Immunosuppressive Drugs for Multiple Sclerosis

What is multiple sclerosis (MS)?

Multiple sclerosis is a medical condition that affects the brain and the spinal cord. A few of the early symptoms of the disease are numbness, tingling sensation, blurry vision, and feeling weak. In this disease, the immune system tends to attack the myelin, which is the protective sheath covering the nerve fibers. When the myelin is damaged, it leads to problems in communication between the brain and the rest of the body. Gradually, due to this disease, the nerves start to deteriorate and lead to permanent damage of the nerves.

Immunosuppressive Treatment of Multiple Sclerosis

Immunosuppressive treatment has been used for the past 30 years for treating multiple sclerosis (MS). The main rationale of using immunosuppressive drugs for MS is that it lies in the hypothesis that this disease is an inflammatory immune-mediated illness, which can take advantage of strong anti-inflammatory activities.

Immunosuppressants have been used because of their ability to suppress the immune system's reaction. Aside from suppressing the immune system, it also reduces the risk of foreign body rejection such as an organ transplant. Drugs such as methotrexate have shown some signs of effectiveness in causing a delay in the disease progression.

Azathioprine has shown fewer effects in the clinical trials when it came to the progression of the disease. Various immunosuppressants have a different mechanism of action against the disease. Since this class of drugs suppresses the immune system, the risk of having any type of infection also increases.

Common Immunosuppressant Drugs

• Imuran (azathioprine)
• Cytoxan (cyclophosphamide)
• Rheumatrex, Trexall (methotrexate)
• Novantrone (mitoxantrone) 

Plegridy (peginterferon beta-1a)

Plegridy is used for treating a worsening condition of multiple sclerosis. This medicine is a protein, which is quite similar to the one found in our body. There is no known proof on how this medicine exactly works. However, it is thought to interfere with a few substances in the body, which are known to cause an outbreak of this disease.

People should not use Plegridy if they are allergic to any contents present in peginterferon beta-1a or to another medicine called peginterferon. There are certain things one should inform the doctor before starting the course of treatment using peginterferon beta-1a:

• Inform the doctor if you are pregnant, planning for a pregnancy, or if you are nursing a baby.
• If you are currently on other types of medication whether over-the-counter or prescription medicine.
• A history of liver-related problems or abnormal functioning of the liver
• If you have any kidney problems
• Any allergies to food or medicine
• Suicidal tendencies
• Seizure attacks
• Bouts of depression

One should use peginterferon beta-1a as directed by the doctor and make sure to check the label for directions and dosing instructions. This medicine is given in the form of an injection deep under the skin of the stomach, back of the upper arm, or thigh. Avoid injecting this medicine in areas where the skin is already irritated, has bruises, or is infected. 

With every dose of injection, one should rotate the site of injection, and should not be given at the same site at all times. Do not change the dosage without the doctor's advice. There have been certain incidents wherein patients have shown changes in their mood or having suicidal tendencies. Thus, any signs of mood changes or suicidal thoughts should be reported to the doctor.

Peginterferon beta-1a is also known to cause flu-like symptoms. Inform the doctor if you experience any of the following signs and symptoms after taking peginterferon beta-1a:

• Weakness
• Muscle aches
• Flu-like symptoms
• Headache
• Mild fever
• Chills
• Nausea
• Pain or swelling at the site of injection

Imuran (azathioprine)

Azathioprine has been commonly used only in cases where one would not want the body to reject any transplanted organ. In short, it prevents organ rejections. This medication is also given in conjunction with other medicines. Azathioprine works by weakening the immune system to help the body accept the new organ and also to prevent any damage to the joints.

This medication has to be taken orally and as directed by the doctor. It can be taken once or twice a day. Make sure to take this medicine with food to avoid an upset stomach. The doctor would decide the dosage based on certain factors such as height and weight of the individual, overall health of the person, and the body’s response to the treatment. Do not increase the dose on your own without consulting the doctor since you will have an increased risk of developing side effects. This medicine should not be taken by a pregnant woman since the drug can be absorbed through the skin and the lungs, thereby causing harm to the unborn child. The common side effects of azathioprine are nausea, vomiting, and diarrhea. Its serious side effects are weakness, pain in the muscles, fever, and rash. Taking an additional dosage of this medicine can lead to an overdose, which can also cause adverse side effects. The symptoms of an overdose include nausea, sore throat, chills, fever, vomiting, and other symptoms of infection.

Gilenya (fingolimod)

This medicine is mainly used to treat worsening conditions of multiple sclerosis. One should not take it as a cure for sclerosis. This medicine works by preventing the lymphocytes from attacking and damaging the nerves in the brain and spinal cord.

Fingolimod can help lessen the number of relapses to avoid the worsening of the disease, and thus, resulting in a delay of disability. Before starting the course of treatment, the doctor would conduct certain tests such as a complete blood count or CBC, blood pressure level, and an eye examination. These tests are all carried out to monitor any side effects after starting the treatment.

Fingolimod has to be taken orally with or without food or as directed by the doctor. Once the first dose is given, the doctor would monitor the condition of the patient for the next six hours to ensure that the heartbeat of the patient does not slow down. If the heartbeat of the patient slows down, then it can result in a serious case of heart attack. If an individual temporarily stops taking fingolimod and then starts again, then the condition would again need to be monitored for six hours.

