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Methotrexate vs Arava
Introduction
For patients with rheumatoid arthritis or other types of inflammatory conditions, certain drugs that alter the immune system's response can help in reducing inflammation and managing symptoms. Methotrexate and Arava are two such medications commonly prescribed for these conditions. They each exert different effects on the immune system, yet both contribute to alleviating discomfort associated with inflammatory diseases. Methotrexate is an antimetabolite and antifolate drug, which works by inhibiting folic acid metabolism thus controlling the rapid growth of cells related to inflammation. On the other hand, Arava (leflunomide) functions as a pyrimidine synthesis inhibitor by preventing proliferation of lymphocytes - a type of white blood cell involved in causing inflammation.
Methotrexate vs Arava Side By Side
| Attribute | Rheumatrex trexall | Arava |
|---|---|---|
| Brand Name | Rheumatrex, Trexall | Arava |
| Contraindications | Should not be taken with certain antibiotics such as trimethoprim-sulfamethoxazole due to increased risk of side effects including a decrease in white blood cell count. | A drug elimination procedure is recommended if switching from Arava to another DMARD like Methotrexate to avoid possible harmful interactions. |
| Cost | For the brand name versions, about $130 for 30 tablets of 2.5 mg. Generic versions can cost as low as under a dollar per day up to slightly over two dollars each day. | For the brand name versions, around $1,400 for 60 tablets of 10 mg. Generic versions can cost from $0.70 to $2 per day depending on the dosage. |
| Generic Name | Methotrexate | Leflunomide |
| Most Serious Side Effect | Severe liver damage, a drop in blood cell count leading to severe fatigue, weakness, and confusion. | Severe liver problems, severe allergic reactions, and severe skin reactions. |
| Severe Drug Interactions | Certain antibiotics might interact with methotrexate and increase the risk of side effects. | Not specified, but as with any DMARD, monitoring for interactions with other drugs is crucial. |
| Typical Dose | 7.5–25 mg per week | 100 mg/day for the first three days, then reduced to 10-20 mg per day |
What is Methotrexate?
Methotrexate (sold under brands like Rheumatrex and Trexall) is a long-standing drug, first approved by the FDA in 1953. It was originally categorized as an antimetabolite and antifolate drug, primarily used for treating cancers. However, it's now more commonly prescribed for rheumatoid arthritis due to its effectiveness in reducing joint inflammation and slowing disease progression. Methotrexate works by suppressing the body’s immune response that contributes to joint inflammation.
On the other hand, Arava (generic name Leflunomide), approved by the FDA in 1998, is a pyrimidine synthesis inhibitor which also serves as a disease-modifying antirheumatic drug (DMARD). Its primary function is to reduce symptoms of active rheumatoid arthritis and psoriatic arthritis by inhibiting an enzyme required for DNA replication thus suppressing rapidly dividing cells such as those found within inflamed joints.
Both drugs have similar uses but their mechanisms of action differ significantly which can result in different side effect profiles. Consulting with your healthcare provider will help determine which option may be most suitable based on individual health status.
What conditions is Methotrexate approved to treat?
Methotrexate is approved for the treatment of several different conditions:
- Rheumatoid arthritis, including juvenile idiopathic arthritis
- Psoriasis and psoriatic arthritis
- Certain types of cancer, such as leukemia, breast cancer, lung cancer, lymphoma and osteosarcoma.
How does Methotrexate help with these illnesses?
Methotrexate is a medication that helps manage rheumatoid arthritis by reducing the activity of the immune system. It does this by inhibiting an enzyme called dihydrofolate reductase, which plays a crucial role in cell growth and division. By blocking this enzyme, Methotrexate reduces inflammation and slows down the progression of joint damage caused by overactive immune responses in conditions like rheumatoid arthritis.
Arava (leflunomide), on the other hand, also modulates the immune system but operates differently to methotrexate. Arava works primarily by inhibiting an enzyme known as dihydroorotate dehydrogenase, which is necessary for DNA synthesis in proliferating cells such as lymphocytes — these are white blood cells that play large roles in the body's immune response.
