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What is Arava?

Arava (leflunomide) is a medication used to treat adults with active rheumatoid arthritis, a condition where the immune system attacks the joints, causing pain and swelling.

Arava works by inhibiting pyrimidine synthesis, a process that produces pyrimidines, which are essential building blocks for DNA and RNA. By inhibiting this process, the growth of immune cells attacking the joints is reduced.

Before starting treatment with Arava, doctors recommend several tests, including:

  • checking for tuberculosis,
  • blood tests to monitor liver function (serum alanine aminotransferase or ALT, an enzyme found in the liver that indicates liver damage when elevated),
  • blood cell counts (including white blood cells, which are part of the immune system,
  • red blood cells measured by hemoglobin or hematocrit count to diagnose anemia, and platelets, which are essential for blood clotting)
  • Pregnancy testing is done for women who could become pregnant, and blood pressure is checked.

Arava should not be used by pregnant women, as it can harm the unborn baby.

It is also not recommended for people with severe liver problems, those allergic to leflunomide (the active ingredient in Arava), or those taking another drug called teriflunomide.

Besides rheumatoid arthritis, Arava is sometimes used off-label (prescribing a drug for conditions not officially approved) to treat juvenile idiopathic arthritis, psoriatic arthritis, refractory dermatomyositis, and systemic lupus erythematosus.

Dosage Information and Usage

Dosage Form and Strengths of Arava

  • 10 mg tablets: White, round film-coated tablet embossed with “ZBN” on one side
  • 20 mg tablets: Light-yellow, triangular film-coated tablet embossed with “ZBO” on one side
  • 100 mg tablets: White, round film-coated tablet embossed with “ZBP” on one side

Usage

The suggested dose of Arava is 20 mg once daily. Treatment may start with or without a loading dose to quickly achieve steady drug levels.

For low-risk patients with liver toxicity or bone marrow suppression, it’s recommended to take a 100 mg loading dose once daily for the initial 3 days, then switch to 20 mg daily.

If the risk is higher, like when taking methotrexate, start with 20 mg daily without a loading dose. The maximum daily dose is 20 mg. If side effects occur, consider reducing the dose to 10 mg daily.

Close monitoring is essential after dose changes and when discontinuing Arava due to the slow elimination of its active metabolite, teriflunomide.

It’s advised to undergo a rapid drug removal process after discontinuing Arava to lower teriflunomide levels in the body. These levels can still be detectable for up to 2 years otherwise.

Storage Information

Store Arava tablets at room temperature, specifically at 25°C (77°F).

It is permissible for the temperature to occasionally range between 15°C and 30°C (59°F to 86°F).

Keep the tablets in their original packaging to protect them from light.

Side Effects of Arava

Common Side Effects

  • Diarrhea
  • Elevated liver enzymes (ALT and AST)
  • Hair loss (alopecia)
  • Rash
  • Nausea
  • Headache

Serious but Rare Side Effects

  • Severe liver damage (hepatotoxicity)
  • Bone marrow suppression (reduced blood cell production)
  • Serious infections
  • Severe allergic skin reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis)
  • Skin ulcers
  • Nerve damage (peripheral neuropathy)
  • Lung disease (interstitial lung disease)

