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Science
Medicine
Chapter 27 Antilipemic Drugs
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Terms in this set (37)
Forms of lipids in the blood
Triglycerides
- stored in adipose tissue, used as an energy source.
Cholesterol
- used to make steroid hormones, cell membranes, and bile acids.
Five classes of Antilipemic drugs
1. Hydrooxymethylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors
2. Bile acid sequestrants
3. B vitamin Niacin
4. Fibric acid derivatives
5. Cholesterol absorption inhibitors
Hydrooxymethylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors
Generic names all end in -statin.
Most effective
drugs for lowering LDL and total cholesterol, in some patients it can also raise HDL and lower triglycerides.
Mechanism of action
-
HMG-CoA reductase is required for cholesterol synthesis, when this enzyme is blocked, cholesterol synthesis decreases. Inhibition of cholesterol synthesis in the liver increases the number of LDL receptors, as a result hepatocytes (liver cells) are better able to remove LDL from the blood and blood levels are decreased.
Used for
- hyperlipidemia (high cholesterol)
Contraindications to the use of HMG-CoA Reductase Inhibitors
Drug allergy.
Pregnancy- risk category X (risk to fetus outweighs any benefit to mom).
Liver disease.
Adverse effects of HMG-CoA Reductase Inhibitors
-
Myopathy
(muscle pain): Risk is higher in patient with small frame, fraility, multi-system disease, renal disease, patients of Asian descent.
- Liver injury
- Cataracts
- GI upset (abdominal pain, constipation, diarrhea, nausea)
- Headache
- Rash
- Insomnia
Interactions with HMG-CoA Reductase Inhibitors
Other lipid lowering drugs can increase the risk of myopathy.
Drugs that inhibit CYP3A3 (an enzyme system)- can raise the level of the statins (increases the risk of liver injury and myopathy).
- Erythromycin
- Ketoconazole, Itraconozole
- HIV protease inhibitors
- Amiodarone
- Cyclosporine
Coumadin (warfarin)
Grapefruit juice.
HMG-CoA Reductase Inhibitors are best taken in the-
A. Morning
B. Afternoon
C. Evening
C. Evening
Endogenous cholesterol is produced by the liver in the evening.
All are dosed once daily.
Examples of HMG-CoA Reductase Inhibitors
Atorvastatin (Lipitor)
Fluvastatin (Lescol)
Lovastatin (Mevacor)
Pravastatin (Pravachol)
Simvastatin (Zocor)
Rosuvastatin (Crestor)
Pitavastatin (Livalo)
Bile Acid Sequestrants
Now considered second line agents for reducing cholesterol. Widely used as adjuncts to the statins.
Used for
-
- high cholesterol (hyperlipidemia).
- pruritus (itching) associated with partial biliary obstruction.
- off label use: diarrhea r/t excessive bile acids.
Three available agents
-
- Colesevelam (Welchol)
- Cholestryramine (Questran)
- Colestipol (Colestid)
Mechanism of action of Bile Acid Sequestrants
Bile acids are normally reabsorbed and reused. Bile Acid Sequestrants prevent this reabsorption and accelerates their excretion (in the stool). An increase in excretion demands an increased synthesis of bile acids. Bile acids require cholesterol for synthesis, so the liver converts more cholesterol into bile acids which decreases the amount of cholesterol in the blood.
Contraindications to the use of Bile Acid Sequestrants
Allergy.
Biliary or bowel obstruction.
Phenylketonuria (PKU)
- an inherited disease. Increases the amount of phenylanine (building blocks of proteins) in the blood. If not treated, can lead to intellectual disability and health problems.
Adverse effects of Bile Acid Sequestrants
- Devoid of systemic side effects because they are not absorbed from the GI tract.
- Constipation
- Nausea
- Bloating/gas
- Indigestion
Administer with meals to decrease GI effect.
Interactions with Bile Acid Sequestrants
May decrease the absorption of orally administered medications.
Bile Acid Sequestrants should be taken 1 hour before or 4 hours after other medications.
Can decrease the absorption of fat-soluble vitamins (A, D, E, K).