Both drugs help to reduce symptoms of rheumatoid arthritis including pain and swelling, but they do so via different mechanisms within our bodies' complex biochemistry. Patients may respond differently to each drug due to factors such as individual metabolism or potential side effects.
What is Arava?
Arava, also known as leflunomide, is a disease-modifying antirheumatic drug (DMARD) that works by suppressing the body's immune system to reduce inflammation and swelling. Arava inhibits an enzyme called dihydroorotate dehydrogenase, which plays a crucial role in the production of DNA and RNA. By blocking this enzyme, Arava hinders the multiplication of rapidly dividing cells like those causing inflammation in rheumatoid arthritis.
This medication was first approved by the FDA in 1998 for treatment of adults with active rheumatoid arthritis or psoriatic arthritis. Unlike methotrexate which has been associated with severe side effects such as liver damage and bone marrow suppression, Arava does not inhibit folic acid metabolism therefore its side-effect profile differs from Methotrexate's. While it can still cause serious side effects such as liver damage, these are less common than with Methotrexate.
However, just like any other medications used for treating autoimmune diseases where they suppress your immune response; it may make you more susceptible to infections. Other possible side effects include diarrhea, nausea and hair loss but these tend to be mild compared to Methotrexate’s potential adverse reactions.
What conditions is Arava approved to treat?
Arava, also known as leflunomide, has been approved by the FDA for the treatment of:
- Rheumatoid arthritis
- Psoriatic arthritis
This medication works to reduce joint damage and improve physical function in patients. It is an effective option for those who have not responded adequately to other treatments such as methotrexate.
How does Arava help with these illnesses?
Arava, or leflunomide, is a disease-modifying antirheumatic drug (DMARD) that plays crucial roles in many biological processes in the body. It works by suppressing the immune system to prevent it from attacking the joints, thus reducing inflammation and pain. Arava also slows down the progression of joint damage caused by rheumatoid arthritis.
In comparison to methotrexate which may cause significant side effects such as liver toxicity and lung problems, Arava's side effect profile tends to be milder with less frequent issues related to liver toxicity, making it an alternative choice for patients who do not tolerate methotrexate well. However, it should be noted that while Arava can be used alone or combined with other DMARDs for more comprehensive treatment plans, its use should always be under close medical supervision due to possible serious side effects like liver injury and blood disorders.
How effective are both Methotrexate and Arava?
Both methotrexate and leflunomide (Arava) are well-established treatments for rheumatoid arthritis, with their initial approvals by the FDA only a few years apart. They function differently in treating autoimmune diseases such as rheumatoid arthritis: Methotrexate is an antimetabolite that inhibits DNA synthesis, while Arava works through immunomodulation by inhibiting pyrimidine synthesis.
The effectiveness of both drugs was directly studied in several double-blind clinical trials. In these studies, both drugs displayed similar efficacy in managing symptoms and slowing disease progression of rheumatoid arthritis; however, they differed slightly in terms of side effects profile. A 2009 clinical trial compared Methotrexate against Arava and found that patients on Arava had somewhat more gastrointestinal complaints.
A meta-analysis published in 2013 demonstrated the effectiveness of Methotrexate starting from the first weeks of treatment. It also showed favorable tolerability over many other DMARDs (Disease-Modifying Antirheumatic Drugs), making it one of the most widely-prescribed treatments worldwide for rheumatoid arthritis.
In contrast to Methotrexate's widespread use, Arava is typically considered a second-line treatment option - often prescribed when patients do not respond satisfactorily to methotrexate or can't tolerate its side effects. Nonetheless, due to its unique pharmacology and mechanism action distinct from other DMARDs, Arava may be an optimal treatment choice for certain patient populations like those resistant or intolerant to Methotrexate.
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At what dose is Methotrexate typically prescribed?
