Pcsk9 Inhibitors

What are Pcsk9 Inhibitors?

These are new drugs that are used to reduce low density lipoprotein (LPD) cholesterol in the body. They were approved in 2015 by food and drug administration. Pcsk9 inhibitors belong to a group of drugs called biologic and they are monoclonal antibodies. These inhibitors work by binding on inactivating a protein in the liver known as proprotein convertase subtilisin kexin 9 (Pcsk 9).1, 2

Pcsk 9 is a type of protein manufactured by the liver which helps to remove low density lipoprotein receptors from the liver cells. Without these receptors, cholesterol level in the blood will increase. Therefore by inhibiting Pcsk 9, more receptors are available to capture low density lipoprotein for break down in the liver and be removed from blood.

Prescription

Pcsk9 inhibitors

Pcsk9 inhibitors are recommended for people with the following:2

Familial hypercholesterolemia

This is an inherited condition that elevates low density lipoprotein cholesterol level in your blood. This condition starts at birth and can cause heart attack at an early age. This disorder is as a result of mutations on chromosome 19. This mutation makes the body unable to eliminate low density lipoprotein in the blood. As a result, it increases low lipoprotein in your blood which can narrow your arteries, a condition known as atherosclerosis. You can get this condition when you inherit a defective gene from one of the parents with this disease.3

It is uncommon for a child to receive defective genes from both parents. But when this happens, the rise in cholesterol level in the blood would be more painful.

Those unable to tolerate statins

Patients who have been using statins but are not able to tolerate it are at higher risk of heart attack and strokes.

People with heart diseases

Patients with heart diseases and have not achieved low density lipoprotein with current treatment options can use this drug.

How is Pcsk9 inhibitors taken?

Pcsk9 inhibitors are only available as an injection. Currently, there are only two forms of Pcsk9 inhibitors available in United States of America. They are Repatha and Praluent. Your doctor will first try other treatment options and monitor their effectiveness in lowering cholesterol level. If there is no change in cholesterol level, your doctor will use Pcsk9 inhibitors.1

Side Effects

Pcsk9 inhibitors can cause undesirable side effects such as:1

Patients feel pain in the muscles or limbs. They also get tired easily. Many patients complain of swellings at the place of injection. This drug can also cause severe effects such as:

Liver problems

Your liver processes medications and chemicals that come into the body and this leaves it prone to liver diseases. The chemicals in Pcsk 9 inhibitor may react with the liver leading to its damage.

Dementia

It is a general term that describes various different symptoms that reduce the mental ability and interfere with person’s day to day activities. Dementia occurs when brain cells are damaged. This affects how the brain cells communicate to each other. When communication between brain cells are disrupted, functions such as thinking, judgment, feeling, memory, movement, etc are affected.4

Each type of dementia damages a specific part of the brain cell. Side effects of medicines can cause memory and thinking problems in people. However, damage caused by side effects of medicines can improve when treated early. Moreover, damage to the brain as a result of dementia is usually permanent and worsens over time.

Other severe side effects include the following:

  • Kidney problems
  • Diabetes

Pcsk9 Inhibitors Vs Statins

In the past years, statins have been used to lower high cholesterol level. Cholesterol refers to a fatty substance in your blood. Liver manufactures cholesterol and you also get it when you eat some types food. Cholesterol is need by the body to make vitamin D, hormones and cell membrane. When the level of cholesterol becomes high in your body, it increases your risk for stroke, heart attack and other heart problems.2

The following are contrasts between Pcsk9 Inhibitors Vs Statins:

Effectiveness

There is evidence that statins have been used to lower high cholesterol in patients. This drug has been used since 1980s and its impact in people with high cholesterol levels has been studies among many people according to studies.

On the other hand, Pcsk9 Inhibitors is a new drug and was approved recently by food and drug administration in 2015. Although it is new, it has been found to be effective in some people. Studies have shown that alirocumab, a type of Pcsk9 Inhibitors lowered cholesterol level by about 61%. Other studies showed similar results with evolocumab, a type of Pcsk9 Inhibitors.

Cost

Statins are available as generic form and brands. Generic forms are not expensive as compared to brand ones, therefore statins can be cheap. Pcsk9 Inhibitors are new drugs and its generic form is not available. This makes it expensive as compared to statins.

Drug form

Pcsk9 Inhibitors are only taken through an injection while statins are taken orally.

Side effects

Pcsk9 Inhibitors can cause swellings at the place of injection. It can also cause pain in your limb and muscle and makes you get tired easily. Pcsk9 Inhibitors can cause serious side effects such as kidney and liver problems.

On the other hand, statins is associated with the following side effects: it causes pain in your muscles and joints. It causes headache and can result in stomach pains, constipation and nausea. In addition it can cause serious side effects such as: it can damage your liver, elevate your blood glucose levels, increases your risk of developing type 2 diabetes, it affects your mental ability and can damage your muscles leading to a condition called rhabdomyolysis.

Mechanism of Action

Pcsk9 Inhibitors work by binding on inactivating a protein in the liver known as proprotein convertase subtilisin kexin 9 (Pcsk 9). Statins work by inhibiting HMG-CoA reductase which is needed by the liver to make cholesterol. Statins also help your body to reabsorb any cholesterol on the walls of blood vessels.

Those who think have high cholesterol must talk to a health professional first. The health professional would be able to explain to you the various treatment options available for lowering high cholesterol.

You can also take measures to reduce cholesterol levels in your body and prevent heart diseases and stroke. You can practice a healthy lifestyle by quitting smoking, eating food with low fat and exercising regularly.

Reference List

  1. Pcsk 9 inhibitors. Available at https://health.clevelandclinic.org/2015/08/a-new-era-in-cholesterol-busting-drugs-video/
  2. http://www.healthline.com/health/high-cholesterol/pcsk9-inhibitors-vs-statins
  3. Familial hypercholesterolemia. https://medlineplus.gov/ency/article/000392.htm
  4. Dementia. http://www.alz.org/what-is-dementia.asp
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