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%
·
Contraindications:
Hypersensitivity, active liver disease, pregnancy, lactation, coadministration
with strong CYP3A4 inhibitors (selected statins)
Vitamin B3 inhibits
very-low-density lipoprotein (VLDL) synthesis.
·
LDL
reduction: 10%
·
High-density
lipoprotein (HDL) increase: 20%
·
Contraindications:
Hypersensitivity, liver disease, active peptic ulcer, severe hypotension,
arterial bleeding
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%
·
Contraindications:
Active liver disease, renal disease, primary biliary cirrhosis, gallbladder
disease
These agents inhibit
sterol transporter at brush border and, consequently, intestinal absorption of
cholesterol.
·
LDL
reduction: 15%
·
Contraindications:
Hypersensitivity, coadministration with statins (if active liver disease)
These agents lower
cholesterol and LDL via bile duct sequestration.
·
LDL
reduction: 15%
·
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
·
Contraindications:
Hypersensitivity, moderate-to-severe hepatic impairment or active liver disease
including persistent increased levels of serum transaminases
These agentsdirectly bind
and inhibit microsomal triglyceride transfer protein (MTP), thereby preventing
ApoB-containing lipoproteins.
·
Reduces
LDL, TC, ApoB, and non-HCL cholesterol
·
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
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
·
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
