Lipid Lowering Drugs Flashcards
with cholesterol synthesis inhibitors, what is the target molecule, why
HMG CoA reductase
*rate limiting enzyme of cholesterol synthesis
how do statins work
they’re structural analogs of mevalonate, competitively inhibiting HMG CoA reductase
how to statins affect metabolism
decrease cholesterol synthesis
increase LDL receptors in liver
what are the 4 main side effects of statins
hepatotoxicity
myopathy
encephalopathy
hyperglycemia
what type of familial hypercholesterolemia are statins ineffective in treating
IIa
what 4 molecule production do statins decrease
dolichol
protein prenylation
level of Heme-A
Coenzyme Q
how does ezetimibe act
blocks dietary cholesterol transporter so there is reduced cholesterol in chylomicrons
what is the effect of decreased cholesterol on number of LDL receptors
lower cholesterol= increase LDL receptors
*cholesterol needs to be brought in from outside due to decreased ability to synthesis endogenous cholesterol, decreasing plasma cholesterol levels
what is the effect of phytosterols, found in plant based oils, on absorptions of dietary fat
decreases
what is the prefix of drugs used as bile acid sequesters
chole- or cole-
what is the effect of bile acid sequestering drugs
prevent resorption of bile acids, increasing conversion of cholesterol to bile to be excreted in stool
how do Alirocumab and Evolocumab work
PCSK9 inhibitors which prevent degradation of surface LDL receptors, allowing for increased LDL internalization and decreased LDL in plasma
what does the suffix -mab mean in drugs
monoclonal antibody
how does Niacin (nicotinic acid, vit B3) work
inhibits lipolysis in fat cells
when is Niacin mainly used
when HDL is low
what are the 3 main side effects of Niacin
flushing
itching
obesity
how do fibrates work
activate PPAR-alpha transcription factor, increasing lipoprotein lipase activity
what is the effect of increased lipoprotein lipase activity with fibrate usage
TAG–>3FA+glycerol–>decreased plasma TAG
what is the effect of fibrate drugs on fatty acid oxidation
increases (decreases TAG synthesis and decreased VLDL)
what are the side effects of fibrates
cholesterol gallstones (increased LDL
Fibrates are mainly used with patients with what plasma levels
high triglycerides
MTTP inhibitors such as Lomitapide block what
chylomicron and VLDL synthesis, lowering plasma triglyceride and cholesterol
what is the main side effect of MTTP inhibitors
lipid filled enterocytes and hepatocytes
how do pancreatic lipase inhibitors such as Orlistat work
inhibit pancreatic and gastric lipases, preventing digestion/reabsorption of dietary fats, decreasing chylomicrons (TAG and cholesterol reduction)
what are 3 plasma affects of omega 3 fatty acids (Lovaza- ALA, EPA, DHA)
decrease plasma TAG
increase HDL
may increase LDL
what are the best drug class to decrease total cholesterol
statins
what is the best drug class to decrease LDL
statins
what is the best drug class to increase HDL
Niacin
what are the 2 best drug classes to decrease TAG levels
Niacin and Fibrates
what is the only drug class to increase HDL
Niacin
