anti-hyperlipidemic drugs

Question 1

Fibric acid derivatives

Answer 1

• Gemfibrozol/ Lopid

* Fenobibrate/ Lofibra

Question 2

Gemfibrozol/ Lopid

Answer 2

Class: Anti-hyperlipidemic, fibric acid derivative
• Indication: Elevated triglyceride levels, low HDL level. Types IV and V hyperlipidemia.
• Char: PO
• Side effects as noted. Contraindicated in patients with pre-existing gallbladder disease and liver disease.

Question 3

HMG-CoA reductase inhibitors

Answer 3

the statin drugs.
• The statin drugs were originally derived from naturally occurring compounds found in fungi.
• Statins block the rate limiting enzyme of cholesterol production in the liver. (blocked product is Mevalonate)

Question 4

Problems with statin drugs

Answer 4

MC: muscle soreness and muscle weakness.
• A potentially life threatening: rhabdomyolysis, the severe and rapid muscle breakdown which can lead to acute renal failure.
• The statin drug, Baycol, was recalled after multiple deaths from rhabdomyolysis.
• Memory and cognitive dysfunction
• Insomnia

Question 5

Coenzyme Q10

Answer 5

HMG CoA reductase is also involved in the production of CoQ10.
• CoQ10 is a crucial component of the oxidative phosphorylation in mitochondria which converts the energy in carbohydrates and fatty acids into ATP
• may account for complaints of muscle soreness, muscle weakness and frank rhabdomyolysis.

Question 6

Additional statin side effects

Answer 6

• Abdominal pain • Nausea
• Diarrhea
• Headache
• Erectile dysfunction

Question 7

Contraindications to statins

Answer 7

• Heavy alcohol use
• Liver disease
• Unexplained elevation of liver enzymes
• Pregnancy
• Lactation

Question 8

Potential statin- drug interactions

Answer 8

when statins are used with drugs such as:
• Fibric acid derivatives
• Macrolides i.e. Biaxin, Erythromycin and Zithromax
• Oral anti-fungals i.e. Ketoconazole
• Protease inhibitors
***all cytochrome 450 inhibitors.

Question 9

Statins

Answer 9

• Atorvastin/ Lipitor
• Fluvastatin/ Lescol
• Lovastatin/ Mevacor
• Pravastatin/ Pravachol
• Rosuvastatin/ Crestor
• Simvastatin/ Zocar

Question 10

Atorvastin/ Lipitor

Answer 10

Class: Anti-hyperlipidemic, HMG-CoA reductase inhibitor
• Indication: Elevated total cholesterol, elevated LDL, low HDL levels. Indicated for symptomatic and non-symptomatic coronary artery disease.
• Char: PO, very effective in ↓’ing cholesterol.
•check thyroid !

Question 11

Atorvastin/ Lipitor SE

Answer 11

Side effects: Muscle soreness and weakness. Check CPK levels to assess for possible rhabdomyolysis when complaints of severe muscle pain are noted.May cause elevated liver enzymes. Follow LFTs – prior to beginning therapy and at 6 weeks and 12 weeks.

CATEGORY X

Question 12

Bile acid sequestrants

Answer 12

Bile acid sequestrants bind cholesterol and form insoluble complexes which are excreted in the feces.
• Compensatory mechanisms increase the number of LDL receptors which serve to bind more LDL, removing LDL particles from the blood stream.
• May interfere with normal fat absorption.
• Bile acid sequestrants are often used in conjunction with niacin.


Question 13

Bile acid sequestrants

Answer 13

• Cholestyramine/ Questran
• Colesevelam/ Welchol
• Colestipol/ Colestid

Question 14

Cholestyramine/ Questran

Answer 14

Class: Anti-hyperlipidemic, bile acid sequestrant.
• Ind: Elevated cholesterol, elevated LDL.
• MOA: Forms an insoluble complex with bile salts resulting in greater amounts of cholesterol being oxidized into bile acids and increased excretion of bile acids in stool.
• Char: PO, administered in tabs or granules.

TAKE OTHER DRUGS AT LEAST ONE HOUR BEFORE OR AT LEAST 4 TO 6 HOURS AFTER QUESTRAN

Question 15

Cholestyramine/ Questran SE

Answer 15

Constipation, bloating, may interfere with the absorption of fat soluble vitamins and folic acid. May delay the absorption of concomitant medications. The use of bile acid sequestrants has not been adequately studied in pregnant women . Cholestyramine is also used to prevent diarrhea in Crohn’s disease patients who have undergone post-ileal resection

CATEGORY C

Question 16

Cholesterol absorption inhibitors

Answer 16

act by reducing the amount of cholesterol that is absorbed by the body.
• Ezetimibe/ Zetia is used to reduce the amount of total serum cholesterol, LDL, triglycerides and apolipoprotein B .
• Ezetimibe is often used in conjunction with a statin when the statin therapy has been insufficient in lowering total serum cholesterol.

