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Teriflunomide (Generic Drug)
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Teriflunomide (Generic) Teriflunomide
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What is Teriflunomide?

Teriflunomide is an FDA-approved medication for adults with certain types of multiple sclerosis (MS), including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease. This medication helps reduce the frequency of MS flare-ups.

Multiple sclerosis (MS) is a chronic disease of the central nervous system, believed to be an autoimmune disorder where the body mistakenly attacks itself. MS affects everyone differently, with some people experiencing only mild symptoms.

However, teriflunomide is not known if it’s safe or effective for children. People with severe liver problems, pregnant women, those not using effective birth control, and anyone allergic to teriflunomide or leflunomide should not take this medication.

Before starting teriflunomide, you should inform your doctor if you have liver or kidney issues, infections, numbness or tingling, diabetes, skin problems, breathing issues, or high blood pressure.

How Does Teriflunomide Work?

Teriflunomide reduces the activity of specific immune cells attacking the nervous system in multiple sclerosis (MS) by targeting an enzyme called dihydroorotate dehydrogenase (DHODH).

This enzyme is essential for producing pyrimidines, the DNA building blocks in fast-growing cells like T and B lymphocytes, which are white blood cells vital for the immune response. By inhibiting DHODH, teriflunomide decreases the number of these active immune cells, lessening inflammation and the immune attack on the nervous system.

While the exact mechanism of teriflunomide in MS isn’t fully understood, it is thought to decrease the activated lymphocytes in the central nervous system (CNS), including the brain and spinal cord.

Dosage Information and Usage

Dosage Form and Strengths of Teriflunomide

Teriflunomide tablets are available as 14 mg tablets. The 14 mg tablet is a blue (pale blue to pastel blue) colored film-coated tablet debossed with the dose strength “14” on one side. Each tablet contains 14 mg of teriflunomide.

Usage

The recommended dose of teriflunomide is either 7 mg or 14 mg taken once daily. You can take the tablet with or without food. Before starting treatment, your doctor will check your liver function and blood cell counts, and screen for tuberculosis.

Women should confirm they are not pregnant before starting teriflunomide. Blood pressure should be checked before and during treatment.

Storage Information

Store teriflunomide tablets at room temperature, between 68°F and 77°F (20°C to 25°C). Keep the tablets in their original container and make sure they are out of the reach of children.

Side Effects

Common Side Effects

  • Headache
  • Diarrhea
  • Nausea
  • Hair thinning or loss (alopecia)
  • Increased liver function test results

Serious but Rare Side Effects

  • Decreased white blood cell count, leading to more frequent infections:
    • fever,
    • tiredness,
    • body aches,
    • chills,
    • nausea,
    • vomiting
  • Serious skin reactions
    • rash,
    • redness,
    • peeling,
    • mouth sores,
    • blisters
  • Allergic reactions
    • difficulty breathing,
    • itching,
    • swelling of lips, eyes, throat, or tongue
  • Severe allergic reactions affecting the liver, kidneys, heart, or blood cells:
    • severe muscle pain,
    • swollen lymph glands,
    • unusual bruising or bleeding,
    • yellowing of skin or eyes,
    • weakness, or tiredness
  • Numbness or tingling in hands or feet, especially for ages over 60, taking certain medicines, or having diabetes
  • High blood pressure
  • New or worsening breathing problems
    • shortness of breath,
    • coughing with or without fever

Warnings and Precautions

  • Hepatotoxicity: Teriflunomide can cause serious liver damage, including liver failure that may require a transplant. This risk is higher in patients with existing liver problems or those taking other liver-affecting medications. Liver function should be monitored regularly during treatment.
  • Embryofetal Toxicity: Teriflunomide can harm an unborn baby. Women who are pregnant or can become pregnant must avoid this medication unless they use effective birth control. Pregnancy must be ruled out before starting treatment.
  • Bone Marrow Effects and Immunosuppression: Teriflunomide can lower white blood cell and platelet counts, increasing the risk of infections. Patients should have blood tests before starting treatment and be monitored for signs of infection.
  • Infection Risk: Patients should not start teriflunomide if they have an active infection. The medication can make it easier to get infections, including serious ones. Report any symptoms of infection to a doctor immediately.
  • Hypersensitivity Reactions: Severe allergic reactions, including anaphylaxis, can occur. Symptoms like difficulty breathing, swelling, and hives require immediate medical attention.
  • Serious Skin Reactions: Teriflunomide can cause severe skin reactions, such as Stevens-Johnson syndrome and toxic epidermal necrolysis. These conditions can be life-threatening and need immediate discontinuation of the drug and medical help.
  • Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS): This severe reaction involves fever, rash, and organ involvement like liver and kidney issues. It requires immediate discontinuation of teriflunomide and medical treatment.
  • Peripheral Neuropathy: Teriflunomide can cause nerve damage leading to numbness or tingling in the hands and feet. Older patients and those on certain other medications are at higher risk. Discontinue if these symptoms occur.
  • Increased Blood Pressure: Teriflunomide can raise blood pressure. Patients should have their blood pressure checked regularly and managed appropriately.
  • Respiratory Effects: Teriflunomide can cause serious lung problems, including interstitial lung disease. New or worsening breathing issues should be investigated, and treatment may need to be stopped.
  • Pancreatitis in Pediatric Patients: Although not approved for use in children, teriflunomide can cause pancreatitis (inflammation of the pancreas). If suspected, the medication should be stopped immediately.
  • Concurrent Use with Immunosuppressive Therapies: Using teriflunomide with other immunosuppressive drugs can increase the risk of side effects. Careful monitoring is required if switching from or adding other immune-modulating therapies.

