Flashcards in anti-hyperlipidemic drugs Deck (29):
Fibric acid derivatives
• Gemfibrozol/ Lopid
• Fenobibrate/ Lofibra
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.
HMG-CoA reductase inhibitors
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)
Problems with statin drugs
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
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.
Additional statin side effects
• Abdominal pain • Nausea
• Erectile dysfunction
***Contraindications to statins***
• Heavy alcohol use
• Liver disease
• Unexplained elevation of liver enzymes
Potential statin- drug interactions
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.
• Atorvastin/ Lipitor
• Fluvastatin/ Lescol
• Lovastatin/ Mevacor
• Pravastatin/ Pravachol
• Rosuvastatin/ Crestor
• Simvastatin/ Zocar
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 !
Atorvastin/ Lipitor SE
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.
Bile acid sequestrants
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.
Bile acid sequestrants
• Cholestyramine/ Questran
• Colesevelam/ Welchol
• Colestipol/ Colestid
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
Cholestyramine/ Questran SE
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
Cholesterol absorption inhibitors
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.
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.
Ezetimibe/ Zetia SE
• 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)
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.
Lab Values of Concern
♥ 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.
• 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)
Medications for hyperlipidemia
• HMG-CoA reductase inhibitors =statins
• Bile acid binding resins
• Cholesterol absorption blockers
Niacin/ nicotinic acid
• 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
Diabetics and Niacin
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.
Niacin/ nicotinic acid SE
• 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
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.
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.
• 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.