Lupus Medications

Most people with systemic lupus erythematosus (SLE) will need to take medication – often a combination of drugs – as part of their treatment at least some of the time. There are several drugs that are known to reduce and help control lupus symptoms. It may take a few weeks or months to determine the right combination for you.

Tips on how to manage and get the most from your treatment

• When taking any medication, make sure you follow the directions. Some drugs should be taken at certain times of the day, to help reduce side effects. Some drugs must be taken on an empty stomach for improved absorption, and some with food to prevent stomach upset. If directions are unclear or you haven’t been advised of any possible side effects or given any instructions, ask your doctor or pharmacist.
• Try to take your medication at the same time(s) each day. Ask what you should do if you miss a dose.
• Ask which side effects are considered serious enough to require immediate medical attention.
• Do not adjust dosages without the input of a physician. Do not stop taking your medication because you are feeling better – this is very dangerous. If your doctor is increasing or tapering your medication, ask him or her to write out a schedule.
• Use a days-of-the-week pill container to organize your medication. It will help you notice when you’ve missed a dose. Transfer your medications into a portable pillbox on a day when you’re eating out or traveling.
• Do not take any new medications, over-the counter, naturopathic or otherwise, until you’ve consulted your rheumatologist. Certain drugs containing sulfonamides (sulfa drugs), which include some antibiotics, can mimic a lupus flare by causing fever, arthritis, skin rashes, sun sensitivity and other problems. Some drugs can also interfere with your other medications.
• Always inform every doctor you see about your lupus and all of the medications you’re taking. It’s a good idea to wear a Medic Alert bracelet and/or carry a card that identifies your medical conditions and lists your drugs. Remember to make updates as necessary.
• Medications are not the only way to help manage lupus symptoms and improve your quality of life. Avoid triggers that can cause flares, such as excessive sun exposure without proper protection, and other lifestyle habits that can put stress on the body, such as smoking, street drugs and excessive alcohol consumption. Eating a healthy diet, getting regular exercise and maintaining a positive attitude are all ways to enhance your ongoing treatment for lupus.
• Keep your drugs away from children and pets, and store them in a cool, dry place (not the bathroom medicine cabinet). Do not take expired medication – return it to your pharmacy for safe disposal.

Lupus Medications

The following is a list of commonly prescribed medications for people living with lupus and their side effects. Please note that you are unlikely to experience all of the possible side effects.

Antimalarials

Antimalarial drugs, such as chloroquine (Aralen), hydroxychloroquine (Plaquenil) or quinacrine, commonly used to treat malaria, have also been involved in the treatment of lupus since the 1950s. Although they have proven to effectively treat skin rashes and arthritis, they are slow-acting drugs and it may take months for them to demonstrate a beneficial effect. However, their effectiveness in treating rashes can usually be seen within a few weeks. They can also help against hair loss, fatigue, nose and mouth ulcers and serositis (inflammation of the lungs and heart lining). And because antimalarials help prevent lupus flares and rarely cause any side effects, they are often prescribed to people with lupus for extended periods of time. Minor short-term effects at the beginning of treatment could include loose stools, diarrhea, abdominal cramps and nausea. The most serious possible complication is damage to the eyes, although this is very uncommon. Nevertheless, patients on antimalarial drugs must see an eye doctor (ophthalmologist) once every six months to 12 months for a checkup.

Corticosteroids

Corticosteroids, such as prednisone, are extremely effective in controlling lupus symptoms. They are used to reduce inflammation and suppress activity of the immune system. But because they can cause a variety of side effects, some of which are quite serious, the dose must be regulated to maximize the beneficial effects while minimizing the negative ones. Side effects occur more frequently when high doses of steroids are taken over a long period of time. The goal is to gradually taper the dosage of these drugs to the minimum dose that controls the disease as soon as it can be done safely. Tapering off steroids too quickly can cause a flare. Short-term conditions include weight gain, a round face (“chipmunk cheeks” or “moon face”), acne, excess facial hair, mood swings, easy bruising, high blood pressure, high blood sugar, increased risk of infection, stomach ulcers, hyperactivity, water retention and an increase of appetite. Long-term effects include “thinning” of the bones (osteoporosis), glaucoma and cataracts, osteonecrosis (damage to the bones caused by impaired blood flow), skin changes, heart disease and stroke. Ask your doctor about preventative measures that can greatly reduce the chance of several long-term side effects, such as taking calcium supplements to help guard against osteoporosis.

