Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharm: 412 > Lipoprotein Metabolism: Part 2, Dyslipidemia > Flashcards

Lipoprotein Metabolism: Part 2, Dyslipidemia Flashcards

1
Q

What is dyslipidemia?

A

A disorder of lipoprotein metabolism, including lipoprotein overproduction of deficiency

**increased level of “bad” LDL cholesterol and also a decrease in the “good” HDL

Major risk factor for cardiovascular disease and 1 in 5 deaths is due to it

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What is coronary heart disease?

A

Disease of the blood vessels supplying the heart muscle

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What is cerebrovascular disease?

A

Disease of the blood vessels supplying the brain

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What is peripheral arterial disease?

A

Disease of blood vessels supplying the arms and legs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What is rheumatic heart disease?

A

Dmg to the heart muscle and heart valves from rheumatic fever, caused by streptococcal bacteria

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What is congenital heart disease?

A

Malformations of heart structure existing at birth

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What is deep vein thrombosis and pulmonary embolism?

A

Blood clots in the leg veins, which can dislodge and move to the heart and lungs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What are the non-modifiable risk factors for cardiovascular disease?

A

age
male
family history of cardiac problems

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What are antihyperlipidemic agents?

A

Drugs or natural products that can be used to reduce cholesterol, triglycerides or both.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What are the antihyperlipidemics?

A 
HMG CoA reductase inhibitors (statins)
PCSK9 Inhibitors 
Cholesterol absorption inhibitors 
Fibric acid derivatives (fibrates)
Omega-3 fatty acids
Bile acid sequestrants
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What is the mech of action of HMG CoA reducatse inhibitors (statins)?

A

Competive inhibitor of HMG CoA reductase, which catalyzes the rate-limiting step of cholesterol synthesis

**liver is the primary target

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What is the number 1 choice to reduce LDL-c?

A

HMG CoA reductase inhibitor (statins)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What is lipophilicity and the side effects?

A

Lipophilic statins penetrate muscle cell at higher degree than hydrophilic statins

**this leads to a pronounced effect in disturbing the normal activity of muscle by inhibiting CoQ10

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What are the adverse effects of statins?

A

Most common is myopathy

Myalgia and cramp are more common than estimated from clinical trials

Can cause liver toxicity due to statin accumulation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What is the mechanism of statin myopathy?

A

They inhibit HMG-CoA reductase which leads to less production of mevalonate pathway metabolites, including CoQ10

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Why do you have to worry about taking grapefruit juice with a statin?

A

Some statins are metabolized in the intestine by an enzyme called CYP3A

Grapefruit juice contains compounds called furanocoumarins that inhibit CPY3A, this results in more drug being absorbed, making it more powerful and can result in severe myopathy and liver toxicity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Is rosuvastatin inhibited by grapefruit juice?

A

NO

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What happens if a person takes a statin and a triglyceride reducing drug like gemfibrozil?

A

They could be at a greater risk of statin side effects

19
Q

How do you deal with the side effects of taking a statin?

A
  1. Take a break from statin therapy (10-14 days off the med can help to determine whether aches and pains are due to statins instead of soemthing else
  2. switch to another statin
  3. take it easy when exercising
  4. reduce the dose of statin or alternate daily dosing
  5. add ezetimibe along with statin
  6. add bile acid sequestrants
20
Q

What is the first AHA/ACC cholesterol treatment guideline?

A

All pts (> 21 years of age) with any form of CVD or LVL-C>190 mg/dl

treat with high dose statins
atorvastatin 40-80 mg or rosuvastatin 20-40 mg with the aim to reduce LDL-C by >50%

21
Q

What is the second AHA/ACC cholesterol treatment guideline?

A

all pts with diabetes (age 40-75 years) with LDL-C 70-189 mg/dl, even without evidence of CVD should receive statin therapy

Treatment: Moderate dose statins, Atorvastatin 10-20 mg, rosuvastatin 5-10 mg to reduce LDL by 30-50%

***HIGH dose of statin is recommended for the same group with high CVD risk

22
Q

What is the third AHA/ACC cholesterol treatment guideline?

A

As previsouly, a specific target of LDL-C goal (<70 or <100) is not recommended

**Also the fourth is pts need to receive intensive lifestyle management

23
Q

Why is the LDL-C goal os low for diabetics?

A

Its because they tend to produce more small LDL particles.

24
Q

What is the example of cholesterol absorption inhibitors?

A

Ezetimie (zetia)

25
Q

What is the mech of action for cholesterol absorption inhibitors?

