32 - lipid lowering drugs Flashcards

1
Q

steps and formation of plaque growth in vessels

A
vessel damage
cholesterol particles inflitrate site
plaque develops within artery
grows as more shit is incorporated
could continue to grow and occlude artery or
rupture and multiple clots may form
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2
Q

_ _ _ and _ contribute to

plaque build up too.

A

LDL’s
Triglycerides
cholesterol - damaged vessel
inflammation IL4 and IL5

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3
Q

mechanical procedures to treat plaque build up in vessels

A

Balloon angioplasty to treat
blocked coronary artery

Stent placement in carotid
artery

High pressure jetting - best

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4
Q

Pharmacological treatments center around _ and _ componetns of plaque buildup

A

cholesterol (LDL and HDL) and triglycerides

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5
Q

stores cholesterol in the blood stream

A

LDL - stores in BS

HDL - regulates LDL storage and promotes excretion

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6
Q

“Poor Lipid Biochemistry” can contribute other health
problems

_ a cluster of biochemical and
physiological abnormalities associated with type 2 diabetes
and cardiovascular disease

A

Metabolic Syndrome:

insulin resistance
high BP and triglyceride levels
low HDL cholesterol

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7
Q

total cholesterol levels

total non-HDL
cholesterol calculated,
below _ considered
desirable

A

130 non HDL cholesterol is desirable

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8
Q

High levels of free fatty
acids are thought to
contribute to _ and lead to
a slew of health issues

A

insulin resistance

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9
Q

A disorder of lipoprotein metabolism, including lipoprotein
overproduction or deficiency.
may be manifested by elevation of the
total cholesterol, the “bad” low-density lipoprotein (LDL) cholesterol and the
triglyceride concentrations, and a decrease in the “good” high-density lipoprotein
(HDL) cholesterol concentration in the blood

A

Dyslipidemia

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10
Q

Drugs used to treat Dyslipidemia

  1. Derivatives of _ acid
  2. Nicotinic Acid
  3. Bile Acid sequestrants
  4. Inhibitors of HMG CoA Reductase (_)
  5. Cholesterol Absorption inhibitors
A
  1. Derivatives of fibric acid
  2. Nicotinic Acid
  3. Bile Acid sequestrants
  4. Inhibitors of HMG CoA Reductase (statins)
  5. Cholesterol Absorption inhibitors
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11
Q

Drugs used to treat Dyslipidemia

agonist of PPARa receptor

Increase peripheral lipolysis
decrease hepatic triglyceride
production
Major net effect: Reduce levels of triglycerides

A

Fibric Acid derivatives

(PPARs) function as transcription factors
regulating the expression of genes.
PPARs play essential roles in the
regulation of cellular differentiation,
development, and carbohydrate,
lipid and protein metabolism.
α (alpha) is expressed in liver,
kidney, heart, muscle, adipose,
and other tissues.

Activated PPAR alpha stimulates fatty acid
catabolism in the liver by inducing the
expression of genes controlling the betaoxidation

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12
Q

Derivatives of fibric acid

Activated _ stimulates fatty acid
catabolism in the liver by inducing the
expression of genes controlling the betaoxidation

A

PPAR alpha

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13
Q

Derivatives of fibric acid

are primarily used for lowering _ (~50%)

A

triclycerides

side effects - abdominal discomfort, diarrhea, nausea, etc

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14
Q

Drugs used to treat Dyslipidemia

Agonist for GPR 109A (and 109B) receptor
Inhibitor of diacylglycerol acyltransferase
GPR109A activation inhibits lipolysis and atherogenic
activity(formation of fatty plaques)

increase HDL cholesterol

block triacyl glycerol (triglyceride) production

A

Nicotinic acid

*Both niacin and
niacinamide are
suitable as vitamin B3
Only niacin (nicotinic acid) is suitable to treat dyslipidemia. Has
nothing to do with vitamin B3 activity and requires doses that are
much higher

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15
Q

major benefits of niacin (nicotinic acid

increase _
decrease _

A

increase HDL

decrease triglyceride

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16
Q

niacin (nicotinic acid) side effects

flushing vasodilation is due to _ release

also have pruritus (itching)
GI distress

A

due to histamine release

and arachidonic acid - PGs on SM

17
Q

Drugs used to treat Dyslipidemia

blocks reabsorption of bile acids
Liver removes cholesterol by converting it to bile acid

keep bile
acids from getting
absorbed as they pass
through the intestine

bile salts via enterohepatic circulation stimulate hepatocytes to secrete more bile salts (which break down fat)

A

Bile Acid sequestrants

Bile acids = A family of
cholesterol like acids

Does more of this if bile acid is prevented from
recirculating

18
Q

In the liver, cholesterol 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 _

A

cholesterol gets converted to bile acid

19
Q

Drugs used to treat Dyslipidemia

Diminish cholesterol by inhibiting HMG CoA reductase

inhibition of the cholesterol biosynthetic pathway

A

statins

Statins lower cholesterol.

They are helpful for people at risk of having a heart attack.

Men and women over 65 who are at risk for cardiovascular
disease but don’t have any known heart problems might
benefit from cholesterol-lowering drugs, a new study suggests

20
Q

The task force recommends the use of low- to moderate-dose of _ in adults without a history of heart disease and who
don’t have current signs of problems but who have one or
more risk factors, including high cholesterol, diabetes, high
blood pressure or smoking, and a calculated 10 percent risk of
a heart attack in the next 10 years

A

statins

21
Q

Drugs used to treat Dyslipidemia

_ drugs - inhibit LDL formation, NPC1L1: a transport protein moving
cholesterol from lumen into enterocyte
(and ultimately back into the blood)
This transport protein is
blocked

inhibit absorption of dietary cholesterol
inhibt reabsorption of biliary cholesterol
lower LDL cholesterol

A

Cholesterol Absorption inhibitors

selectively inhibs intestinal absorption

NO CHANGE IN HDL

side effects - unique because no bloating or farting

22
Q

reduction of cholesterol absorption results in less _

A

less LDL