- Immunosuppressive medication is the class of drugs that reduces or tends to suppress the immune system.
- This makes the body less likely to reject any transplanted organ; hence, they are also called antirejection drugs.
- Drugs such as Methotrexate, azathioprine, Etanercept, and Anakinra are various types of drugs that help to suppress or clear the symptoms caused by rheumatoid arthritis.
What is Rheumatoid Arthritis?
A chronic inflammatory disorder that happens to affect more than just the joints is known as Rheumatoid Arthritis. In a few cases for certain individuals, this medical condition can lead to damage in a wider sense, because it would affect the other body systems, which could include the skin, heart, lungs, blood vessels, and eyes. This is an autoimmune disorder, and it occurs when the individual’s immune system erroneously starts attacking its own body’s tissues. This disease can affect the lining of the joints, which could then lead to painful swelling. This then eventually results in erosion of the bones or bone deformity. The inflammation that happens to come along with this disease can impact the other parts of the body, as well. The treatment options have improved drastically over the ages, but if it is a severe case of rheumatoid arthritis, then it can lead to some forms of physical disability.
What are immunosuppressant drugs?
Immunosuppressant drugs are those drugs that suppress or reduce the immune system strength. Some of these medications that fall under this category are used to make the body less likely to reject any transplanted organ, such as the kidneys, liver, or heart. Hence, these drugs are also called antirejection drugs. Apart from this, other sets of immunosuppressant drugs are also often used to treat various autoimmune disorders, such as rheumatoid arthritis, lupus, or psoriasis.
Immunosuppressive drugs used for Rheumatoid Arthritis
Below is a list of immunosuppressive medications that can be used in the treatment of rheumatoid arthritis:
- Nitrogen mustard
- Azathioprine (Imuran)
- Methotrexate (Rheumatrex dose pack, Trexall)
- Mercaptopurine (Purinethol)
- Etanercept (Enbrel)
- Infliximab (Remicade and Inflectra)
- Chlorambucil (Leukeran)
- Cyclophosphamide (Cytoxan)
- Hydroxychloroquine (Plaquenil)
- Anakinra (Kineret)
- Adalimumab (Humira)
- Golimumab (Simponi)
- Tocilizumab (RoActemra)
- Leflunomide (Arava)
Methotrexate: This medication acts as an anti-inflammatory drug, which is one of the most frequently used immunosuppressants. This is mostly used for severe disease. This medicine starts working within three to six weeks, but the complete effect of this medicine is not present until after 12 weeks of treatment. This medicine should be used in conjunction with another medication; however, if it is used alone, then it loses its effectiveness.
Methotrexate can be used in combination with other medications, such as hydroxychloroquine, leflunomide, or sulfasalazine. This medication can also be combined with various biological response modifier drugs, which have been used for the treatment of patients with early aggressive arthritis. This combination of drugs works better than the single therapy.
Mostly, it is seen that almost 20 percent of the patients taking this drug withdraw due to its side effects. Those side effects would include nausea, vomiting, headache, loss of hair, and pain in the muscles. Methotrexate is also known to reduce the level of folic acid in the body, and this is also harmful and can lead to certain other side effects. Hence, in certain cases the doctors can also prescribe supplements of folic acid to avoid any side effects. However, some say that by doing so, the effectiveness of methotrexate gets reduced.
This medicine is usually given in pills; however, those patients who need higher doses would need to go for the option of injection. There are a few severe side effects that can be toxic, which may include:
- Damage to the kidneys and liver, wherein those who are already suffering from diabetes, alcoholism, and/or obesity are at higher risk. Hence, patients should limit the intake of alcohol.
- There are increases in the chances of getting infections, so this medicine should not be given to patients who are already suffering from herpes zoster virus, any kind of bacterial infection, active or latent case of tuberculosis, or hepatitis B, acute or chronic.
- Those individuals who have poor functioning of the lungs are at higher risk of getting lung disease.
- Pregnant women should not be given this medicine, unless consulting with the doctor, since it can lead to birth defects.
Infliximab: Infliximab was the first chimeric monoclonal antibody that was used to treat rheumatoid arthritis. When a person has rheumatoid arthritis, then due to the symptoms of inflammation, too much of a protein called TNF is produced by the body. This leads to pain, inflammation, and harm of the bones and joints. One cannot term them as painkillers, but they have the ability to modify the disease so that the symptoms start to improve. This would gradually take around two to twelve weeks of time.