Non-Steroidal Anti-Inflammatory Drugs (NSAIDs)

NSAIDs, such as ibuprofen (Motrin, Advil), naproxen (Naprosyn), Celecoxib (Celebrex), diclofenac (Voltaren), and indomethacin (Indocin), among many others, are prescribed for a variety of rheumatic diseases including systemic lupus. These drugs are usually prescribed for joint and muscle pain and arthritis. However, they can also upset the stomach, causing stomach ulcers or bleeding from the gastrointestinal tract. These effects can be minimized by taking NSAIDs with meals, milk and/or other medications to help protect the stomach, such as omeprazole (Losec), misoprostil (Cytotec), or ranitidine (Zantac). Excessive NSAID use can also affect kidney function or worsen blood pressure control. Speak to your doctor if you are taking these drugs, especially if you have high blood pressure, heart problems, a history of ulcer , easy bleeding or kidney problems. Generally, with the use of bloodthinners such as coumadin (warfarin) NSAIDs are relatively contra-indicated, because of the risk of bleeding from the gastrointestinal tract.

Steroid-Sparing Drugs

Steroid-sparing drugs (sometimes called immunomodulating drugs) are immunosuppressive (or cytotoxic) agents that help treat severe systemic lupus. They include mycophenolate mofetil (Cellcept), azathioprine (Imuran), cyclophosphamide (Cytoxan) and methotrexate (Rheumatrex, Trexall), among others. They are similar to corticosteroids in that they suppress inflammation and the body’s immune system. Because they allow people with lupus to lessen their dependence on corticosteroids while helping to bring the disease under control and into remission, they are called “steroid-sparing.” However, they are often given in combination with corticosteroid drugs because steroid-sparing agents are slow-acting.

Like all drugs, these have potentially serious side effects. Steroid-sparing drugs may suppress the bone marrow’s ability to produce blood cells, which can lead to anemia, low white blood cell count, and increased risk of infection. They may also predispose an individual to developing cancer, although these cancers are extremely uncommon. Because of this risk, your doctor will carefully monitor your dosage and duration of immunosuppressive drug treatment.

Mycophenolate Mofetil

Mycophenolate mofetil (MMF) has been used since the early 1990s to help prevent acute rejection of transplanted organs such as kidneys or the heart. Since 2000, it has gained popularity as a steroid-sparing drug in the treatment of people with lupus nephritis (inflammation of the kidneys). Although it is not totally devoid of potentially serious side effects, MMF is thought to be a safer drug than cyclophosphamide. For example, unlike cyclophosphamide, MMF is not associated with bleeding from the bladder (hemorrhagic cystitis) or with infertility due to ovarian failure. Diarrhea and a decrease in white blood cell count are the most commonly noted side effects of MMF.

Azathioprine

Azathioprine is a useful immunosuppressive drug in the treatment of more severe cases of lupus. Since azathioprine is often well tolerated, it is commonly used over long periods to maintain remission in previously severe lupus. Bone marrow toxicity and liver enzymes need to be closely monitored to prevent serious blood cell and liver toxicity.

Cyclophosphamide

Cyclophosphamide is one of the most potent immunosuppressive therapies. It is also used to treat serious lupus manifestations such as nephritis. Although MMF is also used for lupus nephritis, intravenous cyclophosphamide remains an important option in lupus when prompt control of the underlying disease is needed to limit the extent and severity of the damage.

To decrease the chance of bladder-related problems, including hemorrhagic cystitis, when taking oral cyclophosphamide, increase your intake of fluids, especially at bedtime, so that you will wake up during the night to empty your bladder and flush out the chemicals.

