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Medicinal 3 > Antihyperlipidemics: > Flashcards

Antihyperlipidemics: Flashcards

1
Q

What is hyperlipidemia

A

a common disorder in developed countries and is a major cause of coronary heart disease

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2
Q

What does hyperlipidemia caused from

A

abnormalitites in
1. lipid metabolism
2. plasma lipid transport
3. a disorder in the synthesis and degradation of plasma lipoproteins

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3
Q

Where does increased triglycerides come froom

A

Food
the body does NOT produce it -> lowered by diet and exercise

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4
Q

Where does cholesterol come from

A

The liver produces it
when it is high -> drugs
Exercise and diet will NOT lower it

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5
Q

What are lifestyle habits or treatable medical conditions that could cause hyperlipidemia

A

Obesity
Smoking
not exercising
obstructive jaundice
underactive thyroid gland

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6
Q

What are lipids?

A

Heterogenous mixtures of fatty acids and alcohol that are present in the body

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7
Q

What are the major lipids in the blood stream

A

Cholesterol and its esters
Triglycerides
Phospholipids

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8
Q

What are cholesterol derivatives

A
  1. Cortisone
  2. Sex hormones (estrogen + testosterone)
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9
Q

Talk about the chemical structure of cholesterol

A
  1. 4 membered ring (A,B,C,D) ->17 carbons
  2. Not aromatic (except estrogen)
  3. Not planar
    Total 27 carbons
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10
Q

Which ring in cholesterol determines the activity (antiinflammatory, diuretic, hormonal activity)?

A

Ring A

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11
Q

Why do vegetarians have high cholesterol?

A

The body senses the low levels -> liver produces more

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12
Q

What are the functions of cholesterol in the body

A
  1. important for new cells and reparing older cells after injury
  2. Cholesterol is used by adrenal grands -> forming hormones
    (estrogen + testosterone)
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13
Q

What are the normal functions of triglycerides and phospholipids in the body

A
  1. Supplying energy
  2. meeting immediate energy in the muscles
  3. stored in fat for future energy needs
  4. Phospolipids -> cell membrans, generating secondary messengers, storing fatty acids for the use in generation of prostaglandin
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14
Q

What do lipoprotein contain

A

Contains both proteins and lipids bound to another protein (apolipoprotein)

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15
Q

What is the function of lipoproteins

A
  1. Allows fats to move through the water inside and outside the cells
  2. provides structural support and stability, binds to receptor
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16
Q

What are the classification of lipoproteins

A
  1. Chylomicrons
  2. VLDL
  3. IDL
  4. LDL
  5. HDL
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17
Q

What does the biosynthesis of cholestrol start with

A
  1. Acetyl CoA
    then
  2. 3-hydroxy-3-methyl-hlutaryl-CoA
    then
    (using HMG CoA)
  3. Mevalonate
    then
  4. CHOLESTEROL
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18
Q

What are the major drug classes to treat hyperlipidemia

A
  1. STATINS
    HMG CoA reductase
  2. FIBRATES
  3. BILE ACID SEQUESTRANTS
  4. EZETIMIBE
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19
Q

Statins are mostly ______ based

A

Lactone based

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20
Q

What is the rational of statins

A

Competitive binding

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21
Q

What is the SAR of statins

A
  1. 6 membered ring containing C=O (lactone)
    WHICH COULD BE LINEAR
  2. Ethylene bridge (2c)
  3. Bi-Cyclic system -> i can control the hydrophobicity of it
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22
Q

What is the MOA of atorvastatin

A
  1. HMG-CoA reductase
  2. Lowering cholesterol level LDL
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23
Q

SE of atorvastatin

A
  1. Liver failure
  2. Myopathy because of terpinoids
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24
Q

Is Lovastatin Natural or Synthetic

A

Natural

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25
Q

Are fibrates old or new?

