Hyperlipidemia Drugs

Question 1

reversible competitive inhibitor of HMG-COA reductase
inhibits rate-limiting enzyme in cholesterol biosynthesis
increased hepatic cholesterol uptake
increased high affinity LDL receptors
decreased LDL levels
modest reduction in triglycerides
used for HIGH LDL/HYPERCHOLESTEROLEMIA, ACS, ischemic stroke
side effects: HEPATOTOXICITY, MYOPATHY, rhabdomyoliysis –> AKI

Answer 1

SIMVASTATIN (shortest half life; stabilises cholesterol plaque)
atorvastatin, rosuvastatin, fluvastatin, pravastatin, lovastatin, pitavastatin

Question 2

statins have an increased risk of myopathy and rhabdomyolysis when used with… ?

Answer 2

fibrates

Question 3

why are statins used in the management of CAD?

Answer 3

for stabilisation of atherosclerotic plaques

Question 4

bile acid-binding resin
prevents reabsorption of bile acid and increasing cholesterol utilisation for replacement
upregulates LDL receptors
modestly lowers LDL levels
used for HIGH LDL/HYPERCHOLESTEROLEMIA, PRURITUS IN CHOLESTASIS, DIGITALIS TOXICITY
side effects: CONSTIPATION, BLOATING, STEATORRHEA, malabsorption

Answer 4

cholestyramine
colesevelam, colestipol

increases TGs and VLDL in patients with high TGs
AVOID in patients with diverticulitis

Question 5

sterol absorption blocker
selective inhibition of NPC1L1 transporter
decreasing intestinal absorption of cholesterol and other phytosterols
decreases LDL and phytosterols
used for HYPERCHOLESTEROLEMIA/HIGH LDL
side effects: HEPATOTOXICITY
synergistic LDL-lowering effect with statins

Answer 5

Ezetimibe

Question 6

sterol absorption blocker
cholesterol analog, takes place of dietary and biliary cholesterol, decreasing intestinal absorption of cholesterol and other phytosterolemia
does NOT deposit in blood vessel
plant derivative
side effect: GI upset, bloating, impotence (rare), coronary events

Answer 6

sitosterol

Question 7

inhibits lipolysis by hormone sensitive lipase
reduces VLDL synthesis and secretion in liver
reduces hormone-sensitive lipase activity, decreases plasma fatty acid and triglyceride levels in adipose tissue
reduces catabolic rate for HDL
increased clearance
decreases circulating fibrinogen, increases tPA activity
MOST EFFECTIVE AGENT FOR INCREASING HDL LEVELS
decreases catabolism of apoAI
increases HDL cholesterol
used for LOW HDL, HIGH LDL/VLDL
side effects: FLUSHING, HYPERURICEMIA, IMPAIRED GLUCOSE TOLERANCE

Answer 7

Niacin (vitamin B3)

aspirin pre-treatment reduces flushing
AVOID in patients with peptic ulcer disease
potentiates effect of antihypertensives

Question 8

drugs that cause flushing

Answer 8

VANC

vancomycin
adenosine
niacin
CCB

Question 9

fibric acid derivative
activates PPAR-alpha protein and increases expression of lioprotein lipase and apolipoproteins
lowers triglycerides
decreases secretion of VLDL
increases HDL
DOC FOR HYPERTRIGLYCERIDEMIA (low HDL, high LDL)
side effect: INCREASED RISK FOR CHOLESTEROL GALLSTONES
INCREASED RISK OF MYOPATHY AND RHABDOMYOLYSIS WHEN USED WITH STATINS

Answer 9

gemfibrozil
fenofibrate, bezafibrate

FIBRATES UPREGULAT LIPOPROTEIN LIPASE = FULL

Question 10

disadvantageous hyperlipidemic combinations

Answer 10

fibrate + resin = increased risk of cholelithasis
statin + resin = impaired statin absorption
statin + fibrate = increased risk of myopathy and rhabdomyolysis

Question 11

synergistic antihypertensive combinations

Answer 11

niacin + statin/statin + ezetimibe = familial hypercholesterolemia
niacin + resin/statin + fibrate = familial combined hypercholesterolemia