Метортрит

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Метортрит

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Medically reviewed

Rosario Oropesa

Last updated on 22/12/2025

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 Метортрит

Quick Facts: Метортрит

Property Description
Active ingredient Methotrexate (INN)
Pharmacological class Immunosuppressant, DMARD
Chemical type Antimetabolite, Cytostatic agent
Dosage forms Solution for injection, Tablet
Origin / Status Synthetic compound, Prescription-only

What Type of Medicine is Метортрит and Its Core Identity?

Метортрит is a sophisticated synthetic pharmaceutical preparation defined by its active ingredient, Methotrexate (INN), a derivative of 4-amino-10-methylfolic acid. It belongs to the high-level pharmacological class of Immunosuppressants and Antimetabolites. This dual classification is clinically recognized for its potent ability to modulate systemic immune responses.

The core identity of this medication rests on Methotrexate, which functions chemically as a Folic acid antagonist and is also classified as a Cytostatic agent. This action places it uniquely within the category of Disease-Modifying Antirheumatic Drugs (DMARDs), a designation that signifies its established long-term use in managing chronic, debilitating conditions where immune dysfunction is central. As a prescription-only drug, it is intended for careful supervision in patients requiring systemic disease control.

Composition and Available Forms of Метортрит

The preparation is available as a single-ingredient product in two primary formats: an oral tablet and a solution for injection, the latter intended for parenteral routes of administration. The two forms facilitate flexibility in therapeutic delivery. The solution for injection is composed of the active Methotrexate dissolved in an aqueous vehicle, while the tablet form contains the drug compounded with solid excipients. Both forms are designed for systemic absorption to achieve predictable, body-wide therapeutic effects.

General Purpose and High-Level Action

The general purpose of Метортрит is to achieve systemic control over chronic, immune-mediated conditions by regulating the body's overactive defense system. Its high-level action involves the Antifolate mechanism, where it interferes with the necessary metabolic pathways, thereby slowing the rapid division of specific hyperactive immune and inflammatory cells. This fundamental biological interference provides the basis for modulating the underlying chronic disease process, rather than merely treating visible symptoms.

Regulatory References

  1. European Medicines Agency (EMA) EPAR: Jylamvo (Methotrexate)

What side effects are possible with Метортрит?

Possible Side Effects and Safety Information

Methotrexate (Метортрит) is a powerful medication and, while generally well-tolerated at the low, weekly doses used for non-cancer conditions, it can cause side effects. Regular monitoring through blood tests is essential to detect potential complications involving the liver, kidneys, and blood cell counts.

Common Side Effects

Side effects that are frequently reported and often manageable include:

  • Gastrointestinal issues: Nausea, vomiting, diarrhea, and mouth sores (stomatitis) are common. Taking folic acid as prescribed by your doctor can help reduce the risk of these effects.
  • General symptoms: Fatigue, headache, and a temporary thinning or loss of hair.

Serious but Rare Side Effects

Methotrexate is associated with a risk of serious, though infrequent, adverse events. Seek immediate medical attention if you experience signs of:

  • Infection: Fever, chills, sore throat, or other symptoms of infection, as the drug can suppress the immune system.
  • Liver problems (Hepatotoxicity): Yellowing of the skin or eyes (jaundice), dark urine, or pain in the upper right part of the abdomen. Alcohol consumption should be strictly limited or avoided due to increased risk of liver damage.
  • Lung problems (Pulmonary Toxicity): New or worsening shortness of breath, persistent dry cough, or chest pain.
  • Blood cell disorders (Myelosuppression): Unusual bruising or bleeding, or paleness, which can indicate a drop in red blood cells, white blood cells, or platelets.
  • Allergic reaction: Rash, hives, difficulty breathing, or swelling of the face, tongue, or throat.

Critical Safety Information

Methotrexate is contraindicated in pregnancy as it can cause severe birth defects and fetal death. Women of childbearing potential must have a negative pregnancy test before starting treatment and use reliable contraception during therapy and for a specified time after the last dose. Methotrexate can also increase skin sensitivity, so sun exposure should be minimized, and protective measures like sunscreen should be used.

Overdose and Emergency Response

Methotrexate overdose is a severe event documented to primarily affect the hematopoietic and gastrointestinal systems, requiring immediate emergency intervention.

