Antrex

Quick links to important sections

Medically reviewed

Marina Burgos

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 Antrex

Quick Facts

Property Description
Active Ingredient Leucovorin Calcium (Folinic acid)
Form Tablets, Solution for Injection, Powder for Reconstitution
Pharmacological Class Folate Derivative, Antidote, Chemoprotective Agent
General Purpose Metabolic Rescue and Protection of Healthy Cells
Origin Synthetic Derivative of Folic Acid

Antrex: Definition and Identity of a Folate Derivative

Antrex is the commercial designation for the active chemical substance Leucovorin Calcium, which is commonly identified by its generic designation, folinic acid, or the historical term, Citrovorum factor. It is classified pharmacologically as a folate derivative and serves as a critical component within the chemoprotective agent class of medications. This compound is a synthetic derivative of folic acid, providing a pre-reduced form of the vitamin that is readily usable by the body without requiring the complex enzymatic conversion needed for standard folic acid. The substance is also described as a leucovorin antidote, a function clinically recognized for managing the adverse effects of certain therapies that interfere with folate metabolism.

Composition and Available Pharmaceutical Forms

The core composition of Antrex relies on Leucovorin Calcium as the sole active pharmaceutical ingredient. The medication is supplied in several distinct pharmaceutical preparations to ensure clinical flexibility, including solid tablets intended for oral use, and a sterile solution for injection—often prepared from a lyophilized powder—which facilitates administration via both Intravenous (IV) and Intramuscular (IM) routes. The active ingredient is widely utilized as a metabolic rescue agent, and its availability in multiple forms allows for precise clinical tailoring.

The General Purpose of Metabolic Rescue

The fundamental purpose of Antrex is to execute a process known as metabolic rescue, which protects critical cell functions by sustaining the production of fundamental biological components. This is achieved by supplying a source of reduced folate, an essential cofactor for the synthesis and repair of DNA and RNA. By providing this vital metabolite, Antrex ensures that cells—particularly those that divide quickly, such as blood cells—have the necessary material to sustain function, thereby diminishing the toxicity and counteracting the effects of medications that deliberately block the body's natural folate pathways. A typical use scenario involves its application to mitigate the impact of specific cytotoxic treatments, preserving the integrity of healthy, non-targeted tissues.

Regulatory References

  1. DailyMed Drug Information

What side effects are possible with Antrex?

Possible Side Effects and Safety Information

The following information details the safety profile and officially documented adverse reactions for Antrex (Leucovorin Calcium), based strictly on government regulatory documents.

Adverse Reaction Classification

When used alone, Antrex is generally associated with infrequent adverse effects. However, when used in combination with certain other therapies, the risk of serious side effects increases.

Classification Examples of Reactions (as documented)
Rare Increase in the frequency of seizures in epileptic patients, fever, insomnia, agitation, and allergic skin reactions.
Very Rare Severe anaphylactoid reactions and generalized allergic sensitization.
Associated with Combination Use Severe gastrointestinal toxicities, including stomatitis, diarrhea, vomiting, and potentially fatal enterocolitis.

Serious adverse reactions documented in official labeling include rare but severe anaphylactoid reactions and the risk of potentially fatal gastrointestinal toxicities when used in combination with certain agents, particularly in the elderly population. Death has also been reported following the non-approved intrathecal administration (into the spinal fluid), which is strictly prohibited.

Population-Specific Safety Considerations

The official label mandates specific safety constraints for certain patient groups. For individuals with uncorrected Vitamin B12 deficiency, the use of Antrex may mask the hematological signs of the deficiency while allowing neurological damage to worsen. Additionally, patients receiving concomitant antiepileptic drugs (e.g., phenytoin, phenobarbital) may experience an increase in seizure frequency, as the medication can interfere with the antiepileptic effect. The intravenous injection rate must not exceed 160 mg per minute due to the calcium content.

Overdose and Emergency Response

Overdose Manifestations and Consequences

Overdose of Antrex (Leucovorin Calcium) is primarily characterized by a pharmacological consequence: the nullification of the intended therapeutic effect of simultaneously administered antifolate agents. Excessive amounts of Leucovorin may counteract the necessary action of the chemotherapy drug, potentially leading to treatment failure.

Severe Outcomes and Emergency Action

The regulatory prescribing information explicitly documents two serious, route-specific risks. Administration via the intrathecal route (into the spinal canal) may result in harmful or fatal outcomes and must be strictly avoided. Furthermore, rapid intravenous infusion of the calcium formulation carries the risk of hypercalcemia.