Nursing implications for certain Bile Acid Sequestrants
Colesevelam (Welchol)
- fewer GI adverse effects and interactions. Take with 4-8 ounces of fruit juice or water.
Cholestryramine (Questran)
- Phenylketonuria (PKU) issue. Take with meals.
Niacin
Drug of choice for lowering triglyceride levels in patients at risk for pancreatitis.
Also used to treat elevated LDLs and low HDL.
Can be used alone or in combination with other lipid-lowering drugs.
Also used as a vitamin- B3 (the doses used as a vitamin are much lower than those used to treat increased cholesterol).
Adverse effects of Niacin
-
Intense flushing of the face, neck, and ears
can occur in almost all patients receiving Niacin in pharmacologic doses. This reaction diminishes in several weeks and can be minimized by taking 325 mg of aspirin 30 minutes before each dose of Niacin.
- Liver injury
- Hyperglycemia
- Gouty arthritis
- GI upset
- Increased uric acid levels
Preparations of Niacin
Available under several trade names and generically.
Available in immediate release, timed release, controlled release, sustained release, and extended release. Available as capsules and tablets.
Fibric Acid Derivatives (Fibrates)
Considered third-line drugs for managing lipid disorders.
Primarily affects triglycerides (most effective drugs for this); also raises HDL.
Examples
- Gemifibrozil (Lopid), Fenofibrate (Tricor)
Gemifibrozil (Lopid)
Fibric acid derivative.
Used to treat high triglycerides.
Increases the synthesis of lipoprotein lipase which accelerates the clearance of very low density lipoproteins (VLDL) which ultimately lowers triglycerides.
Available in 600 mg tablets; usually give 30 minutes before AM and PM meals.
Adverse effects of Gemifibrozil (Lopid)
Gallstones
Myopathy
Liver disease
Prolonged prothrombin time (can lead to bleeding).
GI upset.
Interactions with Gemifibrozil (Lopid)
Warfarin
- gemifibrozil displaces warfarin from plasma albumin (thereby increasing anticoagulant effects); patients will be prone to bleeding.
Repaglinide (Prandin)
- hypoglycemia.
Sulfonylurea antidiabetic agents
- hypoglycemia.
Statins
- increase the chance of rhabdomyolysis.
Ezetimibe (Zetia)
Miscellaneous Antilipemic drug- Cholesterol absorption inhibitor.
Results in a reduction of cholesterol, lipoproteins, and triglycerides.
May be used alone or in combination with statins.
Used as an adjunct to dietary modifications.
Usual dose is 10 mg/day.
Adverse effects and drug interactions with Ezetimibe (Zetia)
Adverse effects
-
- usually well tolerated.
- some reports of myopathy, rhabdomyolysis, hepatitis, pancreatitis, and thrombocytopenia.
Drug interactions
-
- Fibrates: increases the risk of myopathy + gallstones.
- Bile acid sequestrants: absorption of ezetimibe is decreased when taken together.
- Cyclosporine: when taken together, level of ezetimibe is increased.
Combination products available
Lovastatin/Niacin (Advicor)
Simvastatin/Niacin (Simcor)
Simvastatin/Ezetimibe (Vytorin)
Pravastatin/Aspirin (Pravigard PAC)
Atorvastatin/Amlodipine (Caduet)
Simvastatin/Sitagliptin (Juvisync)
A nurse administering Niacin would implement which action to help to reduce adverse effects?
A. Give the medication with grapefruit juice.
B. Administer a small dose or aspirin or an NSAID 30 minutes before the Niacin dose.
C. Administer the medication on an empty stomach.
D. Have the patient increase dietary fiber intake.
B. Administer a small dose or aspirin or an NSAID 30 minutes before the Niacin dose.
When administering Niacin, the nurse needs to monitor for which adverse effect?
A. Cutaneous flushing
B. Muscle pain
C. Headache
D. Constipation
A. Cutaneous flushing
Which point will the nurse emphasize to a patient who is taking an Antilipemic medication in the "statin" class?
A. The drug needs to be taken on an empty stomach.
B. A low-fat diet is not necessary while taking these medications.
C. It is important to report muscle pain immediately.
D. Improved cholesterol levels will be evident within 2 weeks.
C. It is important to report muscle pain immediately.
A patient is being assessed before a newly ordered Antilipemic medication is given. Which condition would be a potential contraindication?
