Alirocumab

Alirocumab (Praluent) is a PCSK9 (proprotein convertase subtilisin kexin type 9) inhibitor used to treat certain patients with high cholesterol.

What are the uses of this medicine?

This medicine is used:

• in adults with cardiovascular disease to reduce the risk of heart attack, stroke, and certain types of chest pain conditions (unstable angina) requiring hospitalization.
• along with diet, alone or together with other cholesterol-lowering medicines in adults with high blood cholesterol levels called primary hyperlipidemia (including a type of high cholesterol called heterozygous familial hypercholesterolemia), to reduce low-density lipoprotein cholesterol (LDL-C) or bad cholesterol.
• along with other LDL-lowering treatments in adults with a type of high cholesterol called homozygous familial hypercholesterolemia, who need additional lowering of LDL-C.

How does this medicine work?

• 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).

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• a history of a serious hypersensitivity reaction to alirocumab or any of the excipients in Praluent.

What drug interactions can this medicine cause?

• No clinically important drug interactions have been observed with Praluent.

Is this medicine FDA approved?

• It was approved for use in the United States in 2015.

How should this medicine be used?

Recommended Dosage: In adults with established cardiovascular disease or with primary hyperlipidemia, including HeFH

• The recommended starting dose of Praluent is either 75 mg once every 2 weeks or 300 mg once every 4 weeks administered subcutaneously.
• For patients receiving Praluent 300 mg every 4 weeks, measure LDL-C just prior to the next scheduled dose, because LDL-C can vary between doses in some patients.
• If the LDL-C response is inadequate, the dosage may be adjusted 150 mg subcutaneously every 2 weeks.

In adults with HeFH undergoing LDL apheresis or in adults with HoFH:

• The recommended dose of Praluent is 150 mg once every 2 weeks administered subcutaneously.
• Praluent can be administered without regard to the timing of LDL apheresis.

• Assess LDL-C when clinically appropriate. The LDL-lowering effect of Praluent may be measured as early as 4 weeks after initiation.
• To administer the 300 mg dose, give two 150 mg Praluent injections consecutively at two different injection sites.

Administration

• Use Praluent exactly as your healthcare provider tells you to use it.
• Praluent comes as a single-dose (1 time) pre-filled pen (autoinjector). Your healthcare provider will prescribe the dosage that is best for you.
• If your healthcare provider decides that you or a caregiver can give the injections of Praluent, you or your caregiver should receive training on the right way to prepare and give Praluent. Do not try to inject Praluent until you have been shown the right way by your healthcare provider or nurse.
• Praluent is injected under the skin (subcutaneously) every 2 weeks or every 4 weeks (monthly).
• If your healthcare provider prescribes you the monthly dose, you will give yourself 2 separate injections in a row, using a different pen for each injection and 2 different injection sites.
• Do not inject Praluent together with other injectable medicines at the same injection site.
• Always check the label of your pen to make sure you have the correct medicine and the correct dose of Praluent before each injection.
• If you forget to use Praluent or are not able to take the dose at your regular time, inject your missed dose as soon as you remember, within 7 days. Then, if you inject every 2 weeks take your next dose in 2 weeks from the day you missed your dose or if you inject every 4 weeks take your next dose in 4 weeks from the day you missed your dose. This will put you back on your original schedule.
• If you missed a dose by more than 7 days and you inject every 2 weeks wait until your next scheduled dose to re-start Praluent or if you inject every 4 weeks start a new schedule from the time you remember to take your dose.
• If you are not sure when to re-start Praluent, ask your healthcare provider or pharmacist.
• If you use more Praluent than you should, talk to your healthcare provider or pharmacist.
• Do not stop using Praluent without talking with your healthcare provider. If you stop using Praluent, your cholesterol levels can increase.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Injection: 75 mg/mL or 150 mg/mL in a single-dose pre-filled pen

This medicine is available in fallowing brand namesː

• Praluent

What side effects can this medication cause?

The most common side effects of this medicine include:

• redness, itching, swelling, pain, or tenderness at the injection site
• symptoms of the common cold
• flu or flu-like symptoms

Praluent can cause serious side effects, including:

• allergic reactions

What special precautions should I follow?

• Hypersensitivity reactions, including hypersensitivity vasculitis, angioedema, and other hypersensitivity reactions requiring hospitalization, have been reported with Praluent treatment. If signs or symptoms of serious hypersensitivity reactions occur, discontinue treatment with Praluent, treat according to the standard of care, and monitor until signs and symptoms resolve.

What to do in case of emergency/overdose?

In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• Available data from clinical trials and postmarketing reports on Praluent use in pregnant women are insufficient to evaluate for a drug-associated risk of major birth defects, miscarriage or other adverse maternal or fetal outcomes.

Can this medicine be used in children?

• The safety and effectiveness of Praluent have not been established in pediatric patients.

What are the active and inactive ingredients in this medicine?

• Active ingredient: alirocumab
• Inactive ingredients: histidine, polysorbate 20, sucrose, and Water for Injection, USP.

Who manufactures and distributes this medicine?

• Manufactured by:
• sanofi-aventis U.S. LLC, Bridgewater, NJ 08807; A SANOFI COMPANY

What should I know about storage and disposal of this medication?

• Store in a refrigerator at 36°F to 46°F (2°C to 8°C) in the original carton to protect from light.
• Do not freeze.
• Do not shake.
• Praluent may be kept at room temperature up to 77°F (25°C) in the original carton for 30 days.
• If not used within the 30 days, discard Praluent.

• Dailymed label info on Alirocumab
• FDA Alirocumab