A

Blocks absorption of cholesterol in the intestine and liver

This involves NPC1L1, which is the target of ezetimibe which results in lower LDL with little effect on HDL and triglycerides

**usually added with statin when LDL goal is not achieved

26
Q

What is the most preferred drug combo with a statin?

A

Its ezetimibe if the LDL-C goal is not met after max dose statin

27
Q

What is Vytorin?

A

its a combo of simvastatin and ezetimibe

Has been shown to reduce LDL-c over just taking the single statin drug

28
Q

What is a PCSK9 inhibitor?

A

Its a secretory protease in the liver that binds to LDLR and leads to degradation and as a result more LDL particle will be cleared from the circulation

Target and inactivate PCSK9

**dont cause issue with CoQ10

29
Q

What are the PCSK9 inhibitors?

A

Evolocumab

Alirocumab

30
Q

When are PCSK9 inhibitors useless?

A

For people with genetically defective LDL receptors or Apo 100

90% of Familial hypercholesterolemia (FH) patients have mutated LFLR or Apo B100

31
Q

What is the treatment for high triglyceride levels?

A

There is NO specific suggestion

32
Q

What is hypertryglyceridima?

A

It occurs when the level of triglyceride reaches > 150

150-199 = borderline high
200-499 = high
>500 is very high

33
Q

Why isnt elevated triglyceride levels no the target of therapy unless when >500

A

The recommendation is to reduce the levels to <500 with a goal of preventing pancreatitis with drugs

34
Q

What are the three choices of drugs for hypertryglyceridima?

A
  1. Fibrates - if not tolerated well then go to 2
  2. High dose of omega-3 fatty acids (2-4g daily) good choice for people on high statin
  3. Nicotinic acid - only used if fibrate is not tolerated and omega-3 is not helping reach TG goal
35
Q

What are the Fibric acid derivatives – Fibrates (number one choice)

A
  1. Fenofibrate (tricor)
  2. Fenofibric acid derivative (trilipix)
  3. Gemfibrozil (lopid) cheap but not the best choice
36
Q

What is the mech of action for fibrates?

A

Activating ligand for PPAR-a

This is a transcription factor and the major promoter of lipid metabolism in the liver once activated

This leads to a reduced secretion of VLDL particles, together with the enhanced catabolsim of triglyceride-rich particles, this leads to the hypolipidemic effect of fibrates

Most effective in reducing triglycerides (35-50%_
also increases HDL and decreases LDL

37
Q

What is the treatment for high TG?

A

with moderate high TG pts should be evaluated for secondary causes of hyperlipidema (drinking, diabetes, smoking)

Best treatments are lifestyle, food, controlling diabetes - high fiber

with severe or very severe hyperTG a fibrate is used as a first line agent
**this is because patients are at high risk for developing acute pancreatitis

38
Q

What drugs are omega-3 fatty acids?

A

Lovaza is prescription medication that includes 465 mg of EPA and 375 mg of DHA (essential fatty acids)

39
Q

What is the mech of action for lovaza?

A

It reduces hepatic production of TG and increases TG metabolism

Competitive inhibitor of the enzymes responsible for TG synthesis. EPA and DHA increase lipoprotein lipase (LpL) activity, leading to increased TG clearance
***20-50% decrease in TG

40
Q

What drug is nicotinic acid and what is it mech of action?

A

drug: Niacin (niaspan)

Mech of action: Functions in the body after conversion to NAD in the NAD coenzyme system

Most effective in raising HDL lvl (15-35%)
decreases LDL and triglycerides

Side effects: Flushing (skin becomes red)

41
Q

Why do elevated triglycerides cause acute pancreatitis?

A

It leads to increased concentrations of chylomicrons in the blood, chylomicrons are usually formed 1-3 hours post-prandially and cleared within 8 hours

When triglyceride levels exceed 1000 mg/dL, the chylomicrons are almost always present

***this chylomicrons are very large and occlude the pancreatic capillaries leading to ischemia and local inflammation

42
Q

What are the examples of bile acid sequestrants?

A

Cholestyramine (questran)

Colestipol (colestid)

Colesevelam (welchol)

**this also block sugar absorption, used for diabetes

43
Q

What is the mechanism of action of bile acid sequestrants?

A

Binds to bile acids in the intestine and prevents their reabsorption. this causes an increased conversion of cholesterol to bile acids and increase in LDL uptake

**this lowers LDL with little effect on HDL or TG

Side effects: unpleasant GI side effects (bloating, constipation, abdominal pain and nausea)

Pharm: 412 (4 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions