Alirocumab (Subcutaneous)

As a monoclonal antibody belonging to a class of drugs known as PCSK9 inhibitors, Alirocumab is administered by subcutaneous injection to treat high cholesterol.

Overview

Alirocumab, which is often marketed as Praluent, helps to lower cholesterol in patients suffering from atherosclerotic heart disease or heterozygous familial hypercholersterolemia, which are both heart diseases that require LDL-cholesterol to be lowered in order to avoid a potentially harmful build-up of plaque inside the arteries.

By preventing the build-up of cholesterol in the body, the use of Alirocumab makes it easier for patients to function in their daily lives. It can be used in conjunction with a low-cholesterol diet and statins, or as a stand-alone treatment on the recommendation of a doctor.

It is not currently known whether Alirocumab is effective in preventing early death from cardiovascular disease or heart attacks. The drug can also be used off-label as directed by a qualified physician.

Conditions treated

  • High cholesterol
  • Atherosclerotic heart disease
  • Heterohygous familial hypercholersterolemia

Type of medicine

  • Monoclonal antibody

Side effects

Along with the required effects, Alirocumab can also cause unwanted side effects. The most common side effects reported by patients undergoing treatment with this medication include fever, nausea, hives, difficulty breathing or swallowing, reddening of the skin (in particular around the ears), swelling of the face, eyes or inside of the nose, unusual tiredness, weakness, a mucus-producing cough and tightness in the chest.

Most, if not all, of these effects are likely to dissipate the longer the patient takes the medicine, as the body takes time to adjust to it. If any these temporary side effects are causing particular discomfort, the patient is advised to contact their healthcare professional in order find out about ways in which these side effects can be reduced.

The most common side effects and adverse reactions which lead to discontinuation of treatment include allergies and elevated liver enzymes. Some patients have been advised to discontinue Alirocumab use due to hypersensitive reactions including eczema and vasculitis. Others have been forced to stop treatment due to respiratory issues including nasopharyngitis, bronchitis, sinusitis and forms of influenza.

Other side effects associated with the use of Alirocumab could potentially be more serious. If you experience any of the following side effects, you should contact your doctor who may advise a different course of treatment:

  • Diarrhea
  • Generally feeling unwell
  • Headaches
  • Muscle aches and pains
  • Shivering
  • Vomiting
  • Redness, itching or swelling at the site of injection
  • Chills

Exceptionally rare side effects and reactions to Alirocumab include:

  • Bladder pain
  • Cloudy or bloody urine
  • A frequent urge to urinate
  • Tenderness and pain around the cheekbones
  • Swollen joints
  • Difficulty moving
  • Muscle spasms

Although these reactions are less frequent, patients who experience discomfort in these forms are advised to contact a qualified health professional for advice.

Dosage

As with all medications, it is imperative that patients only take Alirocumab as directed by a qualified physician. This means that patients should not take a larger dose than advised, and to only take doses at the prescribed frequency. Patients should also stop taking Alirocumab if advised to by a doctor, even if they have a supply of the medicine remaining.

Alirocumab is available in 2 different dosage strengths; 75mg and 150mg, and is administered via subcutaneous injection. The typical starting dose, as prescribed by a doctor, begins at 75mg every 2 weeks. If the desired effect in the patient is not achieved, the dose can be increased every 2 weeks to a maximum of 300mg until an adequate dose is found.

This medication should be administered into the abdomen, thigh or upper am using a single-dose pre-filled syringe or pen. The injection site should be rotated - this means that every two weeks a different injection site should be chosen in order to avoid tissue damage and to ensure varied application. It should not be co-administered with other intravenous or subcutaneous injectable drugs at the same injection site.

Alirocumab inhibits the PCSK9 protein. The PCSK9 protein binds to the LDLR (low density lipoprotein receptor) which takes cholesterol out circulation in the body. This binding then leads to the downgrading of the receptor, resulting in less LDL cholesterol being removed from circulation. By inhibiting the PCSK9 protein, Alirocumab stops the receptor from being downgraded and ultimately prompts further removal of LDL cholesterol.

Before administering Alirocumab, it should be allowed to warm up to room temperature for at least 30 to 40 minutes prior to use. However, if the drug has been at room temperature for 24 hours or longer, it should not be used. The solution should be inspected for discoloration and particulate matter prior to administration. If discoloration and/or particulate matter is present, it should not be used and should be disposed of immediately.

If patients are self-administering this drug or arranging for home carers/relatives to administer it, correct training on the preparation and administration of the drug should be provided, outlining the risks of incorrectly injecting Alirocumab. The injections should be carefully read by non-professional drug administrators every time the drug is used.

In the event of a missed dose, the injection should be administered within 7 days from the missed dose, before returning to the original patient schedule. If the dose cannot be administered within 7 days, the patient should wait until the next dose and continue with the original schedule.

Interactions

There are currently no known drug interactions pertaining to Alirocumab. However, this does not mean that no interactions exist, and patients who feel that this medicine may be interacting with other prescription medications, OTC remedies or supplements they are currently taking are advised to report their concerns to the FDA.

As with all medications, Alirocumab may interact with other drugs or chemicals within the body. As a result, the medicine can be rendered ineffective, and in some instances, it can cause potential harmful interactions. For these reasons, it is imperative that patients keep a detailed list of all medication they are currently taking - including over the counter remedies, herbal supplements and vitamins.

Warnings

Patients should discuss their personal medical history (including any previous or ongoing health problems) before commencing with Alirocumab treatment. Patients who suffer from allergies should be aware that Alirocumab may contain inactive ingredients which have a propensity to cause allergic reactions.

In some instances, patients have reported hypersensitivity reactions including urticaria, pruritus and vasculitis, which have required hospitalization. In the event of any serious symptoms of hypersensitivity occurring, patients are advised to discontinue treatment with Alirocumab and monitor the condition until symptoms have resolved themselves.

Patients and caregivers should be trained on proper subcutaneous injection techniques involving pre-filled syringes and pens in order to ensure that the medication is correctly administered, and to avoid injuries.

During pregnancy, this medication should only be used if and when clearly required. Patients are advised to discuss the risks with their doctor, who will be able to come to a conclusion as to whether they outweigh the benefits.

It is currently unknown whether Alirocumab is passed into breast milk. Standard advice when no data exists is to proceed with caution when breastfeeding, and to discontinue use of the medication on the advice of your doctor.

In the event of a patient taking too much Alirocumab, they should contact a doctor or healthcare professional, particularly if they are experiencing side effects such as shivering, vomiting, sore skin or general hypersensitivity. If side effects are uncomfortable or unbearable, the patient is urged to contact their local poison control center on 1-800-222-1222 or the emergency services on 911.

Storage

Alirocumab is supplied as a clear, colorless solution supplied in single dose, pre-filled syringes and pens. Each single-use dose is designed to deliver 1mL of 75mg/mL or 1mL of 150mg/mL of the solution.

This medicine should optimally be stored in a medical refrigerator at a temperature between 2C and 8C. The refrigeration unit should have a solid door in order to protect the solution from light. If required, Alirocumab can be kept at standard room temperature (25C) for a total of 30 days, in its original carton to protect it from light. Alirocumab is not suitable for freezing, and should not be shaken or exposed to extreme heat, as this can risk damaging the product or otherwise making it unsuitable and potentially hazardous to inject. Containers of this medicine which have been removed from the refrigerator should be used within 30 days. If the solution is not used within the timeframe, it should be safely discarded.

When disposing of unwanted or unused Alirocumab syringes and pens, patients should take great care to ensure that pets, children or other adults cannot access the drug or accidentally end up taking a dose of it. Syringes have the potential to cause injury, and should therefore be disposed of under the directions of a pharmacist or health professional. Many drug stores offer needle exchange schemes where used and unused sharps can be deposited, where they will be disposed of in a safe and hygienic manner. For further information on how to dispose of unwanted medicines, patients are advised to contact their local waste collection provider for advice.

Summary

Alirocumab is an effective means of reducing cholesterol, and can be used in conjunction with or without a special diet or as an alternative to statins in tablet form. While the drug is a convenient way to provide the body with a dose of monoclonal antibodies which help to collect excess cholesterol, patients are advised that due to the manufacturing processes and ingredients used, some allergens may be present and could potentially cause harmful side effects.

While results are typically satisfactory, Alirocumab may not be a cost-effective treatment for some patients. An annual course of this medicine can cost upwards of $14,000 in comparison to relatively cheap statin tablets, although it may be of interest to patients who for one reason or another are unable to take statins in pill form (due to allergies or an aversion to taking tablets, for example).

High cholesterol has the potential to build up within the body and cause blockages and hardening within the artery walls. If left untreated, this can lead to heart disease which is a potentially fatal condition. Therefore, Alirocumab is considered useful in preventing the development of heart disease, and when used in tandem with healthier lifestyle changes such as the reduced consumption of saturated fats, an increase in physical activity and weight loss it offers the best possible defence against these diseases and conditions.

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Last Reviewed:
December 10, 2017
Last Updated:
April 04, 2018
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