Question 17

Ezetimibe/ Zetia

Answer 17

Class: Anti-hyperlipidemic - cholesterol absorption inhibitor
• Ind: Elevated cholesterol, elevated LDL, elevated Trig. and low HDL
• MOA: Inhibits intestinal absorption of cholesterol at the brush border.
• Char: PO. Often used in conjunction with a statin.

Question 18

Ezetimibe/ Zetia SE

Answer 18

• Side effects: Diarrhea, myalgias, arthralgias, abdominal pain. All of the statin concerns to be observed when Ezetimibe is used with a statin drug.
Cautious use in pregnancy - CATEGORY C

• Ezetimibe is also available as a drug which combines the statin, Simvastatin, with Ezetimibe into a single fixed dose pill, Vytorin.

Vytorin is CATEGORY X (dont use with fibrates)

Question 19

Lovaza

Answer 19

Lovaza is a brand name prescription drug that contains esterified fish oils that are metabolized into Omega-3 fatty acids.
• Lovaza is indicated for lowering elevated triglyceride levels.
• It has also been shown to reduce VLDL- cholesterol and to raise HDL-cholesterol.

• However Lovaza (as well as supplement
versions of fish oils) has also been shown to potentially increase LDL levels*.

liver enzymes should be checked, periodically.

has not been shown to lower the rates of all-cause mortality and cardiovascular mortality.

Question 20

Lab Values of Concern

Answer 20

♥ Total blood cholesterol* > 200 mg/dl
♥ LDL cholesterol > 130 mg/dl
♥ HDL cholesterol 30 mg/dl
• *Keeping in mind that the ratios of LDL: HDL and total cholesterol: HDL is of greater clinical significance than the total serum cholesterol level.

Question 21

Cholesterol ratios

Answer 21

• There are two important ratios that should be considered:
♥ LDL Cholesterol/ HDL Cholesterol (Should not exceed 2.5)
♥ Total Cholesterol/ HDL Cholesterol (Should not exceed 4)

Question 22

Medications for hyperlipidemia

Answer 22

• Niacin
• Fibrates
• HMG-CoA reductase inhibitors =statins
• Bile acid binding resins
• Cholesterol absorption blockers

Question 23

Niacin/ nicotinic acid

Answer 23

• Niacin, a form of vitamin B3, has been shown to effectively lower total serum cholesterol levels.
• Niacin may lower levels of total serum cholesterol and LDL cholesterol by 15% to 20%, while decreasing serum levels of triglycerides by 15% to 35%.
• In addition, niacin has been shown to increase HDL levels by 15% TO 35%.
***decreased levels of alpha-lipoprotein(a)

***niacinamide form doesnt work

Question 24

Diabetics and Niacin

Answer 24

Niacin is known to potentially affect blood sugar control in diabetics, thus blood sugar levels should be more closely monitored in diabetics begun on niacin.

Question 25

Niacin/ nicotinic acid SE

Answer 25

• use of niacin in > 3 grams has resulted in acute side effects of flushing, nausea, gastritis and headache.
• Longer term potential side effects include liver damage, retinal damage, gout and rhabdomyolysis

Question 26

Niacin/ Niaspan

Answer 26

Class: Anti-hyperlipidemic/ B vitamin
• Indication: Elevated total cholesterol, elevated VLDL, LDL, TG and low HDL levels.
• MOA: Exact mechanism of action is not clear. Niacin appears to decrease VLDL synthesis in the liver while also increasing the clearance of VLDL in the plasma.
• Char: PO. Intense flushing and pruritis is common.

Question 27

Niacin/Niaspan SE

Answer 27

Less flushing and itching when ASA or NSAIDs taken 30 minutes to an hour before the niacin dose.

• Follow with LFTs to monitor for any possible hepatic damage.

Also monitor glucose levels. Contraindicated in patients with poorly controlled DM, active liver disease or active peptic ulcer disease.

Question 28

Inositol hexaniacinate

Answer 28

• The non-prescription supplement, inositol hexaniacinate (IH), appears to be the safest form of niacin that is currently available.
• Inositol hexaniacinate appears to be much better tolerated than niacin
• Recommended dose is 500 - 1000 mg given three times daily, with meals.

Question 29

Fibric acid derivatives

Answer 29

Fibric acid derivatives decreases triglyceride production in the liver.
• May decrease TGs up to 20% to 50%
• May increase HDL up to 15%
• The most commonly used drug in this category is Gemfibrozil/Lopid.
• Potential side effects include liver damage, gall stone formation, nausea, diarrhea, GI upset, rhabdomyolysis and myalgias.