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Antihyperlipidemics: Flashcards

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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
Are fibrates old or new?
Older antihyperlipidemics found in 1981
26
Are fibrates the first choice in hyperlipidemia
No, second choice
27
MOA of fibrates
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
How does reducing the levels of fatty acids in fibrates lower level of cholesterol
Since the precursor of cholesterol is Acetyl CoA which comes from fatty acid metabolism
29
SAR of fibrates
1. Free carboxylic A end 2. Branched carbon ( like isobutyl) 3. Ether part (C-O-C)
30
Fibrates are analougs of
Isobutyric acid
31
Mention 2 fibrates drugs
Fenofibrates Gemfibrazil
32
33
Is fenofibrates prodrugs
Yes contains ester next to the isobutyl branch
33
Parasubstituion with Cl or Cl containing ispropyl ring does what to the half life
Increase like in fenofibrate
33
Bile acid sequestrants are also called
Bile acid resins
33
In gemfibrozil we have _____ spacer, what does it affect the activity
n-propyl spapcer inc length of spacer -> inc activity
34
mention drugs under the class of bile acid sequestrants
Cholestryamine Colestipol hydrochrolide Colesevelam
35
What is the MOA of bile acid sequestrants
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
Are bile acids small or large in size
Large molecules in form of micelles
37
To prevent the reabsorption of bile acids in the intestines we need a polymer with a _____ charge
Positive charge so it reacts with - charge of carboxylic aicd of bile acids (ionic bond) and prevents its reab.
38
Any bile acid sequestrant will contain
1. POSTIVE charge 2. Polymer
39
What is the downside of bile acid sequestrants
Reduce the absorption of fat soluble vitamins from blood
40
SE of bile acid sequestrants
1. Flatulance 2. GI distrubances 3. Impaired fat solbule vitamin absorption
41
Ezetimibe is a _____ drug
Orphan no SAR
42
MOA of ezetimibe
Inhibits cholesterol absorption from food in the intestines
43
Is ezetimibe effective
Not really, it will only inhibit 10% of cholesterol absorption from intestines
44
MOA of Orlistat
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
Good side of Orlistat
1. Weight loss 2. Anticancer effects (pancreatic cancer)
45
SE of Orlistat
1. lowering abs. of fat soluble drugs 2. liver damage
45
Is orlistat an orphan drug
Yes
45
Mention an LDL oxidation inhibitor
Probucol
46
47
What does probucol contain in its chemical structure
2 tertiary butylphenol groups LINKED by a dithiopropylidene bridge high lipohilic character Strong antioxidant
48
Sitosterol is a ______ sterol
Plant
49
What is the difference between sitosterol and cholesterol (structurally)
the substituted ethyl group on C24 (on the side chain)
50
MOA of sitosterol
not really understood but inhibition the absorption of dietary cholesterol from GI
51
How well are sitosterol absorbed
Poorly absorbed
52
Uses of sitosterol
1. Anti cholesteremic agent 2. treatment of prostatic oedema
52
SE of sitosterol
Diarrhea Constipation Gi disturbances
53
Where does atorvastatin come from
Red mushroom that is why asians are all fit
54
Fibrates treat hpertriglyceremia or hypercholestermia
Hyper TG
55
Where do fibtrates bind
PPAR-a
56
Do fibrates work fastly, or not and are they potent
Slow Very potent
57
Lines of treatment with high TG patients
1. diet 2. exercise 3. fibtrates lastyl 4. statins
58
CI of orlistat
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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