low (fasting)

The channel opens, the cell hyperpolarizes, L-type Ca channels close, and insulin is not secreted

37

What happens to secretagogues when ATP/ADP is high (after a meal)

Channel is closed, cell depolarizes, L-type Ca channels open, and insulin is secreted

38

What drugs affect the secretagogues process?

Sulfonylureas
Meglitinides
Drugs working on GLP-1 receptors

39

Sulfonylureas

Have a duration of 12-24 hours
Used to generally beat down glucose levels

40

Sulfonylureas mechanism

Sulfonylureas binds to an ATP/ADP regulated K channel complex, reducing the efflux of K ions, leading to the channel to close, depolarizing the membrane, leading to an influx of Ca and secretion of insulin

41

Meglitinides

More rapid onset of action and shorter duration than sulfonylureas
Used before meals
Hypoglycemia is a concern if drug is taken and person doesn't eat

42

Meglitinides mechanism

Very similar to Sulfonylureas
Binds to a ATP/ADP regulated K channel complex, reducing the efflux of K ions, leading to the channel to close, depolarizing the membrane, leading to an influx of Ca and secretion of insulin

43

GLP-1 receptor

Glucagon-like peptide 1 (GLP-1) and Glucose dependent insulinotropic polypeptide (GIP) act at the GLP-1 receptor on B cells and stimulate insulin release

44

Metformin (Biguinide)

A first-line medication used for treatment of type 2 diabetes in conjunction with diet, exercise, and weight loss
Does no stimulate insulin secretion, but is insulin 'sparing'
Usually not accompanied by hypoglycemia

45

What is the mechanism of action of metformin?

Decrease hepatic glucose produciton through a mild inhibition of the mitochondrial respiratory-chain complex
Decreases intestinal absorption of glucose

46

Thiazolidinediones

Decrease insulin resistance
Agonists of the peroxisome proliferator-activated receptor y (PPAR-y)

47

Insulin resistance

Pathological condition in which cells fail to respond to the normal actions of insulin

48

What happens when the body produces insulin under the condition insulin resistance?

The cells in the body are unable to use it efficiently, leading to high blood sugar

49

PPAR-y

Regulates fatty acid storage and glucose metabolism
The genes activated by PPAR-y stimulate lipid uptake and adipogenesis by fat cells

50

What do PPAR-y agonist do?

Diminish insulin resistance

51

a-glucosidase inhibitors

Act by inhibiting the digestion of glucose
Delay digestion and absorption of carbs in the GI tract

52

a-glucosidase

Breaks down starch and disaccharides to glucose