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