Warnings and Precautions

  • Embryo-Fetal Toxicity: Arava can cause serious harm to an unborn baby. It is not safe for use during pregnancy. Women of childbearing age must use effective birth control while taking Arava and undergo a procedure to remove the drug from their body if they plan to become pregnant or if they become pregnant while on the medication.
  • Hepatotoxicity: Arava can cause severe liver damage, which in some cases can be fatal. Patients with liver disease or high liver enzyme levels should not use Arava. Regular monitoring of liver enzymes is necessary, and the drug should be discontinued if significant liver enzyme elevations occur.
  • Procedure for Accelerated Elimination of Arava: The active ingredient of Arava stays in the body for a long time. To quickly remove the drug, a specific elimination procedure can be used, such as taking cholestyramine or activated charcoal. This procedure is important if a patient experiences severe side effects or becomes pregnant.
  • Immunosuppression, Bone Marrow Suppression, and Risk of Serious Infections: Arava suppresses the immune system, which can lead to serious infections and bone marrow suppression. Regular blood tests are needed to monitor for low blood cell counts. If serious infections occur, Arava treatment should be stopped and the accelerated elimination procedure should be started.
  • Stevens-Johnson Syndrome, Toxic Epidermal Necrolysis, and DRESS: These are rare but severe skin reactions that can occur with Arava use. If such reactions develop, stop Arava immediately and start the elimination procedure.
  • Skin Ulcers: Arava can cause skin ulcers. If skin ulcers appear or do not heal properly, discontinuing Arava and starting the elimination procedure may be necessary.
  • Malignancy and Lymphoproliferative Disorders: Although not observed in clinical trials, there is a potential risk of cancer, particularly lymphoproliferative disorders, with the use of immunosuppressive medications like Arava.
  • Peripheral Neuropathy: Arava can cause nerve damage, resulting in symptoms like tingling or numbness in the hands and feet. If these symptoms occur, consider discontinuing Arava and start the elimination procedure.
  • Interstitial Lung Disease: Arava can cause serious lung disease, which can be fatal. Patients with a history of lung disease are at higher risk. New or worsening lung symptoms should be investigated, and Arava should be discontinued if necessary.
  • Vaccinations: Live vaccines should not be given to patients on Arava due to the drug’s long-lasting effects. The safety of other vaccines during Arava treatment is unknown.
  • Blood Pressure Monitoring: Arava can cause high blood pressure. Blood pressure should be checked before starting Arava and monitored regularly during treatment.

Overdosage of Arava

Taking too much Arava can lead to symptoms like diarrhea, stomach pain, low white blood cell count, anemia, and elevated liver enzymes.

If an overdose occurs, a special procedure to quickly remove the drug from the body should be performed. Standard dialysis methods are not effective for removing Arava from the system.

Drug Interactions

  • Potent CYP and Transporter Inducers: Rifampin, a strong inducer of certain enzymes and transporters, can increase the level of teriflunomide (the active form of Arava) in the blood by 40%. Although no dosage change for Arava is needed, caution is advised when using both medications together due to possible increasing levels of Arava with continued use.
  • CYP2C8 Substrates: Teriflunomide can block CYP2C8, an enzyme that helps process certain drugs like paclitaxel and pioglitazone. This blockage can lead to higher levels of these drugs in the body, so their doses might need adjustment when used with Arava.
  • Warfarin: When Arava is taken with warfarin, a blood thinner, it may reduce warfarin’s effectiveness by lowering its peak level by around 25%. Regular monitoring of blood clotting levels (INR) is vital for safety.
  • Oral Contraceptives: Arava can increase the levels of certain hormones in birth control pills, like ethinylestradiol and levonorgestrel. This interaction might require adjustments to the type or dosage of contraceptives used.
  • CYP1A2 Substrates: Teriflunomide could slightly increase CYP1A2 activity, impacting drugs such as duloxetine and theophylline. This may reduce their effectiveness, possibly requiring dose adjustments.
  • Organic Anion Transporter 3 (OAT3) Substrates: Teriflunomide blocks OAT3, a transporter impacting drugs like methotrexate and ciprofloxacin. This can raise drug levels, needing dose adjustments and close monitoring.
  • BCRP and Organic Anion Transporting Polypeptide B1 and B3 (OATP1B1/1B3) Substrates: Teriflunomide blocks BCRP and OATP1B1/1B3, impacting medicines such as Rosuvastatin and Atorvastatin. Keep rosuvastatin dose at or below 10 mg daily. Other drugs in these groups may require lower doses and careful side effect monitoring.

Alternative Medications

Cost & Coupons

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Explore our pricing of Arava (Leflunomide) below:

Strength Quantity Price
10mg 30 tablets $479.00
60 tablets $920.00
90 tablets $1,350.00
20mg 30 tablets $499.00
60 tablets $960.00
90 tablets $1,410.00

With Pharma Giant, you can trust that you are getting quality medication at reasonable prices. We believe that financial constraints should never compromise your health. Choose Pharma Giant to manage your health needs efficiently and affordably because your well-being is our top priority.

