leflunomide

medtigo

leflunomide

Brand Name :

Arava

Synonyms :

leflunomide

Class :

Immunosuppressants, DMARDS

Action and Spectrum

Actions and Spectrum:

leflunomide is a medication used to treat rheumatoid arthritis and other autoimmune disorders. The mechanism of action of leflunomide involves the inhibition of dihydroorotate dehydrogenase (DHODH), an enzyme involved in the de novo pyrimidine synthesis pathway. This leads to a decrease in the proliferation of T and B lymphocytes, which are involved in the pathogenesis of autoimmune diseases.

leflunomide has a broad spectrum of activity against various autoimmune disorders, including rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, and systemic lupus erythematosus. It has also been used to treat other diseases, such as psoriasis, sarcoidosis, and multiple sclerosis. Leflunomide is effective in reducing joint inflammation, slowing the progression of joint damage, and improving physical function in patients with rheumatoid arthritis.

Dosing & Uses

Drug Interaction

Adverse Reaction

Frequency defined

>10%

Respiratory infections (15%)

Diarrhea (17%)

1-10%

Alopecia (10%)

Rash (10%)

Bronchitis (7%)

Abdominal pain (5%)

Accidental injury (5%)

Dyspepsia (5%)

Dizziness (4%)

Hypertension (10%)

Nausea (9%)

Headache (7%)

Abnormal LFT’s (5%)

Back pain (5%)

UTI (5%)

Joint disorder (4%)

Weight loss (4%)

Cough (3%)

Gastroenteritis (3%)

Stomatitis (3%)

Vomiting (3%)

Allergic reaction (2%)

Dry skin (2%)

Pain (2%)

Pneumonia (2%)

Sinusitis (2%)

Infection (4%)

Pruritus (4%)

Anorexia (3%)

Pharyngitis (3%)

Tenosynovitis (3%)

Weakness (3%)

Chest pain (2%)

Eczema (2%)

Paresthesia (2%)

Rhinitis (2%)

Synovitis (2%)

Post-marketing reports

Pancreatitis

Erythema multiforme

Toxic epidermal necrolysis

Agranulocytosis

Neutropenia

Pancytopenia

Thrombocytopenia

Colitis

Stevens-Johnson syndrome

Vasculitis

Leukopenia

Black Box Warning

Black box warning:

leflunomide has a black box warning, the strongest warning that the US Food and Drug Administration (FDA) can require. The black box warning for leflunomide is related to its potential to cause liver injury, which can be severe and even fatal.

The warning states that leflunomide has been associated with acute liver failure, sometimes leading to liver transplant or death. The black box warning also highlights the need for monitoring liver function tests before starting leflunomide and periodically after that.

Contraindication / Caution

Contraindications/caution:

Contraindications:

Hypersensitivity to leflunomide: People who are allergic to leflunomide or any of its ingredients should not take this medication.

Pregnancy: leflunomide can harm an unborn baby. Women who are pregnant, planning to become pregnant, or breastfeeding should not take leflunomide.

Liver disease: leflunomide can cause liver damage. People with liver disease should not take this medication.

Immunodeficiency: leflunomide can lower the body’s ability to fight infection. People with a weakened immune system should not take this medication.

Severe renal insufficiency: leflunomide is not recommended for people with severe kidney disease.

Severe hematologic disorders: leflunomide is not recommended for people with severe blood disorders.

Active infections: leflunomide can worsen infections. People with active infections should not take this medication.

Caution:

Risk of infection: leflunomide can suppress the immune system, increasing the risk of infections. Patients taking leflunomide should be cautious about exposure to people with contagious illnesses, such as the flu or COVID-19.

Risk of gastrointestinal side effects: leflunomide can cause nausea, vomiting, diarrhea, and other gastrointestinal symptoms. Patients should report any persistent or severe gastrointestinal symptoms to their healthcare provider.

Risk of skin reactions: leflunomide can cause skin rash and other dermatological reactions. Patients should notify their healthcare provider if they develop a rash while taking this medication.

Risk of respiratory reactions: leflunomide can cause respiratory symptoms such as cough and shortness of breath. Patients should report any respiratory symptoms to their healthcare provider.

Interaction with other medications: leflunomide can interact with other medications, including warfarin, methotrexate, and cholesterol-lowering. Patients should inform their healthcare provider of all medications before starting leflunomide.

Pregnancy and breast-feeding: leflunomide can cause harm to a developing fetus and should not be taken during pregnancy or while breastfeeding.

Pregnancy / Lactation

Pregnancy consideration: leflunomide can harm an unborn baby. Women who are pregnant, planning to become pregnant should not take leflunomide.

Lactation: Excretion of the drug in human breast milk is unknown

Pregnancy category:

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology:

leflunomide is an immunomodulatory medication that is primarily used to treat rheumatoid arthritis. The pharmacology of leflunomide involves its effects on several biological pathways and cellular processes in the body, including:

Inhibition of dihydroorotate dehydrogenase (DHODH): leflunomide inhibits the activity of DHODH, an enzyme involved in synthesizing pyrimidines, a type of nucleic acid. By inhibiting DHODH, leflunomide reduces the production of pyrimidines, reducing the proliferation of immune cells such as T and B lymphocytes.

Anti-inflammatory effects: leflunomide has been shown to have anti-inflammatory effects by reducing the production of cytokines such as interleukin-1 beta (IL-1β), interleukin-6 (IL-6), and tumor necrosis factor-alpha (TNF-α).

Modulation of the immune response: leflunomide has been shown to modulate the immune response by reducing the activity of T and B lymphocytes and increasing the activity of regulatory T cells.

Metabolism: leflunomide is metabolized in the liver into its active metabolite, A77 1726, which has a half-life of about two weeks. A77 1726 is primarily eliminated from the body via urine.

Pharmacodynamics:

The pharmacodynamics of leflunomide refers to the drug’s effects on the body and its underlying biological mechanisms. leflunomide has several pharmacodynamic effects, including:

Immunosuppression: leflunomide reduces the proliferation of immune cells, including T and B lymphocytes. It achieves this effect by inhibiting the activity of the enzyme dihydroorotate dehydrogenase (DHODH), which is involved in the synthesis of pyrimidines, a type of nucleic acid that is essential for cell division.

leflunomide

No data available for drug.

DRUG INTERACTION

leflunomide

&

leflunomide +

Contraindicated

Serious Use Alternative

Monitor Closely

Minor

leflunomide

No data available for drug.

DRUG INTERACTION

leflunomide

&

leflunomide +

Contraindicated

Serious Use Alternative

Monitor Closely

Minor

medtigo

leflunomide

Brand Name :

Synonyms :

Class :

Action and Spectrum

Dosing & Uses

Drug Interaction

Adverse Reaction

Black Box Warning

Contraindication / Caution

Pregnancy / Lactation

Pharmacology