Infliximab will not be prescribed if the arthritis is not active, if one is suffering from any kind of infection, or if one has multiple sclerosis, cancer, conditions related to heart, or lung fibrosis. Infliximab is given to the person via a drip into the arm or intravenous infusion. This process takes around two hours and needs to be done in the hospital.
The doctor would then check for any signs of side effects; hence, the person is asked to wait for one or two hours. Post the first infusion, the patient would have another infusion two weeks later, and then the third one would be four weeks later. Once this third one is done, the person would need to have one infusion done every eight weeks. Later, this can be done at home and would take less time. The symptoms would start showing improvement from the second week, and in some cases, it would be 12 weeks for the symptoms to go away. This is a long term treatment; hence, one should ensure to complete the entire dose, unless there are any side effects.
Golimumab: Golimumab is an anti-TNF medication that helps to block the TNF, which in turn reduces the inflammation condition in the patients. One should not treat them as painkillers, but they can start showing some improvement in the symptoms, which would take around 12 to 14 weeks. This would mean improvement could be seen after three to four doses. Golimumab will not be prescribed if the arthritis is not active, if one is suffering from any kind of infection, or if one has multiple sclerosis, cancer, a condition related to heart, or lung fibrosis.
Golimumab is given to the patient once per month via injections under the skin. This can be injected into the thigh, upper arm, or stomach. This medicine comes in a 50 mg syringe or pen-like device. If one forgets to take this dose, then you can take it as soon as you remember. If this medicine has been delayed for more than two weeks, then one would need to start a new schedule from the date one has taken the delayed dose. Always remember to never inject oneself with a double dose to make up for the missed dose.
It would take around 12 to 14 weeks for the symptoms to show some signs of improvement. This is a long term treatment; hence, it is important to complete the entire dose, unless there are any side effects. Side effects of this medicine would be reactions to the injections, such as swelling, pain, or redness at the injection site. These effects are nothing to worry about and are quite common. Since Golimumab impacts the immune system, there are chances a person may develop infections. Some symptoms of infections are sore throat and fever, which should be noted to the doctor.
Tocilizumab: Tocilizumab is a type of drug that falls under the category of biological therapy. There is excess protein called IL-6, which gets produced in the body due to certain conditions. This then leads to symptoms such as anemia, feeling of tiredness, or damage to the bones and joints. Tocilizumab blocks this action caused by IL-6, thereby reducing its effects. One cannot call it a painkiller; it can only reduce the symptoms of the disease.
One can start noticing changes in the symptoms from the second week to the 12th week post starting the medication. Tocilizumab is usually prescribed by the doctor along with another combination of methotrexate. The doctor may prescribe Tocilizumab if there is any existing infection or the arthritis is not active. If the person is suffering from diabetes, liver disease, or intestinal ulcers, this medicine would not be prescribed. There are two ways the doctor can give Tocilizumab. It can be in the form of a drip into the vein, which can take around an hour and has to be done once every four weeks. The other way is via injection once a week. Later on, this can be given at home by any family member. This is again a long term treatment and has to be completed, unless one experiences any side effects.
Azathioprine: This falls under the category of disease-modifying anti-rheumatic drug (DMARD). It helps to reduce the defense mechanism of the body, which in certain conditions can be overactive. Azathioprine is known to modify the underlying process of the disease so that it limits further damage to the tissues and avoids any kind of disability. This is a long term treatment, and it would take around six to twelve weeks for the symptoms to start showing some improvement.
If one is suffering from liver or kidney problems, or has problems with bone marrow, then Azathioprine needs to be used with caution. Inform the doctor of the same. Azathioprine is available in tablet form and should be taken once or twice in a day. It can be taken with or without food. Initially, the doctor would prefer to start on a lower dose and gradually increase it, depending on any side effects of the same. Azathioprine is known to cause certain serious GI problems; patients may experience nausea, vomiting, or pain in the stomach. In serious conditions, it can lead to reduction in the white blood cells.
Etanercept: Etanercept is an anti-TNF drug. When there is too much of protein called TNF produced by the body, it leads to inflammation, pain, and damage to the bones and joints. The use of anti-TNF medications is to block the action caused by TNF and thus reduce the inflammation. This is the first drug that was used for the treatment of rheumatoid arthritis. Etanercept can modify the symptoms caused by the disease. It is not a painkiller, nor can it cure the disease.
The symptoms start showing improvement by the second week. The doctor may not prescribe Etanercept if the patient is suffering from severe forms of infection, has cancer, or has lung fibrosis. Etanercept can be taken once or twice in a week as an injection. Previously, this medication was available under the brand name Enbrel; later, a new version was developed with the brand name Benepali. This is referred to as a bio-similar. The possible side effects of Etanercept are nausea, mild fever, runny nose, rash, or pain in the stomach.
