Drugs for Management of Dyslipidemia Lecture PDF Flashcards
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What is the rate limiting step of cholesterol formation
3 hydroxy 3 methylglutaryl coenzyme A (HMG-CoA)
One of the most serious reactions to statin drugs
-fatal rhabdomyolysis
Statin mech of action
Inhibition of HMG CoA reductase resulting in increase # of LDL cholesterol receptors in the liver ultimately decreasing overall level of LDL in bloodstream
Most statins are given in the evening because…
….cholesterol synthesis increases during night
Only statin with FDA approval for increasing of HDL cholesterol even though many do this to some extent anyways
simvastatin (zocor)
Statin therapeutic uses (6)
- hypercholesterolemia (lowering LDL-C)
- primary prevention of CV events
- 2ndary prevention of CV events
- primary prevention in those with normal LDL levels
- Post MI therapy
- diabetes even those without high cholesterol who have just one additional risk factor
Statin administration
PO, 30-90% bioavailable and acts on liver
Statin drug interactions which 4 agents and what 4 drugs
4 agents (artovastatin, cervivastatin, lovastatin, and smivastatin) can see interaction with
- itraconazole
- cyclosporine
- erythromycin
- grapefruit juice
Statins ADR’s (4)
- GI disturbances
- hepatotoxicity (recommends baseline liver enzyme measurement before starting statins)
- rhabdomyolysis (rare but needs warning to patient)
- new onset of diabetes (risk less than benefits)
Statin use is completely contraindicated in…
….pregnancy
Ezetimibe (zetia) drug class and mech of action
- Cholesterol absorption inhibitor
- selectively inhibits intestinal absorption of dietary and biliary choesterol at brush border of small intestine leading to decreased delivery to liver and therefore reducing all overall blood cholesterol levels
Ezetimibe (zetia) ADR’s (3)
- diarrhea
- rhabdo
- hepatitis
PCSK9 inhibitors mech of action
Binds to LDL receptors on hepatocytes promoting receptor degradation thereby preventing LDL-C clearance from blood increasing serum LDL-C conc.
PSCK9 inhibitors ADR
-neurocognitive events
Alirocumab (praluent)/Evolocumab (repatha) drug class and therapeutic use
- PCSK9 inhibitor
- approved as adjunct to diet and statin therapy for adults with hypercholesterolemia
Bile acid binding resins function and 3 example agents
Were once main drug for decreasing LDL level, today primarily reserved for adjunct therapy with statins that form insoluble complex with bile acids in intestine, relies on liver’s ability to produce LDL receptors
includes cholestyramine, colestipol, and colesvelam
Bile binding resins drug interactions (1)
-form insoluble complexes with other drugs preventing absorption including statins, require medication be given 2 hours before or 4-6 hrs after
Fibrates function and what is it the most effective drug for?
Activate nuclear transcription factor peroxisome proliferator activated receptor (PPAR a) which regulates genes that control lipid and glucose metabolism, inflammation, and endothelial function, most effective drug for decreasing triglycerides
Gemfibrozil (lopid) therapeutic uses (2)
- lower VLDL and triglycerides
- raise HDL
fenofibrate (tricor, lofibra, triglide, anatara) function
Treat hypertriglyceridemia in pts not responding to dietary measurements, lowers triglycerides by decreasing VLDL
Nicotinic acid (niacin) function
Lowers all plasma lipoproteins and triglycerides
Long chain omega 3 polyunsaturated fatty acids (PUFA’s) function
Lower triglycerides and decrease fasting conc. by 20-50% b
Alirocumab function and drug class
Human monoclonal Ab that acts as a PCSK9 inhibitor
Only fibrate with demonstrated beneficial effects on CV outcomes, but contraindicated in use with statins for risk of myopathy
-Gemfibrozil