Element Official Regulatory Documentation
Documented Overdose Manifestations Severe bone marrow suppression (leukopenia, thrombocytopenia, anemia) and profound gastrointestinal damage (ulcerative stomatitis, mucositis, gastrointestinal bleeding).
Life-Threatening Outcomes Acute renal failure, sepsis, and documented fatal outcomes, particularly following dosing errors.
Antidote Information The specific antidote is Calcium folinate (Folinic acid), which is mandated for immediate administration upon suspected overdose.
Specific Overdose Risk Highest risk of fatal outcomes is associated with the accidental daily administration instead of weekly dosing for non-neoplastic indications.

When Immediate Medical Help is Required

Seek emergency medical attention immediately upon any suspected overdose exposure. Management procedures involve the prompt administration of the specific antidote, Calcium folinate, ideally within one hour. Supportive measures, such as hydration and urine alkalinization, are required to prevent drug precipitation in the renal system. Continuous monitoring of serum methotrexate levels is mandated until they fall below 10^-7 mol/L. Patients with impaired renal function or fluid accumulation are noted in regulatory documents to be at specific risk for delayed drug elimination and increased toxicity.

Therapeutic Uses of Метортрит

What Метортрит Treats: Main Uses and Benefits

Метортрит is relevant for conditions requiring supportive systemic management of immune-mediated inflammatory or cellular activity. This medicine is considered relevant for the management of systemic chronic inflammatory conditions, notably Rheumatoid Arthritis and Polyarticular Juvenile Idiopathic Arthritis (pJIA), and severe Psoriasis. It is also applied in oncology for specific neoplastic diseases, including types of lymphoma and leukemia.

Management of Chronic Inflammatory Joint Diseases

This medicine is applied in situations where symptoms related to physical discomfort—specifically persistent joint pain, swelling, and stiffness—interfere with daily functioning. The therapeutic role is to support the easing of the overall symptom load and assists with maintaining functional stability during periods of heightened symptoms.

“This medication is considered relevant in conditions involving inflammatory or irritative processes that require long-term supportive management.”

Control and Symptomatic Support

Метортрит is generally considered relevant for addressing symptom clusters that may become intense or disruptive in conditions where symptoms may intensify temporarily. This treatment is applied in addressing conditions where symptoms are related to heightened physiological activity. It is relevant for easing symptoms related to systemic imbalance and can provide supportive relief when symptoms interfere with routine activities. It assists with maintaining functional stability and supports general well-being during symptomatic phases.

Quick Fact: Symptomatic Support in Inflammatory Conditions
Therapeutic Focus Supports easing symptoms related to systemic imbalance in chronic inflammatory conditions.
Symptom Focus Persistent joint pain, stiffness, and chronic swelling.
Patient Benefit Assists with maintaining functional stability and supports general well-being.

Eligibility and Restrictions for Use

The use of Метортрит (methotrexate) is governed by strict eligibility rules documented in official regulatory labeling. It is generally prescribed to select adults and children (for polyarticular juvenile idiopathic arthritis) who meet specific diagnostic criteria for conditions like rheumatoid arthritis or severe psoriasis.

Contraindications (Who Must Not Use)

This medicine is contraindicated in several specific populations due to the high risk of serious harm, as defined in official regulatory documents. These include:

  • Pregnant women (for non-neoplastic diseases) because it is a known human teratogen that can cause fetal death or severe birth defects. Both men and women of reproductive potential must use effective contraception during and for a specified period after treatment.
  • Individuals with a known severe hypersensitivity or allergic reaction to methotrexate.
  • Patients with significant pre-existing organ compromise, such as severe renal impairment (creatinine clearance less than 30 mL/min) or severe liver disease/chronic liver disease (e.g., cirrhosis, bilirubin levels > 5 mg/dL).
  • Those with alcoholism or excessive alcohol intake, as this significantly increases the risk of serious hepatotoxicity.
  • Patients with pre-existing serious blood disorders (e.g., leukopenia, thrombocytopenia, significant anemia) or a major immunodeficiency syndrome.

Lactation: Breastfeeding is generally not recommended or is contraindicated while taking this medication.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Regulatory documentation defines the interaction profile of Метортрит (Methotrexate) based on effects on drug clearance, potential for additive toxicity, and formal restrictions.

Pharmacokinetic and Toxicity Interactions

Co-administration with several products is documented to increase systemic exposure to the medicine, primarily due to interference with its elimination. Nonsteroidal Anti-Inflammatory Drugs (NSAIDs), including Ibuprofen and Naproxen, and Proton Pump Inhibitors (PPIs) are officially stated to potentially elevate and prolong serum methotrexate levels by competitively inhibiting renal transporters, increasing the risk of toxicity.

