Artrilab

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Medically reviewed

Marina Burgos

Last updated on 10/01/2026

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Artrilab

Property Description
Active ingredient Leflunomide (INN)
Form Film-coated tablet
Pharmacological class Disease-Modifying Antirheumatic Drug (DMARD)
General purpose Systemic control of chronic inflammation
Origin Synthetic isoxazole derivative

What Type of Medicine is Artrilab?

Artrilab is a prescription-only medication categorized as a conventional, non-biological Disease-Modifying Antirheumatic Drug (DMARD). This classification is reserved for agents that actively modify the course of chronic inflammatory conditions, contrasting with symptom-based treatments. The compound is a synthetic isoxazole derivative, a unique molecular structure within its therapeutic class. Artrilab is specifically supplied for oral administration as a film-coated tablet.

Leflunomide: The Composition and Nature

The essential active ingredient in Artrilab is Leflunomide. Its defining characteristic is its function as a prodrug, meaning the molecule is inert upon ingestion and requires metabolic conversion into its therapeutically active compound, Teriflunomide (metabolite A77 1726). This feature differentiates it from drugs that are active immediately upon administration. The active metabolite, Teriflunomide, is clinically recognized for its sustained immunosuppressant activity over time. The product is a single-ingredient formulation, focusing solely on the targeted action of Leflunomide.

What is the General Purpose of Artrilab?

The primary purpose of Artrilab is to achieve systemic control by moderating the destructive processes central to chronic inflammatory diseases. The medicine's action is rooted in its highly specific antiproliferative activity: it selectively inhibits the enzyme dihydroorotate dehydrogenase (DHODH), thereby preventing the rapid multiplication of specific disease-driving immune cells known as lymphocytes. This mechanism is designed to reduce the intensity of widespread inflammation, serving the critical function of slowing potential structural joint damage.

What side effects are possible with Artrilab?

Possible side effects and safety information

The safety profile of Artrilab (Leflunomide) is characterized by several serious risks officially documented by regulatory authorities, which necessitate specific usage constraints. The most critical concerns involve the potential for severe liver injury (hepatotoxicity) and fetal harm (teratogenicity), risks that are highlighted in official prescribing information.

Adverse reactions are classified by frequency across various System-Organ Classes (SOC):

Classification Representative Side Effects (SOC)
Very Common (≥1/10) Diarrhea, Headache (Gastrointestinal, Nervous System)
Common (1% to 10%) Nausea, Vomiting, Alopecia (hair loss), Elevated liver enzymes, Hypertension (Gastrointestinal, Skin, Hepatobiliary, Vascular)
Rare (<0.1%) Severe liver injury (Hepatitis, Hepatic failure), Interstitial Lung Disease (ILD) (Hepatobiliary, Respiratory)
Very Rare (<0.01%) Stevens-Johnson syndrome (SJS), Pancytopenia (Skin, Blood)

Serious Adverse Reactions and Constraints

The label documents the risk of serious infections, including opportunistic infections, due to the medicine's immunosuppressant activity. Rare but documented events include severe lung inflammation (Pneumonitis) and severe bone marrow suppression (Pancytopenia, Agranulocytosis).

Regarding time-related patterns, severe liver injury has been reported most frequently within the first 6 to 12 months of starting treatment. Due to the long half-life of its active metabolite, adverse effects may persist or appear for a sustained period after discontinuation.

Artrilab is contraindicated in specific patient populations, including women who are pregnant or planning to become pregnant, and those with severe pre-existing hepatic impairment or severe immunodeficiency states. These constraints structure the official understanding of the medicine’s risk profile.

Overdose and Emergency Response

Overdose and When to Seek Help

Regulatory authorities mandate that immediate medical attention must be sought if an overdose of Artrilab (Leflunomide) is suspected. Overdose may manifest through several documented signs and symptoms. These can include gastrointestinal effects such as diarrhea and stomach pain, as well as systemic signs like extreme tiredness, pale skin, fast heartbeat (tachycardia), and shortness of breath. A critical biochemical finding documented in overdose situations is the elevation of liver enzymes.

