Antihyperlipidemics Flashcards
What is the suffix to remember for HMG-CoA reductase inhibitors?
“statins”
What are the S/E of HMG reductase inhibitors?
rhabdomyolysis
hepatotoxicity
myalgia, myopathy
What are some tests you should run before giving HMG-CoA inhibitors?
check creatine kinase
check liver function tests
What are some important drug interactions to remember when taking HMG-CoA inhibitors?
- Gemfibrozil (inc. rhabdomyolysis)
- Cytochrome P450 inhibitors enhance toxicity of statins (exception Pravastatin because it isn’t metabolized through this pathway)
How is HMG-CoA reductase inhibition beneficial for patients with dyslipidemia?
- dec liver cholesterol
- inc LDL receptor expression
- dec. plasma LDL
- dec VLDL synthesis result in: dec triglyceridemia
Name some important HMG-CoA reductase inhibitors to remember.
atorvastatin, rosuvastatin
What are some bile acid sequestrant drugs that are important to remember?
cholestyramine and colestipol
What is the MOA of bile acid sequestrants? Benefits?
complexation of bile salts in the gut resulting in
- dec. enterohepatic recirculation of bile salts
- inc. in new bile salt synthesis by the liver
- dec. liver cholesterol
- inc. LDL receptor expression
- dec blood LDL
S/E of bile acid sequestrants.
- Increase VLDL and triglycerides
- GI disturbances
- Malabsorption of lipid-soluble vitamins
What are some important drug interactions to remember with bile acid sequestrants?
warfarin
thiazides
digoxin
Contraindications to remember with bile acid sequestrants? ( What people shouldn’t be taking them?
those with hypertriclyceridemia
How do the nicotinic acid drugs work to affect persons with dyslipidemias?
decrease cAMP and inhibits lipolysis in adipose tissue; with fewer free fatty acids hepatic TG and VLDL synthesis dec.
Name the nicotinic acid drugs that are useful in treating dyslipidemia.
Niacin (Vit. B3)
What are the S/E of the Nicotonic acid drugs?
flushing, pruritis, burning pain (use aspirin)
hepatoxicity
hyperglycemia
Name the important fibrate drugs that you need to remember.
Gemfibrozil, Fenofibrate
What is the MOA of fibrates?
binds to the PPARα and increases expression of lipoprotein lipases
What are the benefits of using fibrates to treat dyslipidemias?
- dec VLDL and IDL (intermediate density lipoprotein)
- modest dec LDL (however in some patients with combined hyperlipidemia in inc. LDL
- inc HDL (most patients)
Main indication for use of fibrates?
hypertriglyceridemia
What are the S/E of fibrates?
gallstones, myositis
MOA of Ezetimibe
prevents intestinal absorption of cholesterol resulting in dec. LDL
prevents absorption by targeting Niemann-Pick C1-Like 1 (NPC1L1) which is a sterol transporter located on the brush border of the SI
S/E of Ezetimibe.
GI distress
Name the important PCSK9 inhibitors to remember.
Alirocumab, Evolocumab
What is PCSK9?
proprotein convertase subtilisin kexin 9 is a hepatic protease that promotes the destruction of LDL receptors
MOA of PCSK9 inhibitors and benefit.
block PCSK9 which can lower LDL 50-60% above that achieved by statin therapy alone
Orlistat indication?
weight loss
MOA of Orlistat?
inhibits pancreatic lipase > dec. triglyceride breakdown in the intestine
S/E of Orlistat?
oily stools (steatorrhea), diarrhea; dec absorption of lipid soluble vitamins
ROA for PCSK9 inhibitors?
subQ
What are monoclonal antibodies?
antibodies produced by a cell line “cell clone” derived from a single B lymphocyte
Are PCSK9 inhibitors monoclonal antibodies?
yes