Methotrexate is typically prescribed at doses ranging from 7.5–25 mg per week for the treatment of rheumatoid arthritis, while Arava (leflunomide) is usually administered at a dose of 10-20 mg/day. For most individuals, methotrexate can begin to show effects within three to six weeks, whereas Arava may take up to four weeks or longer before its full benefits are felt. With both medications, the dosage could be adjusted based on individual response and side effects experienced by patients. The maximum weekly dose for Methotrexate should not exceed 25mg/week and daily dosage for Arava shouldn't exceed 20mg/day under any circumstances.
At what dose is Arava typically prescribed?
Arava treatment usually starts at a dosage of 100 mg/day for the first three days. After this initial period, the dose is typically reduced to 10-20 mg per day, depending on your doctor's advice and how well you tolerate Arava. This single daily dose can be taken with or without food. For maximum effectiveness, it's important to take Arava consistently every day, ideally around the same time each day. It may take up to a month or more before you begin noticing improvements in your condition due to Arava's gradual effect on immune system regulation.
What are the most common side effects for Methotrexate?
Common side effects of Methotrexate can include:
- Nausea, vomiting, and indigestion
- Diarrhea or mouth sores
- Abdominal discomfort and loss of appetite
- Fatigue (general weakness)
- Skin rash, redness or itching
- Dizziness or feeling faint
- Temporary hair loss
Whereas common side effects for Arava (leflunomide) may encompass:
- Diarrhea
- Nausea, stomach pain
- Weight loss (anorexia)
- Headaches
- Dizziness and fatigue -Tingling or numbness in hands or feet (peripheral neuropathy) -Rash, dry skin.
These are not exhaustive lists. If any new symptoms develop while taking either medication, it is important to consult with a healthcare provider immediately.
Are there any potential serious side effects for Methotrexate?
Arava, like Methotrexate, is a drug used to treat rheumatoid arthritis. Serious but rare side effects may include:
- Any signs of infection: fever, sore throat, or cough;
- Signs of an allergic reaction such as hives; difficulty breathing; swelling in your face or throat
- Vision changes such as blurred vision or sensitivity to light;
- Rapid heart rate (tachycardia) resulting in pounding sensation within the chest;
- A drop in blood cell count leading to severe fatigue, weakness and confusion;
- Severe liver damage - yellowing eyes/skin (jaundice), dark urine, severe stomach/abdominal pain/persistent nausea/vomiting.
If any of these symptoms occur while taking Arava you should seek medical attention immediately. In comparison with Methotrexate there are some differences in potential adverse events. Always remember that all medication decisions should be made collaboratively with your healthcare provider based on a thorough evaluation of risks versus benefits for each individual patient's circumstances and preferences.
What are the most common side effects for Arava?
Arava (leflunomide) can have the following side effects:
- Upset stomach or diarrhea
- Mild skin rashes
- Hair loss
- Weight loss
- Headache, dizziness
- Increased blood pressure
- Muscle aches and joint pain While these are common side effects, serious adverse reactions such as liver damage, severe infections due to lowered immunity, and rare occurrences of lung disease have also been associated with Arava. Therefore, regular monitoring is crucial when taking this medication.
Are there any potential serious side effects for Arava?
While Arava is generally well-tolerated, it's important to note that in some cases, serious side effects can occur. These may include:
- Signs of a severe allergic reaction such as hives; difficulty breathing; swelling of your face, lips, tongue, or throat
- Severe skin reactions including fever, sore throat, swelling in your face or tongue and burning eyes which might be accompanied by skin pain followed by a red or purple rash that spreads (especially in the face or upper body) causing blistering and peeling
- Unusual changes in mood or behavior
- Blurred vision and other visual disturbances like eye pain
- Rapid heartbeat which could indicate cardiovascular complications
- Liver problems – right-sided abdominal pain, yellowing of eyes/skin (jaundice), dark urine
- Lung problems - new onset cough or shortness of breath.
If you experience any of these symptoms while taking Arava, seek immediate medical attention.
Contraindications for Methotrexate and Arava?
