List of medications which are helpful in the treatment of rheumatoid arthritis
Rheumatoid arthritis (RA) mainly is a complicated disease that has potential in order to affect not just only the joints but other parts (specifically joints) of the body as well. It is basically an autoimmune disease. The body has a complex immune system comprising cells and proteins that work to keep you healthy, by fighting off infections and protecting against cancer. The ‘auto’ of autoimmune disease implies that the immune system has made a mistake and is attacking its own body. In Rheumatoid Arthritis this is seen with the inflammation (pain and swelling) appearing within the joints. However, apart from this, the entire body can be involved, with the common symptoms of extreme fatigue or tiredness, and when the disease is majorly active, feeling unwell, with the symptoms a bit like flu.
Sometimes (although quite less commonly in today’s era due to the advanced treatment) inflammation may develop other than the joints, such as the skin, eyes or lungs, also people with rheumatoid arthritis are more likely at the higher risk of cardiovascular disease. Principal aims of the treatment: In order to treat Rheumatoid Arthritis the main aims are as follows: •
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To reduce inflammation and its side effects: pain, swelling, stiffness and fatigue. To protect the body from the risk of damage to the joints and bones caused by uncontrolled inflammation. To protect other organs in the body that might be affected by the uncontrolled inflammation. To maintain the ability to lead a normal life, with minimal impact on relationships, family, home, work and leisure.
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Anti-inflammatories work in two ways: to relieve pain; and to reduce inflammation (swelling, redness, heat and pain). In order to reduce the pain, the effect from the prescribed NSAID dose consumed either with or after the food can be felt after the initial dose. It may take 7 days in order to achieve the complete pain relief. To reduce inflammation (the swelling in the joints) a regular dose must be taken (with or after food) thereby keeping a constant level of the drug in the bloodstream and the full benefit in reducing swelling may take up to three weeks. Occasionally, NSAIDs may take longer than three weeks to be fully effective in controlling the swelling, redness, heat and pain. On the crucial juncture, an alternative NSAID can be needed for improved control of the symptoms.
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NSAIDs should only be used for the shortest possible time. Which drug is prescribed?
1. NSAIDs There is a little difference between the NSAIDs and the way they act but individuals may have considerable differences in the way they work and respond to them. •
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Ibuprofen specifically combines the benefits of the pain relief, reduction of the inflammation and lowering of the fever. It has a few side effects than the other NSAIDs but its anti-inflammatory properties are a little weaker. Naproxen, a quite effective NSAID which is well tolerated. Dexibuprofen recently reintroduced NSAID. The drug appears to act rapidly with statistically significant reducing the side effects including cardiovascular disease. Diclofenac is absolutely identical to the Naproxen. Indomethacin, a little bit more useful than the naproxen but may be responsible for causing several side effects including dizziness, gastro-intestinal disturbance and headache. Piroxicam is quite similar in effect as naproxen but it acts for longer so the one dose everyday is effective. It may be responsible for more gastro-intestinal adverse reactions and also may cause frequent skin reactions. Meloxicam can be prescribed for long term treatment of rheumatoid arthritis and it should be taken once daily. Most commonly reported side effects: As with any medication, NSAIDs have a number of possible side effects, although it is important to remember that these are only potential side effects. They may not occur at all.
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nausea diarrhoea bleeding ulceration rash bronchospasm (mimicking asthma) swelling of lips, tongue, around the eyes headache dizziness nervousness, ringing in the ears 2. Sulfasalazine: Sulfasalazine is a DMARD (disease modifying antirheumatic drug). Sulfasalazine should be prescribed in the form of a single DMARD or should be prescribed at about the same time as any other DMARD. It can be frequently prescribed together with the methotrexate. Background:
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It (Sulfasalazine) was launched in the year of 1950s, initially in order to treat inflammatory bowel disease. It was considered for treating rheumatoid arthritis (RA) as it was believed that the bacterial infections are the main cause of this form of arthritis. After the positive outcomes from clinical trials/studies in the late 1970s this drug was used more extensively in treating RA and also used for some forms of juvenile arthritis but not extensively. Sulfasalazine also can be used to treat inflammatory ulcerative colitis, crohn’s disease and bowel disease. How long does it take to work?
Sulfasalazine is available in liquid form or tablets. The daily recommended dose of the sulfasalazine should be gradually increased each week, usually for the 21 days, until the maximum recommended/prescribed daily dose has been achieved. For controlling the signs and symptoms of Rheumatoid Arthritis with the sulfasalazine might take up to 3 months or may be longer. Most commonly reported side effects: As like any other drug, sulfasalazine may also cause a number of adverse reactions, although it is important in order to remember that these side effects are only potential side effects. These include: • • • • • • • • • • • • • • •
Nausea (feeling sick) Vomiting Dizziness Headache Diarrhoea Loss of appetite Skin rash Raised temperature Insomnia Itching of skin Tinnitus Bruising Sore throat Mouth ulcers Cough 3. Methotrexate: Methotrexate (MTX), mainly ranked as the ‘gold standard’ DMARD (disease modifying anti-rheumatic drug) for controlling the inflammatory arthritis.
