Dyslipidemia Meds

Question 1

HMG-CoA-Reductase inhibitors

Answer 1

Statins - reduce cholesterol synthesis which increases the number of LDL receptors on the liver, permitting more uptake of LDL from the plasma.

Inhibit cholesterol synthesis by inhibiting the rate-limiting enzyme in the cholesterol synthesis pathway, which increases hepatic LDL receptors. The increase in LDL receptors ultimately causes the reduction in serum LDL.

Question 2

Statin overall effect

Answer 2

Decrease LDL
Decrease triglycerides
Increase HDL

Only approved Meds for managing cardiovascular risk

Question 3

Dietary cholesterol blockers

Answer 3

Act on cells of the brush border of the small intestine to inhibit dietary cholesterol absorption, which decreases intestinal cholesterol delivered to the liver. Inhibit reabsorption of cholesterol secreted in the bile

Question 4

Overall effect of dietary cholesterol blockers

Answer 4

Decreases LD cholesterol
Decreases triglycerides
Small increase in HDL

Used in combo with other statins

Question 5

Fibrates

Answer 5

PPAR-alpha agonists in hepatocytes

Agonism of PPAR-alpha increases liver uptake and break down of triglycerides from the plasma.

Question 6

Overall effect of fibrates

Answer 6

Decrease TG from serum levels, decrease VLDL production. Modest increase in HDL.

PRIMARILY USED TO TREAT HIGH TGs

Question 7

PPAR-alpha plays important role in

Answer 7

Lipid and or glucose homeostasis. PPAR-alpha is a transcription factor that will translocate to the cellular nucleus and regulate genes related to lipid and or glucose homeostasis. That is why fibrates induce the PPAR-alpha receptors to increase hepatic uptake and catabolism of TGs!

Question 8

Omega-3 fatty acids

Answer 8

Primarily used to treat high TGs

Question 9

Atorvastatin (Lipitor)

Answer 9

Class: Statin
Indication: Hypercholesterolemia, prevention of HD in at risk patients, and patients who need treatment for high TGs who already have high cholesterol (combined effort).
Mechanism: HMG-CoA Reductase inhibitor
Dose: at nighttime

ADE: GI probs, 3M’s: myalgias, myopathy, rhabdomyolysis, headache and memory probs, increased risk of type II DM,
INTERACTIONS: fibrates (muscle injury), grapefruit juice. Serum levels increased by Meds that inhibit CYP

Question 10

Ezetimibe (Zetia)

EDDIE

Answer 10

CLASS: Dietary cholesterol absorption inhibitor
INDICATION: Hypercholesterolemia (can be used with statins)
MOA: dietary inhibition of cholesterol
*parent drug and metabolite active

ADE: the 3M’s: Myalgia, myopathy, rhabdomyolysis; gallstones, hepatitis, pancreatitis, thrombocytopenia.
INTERACTIONS: combo with statin cocktail can increase risk of liver damage. Combo with fibrates increases risk of gallstones and myopathy. (AVOID in hepatic impairment)

Question 11

Gemfibrozil (Lopid)

George

Answer 11

Class: fibrate
INDICATION: elevated TG’s
MOA: PPAR-alpha agonists- increase hepatic uptake and clearance of TG’s (take before food)

ADE: Rash, GI upset, Gallstones (GG), hepatotoxicity, myopathy.
CONTRA: severe kidney disease
INTER: statins (increased myopathy), Warfarin (increased anti-coagulation effects)

Question 12

Omega-3-Acid (fish oil) (Lovaza)

Answer 12

CLASS: Omega-3 FA
INDICATION: elevated TGs (>500) adjunct to diet
ADE: Burping, GI upset change in taste. Can prolong bleeding.
*caution fish or shellfish allergy.
*do not take before surgery

INTER: Anti-platelet or anti-coagulant medications can increase bleeding risk

Question 13

PCSK9 Inhibitors

Answer 13

Monoclonal antibodies that block the action of the PCSK9 protein. Prevent the PCSK9 protein from binding to the LDL receptors, thus allowing