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Heart Pharm > Hyperlipidemia > Flashcards

Hyperlipidemia Flashcards

1
Q

Statins
(Lovastatin, Simavastatin, Atorvastatin, Fluvastatin, Rosuvastatin, Pravastatin)

  • Indication/DRUG OF CHOICE
  • MOA
  • Effect on serum lipids
A

Indication: High LDL
Drug of choice: increased LDL and primary and secondary prevention of CHD
MOA:
1. Inhibits HMG-CoA Reductase–>decreased cellular cholesterol
2. Triggers SREBP transcription factor
–> increased LDLR receptors
3. increased LDL receptors leads to increased clearnce of LDLs from the serum
4. LDLs are internalized and their cholesterol can be excreted in the bile

Effect on serum Lipids:

  1. Decreased LDL (20-60%)
  2. decreased TG (10-20%)
  3. increased HDL (5-10%)
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2
Q

What are the Adverse Effects of statins?

A
  1. muscle myalgia/myopathy
  2. Rhabdomyolysis *******
  3. Hepatitis
  4. Small risk to type 2 diabetes
    - contraindicated in liver disease*
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3
Q

Drug interactions with statins?

A
  1. CYP3A4 inhibitors (increased L,S,A)
    e. g. erythromycin, cyclosporin, ketoconazole, HIV prot inhibs, and grapefruit juice
  2. CYP3A4 inducers (decrease L, S, A)
    e. g. phenytoin, phenobarbital, rifampin
  3. CYP2C9 inhibitors ( increase F,R)
    e. g. ketoconazole/metronidazole
  4. Gemfibrozil
    - decrease OAPT/decrease glucuronidation–>increase ALL statins
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4
Q

What statin has no CYP450 metabolism and is hepatically/renally excreted and has fewer muscle adverse side effects and can use with cyclosporin?

A

Pravastatin

-still undergoes glucuronidation(they all do)

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5
Q

What are the bile acid binding resins?

A

Cholestryramine
Colestipol
Colesevelam

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6
Q

Cholestryramine/Colestipol/Colesevelam *Indication

  • MOA
  • Effect on serum lipids
A

Indication:
High LDL
(can see a small increase in serum triglycerides-because bile acids normally serve to suprpress endogenous tryglyceride synthesis)

MOA:
1. Binds bile acids and prevents reabsorption

  1. This leads to an increase in cholesterol 7 alpha hydroxylase(rate limiting enzyme in bile acid synthesis, resulting in increased conversion of cholesterol to bile acids)
  2. decrease cholesterol
  3. Increase in LDLR
  4. Increase LDL clearance
Effects on Serum Lipids:
Decrease LDL (10-25%)
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7
Q

What are the therapeutic uses for resins?

A
  1. reduce risk of CHD events
    - second line agent to statins
  2. combination with statin
  3. patients who cant take statins
    - women who are lactating or preg and children
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8
Q

Which resin doesnt interfere with drug absorption or asbsorption of fat soluble vitamins at high concentrations?

A

colesevelam

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9
Q

What is a contraindication to taking resisn?

A

can increase TG levels in hypertriglyceridemia and type 3 dysbetalipoproteinemia
Conctraindicated TG>400mg/dL

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10
Q

What is the inhibitor of cholesterol absorption?

A

ezetimibe

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11
Q

MOA of ezetimibe?

A
  1. inhibits NPC1L1 involved in the absorption of dietary and biliary cholesterol in small intestine
  2. reduced cholesterol absorption results in the decreased delivery of cholesterol to the liver, thereby reducing VLDL and LDL production and increasing LDLR
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12
Q

What are the therapeutic uses of ezetimibe?

A
  1. reduces LDL-C in patients with primary hypercholesterolemia
    - i.e. not completely dependent upon intact LDLR
  2. combine with statin
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13
Q

What are the PCSK9 inhibitor drugs?

A

Alirocumab

Evolocumab

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14
Q

What are the indications of Alirocumab and Evolcumab?

A

Hetero FH

High LDL not controlled with maximum statins or statin intolerant

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15
Q

What is the mechanism of action for Aliocumab and Evolocumab?

A

Inhibit PCSK9—>blocks normal targeting of LDLR to lysosome –>increases LDL R-expression–>LDL clearance

—->Decreased LDL (>50%) !

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16
Q 
Lomitapide
Indications
MOA
Effects on serum lipids
Adverse effects/contraindications
A

Indication:
Homo FH

MOA

  1. Inhibits MTP(microsomal triglyceride transfer protein-required for assembly of both chylomicrons and VLDLs) in both enterocytes and liver
  2. decrease production of chylomicrons, VLDL and LDL

Effects on serum lipids

  1. Decrease Chylomicrons
  2. decrease VLDL
  3. Decrease LDL

Adverse Effects/Contraindications

  1. Hepatotoxicity
  2. Contraindicated in Pregnancy
17
Q 
Mipomersen
Indications
MOA
Effects on serum lipids
Adverse effects/contraindications
A

Indications
Homo FH

MOA

  1. Antisense oligonucleotide specific for apoB100
  2. Reduces expression of apoB100 resulting in reduced VLDLs and hence lower levels of LDLs.

Effects on serum lipids
Decreased VLDL and LDL

Adverse effects/contraindications
Hepatotoxicity
Contra: Mild/moderat hepatic impairment

18
Q

Niacin

Primary clinical Effect

A

30-80% reduction in tryglycerides *
10-20% reduction in LDLs
10-30% increase in HDLs-MOST EFFECTIVE DRUG AT RAISING HDLs***

High VLDL
High LDL
Low HDL

19
Q

What are the five mechanisms of action of niacin?

A
  1. dereased lipolysis in adipocytes
    - ->decreased FFA–>decreased VLDL
  2. Inhibits DGAT2
    - ->decreased VLDL synthesis
  3. reduces expression of APC111–>increased LPL—>increased VLDL clearnace
  4. increased apoA1 expression–>increased HDL production
  5. decreased LP(a)–>decreased thrombosis
20
Q

What are the adverse side effects of niacin?

A
  1. skin flushing (tx-nsaid)
  2. decreased secretion of uric acid-risk of gout
  3. exacerbates peptic ulcers
21
Q

What are the fibrates drug names?

A

Gemfibrozil and Fenofibrate

22
Q

What are fibrates indicated for?

A

High VLDL

Low HDL

23
Q

What are mechanisms of action for fibrates?

A

ligands for PPAR alpha TF

  1. Decreased ApoC3/Increased LPL expression/Increased Fatty acid oxidation
    - -> decreaded VLDL synthesis
    - –>increaded VLDL clearance
  2. Increased apoA1 expression
    - ->increased HDL production
24
Q

What are fibrates effects on serum lipids?

A 
Decrease TG (40-60%)
Decreased LDL (10-20%)
Increased HDL (10-20%)
25
Q

What are the adverse side effects to fibrates?

A

Increased gallstones
Myopathy and Rhabdomyolysis (more common with gemfibrozil) leading to acute renal failure
-increased risk when given with statin
Contraindicated in severe renal/hepatic disease

26
Q

What are the drug reactions seen with fibrates?

A
  1. strong protein binders
    - increase warfarin–>increased risk of bleeding
    - increase sulfonylureas–>increased hypoglycemia
  2. statin interaction
    - inhibit OAP2/glucuronidation
    - increased statins–>increased rhabdomyolysis esp gemfibrozil

Heart Pharm (14 decks)

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