ຢາລົດໄຂມັນ

ຢາລົດໄຂມັນ ( Lipid-Lowering Agents )

HMG-CoA reductase inhibitors (statins)

These agents inhibit the rate-limiting step in cholesterol biosynthesis by competitively inhibiting HMG-CoA reductase.

·         Low-density lipoprotein (LDL) reduction: 25%-60%

·         Examples: Atorvastatin, fluvastatin, lovastatin, pitavastatin, pravastatin, rosuvastatin, simvastatin

·         Contraindications: Hypersensitivity, active liver disease, pregnancy, lactation, coadministration with strong CYP3A4 inhibitors (selected statins)

Vitamin B3

Vitamin B3 inhibits very-low-density lipoprotein (VLDL) synthesis.

·         LDL reduction: 10%

·         High-density lipoprotein (HDL) increase: 20%

·         Example:  Niacin

·         Contraindications: Hypersensitivity, liver disease, active peptic ulcer, severe hypotension, arterial bleeding

Fibrates

These agents enhance lipoprotein lipase, resulting in increased VLDL catabolism, fatty acid oxidation, and triglycerides elimination). They decrease hepatic extraction of free fatty acids.

·         LDL reduction: 15%

·         Triglyceride reduction: 35%

·         Examples: Gemfibrozil, fenofibrate, fenofibrate (micronized), fenofibric acid

·         Contraindications: Active liver disease, renal disease, primary biliary cirrhosis, gallbladder disease

2-Azetidiones

These agents inhibit sterol transporter at brush border and, consequently, intestinal absorption of cholesterol.

·         LDL reduction: 15%

·         Examples: Ezetimibe

·         Contraindications: Hypersensitivity, coadministration with statins (if active liver disease)

Bile acid sequestrants

These agents lower cholesterol and LDL via bile duct sequestration.

·         LDL reduction: 15%

·         Examples: Cholestyramine, colesevelam, colestipol

·         Contraindications: Biliary/bowel obstruction, serum triglycerides >500 mg/dL, history of hypertriglyceridemia-induced pancreatitis

Apolipoprotein B antisense oligonucleotide

These agents target messenger RNA for apolipoprotein B (apoB)–100, the principal apolipoprotein of LDL and its metabolic precursor, VLDL.

·         Reduces LDL, ApoB, total cholesterol (TC), and non-HDL cholesterol

·         Example: Mipomersen

·         Contraindications: Hypersensitivity, moderate-to-severe hepatic impairment or active liver disease including persistent increased levels of serum transaminases

MTP inhibitor

These agentsdirectly bind and inhibit microsomal triglyceride transfer protein (MTP), thereby preventing ApoB-containing lipoproteins.

·         Reduces LDL, TC, ApoB, and non-HCL cholesterol

·         Example: Lomitapide

·         Contraindications: Pregnancy, coadministration with strong CYP3A4 inhibitors (lomitapide exposure increased 27-fold), moderate-to-severe hepatic impairment or active liver disease including persistent increased levels of serum transaminases

Omega 3 acids

These agents inhibit acyl CoA:1,2-diacylglycerol acyltransferase.

·         Reduces non-HCL cholesterol, ratio of total cholesterol to HDL-C, VLDL, Apo-C, phospholipase A2, and arachidonic acid

·         Examples: Omega 3 fatty acids, omega 3 carboxylic acids, icosapent

·         Contraindications: Hypersensitivity

Reference:

Author

Buck Christensen Medscape Editorial Staff

Specialty Editor Board

Mary L Windle, PharmD Adjunct Associate Professor, University of Nebraska Medical Center College of Pharmacy; Editor-in-Chief, Medscape Drug Reference