Overdosage

There is limited data on teriflunomide overdose in humans. Studies show that healthy individuals tolerate doses of up to 70 mg daily for 14 days without severe side effects. If a significant overdose or toxicity happens, it is advised to use cholestyramine or activated charcoal to help remove the drug from the body more quickly.

Drug Interactions With Other Medications

  • Impact of Teriflunomide Tablets on CYP2C8 Substrates: Teriflunomide blocks CYP2C8, a liver enzyme that breaks down drugs like paclitaxel and pioglitazone. Taking these drugs with teriflunomide can cause them to stay in the body longer and increase their effects. Doctors should keep an eye on patients and adjust the doses of these drugs if necessary.
  • Effect of Teriflunomide Tablets on Warfarin: When teriflunomide is used with the blood thinner warfarin, it can reduce warfarin’s effectiveness by about 25%. It’s important to monitor the international normalized ratio (INR) to ensure warfarin is working properly.
  • Effect of Teriflunomide Tablets on Oral Contraceptives: Teriflunomide can raise the levels of hormones like ethinylestradiol and levonorgestrel in oral contraceptives. This might impact their effectiveness, so doctors may need to adjust the type or dose of contraceptives used with teriflunomide.
  • Effect of Teriflunomide Tablets on CYP1A2 Substrates: Teriflunomide might slightly increase the activity of CYP1A2, an enzyme that breaks down drugs like duloxetine and theophylline. This could make these medications less effective, so careful monitoring and possible dosage adjustments are needed.
  • Effect of Teriflunomide Tablets on Organic Anion Transporter 3 (OAT3) Substrates: Teriflunomide inhibits OAT3, a protein that helps remove drugs from the body. When taken with teriflunomide, drugs like methotrexate and furosemide, which are cleared by OAT3, may build up in the body. Monitoring and adjusting doses might be needed to avoid adverse effects.
  • Effect of Teriflunomide Tablets on BCRP and OATP1B1/1B3 Substrates: Teriflunomide inhibits BCRP and OATP1B1/1B3, proteins essential for drug transport within the body. For medications such as rosuvastatin and methotrexate, which depend on these proteins, dosage adjustments may be necessary to avoid toxicity. Close monitoring for elevated drug levels is crucial when using these medications alongside teriflunomide.

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Please note: A prescription is required to order Teriflunomide. 

Frequently Asked Questions

Teriflunomide is a medication used to treat relapsing forms of multiple sclerosis (MS). It reduces inflammation and immune responses that can damage brain and spinal cord nerve cells.
Yes, teriflunomide can cause itching as a possible side effect. Itching, also known as pruritus, is listed as a common side effect in the prescribing information for teriflunomide.
Teriflunomide is considered an immunomodulatory agent. It works by affecting the immune system to reduce inflammation and the activity of immune cells that could potentially damage nerves. While it doesn’t suppress the immune system as strongly as traditional immunosuppressants used in conditions like organ transplantation, teriflunomide helps modify immune responses in multiple sclerosis (MS) to manage the disease’s effects on the nervous system.
Teriflunomide modifies the body’s immune response by reducing certain cells, leading to decreased inflammation in the central nervous system. This helps treat conditions such as multiple sclerosis (MS), potentially preventing nerve damage and reducing the severity of MS symptoms.
No, it is not recommended to crush teriflunomide tablets. Teriflunomide tablets should not be crushed, split, or chewed. They should be swallowed whole with water.
Yes, teriflunomide may raise blood pressure in certain patients. It’s crucial to monitor your blood pressure consistently while using this medication. Let your doctor know if you observe higher readings. Clinical trials showed that 3.1% to 4.3% of teriflunomide patients had hypertension, compared to 1.8% on placebo.
Teriflunomide was approved by the FDA in September 2012 for patients with relapsing-remitting multiple sclerosis (RRMS).
Teriflunomide can stay in your system for a long time. In healthy adults, it usually takes up to four months after stopping the medication for most of it to be eliminated from the body. However, for some people, it can take up to two years to completely clear teriflunomide from their system.
The best time of day to take teriflunomide is the time that you can consistently take it every day. It can be taken with or without food, but it’s important to take it once daily as directed by your doctor.
  • Headache
  • Hair thinning
  • Diarrhea
  • Nausea
  • Abnormal liver tests
  • Increased blood pressure
  • Tingling or numbness

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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