Cardio: Drugs Used for Hyperlipidemia Flashcards
MOA of Statins (specifically for lipids)
Competitively block HMG-CoA reductase
-means less mevalonate made
What else can statins do, besides lowering lipids?
Plaque Stabilization
Reduce Inflammation
-Decrease CRP
Reverse Endothelial Dysfxn
-increase NO and reduce LDL oxidation
Decrease Thrombogenicity
-reduce expression of TF on endothelial cells
Indications of Statins?
CV disease-especially if hyperlipidemia
Contrainidcations of Statins?
Active Hepatic disease
-statins can increase injury and LFTs
Pregnancy
-teratogenic
Adverse effects of Statins?
Myopathy
-see an increase in CK
Diabetes (new onset)
Hepatotoxicity
Possible Neurologic effects (not serious)
Do statins interact with other drugs?
Yes, they are metabolized by the CYP450 system (CYP3A4 or CYP2C9)
-drugs that interfere will increase/decrease levels
What groups of people may require a dose reduction of statins?
Older people and East Asians
Which statins drugs are metabolized by CYP3A4 and which are CYP2C9?
CYP3A4
-Atorvastatin, Simvastatin, Lovastatin
CYP2C9
-Fluvastatin
MOA of Ezetimibe
Inhibits PC1L1 protein to impair dietary and biliary cholesterol absorption at brush boarder of the intestine
-decrease LDL
If you are choosing a drug to add to Statins, what is first choice: ezetimibe or PCSK9 inhibitors?
Ezetimibe>PCSK9
Indications for Ezetimibe?
Hyperlipidemia
-Familial (homozygous) or Acquired
Contraindications of Ezetimibe?
Active Hepatic Disease/severe impairment in combo with statins
-Raise in AST/ALT
Pregnancy in combo with Statins
Adverse effects of ezetimibe?
Most common: headache, runny nose, sore throat, some body aches
What toxicity is associated with ezetimibe?
Skeletal muscle toxicity with concomitant use with statins
-especially if over 65, have hypothyroidism or renal impairment
What are the PCSK9 inhibitors?
Alirocumab and Evolocumab
MOA of the PCSK9 inhibitors?
Decrease the amount of LDL receptor degredation
-therefore more LDL is taken out of the circulation