Teriflunomide - An Effective Treatment for Multiple Sclerosis

Drug Overview

Teriflunomide is a drug that has both anti-inflammatory and immunomodulatory properties. It acts by inhibiting the synthesis of pyrimidine. It is mostly used to manage the relapsing type of multiple sclerosis. The Food and Drug Administration (FDA) has approved Teriflunomide for managing multiple sclerosis but with the warning of hepatotoxicity and teratogenicity. Read the article in detail to know more about the usage, side effects, warnings, dosage, and mechanism of action of Teriflunomide.

How Does the Drug Teriflunomide Work?

The exact mechanism of Teriflunomide is not known yet. However, the proposed mechanism of the drug is that it acts by inhibiting the mitochondrial enzyme dihydroorotate dehydrogenase, which inhibits the synthesis of pyrimidine, thereby reducing the number of lymphocytes in the central nervous system. Much research still needs to be done to understand the exact mechanism of Teriflunomide in managing multiple sclerosis.

Uses

Teriflunomide drug is used to manage different variants of multiple sclerosis (a neuromuscular disease), such as

• Remitting form of multiple sclerosis.

• Relapsing form of multiple sclerosis.

• Secondary and progressive variants of multiple sclerosis.

• Clinically isolated variants of multiple sclerosis.

Doses

• Teriflunomide is available in oral tablets in two different dosages of 7 mg and 14 mg.

• It has to be taken orally with water. It can be consumed with or without food in the dosage prescribed by the doctor.

Warnings

Risk of Teratogenicity: Teriflunomide's use carries a teratogenicity risk, so it should be avoided in pregnant and lactating mothers.

Risk of Hepatotoxicity: Teriflunomide should be avoided in patients with hepatic impairment as it carries the risk of liver failure and death. It is advised to inform the doctor quickly in case of any symptoms like dark urine, abdominal pain, or jaundice (yellowish discoloration of the skin of eyes and skin is noticed).

Risk of Immunosuppression: Teriflunomide decreases the overall white blood cell count and has a risk of bone marrow suppression.

For Patients

What is Multiple sclerosis?

It is an autoimmune condition (when the defense mechanism of the body acts against its body cells) affecting the central nervous system (brain and spinal cord), resulting in demyelination of the nerve fibers. The associated signs and symptoms of multiple sclerosis are vision impairment, tingling and numbness in the limbs, loss of memory, and urinary problems.

Stages of Multiple Sclerosis

There are three stages of multiple sclerosis

• Relapsing stage.

• Primary progressive stage.

• Secondary progressive stage.

Know More About Teriflunomide Medication:

When and Why to Take Teriflunomide?

• Teriflunomide is a drug prescribed to adults with different variants of multiple sclerosis after a thorough examination of the patient's condition by the doctor.

• Teriflunomide is prescribed to the patient with multiple sclerosis to minimize the underlying symptoms by decreasing the swelling and immune cell activity that can cause damage to the nerve.

Effectiveness of Teriflunomide Against Multiple Sclerosis:

Teriflunomide is quite effective in reducing the symptoms associated with multiple sclerosis cases, like tingling and numbness in the limbs, memory loss, and bowel dysfunction.

Things to Inform The Doctor Before They Prescribe Teriflunomide Medication:

• Before starting with the drug Teriflunomide inform the doctor of any liver disease as the drug has a toxic effect on the liver.

• Inform the doctor if pregnant or planning to become pregnant, as the drug carries the risk of teratogenicity.

• Tell the doctor in case of any allergy to any drug or composition.

• Breastfeeding mothers should inform the doctor before starting the Teriflunomide drug as it carries the risk of teratogenicity

• Inform the doctor of any underlying diseases like tuberculosis, recent lung infections, or a history of any lung disease.

• Inform the doctor about any live vaccine administered recently or within the past six months.

• Inform the doctor in case of any history of blood disorders or immune system disorders.

Starting Teriflunomide Medication

How To Take Teriflunomide?

