Products
Lipid-lowering agents are mainly sold as tablets and capsules as monopreparations and combination preparations. Some other dosage forms exist, such as granules and injectables. Statins have established themselves as the most important group at present.
Structure and properties
The chemical structure of lipid-lowering agents is inconsistent. However, within the class, groups with comparable structures can be identified (see below).
Effects
The agents have lipid-lowering properties. For example, they reduce LDL-C, VLDL, total cholesterol, triglycerides, ApoB, and increase the “good cholesterol” HDL-C. Effects include inhibition of cholesterol synthesis, interaction with nuclear receptors, inhibition of intestinal cholesterol absorption, and promotion of LDL-C receptor degradation in liver cells.
Indications
Indications for use include:
- Hypercholesterolemia
- Mixed dyslipidemia
- Hypertriglyceridemia
- For primary or secondary prevention of cardiovascular events such as myocardial infarction or stroke.
Dosage
According to the drug label. Lipid-lowering agents are usually taken perorally. PCSK9 inhibitors must be injected subcutaneously. In addition to drug therapy, a healthy diet and adequate physical activity are recommended.
Agents
Statins:
- Atorvastatin (Sortis, generic).
- Fluvastatin (Lescol, generics)
- Pitavastatin (Livazo)
- Pravastatin (Selipran, generics)
- Rosuvastatin (Crestor, generics)
- Simvastatin (Zocor, generics)
Fibrates:
- Bezafibrate (Cedur retard)
- Fenofibrate (Lipanthyl)
- Gemfibrozil (Gevilon)
Nicotinic acid and derivatives:
- Nicotinic acid (Tredaptive, out of trade).
- Acipimox (Olbetam)
Ion exchange resins:
- Colestyramine (Quantalan)
- Colestipol (Colestid)
- Resina polystyrenolica anionica fortis (divistyramine, ipocol).
Cholesterol absorption inhibitor:
MTP inhibitors:
- Lomitapide (Lojuxta)
PCSK9 inhibitors:
- Alirocumab (Praluent).
- Evolocumab (Repatha)
ATP citrate lyase inhibitors:
- Bempedoic acid (Nilemdo).
Cannabinoid antagonists:
- Rimonabant (Accomplia, out of commerce).
CETP inhibitors:
- E.g., torcetrapib (not commercially available).
Natural lipid-lowering agents, phytopharmaceuticals:
- Polyunsaturated fatty acids: omega-3 fatty acids.
- Garlic
- Artichoke
- Green tea
- Javanese turmeric
- Mucilage drugs: Indian psyllium, flaxseed, possibly also fenugreek.
- Guar
- Red mold rice (may not be distributed in many countries).
- (cinnamon)
Contraindications
Full precautions can be found in the drug label.
Interactions
Some lipid-lowering agents are substrates of CYP3A and of drug transporters. Inhibitors of this enzyme or the transporters may increase adverse effects.
Adverse effects
Potential adverse effects of lipid-lowering agents include (selection, examples from all groups):
- Indigestion
- Muscle and joint pain, muscle cramps, pain in the extremities, muscle spasms, joint swelling, back pain
- Headache
- Flush
- Hypersensitivity reactions
- Central disorders such as headaches and dizziness
- Very rarely, life-threatening disintegration of skeletal muscle may occur (rhabdomyolysis). This mainly affects the statins.
