Drugs that work against high levels of lipids (fats) in the blood.
bile acid sequestrants
Cholesterol-lowering drugs that bind with cholesterol-containing bile acids in the intestines and remove them via bowel movements.
A fatty, waxy material that our bodies need to function. It is present in cell membranes everywhere in the body.
used to produce hormones, vitamin D, and bile acids that help digest fat
cholesterol absorption inhibitors
Cholesterol-lowering drugs that prevent the uptake of cholesterol from the small intestine into the circulatory system.
High blood fat levels that are related to genetic or inherited factors.
Lipid-lowering drugs that are used primarily to lower triglycerides and, to a lesser extent, LDL (“bad”) cholesterol.
high-density lipoprotein (HDL)
The “good” cholesterol that exists in the body.
High levels of blood fats (plasma lipoproteins).
High levels of triglycerides in the blood.
low-density lipoprotein (LDL)
The “bad” cholesterol that exists in the body.
Special type of vitamin B that helps to decrease blood cholesterol levels.
A condition in which skeletal muscle cells break down, releasing myoglobin. Risks with this condition include muscle breakdown and kidney failure because myoglobin is toxic to the kidneys.
A class of drugs used to lower LDL (“bad”) cholesterol and triglycerides by inhibiting their production by the body.
The chemical form of most fats in foods and the human body.
Chronic hyperlipidemia can lead to:
Coronary artery disease (angina, heart attack).
Peripheral vascular disease, which leads to organ damage or impairment.
Xanthomas (skin atheromas—abnormal fat deposits).
Partial blockage of the coronary arteries manifests as:
Complete blockage: MI
When are antihyperlipidemics prescribed?
fail to decrease lipids with lifestyle changes such as reduced-fat diets, increased exercise, smoking cessation, and weight loss; esp with HTN, diabetes, CAD, stroke.
Before giving hyperlipidemics, you should:
- Get current meds - Preggers/planning? - Ck hx for liver or muscle probs - Draw blood lipid/liver function panel before admin first dose - Ck labs
Can a pt eat or drink before lipid panels are drawn?
Not for eight hours. Must be drawn every 3-6 mos to check for drug
After giving a antihyperlipidemic, you should:
- Ask pt about muscle soreness, pain, weakness - Ck for s/s liver dmg: jaundice, dark urine, light-colored stools - Ck liver function panel. Alert doc with abnormal results - Females tell doc if preggers/suspect
What are the five classes of antihyperlipidemics?
HMG CoA reductase inhibitors "Statins" bile acid sequestrants cholesterol absorption inhibitors fibrates nicotinic acid
What is the normal adult dosage for the statin atorvastatin (Lipitor) ?
Adults: 10-80 mg/oral daily
What is the normal adult dosage for the statin simvastatin (Zocor) ?
Adult: 5-80 mg/oral daily in evening
Zocor vs Cozaar
Zocor is a lipid-lowering statin, whereas Cozaar is a blood pressure– lowering angiotensin II receptor antagonist
What is the purpose of antihyperlipidemics?
•Total cholesterol is decreased.
•Triglycerides are decreased.
•LDL is decreased.
Statin side effects:
Upset stomach, gas, constipation, abdominal pain, and cramps may occur. These symptoms are usually mild and disappear as the body adjusts to the drug
Statin adverse effects:
s/s of rhabdomyolysis:
general muscle soreness, muscle pain and weakness, vomiting, stomach pain, and brown urine. The urine turns brown because small reddish-brown pieces of broken-down muscle are removed from the body through the urine
s/s of early liver dmg:
s/s of late liver dmg:
yellowing(jaundice)of the skin, whites of the eyes, and roof of the mouth; pain over the liver on the right side just below the ribs; darkened urine; and pale gray-colored stools. The bile and bilirubin made by the liver normally leave the body in the stool, giving stool a medium-to–dark brown color
BEFORE giving statins, you should:
- Ck kidney function test (rhabdo precursor) - Ask about alcohol consumption (do not prescribe to pts who have more than 2 drinks/day b/c liver stress)
AFTER giving statins, you should:
- monitor for DEC liver function - monitor for muscle breakdown/rhabdo
What do you teach pts about taking statins?
- Some are taken 2xs/day - Some are only taken in the evening
How do children rx to statins?
use in children is rare not recommended in children younger than 8 yo
How do preggers/breastfeeding rx to statins?
Class X Fat is essential to brain development in the fetus and infant. When there is not enough fat in the body during pregnancy and infancy, the fetus can suffer poor brain development and mental retardation.
How do elderly rx to statins?
- Ck hx of muscle/liver disease - Remind to tell doc about soreness & muscle problems
What is the purpose of bile acid sequestrants?
•LDL cholesterol level is decreased.
•HDL cholesterol level is increased.
Side effects of bile acid sequestrants
gastrointestinal symptoms, including constipation, bloating, nausea, vomiting, and gas
Adverse effects of bile acid sequestrants
- decrease the ability of the body to absorb oral drugs - inhibit fat-soluble vitamins (A, D, E, and K), so patients may need to take a daily vitamin supplement - may change the action of the anticoagulant warfarin (Coumadin) - Ck INR
How do bile acid sequesterants interact with warfarin?
