Hypolipidemics Flashcards
Niacin
Class
Nicotinic Acid
Niacin
MOA
Reduction of liver triglyceride synthesis –> less hepatic VLDL (thus, LDL) production; Dec lipolysis in adipose tissue –> dec FFA transport to liver (thus, less trigs); Dec hepatic clearance of ApoAl (raising HDL)
Niacin
Uses
Best agent to Inc HDL (30-40%);
As good as fibrates and statins at lowering Trigs (35-45%); Lowers LDL (20-30%);
Hypertriglyceridemia & low HDL
Niacin
Impt SE
Flushing
Pruritis of face/upper trunk
Rases
Acanthosis Nigricans (hyperpigmentation)
Niacin
Other SE
Hepatotoxicity Hyperuricemia Hyperglycemia Dyspepsia/Reactivation of PUD Toxic ambylopia (rare) Tachyarrhythmias (afib in elderly) Myopathy
Niacin
Misc
Water sol B vit complex at [low]; Hypolipidemic at [high];
SE limit compliance (<50%)
Prevent flushing/pruritis with ASA
Niacin
Contraindications
DM
Gout
Name the two Fibric Acid Derivatives (GF)
Gemfibrozil
Fenofibrate
Gemfibrozil & Fenofibrate
Class
Fibric Acid Derivatives
Fibrates
Gemfibrozil & Fenofibrate
MOA
Unknown; may interact with peroxisome proliferator-activated receptor (PPAR-alpha) to stimulate LPL synthesis –> enhance TG-rich lipoprotein clearance; Inhibits apoC-III expression –> inc VLDL clearance; Stimulation of apoA-I and apoA-II –> inc HDL
Gemfibrozil & Fenofibrate
Uses
Severe Hypertriglyceridemia;
Marked reduction in VLDL (thus, Trigs);
Variable and small effect on LDL;
Small inc in HDL (10%)
Gemfibrozil & Fenofibrate
Impt SE
Potentiates oral anticoagulants (displace from albumin);
Increase Bile Lithogenicity;
Myositis Flu-like syndrome (5% of pts)
Gemfibrozil & Fenofibrate
Misc
Inadvisible to give with a statin due to higher myositis risk
Name the 3 Bile Acid Sequestrants (CCC)
Colestipol
Cholestyramine
Colesevelam
Bile Acid Sequestrants
MOA
(Colestipol, Colestyramine, Colesevelam)
Very positively charged resins bind negatively charged bile acids –> inhibit their reabsorption and inc cholesterol loss;
Leads to increase in LDL receptors in liver, thus dec LDL in blood
Bile Acid Sequestrants
Uses
(Colestipol, Colestyramine, Colesevelam)
Decrease LDL (25%); Slight inc (5%) in TG and HDL
Bile Acid Sequestrants
Impt SE
(Colestipol, Colestyramine, Colesevelam)
Very safe;
Only hypolipidemic indicated for children bc not systemically absorbed;
Impairs fat sol vit absorption;
Binds other drugs (cardiac glycosides, coumarins)
Bile Acid Sequestrants
Other SE
(Colestipol, Colestyramine, Colesevelam)
Bloating
Dyspepsia
Constipation
Gritty/Bad taste
Bile Acid Sequestrants
Misc
(Colestipol, Colestyramine, Colesevelam)
Standard Tx in combo with statins;
Contraindicated in hypertriglyceridemia
STATINS
- Loyal
- Sexual
- Partners
- Fear
- Adorable
- Rabbit
- Pitas
Lovastatin Simvastatin Pravastatin Fluvastatin Atorvastatin Rosuvastatin Pitavastatin
Statins - Class
Lovastatin, Simvastatin, Pravastatin, Fluvastatin, Atorvastatin, Rosuvastatin, Pitavastatin
HMG-CoA Reductase Inhibitors
Statins - MOA
Lo-, Sim-, Pra-, Flu-, Ator-, Rosu-, Pita-
Inhibits HMG-CoA reductase formation of mevalonate –> activation of SREBP (membrane bound transcription factor that increases LDL-R synthesis and lessens degradation); Reduction in cholesterol dec VLDL syn –> Lowering TG
Statins - Uses
Lo-, Sim-, Pra-, Flu-, Ator-, Rosu-, Pita-
Reduce LDL (20-55%) Reduce TG (25%) Increase HDL (5-10%) Dyslipidemia (dec fatal/non-fatal CHD/strokes; total 20% mortality dec)
Statins - Impt SE
Lo-, Sim-, Pra-, Flu-, Ator-, Rosu-, Pita-
Very few
Hepatic Dysfunction in 1%
Myopathy/Rhabdo (reduced if factors inhibiting statin catabolism lacking)
