Alirocumab
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Information about Alirocumab
Alirocumab is a human monoclonal antibody to PCSK9 (proprotein convertase subtilisin/kexin type 9), a circulating protein that modulates the activity of the LDL cholesterol receptor in the liver. The monoclonal antibody lowers serum LDL cholesterol and is used to treat severe hypercholesterolemia. Alirocumab therapy has been associated with a low rate of serum aminotransferase elevations and has yet to be linked to instances of clinically apparent acute liver injury.
Mechanism of action of Alirocumab
Alirocumab (al" i rok' ue mab) is a human IgG1 monoclonal antibody to proprotein convertase subtilisin/kexin type 9 (PCSK9), a serine protease that decreases the activity of the LDL cholesterol receptor in the liver. Inhibition of PCSK9 increases the low density lipoprotein (LDL) cholesterol receptor, leading to an increased uptake of LDL particles and a decrease in serum LDL cholesterol. Patients with a genetic deficiency in PCSK9 have low levels of LDL cholesterol, and inhibition of the protein activity with monoclonal antibody leads to a marked lowering of LDL cholesterol. In several controlled trials, alirocumab was shown to lower LDL cholesterol in persons with heterozygosity for familial hypercholesterolemia and in persons at risk for atherosclerosis who have been unable to achieve adequate cholesterol lowering with standard lipid lowering agents (statins). Alirocumab
FDA approval information for Alirocumab
Alirocumab was approved for use in the United States in 2015. The current indications are limited to patients with severe hypercholesterolemia who are heterozygous for familial hypercholesterolemia or who have had clinical complications of atherosclerosis and an inadequate response to standard therapies. Alirocumab should be given in combination with advice on diet and exercise and is usually used in combination with oral lipid lowering agents such as statins. Alirocumab is available in solution in single use syringes or pens of 75 or 150 mg/mL under the brand name Praluent.
Dosage and administration for Alirocumab
The recommended initial dose is 75 mg administered subcutaneously every two weeks, which can be raised to 150 mg every two weeks based upon tolerance and response.
Side effects of Alirocumab
Side effects are uncommon and rarely serious, but include injection site reactions (7%) and myalgia (4%). Rare, but potentially serious side effects may include memory impairment, neurocognitive defects, confusion and hypersensitivity reactions.
Lipid lowering medications
- Niacin (Nicotinic Acid)
- Miscellaneous
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