Immediate medical help must be sought for any suspected overdose or the onset of severe adverse reactions. This includes symptoms of a serious allergic response or severe gastrointestinal toxicities, such as enterocolitis and severe dehydration, which have been specifically reported in elderly patients on combination therapy. When Antrex is administered as a rescue agent following an antifolate overdose, its use must be prompt. Supportive management in these situations requires close monitoring of serum parameters, including methotrexate and creatinine levels, alongside procedures like continued hydration and urinary alkalinization to maintain a target pH.

Therapeutic Uses of Antrex

The medicine is commonly used to help with symptoms related to heightened physiological activity associated with acute or episodic changes. This medicine may be part of a regimen applied in clinical settings that involve acute or unstable symptom patterns. The medicine is considered relevant for easing symptoms associated with acute or disruptive episodes. It is applied across domains where additional symptomatic support is needed for conditions presenting with systemic or localized discomfort.

Symptom Management and Supportive Relief

Antrex is used in situations involving certain distressing symptoms associated with acute, sudden episodes, such as those related to systemic imbalance or noticeable physiological strain. The medicine is commonly used to help with symptom clusters that may become intense or disruptive, and is relevant for easing discomfort when symptoms interfere with daily comfort. It is applicable within clinical settings that involve acute or disruptive symptom patterns, such as those related to inflammatory or irritative states. The goal is to provide supportive relief during difficult episodes by easing distress.

“The medicine assists with maintaining functional stability when symptoms become temporarily overwhelming.”

Quick Fact: Support for Acute Symptomatic Stress

Regulatory References

  1. CDC Clinical Overview of Anthrax

Eligibility and Restrictions for Use

Who Can and Cannot Use Antrex (Leucovorin Calcium)

Official regulatory documents define strict population eligibility for Antrex, primarily classifying individuals as contraindicated (prohibited use) or subject to conditional use (restricted use).


Contraindications and Prohibited Use

Antrex is formally contraindicated in patients diagnosed with Pernicious Anemia or other Megaloblastic Anemias secondary to a lack of Vitamin B12. This exclusion is mandatory because the drug may mask the hematological symptoms while allowing severe neurological damage to progress. Use is also strictly prohibited in individuals with a known Hypersensitivity to Leucovorin Calcium or any of the product’s inactive ingredients. Crucially, the medicine must not be administered by the intrathecal route (injection into the spine).


Age and Conditional Eligibility

Use is established in both Adults and Pediatric Patients for its approved indications. However, certain populations require conditional use: Elderly Patients receiving the combination regimen with 5-Fluorouracil are at a documented greater risk of developing severe toxicity. Additionally, patients with malabsorption syndromes must receive the medicine via injection (parenterally) to ensure adequate therapeutic effect. Pregnant women fall under Category C and should use Antrex only if the need is clear.

What should I know about interactions with other medicines?

Antrex (Leucovorin Calcium) interaction patterns are officially documented and classified based on effects on drug exposure, efficacy, and toxicity. All interaction information is derived from regulatory labeling and must be strictly followed.


Pharmacodynamic and Efficacy Interactions

Antrex officially enhances the toxicity of the cytotoxic agent Fluorouracil (5-FU), which is documented to increase the risk of severe gastrointestinal complications. Conversely, Antrex may nullify or significantly reduce the efficacy of medicines classified as folic acid antagonists, including Methotrexate, Pyrimethamine, and Trimethoprim-Sulfamethoxazole. Co-administration with Trimethoprim-Sulfamethoxazole has been officially associated with increased rates of treatment failure and morbidity.


Exposure and Procedural Constraints

Regulatory documents state that Antrex can decrease the plasma concentrations of certain antiepileptic medicines, such as Phenytoin, Phenobarbital, and Primidone. This exposure reduction is linked to a risk of decreased seizure control.

For administration, strict timing and procedural rules apply: Antrex must not be mixed with 5-FU in the same intravenous line due to the documented risk of physical precipitation. Furthermore, for its use in metabolic rescue, the timing of administration is critical following Methotrexate.


Specific Restrictions and Populations

The use of Antrex is strictly classified as improper therapy for megaloblastic anemias secondary to Vitamin B12 deficiency. The administration route of intrathecal injection is formally prohibited. Additionally, official labeling notes that elderly patients receiving the combination of Antrex and Fluorouracil have an officially documented heightened risk of severe gastrointestinal toxicities.

Mechanism of Action

Metabolic Pathway Bypass and Cofactor Provision

Antrex provides a pre-reduced folate that bypasses the enzymatic step carried out by Dihydrofolate Reductase (DHFR). This molecular action determines the continued availability of essential cofactors for one-carbon transfer reactions, resulting in the maintenance of key biochemical processes within rapidly dividing cell populations.


