Antihyperlipidemics - Miscellaneous: Nursing pharmacology

Antihyperlipidemics are medications used to treat clients with dyslipidemia, which refers to increased blood levels of lipids, such as cholesterol and triglycerides. In addition, they’re indicated to decrease the risk of cardiovascular events. Antihyperlipidemics include different classes of medications, including niacin, also known as vitamin B3 or nicotinic acid; PCSK9 inhibitors, like alirocumab and evolocumab; and omega-3 fatty acids, like icosapent and fish oil.

Let’s start with niacin, which is taken orally. Once administered, it works by inhibiting the enzyme lipoprotein lipase in adipose tissue, which decreases the release of free fatty acids into the bloodstream. As a result, there’s less fatty acids available for the liver to produce triglycerides. For that reason, niacin is primarily used to treat hypertriglyceridemia. LO1-LO3

Now, a common side effect is “niacin flush,” which leads to a red, flushed face, and pruritus. Clients may also experience headaches, dizziness, insomnia, and paresthesia or a sensation of pins and needles, as well as gastrointestinal side effects, including abdominal pain, nausea, vomiting, diarrhea, or flatulence. Other side effects include hyperglycemia, hyperuricemia, and hepatitis with increased blood transaminases.

Niacin is contraindicated in clients with active hepatic disease or peptic ulcer disease, as well as in those with arterial hemorrhage. Caution should be taken during pregnancy and breastfeeding, as well as in clients with cardiovascular disease, diabetes, or gout. Additional precautions should be taken in clients with hepatic or renal impairment, as well as in those who consume large amounts of alcohol.

Next, we have PCSK9 inhibitors, like alirocumab and evolocumab, which are monoclonal antibodies administered via subcutaneous injection. Once administered, these medications target the PCSK9 protein that’s normally secreted by liver cells and binds to LDL receptors on the cell’s surface, causing them to be uptaken and broken down intracellularly. PCSK9 inhibitors bind to these proteins to prevent LDL receptor breakdown. This mechanism increases the overall quantity of LDL receptors on liver cells and thus causes a large decrease in LDL in the bloodstream, which is sometimes referred to as “bad” cholesterol, while providing a slight increase in HDL, which is sometimes referred to as “good” cholesterol. For that reason, these medications are used to treat familial hypercholesterolemia and atherosclerotic disease.

Side effects include local injection site reactions, and hypersensitivity reactions. Some clients may also present with flu-like symptoms, cough, diarrhea, and hepatic side effects like increased blood transaminases, as well as muscle spasms and myalgia. There are no major contraindications, but they should be used cautiously during pregnancy and breastfeeding.

Finally, there’s omega-3 fatty acids like icosapent and fish oil, which are taken orally. Once absorbed into the bloodstream, these medications act by decreasing lipogenesis in the liver, which ultimately reduces the production of VLDLs. In addition, omega-3 fatty acids also increase the activity of lipoprotein lipase, which subtracts triglycerides from VLDLs, decreasing its levels in the blood. So, overall, these medications help decrease VLDL levels.

Common side effects of omega-3 fatty acids include abdominal pain, constipation, or diarrhea, as well as myalgia and arthralgia, and gout. Some clients may also present with more serious side effects, such as hemorrhage, especially in those who take anticoagulant or antiplatelet medications; as well as cardiovascular side effects like arrhythmias or peripheral edema. Omega-3 fatty acids have no major contraindications, but they should be used with caution in clients who are allergic to fish or shellfish, as well as in clients with coagulopathy or hepatic impairment. Precautions should also be taken during pregnancy and breastfeeding.