A

Older antihyperlipidemics found in 1981

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26
Q

Are fibrates the first choice in hyperlipidemia

A

No, second choice

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27
Q

MOA of fibrates

A
  1. Stimulate B-oxidation of fatty acids in the mitochondia -> decreasing plasma levels of fatty acids and triacylglycerol
  2. Activation of lipoprtein lipase
  3. PPAR-a (trascription factor thats why it takes time to see results)
  4. Increases HDL cholesterol

NOT EFFECTIVE IN LOWERING LDL + CHOLESTEROL

28
Q

How does reducing the levels of fatty acids in fibrates lower level of cholesterol

A

Since the precursor of cholesterol is Acetyl CoA which comes from fatty acid metabolism

29
Q

SAR of fibrates

A
  1. Free carboxylic A end
  2. Branched carbon ( like isobutyl)
  3. Ether part (C-O-C)
30
Q

Fibrates are analougs of

A

Isobutyric acid

31
Q

Mention 2 fibrates drugs

A

Fenofibrates
Gemfibrazil

33
Q

Is fenofibrates prodrugs

A

Yes
contains ester next to the isobutyl branch

33
Q

Parasubstituion with Cl or Cl containing ispropyl ring does what to the half life

A

Increase

like in fenofibrate

33
Q

Bile acid sequestrants are also called

A

Bile acid resins

33
Q

In gemfibrozil we have _____ spacer, what does it affect the activity

A

n-propyl spapcer

inc length of spacer -> inc activity

34
Q

mention drugs under the class of bile acid sequestrants

A

Cholestryamine
Colestipol hydrochrolide
Colesevelam

35
Q

What is the MOA of bile acid sequestrants

A

Prevents the reabsorption of bile acids in the intestines -> increase removal by feces

the body will then use the cholesterol in serum and convert it to bile acids

36
Q

Are bile acids small or large in size

A

Large molecules in form of micelles

37
Q

To prevent the reabsorption of bile acids in the intestines we need a polymer with a _____ charge

A

Positive charge

so it reacts with - charge of carboxylic aicd of bile acids (ionic bond) and prevents its reab.

38
Q

Any bile acid sequestrant will contain

A
  1. POSTIVE charge
  2. Polymer
39
Q

What is the downside of bile acid sequestrants

A

Reduce the absorption of fat soluble vitamins from blood

40
Q

SE of bile acid sequestrants

A
  1. Flatulance
  2. GI distrubances
  3. Impaired fat solbule vitamin absorption
41
Q

Ezetimibe is a _____ drug

A

Orphan
no SAR

42
Q

MOA of ezetimibe

A

Inhibits cholesterol absorption from food in the intestines

43
Q

Is ezetimibe effective

A

Not really,
it will only inhibit 10% of cholesterol absorption from intestines

44
Q

MOA of Orlistat

A

acts in the gastrointestinal (GI) tract via covalent binding to the serine residues located on the active site of both gastric and pancreatic lipase.

45
Q

Good side of Orlistat

A
  1. Weight loss
  2. Anticancer effects (pancreatic cancer)
45
Q

SE of Orlistat

A
  1. lowering abs. of fat soluble drugs
  2. liver damage
45
Q

Is orlistat an orphan drug

45
Q

Mention an LDL oxidation inhibitor

47
Q

What does probucol contain in its chemical structure

A

2 tertiary butylphenol groups LINKED by a dithiopropylidene bridge

high lipohilic character
Strong antioxidant

48
Q

Sitosterol is a ______ sterol

49
Q

What is the difference between sitosterol and cholesterol (structurally)

A

the substituted ethyl group on C24 (on the side chain)

50
Q

MOA of sitosterol

A

not really understood but

inhibition the absorption of dietary cholesterol from GI

51
Q

How well are sitosterol absorbed

A

Poorly absorbed

52
Q

Uses of sitosterol

A
  1. Anti cholesteremic agent
  2. treatment of prostatic oedema
52
Q

SE of sitosterol

A

Diarrhea
Constipation
Gi disturbances

53
Q

Where does atorvastatin come from

A

Red mushroom
that is why asians are all fit

54
Q

Fibrates treat hpertriglyceremia or hypercholestermia

55
Q

Where do fibtrates bind

56
Q

Do fibrates work fastly, or not and are they potent

A

Slow
Very potent

57
Q

Lines of treatment with high TG patients

A
  1. diet
  2. exercise
  3. fibtrates
    lastyl 4. statins
58
Q

CI of orlistat

A
  1. chronic malabsorption syndrome,
  2. cholestasis,
  3. during pregnancy or breastfeeding and
    4.in patients with known hypersensitivity to orlistat

Medicinal 3 (6 decks)

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