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Immunosuppressive Drugs for Treating Lupus

Immunosuppressive Drugs for Treating Lupus

Immunosuppressive drugs, as the name suggests, are medications that help suppress the immune system. They are mainly used to help recipients of transplanted organs prevent their body from rejecting the newly transplanted organ by suppressing the immune system.  The use of immunosuppressive drugs is also helpful in patients with autoimmune diseases which include lupus.

How do they help lupus patients?

Lupus is an autoimmune disease where the body's immune system attacks the healthy tissues and organs of the body. Immunosuppressive drugs work on a cellular level where they interfere with DNA synthesis. DNAs are responsible for carrying the instructions for cellular processes, and the interference in their synthesis helps prevent the cells of the immune system from dividing. Incomplete cell processes cause the cells of the immune system to die, resulting in the suppression of the immune system.

Immunosuppressive drugs help in controlling some serious complications of lupus that affect major organs such as the brain, lungs, heart, and kidneys. Performing diagnostic procedures, such as an organ biopsy, is required to help determine the most effective immunosuppressive drug to be used in the treatment.

Immunosuppressive drugs are also referred to as steroid-sparing or adjuvant since they can be added to or completely replace steroid therapy. This helps decrease or totally prevent the side effects of using steroid therapy. The use of immunosuppressive drugs can, therefore, eliminate or lessen the need for using steroids and help alleviate the symptoms of lupus.  

Precautionary measures for patients

There is a high risk of infection in patients treated with immunosuppressive drugs due to the fact that immunosuppressive drugs lower the defenses of the immune system. If you are taking these medications, you should make sure to practice having a good personal hygiene and remember to wash your hands regularly. You must avoid people with colds or other highly contagious illnesses. Taking steroid medications can suppress symptoms of fever which can leave you unaware that you are already ill. If you are taking immunosuppressive drugs in addition to steroid therapy, it is recommended to get in touch with your doctor for any sign of illnesses or infections.

Although the use of immunosuppressive drugs is known to increase the risk of cancer, it may, however, decrease the risk of cancer development in lupus patients. Lupus is believed to increase the risk of cancer, and early treatment of its symptoms with immunosuppressive drugs can help prevent some serious complications, therefore, decreasing the risk of having cancer. Controlling your lupus activity is very important in preventing the development of life-threatening complications.

Types of immunosuppressive drugs and their common brands

Cyclosporine - Neoral, Sandimmune, Gengraf

Cyclosporine is an immunosuppressive drug originally used to help suppress the immune system of kidney transplant patients to prevent their body from rejecting the transplanted organ. Cyclosporine works by blocking the function of T-lymphocytes or T-cells in your immune system. Nowadays, Cyclosporine is prescribed for patients with lupus nephritis where there is an inflammation in the kidneys due to lupus. Cyclosporine can also help in the relief of pain, stiffness, and swelling due to the inflammation of joints related to lupus arthritis.

Dosage: The initial dosage for cyclosporine is computed according to your body weight. The dosage is then gradually increased depending on your body's tolerance to the drug. Patients usually take 75 to 100 mg per day, and the effects usually take place after about 3 months.  

Side effects: Some side effects related to Cyclosporine intake include headaches, hypertension, stomach pain, vomiting, diarrhea, hyperuricemia or the buildup of uric acid in the blood and gout, and the inflammation of joints usually in the big toe due to an increase in uric acid. The side effects may eventually disappear after the treatment is reduced or discontinued. It will be advisable to consult your doctor when you start to experience any of these side effects so that the dosage can be adjusted.

Contraindication: Avoid eating grapefruit or drinking grapefruit juice when taking cyclosporine. Grapefruit increases the absorption of cyclosporine in your body. Cyclosporine is not recommended for patients who are pregnant or planning to be pregnant since it may cause serious complications during pregnancy such as premature labor and fluid retention in the baby. It is also contraindicated in breastfeeding patients.

Methotrexate - Rheumatrex

Methotrexate is commonly used to treat rheumatoid arthritis, and it is used to treat joint pain and inflammation of polyarthritis in lupus patients. Methotrexate interferes with folic acid production in a cellular level resulting in a reduction in the growth of certain cells of the immune system. It is also steroid-sparing since it can be used to replace steroids to lower the dosage of steroid therapy.

Dosage: Methotrexate is usually taken in doses of 7.5 to 25mg per week and can also be administered as an injection. Patients taking methotrexate usually feel the effects in 3 to 6 weeks but it may take up to 3 months. It is important to take the medication as prescribed, and it is recommended to consult your doctor if you miss a dose.

Side effects: Patients are unlikely to experience the side effects of methotrexate; however, you are more likely to experience the side effects as the dosage of the medication increases. The side effects of methotrexate usually involve the reduced production of folic acids in cells. For this reason, your doctor may advise you to take folate supplements to counter the side effects of the medication.