The side effects of fingolimod are diarrhea, back pain, coughing, and headaches. Contact your doctor immediately if the side effects are worsening. Fingolimod is also known to raise blood pressure levels. For this reason, make sure to monitor your blood pressure level at regular intervals. Fingolimod also has the chance of causing skin cancer. Inform the doctor right away if you notice suspicious skin lesions.

Tysabri (natalizumab)

Natalizumab is known to treat certain types of multiple sclerosis and slow down the progression of the disease. It also prevents the symptoms from worsening. This medication is usually given to MS patients who cannot use other medications due to certain reasons.

Natalizumab is known as a monoclonal antibody. There are claims that this medicine tends to block certain inflammatory cells. It blocks the cells from getting into the brain to slow down the disease. Natalizumab should not be used if you are allergic to any of its contents. Before taking this medicine, inform your doctor if you have the following conditions:

• If you are pregnant or planning for a pregnancy
• Breastfeeding
• If you have kidney-related problems
• Food or drug allergies
• If you are taking OTC or prescription medications
• History of liver problems
• If you are undergoing chemotherapy

Use natalizumab as directed by the doctor and make sure to check the label for directions and dosing instructions. Natalizumab is given in the form of an injection deep under the skin. The medication can lead to dizziness, especially when taken with alcohol.

This medicine can also lower the body's ability to fight infections. Contact the doctor if you notice symptoms such as fever, cough, sore throat, or chills. In certain patients, fatal infections of the brain or spinal cord have been reported after using natalizumab. The common side effects of this medicine include:

• Diarrhea
• Stomach pain
• Muscle cramps
• Joint pain
• Nausea
• Headache 
• Pain in the legs or arms
• Tiredness

The drug's severe side effects are:  

• Shortness of breath
• Chills
• Persistent cough
• Difficulty in breathing
• Swelling of the mouth, lips, face, and tongue
• Issues with eyesight
• Irregular heartbeat
• Suicidal tendencies

Interferon Beta-1b Injection 

Interferon beta-1b comes in the form of injection and is given to patients to reduce frequent symptoms of relapsing multiple sclerosis. Interferon beta-1b falls under the category of immunomodulators.

Interferon beta-1b injection is available in powder form, which needs to be mixed with a liquid before skin injection. This medicine is usually injected into the patient every other day. One should inject this medicine almost the same time every day. Check with the doctor on the dosage level and other instructions. Do not inject more or less of the amount of the medicine to avoid certain side effects. The doctor would initially start with a lower dose and gradually increase the dosage depending on the condition of the patient. The first dose would be given at the hospital under the doctor’s guidance. After the first dose, you can take the injections at home with the help of a friend or any member of the family.

Mix only one vial of the interferon beta-1b at a time. Do not mix the medication and then keep it out for long. Either it can be done right before one plans to take the injection or it can be mixed in advance and kept in the refrigerator and use within 3 hours of mixing it. Interferon beta-1b can be injected under the skin in any part of the body such as the abdomen, back of the upper arms, thighs, or buttocks. Do not inject it near the navel or waistline.

Inform the doctor if you are allergic to any of the drug's contents. Interferon beta-1b can lead to certain side effects such as:

• Weakness
• Headache
• Unusual vaginal bleeding
• Tight muscles 
• Lack of coordination
• Changes in the sex drive, especially in men

Inform the doctor immediately if you experience the following serious side effects:

• Nausea
• Vomiting
• Extreme tiredness
• Dark urine 
• Loss of appetite
• Insomnia
• Hallucination
• Suicidal tendencies
• Skin turning pale
• Shortness of breath

Copaxone (glatiramer acetate injection)

Glatiramer is a polypeptide mixture used for the treatment of worse multiple sclerosis conditions. Certain studies suggest that the drug acts by changing immune system processes, which are responsible for the effects of multiple sclerosis.

You should not use glatiramer if you are allergic to any of its contents. Before treatment, it is very important to inform the doctor if you are planning to get pregnant or is pregnant, if you have food or drug allergies, or if you are currently on any prescribed or OTC medication.

Glatiramer should be used exactly as prescribed by the doctor and also read the instructions mentioned on the label of the packaging. Glatiramer is given in the form of an injection at the hospital. It can be injected under the skin on the stomach, thigh, upper arm, or on the outer hip. The injection sites should be rotated on every dose.

The common side effects of glatiramer are:

• Mild redness, swelling, or pain at the site of injection
• Back pain
• Lump at the site of injection
• Vomiting
• Nausea
• Weakness
• Weight gain

The severe side effects include:

• Irregular breathing
• Vision changes 
• Hardening of the skin
• Difficulty in swallowing
• Pain or tightness in the chest region
• Dizziness
• Swollen glands

Side Effects of Immunosuppressive Drugs

One of the major side effects of immunosuppressive drugs is the increased risk of infections since they tend to suppress the immune response. Other less serious side effects of immunosuppressants are nausea, increased hair growth, vomiting, trembling of the hands, and loss of appetite. These side effects usually subside as the body gets used to the drug.