A Brief Review on Dyslipidemia for Pharmacists

  • General information:
    • Dyslipidemia is defined as a condition in which an individual has elevated cholesterol or lipids in an individual’s blood such as the following:
      • HDL: “Good” cholesterol
      • LDL: “Bad” cholesterol
      • Triglycerides (TGs)
    • LDL cholesterol can form plaques in vessels
    • HDL cholesterol helps remove LDL
    • TGs are formed in fat cells when calories are not burned right away
  • Symptoms:
    • Regarded as a silent disease in which patients are unaware of having it
  • Types and causes:
    • Primary dyslipidemia:
      • Inherited through genetics
    • Secondary dyslipidemia
      • Caused by lifestyle factors such as the following:
        • Obesity
        • Diabetes
        • Hypothyroidism
        • Alcoholism
  • Risk factors:
  • Review of lab values**:
 Total cholesterolHDL  LDLTGs
Desirable< 200> 40 (men) > 50 (women)  < 100< 150
Borderline200 – 239   130-159150-199
High  > 240     160-189  200-499  
Very high      > 190> 500

**All units are in mg/dL

  • Treatment options:
Class and Mechanism of ActionGeneric (Brand) NamesSide EffectsBlack Box WarningsContraindications
Statins: Inhibits the rate-limiting step for cholesterol synthesis by inhibiting HMG-CoA reductase   **first-line**Atorvastatin (Lipitor) Rosuvastatin (Crestor) Simvastatin (Zocor) Pravastatin (Pravachol) Pitavastatin (Livalo) Fluvastatin (Lescol) Lovastatin (Mevacor) Simvastatin + Ezetimibe (Vytorin)  Myalgia Arthralgia Myopathy Diarrhea Cognitive impairmentSkeletal muscle effects  

Hepatotoxicity (increased LFTs)
Pregnancy Breastfeeding  

Use with cyclosporine  

Active liver disease
Bile Acid Sequestrants: Inhibits absorption of bile acids into blood which ultimately aids in reducing LDL  Cholestyramine (Questran) Colesvelam (Welchol) Colestipol (Colestid)  Abdominal pain Cramping Flatulence Constipation Increased TGs Increased LFTs   Esophageal obstruction   Cholestyramine: Biliary obstruction  
Colesvelam: Bowel obstruction and TGs > 500
Fibrates: PPAR-α agonist; inhibits TG synthesis and decreases VLDLGemfibrozil (Lopid) Fenofibrate (Tricor)  Abdominal pain Dyspepsia Increased LFTs  
Upper respiratory tract infection (URTI)  
Risk of myopathy with concurrent statin use   Increased serum creatinine   CholelithiasisLiver disease Renal disease Gallbladder disease  

Use with repaglinide
PCSK-9 Inhibitors: Monoclonal antibodies that decrease LDLAlirocumab (Oraluent) Evolocumab (Repatha)Flu Cold URTI Injection site reaction   Urinary tract infection (UTI)    
2-Azetidinones: Inhibits absorption of cholesterol at the small intestineEzetimibe (Zetia)Myalgia Arthralgia Diarrhea URTI  Skeletal muscle effectsAvoid in patients with hepatic impairment
Fish Oils: Unknown mechanism of action    Omega-3 Acid (Lovaza) Icosapent Ethyl (Vascepa)Dyspepsia Flatulence Burping Increased LDLCaution in those with a fish/shellfish allergy 
Nicotinic acid/Vitamin B3: Decreases synthesis of VLDL, LDL, and TGs  Niacin (Niacor, Niaspan)Flushing Pruritis Nausea Vomiting Diarrhea Cough

Hyperglycemia Hyperuricemia  
Orthostatic hypotension  
Hepatotoxicity  

Rhabdomyolysis with concurrent statin use
Liver disease  

Arterial bleed  

Peptic ulcer disease
High-Intensity Statin Therapy (Lowers LDL on average by > 50%)Moderate-Intensity Statin Therapy (Lowers LDL on average by 30-49%)  
Atorvastatin 40-80 mg Rosuvastatin 20-40 mgAtorvastatin 10-20 mg
Rosuvastatin 5-10 mg
Simvastatin 20-40 mg
Pravastatin 40-80 mg
Lovastatin 40 mg
Fluvastatin 40 mg
Pitavastatin 2-4 mg  
  • Additional notes:
    • Statins
      • Patient must contact their doctor for any muscle symptoms or dark urine
      • Simvastatin, lovastatin, and fluvastatin must be taken at bedtime
      • Avoid gemfibrozil, niacin (> 1 gram), and colchicine
      • Simvastatin and lovastatin:
        • Avoid strong CYP3A4 inhibitors such as azoles, erythromycin, clarithromycin, HIV protease inhibitors, cobicistat, nefazodone, cyclosporine, grapefruit juice
    • Bile Acid Sequestrants
      • Take with food and water (colesevelam)
      • Space out with multivitamins
        • At least 4 hours of one another
      • ACC/AHA guidelines do not recommend use if TGs are > 300
    • Fibrates
      • Can increase LDL when TGs are high
      • Patient must contact their doctor for any muscle symptoms, dark urine, abdominal pain, nausea, or vomiting
    • PCSK-9 Inhibitors
      • Store in fridge
      • Prior to administration allow for syringe to warm up to room temperature for 30-45 minutes
        • Inspect for any particles and/or color changes
      • Rotate injection sites
        • Alirocumab and evolocumab: Subcutaneous injections given in the thigh, upper arm, or abdomen (except within 2 inches from belly button)
    • 2-Azetidinones (Zetia):
      • Avoid concurrent use with gemfibrozil
      • Monitor LFTs with concurrent statin or fibrate use
      • Give 2 hours before or 4 hours after bile acid sequestrants
      • Patient must contact their doctor for any muscle symptoms or dark urine
      • Concurrent use with cyclosporine may increase levels of both drugs
    • Nicotinic acid/Vitamin B3
      • Must be taken with food
      • Monitor LFTs
      • Niaspan:
        • IR: Flushing/itching
        • ER: Less flushing than IR; take at bedtime
      • Avoid spicy food and ethanol
      • Take 4-6 hours after bile sequestrant acids
  • Treatment algorithm:
Prevention type  SituationTreatment
        Primary preventionLDL > 190 mg/dLHigh-intensity statin  
Primary preventionAge 40-75LDL 70-189 mg/dLPatients with diabetesModerate-intensity statin, unless 10-year ASCVD risk > 7.5%  
Primary preventionEvaluating 10-year clinical atherosclerotic cardiovascular disease (ASCVD) score  ASCVD risk > 7.5%: high intensity statin
 
ASCVD risk > 5% but <7.5%: moderate-intensity statin  
Secondary preventionPatients with clinical ASCVD< 75 years old: high intensity statin 
> 75 years old: moderate-intensity statin  

We hope this review helped refresh your clinical knowledge on dyslipidemia!

Best of luck,

Sam Tamjidi

RxPharmacist Team

References:

  1. Micromedex Solutions. Greenwood Village, CO: Truven Health Analytics. http://micromedex.com/. Accessed October 30, 2020.