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Statins:
- MOA?
- CI?
- Warning?
- SE?
- Dosing Times?
- Avoid With?
- MOA: inhibits HMG-CoA --> prevents cholesterol synthesis
- CI: Acute liver disease || Pregnancy || Breastfeeding
- Warning: Skeletal muscle effects (myopathy, rhabdomyolysis)
- SE: Myalgias || Arthralgias || Myopathy || short term Memory Loss
- Take HS: Simvastatin || Fluvastatin || Lovastatin
- Inc Risk Myopathies == avoid with fibrate (Gemfibrozil) and Niacin products
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Statin Equivalent Doses
- "Pharmacist Rock At Saving Lives & Preventing Flu"
- Pravastatin _ 2 mg
- Rosuvastatin _ 5 mg
- Atorvastatin _ 10 mg
- Simvastatin _ 20 mg
- Lovastatin _ 40 mg
- Pitavastatin _ 40 mg
- Fluvastatin _ 80 mg
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-
Lescol
Lescol XL
- Fluvastatin
- - Lescol -- take in the evening
- - Lescol XL -- taken daily
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Mevacor
Altoprev
- Lovastatin
- - Mevacor -- IR _ take with evening meal
- - Altoprev -- ER _ take HS
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-
-
Crestor
- Rosuvastatin
- -- exposures are 2x greater in Asian pts == consider 5 mg starting dose
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Zocor
- Simvastatin
- -- take in the evening
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Vytorin
Simvastatin PLUS Ezetimibe
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Ezetimibe:
- MOA?
- IMPROVE-IT Study?
- MOA: inhibits absorption of cholesterol at the brush border of the small intestine
- IMPROVE-IT: addition of moderate-intensity statin therapy in stable patients with recent ACS, who had LDL cholesterol levels within guideline recommendation, further lowered the risk of CV events (Ezetimibe + Statin >> Statins)
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Bile Acid Sequestrants:
- MOA?
- CI?
- SE?
- NOTES?
- MOA: binds bile acid in the intestine, forming a complex that is excreted in the feces
- CI: Colesevelam _ bowel obstruction || TG > 500 mg/dL || Hx of hyperglyceridemia-induced pancreatitis
- SE: Constipation || Abd pain || Cramping || Gas || Bloating || Inc TG
- NOTES: ACC/AHA guidelines do not recommend using these agents when TGs are >/= 300 mg/dL
- - May decrease absorption of fat-soluble vitamins (A, D, E, K), folate, iron --> separate administration times
- - Colesevelam _ may be considered as an option in Pregnant patients
- - Colesevelam _ most commonly used || less drug interactions
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Welchol
- Colvesevelam
- -- Bile Acid Sequestrant
- -- take with a meal and liquid
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Fibrates:
- MOA?
- CI?
- SE?
- NOTES?
- MOA: PPARalpha activators --> upregulate the expression of apolipoprotein C2 (apoC--II) and apolipoprotein A1 (apoA-I) --> apoC-II increase lipoprotein activity ==> increase catabolism of VLDL particles [DEC TG signigicantly]
- CI: Severe liver disease || Severe Renal disease || Gallbladder disease || Nursing mothers
- SE: Abd pain || dyspepsia
- NOTES: Signifcantly reduces TG --> but can increase LDL when TG are high
- - Lopid _ BID dosing -- 30 min before breakfast and dinner
- - Antara / Fibricor / Tricor / Triglide / Trilipix _ take QD, with or without food
- - Fenoglide / Lofibra / Lipofen _ take QD, with food
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Antara / Fibricor / Tricor / Trilipex
Fenoglide / Lofibra / Lipofen
- Fenofibrate
- Fenofibric Acid
- -- Fibrates
- -- Antara / Fibricor / Tricor / Triglide / Trilipix _ take QD, with or without food
- -- Fenoglide / Lofibra / Lipofen _ take QD, with food
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Lopid
- Gemfibrozil
- -- Fibrates
- -- take BID _ 30 minutes before breakfast and dinner
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Niacin
- MOA?
- Warnings?
- SE?
- NOTES?
- MOA: decreases the rate of hepatic synthesis of VLDL (dec TG) and LDL
- Warnings: Hepatotoxicity
- SE: Flushing || Pruritis (itching) || N/V/D || hyperglycemia || hyperuricemia (gout)
- NOTES: Niaspan == best clinical choice _ less flushing and less hepatotoxicity
- - CR and SR Formulation == less flushing but MORE hepatotoxicity
- - IR == poor tolerability due to flushing/itching
- - Reduce flushing -- ASA 325 mg (or ibuprofen 200 mg) 30-60 min before dose
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Niaspan
- ER Niacin
- -- take HS after a low-fat snack (most flushing will occur at night
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Fish Oils
- Indication?
- Warnings?
- SE?
- NOTES?
- Indication: Omega Fatty Acids == as adjunct to diet in patients with TGs > 500 mg/dL
- Warnings: caution in patients with fish and/or shellfish allergy
- SE: Eructation (burping) || dyspepsia
- NOTES: can prolong bleeding time --> monitor INR
- - Lovaza _ can INC LDL
-
Lovaza
- Omega-3 Acid Ethyl Esters
- -- Fish Oils
- -- take 4 caps D -OR- 2 caps BID
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PCSK9 (Proprotein Convertase Subtilisin Kexin Type 9 Inhibitors)
- MOA?
- SE?
- NOTES?
