Antihyperlipidemics Flashcards
what are the two major lipids?
cholesterol and triglyceride
what do lipoproteins do?
transport cholesterol and triglycerides in blood
chylomicrons are made of mostly ____
triglycerides
VLDLs are made of mostly ___
triglycerides
LDLs are made of mostly ____
cholesterol
HDLs are made of mostly ___
proteins
Apo A-1
in HDL, reverse cholesterol transport
Apo B-100
in VLDL, IDL, LDL - is LDL receptor ligand and bad
Apo B-48
in chylomicrons - produced in intestine
Apo E
reverse cholesterol transport with HDL
Apo CII
in chylomicrons and VLDL
binds LPL to enhance TG lipolysis
LPL does what
breaks VLDL to LDL
HL does what
IDL to LDL
cholesterol synthesis pathway
acetoacetyl coa - HMG Coa - mevalonate - cholesterol
what ratio is key in assessing risk of CVD
total cholesterol to HDL
greater than 4.5 is increased risk CVD
hyperlipoproteinemia diseases
atherosclerosis, premature CAD, stroke
hypertriglyceridemia diseases
pancreatitis, xanthomas, CHD
MOA of bile acid resins
inhibit reabsorption of bile acids from intestine , up regulate LDL receptors in liver
bile acid resins side effects
constipation and bloating
bile acid resins drug interactions
acetaminophen, thiazides, ezetimibe, oral contraceptives, warfarin, digoxin, fibrates, TZDs, steroids
ezetimibe mechanism of action
inhibits cholesterol absorption from diet, inhibits NPC1L1
ezetimibe adverse effects
well tolerated, low incidence of muscle pain
statin mechanism of action
competitively inhibit HMG-CoA reductase the rate limiting step in cholesterol biosynthesis, upregulate LDL receptors so more hepatic uptake of LDL
HMG-CoA reductase inhibitors indications
hypercholesterolemia and after MI
prodrug statins
lovastatin and simvastatin
statin CYP 3A4 substrates
lovastatin, simvastatin, atorvastatin
statin CYP 2C9 substrates
fluvastatin, rosuvastatin
statin sulfation metabolism
pravastatin
pitavastatin undergoes ____
enterohepatic recirculation
statin adverse effects
skeletal muscle effects, rhabdomyolysis, hepatotoxicity, increased incidence of type 2 diabetes
bempedoic acid is used for ___
adjunct to statins, heterozygous familial, ASCVD
bempedopic acid side effect
gout
PCSCK9 MOA
inhibits degradation of PCSK9 receptors in liver
increase LDL-R and reduce LDL levels
PCSK9 inhibitors directions
injection subq every 2 weeks
inclisiran MOA
hybridizes PCSK9 mRNA and directs degradation
incliserin used for
adjunct to statins in HeFH and ASCVD
Apo B lipoprotien inhibitors use
homozygous familial
apo B lipoprotein inhibitors drugs
lomitapide, mipomersen, evinacumab
lomitapide MOA
inhibits assembly apo B by inhibiting MTTP, interferes with chylomicron and VLDL making
lopitamide indication and warning
homozygous familial
liver damage risk - Rx program
does lopitamide MOA require LDL-R
no
mipomersen MOA
anti-sense oligonucleotide inhibitor of apo B100
mipomersen indication and warning
homozygous familial
liver damage (hepatic steatosis)
evinacumab indication and MOA
homozygous familial
increases LPL
does evinacumab require LDL-R
no
fibric acid MOA
PPAR-alpha activators
must undergo activation
reduce serum triglycerides
fibric acid side effects
skeletal muscle / rhabdo - caution with statins
fibric acid drug interaction
warfarin, increase effects
niacin mechanism
reduce serum triglycerides, increase HDL
niacin targets and actions
decrease fatty acid transport to liver
decrease triglyceride export via VLDL
increase HDL and reverse transport
decrease cholesterol via HDL transport
niacin use
raising HDL
niacin adverse effects
prostaglandin mediated vasodilation and flushing/itching
treat with ibuprofen or aspirin
omega 3 indications
TGs over 500
adverse effects omega 3
can increase LDL
Friedwald Equation
calculates LDL-c
LDL = TC - HDL - TG/5
high intensity statins
atorvastatin 40-80 mg
rosuvastatin 20-40 mg
low intensity statins
simvastatin 10 mg
pravastatin 10-20 mg
lovastatin 20 mg
fluvastatin 20-40 mg
hydrophilic statins
rosuvastatin and pravastatin
simvastatin contraindications
-onazole, -omycin, gemfibrozil, danazol
do not exceed 10mg simvastatin
verapamil
diltiazem
do not exceed 20mg simvastatin
amiodarone
amlodipine
fibrates contraindications
hx gallbladder disease
dialysis
persistent liver disease
PCSK9 inhibitors adverse effects
influenza, injection site reaction