Both methotrexate and Arava, along with most other disease-modifying antirheumatic drugs (DMARDs), may worsen symptoms of rheumatoid arthritis in some people. If you notice your joint pain or inflammation worsening, please seek immediate medical attention.
Neither methotrexate nor Arava should be taken if you are taking, or have recently been taking, certain antibiotics such as trimethoprim-sulfamethoxazole. Always tell your physician which medications you are taking; these antibiotics might interact with methotrexate and increase the risk of side effects, including a decrease in white blood cell count that can lead to serious infections.
Also keep in mind that both Methotrexate and Arava can potentially cause liver damage over time; regular monitoring by your doctor is necessary when on either medication to ensure liver function remains healthy.
Arava stays in the body for a long time after discontinuation due to its long half-life. A drug elimination procedure is recommended if switching from Arava to another DMARD like Methotrexate to avoid possible harmful interactions.
How much do Methotrexate and Arava cost?
For the brand name versions of these drugs:
- The price for 60 tablets of Arava (10 mg) averages around $1,400, which works out to approximately $23–46/day, depending on your dose.
- The price for 30 tablets of Methotrexate (2.5 mg) averages about $130, working out to roughly $4.33/day.
Thus, if you are in the higher dosage range for Arava (i.e., 20 mg/day or more), then brand-name Methotrexate is less expensive on a per-day treatment basis. However, cost should not be a primary consideration in determining which of these drugs is right for you.
For the generic versions of Methotrexate and Arava(leflunomide), costs are significantly lower:
- Leflunomide (10 mg tablets) is available in packs from 30 capsules and above with approximate costs ranging from $0.70 to $2 per day depending upon dosages that could go up to 20mg daily.
- Methotrexate comes in packages as small as four up to hundreds (2.5 mg). Depending upon how many you buy at once and where you purchase them, your costs may run from as low as under a dollar per day up to slightly over two dollars each day.
Popularity of Methotrexate and Arava
Methotrexate, both in its generic form and brand names such as Rheumatrex and Trexall, is a cornerstone of rheumatoid arthritis treatment. It was estimated to have been prescribed to about 1.2 million people in the US in 2020. Methotrexate accounted for nearly 50% of disease-modifying antirheumatic drug (DMARD) prescriptions in the US, thus making it the most commonly used DMARD. Its use has been generally consistent over recent years.
Leflunomide or Arava on the other hand was prescribed to approximately 97,000 people in America during last year. In terms of DMARD prescriptions across the nation, leflunomide accounts for just under 5%. The prevalence of Arava as an option for rheumatoid arthritis management has remained steady over the past decade but lags significantly behind methotrexate due to its higher cost and slightly increased risk profile.
Conclusion
Both Methotrexate and Arava (leflunomide) have a long history of use in patients with rheumatoid arthritis, backed by several clinical studies indicating their efficacy over placebo treatments. They may be used together under careful monitoring due to potential additive toxicities, particularly liver damage and immunosuppression. Both drugs work primarily on the immune system but through different mechanisms: methotrexate inhibits dihydrofolate reductase enzyme which is necessary for cell growth while Arava works mainly by inhibiting pyrimidine synthesis essential for DNA replication.
Methotrexate is often considered as a first-line treatment option due to its fast onset of action and proven effectiveness, whereas Arava might be considered as an alternative or adjunctive therapy in patients intolerant to methotrexate or who did not respond well to it.
Both medications are available generically; however, even then methotrexate tends to cost less than Arava. An adjustment period may also be required for both drugs since benefits might not become apparent immediately after starting them.
The side effect profile between these two medications differs somewhat: common side effects of Methotrexate include nausea and liver toxicity, while hypertension and diarrhea are more commonly associated with Arava. As they can both potentially harm the liver and reduce immunity leading to infections, regular blood tests are usually conducted during treatment with either drug. Patients should promptly seek medical help if they experience any severe side effects such as shortness of breath or persistent vomiting.
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Refrences
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