Bone marrow toxicity should also be monitored closely by blood test. Nausea and hair loss are other possible side effects, as is increased risk of bladder cancer, which can be treated successfully if caught early. Therefore, people taking this drug should have regular urine tests for the rest of their lives.

Risk of skin cancer may also increase slightly when you take this drug, so avoid sun exposure and report any skin conditions to your doctor. Also, cyclophosphamide can lead to infertility due to ovarian failure, as it can cause the ovaries to reduce its production of hormones. The younger you are when you take this medication, the lower your chance of ovarian failure. You should discuss your options with your specialists, especially if you are a young woman who plans to have a family. Methotrexate is used for people with milder lupus manifestations that cause arthritis or pleuritis (inflammation of the lung’s lining).

Methotrexate

Methotrexate is convenient in that it only needs to be taken once a week by mouth or injection. Side effects include nausea, mouth sores, blood problems, liver damage and moderate hair loss.

Prolonged treatment with methotrexate may also lead to folic acid deficiency. To reduce the risk of these side effects a maximum daily dose of 5 mg of folic acid is recommended for patients taking methotrexate on a regular weekly basis (but skipped on the day methotrexate is taken). Other more serious, although rare, side effects include low blood white cell and platelet counts. Methotrexate can also affect the liver and kidneys, which will need to be monitored periodically. If liver function tests are persistently abnormal, your doctor may order a liver biopsy. Avoid drinking any alcohol while on methotrexate. Drinking alcohol while you’re taking methotrexate can cause serious liver problems.

People can also develop lung inflammation shortly after starting methotrexate treatment, but that side effect is rare. If you experience pneumonia-like symptoms such as shortness of breath, fever and coughing, seek urgent medical attention. This drug should not be taken 3 months prior to conception or during pregnancy as it can cause miscarriages and birth defects. It should be noted that if you are in your child-bearing years, you should practise birth control while on many of the steroid-sparing agents – discuss this with your rheumatologist.

Cyclosporine (Neoral®)

Originally developed to prevent rejection of kidney and
other organ transplants, cyclosporine has been used to treat rheumatic diseases,
including lupus. This medication modifies the immune system without decreasing cell
counts. However, it may elevate blood pressure and reduce kidney function. For
these reasons, its use in lupus treatment has decreased.

Mycophenolate mofetil (CellCept®)

Developed to prevent the rejection of transplanted organs, mycophenolate is increasingly used as an alternative to cyclophosphamide for lupus with kidney involvement. It may be useful for other forms of lupus activity also. Mycophenolate works by curbing the excessive activity of lymphocytes (a type of white blood cell). It is often well tolerated, although it can cause nausea and diarrhea. When you take this drug, regular lab tests, including cell counts, are required.

Leflunomide (Arava®)

Leflunomide is an anti-inflammatory medication that can help to reduce the pain and swelling or arthritis and can decrease damage to joints. Like cyclosporine, this medication is not used very often in lupus treatment.

Rituximab (Rituxanis®)

is a cancer drug that works by decreasing the activity of white blood cells known as lymphocytes. Studies of people with severe lupus who did not respond to initial treatment with other drugs and were then treated with rituximab have shown great promise. Because this drug is relatively new, must be given by injection, and is very expensive, it is reserved for very severe cases. Recently, reports of a rare but serious complication have arisen, related to a brain infection causing death. However, this drug has been used safely in many people with severe lupus who did not respond to other treatment; thus, rituximab is an option for difficult cases.

BENLYSTA™

Is a prescription drug used to treat adults with lupus. This medication has been studied and approved by Health Canada for use in lupus patients. It is the first authorized treatment for lupus in almost 50 years; it is the first drug developed specifically to treat lupus. The active ingredient in BENLYSTA™ is belimumab, which is in a group of medicines called monoclonal antibodies. Lupus is a disease of the immune system. People with active lupus often have high levels of a certain protein in their blood. BENLYSTA™ binds to and limits the activity of the protein.The inactive ingredients in BENLYSTA™ are citric acid, polysorbate 80, sodium citrate and sucrose.

