Pharm - Cholesterol Meds Flashcards
When treater high cholesterol, what is the first line of treatment unless what is already present?
First thing to do is manage/change the diet unless the patient already has CAD or PVD or genetic high cholesterol, then do diet and drug.
What are 3 dietary recommendations for lowering cholesterol?
Fat calories less than 20-25% of daily intake, saturated fats less than 8% of daily intake, and cholesterol less than 200mg/day.
What are the 6 families of drugs to treat high cholesterol?
HMG CoA reductase inhibitors, niacin, fibrates, bile acid resins, cholesterol absorption inhibitors, new treatments.
Statins are most effective against treating what specifically?
Most effective in lowering LDL levels.
MOA for statins and what are the two effects?
Inhibit HMG CoA reductase, rate limiting step in cholesterol synthesis. Lowers cholesterol synthesis, but also up regulates LDL receptors and pulls more cholesterol into the cells out of the blood.
Top 4 statins as far as potency?
Atorva, rosu, simva, and pitava
What is important to note about the pharmacokinetics of statins?
They have extensive first pass effect in the liver, so their dominant effect is in the liver.
Adverse effect of statins?
Elevated liver enzymes.
Niacin is used to treat what 3 things?
Lower TG, lower LDL and best at raising HDL.
MOA for niacin?
Inhibits lipolysis which reduces circulating free fatty acids. Decreases break down of HDL.
What 2 effects do fibrates have on lower cholesterol?
Lower TG and increase HDL
What do statins do to muscle?
Break down, so creatine kinase activity may rise.
What patient population is contraindicated for statins?
Pregnancy
Most common adverse effect of niacin?
Beta alanine rush.
Niacin is contraindicated in what patients?
Liver disease
MOA for fibrates?
Agonists for PPARs, which increase lipoprotein lipase and break down fatty acids and lead to lower TG.
2 top adverse effects of fibrates?
GI disturbances are most common. Gallstones because increase biliary cholesterol excretion.
1 effect of using bile acid resins?
Lower LDL
MOA for bile acid/salt resins?
They bind the bile acids/salts and form a complex to be excreted. Because of the drop in bile acids/salts, hepatocytes increase conversion of cholesterol to bile acids. This also drops cholesterol levels, so LDL receptors are unregulated and clear more cholesterol from the blood.
Most common adverse effects of bile acid resins?
GI disturbances
MOA of cholesterol absorption inhibitors?
Selectively inhibits intestinal absorption of cholesterol
1 effect of using cholesterol absorption inhibitors?
Lower LDL
What do the new treatment drugs treat, what type of high cholesterol?
Homozygous familial high cholesterol
MAO for lomitapide?
Inhibits MTP which lowers production of chylomicrons and VLDL which leads to lowering of LDL.
MOA for Mipomersen?
Inhibitor of APOB
Black box warning for mipomersen?
Liver toxicity
What 3 drug families lower LDL and rank them in order of effectiveness?
Statins, bile acid resins, and niacin
Top 3 drug families to increase HDL and rank them in order of effectiveness starting with strongest?
Niacin, fibrates and statins
Top 3 drug families to lower TG and rank them in order of effectiveness starting with strongest?
Fibrates, niacin and statins
What are the two types of clots?
White and Red
