Lipid Lowering Medication Flashcards
LDL
Bad cholesterol
-mainly responsible for development of atherosclerosis
Brings cholesterol to the cells for utilization
*Deposits extra cholesterol into vascular tissues ->atherosclerosis
Most LDL removed by the liver
-Liver disease=problem
HDL
Good cholesterol
Removes excess cholesterol from the cells and brings them to liver to be excreted
Can also remove cholesterol from directly from artery walls
Stops atherogenic lipoproteins from oxidizing
Medications Lowering LDL Levels
Statins Ezetimibe Bile Acid Sequesterants PCSK9 Inhibitors Niacin
Medications Lowering Triglyceride Levels
Omega 3s
Niacin
Fibrin Acid Derivatives
High Intensity LDL Lowering Statins
Greater than or equal to 50%
Atorvastatin 40-80mg
Rosuvastatin 20-40mg
Moderate Intensity LDL Lowering Statin Medications
30-50%
Atorvastatin 10-20mg Rosuvastatin 5-10mg Simvastatin 20-40mg Pravastatin 40-80mg Lovastatin 40mg
Adverse Effects Statins
Pregnancy Category X
Hepatic Dysfunction/Headache
Muscle Complications: Myalgia, Myopathy, Rhabdomyolysis
-women, order age, people with severe kidney dysfunction or liver issues(increased LFTs or abuse alcohol) higher risk of muscle problems
*switch to ROSUVASTATIN
STATINS DDIs
Atorvastatin, Lovastatin, Simvastatin : CYP3A4
-avoid grapefruit juice, protease inhibitors, antifungals, warfarin
Binding: Bile Acid Sequestrants and Calcium containing products
Simvastatin and Amlodipine
*max dose of simvastatin is 20mg when given with amlodipine
*rule of thumb: use ROSUVASTATIN if patient is taking multiple meds
Bile Acid Sequestrants TARGET and MOA
TARGET: lower LDL
- Not actually absorbed
- bind to bile acid in GI tract to increase excretion
- less bile acid in circulation
- more cholesterol is utilized to create more bile acids
- decreased LDL in circulation
- not absorbed, will have no systemic side effects
- given usually when a patient cannot have statin
- LAST LINE FOR LDL LOWERING
Bile Acid Sequestrants Generic Drugs
Cholestyramine -powder
Colestipol -powder
Colesevelam -tablets
Bile Acid Sequestrants ADVERSE EFFECTS and INTERACTIONS
Adverse effects:
- poorly tolerated
- significant GI side effects: bloating, gas, constipation, abdominal pain
- increased TGs
Interactions:
- bind to many medications, make them ineffective
- give medication 1 hour before or 4 hours after warfarin, levothroxine, digoxin, statins
Niacin TARGET and MOA
Targets: TG
-possibly can increase HDL and lower LDL
MOA:
- decreases VLDL synthesis (LDL is a byproduct of VLDL synthesis)
- reduces breakdown of HDL
Vitamin B3: available over the counter at low doses
-but we want patients to be prescribed because of the poor side effects
Niacin ADVERSE EFFECTS and DDIs
Adverse effects:
- flushing (pretreatment with aspirin or NSAID)
- pruritis (itchiness)
- increase using acid and/or glucose (not good for diabetes)
- nausea
- abdominal discomfort
Pregnancy Category X
DO NOT COMBINE WITH STATINS
-maybe use in statin intolerant patients
Ezetimibe TARGET and MOA
Cholesterol absorption inhibitor
Target: LDL
-no effect on TG
MOA:
- stops absorption of cholesterol in the intestines
- less cholesterol=less chylomicrons=less serum LDL
Second Line Treatment after Statins
-often used in combo with statins
Ezetimibe ADVERSE EFFECTS and DDIs
Adverse effects:
- diarrhea
- arthralgia
- fatigue
- in combo with statins- increased LFTs
Do NOT administer with Bile Acid Sequestrants
Fibrin Acid Derivatives TARGETS and MOAS
Target: TGs
- use in patients with TG >500
- number 1 treatment for lowering TG levels
MOA:
- agonist at PPAR-alpha receptors
- decreased VLDL synthesis in liver
- increase lipolysis
- higher clearance of TGs
Fibric Acid Derivatives Generic Drug Names
Gembfibrozil
Fenofibrate
Fibric Acid Derivatives ADVERSE EFFECTS and DDIs
Adverse effects:
- myopathy (especially when using with statins)
- increased LFTs
- nausea
- GI upset
- skin rash
DO NOT GIVE GEMFIBROZIL WITH SIMVASTATIN
- contraindication
- BUT can use other fibric acid derivatives with other statins
Omega 3s TARGET and MOA
Target: TGs
MOA:
- inhibition of TG secretion from the liver
- promotes metabolism of TG
Omega 3s Drug Names
Available OTC and RX
-OTC fish oil
RX:
- Vascepa
- Lovaza
OTC formulations can vary
- must watch for this
- patients with >500TGs need RX in capsule form rather than OTC
Omega 3s ADVERSE EFFECTS
Fishy taste (can put in freezer to combat this)
Burping
Antiplatelet effect at very high doses
- potential risk for bleeding
- must stop before surgery especially if on statin and aspirin too
PCSK9 Inhibitors TARGET and MOA
Target: LDL
-HUGE effect:can lower LDL up to 70%
MOA:
- monoclonal antibodies that stop PCSKP proteins
- PCSK9 proteins normally increase free LDL in system
- these drugs allow for more LDL to be cleared from the blood
WORKS BEST for FAMILIAL HYPERCHOLESTEROLEMIA
- but very expensive, so reserve for patients who fail other agents
- ex: familial hypercholesterolemia patient not responding to statin
PCSK0 Inhibitors Drug Agents
Alirocumab
Evolocumab
Injectible Only
PCSK9 Inhibitors ADVERSE EFFECTS and DDIs
Adverse Effects
- injection site reactions
- non specific effects common with monoclonal antibodies (headache, arthralgia, myalgia, limb pain, fatigue
Drug Interactions
- NONE that we know of
- encourage use with statins