Oral antibiotics, such as penicillins and sulfonamides, are also documented to reduce the drug’s renal clearance, which can lead to increased serum concentrations. A separate restriction applies to drugs that are highly plasma protein-bound, which may increase the free concentration of the medicine in the blood.

Documented Pharmacodynamic Effects

The label notes an Additive Organ Toxicity risk. Co-administration with other hepatotoxic products, including alcohol, may officially increase the risk of liver damage. Furthermore, the combination of the medicine with radiotherapy is documented to increase the risk of soft tissue necrosis and osteonecrosis.

Food and Supplement Restrictions

Folic Acid supplements are documented to potentially reduce the clinical effectiveness of the medicine by acting as an antagonist, especially in neoplastic disease treatment. This interaction is rooted in competitive metabolic antagonism. Timing rules officially apply to the oral tablet, which may require administration separated by a meal to mitigate effects on absorption.

Population-Specific Notes

The interaction risk is officially noted to be heightened in populations with renal impairment and in those with third-space accumulations (e.g., ascites), as elimination is reduced, affecting how other interacting drugs modulate plasma levels.

Mechanism of Action

How Метортрит Works: Mechanism of Action

The drug exerts its systemic effect through two coordinated mechanistic domains. Firstly, it functions as a folic acid antagonist, competitively inhibiting the enzyme Dihydrofolate Reductase ( DHFR) to limit the availability of reduced folates required for the synthesis of nucleotides, thereby restricting the proliferation of activated immune cells.

Secondly, and crucial for its prolonged physiological effect, the drug is modified intracellularly into Polyglutamates ( MTX-PG), which inhibit AICAR Transformylase ( ATIC) in the purine synthesis pathway. Inhibition of ATIC leads to the accumulation and subsequent release of adenosine into the extracellular space. This increased adenosine acts as an indirect signaling molecule, activating surface Adenosine Receptors ( A2 A, A3) on inflammatory cells. This activation initiates an inhibitory cascade that downregulates the release of key pro-inflammatory cytokines (e.g., TNF-alpha) and limits the adhesion and migration of immune cells. This combined molecular cascade results in systemic anti-inflammation and immunomodulation at the physiological level.

Dosage and Administration Information

Official Administration Guidelines for Метортрит (Methotrexate)

The official instructions for Метортрит detail a highly structured administration protocol that defines the dose, frequency, and route based on the condition being addressed. The medication is approved for use via Oral (PO) tablet, and Parenteral routes including Subcutaneous (SC), Intramuscular (IM), Intravenous (IV), and Intrathecal (IT) injection.

Frequency and Dosing Principles

For chronic inflammatory conditions such as Rheumatoid Arthritis or Psoriasis, the essential instruction is to administer the medication Once Weekly. This weekly schedule is a mandatory constraint, and daily administration is strictly prohibited for these indications. Dosing for adults typically ranges from 7.5 mg to 25 mg per week, with administration adjustments defined by the patient's response.

Administration Scope Official Label-Based Instructions
Route of Administration Oral, Subcutaneous, Intramuscular, Intravenous, Intrathecal
Dosing Schedule Once Weekly (e.g., 7.5 mg to 25 mg) for chronic conditions; Cyclic protocols for oncology
Age-Group Rules Dosing for Polyarticular Juvenile Idiopathic Arthritis (pJIA) is calculated based on Body Surface Area (BSA).
Preparation Requirements Only the preservative-free formulation is approved for sensitive routes like intrathecal injection.

Procedural Context

Administration involving high doses, such as those used in specific oncology protocols, requires specialized procedural support, including measures like urinary alkalinization and subsequent Calcium Leucovorin rescue. For the oral form, consumption with food may result in a delay in drug absorption. The procedural rule for a missed dose is to immediately consult a specialist to determine the appropriate subsequent action.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Метортрит

Метортрит (Methotrexate) was studied in the context of specific chronic inflammatory and neoplastic conditions. The research is derived from established sources, including large Randomized Controlled Trials (RCTs) and scientific reviews. These studies help describe group patterns but do not determine whether an individual will respond similarly. Findings reflect the specific conditions under which they were conducted.


Evidence for Use in Rheumatoid Arthritis (RA)

The research base for its use in adult Rheumatoid Arthritis (RA) is extensive. Studies exploring this area include many Randomized Controlled Trials (RCTs) and subsequent large-scale Systematic Reviews and Meta-analyses. These trials examined patient groups over defined time intervals, often compared outcomes related to physical discomfort to a placebo or active control agents.

