Alirocumab - An Adjunct Treatment for High Cholesterol Levels

What Is Alirocumab?

Alirocumab is a medicine that helps lower bad cholesterol when healthy food and other medicines do not work well enough. It is often used for people who are born with very high cholesterol or have heart problems. This medicine helps the body clean extra cholesterol from the blood, which can protect the heart and lower the chance of heart attacks and strokes.

Is Alirocumab FDA-approved?

Yes, Alirocumab received FDA (the United States Food and Drug Administration) approval as a second-line intervention to reduce cholesterol levels in July 2015. The FDA approval was bound by extensive clinical trials determining its safety and efficacy.

In 2021, the FDA included Alirocumab for the indication of treating adults with heterozygous familial hypercholesterolemia (a heritable condition of high cholesterol). Nevertheless, the drug is not meant to be given alone but in conjunction with other interventions.

How Does Alirocumab Work?

• Alirocumab is given as an injection under the skin (subcutaneous injection).

• It belongs to a group of medicines called PCSK9 (proprotein convertase subtilisin/kexin type 9) inhibitors.

• Alirocumab blocks an enzyme called PCSK9, which is made by the liver.

• PCSK9 normally increases bad (LDL) cholesterol levels in the blood.

• By blocking PCSK9, alirocumab helps the body remove more LDL cholesterol.

• This lowers cholesterol buildup in blood vessels (atherosclerosis).

• It also helps reduce blood clot formation.

• When used in the right dose along with a healthy diet, alirocumab helps prevent heart attacks and other heart-related problems.

Uses of Alirocumab:

• Homozygous Familial Hypercholesterolemia: A genetic condition where people have very high bad (LDL) cholesterol from birth. It often shows up at a young age (20 to 40 years) and happens because of a change in a gene.

• Cardiovascular Events: When cholesterol builds up in artery walls, it can cause heart attacks, strokes, and chest pain (angina).

• Primary Hyperlipidemia: A genetic disorder that causes high fat (lipid) levels in the blood, increasing the risk of heart disease and repeated attacks of pancreatitis.

How Is Alirocumab Given?

• Given as an injection just under the skin (subcutaneous).

• Administered using a pre-filled pen with the medicine ready to use.

• Given every 2 or four weeks, depending on the prescribed dose.

Alirocuman Dosage:

Homozygous Familial Hypercholesterolemia

• In Adults, 50 mg subcutaneous injection is given once every two weeks.

Primary Hyperlipidemia and Reducing the Risk of Cardiovascular Events

• Every 2-Week Dose: 75 mg subcutaneous injection is given once every two weeks. The dosage is increased depending on the patient's response.

• Every Four Weeks: 300 mg subcutaneous injection is administered once every four weeks. The dose adjustments are recommended based on clinical evaluation.

Precaution: The maximum dosage should not be increased by more than 150 mg every two weeks.

How Effective Is Alirocumab?

Alirocumab is a safe, sound, and efficient drug. Studies and interventions uncover that Alirocumab injection significantly lowers LDL cholesterol levels, along with dietary consideration and statin therapy. And higher doses result in profound LDL reductions.

What Are the Warnings and Precautions for Alirocumab?

In many instances, Alirocumab might result in severe and life-threatening hypersensitivity reactions called anaphylaxis. Discontinue the treatment and seek out a doctor if one encounters signs of allergic reactions. The symptoms include rashes, hives, swelling, and difficulty breathing. Also, one with a history of allergy should not recommence the therapy.

For Patients

What Are the Things to Inform the Doctor Before Taking Alirocumab?

• Tell your doctor if you are allergic to Alirocumab or any other ingredients in the medicine.

• Inform your doctor about all medicines, vitamins, or herbal supplements you are taking, so the dose can be adjusted and side effects monitored.

• Share your current and past health conditions with your doctor.

• Tell your doctor if you are planning to become pregnant, pregnant, or breastfeeding.

• Consult your doctor if you become pregnant while using Alirocumab.

Directions for Alirocumab Injection:

• Carefully read the instructions that come with the pen or syringe.

• Take the syringe out of the refrigerator and let it warm to room temperature for 30 to 40 minutes.

• Do not heat it in hot water. Use the syringe within 30 days of taking it out. Do not shake the medication.

• Check that the liquid is clear and has no particles; do not use it if it looks discolored or damaged.

• Avoid using a damaged syringe, pen, or cap. Clean the injection area with alcohol.

• Remove the cap carefully and inject slowly and gently as your doctor instructed. After injection, dispose of the needle safely.

Important:

Use the Alirocumab injection as per the physician’s instructions. One should not use the medication more or less than the prescribed dosage. Also, the therapy should not be continued for a longer span than advised.

Drug Storage:

• Store the Alirocumab syringe or pen in the refrigerator, but do not freeze.

• The injection can be stored with its actual carton at room temperature (up to 77 degrees Fahrenheit) for up to 30 days.

• Also, use the medication within 30 days after being withdrawn from the refrigerator.

• Dispose of any outdated or unused medication safely.

• The medication should be kept out of reach of children.

Drug Disposal:

• Firstly, discard the used needles in a rigid, tight container so the needles cannot poke out.

• Then, safely dispose of them in a way that prevents the children, companions, and pets from reaching the used needles.

• The syringe and dosing pen should not be flushed in the toilet, thrown in the community garbage, or poured into the channel.

• Instead, dispense safely following the local and state laws.

What Should Be Done When a Dose Is Missed?

Every Two Weeks

• If It Is Within the Range of Seven Days of the Missed Dose - For people who miss the dose based on medication every two weeks, take the injection right after the thought. Then, recommence with the actual schedule.

