AntiLipidDrugs Flashcards
If patients have myalgia as a side effect on one statin can try the patient on another statin?
Yes. myalgia does not rule out the class altogether. Patients may tolerate a different statin – if failed multiple statins, change drug class
MOA of statins
Inhibits HMG-CoA reductase, reducing cholesterol synthesis.
Fibric acid derivatives MOA
Activates PPAR-alpha, increasing lipolysis and elimination of triglyceride-rich particles.
increase lipolysis of triglycerides via lipoprotein lipase, resulting in a decrease of 50% or more in triglyceride levels.
Bile acid sequestrants MOA
exchange chloride ions for negatively charged bile acids, promoting a 10-fold increase in bile-acid excretion.
Binds bile acids in the intestine, preventing their reabsorption
Increased clearance results in enhanced conversion of cholesterol to bile acids by the liver.
Bile acid sequestrants drugs
Cholestyramine (Questran), Colestipol (Colestid)
Fibric acid derivatives drugs
Gemfibrozil (Lopid), Fenofibrate (TriCor)
What class is Ezetimibe (Zetia), what is its MOA?
Inhibits absorption of cholesterol at the brush border of the small intestine.
Active liver disease is a contraindication for all antilipidemics except ?
the bile-acid sequestrants
Cholestyramine (Questran), Colestipol (Colestid).
Cholestyramine(Questran) can do what to Amio?
Decrease amio levels
How are bile acid sequestrants absorbed and distributed?
Cholestyramine and colestipol are not absorbed at all and have no distribution. Their action is entirely related to binding bile acids in the gut
Contrainidcation of Cholestyramine(Questran) and a caution for bile acid sequestrants
Cautious use of the bile-acid sequestrants is suggested for patients with a history of constipation. Phenylketonuria (PKU) is a contraindication.
Indication for Bile Acid Sequestrants
HLD
Cholestyramine(Questran) comes in what form
powder
bile-acid sequestrants’ major side effects are
Side Effects: Gastrointestinal disturbances (constipation, bloating).
Plasma half life of statins are generally short except
Atorvastatin half-life of which is 14 hours
Statins, particularly atorvastatin, do what to digoxin levels?
Increase!
Grapefruit ingestion should be avoided with which statins
simvastatin, lovastatin, and atorvastatin
Most potent statin drug?
Rosuvastatin,
atorvastatin second most potent
Rosuvastatin and others in the class, could cause an increase in the likelihood of developing.
Diabetes. risk for CV event greater, so shouldn’t be stopped
Rosuvastatin, more or less, likely to have myalgias
Less
All HMG-CoAReductaseInhibitors(statins) are contraindicated in?
in pregnancy or active hepatic disease
Gemfibrozil(Lopid) is contraindicated with concurrent use of which drugs
DDI w/statins (contraindicated with lovastatin
and simvastatin)
Gemfibrozil(Lopid) is what class of drug
Fibric acid derivatives
Gemfibrozil excreted?
Mostly unchanged in urine, so monitor impaired renal functoin
Avoid concurrent use of Gemfibrozil and?
Atorvastatin - increased myopathy and rhabdomyolysis risk
Side Effects of Gemfibrozil
dyspepsia, abdominal pain, and diarrhea. They may also produce cholelithiasis secondary to their increased cholesterol excretion into the bile. They are discontinued if gallstones are found.
most potent triglyceride-lowering agents because of their effect on VLDL?
Fenofibrate and gemfibrozil
aka fibric acid derivatives
Best meds to increase HDL
Gemfibrozil and fenofibrate are the next best at increasing HDL, followed by some reductase inhibitors.
Is Ezetimibe absrobed?
No, works in the gut
True or False, Ezetimibe can be used with statins or solo if statin not tolerated.
True. Ezetimibe (Zetia) is approved for combination of these statins for added effect or for solo use in HF if statins are not tolerated
When is Evolocumab used?
PCSK9 inhibitors are used in conjunction with high-dose statins and other lipid-lowering medications when desired outcomes are not met in very high-risk CV patients
What drug class is Evolocumab and Alirocumab
PCSK9 Inhibitors
PCSK9 inhibitors MOA (evolocumab and alirocumab)
monoclonal antibodies that alter the activity of a protein that transports LDL into the liver for recycling into the system. Consequently, there are more lipoprotein receptors on the liver for removal, which results in lower LDL levels in the serum.
How are PCSK9 inhibitors given
PCSK9 inhibitors are given every 2 weeks or only once a month using a single-dose pen–like device.
