Antihyperlipidemic

Question 1

What is the class, brand name, and dosage form for Ezetimibe?

Answer 1

Antihyperlipidemic and Cholesterol Absorption inhibitor

Brand name: Zetia

Dosage Form: 10mg oral tablets

Question 2

Ezetimibe indications?

Answer 2

familial hypercholesterolemia-homozygous (atorvastatin or simvastatin)

Mixed hyperlipidemia (used in combination with fenofibrate)

primary hypercholesterolemia (used alone or with a statin) —– genetic defects resulting in high cholesterol

Question 3

Ezetimibe MOA?

Answer 3

Ezetimibe localizes at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver. This causes a reduction of hepatic cholesterol stores and an increase in clearance of cholesterol from the blood; this distinct mechanism is complementary to that of statins and of fenofibrate.

Question 4

Ezetimibe contraindiction?

Answer 4

Hypersensitivity to ezetimibe, gallbladder disease, severe hepatic dysfunction, concurrent use with a statin in a pregnant or nursing mother

Question 5

Ezetimibe ADR?

Answer 5

Common: None

Less Common: Abdominal pain, constipation, diarrhea, headache, increased liver enzymes, myopathy, nausea

Serious: Rhabdomyolysis, cholelithiasis (gallstones), hepatotoxicity, agranulocytosis (abnormally low number of granulocytes), pancreatitis

Question 6

Ezetimibe Monitoring?

Answer 6

Efficacy: Reduction in total cholesterol, LDL-cholesterol, and triglycerides levels; increase in HDL-cholesterol levels.

Toxicity: Signs/symptoms of rhabdomyolysis (myalgias, dark urine, arthralgias, fatigue), yellowing of eyes or skin, severe abdominal pain, LFT and CBC, SCr.

Question 7

Ezetimibe Counseling Points?

Answer 7

Take with or without food and may be taken at the same time as a concurrent statin. In patients receiving a bile acid sequestrant concurrently, ezetimibe should be taken at least 2 h before or 4 h after the bile acid sequestrant is taken.

Question 8

Fenofibrate brand name, dosage form, class?

Answer 8

Class antihyperlipidemic
Brand name: Antara, Fenoglide, lipofen, lofira, tricor, trilipox
Dosage form: oral tablet, oral capsule, oral capsule DR

Question 9

fenofibrate indications?

Answer 9

hypercholesterolemia, primary hypercholesterolemia, or mixed dslipidemia

hypertriglyceridemia, frederickson type 4 and 5 hyperlipidemia

Question 10

fenofibrate MOA?

Answer 10

Fibric acid derivatives activate peroxisome proliferator-activated receptor α (PPARα), which increases lipolysis and elimination of triglyceride-rich particles from plasma by activating lipoprotein lipase and reducing production of apoprotein C-III (an inhibitor of lipoprotein lipase activity). The resulting fall in triglycerides produces an alteration in the size and composition of LDL from small, dense particles to large buoyant particles. These larger particles have a greater affinity for cholesterol receptors and are catabolized rapidly.

Question 11

Fenofibrate contraindication?

Answer 11

Hypersensitivity, gallbladder disease, severe renal or hepatic dysfunction, nursing mothers

Question 12

Fenofibrate ADR?

Answer 12

Common: Hyperhomocysteinemia

Less common: Abdominal pain, constipation, diarrhea, headache, increased liver enzymes, myopathy, nausea, rash, thrombophlebitis

Serious: Rhabdomyolysis, cholelithiasis, hepatotoxicity, mood disorder, impotence, agranulocytosis, nephrotoxicity, pancreatitis

Question 13

Fenofibrate Monitoring:

Answer 13

Efficacy: reduction in total cholesterol, LDL-cholesterol, and triglycerides levels; increase in the HDL-cholesterol levels

Toxicity: Signs/symptoms of rhabdomyolysis (myalgias, dark urine, arthralgias, fatigue), yellowing of eyes or skin, severe abdominal pain; monitor LFT, CBC at baseline, 12 wk after initiation of therapy, or dose increases; serum creatine kinase should be measured in patients experiencing muscle pain and in those receiving other drugs associated with myopathy.

Question 14

Fenofibrate key counseling points:

Answer 14

Fenoglide tablets and Lipofen R capsules should be given with food; others can be taken without food. Take 1 h before or 4-6 h after a bile acid binding resin. Products are not interchangeable. Do not use if you have severe kidney disease or liver disease.

statins are first line therapy due to evidence of lower rates of cardiovascular events or death and fibrates should be reserved for patients with triglycerides of 500 mg/dl or failing lifestyle changes; MONITOR CLOSELY IS CO-ADMINSTERED WTH STATIN**

Question 15

Gemfibrozil —— class, brand name and dosage form?

Answer 15

Class: antihyperlipidemic and fibric acid
Brand name: Lopid
Dosage form: Oral tablet

Question 16

Gemfibrozil —– indications?

Answer 16

Coronary arteriosclerosis; prophylaxis-familial combined hyperlipidemia: 600 mg po bid

Familial type V hyperlipoproteinemia-Fredrickson type IV hyperlipoproteinemia: 600 mg po bid
Off-Label Uses. None

Question 17

Gemfibrozil —— MOA?

Answer 17

Fibric acid derivatives activate PPAR-α, which increases lipolysis and elimination of triglyceride-rich particles from plasma by activating lipoprotein lipase and reducing production of apoprotein C-III (an inhibitor of lipoprotein lipase activity). Activation of PPAR-α also induces an increase in the synthesis of apoproteins A-I and A-II and HDL-cholesterol.

Question 18

Gemfibrozil ——- contraindication?

