Drugs for hyperlipidemia Flashcards
A disorder where there are abnormally elevated levels of fat particles in the blood
Hyperlipidemia
also known as the fat particles in the blood
Lipids
what are the four major types of lipid
Chylomicrons
Very low-density lipoproteins
low-density lipoproteins
high-density lipoproteins
Chylomicrons are produced in
gut from dietary lipids
This type of lipoprotein is composed mostly of triglycerides and small amounts of cholesterol
chylomicrons
VLDL (very low-density lipoproteins) are produced in?
liver
what is the function of chylomicrons and VLDL
They are responsible for delivering energy-rich triglycerides to cells throughout the body
An enzyme located on the capillary walls that are responsible for the release of fatty acids from lipoproteins
Lipoprotein lipase
this contains a higher percentage of cholesterol
LDL (low-density lipoproteins)
A high concentration of LDL is considered
bad cholesterol
what is the function of LDL
deliver cholesterol to cells
half of the circulating LDL is taken up by the liver because?
the liver uses it to synthesize bile acid
This is composed mainly of protein with a small number of lipids
HDL (high-density lipoprotein)
what is the mechanism of action of HDL
Transports excess cholesterol from the peripheral cells back to the liver
HDL is produced in?
small intestine and liver
Statins are commonly known as
HMG-CoA reductase inhibitors
what does HMG-CoA inhibit?
it inhibits the conversion of HMG-CoA (hydroxymethylglutaryl coenzyme A) to mevalonate
It is a rate-controlling enzyme
HMG-CoA reductase
It is a cholesterol precursor in the liver
Mevalonic acid
what happens when you inhibit HMG-CoA reductase
less synthesized mevalonic acid which results in a low concentration of cholesterol in the liver
this leads to decrease secretion of VLDL
low intracellular cholesterol levels
What are drugs under HMG-CoA?
atorvastatin fluvastatin lovastatin pravastatin rosuvastatin simvastatin
Nicotinic acid is commonly known as
niacin
nicotinic acid is normally found in
adipose tissue
what enzyme does niacin inhibit
hormone-sensitive lipase
it is the enzyme responsible for the breakdown of triglyceride to free fatty acids
hormone-sensitive lipase
what happens when nicotinic acid inhibits hormone-sensitive lipase?
There will be no or less free fatty acid for the liver to synthesize thus resulting to decrease hepatic VLDL which leads to decrease levels of VLD
Fibrates are also known as
finofibrate derivatives
PPAR-alpha stands for
peroxisome proliferator-activated receptor alpha
Nuclear transcription receptor that is found in metabolic active tissues such as liver and adipose tissue
PPAR-alpha
PPAR-alpha is normally found in
liver and adipose tissue
it is a protein that inhibits lipoprotein lipase activity
Apo-CIII
it is an adipocyte enzyme that cleaves fatty acids from intracellular triglycerol
Hormone-sensitive lipase
is an adipocyte enzyme that cleaves fatty acids from circulating lipoproteins
lipoprotein lipase
Their binding induces activation or inhibition of certain genes that code for proteins involved in lipid metabolism
Binding of Fibrates and PPAR-alpha
Fibrates increase the expression of these proteins that are a major component of HDL
Apo-AI and Apo-AII
these are the major component of HDL production
Apo-AI and Apo-AII
drugs that are under fenofibrate derivatives
fenofibrate
gemfibrozil
This activates nuclear transcription receptor PPAR-alpha
Fibrates
It increases the expression of lipoprotein lipase
fibrates
Also known as bile acid resins
bile acid sequestrants
bile is stored in?
gallbladder
Bile acid sequestrants serve as
ion exchange resin
responsible for the transportation of excess cholesterol from the peripheral cells back to the liver
HDL
examples of bile acid sequestrant
Colesevelam
Colestipol
cholestyramine
Free cholesterol either comes from
dietary sources
bile
In the normal mechanism of cholesterol absorption, it firsts bind to a protein called
NPC1L1
ACE inhibitors can elevate which levels
bradykinin
This peptide causes blood vessels to dilate by stimulating the release of nitric oxide and prostacyclin
Bradykinin