Drugs for Dyslipidemia (Part 02) Flashcards
Example of Drug/s that can cause Mild to Moderate Degrees of Dyslipidemia
- Beta Blockers
- Thiazide Diuretics
- Antiretroviral Drugs
- Hormonal Agents
Pharmacologic Intervention of Dyslipidemia
- HMG-CoA Reductase Inhibitors
- Bile Acid Sequestrants
- Nicotinic Acid
- Fibric Acid Derivatives
5.A. Cholesterol Absorption Inhibitors
5.B. Lipid-Regulating Agent
Drug/s under HMG-CoA Reductase Inhibitors
• Statins
– Rosuvastatin (Crestor)
– Atorvastatin (Lipitor)
– Simvastatin (Zocor)
– Lovastatin (Mevacor)
– Pravastatin (Pravachol)
– Fluvastatin (Lescol)
Act by inhibiting the enzyme HMG-CoA reductase, the enzyme controlling the first committed step of cholesterol synthesis in the liver.
Statins
Most potent cholesterol and LDL lowering drug.
Statins
Usually administered in the evening because most hepatic cholesterol production occurs during the night.
Statins
__________ (14 hours) and __________ (19 hours) may be given any time of the day because of its longer half-life.
Atorvastatin and Rosuvastatin
A/E of Statins
- Hepatotoxicity
- Myositis and Rhabdomyolysis
- GI Symptoms
- Teratogenic
(T/F): If Statins combined with Gemfibrozil—increases the risk of Rhabdomyolysis.
T
__________ and __________ may prolong bleeding time with Warfarin.
Lovastatin and Rosuvastatin
Drug/s under Bile Acid Sequestrants
• Resins
– Cholestyramine
– Colestipol (Colestid)
– Colesevelam (WelChol)
They bind bile acids in the intestine through anion exchange; this reduces the enterohepatic recirculation of bile acids, which releases feedback regulation on conversion of cholesterol of bile acids in the liver.
Resins
Only useful for isolated increase in LDL.
Resins
Powder Old Resins
• Cholestyramine
• Colestipol
A/E of Resins
- Constipation
- Bloating
- Epigastric Fullness
- Nausea
- Flatulence
Drug/s under Nicotinic Acid / Vitamin B3
Niacin
Inhibit the mobilization of free fatty acids from peripheral adipose tissue to the liver which reduces synthesis and secretion of VLDL particles by the liver.
Niacin
The strongest in increasing HDL and useful in Hypertriglyceredemia.
Niacin
(T/F): Niacin functions after conversion to Nicotinamide Adenine Dinucleotide (NAD) in the NAD Co-Enzyme System.
T
It is extended release formula better than other forms due to less side effects.
Niaspan
A/E of Niacin
- Flushing and Headache
- Increasing Blood Glucose
- Hyperuricemia
- Hepatotoxicity
Drug/s under Fibric Acid Derivatives
• Fibrates
– Gemfibrozil (Lopid)
– Fenofibrate (Tricor)
Increases activity of Peroxisome Proliferator-Activated Receptor-Alpha, this increases synthesis of lipoprotein lipase, therefore, increasing clearance of triglycerides.
Fibrates
Stimulate supply fatty acid oxydation, which limits the supply of triglycerides and decreases VLDL synthesis.
Liver
Agent of Choice in Hypertriglyceridemia
Fibrates
Drug/s under Cholesterol Absorption Inhibitor
Ezetimibe (Zetia)
A prodrug that is converted in the liver to the active glucuronide form. Monotherapy or in combination with statin. Not recommended with fibrates. Reduces LDL number. It is also used in phytosterolemia—this is rare genetic disorder that results from impaired export of phytosterols.
Ezetimibe (Zetia)
A/E of Ezetimibe (Zetia)
- Diarrhea
- Cough and Fatigue
Drug/s under Lipid Regulating Agent
Omega 3
Decreases hepatic production of TG and VLDL.
Omega 3
Omega 3 Fatty Acids
• Alpha-Linolenic Acid (ALA)
• Eicosapentaenoic Acid (EPA)
• Docosahexaenoic Acid (DHA)
Drug/s under Investigation
Newer Agents
Drug/s of Newer Agents
• Cholesteryl Ester Transferring Protein
– Torcetrapib
– Anacetrapib
A unique, patented blend of plant sterols and stanols that is extracted from coniferous (pine) trees.
Reducol®
Blocks the absorption of cholesterol in the gut without being absorbed into the body.
Reducol®
