Summary Table of Drugs Used in Dyslipidemia Flashcards
Which drug: MOA
Inhibit HMG-CoA reductase
Statins
Which drug: MOA
Peroxisome proliferator- activated receptor-alpha (PPAR-α) agonists
Fibrates
Which drug: MOA
- Binds bile acids in gut
- prevents reabsorption
- increases cholesterol catabolism
- upregulates LDL receptors
Bile acid sequestrants
Which drug: MOA
Blocks sterol transporter NPC1L1 in intestine brush border
Cholesterol absorption inhibitor
Which drug: MOA
- Decreases catabolism of apo AI
- reduces VLDL secretion from liver
Niacin
Which drug: MOA
Complexes PCSK9
PCSK9 humanized monoclonal antibodies
Which drug: Effects
- Reduce cholesterol synthesis and upregulate low-density lipoprotein (LDL) receptors on hepatocytes
- modest reduction in triglycerides
Statins
Which drug: Effects
- Decrease secretion of very- low-density lipoproteins (VLDL)
- increase lipoprotein lipase activity
- increase high- density lipoproteins (HDL)
Fibrates
Which drug: Effects
Decreases LDL
Bile acid sequestrants
Which drug: Effects
- Inhibits reabsorption of cholesterol excreted in bile
- decreases LDL and phytosterols
Cholesterol absorption inhibitor
Which drug: Effects
- Increases HDL
- decreases lipoprotein(a) [Lp(a)], LDL
Niacin
Which drug: Effects
Inhibits catabolism of LDL receptor
PCSK9 humanized monoclonal antibodies
Which Drug: Clinical Applications
- Atherosclerotic vascular disease (primary and secondary prevention)
- acute coronary syndromes
Statins
Which Drug: Clinical Applications
Hypertriglyceridemia, low HDL
Fibrates
Which Drug: Clinical Applications
Elevated LDL, digitalis toxicity, pruritus
Bile acid sequestrants
Which Drug: Clinical Applications
Elevated LDL, phytosterolemia
Cholesterol absorption inhibitor
Which Drug: Clinical Applications
- Low HDL
- elevated VLDL, Lp(a); elevated LDL in statin- unresponsive or intolerant patients
Niacin
Which Drug: Clinical Applications
Familial hypercholesterolemia not responsive to oral therapy
PCSK9 humanized monoclonal antibodies
Which Drug: PK, Toxicities, Interactions
- Oral
- Duration 12-24 h
- Toxicity: Myopathy, hepatic dysfunction
- Interactions: CYP-dependent metabolism (3A4, 2C9) interacts with CYP inhibitors/competitors
Statins
Which Drug: PK, Toxicities, Interactions
- Oral
- duration 3–24 h
- Toxicity: Myopathy, hepatic dysfunction
Fibrates
Which Drug: PK, Toxicities, Interactions
- Oral
- taken with meals
- not absorbed
- Toxicity: Constipation, bloating
- interferes with absorption of some drugs and vitamins
Bile acid sequestrants
Which Drug: PK, Toxicities, Interactions
- Oral
- duration 24 h
• Toxicity: Low
incidence of hepatic dysfunction, myositis
Cholesterol absorption inhibitor
Which Drug: PK, Toxicities, Interactions
- Oral
- large doses
- Toxicity: Gastric irritation, flushing, low incidence of hepatic toxicity
- may reduce glucose tolerance
Niacin
Which Drug: PK, Toxicities, Interactions
- Parenteral
- Cost ~ $14,000/year
- Toxicity: injection site reactions, nasopharyngitis, flu-like symptoms, rarely myalgia, neurocognitive and ophthalmologic events
PCSK9 humanized monoclonal antibodies
