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Medicinal Chemistry > Lipid Lowering > Flashcards

Lipid Lowering Flashcards

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1
Q

Blocks conversions of cholestend to bile acids

A

Bile and resins

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2
Q

Lowers plasma LDL by indirectly increasing rate of LDL clearance from plasma

A

Bile acid resin

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3
Q

What enzyme does bile acid block and with what effect

A

Inhibits 7 alpha hydroxylase

Blocks conversion of cholesterol to bile acids

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4
Q

What is the other mechanism of action of bile acids in the GI tract

A

Bind major bile acids and increase their fecal excretion

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5
Q

What is the effect of bile acids MOA in the GI

A

Net decrease of bile acids returned to the liver

Removing the negative inhibition of 7 alpha hydroxylase to make more bile acids from cholesterol

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6
Q

What is the effect of hepatic cholesterol reduction due to bile acid production

A

Increase in LDL receptor expression

Increase in uptake of plasma LDL

HMG-COA reductase induction

Increased cholesterol biosynthesis

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7
Q

What is the crosslinking agent of bile acid resins

A

Positively charge groups with amines acting as a binding site for bill acids

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8
Q

What are ADR of bile acids

A

Constipation is common

Increased frequency of loose stool

Hypoprothrombonemia (impaired clotting)

Bleeding events since bile acids bind Vit K

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9
Q

What are bile acids drug interaction

A

Bind acidic compounds and can decrease oral absorption

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10
Q

What medication is of major concern with bile acids therapy and vit K

A

Warfarin. Vitamin K is important concern can induce supratherapeutic INR

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11
Q

How is drug interaction avoided for patients on bile acid resins

A

Take 1 hour before or 4 hours after bile acids.

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12
Q

What is the mechanism of action of statins and why

A

Block HMG- COA reductase because it is the rate limiting step in cholesterol biosynthesis

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13
Q

Blocking of HMG-COA reductase by statins lead to what effect

A

Decreased cholesterol, increasing expression of HMG-COA reductase and LDL receptors

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14
Q

What are other mechanism of action of statins

A

Inhibit cholesterol synthesis

Enhance LDL uptake

Recheck VLDL precursors

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15
Q

What is the primary mechanism of lowering LDL levels with statins

A

Enhanced LDL receptor expression

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16
Q

What are the natural or semi-synthetic statins

A

Lovastatin (mushroom)

Simvastatin

Pravastatin (bacteria)

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17
Q

Which two natural or semi-synthetic are inactive produng form and why

A

Lovastatin and Simvastatin due to Lactone ring

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18
Q

Metabolized by CYP3A4

A

Simvastatin and lovastatin

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19
Q

Not metabolized by 3A4

A

Pravastatin

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20
Q

What are the synthetic statins

A

Fluvastatin - Lescol

Atorvastatin - Lipitor

Pitavastatin - Livalo

Rosuvastatin- Crestor

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21
Q

2C9 (70%) and 3A4 (20%)

A

Fluvastatin

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22
Q

Mostly 3A4

A

Atorvastastin

23
Q

2C9 and lactonization

A

Pitavastatin

24
Q

Partly 2C9 (10%)

A

Rosuvastatin

25
Q

What are the toxicity of statins

A

GI

Rhabdomylosis

Avoid in pregnancy and lactation due to muscle effect

Mild increase in creatnine phosphokinase

Increased myopathy

26
Q

What drug class increase myopathy when given with statins

A

3A4 inhibitors

27
Q

3A4 inhibitors

A

Cyclosporine

Azole of antifungal

macrolides: erythromycin and clarithromycin

HIV protease inhibitors

Nefazodone

Grapefruit juice

Verapamil

28
Q

How does statin induce myoporthy

A

Blocking mevalonate production, decreases ubiquinones (coenzyme Q) required for electron transfer through mitochondrial membrane

29
Q

What is PCSK9

A

Protein that bind to LDL receptors promoting its degradation and increases plasma levels of circulating LDL

30
Q

What are medication is used to lower lipid in this pathway

A

PCSK9 inhibitor

31
Q

What medication are classified under PCSK9 intribitors

A

Evolocumab, Repatha

Alirocumab, Praluent

32
Q

What type of drugs are PCSK9

A

Monoclonal antibodies that binds to circulating PCSK9

33
Q

What is the effect of PCSK9 binding

A

Increase in LDL receptors and LDL-Cholesterol clearance in plasma

34
Q

How is PCSK9-Inhibitors administered

A

2-4 weeks injections

35
Q

What patient group is placed on PCSK-9 inhibitors

A

LDL:500-600 mg/dL

Patient with hypertipidemia or hypercholestrolemia

36
Q

Which medication is a cholesterol transport inhibitor

A

Ezetimibe (Zetia)

37
Q

What is the drug class of ezetimibe

A

Azetidinones

38
Q

What is the effect of ezetimibe

A

Inhibits cholesterol absorption

Decreasing cholesterol and increasing its brosynthests

Causing overall lowering of LDL

39
Q

True or false: ezetimibe interfers with absorption of other compounds

A

False

40
Q

Where is ezetimbe metabolized

A

Intestinal wall and liver

41
Q

What is the major active metabolite of ezetimibe

A

Phenolic glucuronide

42
Q

How is the glucuronide metabolite metabolized

A

Excreted in bile and undergoes enterohepatic recirculation

43
Q

When is ezetimbe used

A

When patient has failed all therapy

Can be used as mono therapy or in combo with statins

44
Q

Toxicity of ezetimbe

A

Abdominal pain

Diarrhea

Cramping

Fatigue

Back pain

When used with statin incidence of myopathy is the same with statin monotherapy

45
Q

Fibrates Effects

A

Decrease plasma triglycerides

Significantly decrease in VLDL levels

Increase HDL levels

46
Q

Mechanism of action fibrates

A

Binds to PPAR a

Causes effects on lipoprotein metabolism

Activation of PPARs and altered gene expression

47
Q

Fibrates binding toPPARa causes

A

Fatty and oxidation, lowering VLDL

48
Q

Fibrate stimulation of lipoprotein lipase causes

A

Removal of TG from plasma VLDL

49
Q

What to all fibrates do

A

Increase turnover and removal of cholesterol from liver

50
Q

True or false: Fenofibrate and chlorofibrate are prodrugs

A

True

51
Q

Metabolism of Fibrates

A

undergo hydrolysis to produce acid form

Active metabolite can be further oxidized or conjugated until products are inactive

52
Q

Active fibrates

A

Gemfibrozil

Ciprofibrate

Bezafibrate

53
Q

How are active fibrates deactivated

A

Oxidation and conjugation

54
Q

Fibrate toxicity

A

Chlorofibrate has many side effects
§ Higher morbidity and mortality § Malignancy, gallbladder disease, pancreatitis

§ Like HMGRIs, they can cause myopathy,
myositis, rhabdomyolysis

§ Increased risk of gallstones due to increased excretion of cholesterol in bile

§ Increases hypoprothrombinemic effect when taken with anticoagulants (low prothrombin)

Medicinal Chemistry (2 decks)

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