The most serious outcome officially described in regulatory information is the risk of severe and potentially fatal liver failure (hepatotoxicity). This severe toxicity can progress to conditions such as coagulopathy (clotting disorders) and encephalopathy. Patients with pre-existing hepatic impairment are specifically noted in labeling to be at a heightened risk for severe toxicity outcomes.

Immediate Emergency Actions

If a person has collapsed, is seizing, or is experiencing severe trouble breathing, emergency services must be contacted immediately. There is no specific antidote known for this compound. Due to the long half-life of the active metabolite, official guidance requires procedures for accelerated clearance, such as the administration of cholestyramine or activated powdered charcoal. Management is strictly symptomatic and supportive, and hospital monitoring may be required to observe the potential for delayed, severe effects.

Therapeutic Uses of Artrilab

What Artrilab Treats: Main Uses and Benefits

This medicine is commonly used in conditions characterized by inflammatory processes, such as Rheumatoid Arthritis (RA) and Psoriatic Arthritis (PsA) in adults. The medicine is relevant for conditions presenting with systemic or localized discomfort, such as active rheumatoid arthritis and active psoriatic arthritis. Artrilab is considered relevant for patients with chronic conditions, as it may play a role in managing symptoms related to active, progressive conditions, contributing to maintaining functional stability during long-term disease management.

The medication is applied in therapeutic domains involving certain distressing symptoms associated with active inflammation, which includes reducing persistent joint swelling and tenderness. It is relevant for managing symptoms that interfere with daily comfort, and may assist with easing debilitating, systemic fatigue related to high disease activity.


Quick Fact: Symptom Support in Inflammatory States

Artrilab is commonly used to help manage symptoms related to inflammatory or irritative states. It supports patients during episodes of heightened discomfort by contributing to easing the overall symptom load.

Regulatory References

  1. European Medicines Agency overview

Eligibility and Restrictions for Use

Who can and cannot use Artrilab?

Artrilab (Leflunomide) is officially permitted for adult patients (18 years and older) with active Rheumatoid Arthritis or Psoriatic Arthritis, as established by major regulatory bodies. Use in patients under 18 years of age is not recommended because the efficacy and safety profile has not been established.

The medicine is strictly contraindicated for several populations. These absolute prohibitions include pregnant women and breast-feeding women. Absolute non-eligibility also applies to patients with severe hepatic impairment and those with moderate to severe renal insufficiency, primarily due to limited clinical experience or safety risks defined in the regulatory label.

Use is also prohibited for individuals with severe immunodeficiency states (e.g., AIDS), severe hypoproteinaemia, or any known hypersensitivity to leflunomide or its active metabolite, teriflunomide. Additionally, treatment should not be initiated in patients with a serious or active infection. Special restrictions apply to women of childbearing potential, who must use reliable contraception, and to male patients who intend to father a child, requiring a drug elimination procedure.

What should I know about interactions with other medicines?

Artrilab Interactions with other medicines and products

This section outlines interactions with other medicinal products and substances as documented in official regulatory prescribing information for Artrilab (Leflunomide).


Documented Pharmacokinetic Interactions

The active metabolite of Artrilab, Teriflunomide, can modulate the clearance of co-administered drugs by inhibiting or inducing specific drug-metabolizing enzymes and transporters. The metabolite is documented to inhibit enzymes like CYP2C8 and transporters such as BCRP, OAT3, and OATP1B1/B3. This action may increase the exposure of co-administered medicines, including certain statins (like Rosuvastatin and Simvastatin) and Methotrexate. Conversely, the active metabolite is documented to induce CYP1A2, which can decrease the exposure of drugs metabolized by that pathway.


