Pharm Lilley Ch 27 Antilipemic Drugs

Antilipemic drugs
Drugs that lower lipid levels, used as adjunct to diet therapy; drug choice based on patient; diet & exercise should be tried at least 6 mos and fail before drug therapy is considered; CONTRAINDICATED for biliary obstruction, liver dysfunct., active liver disease; patients with long-term therapy may need supplemental vitamins A,D&K, take with meals; powder forms must be takin with liquid, mixed thoroughly/not stirred, NEVER taken dry and other meds must be taken 1 hr before or 4-6 hrs after meals to avoid absorption interference; MAY TAKE several weeks to show effectiveness; HMG-CoA reductase inhibitors (HMGs, or statins), bile acid sequestrants, niacin (nicotinic acid), fibric acid derivatives (fibrates), cholesterol absorption inhibitor (zetia), combo drugs (Vytorin)

Triglycerides & Cholesterol
two primary forms of lipids in the blood, water-insoluble fats that must be bound to apolipoproteins;

apolipoproteins
specialized lipid carrying proteins

lipoprotein
combination of triglyceride or cholesterol with apolipoprotein; transports lipids via the blood

Very-low-density lipoprotein (VLDL)
produced by the liver, transports endogenous lipids to the cells

Low-density lipoprotein (LDL)
“bad cholesterol”

High-density lipoprotein (HDL)
“good cholesterol” believed to be cardioprotective, responsible for “recycling” of cholesterol

Coronary Heart Disease
the risk of of CHD in patients with cholesterol levels of 300 mg/dL is 3-4x greater than that in patients with levels less than 200 mg/dL; risks include males 45+, family history of CHD/MI, smoking, hypertension, low HDL -40mg/dL, diabetes; having higher HDL reduces risk slightly

HMG-CoA Reductase Inhibitors (HMGs or statins)
Most potent LDL reducers, work by inhibiting HMG-CoA reductase which is used by the liver to produce cholesterol; USED FOR first-line drug therapy for hypercholesterolemia, treatment of types 2a and 2b hyperlipidemias; reduces LDL by 30-40%, increases HDL by 2-15%, reduces triglycerides by 10-30% ADVERSE EFFECTS mild GI disturbances, rash, myopathy (muscle pain) / rhabdomyolysis, elevated liver enzymes, liver disease; INTERACTS warafarin, erythromycin, clarithromycin, gemfibrozil, HIV/Hep C inhib, grapefruit juice. DO NOT USE PREGNANCY CATEGORY X or breast feeding. Drugs best taken at bedtime correlates with bodies natural diurnal rhythm of cholesterol production.
pravastatin (Pravachol), simvastatin (Zocor), atorvastatin (Lipitor), fluvastatin (Lescol), rosuvastatin (Crestor), pitavastatin (Livalo)

Bile Acid Sequestrants
Prevent resorption of bile acids from small intestine, allows them to absorb more cholesterol USED FOR type 2 hyperlipoproteinemia, pruritus assoc w/partial biliary obstruction (cholestyramine), can be used with statins; ADVERSE constipation, gas & GI disturbances TOXICITY causes GI obstruction, treatment involves restoring gut motility; OTHER DRUGS MUST BE TAKEN 1 hour before or 4-6 hrs after bile acid sequestrants CONTRAINDICATED for complete biliary obstruction or PKU
cholestyramine (Questran), colestipol hydrochloride (colestid), colesevelam (Welchol), bile acid-binding resins/ion-exchange resins

Niacin (Nicotinic Acid)
Vitamin B3, lipid lowering properties, increase lipase activity which breaks downs lipids, reduces metabolism of cholesterol and triglycerides; USED TO lower triglyceride, cholesterol, LDL, increase HDL, treats 2a,2b,3,4 and 5 hyperlipidemias; require higher dose than whats used as vitamin, effective, inexpensive, can be used in conjunction with lipid-lowering drugs ADVERSE flushing, pruritus, GI dist; start with lower dose and gradually increase, take with meals

Fibric Acid Derivatives (Fibrates)
activates lipase, suppress free fatty acid, inhibit triglyceride synthesis, increase secretion of cholesterol in bile USED FOR treatment of 3, 4 and 5 hyperlipidemias, decrease triglyceride level and increase HDL by 25% ADVERSE GI, blurred vision/headache, gallstones, prolonged prothrombin time, altered liver studies INTERACTS anticoags, increase rhabdomyolisys when given with statin, lab value monitoring important
gemfibrozil (Lopid), fenofibrate (Tricor)

Cholesterol Absorption Inhibitor
Inhibits cholesterol absorp., reduces cholesterol, LDL and triglycerides, increases HDL, can combine with statins, ONLY USED when patients haven’t responded to other therapy; NOT recommended for use with fibrates or bile acid sequestirants;
ezetimibe (Zetia)

Garlic
used as antispasmodic, antihypertensive, antiplatelet, lipid reducer ADVERSE dermatitis, vomitting, diarrhea, gas, antiplatelet activity INTERACTS with warfarin, diazepam, enhanced bleeding with NSAIDs

Flax
Seed and oil, USED for atherosclerosis, hypercholesterolemia, GI dist, menopause ADVERSE diarrhea, allergic react. INTERACTS antidiabetics and anticoagulants

Omega3 Fatty Acids
fish oil products, USED to reduce cholesterol, ADVERSE rash, gas, allergic reactions, INTERACTS anticoagulants

combo drug VYTORIN
combo tablet that contains both the statin drug simvastatin and the cholesterl absorption inhibitor ezetimibe (Zetia)

Rhabdomyolysis
INCREASED RISK WITH STATINS breakdown of muscle protein accompanied by myoglobinuria, which is the urinary elimination of the muscle protein myoglobin. This abnormal urinary excretion of protein can place a severe strain on the kidneys, leading to acute renal failure and even death. Is dose dependent and is more common in patients receiving a statin in combo with cyclosporine, niacin, gemfibrozil (a fibrate), or erythromycin. Advise patients receiving statin therapy to immediately report any unexplained muscular pain or discomfort. When recognized early, it is usually reversible with discont of the statin. prescribers should use min effective doses, with regular laby monitoring of liver and kidney function (every 3 to 6 months). Patients should immediately report muscle soreness, changes in urine color, fever, malaise, nausea, or vomiting.

Lipoprotein the combination of triglyceride or cholesterol with apolipoprotein Very low density lipoprotein produced by the liver, transports endogenous lipids to the cells WE WILL WRITE A CUSTOM ESSAY SAMPLE ON ANY TOPIC SPECIFICALLY FOR YOU FOR ONLY $13.90/PAGE Write …

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HMG-GA Reductase Inhibitors drugs -Statin, Lipitor HMGA-GA effect Decrease rate of cholesterol production WE WILL WRITE A CUSTOM ESSAY SAMPLE ON ANY TOPIC SPECIFICALLY FOR YOU FOR ONLY $13.90/PAGE Write my sample Statin adverse reaction Mild transient GI disturbances, increase …

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