A. Diabetes insipidus
B. Pulmonary fibrosis
C. Liver cirrhosis
D. Myocardial infarction
C. Liver cirrhosis
A patient is currently taking a statin. The nurse considers that the patient may have a higher risk for developing rhabdomyolysis when also taking which product?
A. NSAIDs
B. A fibric acid derivative
C. Orange juice
D. Fat-soluble vitamins
B. A fibric acid derivative
The nurse is administering cholestyramine (Questran), a bile acid sequestrant. Which nursing intervention(s) is appropriate? (Select all that apply)
A. Administering the drug on an empty stomach.
B. Administering the drug with meals.
C. Instructing the patient to follow a low-fiber diet while taking this drug.
D. Instructing the patient to take a fiber supplement while taking this drug.
E. Increasing fluid intake.
F. Not administering this drug at the same time as other drugs.
B. Administering the drug with meals.
D. Instructing the patient to take a fiber supplement while taking this drug.
E. Increasing fluid intake.
F. Not administering this drug at the same time as other drugs.
A patient has been taking simvastatin (Zocor) for 6 months. Today he received a call that he needs to come to the office for a "laboratory check". The nurse expects which laboratory studies to be ordered at this time? (Select all that apply)
A. PT/INR
B. Total cholesterol
C. Triglyceride
D. Liver function studies
E. Complete blood count
F. HDL and LDL levels
B. Total cholesterol
C. Triglyceride
D. Liver function studies
F. HDL and LDL levels
Patients taking cholestyramine (Questran) may experience which adverse effects?
A. Blurred vision and photophobia
B. Drowsiness and difficult concentrating
C. Diarrhea and abdominal cramps
D. Belching and bloating
D. Belching and bloating
The nurse will instruct the patient taking antilipemic drugs about which dietary measures? (Select all that apply)
A. Taking supplements of fat-soluble vitamins
B. Taking supplements of B vitamins
C. Increasing fluid intake
D. Choosing foods that are lower in cholesterol and saturated fats
E. Increasing the intake of raw vegetables, fruit, and bran.
A. Taking supplements of fat-soluble vitamins
C. Increasing fluid intake
D. Choosing foods that are lower in cholesterol and saturated fats
E. Increasing the intake of raw vegetables, fruit, and bran.
In reviewing the history of a newly admitted cardiac patient, the nurse knows that the patient would have a contraindication to antilipemic therapy of which condition is present?
A. Liver disease
B. Renal disease
C. Coronary artery disease
D. Diabetes mellitus
A. Liver disease
A patient taking a statin calls the office to report an increase in muscle pain. Which information takes priority as the nurse communications with the patient?
A. This could be the sign of a serious side effect, stop taking the medication immediately.
B. You should take a dose of ibuprofen for the next few days.
C. This is an expected occurrence; continue the dose as prescribed.
D. Did you pull a muscle or injure yourself?
A. This could be the sign of a serious side effect, stop taking the medication immediately.
The nurse is preparing to administer a newly ordered statin drug to a patient and is reviewing the patient's list of current medications. Which medications may cause an interaction with the statin drug? (Select all that apply)
A. Warfarin (Coumadin)
B. Metformin (Glucophage)
C. Erythromycin (Erythrocin)
D. Cyclosporine (Gengraf)
E. Gemfibrozil (Lopid)
A. Warfarin (Coumadin)
C. Erythromycin (Erythrocin)
D. Cyclosporine (Gengraf)
E. Gemfibrozil (Lopid)
Nursing implications for certain HMG-CoA Reductase Inhibitors
Atorvastatin (Lipitor)
- better for renal patients.
Fluvastatin (Lescol)
- better for renal patients. Can decrease platelets and WBCs.
Pravastatin (Pravachol)
- fewer side effects. Can increase blood glucose levels.
Simvastatin (Zocor)
- can increase blood glucose levels.
Rosuvastatin (Crestor)
- biggest risk for rhabdomylosis (breakdown of muscle tissue): higher risk for myopathy for patients of Asian ancestry.
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