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Pharmacology > Hyperlipidemias > Flashcards

Hyperlipidemias Flashcards

1
Q

Name the 6 groups used in the treatment of hyperlipidemias

A
  1. Statins
  2. Fibrates
  3. Resins/ Bile Acid Sequestrians
  4. Cholesterol absorption inhibitors/ Ezetimibe
  5. Niacin
  6. PCSK9 Inhibitors
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2
Q

Statins Examples

A

ATORVASTATIN FLUVASTATIN ROSUVASTATIN SIMVASTATIN

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3
Q

Stains MOA

A

Blocks enzyme HMG-COA reductase
Decreases intracellular total cholesterol because mevelonate needs this to become cholesterol. Decreases cholesterol makes the liver increase LDL receptors to increase cholesterol therefore bringing in LDL from blood.
(HMG-COA won’t be converted to Mavulonic acid (precursor of cholesterol) → Upregulates LDL-r

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4
Q

Statins S/Es

A 
Liver Toxicity
Increased liver enzymes/ aminotransferases
Headache
Nausea
Skin Rashes
Hepatotoxicity
GI disturbances
Myopathy 
Rhabdo ( Rhabdo occurs when damaged muscle tissue releases its proteins and electrolytes into the blood.)
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5
Q

Contraindications of Statins

A

Unexplained elevated levels of aminotransferase

Pregnancy/ Teens/ Kids

Active hepatic disease

History of liver disease

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6
Q

Niacin MOA

A

Strongly inhibits lipolysis in adipose tissue, thereby reducing production of free fatty acids

Reduced liver triglyceride levels decrease hepatic VLDL production, which in turn
reduces LDL-C plasma concentrations

Decreases catabolism of apoA-1

Reduces VLDL secretion from liver

Increased HDL cholesterol

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7
Q

Niacin USES

A

● Familial hyperlipidemias
● severe hypercholesterolemia
● Low HDL cholesterol
● Elevated VLDL and LDL

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8
Q

Niacin Side/Effects

A

Intense cutaneous flushing
Hyperurcemia and Goat
Incr. risk of hyperuricemia

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9
Q

Niacin CONTRAINDICATIONS

A

Diabetes,
kidney and liver disease
hypertension

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10
Q

Fibrate examples

A

Gemfibrozil

Fenofibrate

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11
Q

Fibrate MOA

A

● PPAR-ɑ(alpha) agonist
● Peroxisome proliferator–activated receptors (PPARs) are members of the nuclear
receptor family that regulate lipid metabolism.
● PPARs function as ligand-activated transcription factors
● Upon binding to their natural ligands (fatty acids or eicosanoids) or antihyperlipidemic
drugs, PPARs are activated.
● They then bind to peroxisome proliferator response elements, which ultimately leads to
decreased triglyceride concentrations through increased expression of lipoprotein lipase (Figure 22.9) and decreased apolipoprotein (apo) CII concentration

Similarly it binds to ppr-a found in adipose tissue and when bound it inactive dates certain genes involved in fat metabolism

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12
Q

Fibrates USES

A

● Hypertriglyceridemias
● type III hyperlipidemia (dys-beta-lipo-protein-emia

decreases triglycerides

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13
Q

Fibrates ADVERSE EFFECTS

A

● mild gastrointestinal (GI) disturbances
● Formation of cholesterol gallstones- d/t increased biliary excretion
● Myositis
● Myopathy - for patients taking gemfibrozil and statins together
● Rhabdomyolysis - for patients taking gemfibrozil and statins together
● Both fibrates may increase the effects of warfarin
Leukopenia
Decreased hematocrits
Pancreatitis

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14
Q

Fibrates CONTRAINDICATIONS

A

● renal insufficiency
● gemfibrozil is contraindicated with simvastatin
● gemfibrozil with any statin should be avoided
● severe hepatic or renal dysfunction
● patients with preexisting gallbladder disease
● biliary cirrhosis
Pregnancy
Hepatorenal dysfunction
Gallbladder

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15
Q

Bile acid sequestrants/ Resins EXAMPLE

A

CHOLESTIPOL CHOLESTYRAMINE CHOLESEVALAM

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16
Q

Bile acid sequestrates/ Resins MOA

A

Bind to bile acids preventing their reabsorption back into blood because they function as anion exchange resins –> An insoluble resin/bile acid complex–> leading to no reabsorption because bile acids are made from cholesterol so hepatocytes increase ldl receptors to replace the lost cholesterol by bringing in more cholesterol leading to a decreased blood LDL

● anion-exchange resins that bind negatively charged bile acids and bile salts in the small intestine

● The resin/bile acid complex is excreted in the feces, thus lowering the bile acid concentration

● This causes hepatocytes to increase conversion of cholesterol to bile acids, which are essential components of the bile.