• Teriflunomide is available in oral tablet form at 7 mg and 14 mg.

• The drug can be taken with or without food once daily in the dosage prescribed by the doctor based on the patient's condition.

• It is advised to take the tablet as a whole with water and not to crush or chew the tablet.

Things to Do After One Starts Taking Teriflunomide

Look Out for the Side Effects

Common side effects associated with Teriflunomide are:

• Loss of hair.

• The blurring of vision.

• Toothache.

• Pain in the joints and muscles.

• Weight loss.

• Acne.

• Stomach upset.

• Nausea and vomiting.

• Stuffy nose.

• Shivering.

• Depression.

Serious side effects associated with Teriflunomide are

• Headache.

• Dizziness.

• Confusion.

• Pale skin.

• Fever, cough, and chills.

• Sore throat.

• Numbness and burning sensation in the hands and feet.

• Loss of muscular coordination and tone.

• Difficulty in swallowing.

• Rashes and peeling of the skin.

• Shortness of breath.

• Cold and gray skin.

• Swelling of the lips, face, and mouth.

• Chest tightness.

There are various other side effects of Teriflunomide. It is advised to inform the doctor immediately in case any side effects are observed.

Dietary Alterations: There is no such dietary alteration needed when on Teriflunomide. Teriflunomide can be taken with or without food.

What Should Be Done if the Dose Is Missed?

If the dose is missed or forgotten then take the dose as soon as remembered. Avoid taking double doses to compensate for the missed dose.

What Should Be Done in Case of Overdose of Teriflunomide?

In case of an overdose of Teriflunomide, inform the doctor as soon as possible and call the poison control center. In case of severe side effects like breathlessness and seizures, call the emergency services quickly and inform the poison control center.

What should be Avoided When on Teriflunomide Medication?

• Avoid close contact with persons with cold, flu, or upper respiratory tract infections as it may worsen the infections.

• Avoid receiving any live vaccine when on Teriflunomide medication and until six months after stopping the drug Teriflunomide.

• Avoid contact with individuals with live vaccines administered recently.

• Avoid the sports activities that increase the chances of cuts, bruises, and injury as it can worsen the condition.

Storage of Teriflunomide:

• The tablets of Teriflunomide are stored at room temperature of around 20 to 25 degrees Celsius.

• The drug Teriflunomide should be kept away from the heat, light, and moisture.

• Discard the drugs which are expired.

• Avoid discarding the medication in the drain or flushing the medication.

• Keep the drug away from the childrens and pets.

Avoid Self-Prescription: Teriflunomide should be consumed only if prescribed by the doctor after examining the patient and based on the clinical condition. The drug should be consumed in the exact dosage and schedule as prescribed by the doctor to minimize or reduce the adverse effects.

Staying On Teriflunomide:

• Teriflunomide should be taken at the exact dosage and schedule as prescribed by the doctor.

• Inform the doctor quickly in case any dose is missed.

• Check for improvement in the health status and symptoms. Inform the doctor about it in the follow-up visits.

• In case of worsening symptoms and health status, inform the doctor immediately.

For Doctors

Indications: Teriflunomide is indicated in patients with remitting, relapsing, and secondary progressive multiple sclerosis.

Pharmacology:

Mechanism of Action: Teriflunomide is an immunomodulatory agent that acts by restricting the synthesis of pyrimidine. The exact mechanism, however, is yet not known. Teriflunomide inhibits the mitochondrial enzyme dihydroorotate dehydrogenase, which inhibits the pyrimidine formation thereby resulting in decreased formation of activated lymphocytes in the central nervous system showing anti-inflammatory effects.

Pharmacodynamics: Teriflunomide is an immunomodulatory and anti-inflammatory agent that acts by inhibiting the formation of pyrimidine, thus reducing the volume of activated lymphocytes in the central nervous system.

Ingredients:

Active Ingredient: The only active ingredient is Teriflunomide.

Inactive Ingredients: The inactive ingredients are:

• Starch.