Adalimumab: This is again an anti-TNF medication. Hence, it blocks the production of TNF, which reduces the effects of inflammation in the body. Adalimumab can modify the symptoms caused by the disease. It is not a painkiller, nor can it cure the disease. The symptoms start showing improvement by the second week. The doctor may not prescribe this medicine if the patient is suffering from severe forms of infection, has cancer, or has lung fibrosis.
Adalimumab is given by way of injection once every two weeks in the dosage of 40mg. This is a long term treatment, and hence, it is important to complete the entire course, unless there are any side effects. The injections side effects, such as redness, swelling, or pain, would subside gradually. Since Adalimumab has an impact on the immune system, it can tend to cause some serious infections. Hence, inform the doctor if you notice any symptoms, such as fever, diarrhea, or coughing. This medicine is used alone or in combination with other DMARDs or methotrexate. This is known to show promising results for children.
Anakinra: Anakinra is available under the brand name Kineret. This drug was approved in 2001. This medication can be used either alone or with another medicine. This helps to slow down the damage caused to the joints and also to reduce the pain and swelling caused by the disease. Anakinra is a man-made form of protein. This is similar to other drugs, which help to block the effects of protein, which in turn leads to less inflammation in the joints.
Anakinra is given in the form of an injection once per day or as directed by the doctor. The common side effects of Anakinra injections would be redness, swelling, and pain at the site; however, it is quite normal to experience side effects, and they would go away quickly. Apart from these, Anakinra is also known to cause other side effects, such as infections in the joints, skin, or bone, which become serious if immediate medical help is not sought.
Hydroxychloroquine: Hydroxychloroquine falls under the category of DMARDs. It helps to regulate the immune system, which can tend to be overactive sometimes. Hydroxychloroquine helps in the treatment of the symptoms caused due to arthritis. From the long term perspective, Hydroxychloroquine is known to treat stiffness in the joints, pain, and swelling. It can take as long as 12 weeks for the symptoms to show any improvement. Hydroxychloroquine is taken in combination with methotrexate.
This medicine was originally used for treating malaria, but now it’s mostly used for treatment of mild or progressive arthritis. At times, it would take six months to show the full benefit of this medicine. Hydroxychloroquine causes fewer side effects compared to the other DMARDs. However, nausea and diarrhea are a couple of the most common side effects of this medicine. Hydroxychloroquine is available in a tablet form and can be taken orally with or without food. The correct dose would be advised by the doctor. Initially, the patient would be started on 200mg to 400mg, and later, depending on the status, they may gradually decrease the dose.
Leflunomide: Leflunomide is another drug that falls under the category of DMARDs. It dampens the underlying disease, instead of simply working on treating the symptoms. It reduces the activity of the immune system, which can tend to be overactive in certain conditions. It helps to reduce pain, swelling, and stiffness in the body. It can take weeks for the effects to show up, and in certain cases, it can take six to twelve weeks for the complete treatment.
Leflunomide can be given in combination with other DMARDs, or it can be given alone. Leflunomide is available in tablet form and should be given once a day. The tablet should not be crushed, chewed, or broken open. It should be taken as a whole. It can be taken with or without food. The doctor may prescribe starting with 10mg or 20mg per day. Common side effects associated with Leflunomide include hair loss, rash, nausea, and diarrhea. The serious side effects include damage to the liver and potential risk of injury.
Side effects and Interactions
Various types of immunosuppressant drugs would have different side effects, and they also vary from person to person. To find out the side effects of a particular type of drug, check with the doctor while they prescribe the certain medication for you, and feel free to ask the pharmacist any questions you may have about the drug. However, one thing to note is that all of the immunosuppressant drugs carry the risk of infection. When this drug weakens the immune system, the body becomes weak and less resistant to various types of infections. This means that one is more likely to contract infections, and at the same time, it also makes it harder to get that infection treated. If one experiences any of the below-mentioned symptoms pertaining to the infection, then it is time to check with the doctor.
- Pain during urinating
- Having trouble while urinating
- Frequent urge to urinate
- Lower back side pain
- Feeling weak
- Unusual tiredness
One should also provide a list of all those medicines that are currently in use before the doctor prescribes any of the immunosuppressants. The list should also include vitamins, supplements, over-the-counter medications, and prescription drugs. The doctor would judge the factor of interactions and then prescribe the appropriate drug to be taken. Similar to the side effects, the risk of drug interaction would depend from drug to drug.