Restrictions and Additive Risk

Classification Constraint or Requirement
Formal Contraindication Co-administration with Teriflunomide is strictly prohibited to avoid excessive systemic exposure.
Pharmacodynamic Risk Combining with other potentially hepatotoxic or myelosuppressive treatments may result in an increased risk of serious adverse reactions due to additive toxicity.
Switching Procedure A mandatory washout procedure is required when switching to certain other DMARDs due to the long persistence of the active metabolite in the body.
Lifestyle Caution Caution is advised regarding alcohol intake due to the officially noted risk of increased hepatotoxicity.

Mechanism of Action

How Artrilab Works: Mechanism of Action

The mechanism of Artrilab is driven by its active metabolite, Teriflunomide, which initiates a highly selective anti-metabolite action to interrupt the proliferation cycle of specific immune cell populations.

Targeted Inhibition of Pyrimidine Synthesis

Teriflunomide acts as a selective and reversible inhibitor of the mitochondrial enzyme Dihydroorotate Dehydrogenase (DHODH). This primary molecular interaction blocks the rate-limiting step of the cell's de novo pyrimidine synthesis pathway. This inhibition results in the immediate depletion of the pyrimidine nucleotides required for DNA and RNA creation.

Selective Cytostasis and Systemic Modulation

Nucleotide depletion causes activated T and B lymphocytes to stop dividing and arrest in the G1 phase of the cell cycle (cytostasis). This targeted mechanism limits the rapid clonal expansion of specific immune cell populations, leading to a sustained modulatory effect on the adaptive immune system. By limiting the number of activated lymphocytes, the drug reduces the overall cellular capacity to produce and release pro-inflammatory cytokines (like TNF-alpha and IL-6) into circulation, thereby altering overactive systemic responses.

Dosage and Administration Information

How to Use Artrilab

Artrilab (Leflunomide) is administered according to a specific, continuous regimen to ensure consistent systemic control. This medication is available as a film-coated tablet and is taken via the oral route.


Official Dosing and Frequency

Usage typically begins with a short, high-dose loading phase to quickly achieve effective levels of the active metabolite, Teriflunomide, in the body. The subsequent maintenance phase establishes a steady, long-term dosing pattern. Treatment initiation is generally intended to be supervised by specialists experienced in chronic inflammatory conditions.

Regimen Phase Dose Frequency
Initial Loading Dose 100 mg Once daily for 3 days
Standard Maintenance Dose 20 mg Once daily
Reduced Maintenance Dose 10 mg Once daily (if 20 mg is not tolerated)

Administration Context and Special Conditions

Artrilab tablets should be swallowed whole with sufficient liquid. The medication may be taken with or without food, as meal timing does not significantly affect its absorption. The overall treatment is continuous and long-term, characteristic of Disease-Modifying Antirheumatic Drugs (DMARDs).

Population Considerations: No dose adjustment is required for older adults (65+). However, use in patients under 18 years is not recommended. Furthermore, due to the drug’s long half-life, a specialized accelerated elimination procedure using agents like cholestyramine is recommended upon discontinuation when rapid clearance is required, such as in women of child-bearing potential.

Note: Omission of the initial loading dose may be considered for patients deemed to be at increased risk of adverse events, allowing for a slower dose escalation.

Recent Clinical Evidence

Artrilab: Recent Clinical Evidence

The following is a summary of key findings from clinical research on Artrilab (leflunomide) in adults with specific rheumatic conditions. This information describes what studies have evaluated, and does not constitute medical advice or a guarantee of individual outcomes.


Core Efficacy Research

Research explored the role of Artrilab in the management of active rheumatoid arthritis (RA). Studies investigated whether the drug may be associated with a reduction in pain and inflammation and an inhibition of joint destruction over time.

  • Study Design: The primary data came from randomized, double-blind, placebo-controlled clinical trials, which represent the strongest type of evidence.
  • Key Finding: Studies evaluating the reduction of disease signs and symptoms, as measured by criteria such as the ACR scores, indicated that symptoms resolved for a greater proportion of participants in the active treatment group compared to the placebo group.
  • X-ray Analysis: Long-term trials included radiological assessment and evaluated whether the treatment influenced the progression of structural joint damage (erosions and joint space narrowing).