Two ways: - DEC the absorption of vitamin K, which would intensify the effects of warfarin and increase the risk of bleeding - Can also directly bind warfarin in the intestinal tract and cause its rapid elimination. This action inactivates the activity of warfarin and increases the risk of clot formation
What should you do BEFORE giving a bile acid sequesterant?
- do NOT give within 2 hrs of giving other oral mes; can inhibit absorption - ask if pt is constipated; common side effect
What should you do AFTER giving a bile acid sequesterant?
- Ck GI symptoms: N&V, constipation, bloating, gas - Pt on warfarin: s/s bleeding & INR - Monitor constipation
What do you teach a pt about bile acid sequesterants?
- Take with meals - Do not take other drugs q2hr before; 4-6 hrs after - Mix powders with 4-6 oz of fruit juice/water - Tablets should be taken with a lot of water to prevent GI symptoms - s/s of bowel obstruction - Take q2hr before/after antacids
s/s of bowl obstruction
abdominal pain, bloating, vomiting, and diarrhea or constipation
How do children rx to bile acid sequestrants?
Cholestyramine (Questran) and colestipol (Colestid) should be avoided in children because they can cause intestinal obstructions.
Safe use of colesevelam (Welchol) has not been established in children
How do preggers/breastfeeding rx to bile acid sequestrants?
Class C: cholestryramine, colesevelam Class B: colestipol Unsure: colesevelam
Controversial b/c fetus needs constant level of cholesterol for brain developmen
When are cholesterol absorption inhibitors normally prescribed?
When low-fat, low cholesterol diet does not work Pts who can not take statins
What is the normal adult dosage for the cholesterol absorption inhibitor ezetimibe (Zetia)?
10 mg/oral daily
What is the purpose of cholesterol absorption inhibitors?
•Level of LDL cholesterol is decreased.
•Level of total cholesterol is decreased.
Side effects of cholesterol absorption inhibitors
GI: stomach pain and diarrhea fatigue, back pain, joint pain, rash, and sinusitis Less common side effects include cough, sore throat, and viral infections. When combined with a statin: c/p, dizziness, headache, muscle pain, and URI
What potentiates Zetia?
Fenofibrate (Tricor), gemfibrozil (Lopid), and cyclosporine
muscle problems such as pain, aches, tenderness, or weakness
Adverse effects of cholesterol absorption inhibitors
swelling beneath the skin, usually around the eyes, nose, and lips, caused by blood vessel dilation
What should you do before giving a cholesterol absorption inhibitor?
- Ask if the pt has a hx of liver disease or muscle disorders - Ck to see if liver function test worsen
What should you do AFTER giving a cholesterol absorption inhibitor?
- Ck pt for DEC liver function (DEC appetite, fatigue, jaundice) - Monitor muscle aches/pains - Monitor fatigue/abdom pains - Monitor for facial swelling (angioedema)
What do you teach pts about cholesterol absorption inhibitors?
- Report muscle pain, tenderness, weakness - Take med @ same time every day - It can be taken at the same time as a statin drug but should be given at least 2 hours before or 4 hours after bile acid sequestrants - Go to ER if swelling of tongue/face/dysphagia/dyspena
How do children rx to cholesterol absorption inhibitors?
Safety unsure under the age of 10 yo.
How do preggers/breastfeeding rx to cholesterol absorption inhibitors?
Class C safe use of this drug during pregnancy has not been established. During breastfeeding, this drug should only be used if the benefits outweigh possible risks
The main effects of fibrates are to
decrease blood triglyceride levels and cause a mild increase in HDL (or “good” cholesterol).
Side effects of fibrates:
stomach upset and diarrhea GI:indigestion or heartburn (dyspepsia) and nausea Pts may also experience muscle weakness, headache, pruritus, and rash
Adverse effects of fibrates:
- pt with kidney disease: fibrates may INC creatinine levels. - Fibrates increase cholesterol loss in bile, which may lead to the development of cholesterol-based gallstones. - Bleeding can also occur in the patient taking fibrates.
What fibrate potentiates statins?
Gemfibrozil (Lopid) interferes with the breakdown of statin drugs, causing higher levels of statins in the blood. This can lead to statin side effects such as muscle damage, muscle weakness, rhabdomyolysis, or liver damage
What should you do before giving fibrates?
- Monitor pt for kidney/liver/gallbladder disease (changes in urine output, decreased appetite, fatigue, weakness, nausea, and vomiting) - Pts on warfarin: monitor for bleeding - Ck liver/kidney function labs
What should you teach a pt about taking fibrates?
- Take 30 min before meals - Given before morning & evening meals - Avoid 2+ alcoholic drinks day - Do not drink grapefruit juice with fibrates - Pts on warfarin: s/s of bleeding
How do preggers/breastfeeding rx to fibrates?
Class C Fibrates can cross the placenta and affect fetal brain development. Affects not well studied.
How do elderly rx to fibrates?
- INR test weekly - More likely to be on warfarin; higher bleeding risk
Nicotinic acid is given in doses:
much higher than the normal daily requirement.
What is the purpose of nicotinic acid?
•Total cholesterol level is decreased.
•Total triglyceride level is decreased.
•LDL cholesterol level is decreased.
•HDL cholesterol level is increased.
Side effects of nicotinic acid?
itching and nasal inflammation because the drug makes blood vessels dilate GI: N&V, indigestion, gas, abdom pain Flushing Hot flashes Chills Headaches Tachycardia Dyspnea Syncope Diaphoresis Fluid retention edema
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