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Pharm exam 3 > Lipid drugs > Flashcards

Lipid drugs Flashcards

1
Q

describe the growth of plaque in arteries

A

cholesterol infiltrates artery wall > plaque forms > plaque grows > plaque grows to block artery or ruptures and blood clots form

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2
Q

what is bad cholesterol

A

LDL= stored in blood stream

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3
Q

what contributes to plaque build up

A

LDL and triglycerides

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4
Q

what is good cholesterol

A

HDL

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5
Q

what does HDL do

A

regulates LDL storage and promotes secretion

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6
Q

what are the 3 mechanical means of clearing plaque buildup

A

balloon angioplasty, stents, high pressure jetting

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7
Q

what are the 5 drugs to treat Dyslipidemia

A 
fibrates
nicotinic acid
bile acid sequestrates
inhibitors of HMG CoA reductase
cholesterol absorption inhibitors
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8
Q

What do fibric acid derivatives do (fibrates)

A

Fibrates= INC peripheral lipolysis and DEC hepatic triglyceride
DEC Trigylceride levels!!

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9
Q

What are fibrates agonists of and what does this lead to

A

Fibrates = agonists of PPAR alpha - interaction leads to lipid metabolism and atherosclerosis

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10
Q

What is the concern of long term fibrate use?

A

concern about an INC in non cardiac mortality in patients on long term fibrate use

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11
Q

name the side effects of antilipemics (fibrates)

A

abdominal discomfort, diarrhea, nausea, blurred vision, INC risk of gallstones, prolonged prothrombin time, INC liver function

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12
Q

What are suitable as vitamin B3

A

niacin and niacinamide

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13
Q

what is the only vitamin B3 suitable for treating dyslipidemia

A

NIACIN!

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14
Q

Does the Vitamin B3 activity of niacin affect its activity in lipid control

A

NO!! must use high high doses

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15
Q

What are the 2 actions of nicotinic acid

A
  1. agonist of GPR 109A and 109B receptors

2. inhibitor of diacylglycerol acetyltranferase

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16
Q

describe the pathway of Nicotinic acid MoA

A

acts on GI inhibiting cAMP > inhibit PKA > inhibit HSL > INC good cholesterol

17
Q

Side effects of Niacin (nicotinic acid)

A

flushing (due to histamine release), itching, GI distress

18
Q

What are cholestyramine and colesevelam

A

bile acid sequestrants

19
Q

how do bile acid sequestrates work

A

keep bile acids from getting absorbed as they pass through intestine thus DEC secretion of bile salts to hepatocytes

20
Q

what stimulates hepotcytes to secrete more bile salts

A

95% of the bile salts reabsorbed into intestinal capillaries via enterohepatic circulation

21
Q

What happens in the liver to cholesterol

A

cholesterol is converted to bile acid which is excreted to the intestine through the action of C7H

22
Q

by preventing bile acid resorption what doe bile acid sequestrates do

A

INC cholesterol metabolism to bile acid

23
Q

What do bile acid sequestrates do to LDL? to HDL? Triglycerides (TG)?

A

Bile Acid Sequestrates
reduced LDL by 5-30%
INC HDL by 3-5%
INC trigylcerides

24
Q

side effects of bile acid sequestrates

A

GI distress and constipation

DEC absorption of other drugs

25
Q

Contraindications of bile acid sequestrates

A

PTS with dysbetalipoproteinemia

PTS with HIGH triglyceride levels (HIGHer than 400 mg/dl)

26
Q

what do inhibitors of HMG CoA reductase (statins) do

A

block HMG CoA thus preventing cholesterol synthesis and lowering levels of LDL

27
Q

What 2 drugs to lower cholesterol have the most side effects

A

FIbrates and Statins

28
Q

what 2 drugs to lower cholesterol have the least side effects

A

Cholesterol absorption inhibitors and bile acid sequestrates

29
Q

What is the current opinion on statins and longevity of life

A

Statins are helpful for people at risk of having a heart attack

30
Q

What do cholesterol absorption inhibitors do?

A

inhibit LDL formation by inhibiting absorption of dietary cholesterol and reabsorption of billiard cholesterol

31
Q

what is NPC1L1? what blocks NPC1L1?

A

NPC1L1: a transport protein moving cholesterol from lumen into enterocyte and back into blood
NPC1L1 is blocked by Ezetimibe

32
Q

Describe the MoA of Ezetimibe

A

Ezetimibe selectively inhibits intestinal cholesterol absorption by DEC intestinal delivery of cholesterol to liver and INC expression of hepatic LDL receptors

33
Q

What do Ezetimibe and its active gluconoride do?

A

both metabolite circulate enterohepatically delivering agent back to site of acton and limiting systemic exposure

34
Q

what does ezetimibe do to LDL

A

lowers LDL by 18-20% and can be used as “add- on” to statins

DOES NOT change TG and HDL

35
Q

What are adverse effects of Ezetimibe (cholesterol absorption inhibitors)?

A

Main: abdominal pain and diarrhea
Minor: headache, dizziness, fatigue, URI, back pain, muscle aches, and pain

Pharm exam 3 (3 decks)

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