● intracellular cholesterol concentrations decrease, which activates an increased hepatic uptake of cholesterol-containing LDL-C particles, leading to a decrease in plasma LDL-

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17
Q

Bile acid sequestrates/ Resins USES

A

● type IIA hyperlipidemias
● type IIB hyperlipidemias
● Pruritus
● type 2 diabetes

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18
Q

Bile acid sequestrants/resins SIDE EFFECT

A
  1. Bloating
  2. Constipation
  3. GI disturbances, such as constipation, nausea, and flatulence,
  4. Decreased absorptions of fat soluble vitamins ADEK + Folate
    Decreased absorptions of thiazide diuretics
    Decreased absorptions of warfarin
    Decreased absorptions of digoxin
19
Q

Bile acid sequestrants/resins CONTRAINDICATIONS

A

hypertriglyceridemia

20
Q

Cholesterol absorption inhibitors: EXAMPLE

A

EZETIMBE

21
Q

Cholesterol absorption inhibitors: USE

A

Hyperlipidemia
Good for those unresponsive to statins

Elevated LDL cholesterol
Phytosterolemia

22
Q

Cholesterol absorption inhibitors: EZETIMBE

MOA

A

Cholesterol binds to NPC1L1 and undergoes endocytosis with CLATHRIN-AP2 before releasing cholesterol endocytosis is blocked.

Reduces intestinal uptake of cholesterol by inhibiting sterol transporter NPC1L1
inhibits absorption of dietary and biliary cholesterol in the small intestine, leading to a decrease in the delivery of intestinal cholesterol to the liver
his causes a reduction of hepatic cholesterol stores and an increase in clearance of cholesterol from the blood

Similarly, ezetimibe inhibits intestinal uptake of dietary and biliary cholesterol at the level of the brush border of the intestine.
This happens by the interaction with NPC1L1 without affecting the absorption of fat soluble nutrients
By inhibiting cholesterol absorption ezetimibe decreases amount of cholesterol delivered to the liver hence the liver is unregulated LDL-r expression leading to higher clearance of LDL from blood

23
Q

Cholesterol absorption inhibitors: EZETIMBE

SIDE EFFECTS

A 
Diarrhea 
Myalgia 
Increased LFT
Gi distress
Hepatic dysfunction
Myositis
Abdominal pain
Non-specific backspin
24
Q

Cholesterol absorption inhibitors: EZETIMBE

CONTRAINDICATIONS

A

homozygous familial hypercholesterolemia

moderate to severe hepatic insufficiency

25
Q

PCSK9 inhibitors: EXAMPLES

A

ALIROCUMAB

EVOLOCUMAB

26
Q

PCSK9 inhibitors: USE

A

● heterozygous or homozygous familial hypercholesterolemia
● clinical ASCVD
● statin intolerance

27
Q

PCSK9 inhibitors: MOA

A

Inhibits PCSK9 (enzyme) from breaking down LDL receptors

PCSK9 inhibitors are monoclonal antibodies that bind to and inactivate PCSK9 (propprotein converts subtilisin 9)
● —> more LDL receptors available for removal of LDL in circulation
● —> decreased LDL

28
Q

PCSK9 inhibitors: SIDE EFFECTS

A

Neurocognitive problems reactions at injection site flu-like symptoms

● Expensive
● Injection site reaction
● Nasopharyngitis
● Flu like symptoms
3rd line of therapy = They are indicated as a third option after statins, and if statins don't work, Ezetimibe with a decreased concentration of statins or Ezetimibe alone. You can also try Cholestyramine/ Cholestelevel and derivatives. Where could it be given first - genetic conditions such as familial hypercholesterolemia and if patient has statin intolerance)
29
Q

PCSK9 inhibitors: CONTRAINDICATIONS

A

Pregnancy

Angioedema

30
Q

What is the first line treatment in hyperlipidemia

A

Statins

31
Q

What is the second line treatment treatment of hyperlipidemia

A

Fibrates

32
Q

What is the main side effect of drugs use in hyperlipidemia

A

Myopathy
Hepatotoxicity
Headaches
GI Disturbances

*Leukopenia and pancreatitis are specific to Fibrates

33
Q

What is the best drug too reduce triglycerides

A

Statins

ESPECIALLY ARTOVASTATIN & RORTURVASTATIN

34
Q

WHAT IS THE BEST DRUG TO REDUCE ALL HYPERLIPIDEMIAS

A

STATINS

35
Q

Dyslipidemia group 1

A

Group 1= Primary Hyperchylomicronemia

-High level o chylomicrons

36
Q

Dyslipidemia Group 2a

A

G2a= Familial Hypercholesterolemia

High LDL levels

37
Q

Dyslipidemia group 2B

A

G2B= Familial mixed hyperlipidemia

High; VLDL, TGs, LDL

38
Q

Dyslipidemia Group 3

A

G3= Familial Dyslipoproteinemia

Increase IDL, TG, TC

39
Q

Dyslipidemia Group 5

A

G5= Mixed hypertriglyceridemia

Mainly increased TG & CYLOMICRONS (CHM)

40
Q

Dyslipidemia Group 4

A

G4= Hypertriglyceridemia

Increase VLDL, TG

41
Q

What is the formula used to measure lipids

A

Friderwald Formula

LDL-c = TC- HDL -C
_______________ mg/dL
TG/5

42
Q

Stains Indication

A

All Hyperlipidemias ( Drastically decreases triglycerides)

43
Q

Discuss the pleiotropic effect of statins

A

Statins may be used to treat MI because :

  1. It increases Nitric Oxide leading to vasodilation
  2. Has antithrombin effects
  3. Has antiinflammatory effects
  4. Stabilises plaque formation
  5. Used in patients with increased risk of stroke or MI
  6. Improvement of endothelial dysfunction,
  7. A ntioxidant properties

Pharmacology (22 decks)

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