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Methotrexate was introduced in the year of 1947 and was recommended for the first time to treat leukaemia and other forms of the cancer. From the year of 1980s, MTX was used in order to treat adult patients with the RA but in lower doses (than doses used for cancer and leukaemia) after the clinical trials had specified its benefits in Rheumatoid Arthritis. Most commonly reported side effects: Like any other medication, MTX has a number of possible adverse reactions, although it is crucial in order to consider that these are only potential adverse effects. They may not appear at all. Side effects may include:
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Nausea Loss of appetite Vomiting Diarrhoea Mouth ulcers Skin rash Headaches Mild hair loss Fever Symptoms of infection Bruising Bleeding Increased sensitivity to sunlight Mood swings
4. Hydroxychloroquine: Hydroxychloroquine is a treatment for malaria but has been shown to have an effect on the messaging system between cells by interrupting the inflammatory response. It is this mechanism that is beneficial in both RA and juvenile idiopathic arthritis (JIA). It is commonly used in combination with one or two other disease modifying anti-rheumatic drugs (DMARDs), particularly methotrexate. Background: •
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Hydroxychloroquine was initially developed as the drug ‘chloroquine’ in order to treat malaria. Chloroquine was modified to hydroxychloroquine to reduce the possible adverse reactions that were basically causing eye problems. How does it work?
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Hydroxychloroquine is available as a form of 200mg tablet. The function of hydroxychloroquine is not fully understood and it is a cumulative effect over several weeks prior to any benefit is seen. Blood tests for hydroxychloroquine are checked prior to the treatment initiates and then as frequently as the doctor instructs, usually at the clinic visits. When this drug is prescribed together with other DMARDs the blood test frequency should be regular, on behalf of the recommendations for other DMARD(s). Most commonly reported side effects: As with any medication, hydroxychloroquine has a number of possible side effects, although it is important to remember that these are only potential side effects and they may not occur at all. Side effects may include:
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Loss of appetite Anorexia Headache Rash Itching, Blurring Abdominal pain Cramps Nausea Diarrhoea Vomiting Blood disorders 5. Leflunomide: Leflunomide is a DMARD (disease modifying antirheumatic drug) developed in order to control the inflammatory arthritis. Leflunomide, basically is a prodrug, it means that it will be inactive until it is consumed. Leflunomide is changed into the active drug inside the patient’s own body. Background: Leflunomide has been recommended as a diseasemodifying anti-rheumatic drug in order to treat rheumatoid arthritis (RA) since the earlier year of the 2000s. How does it work? Leflunomide mainly acts on the enzyme in the body in order to limit the excessive reaction of the cells, which are usually involved during the inflammation, thereby reducing the pain, swelling and problems of Rheumatoid Arthritis.
Most commonly reported side effects: As like any other medicine, leflunomide also has a number of probable adverse effects, although it is necessary in order to remember that these side effects are only potential side effects and may not occur. Side effects may include: • • • • • • • •
Increased blood pressure Unexplained diarrhoea Inflammation of the lining of the mouth Increased susceptibility to infections Shortness of breath Cough Numbness Tingling of feet or hands 6. Ciclosporin (Neoral): Ciclosporin treatment for rheumatoid arthritis is usually an ‘add-on’ treatment to supplement the main disease modifying drug (eg methotrexate) or to enable the reduction of regular steroid treatment. Note: Ciclosporin is also used to minimise the possibility of rejection of transplanted organs as well as for other inflammatory conditions. Background: Ciclosporin was developed in the 1970s and its impacts on dampening down the immune system involved in treating rheumatoid arthritis (RA) as well as after the heart and kidney transplants. Most commonly reported side effects: As with any medication, ciclosporin has a number of possible side effects, although it is important to remember that these are only potential side effects and they may not occur at all.
Close monitoring with blood tests is important as well as regular blood pressure monitoring and after 6 months of treatment kidney function needs to be checked. When Neoral is prescribed together with the other drug that affects the immune system, monitoring will be according to which drug has the most frequently required regimen. Side effects may include: • • • • • • • • •
nausea vomiting diarrhoea swollen gums raised blood pressure fever fatigue headache increased risk of infections 7. Azathioprine: Azathioprine is used to control severe active rheumatoid arthritis, usually as an ‘add on’ treatment to supplement the main disease modifying drug (DMARD) or to enable the reduction of regular steroid treatment. Note: Azathioprine is also used to minimise the possibility of rejection of transplanted organs as well as for other inflammatory conditions. Azathioprine basically damps down the immune system by reducing or slowing the cell division rate amongst the existing inflammatory cells.