Research examined several outcomes related to systemic or functional imbalance, including changes in the number of tender and swollen joints, and how participants rated their overall disease activity. Long-term observational studies evaluating daily-life functioning were also applied in studies examining patient-reported experiences, tracking measures of physical disability and radiographic progression over several years.

Studies reported measurements demonstrating that participants reached defined response thresholds. However, research highlights changes measured during the study period only. Research describes patterns where a notable number of patients showed suboptimal response rates when examined for short-term symptom changes alone. Data gathered from long-term effects are not fully established through RCTs, as most persistence data are derived more extensively from observational studies.


Evidence for Use in Polyarticular Juvenile Idiopathic Arthritis (pJIA)

Research for Juvenile Idiopathic Arthritis (JIA), particularly the polyarticular course, was evaluated in studies that explored outcomes reflecting daily functioning or activity level in children and young people. These studies include both RCTs and analyses that pool data from existing trials. Studies explored how symptoms evolved in the observed populations, monitoring changes in joint activity and the achievement of specific disease activity response criteria.

Findings were mixed across some of the pooled analyses. While research was conducted that recorded improvement in some groups, the certainty remains low in some systematic reviews. This is primarily because the sample sizes were modest in many of the underlying trials, and there is limited information for long-term outcomes that track sustained health and development.


What Is Still Uncertain About Метортрит Research

Research highlights several areas where data are still emerging or where the certainty remains low. One key limitation is that comparative evidence is lacking for certain new combinations or strategies. Additionally, for the anti-inflammatory indications, follow-up durations were limited in many primary RCTs, meaning the information on long-term outcomes are not fully established outside of less controlled observational data.

Frequently Asked Questions (FAQ)

Common questions about Метортрит (FAQ)

Q: Does this medication make you sleepy or dizzy?

Yes, official product information indicates that dizziness and somnolence (sleepiness) are among the most common adverse reactions reported in adult clinical trials. This information is included in the safety warnings.

Q: Can I take this medicine with food?

Regulatory documents state that this medication may be taken orally with or without food. There are no specific restrictions on timing your dose relative to meals.

Q: What is the specific maximum dose per day?

The official product labeling defines a maximum recommended dose for adults. This limit is typically 600 mg/day for most conditions, though the maximum dose for Fibromyalgia is lower at 450 mg/day. The prescribing healthcare provider determines the appropriate dosage regimen.

Q: What should I avoid drinking while taking this medication?

The official label warns about the risk of dizziness and somnolence. Due to these potential effects, caution is advised when using the medicine alongside other Central Nervous System (CNS) depressants, which includes alcohol. Official information indicates that co-use could potentially increase the risk of these side effects.

Q: Is this medication safe to take if I have kidney problems?

Regulatory guidelines require dose adjustments based on a patient’s reduced renal function (kidney problems). The prescribing doctor assesses this factor before starting or adjusting treatment. This step is necessary because kidney function affects how the medicine is cleared from the body.

Q: How should I stop taking this medicine when I no longer need it?

Regulatory warnings state that when the medication is discontinued, it should be tapered gradually over a minimum period of one week. Abrupt discontinuation is discouraged, as this could potentially increase the risk of certain adverse events.

Q: Is it safe for pregnant women to use this drug?

Official information states that there are no adequate and well-controlled studies of the medication in pregnant women. Animal studies suggest potential risks to the fetus. The label notes that patients who become pregnant while on this medication may be asked to consult with their healthcare provider and consider enrollment in the NAAED Pregnancy Registry.

Q: Does this medicine affect fertility in men?

Animal studies showed some negative effects on the reproductive system in male rats. However, a clinical trial in healthy male subjects found that taking the medication at the maximum recommended dose for three months did not affect sperm motility. This information is available for review with a healthcare provider.

How should Метортрит be stored and disposed of?

How to Store and Dispose of Метортрит (Methotrexate): Official Guidance

Storage Requirements

Methotrexate must be stored in its original packaging at controlled room temperature ( 20 C to 25 C) and protected from light. Multi-dose vials, after first puncture, must be refrigerated ( 2 C to 8 C) and used within 30 days. All forms of the medicine must be stored locked up and kept out of the reach and sight of children and pets.

Handling and Disposal

Methotrexate is classified as a cytotoxic and hazardous drug. Contaminated sharps, including needles, syringes, and used pens, must be placed immediately into a dedicated puncture-resistant, cytotoxic sharps container.

Disposal must be conducted according to local, state, and national regulations, typically through a drug take-back program or an authorized hazardous waste collection service. Do not dispose of any Methotrexate product in household trash or down the drain.

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

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