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Prophylaxis of Coronary Heart Disease
Drugs that lower cholesterol (and Nitrates)
50
Pharmacology
Undergraduate 3
03/18/2010

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Term
Example of HMG-CoA reductase inhibitor.
Definition
Statins.
Term
Mechanism of action of HMG-CoA reductase inhibitor.
Definition
Statins inhibit the enzyme (HMG-CoA) that synthesizes cholesterol and increases the # of LDL receptors on liver cells; therefore, decreasing LDL levels. Can also increase HDL levels and lower TGs- effect unknown.
Term
Indication of HMG-CoA reductase inhibitor.
Definition
Hypercholesterolemia and mixed dyslipidemias; elevated LDL cholesterol that cannot be controlled via diet and exercise; pts w/high risk of CV events, post MI, diabetes.
Term
Contraindications of HMG-CoA reductase inhibitor.
Definition
Pts w/ viral or alcoholic hepatitis and pregnant woman. Caution in pts w/nonalcoholic fatty liver disease, those who drink alcohol excessively, those taking fivrates or ezetimibe or agents that inhibit CYP3A4.
Term
Serious adverse effects of HMG-CoA reductase inhibitor.
Definition
Hepatotoxicity (can injure liver, but jaundice and further signs are rare); rabdomyelysis (breakdown of skeletal muscle- release of chemicals into bloodstream); Myopathy (can rarely cause muscle injury, mechanism unknown); peripheral neuropathy.
Term
Common adverse effects of HMG-CoA reductase inhibitor.
Definition
Side effects uncommon. Dizziness, insomnia, chest pain, weakness, headache, rhinitis, blurred vision, rash, and some GI disturbances (abdominal cramps, flatulence, constipation)- all usually mild and transient.
Term
Preadministration assessment of HMG-CoA reductase inhibitor.
Definition
Baseline lipid profile, full cholesterol profile, LFT and CKs, pregnancy test, dietary Hx (for fat consumption)
Term
Monitoring of HMG-CoA reductase inhibitor.
Definition
Cholesterol levels should be monitored monthly (serum cholesterol); liver function tests for hepatotoxicity, if unexplained muscle pain, CK level should be measured- if > 10X ULN, statin should be withdrawn.
Term
Patient education of HMG-CoA reductase inhibitor.
Definition
Take lovastatin w/ evening meal, all others can be taken w/out regard to food- all statins should be taken in the evening (body makes more cholesterol at night); inform PCP if muscle pain or tenderness developes. Promote diet, exercise, and lifestyle changes.
Term
Example of Bile-acid sequestrants.
Definition
Colesevalam.
Term
Mechanism of action of Bile-acid sequestrants.
Definition
Reduces LDL cholesterol by binding to bile salts, preventing reabsorption. Increases receptors on hepatocytes. Body picks up more LDL to make more bile salts, so less LDL in body. Often used in combo w/statin. Doesn't raise HDL, may raise TGs.
Term
Indication of Bile-acid sequestrants.
Definition
High LDL cholesterol and hyperglycemia in diabetic patients.
Term
Contraindication of Bile-acid sequestrants.
Definition
Genetic inability to increase synthesis of liver LDL receptors.
Term
Serious adverse effects of Bile-acid sequestrants.
Definition
The drug remains in the GI tract, so there are no systemic effects.
Term
Common adverse effects of Bile-acid sequestrants.
Definition
GI tract- constipation, bloating, nausea, indigestion. Some older forms of the drug can inhibit vitamin absorption.
Term
Preadministration assessment of Bile-acid sequestrants.
Definition
Baseline cholesterol levels (LDL, HDL, and THs/VLDLs). Identify CHD risk factors (smoking, obesity, age, family Hx, and high BP).
Term
Monitoring of Bile-acid sequestrants.
Definition
Monitor cholesterol levels and for GI side effects.
Term
Patient education of Bile-acid sequestrants.
Definition
Vitamin supplements may be needed. To reduce constipation, increase fiber and fluids. Take other meds 1hr before or 4hrs after to minimize absorption problems.
Term
Mechanism of action of Nicotinic acid.
Definition
Decreases productin of VLDLs by inhibiting lipolysis, causing LDL #s to fall as well.
Term
Indication of Nicotinic acid.
Definition
For pts w/high LDL #s and low HDL #s, especially for those at risk of pancreatitis.
Term
Contraindications of Nicotinic acid.
Definition
Pts w/active liver disease or those w/sever or recurrent gout. Caution in pts w/DM, asymptomatic hyperuricemia, mild gout, and peptic ulcer disease.
Term
Serious adverse effects of Nicotinic acid.
Definition
Hepatotoxic- more likely w/slo-niacin (long acting formulation) especially if in high doses or when used w/a statin. Hyperglycemia, gouty arthritis.
Term
Common adverse effects of Nicotinic acid.
Definition
Flushing, itching (occurs in almost all pts, will diminish in several weeks), GI rxns are also common
Term
Preadministration assessment of Nicotinic acid.
Definition
Baseline cholesterol levels (LDL, HDL, and THs/VLDLs). Identify CHD risk factors (smoking, obesity, age, family Hx, and high BP); liver function tests to check liver condition.