Other side effects of methotrexate include nausea and vomiting, and it can also increase the risk of having abnormal results in liver function tests. Drinking alcohol is prohibited when taking methotrexate to avoid irreversible damage to your liver. Make sure to let your doctor know if you have a history of having any liver disease. Contact your doctor immediately if you have any of the mentioned side effects.

Contraindications: As with other immunosuppressive medications, methotrexate is highly contraindicated in pregnant patients since this can cause serious birth defects to your child. Consult your doctor if you have plans of getting pregnant before treatment.

Belimumab - Benlysta

Belimumab is a human monoclonal antibody approved by the FDA to be used as a treatment for lupus. Belimumab was developed to specifically target and block the biological activity of B-lymphocyte stimulator or BLyS. BLyS are responsible for prolonging the survival of B cells that cause the production of autoantibodies. These antibodies attack the body's own tissues. Belimumab helps in the reduction of autoantibodies and controls the autoimmune disease activity.

Dosage: The dosage of Belimumab depends on your weight with the dose of 10mg/kg administered intravenously on a scheduled basis.

Side effects: Patients have notably higher tolerance for belimumab. Some side effects include infusion reactions, infections, nausea, headache, and fatigue.

So far, belimumab is not indicated for patients with severe active lupus nephritis or active central nervous system (CNS) lupus.

Azathioprine - Imuran

Azathioprine is an immunosuppressive drug which is anti-inflammatory in nature. It helps decrease disability and joint damage in patients with lupus. Imuran was proven effective in improving lupus that affect the liver and kidneys. It works by preventing white blood cells or leukocytes from spreading. Imuran may be used to reduce the amount of steroid being given to a patient. Imuran is usually given in a pill form. Imuran, being a slow-onset medication takes around 6 to 12 weeks to have noticeable effects.

Side effects: Common side effects of Imuran include nausea, vomiting, stomach pain, and diarrhea. You may take this medication with food to reduce these side effects. Since Imuran decreases white blood cells, it is recommended to have regular blood tests when taking this medication.

Contraindications: As with other immunosuppressives, they are contraindicated in patients who are pregnant due to the serious effects on the baby. It is also advisable to tell your doctor if you are taking other medications since it can have a reaction with Imuran.

Chloroquine - Aralen and Hydroxychloroquine - Plaquenil

Chloroquine and Hydroxychloroquine were originally used in malaria treatment and prevention. Aside from being anti-malarial drugs, these medications were also proven to be effective in the treatment of lupus. These medications have been proven effective in relieving muscle and joint pain, as well as improving skin rashes, pleuritis, pericarditis, and other symptoms including fatigue and fever. These medications also help in preventing lupus from spreading to certain organs such as the kidneys and central nervous system. Antimalarials are effective in controlling lupus long term. Antimalarials can be taken in addition to steroids in steroid therapy to help reduce the amount of steroids being given which can help reduce the side effects from steroid therapy. It usually takes around 1 to 3 months for these medications to fully take effect.

Side effects: Most patients do not experience any side effects from anti-malarial drugs. Some side effects may include stomach cramps, abdominal bloating, and upset stomach, but these can be reduced by taking these medications with food. One of the most serious side effects for Plaquenil and Aralen is damage to the retina. It is advisable to consult with an ophthalmologist if you are taking these medications for 5 years or more.

Contraindications: Smoking reduces the therapeutic effects of these medications; hence, you should not smoke when taking them.

Cyclophosphamide - Cytoxan

Cytoxan is a cytotoxic medication only prescribed to lupus patients with severe kidney problems when other medications are proven ineffective.

Dosage: Cytoxan can be taken in tablet form, but it is usually given intravenously. The IV infusion usually takes around 15 to 60 minutes, and the medication may be given to the patient before the treatment to reduce nausea. It may take a few weeks to a few months to notice some improvement in your lupus symptoms.

Side effects: Side effects of Cytoxan include nausea, vomiting, alopecia or hair loss, and skin rashes. More side effects have been reported when it is taken in tablet form. Bladder problems may arise when taking Cytoxan, so increasing fluid intake is advisable to help relieve this symptom. Serious side effects of Cytoxan include a decrease in white blood cell count, that usually occurs approximately 8 to 12 days from initial treatment. It is recommended for patients to have blood tests to decide if your dosage should be changed.

Contraindications: As with other immunosuppressive drugs, Cytoxan is highly contraindicated in pregnant patients since it can cause serious harm to the fetus. Cytoxan also targets healthy cells aside from the immune cells making you more prone to developing cancer. Bladder cancer and leukemia are among the most commonly developed cancers when taking cytoxan, so your doctor should do regular blood and urine tests. This is also the reason why Cytoxan is the last resort for lupus treatment.

Reviews on the use of immunosuppressive drugs for lupus treatment

Several studies have been done about lupus treatments, and it was proven that adhering to the treatment is the most effective way of overcoming lupus. The notable decrease in treatment adherence usually leads to lupus relapse, kidney problems, and hospitalizations. Always consult with your doctor if you experience any adverse effects from your treatment instead of stopping the treatment altogether.