What are the potential advantages of BENLYSTA™ over existing treatment
options for lupus?

When given together with other drugs for lupus, BENLYSTA™ decreased lupus disease activity in more than the other drugs alone.

Who should be considered for BENLYSTA™?

BENLYSTA™ is indicated in addition to standard therapy for reducing disease
activity in adult patients (18 years of age and older) with active lupus.
The efficacy of BENLYSTA™ has not been established in the following groups:
o Patients with severe active lupus nephritis
o Patients with severe active central nervous system lupus
o Patients with black African heritage
o Patients less than 18 years of age

What are the warnings and precautions associated with BENLYSTA™?

Immunization: Live vaccines should not be given for 30 days before, or concurrently with BENLYSTA™ as clinical safety has not been established. No data is available on the secondary transmission of infection from persons receiving live vaccines to patients receiving BENLYSTA™. Because of its mechanism of action, BENLYSTA™ may interfere with the response to immunizations. The efficacy of concurrent vaccination in patients receiving BENLYSTA™ is not known. Limited data suggest that BENLYSTA™ does not significantly affect the ability to maintain a protective immune response to immunizations received prior to the administration of BENLYSTA™.

Can BENLYSTA™ be used during pregnancy?

There are no adequate and well-controlled clinical studies using BENLYSTA™ in pregnant women and therefore the effects of BENLYSTA™ on pregnant women are not yet known.
· Women of childbearing potential should use adequate contraception while using
BENLYSTA™ and for at least four months after the final treatment. Safety and
efficacy have not been established in patients less than 18 years of age.

How will I receive BENLYSTA™?

· Your healthcare provider will decide on the correct dose of BENLYSTA™ depending on your body weight. The usual dose is 10 mg for each kilogram of your body weight.
· You will be given BENLYSTA™ by a trained healthcare provider through a needle
placed in a vein (intravenously or IV).
· It takes approximately 1-3 hours to give you the full dose of the drug.
· To help reduce your chance of having a reaction during treatment, it is recommended that an antihistamine be used such as Benadryl.
· How often a patient needs to be on BENLYSTA™ depends on the individual’s
condition and the advice from their healthcare provider. The recommended
dosing of belimumab is administered by IV at two-week intervals for the first three
doses and every four weeks thereafter.

Will BENLYSTA™ cooperate with my other medications and vitamins etc.?

· Tell your healthcare provider about all the drugs you take, including prescription
and non-prescription drugs, vitamins, and herbs. Keep a list of all your drugs and
show it to your doctor and pharmacist when you get a new prescription.
What are the side effects both long and short term?
· Please refer to the “Warnings and Precautions” section of the Product MonoLupus  graph for important safety information. A copy of the BENLYSTA™ Product
Monograph can be found at www.gsk.ca.

What can we expect to be paying for BENLYSTA™?

· The cost will depend on the inclusion of BENLYSTA™ in government assisted
drug plans and employee benefit plans.
For more information about BENLYSTA™ go to: www.BENLYSTA.com or call 1-877-423-6597

*BENLYSTA™ is a trademark of Human Genome Sciences, Inc., used under license
by GlaxoSmithKline Inc.

Summary

NSAIDs are generally well tolerated by people with lupus. Remember to take them exactly as prescribed. Take NSAIDs with food to reduce some of the minor stomach side effects. More serious gastrointestinal bleeding side effects may be decreased with the use of a medication to protect the lining of the stomach. Some NSAIDs may be safely continued if you are pregnant. Notify your doctor if you become pregnant while taking NSAIDs. Here are some helpful tips to manage and get the most from your NSAIDs: · Try to take your medication at the same time each day, and try not to miss a · Know more about which side effects are considered serious enough to require immediate medical attention. · Do not adjust dosages without the input of a doctor and do not stop taking your medication because you are feeling better. Speak to a doctor first. · Use a days-of-the-week pill container to organize your medications. This will help you notice when you’ve missed a dose. Transfer your medications to a portable pillbox when you’re eating out or travelling.