- MOA: binds to PCSK9 --> inhibits binding of PCSK9 to LDLR (PCSK9 binds to LDL receptors on hepatocyte surfaces to promote LDLR degradation) ==> increases number of LDLR to clear circulating LDL
- SE: Injection site reaction
- NOTES: monoclonal antibodies == for FH
- - Alirocumab == indicated for heterozygous familial hypercholesterolemia (HeFH or ASCVD)
- - Evolocumab == incidated for BOTH HoFH and HeFH
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Praluent
- Alirocumab
- -- PCSK9 _ indicated for HeFH
- -- SC injection (thigh, abdomen, upper arm)
- -- store in refrigerator
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Repatha
- Evolocumab
- -- PCSK9 _ indicated for HoFH and HeFH
- -- SC injection
- -- store in refrigerator
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Juxtapid
- Lomitapide
- -- PO daily
- -- REMS program _ risk of hepatotoxicity
- -- CI: Pregnancy
- -- Avoid CYP 3A4 inhibitors
- -- $$$ ($433,000/yr)
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Kynamro
- Mipomersen
- -- SC once weekly
- -- REMS program _ risk of hepatotoxicity
- -- CI: Active Liver disease
- -- $$$ ($433,000/yr)
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Requires REMS program (2)
- Lomitapide (Juxtapid)
- Mipomersen (Kynamro)
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Injectable Medications (3)
- Alirocumab (Praluent)
- Evolocumab (Repatha)
- Kynamro (Mipomersen)
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Most Hepatotoxic (2 classes)
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4 Statin Benefit Group
- 1 - presence of clinical ASCVD, including Heart Disease (ACS, S/P, MI, stable or unstable angina, coronary or other arterial revascularization), Stoke, TIA or peripheral arterial disease thought to be of atherosclerotic origin
- 2 - Primary elevations of LDL >/= 190 mg/dL
- 3 - Diabetes and age 40-75 years with LDL between 70-189 mg/dL4 - Patients 40-75 years of age with LDL between 70-189 mg/dL and estimated 10-year ASCVD risk of >/= 7.5% (using global risk assessment tool)
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Classification Of Cholesterol and TG Levels (mg/dL)
- LDL
- HDL
- TG
- Non-HDL
- LDL: < 100 = Desirable || >/= 190 = Very High
- HDL: < 40 (men) = Low || < 50 (women) = Low
- TG: < 150 = Desirable || >/= 500 = Very High
- Non-HDL: < 150 = Desirable || >/= 220 = Very High
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High-Intensity Statin _ Treatment Options (2)
- Atorvastatin _ 40 - 80 mg Daily
- Rosuvastatin _ 20 - 40 mg Daily
- -- Daily dose Decrease LDL > 50%
-
Low-Intensity Statin _ Treatment Options (5)
- Simvastatin _ 10 mg Daily
- Pravastatin _ 10 - 20 mg Daily
- Lovastatin _ 20 mg Daily
- Fluvastatin _ 20 - 40 mg Daily
- Pitavastatin _ 1 mg Daily
- -- Daily dose Decrease LDL < 30%
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Moderate-Intensity Statin _ Treatment Options (7)
- Atorvastatin _ 10 - 20 mg Daily
- Rosuvastatin _ 5 - 10 mg Daily
- Simvastatin _ 20 - 40 mg Daily
- Pravastatin _ 40 - 80 mg Daily
- Lovastatin _ 40 mg Daily
- Fluvastatin XL _ 80 mg Daily
- Fluvastatin _ 40 mg BID
- Pitavastatin _ 2 - 4 mg Daily
- -- Daily dose Decrease LDL 30% - 40%
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HIGH-INTENSITY Statin Treatment Intensity Based on Patient Risk
- Secondary Prevention:
- -- Clinical ASCVD </= 75 years of age
- Primary Prevention:
- -- Primary elevation of LDL >/= 190 mg/dL
- -- Diabetes and Age 40-75 years with LDL between 70-189 mg/dL and estimated 10-year ASCVD risk >/= 7.5%
- -- Age 40-75 years with LDL between 70-189 mg/dL and estimated 10-year ASCVD risk >/= 7.5%
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MODERATE-INTENSITY Statin Treatment Intensity Based on Patient Risk
- Secondary Prevention:
- -- Clinical ASCVD > 75 years of age
- Primary Prevention:
- -- Age 40-75 years with LDL between 70-189 mg/dL and estimated 10-year ASCVD risk >/= 7.5% _ (moderate and high intensity)
- -- Diabetes and Age 40-75 years with LDL between 70-189 mg/dL and estimated 10-year ASCVD risk < 7.5%
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Statin Equivalent Doses
- "Pharmacists Rock At Saving Lives & Preventing Flu"
- Pravastatin _ 2 mg
- Rosuvastatin _ 5 mg
- Atorvastatin _ 10 mg
- Simvastatin _ 20 mg
- Lovastatin _ 40 mg
- Pitavastatin _ 40 mg
- Fluvastatin _ 80 mg
-
Drug-Drug Interactions _ SIMVASTATIN
- Max 10 mg/day (3)
- Max 20 mg/day (4)
- Max 10 mg/day:
- -- Verapamil || Diltiazem || Dronedarone
- Max 20 mg/day:
- -- Amiodarone || Amlodipine || Lomitapide || Ranolazine
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Drug-Drug Interactions _ LOVASTATIN
- Max 20 mg/day (5)
- Max 40 mg/day (2)
- Max 20 mg/day:
- -- Danazol || Diltiazem || Verapamil || Dronedarone || Amlodipine
- Max 40 mg/day:
- -- Amiodarone || Ticagrelor
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