Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
35 Cards in this Set
- Front
- Back
Chylomicrons
|
largest lipoproteins and have the lowest density
|
|
VLDL
|
endogenous triglycerides (are bad); catabolized by LPL, and have a short half-life
|
|
IDL
|
cholesteryl esters, converted to LDL by hepatic lipase
|
|
LDL
|
apoB-mediated uptake by LDL receptor, and have a long half-life
**Bad Cholesterol** ** > 190 is high ** |
|
HDL
|
phospholipids cholesteryl esters, removed by hepatic scavenger receptor B secreted to bile, steroid synthesis, VLDL synthesis
**Good Cholesterol** ** < 40 is low ** |
|
Hypertriglyceridemia (VLDL)
|
Diabetes, oral contraceptives (estrogen- which act to decrease LDL levels in the plasma), hypothyroidism, hypopituitarism, high sugar diet, and high alcohol intake (increased production and decreased clearance of VLDL)
|
|
Hypercholesterolemia (LDL)
|
High cholesterol (fat) diet, hypopituitarism, and hypothyroidism (decreased LDL receptors)
|
|
Classification of Lipoprotein Analysis Results (mg/dl)
|
Total Cholesterol: >240 is high
LDL Cholesterol ("bad"): >190 is high HDL Cholesterol ("good"): <40 is low Triglycerides: >500 is high |
|
Statins: Mechanism of Action
|
Competition with HMG-CoA to prevent mevalonate synthesis, resulting in decrease of cholesterol synthesis and upregulation of LDL receptors
|
|
Common Statins
|
Lovastatin (Mevacor)
Simvastatin (Zocor) Pravastatin (Pravachol) Atorvastatin (Lipitor) Rosuvastatin (Crestor) |
|
Long-Lasting Statins
|
Atorvastatin and Rosuvastatin
Given as a single daily dose |
|
Short-Lived Statins
|
Lovastatin, Simvastatin, Pravastatin
Given in multiple doses daily |
|
Statins: Side Effects
|
Myopathies- major side effect; characterized by intense myalgia which progresses with the use of statin
Hepatotoxicity (take extra care of pts. with heavy drinking history) Pregnancy Children |
|
What Statins can be administered to children 11 and older?
|
Atorvastatin, Lovastatin, and Simvastatin
|
|
What Statins can be administered to children 8 or older?
|
Provastatin
|
|
Niacin (Nicotinic Acid)
|
- Water soluble B vitamin complex
- The lipid lowering effect requires higher concentration than the vitamin effect - Best agent available to increase HDL levels (30-40%) - Decrease triglyceride levels (35-45%) - Reduce the LDL levels (20-30%) -Prescribed to a pt. with low HDL levels |
|
Niacin (Nicotinic Acid): Mechanism of Action
|
Reduces triglyceride levels in the liver by inhibiting synthesis and esterification of free fatty acids; reduction in the free fatty acid levels leads to decrease in VLDL production and LDL levels
|
|
Crystalline Niacin: Administration
|
Immediate release
Available OTC Best tolerated when starting with low doses (100mg twice daily) and increasing stepwise to 1.5-2g/daily |
|
Sustained Release Niacin: Adminstration
|
Allows continuous release of the drug for 6-8 hours after ingestion (it is claimed to have less side effects)
|
|
Extended-Release Niacin: Administration
|
Requires a prescription and is less hepatotoxic
|
|
Niacin Absorption
|
Peak plasma concentration occurs 30-60 minutes after administration for the regular niacin
Sustained-release niacin was developed to lessen the side effects |
|
Niacin: Side Effects
|
Digestive Tract: dyspesia (heart burn)--which is accentuated by coffee, tea, or alcohol; Should be avoided in pts. with a peptic ulcer
Cutaneous Effects: flushing and pruritus (itchy skin)--can be prevented by aspirin Pregnancy: birth defects Hepatotoxicity: elevated transaminases; has toxic effects to the liver Hyperglycemia: limits niacin use in diabetic pts.; elevates uric acid levels and may reactivate gout |
|
Bile-acid Sequestrants (Resins): Mechanism of Action
|
The oldest and safest lipid lowering agents.
Mech. of Action: Enhance bile acid synthesis; deplete hepatic cholesterol content; upregulate LDL receptors, but increase triglyceride synthesis |
|
Bile-acid Sequestrants (Resins): Side Effects and Administration
|
Side Effects: bind directly and may interfere with absorption of many drugs, including statins
Administration: - recommend administration of other drugs 1 hr. before or 3-4 hrs. after Resin dose - recommended for pts. 11-20 yo and taken before eating - administered as bulk (4-5g/dose) |
|
Fibric Acid Derivatives
|
Mechanism of Action: bind to peroxisome proliferator activated receptors (PPAR) and stimulate beta-oxidation of fatty acids (prevents FA from being incorporated in VLDL and LDL levels); strongest agent to decrease triglyceride levels
Administration: - Clofibrate: 2g/day - Gemofibrozil: 600mg/twice daily - Fenofibrate: 145 or 200 mg/day |
|
Fibric Acid Derivative Recommendations
|
Pts. with type III hyperlipoproteinemia, severe hypertriglyceridemia (>1000mg/day), type II diabetes or metabolic syndrome
* Should not be used by children or pregnant women |
|
Fibric Acid Derivatives: Beneficial Effects
|
Lipid lowering activity
Antithrombotic Immunomodulation Antiinflammatory Actions |
|
Ezetimibe: Inhibition of Dietary Cholesterol Uptake: Mechanism of Action
|
Specifically blocks the function of Niemann-Pick C1-like 1 (NPC1L1) protein, a newly identified sterol influx transporter, facilitating cholesterol absorption
The compensatory increase in endogenous cholesterol synthesis is prevented by use of statins |
|
Ezetimibe: Inhibition of Dietary Cholesterol Uptake: Side Effects
|
Increase in cancer incidence in pts. treated with Vytorin
Fetal abnormalities, so DO NOT give to pregnant women |
|
Ezetimibe: Inhibition of Dietary Cholesterol Uptake: Administration
|
20 mg/daily- reduce LDL levels by 15-20%; recommended as a combinatorial therapy with Statins (Vytorin--no side effects)
Bile-acid sequestrants inhibit Ezetimibe absorption and should not be combined |
|
Combination Therapy: Statins + Niacin
|
Enhances effects of statins but also increases risk of myopathies
**Good Combo.** |
|
Combination Therapy: Statins + Bile-acid Sequestrants
|
Enhances effects of statins on LDL-C levels by 20-30%
|
|
Triple Combinatory Therapy: Statins, Resins, Niacin
|
Reduce LDL-C up to 70%
**Most Effective Combo.** - but side effects are unbearable |
|
Vytorin: Combination of Simvastatin and Ezetimibe
|
Decrease LDL-C levels by 60% after 24 weeks
|
|
Summary of the Lipid Lowering Agents
|
Statins: Big Decrease in LDL, Increase HDL, Decrease Triglyceride; liver toxicity, myopathies, pregnancy
Niacin (Nicotinic Acid): Decrease LDL, Increase HDL, Decrease TG; rash, ulcer, gout, diabetes, liver toxicity Bile-acid Sequestrants (Resins): Decrease LDL, Increase HDL; constipation, GI discomfort Fibric Acid Derivatives: Decrease LDL, Increase HDL, Big Decrease in TG; nausea, headache Inhibitors of Cholesterol Absorption (Ezetimibe): Decrease LDL, Decrease HDL; pregnancy, resins inhibits absorption, may be not as safe as previously considered |