Answer 18

Hypersensitivity to gemfibrozil, concurrent repaglinide or simvastatin, gallbladder disease, severe renal or hepatic dysfunction

Question 19

Gemfibrozil ——- ADR?

Answer 19

Common: Indigestion

Less common: Abdominal pain, atrial fibrillation, constipation, diarrhea, headache, increased liver enzymes, myopathy, nausea, rash

Serious: Rhabdomyolysis, cholelithiasis, hepatotoxicity, mood disorder, impotence, agranulocytosis

Question 20

Gemfibrozil —— Monitoring?

Answer 20

Efficacy Monitoring: Primary, reduction in triglyceride levels. Secondary, reduction in total cholesterol, LDL-cholesterol, increase in HDL-cholesterol levels. Monitor baseline and every 6 mo.

Toxicity: Seek medical attention if signs/symptoms of rhabdomyolysis (myalgias, dark urine, arthralgias, fatigue), yellowing of eyes or skin, and severe abdominal pain. LFTs and complete blood counts should be performed at baseline, 12 wk after initiation of therapy or dose increases. Serum creatine kinase should be measured in patients experiencing muscle pain and in those receiving other drugs associated with myopathy.

Question 21

Gemfibrozil ——– Key counseling points?

Answer 21

Take 30 min before breakfast and dinner. Instruct patient to report signs/symptoms of rhabdomyolysis, jaundice (yellowing of skin or eyes), or renal failure

**not first or second line of treatment; should not be co-administered with Statins due to heightened risk of rhabdomyolysis*

Question 22

Niacin —– Brand name, class, and dosage form?

Answer 22

Brand name: Niaspan, SLo-Niacin
Class: Antihyperlipidemic
Dosage Form: Oral capsule ER, oral tablet, oral tablet ER

Question 23

Niacin ——- Indications?

Answer 23

Coronary arteriosclerosis, hypercholesterolemia: Extended release, 500 mg po daily hs, may titrate to 2000 mg/d

Dyslipidemia: Immediate release, 100-1000 mg po tid, may titrate to 3000 mg/d; extended release, 500-2000 mg po daily hs, may titrate to 2000 mg/d

AMI, secondary prophylaxis: Extended release, 500-2000 mg po daily hs, may titrate to 2000 mg/d

Question 24

Niacin —— MOA?

Answer 24

Not well-defined. May involve partial inhibition of release of free fatty acids from adipose tissue, and increased lipoprotein lipase activity, which may increase the rate of chylomicron triglyceride removal from plasma. Niacin decreases the rate of hepatic synthesis of VLDL and LDL.

Question 25

Niacin ——— contraindications?

Answer 25

Hypersensitivity to niacin, active liver disease, PUD, arterial hemorrhage

Question 26

Niacin —————- ADR?

Answer 26

Common: Flushing and headache

Less Common: Atrial fibrillation, pruritus, rash, nausea, vomiting, reduced platelet count, elevated LFTs, myalgia

Serious: Hypophosphatemia, hepatotoxicity, rhabdomyolysis

Question 27

Niacin —— Key patient counseling points?

Answer 27

Start with a low dose and titrate based on tolerability (primarily flushing). Avoid alcohol and warm beverages with niacin to reduce flushing. If discontinued for several days, may need to restart on a lower dose and retitrate. Aspirin or NSAID 30 min prior to niacin may reduce flushing. Take at bedtime with a low-fat snack to help with flushing

**Vitamin B3

Question 28

OMEGA-3-ACID ETHYL ESTERS: Brand name, dosage form, class

Answer 28

Brand name: Lovaza
Dosage form: oral capsule liquid filled, oral capsule DR, oral tablet,chewable

Class: Antuhyperlipidemic, OMEGA-3 fatty acids

Question 29

OMEGA-3-ACID ETHYL ESTERS: indication?

Answer 29

Hypertriglyceridemia, adjunct to diet in adults with triglyceride levels 500 mg/dL or higher: 4 g po daily or divided into 2 doses

Question 30

OMEGA-3-ACID ETHYL ESTERS: MOA and Contraindication?

Answer 30

Potential mechanisms of action include inhibition of acyl-CoA:1,2-diacylglycerol acyltransferase, increased mitochondrial and peroxisomal β-oxidation in the liver, decreased lipogenesis in the liver, and increased plasma lipoprotein lipase activity. Lovaza may reduce the synthesis of triglycerides in the liver because eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) are poor substrates for the enzymes responsible for TG synthesis, and EPA and DHA inhibit esterification of other fatty acids.

Contraindication: Hypersensitivity to omega-3-acid ethyl esters, fish, or shellfish

Question 31

OMEGA-3-ACID ETHYL ESTERS: ADR?

Answer 31

Common: Diarrhea

Less Common: indigestion, taste alterations, rash, burping, arthralgia

Serious: Anaphylaxis, elevated LFTs

Question 32

OMEGA-3-ACID ETHYL ESTERS: Monitoring and key counseling points/clinical pearls?

Answer 32

Efficacy: reduction in triglyceride levels

Toxicity: LDL, LFTs

Key counseling points/clinical pearls: Swallow the whole capsule; take with food. Seek medical attention if severe rash, chest pain, heart palpitations, or shortness of breath.

Omega-3-acid ethyl esters are available OTC as fish oil and contain lower amounts of DHA and EPA than the prescription version. OTC products have varying amounts of DHA and EPA. Each Lovaza capsule contains ∼375 mg of DHA and 465 mg of EPA. Treatment of hypertriglyceridemia with omega-3-acid ethyl esters has shown to be equivalent to gemfibrozil in efficacy. Omega-3-acid ethyl esters have not been shown to decrease cardiovascular mortality. Freezing capsules may decrease fishy taste*