What is alirocumab, and how does it work (mechanism of action)?
Alirocumab is a man-made injectable drug that reduces cholesterol levels in the blood. It is the first member of a new class of drugs called proprotein convertase subtilisin kexin type 9 (PCSK9) inhibitors. Cholesterol is carried in the blood to a large extent by particles of low density lipoproteins that are removed from the blood by liver cells. The particles are removed from the blood by low-density lipoprotein receptors (LDLR) on liver cells. PCSK9 is a protein on liver cells that promotes the destruction of LDLR. Therefore, a decrease in LDLR levels by PCSK9 results in higher blood levels of LDL cholesterol.
Alirocumab is an antibody, which means that it is a protein that binds to another protein and inactivates it. Alirocumab binds to the PCSK9 protein and prevents it from destroying LDLR. By inhibiting PCSK9, Alirocumab increases the number of LDLRs available to remove LDL cholesterol and consequently reduces LDL cholesterol levels in blood. The FDA approved alirocumab in July 2015.
What brand names are available for alirocumab?
Is alirocumab available as a generic drug?
Do I need a prescription for alirocumab?
What are the side effects of alirocumab?
The most common side effects associated with alirocumab treatment include
Other side effects include
Liver problems were reported in 2.5% of patients treated with alirocumab compared to 1.8% in patients treated with placebo.
What is the dosage for alirocumab?
The recommended starting dose of alirocumab is 75 mg via subcutaneous injection (into the fat layer underneath the skin) every 2 weeks. If the LDL cholesterol lowering response is not adequate with this starting dose, the dosage may be increased to a maximum dosage of 150 mg every 2 weeks. LDL cholesterol levels should be measured within 4 to 8 weeks of starting therapy to assess response to treatment, and a decision should be made whether or not to adjust the dose.
Alirocumab should only be injected by subcutaneous injection into the thigh, abdomen, or upper arm. Injection sites should be rotated with each injection to prevent or reduce injection site reactions and irritation. Alirocumab should not be co-administered with other injectable drugs at the same injection site.
Which drugs or supplements interact with alirocumab?
No clinically significant drug-drug interactions are listed for alirocumab.
Is alirocumab safe to take if I'm pregnant or breastfeeding?
There is no data on the use of alirocumab in pregnant women.
It is not known if alirocumab can enter human milk or cause harm to the nursing infant.
What else should I know about alirocumab?
What preparations of alirocumab are available?
Single dose pre-filled pens and single-dose pre-filled glass syringes, each designed to deliver 1 ml of 75 mg/ml or 150 mg/ml.
How should I keep alirocumab stored?
Alirocumab should be stored in the refrigerator at 2 C to 8 C (36 F to 46 F) and protected from light and extreme heat. It should not be frozen.
Alirocumab (Praluent) ia man-made prescription drug prescribed in addition to exercise, diet, and statin drugs to reduce LDL cholesterol levels adults with heterozygous familial hypercholesterolemia or adults with heart problems related to excess cholesterol in the body. Alirocumab is the first member of a new class of drugs called (PCSK9) proprotein convertase subtilisin kexin type 9 inhibitors. Side effects, drug interactions, dosing, storage, and pregnancy and breastfeeding safety information is provided.
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Related Disease Conditions
High cholesterol and triglyceride levels increase the risk of cardiovascular disease. Getting your cholesterol and triglyceride levels in an optimal range will help protect your heart and blood vessels. Cholesterol management may include lifestyle interventions (diet and exercise) as well as medications to get your total cholesterol, LDL, HDL, and triglycerides in an optimal range.
Lower Cholesterol Levels with Diet and Medications
High-density lipoprotein (HDL) cholesterol is considered "good" cholesterol because it actually works to keep the LDL or "bad" cholesterol from building up in your arteries. Foods like extra lean meats, skim milk, and vegetable-based "butter-like" substitutes may help decrease LDL levels in the bloodstream.
Heart disease (coronary artery disease) occurs when plaque builds up in the coronary arteries, the vessels that supply blood to the heart. Heart disease can lead to heart attack. Risk factors for heart disease include: Smoking High blood pressure High cholesterol Diabetes Family history Obesity Angina, shortness of breath, and sweating are just a few symptoms that may indicate a heart attack. Treatment of heart disease involves control of heart disease risk factors through lifestyle changes, medications, and/or stenting or bypass surgery. Heart disease can be prevented by controlling heart disease risk factors.
Heart Disease in Women
Heart disease in women has somewhat different symptoms, risk factors, and treatment compared to heart disease in men. Many women and health professionals are not aware of the risk factors for heart disease in women and may delay diagnosis and treatment. Lifestyle factors such as diet, exercise, tobacco use, overweight/obesity, stress, alcohol consumption, and depression influence heart disease risk in women. High blood pressure, high cholesterol, and diabetes also increase women's risk of heart disease. Electrocardiogram (EKG or ECG), stress-ECG, endothelial testing, ankle-brachial index (ABI), echocardiogram, nuclear imaging, electron beam CT, and lab tests to assess blood lipids and biomarkers of inflammation are used to diagnose heart disease. Early diagnosis and treatment of heart disease in women saves lives. Heart disease can be prevented and reversed with lifestyle changes.
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