• If It Exceeded Seven Days From the Missed Dose - In this case, skip the missed dose and look for the succeeding date of the regular schedule.

Every Four Weeks

• If It Is Within the Range of Seven Days of the Missed Dose: One can inject the missed dose as soon as they think of it and then restart with the original checklist.

• If It Exceeded Seven Days From the Missed Dose: Inject the missed dose and commence a new four-week schedule from this day.

Nevertheless, one should refrain from injecting the double dose as compensation for the missed one. Instead, seek a doctor in case of doubts.

Side Effects:

Pain, redness, swelling, or itching at the injection site is common, though. In addition, Alirocumab has several side effects, which usually subside with the drug therapy as the body adapts. Nevertheless, seek professional help if these signs persist and are distressing.

Side Effects of Alirumab:

• Bleeding, bruising, redness, swelling, hives, numbness, infection, itching, inflammation, scarring, rashes, soreness, burning, and ulceration at the injection site.

• Cough.

• Chills.

• Diarrhea.

• Headache.

• Loss of appetite.

• Muscle spasms, pain, and cramps.

• Sore throat.

• Unusual sweating.

• Shivering.

• Vomiting.

• Insufficient sleep.

• Flu-like symptoms.

In addition, people may experience certain harmful signs that require medical attention at the earliest. So, reach out to the doctor if one has any of the following.

• Chest pain or discomfort.

• Trouble breathing or swallowing.

• Rapid heartbeat.

• Itching, hives, or skin rashes.

• Irritation.

• Dry hoarseness of voice.

• Pain, stiffness, or swelling of the joints.

• Unusual fatigue.

• Nausea.

• Swelling of face, lips, arms, or eyelids.

• Skin redness, particularly of the ears.

In Cases of Emergency or Overdosage:

Alirocumab overdose leads to dangerous levels of the drug held in the system. The alarming signs include collapse, seizure, difficulty breathing, and inability to wake. Reach out to the doctor or emergency helpline immediately when excessive amounts of the drug are injected.

For Doctors:

Indications

• Reducing the risk of hospitalization with certain cardiovascular events, such as myocardial infarction, unstable angina, and stroke, in those adults with prevailing cardiovascular disease.

• For lowering low-density lipoprotein (LDL) cholesterol levels in the body as an adjunct drug with other LDL-C therapies, including in the treatment of heterozygous familial hypercholesterolemia.

• Alirocumab alone or in conjunction with lipid-lowering agents is indicated and used as an adjunct to diet in the management of primary hyperlipidemia.

Contraindications of Alirocumab

Alirocumab is strictly contraindicated in people with a history of severe hypersensitivity reactions to Alirocumab.

• Hypersensitivity vasculitis.

• Angioedema.

• Hypersensitivity requiring hospitalization.

Pharmacology of Alirocumab

Mechanism of Action

Alirocumab is a human monoclonal antibody. Means it is a type of laboratory-made protein that targets a specific molecule in the body. It works by blocking an enzyme called PCSK9, which is often overactive in people with familial or genetic high cholesterol.

Normally, PCSK9 attaches to LDL receptors in the liver and causes them to break down, so the liver can’t remove LDL cholesterol from the blood effectively. By inhibiting PCSK9, alirocumab allows the liver to recycle LDL receptors and remove more LDL cholesterol from the blood, increasing cholesterol clearance.

Pharmacodynamics

Alirocumab diminishes the levels of PCSK9 depending on the concentration.

Absorption

• Alirocumab is administered subcutaneously and absorbed into the bloodstream.

• The maximum concentrations (Peak plasma time) were reached within an average time of three to seven days.

• The absolute bioavailability after subcutaneous administration is 85 percent.

Distribution

• Alirocumab is chiefly and widely distributed through the circulatory system.

• Extravascular distribution is minimal.

• The volume of distribution is 0.04 to 0.05 L/kg.

Metabolism

• Specified metabolism studies for Alirocumab have not yet been conducted.

• Preliminary data show that Alirocumab is a protein, and it gets metabolized and degraded into small peptides and distinctive amino acids.

Elimination

Monoclonal antibodies are not excreted by means of hepatic or renal pathways.

Drug Interactions

The studies show that Alirocumab has no reported mild, moderate, or severe drug interactions with other drugs, herbal supplements, or food. Nevertheless, the risk of adverse effects can be increased with certain medications.

Clinical Trial

A clinical study was done with many participants to see how well Alirocumab lowers LDL (bad) cholesterol. The study was randomized, placebo-controlled, and double-blind (participants were randomly assigned to groups, some received a fake treatment, and neither the participants nor the researchers knew who got the real medicine).

Alirocumab was used along with other treatments, like diet changes or statins. After 12 weeks, the results were compared between the group receiving Alirocumab and the placebo group in patients with high cholesterol.

Results

Clinical trials have shown that Alirocumab effectively lowers cholesterol. Data from 12 randomized controlled trials with around 6,019 patients demonstrated that Alirocumab significantly reduces LDL-C (bad cholesterol) and improves HDL-C (good cholesterol) levels.

Other Specifications

• Pregnancy: There is not enough information to know how Alirocumab affects pregnant women or babies.

• Breastfeeding: There are limited data on the effects of Alirocumab on infants. Doctors weigh the benefits and risks before prescribing it to breastfeeding mothers.

• Children: Alirocumab has not been tested in children, so its safety and effectiveness in this age group are unknown.

• Older Adults: Studies do not show major problems in elderly patients, but older people may be more sensitive, so doctors monitor them carefully.