Dosage and Administration Studies

Research has also examined the drug's role in specific populations and the effects of different dosing schedules.

Study Focus Research Objective
Dosing Regimen Trials reviewed the effects of different dosing schedules, including the use of an initial loading dose versus a steady daily dose, to determine the time until clinical response was reported.
Combination Use Studies assessed the effect of Artrilab when used in combination with other established disease-modifying antirheumatic drugs (DMARDs) compared to using a single drug.

Long-term Effects

The duration of the studies evaluated the drug's effects during long-term use, documenting tolerability profiles and the frequency of adverse events over periods lasting up to several years. Continued research monitors the long-term impact on disease progression and functional status.

Key Studies & References

  1. ACR/EULAR 2017 classification criteria for rheumatoid arthritis
  2. 2021 American College of Rheumatology Guideline for the Treatment of Rheumatoid Arthritis

Frequently Asked Questions (FAQ)

Common questions about Artrilab (FAQ)

Q: How long after starting Artrilab can a patient generally expect to notice effects?

Studies and official information indicate that the full therapeutic benefit of Artrilab may take time to become noticeable. It is possible for a patient to experience the full therapeutic benefit only after 6 to 12 weeks of continuous use. The full effect may take time to develop.


Q: Are there any known long-term health risks associated with taking Artrilab for many years?

Regulatory documents highlight potential major adverse effects such as severe infection, significant lung injury, and blood disorders (cytopenia) that may occur over time. For this reason, official guidance recommends and often involves regular blood tests and clinical monitoring to assess these potential long-term risks during therapy.


Q: What are the signs of a potential allergic reaction to Artrilab?

According to official product information, signs of a potential severe allergic reaction include hives, difficulty breathing, or swelling of the face, lips, tongue, or throat. If any of these signs appear, it is recommended to contact emergency medical services right away.


Q: Does Artrilab carry a specific warning from regulatory bodies, such as a Boxed Warning?

Yes, the medication carries a Boxed Warning from regulatory bodies, which is the strongest safety notice. This warning specifically highlights the critical risks of severe liver injury (hepatotoxicity) and the potential for fetal harm (teratogenicity).


Q: Does Artrilab interact with any specific types of food or beverages?

The official prescribing information states that Artrilab can be taken with or without food, as meal timing does not significantly affect how it is absorbed. The primary lifestyle caution noted is that caution regarding alcohol intake is noted due to the documented risk of increased liver injury.


Q: Do interactions with Artrilab tend to increase or decrease its effect?

Official warnings focus on how Artrilab interacts with other medicines that affect the immune system or the liver. Combining it with other immunosuppressive or potentially hepatotoxic (liver-damaging) agents can lead to additive toxicity, meaning an increased risk of severe adverse effects.


Q: How is the research evidence for Artrilab generally summarized by regulatory bodies?

Regulatory summaries based on clinical trials indicate that Artrilab is considered effective in controlling joint inflammation and is associated with retarding the progression of structural joint damage. The evidence base is generally considered comparable to that of certain other Disease-Modifying Antirheumatic Drugs (DMARDs).


Q: Does Artrilab require special monitoring like regular blood tests or check-ups?

Yes, official guidance advises that regular monitoring is necessary throughout treatment. This typically involves blood tests, specifically for liver enzyme levels (ALT) and complete blood counts (CBCs). This monitoring is particularly crucial during the initial months to check for specific adverse effects.


Q: Are there generic versions of Artrilab currently available on the market?

Yes, the active ingredient in Artrilab, which is called Leflunomide, has generic versions that have been approved by the FDA and are generally available. The generic versions contain the same active ingredient and are approved by the FDA as therapeutically equivalent to the brand-name drug.


Q: What happens if a patient stops taking Artrilab suddenly?

Because the active compound can remain in the body for up to two years, an accelerated drug elimination procedure may be used to quickly reduce the concentration of the active metabolite in the system when treatment is stopped.