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Frequently Asked Questions

Arava is used to treat rheumatoid arthritis in adults. It helps reduce inflammation, pain, and joint damage associated with the condition.
Arava is a drug that modulates the immune system to protect normal tissues and joints. It blocks a particular enzyme that triggers rapid white blood cell growth, reducing inflammation and joint damage from rheumatoid arthritis.
Arava is taken orally, usually in the form of a tablet. The dosage can vary based on individual tolerance and other factors.
The generic name of Arava is leflunomide.
Patients on Arava will have regular check-ups with their doctor to monitor their health. Before treatment starts, blood pressure and blood tests will be done to check platelet, white blood cell, and hemoglobin levels. Monthly monitoring for the first 6 months, then every 6-8 weeks. If Arava is used with other immunosuppressants like methotrexate, more frequent monitoring may be necessary. Liver enzyme levels will be checked for any damage. If Arava is stopped, it may take up to 2 years for the ingredients to clear from the body, so close monitoring is crucial, especially after dose reduction.
The most frequently reported side effects of Arava include:
  • Diarrhea
  • Headache
  • Nausea
  • Elevated liver enzymes
  • Hair loss
  • Rash
  • High blood pressure
  • Back pain
  • Stomach discomfort
  • Abdominal cramps
  • Allergic reactions
  • Bronchitis
  • Dizziness
  • Mouth sores
  • Itching
  • Sinus infections
  • Vomiting
  • Tendon sheath inflammation
Some less common but potentially serious side effects of Arava include:
  • Liver damage
  • Bone marrow suppression
  • Numbness and pain in hands and feet
  • Interstitial lung disease
The duration of Arava’s side effects can vary. Some side effects, like diarrhea, may resolve within a couple of weeks as your body adjusts to the medication. However, the persistence of side effects depends on the individual and the specific side effects experienced.
Before starting treatment with Arava, patients should be aware of the following precautions:
  • Ensure pregnancy is excluded before starting Arava. Females must use effective contraception and avoid pregnancy until the drug elimination process is complete.
  • Do not use Arava if you are hypersensitive to leflunomide or teriflunomide.
  • Arava is not recommended for patients with active infections. Screen for tuberculosis (TB) before beginning treatment.
  • Stevens-Johnson syndrome, a rare but serious skin condition, may occur. If this happens, stop Arava immediately and undergo an accelerated drug elimination procedure.
  • Be aware that interstitial lung disease, which can be severe or fatal, may develop. If symptoms worsen, discontinue Arava and proceed with accelerated elimination.
  • Inform your doctor about all medications and supplements you are taking, as interactions with other drugs can lead to serious side effects.
Arava is not typically associated with weight gain. A 2016 study suggests that people with rheumatoid arthritis (RA) taking leflunomide (Arava) are more likely to experience weight loss.
Arava can remain in your system for varying lengths of time. In healthy adults, it generally takes about 10 weeks, or roughly 2.5 months, for most of the drug to be eliminated after the last dose. However, for some individuals, it may take up to two years for Arava to completely clear from the body.
Arava may take some time to show its full effects. Patients typically begin to see benefits within 6 to 12 weeks after starting the medication. It’s important to take the medication as directed, usually 20 mg once daily, and with food to help with absorption.
Arava is not commonly associated with direct kidney damage. However, it can have effects on overall kidney function, especially in patients with pre-existing kidney conditions or when used with other medications that affect the kidneys.
Yes, Arava can be taken long-term. It is designed as a long-term treatment for conditions like rheumatoid arthritis.
No, Arava is not a controlled substance. It is a non-biologic, disease-modifying antirheumatic drug (DMARD) used to treat rheumatoid arthritis in adults. Unlike controlled substances, it is not regulated under specific restrictions related to abuse or dependency.
Arava tablets should not be crushed or chewed; they must be swallowed whole.
Arava was approved by the U.S. Food and Drug Administration (FDA) in 1998. It was developed by Sanofi Aventis.
Arava is typically taken as a 10 mg or 20 mg tablet once a day. However, in some cases, your healthcare provider may prescribe it every other day.
It is not advisable to stop taking Arava abruptly. Doing so could cause your rheumatoid arthritis symptoms to return.
Certain drugs may interact with Arava and potentially cause adverse effects. It’s important to avoid or carefully manage the following:
  • Methotrexate
  • Rifampin
  • Warfarin
  • Live vaccines

Disclaimer

Pharma Giant provides medical information to help you better understand medications and medical conditions.This content is for informational use only and does not replace advice from a licensed medical practitioner. Consult your doctor or pharmacist before starting or changing any medication. All our partners follow strict safety standards set by their country’s health authorities to make sure you receive safe and high-quality medications.

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