Term
Monitoring of Nicotinic acid.
Definition
Monitor cholesterol levels, liver function tests to make sure liver isn't being damaged, blood lipid levels should be continually monitored.
Term
Patient education of Nicotinic acid.
Definition
Advise pts to use immediate-release formulations or ER, not long-acting (slo-niacin). Take w/meals to reduce stomach upset. Diet modification counseling. Flushing can be lessened if aspirin is taken before, also if taking ER form.
Term
Mechanism of action of Ezetimibe.
Definition
Inhibits cholesterol absorption by acting on cells of brush border of the small intestine to inhibit cholesterol absorption. Reduces LDL, TG, total cholesterol, and might slightly increase HDL. Blocks dietary and bile cholesterol.
Term
Indication of Ezetimibe.
Definition
Reduce total cholesterol and apolipoprotein B (transports fat to nonhepatic tissue) w/diet modicigation. Greater effect when used w/a statin.
Term
Contraindications of Ezetimibe.
Definition
Hepatic disease/hepatic insufficiency, severe allergy
Term
Serious adverse effects of Ezetimibe.
Definition
Drug-drug interactions, gall stones, myopothy
Term
Common adverse effects of Ezetimibe.
Definition
GI upset
Term
Preadministration assessment of Ezetimibe.
Definition
Total cholesterol levels (TG, LDL, HDL), know other drugs being taken at the same time.
Term
Monitoring of Ezetimibe.
Definition
Drug levels of Ezetimibe, liver damage (indicated by transaminase levels), liver function tests
Term
Patient education for Ezetimibe.
Definition
Talk to provider before beginning other drugs because of drug-drug interactions. Lower dietary cholesterol.
Term
An example of Fibric acid derivatives.
Definition
Gemfibrozil.
Term
Mechanism of Fibric acid derivatives.
Definition
Interacts w/specific receptor subtypes to decrease VLDL production by liver, so lowers plasma TG levels. Can slightly raise HDL levels pts w/normal TG levels, can reduce LDL to minor extent. If TG levels are high, can actually raise LDL levels.
Term
Indication of Fibric acid derivatives.
Definition
Used to reduce TGs, not very effective at lowering LDL, may be used to raise HDL. Principal indication is hypertriglyceridemia.
Term
Contraindications of Fibric acid derivatives.
Definition
Pts w/liver disease, severe renal dysfunction, and gallbladder disease. Also those on warfarin. Caution w/those on statins.
Term
Serious adverse effects of Fibric acid derivatives.
Definition
Gallstones, Myopothy, liver disease (may disrupt liver function)
Term
Common adverse effects of Fibric acid derivatives.
Definition
GI upset, rash
Term
Preadministration assessment of Fibric acid derivatives.
Definition
Baseline cholesterol levels (LDL, HDL, and THs/VLDLs). Identify CHD risk factors (smoking, obesity, age, family Hx, and high BP); pre-existing muscle pain; liver function.
Term
Monitoring of Fibric acid derivatives.
Definition
Monitor blood lipids, liver function, muscle pain.
Term
Patient education for Fibric acid derivatives.
Definition
Take 30 minutes before morning and evening meals. Inform pts of gallbladder symptoms, notify PCP if noticed. Also signs of muscle injury. Promote diet, exercise, and lifestyle changes.
Term
Mechanism of action of Nitrates
Definition
Vasodilates smooth muscles, acts mostly on veins, only slightly on arterioles. Stable Angina- decreases pain by decreasing oxygen demand (dilate veins leading to reduced venous return leading to reduced ventricular filling leading to reduced preload leading to reduced oxygen demand) Varient angina- relaxes/prevents spasm in coronary arteries leading to increased oxygen supply, not reduction in oxygen demand)
Term
Indications for Nitrates.
Definition
Angina attacks.
Term
Contraindications for Nitrates.
Definition
Use w/sildenafil (viagra) or other PDE5 inhibitors (erectile dysfunction drugs); very important to ask- BOTH men and women.
Term
Common adverse effects of Nitrates.
Definition
Headace- will lessen over first few weeks of treatment, use aspirin or tylenol. Orthostatic hypotension. Tachycrdia- b/c BP is lower, HR will increase to make up for it (pretreat w/a beta blocker or Ca channel blocker).
Term
Preadministration assessment for Nitrates.
Definition
Baseline for frequency, intensity, location, and triggers of angina attacks. Monitor BP before and after each dose.
Term
Forms of Nitrates
Definition
Sublingual- under tongue, wait 5 min and call 911 if not relieved, can take 2 more in next 10 min. SR- taken daily to avoid attacks. Transdermal/Topical- on skin, covered, to protect against attacks. Translingual- spray into mouth for termination of attack. Transmucosal- between gums and upper lip, dissolves in 3-5 hrs, to terminate attacks. IV- used in ICU/ER when SL isn't working
Term
Patient education for Nitrates.
Definition
Tell pt to sit/lie down in case of orthst hypotens. Promote wt reduction, exercise, smoking cessation, avoid alcohol. Tolerance can develope rapidly, use lowest dose able on an intermittent schedule (drug-free for at lest 8 hrs). Needs to be discontinued slowly.
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