Q: Can Artrilab cause drowsiness or affect a person's ability to operate machinery?

According to official product information, side effects such as dizziness and headache are reported as common. Official guidance notes that caution may be necessary when performing activities like driving or operating machinery if these effects are experienced.


Q: Is weight change (gain or loss) noted as a common general side effect of Artrilab?

Regulatory side effect listings indicate that weight loss has been noted as a potential general side effect. This has been reported particularly in clinical trial populations using higher doses of the medication.


Q: Is it typical for minor side effects, like nausea, to decrease after the first few weeks of treatment?

Studies and patient information indicate that common gastrointestinal side effects, such as diarrhea and nausea, are typically mild. These minor effects are reported to generally improve or resolve over time with continued treatment.


Q: Can Artrilab be taken safely with common over-the-counter (OTC) pain or cold medicines?

Official regulatory warnings note the need for caution when combining Artrilab with over-the-counter products that may also affect the liver. This includes common pain relievers like acetaminophen (Tylenol), due to the potential risk of additive liver injury.


Q: Are there any herbal supplements or vitamins that are known to interact with Artrilab?

Regulatory product monographs generally state that specific interactions with herbal products or vitamins have not been established in clinical trials. All supplements should be discussed with a healthcare provider.


Q: What does it mean if a doctor prescribes Artrilab for an 'off-label' condition?

Off-label use refers to when a healthcare provider prescribes a medicine for a condition that is not listed in the official, regulatory-approved indications. This practice is based on the provider's medical judgment and is supported by clinical literature, rather than the drug's label.


Q: How long has Artrilab been available for prescription use?

The drug's active ingredient, leflunomide, was initially approved for prescription use by the FDA in 1998 for specific rheumatic conditions. This means the medication has been available on the market for several decades.


Q: Is Artrilab classified as a controlled substance in the U.S. or other regions?

No, the active ingredient in Artrilab, leflunomide, is not classified as a controlled substance under the U.S. Controlled Substances Act or similar regulations in most regions.


Q: Can taking Artrilab affect a person's mood or energy levels?

According to official reports, asthenia (unusual tiredness or weakness) is noted as a common side effect of the medication. Additionally, anxiety has been reported as a less common side effect associated with the use of the drug.


Q: What should a patient do if they accidentally take more Artrilab than usual?

In the event a patient takes more of the medication than prescribed, regulatory information states that emergency medical attention is necessary. This involves contacting emergency services or a poison control center right away.


Q: Is Artrilab used as a first-line treatment or usually after other drugs have failed?

Therapeutic consensus suggests that Artrilab is often considered for patients who have had an inadequate response to other initial Disease-Modifying Antirheumatic Drugs (DMARDs). It may also be used in combination with current medicines to achieve better disease control.


Q: What is the standard procedure for reporting a suspected side effect from Artrilab?

Reporting of suspected adverse reactions is handled through the national regulatory body. In the US, this is often done using the MedWatch system, and in the UK, it is the Yellow Card scheme.


Q: Can Artrilab interfere with the effectiveness of birth control pills?

The active metabolite of Artrilab has been shown to induce the CYP1A2 enzyme in the liver. This mechanism may potentially decrease the exposure of other medicines metabolized by this pathway, which can include certain types of hormonal contraceptives.

How should Artrilab be stored and disposed of?

How to Store and Dispose of Artrilab?

The official product labeling for Artrilab (Leflunomide) specifies strict storage and disposal requirements to ensure the medication's stability and environmental safety.

Required Storage Conditions

Artrilab tablets must be stored at room temperature, specifically below 25 C (77 F). The product must be kept in the original packaging or blister pack, and the container must remain tightly closed to protect the medicine from moisture. Consistent with all prescription medicines, Artrilab must be stored out of the sight and reach of children.

Official Disposal Rules

Unused or expired Artrilab must not be discarded by pouring it down a drain, flushing it down a toilet, or throwing it into household waste. Disposal must follow local requirements for pharmaceutical waste to ensure environmental protection.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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