Background: Azathioprine has been widely prescribed since the 1960s. The benefit of treatment with azathioprine can take weeks or months to be established. Most commonly reported side effects: As with any medication, azathioprine has a number of possible side effects, although it is important to remember that these are only potential side effects and they may not occur at all. Close monitoring of weekly blood tests for the first 8 weeks (or as advised) of treatment is very important. Side effects may include: • • • • • • • •
nausea vomiting diarrhoea throat ulcers fever infections bruising bleeding 8. Tofacitinib (Xeljanz): Tofacitinib citrate is approved in order to treat adult patients with moderately to severely active rheumatoid arthritis (RA) who have had an inadequate response to, or who are intolerant of, methotrexate. Tofacitinib citrate is also recommended for use in the treatment of adult patients who are with moderate to severe active ulcerative colitis.
Background: It is in the janus kinase (JAK) inhibitor class, discovered and developed by the National Institutes of Health and Pfizer. Most commonly reported side effects: As with any medication, tofacitinib 5 mg has a number of possible side effects. These may include: • • • • • • • • • • • • • • •
headache runny or stuffy nose joint pain rash muscle weakness muscle pain diarrhea feeling queasy heartburn upset stomach cough dizziness vomiting back pain nose or throat infection Other existing DMARDs which are also quite effective, listed as follows:
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baricitinib (Olumiant) Upadacitinib (Rinvoq) BIOLOGIC THERAPIES: Biologic drugs for the treatment of rheumatoid arthritis (RA) are made from proteins. They act by blocking the activity of the key chemical or cell or protein involved
in causing inflammation that is responsible for rise to joint swelling and other symptoms. They are impactful and specific therapies that can target every specific part of our immune system. When choosing the biosimilar or biologic, for the very first time, it’s likely that you will be initiated on one of the biosimilar anti-TNF or anti-TNFs. Anti-TNF drugs: Generic drug name: adalimumab Brand name: Humira Target cells of immune system: anti-TNF Dose and method of administration: 40mg by subcutaneous (under the skin) injection every other week. Generic drug name: certolizumab pegol Brand name: Cimzia Target cells of immune system: anti-TNF Dose and method of administration: 400mg by subcutaneous injection at weeks 0, 2 and 4 (given as two injections of 200mg), and then 200mg every other week thereafter. Generic drug name: etanercept Brand name: Enbrel Target cells of immune system: anti-TNF Dose and method of administration: Etanercept 25mg twice a week, or etanercept 50 mg weekly by subcutaneous injection. Generic drug name: golimumab Brand name: Simponi Target cells of immune system: anti-TNF
Dose and method of administration: 50mg monthly by subcutaneous injection. Generic drug name: infliximab Brand name: Remicade Target cells of immune system: anti-TNF Dose and method of administration: 3mg per kg of body weight by intravenous infusion, repeated 2 weeks and 6 weeks after the first infusion, then every 8 weeks. Other Biologic Drugs, Targeting Different Inflammatory Chemicals: Generic drug name: tocilizumab Brand name: RoActemra Target cells of the immune system: IL-6 (interleukin 6) receptor inhibitor. Dose and method of administration: 8mg/kg of body weight as intravenous infusion each month. Generic drug name: sarilumab Brand name: kevzara Target cells of immune system: IL-6 receptor inhibitor. Dose and method of administration: 200 mg once every two weeks, administered as a subcutaneous injection. Generic drug name: rituximab Brand name: Mabthera Target cells of immune system: B-cell depletion of lymphocytes (1 type of white blood cell). Dose and method of administration: Intravenous infusion twice, two weeks apart, repeated every 6-12 months.
Generic drug name: abatacept Brand name: Orencia Target cells of immune system: Antibody blocking T-cells. Dose and method of administration: 3 x Intravenous infusions every two weeks, thereafter monthly. Possible side effects: Possible side effects with other biologic drugs: abdominal pain, diarrhoea, mouth ulcers, altered blood tests, dizziness, hypertension, infections (upper respiratory tract), migraine, flushing, fatigue and others. If you experience such reactions, immediately remember in order to report to the medical team caring for you. Steroids: Steroids are also known as corticosteroids or glucocorticoids. They are used to help control many forms of arthritis. Note: This article exists just for informative purposes. In order to know more about any specific product please see full prescribing information.
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