7. Anti-hyperlipidemics Flashcards
Hyperlipidemias have been classified into ___ major subtypes.
5
Coronary heart disease (CHD) causes ___ of all deaths in US
1/2
The incidence of CHD correlates with elevated levels of ________& _________ and low levels of ________ cholesterol
LDL cholesterol, triacylglycerols, HDL
T/F The most common types of hyperlipidemias involve elevated LDL (IIa) > VLDL (IV) or both LDL and VLDL (IIb)
False.
Other way around
T/F Risk factors for CHD include cigarette smoking, hypertension, obesity, diabetes, and family history
True
Anti-hyperlipidemic therapies aim to:
a. increase degradation
b. increase removal
c. decrease absorption
d. decrease carrier production
e. all of the above
e. all of the above
What is the therapeutic goals of anti-hyperlipidemics?
LDL and HDL about the same amount in our body
What are the anti-hyperlipidemic drug classes?
- HMG CoA Reductase Inhibitors (Statins)
- Fibrates
- Niacin
- Cholesterol Absorption Inhibitors
- Bile Acid Sequestrants
- Omega-3 Fatty Acids
What are the HMG CoA Reductase Inhibitors (Statins)?
1. Atorvastatin [Lipitor®] "MOST COMMON" 2, Rosuvastatin [Crestor®] 3. Simvastatin [Zocor®] 4. Pravastatin [Pravachol®] 5. Lovastatin [Mevacor®]
Which HMG CoA Reductase Inhibitors (Statins) has the highest percentage on Serum LDL chlesterol reduction produced?
Atorvastatin (50%) and Rosuvastin (50%)
Which HMG CoA Reductase Inhibitors (Statins) has the lowest percentage on Serum LDL chlesterol reduction produced?
Fluvastatin (24%)
Which HMG CoA Reductase Inhibitors (Statins) has the highest percentage on Serum triacylglycerol reduction produced?
Atorvastatin (29%)
Which HMG CoA Reductase Inhibitors (Statins) has the lowest percentage on Serum triacylglycerol reduction produced?
Fluvastatin (10%)
Which HMG CoA Reductase Inhibitors (Statins) has the highest percentage on Serum HDL cholesterol increase produced?
Pravastatin (12%) and Simvastatin (12%)
Which HMG CoA Reductase Inhibitors (Statins) has the lowest percentage on Serum HDL cholesterol increase produced?
Atorvastatin (6%)
Which HMG CoA Reductase Inhibitors (Statins) has the longest Plasma half-life (hr)?
Rosuvastatin (19hrs)
Which HMG CoA Reductase Inhibitors (Statins) has the shortest Plasma half-life (hr)?
Fluvastatin, Pravastatin and Simvastatin
“all have 1-2 hrs half-life”
Which HMG CoA Reductase Inhibitors (Statins) can penetrate the central nervous system?
Lovastatin and Simvastatin
What is the indication for Atorvastatin?
Hyperlipidemia/CVD Prevention
The mechanism of action of Atorvastatin is competitively inhibits ________ which is responsible for an early, rate-limiting step in cholesterol biosynthesis.
It also increases hepatic ______receptors, enhancing catabolism.
HMG-CoA Reductase, LDL
What is the common adverse effect when taking Atorvastatin?
The 50% probability of cataract in statin users occurred at age 51.7 and 54.9 years in patients with type 2 diabetes and without diabetes, respectively, vs at age 55.1 and 57.3 years in non-statin users, respectively
Which Statin drugs cause the least significant side effects?
Simvastatin and Pravastatin
What is the drug interactions of Cyclosporin, Erythromycin, Azole antifungals in the presence of Atorvastatin?
Decrease metabolism —-> Myopathy exacerbation
What is the contraindications/cautions when taking Atorvastatin?
Azole antifungals
-Production of endogenous steroids, whose activities or levels may be reduced by ketoconazole may be further blunted at adrenal and gonadal levels by statins
What is Fibrates?
That’s a class of anti-hyperlipidemic drugs.
What are the Fibrates (anti-hyperlipidemic) drugs?
- Fenofibrate [Tricor®, Lofibra®, Triglide®] “MOST COMMON”
2. Gemfibrozil [Lopid®]
- The Mechanism of Action of Fenofibrate is to stimulates nuclear receptor ______ which modulates transcription of ______ genes in liver, muscle and adipose tissue
- It also enhances ______ production; inhibits ______ synthesis and stimulates catabolism of ______.
PPAR, insulin sensitive
HDL, triglyceride, triglyceride-rich lipoproteins
What is the drug interactions of Acyclovir, Aminoglycosdes, cyclosporine, and Ganciclovir with Fenofibrate?
Impaired renal elimination
Fenofibrate impaired metabolism of ________.
Sulfonylureas
What is Niacin?
It’s one of the anti-hyperlipidemic drug classes.
What are the Niacin drugs?
Nicotinic Acid [Vitamin B3, Niacin, Niaspan®, Slo-Niacin®]
What is the drug indication of Niacin?
Hypertriglyceridemia, Hypercholesterolemia and Mixed Dyslipidemia
Dosing [50-1000mg]
- 1500-3000mg/d
The mechanism of action of Niacin is to Inhibits _____ in adipose tissue, resulting in reduced hepatic _____ synthesis and production of _____ in the plasma.
lipolysis, VLDL, LDLs
Niacin induces prostaglandin D2 production which causes..
vasodilation (flushing) and hypothetically Mueller cell toxicity
Ocular effects self-resolve in about ___ wks following discontinuation of therapy.
2
What is the drug interactions of Alpha-blockers and beta-blockers in the presence of Niacin?
Additive
What do you have to be cautious about when taking Niacin?
Diabetes because it elevates blood sugar
Surgery because it has anti-platelet effects
