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
Does age, sex, amount of statins or presence of diabetes affect the effect of PCSK9 inhibitors?
No.
-page 11
Indications for the PCSK9 inhibitors?
Pateitns with heterozygous FH or those with CVD due to hyperlipidemia
Adverse effects of the PCSK9 inhibitors (both evolocumab and Alirocumab)?
Evolocumab
-runny nose, sore throat, cold/flu like symptoms
Alirocumab
-injection site reactions, muscle pain, eye-events
MOA of Bile Acid Binding resins?
Bind and block the reuptake of bile acids to force liver to make more
-lowers the amount of LDL
Indications of the Bile Acid Binding drugs?
Hypercholesterolemia
Contraindications to Bile Acid Binding drugs/
Hypertriglyceridema (>400)
-cause increase in TGs
Dysbetalipoproteinemia
Decreased GI motility or SBO
Which of the lipid lowering drugs can cause pancreatitis?
Bile Acid Binding drugs
-increase in triglycerides can cause pancreatitis
Adverse effects of bile acid binding drugs?
GI upset Elevated LFTs Elevated Triglycerides Fat Soluble vitamin def -ADEK
What metabolic disorder should you be cognizant of when prescribing the bile acid binding drugs?
Phenylketonuria
-each packet of Colesevelam contains Phenylalanine
MOA of Fibrates
Bind and activate PPARa
-increases metabolism of TGs and increase production of HDL
What are the indications for the fibrates?
Dyslipidemia
Hypertriglyceridemia
What drugs are fibrates?
Fenofibrate
Fenofibric Acid
Ge fibrozil
Contraindications of the fibrates?
Severe Kidney disease (increase Creatinine)
Active liver disease
Gallbladder disease
Nursing Mothers
Should fibrates be taken with statins?
No! Increases the amount of muscle toxicity
Other Adverse effects of fibrates?
Increase AST, ALT, CPK, and rhinitis
GALLSTONES**
Are fibrates safe for nursing mothers?
Nope, as they appear in breast milk
MOA of Niacin
Not completely understood..
-Reduces cholesterol and TG, increases HDL
May increase LPL and release of FFA
Indications for Niacin drugs?
Reduce total and LDL cholesterol
-can also reduce risk of recurrent nonfatal MI
Contraindications of niacin?
Liver diease
Active Peptic Ulcers
Arterial bleeding
Adverse effects of Niacin?
Flushing
-give with NSAIDs
Increase Blood sugar
-diabetics
Increase uric acid
-gout!
Increase AST/ALT
Increase Muscle toxicity (CK)
What diseases should niacin not be used in?
Diabetics Liver disease Gout Kidney Disease PUD
Does niacin prolong coagulation?
Has been shown to prolong PT
What drugs does niacin interact with?
Bile Acid binders
Statins
Vitamins can potentiate side effects
What should you do with Warfarin in a patient taking statins?
May have to decrease the dose
What drugs are niacin?
Niacor: oral
Niaspan: oral-exended release tablet