• Silicon dioxide.

• Lactose monohydrate.

• Magnesium stearate.

• Microcrystalline cellulose.

• Polyethylene glycol.

• Titanium dioxide.

• Ferric oxide yellow.

• Talc.

Absorption: The peak plasma concentration is reached after a single dose of oral Teriflunomide within one to four hours.

Distribution: The volume of distribution is around 11 liters after a single dose of Teriflunomide intravenously.

Metabolism: Teriflunomide is metabolized primarily through hydrolysis. Other secondary pathways are oxidation and sulfate conjugation.

Elimination: Teriflunomide is eliminated primarily through bile. Thirty-seven percent of the drug is eliminated from feces and 26 percent from urine.

Protein Binding: Almost 99 percent of the drug Teriflunomide is extensively bound to plasma proteins.

Total Body Clearance: The drug Teriflunomide has an average clearance of 30 mL per hour.

Toxicity:

• Teriflunomide shows toxic effects in pregnant and lactating mothers as it carries the risk of teratogenicity. So, it should be strictly avoided in pregnant and lactating mothers.

• The drug also carries the risk of hepatotoxicity and liver failure, so it should be strictly avoided in patients with liver impairment.

Half-Life: The estimated half-life of the drug is around 18 to 20 days.

Warning and Precautions:

• Teriflunomide should be avoided in pregnant and lactating women as it has a risk of teratogenicity, according to the studies.

• Teriflunomide should be avoided in patients with liver impairment as it is toxic to the liver and can result in liver failure or death due to toxicity.

• Teriflunomide should be avoided in patients with bone marrow disease, lung infections, and other serious infections. The drug can only be started in such patients after treating the underlying infection.

Doses and Forms:

The drug Teriflunomide is available in oral tablets form in the dosage of 7 mg and 14 mg.

Administration of the Drug:

• The drug Teriflunomide is prescribed orally, one tablet daily with water in the dosage recommended by the doctor after a thorough examination and monitoring of the patient's clinical condition.

• The patient's ALT (alanine amino transaminase) and bilirubin levels are monitored for six months after starting the drug.

• For children, the doctor determines the drug dosage based on the patient's symptoms.

• All the lab tests like complete blood cell count, liver function test, and kidney function test should be performed by the doctor before starting the Teriflunomide medications.

Contraindications:

• The drug Teriflunomide is contraindicated in patients with liver impairment as it is toxic to the liver and can result in liver failure.

• The drug Teriflunomide is contraindicated in pregnant and lactating mothers due to its teratogenic potential.

• The drug Teriflunomide is contraindicated in patients with underlying severe infection or bone marrow disease as it carries the risk of immunosuppression. It should only be started after the control of the underlying infections.

Drug Interactions:

• Adenovirus 7 live vaccine, if combined with Teriflunomide increases the risk of severity of infections..

• There is an increased risk of adverse side effects if the drug Teriflunomide is combined with Abatacept and Adalimumab.

• Teriflunomide, when combined with the drug Acetaminophen reduces its serum concentration.

• Teriflunomide, when combined with the drug Acyclovir, reduces its serum concentration.

• When combined with activated charcoal, the serum concentration of the Teriflunomide decreases.

Other Specifications:

• Teriflunomide in Pregnant and Lactating Women: Teriflunomide should be strictly avoided in pregnant and lactating women as it carries the risk of teratogenicity. Teriflunomide should be avoided in breastfeeding mothers as it can harm the fetus.

• Teriflunomide in Patients with Liver Impairment: There is an increased risk of liver failure and death if the drug Teriflunomide is used in patients with liver impairment. So, because of the hepatotoxic nature of the drug, it should be avoided strictly in patients with underlying liver disease.

• Teriflunomide in Patients with Severe Infections: Teriflunomide should be used cautiously in patients with severe infections, lung infections, or bone marrow disease. In such patients, drugs should be initiated only after the infection control is achieved, as it can result in immunosuppression.