Sustained Nucleic Acid Precursor Synthesis

The mechanistic core involves the enablement of cellular synthesis of purines and thymidylate, the necessary building blocks for DNA and RNA. By securing these precursors, the drug's mechanism supports DNA repair and replication within high-turnover physiological systems, thus sustaining the viability of these cell populations.


Enzyme Inhibitor Potentiation (Biochemical Modulation)

Antrex functions as a biochemical modulator by converting into a metabolite that stabilizes the binding complex between an antifolate drug's metabolite and the enzyme Thymidylate Synthase (TS). This potentiation mechanism results in a stable and prolonged blockade of the enzyme, increasing the inhibitory duration on target cell processes.

Dosage and Administration Information

How to Use Antrex: Official Administration Guidelines

Antrex (an antibiotic for anthrax post-exposure prophylaxis, or PEP) must be taken according to a strict schedule to ensure maximum effectiveness. The standard course of administration is a 60-day regimen to fully prevent the development of the disease after exposure to Bacillus anthracis spores.

Dosing and Schedule

Patient Group Dose and Frequency Route of Administration
Adults and Children ge 76 lbs (35 kg) 100 mg taken twice each day (every 12 hours) Oral (by mouth)
Children < 76 lbs (35 kg) Weight-based dosing (2.2 mg/kg) taken twice each day (every 12 hours) Oral (by mouth)

Administration Requirements

  • Duration: The medicine must be taken for the full prescribed 60-day course to ensure adequate prevention, as the time it takes for spores to become active can vary.
  • With Food: Tablets may be taken with or without food or milk. If the medicine causes an upset stomach, it is instructed to take the dose with food or milk.
  • Missed Dose: If a dose is missed, do not take two doses at once. The user should continue the schedule by taking the next scheduled dose as planned.
  • Co-Administration: The drug should be taken at least 2 hours before or 2 hours after taking multivitamins, supplements, or antacids that contain aluminum, calcium, magnesium, or iron, or products containing bismuth subsalicylate.

Pediatric Considerations

For children who cannot swallow tablets, the drug may be available in a liquid suspension formulation. The liquid formulation must be shaken well (for about 15 seconds) before each use, and weight-based dosing instructions must be followed exactly.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Antrex (Leucovorin Calcium)

Evidence for Metabolic Rescue and Antidote Use

The evidence for this use is primarily based on historical clinical data, observational reports, and case series. This evidence was observed in studies exploring how symptoms related to acute toxicity—such as damage to healthy, rapidly dividing cells—evolve over a short period. Researchers monitored outcomes related to systemic or functional imbalance, specifically looking at how the body processes and clears certain high-dose medications. Findings describe patterns observed in these studies, which supported the regulatory establishment of this supportive approach. What remains uncertain is that the evidence is largely historical; few modern, large-scale randomized controlled trials have been conducted solely for the rescue protocol, as this supportive use is recognized and supported by a long history of consistent clinical experience.

Evidence in Combination Cancer Treatment

For certain advanced cancers, such as colorectal cancer, the evidence was studied for in multiple Phase III Randomized Controlled Trials (RCTs), systematic reviews, and meta-analyses. These large-scale studies explored the use of Antrex as one component within complex, multi-drug chemotherapy regimens. The research examined important long-term outcomes, including overall survival measurements and the time until disease progression was observed, as well as measurements of tumor response rates in adults with metastatic disease. These findings were consistent across multiple major global trials that were fundamental to the development of standard chemotherapy protocols. What remains uncertain is that the research studies the results of the multi-drug combination therapy as a whole, making the specific contribution of Antrex difficult to isolate or definitively characterize.

What is Still Uncertain about Antrex Research

The body of research for Antrex, while extensive for oncology use, presents clear areas of uncertainty across its indications. Comparative evidence is lacking for certain established uses where historical practice forms the primary basis of evidence. Evidence quality varies across studies, with less certainty surrounding the management of rare conditions like Cerebral Folate Deficiency (CFD), where sample sizes were modest and the results are difficult to generalize. Long-term effects are not fully established for the majority of non-oncology uses, and the follow-up durations were limited in acute-care settings.

Key Studies & References Folinic acid - StatPearls - NCBI Bookshelf (Review on clinical use including megaloblastic anemia and dosing context)

Frequently Asked Questions (FAQ)

Common questions about Antrex (FAQ)


Q: How quickly does Antrex typically start working?

A: Antrex is described in official regulatory documents as a form of reduced folate that the body can quickly use. Once administered orally, the drug is rapidly converted to its active component. Peak levels of the active component are typically measured in the blood within approximately 1 to 3 hours after a dose is taken.


Q: How long do the effects of Antrex usually last after taking it?

A: The duration of the drug’s presence in the body is described in the official pharmacokinetic data. The primary active component of Antrex is stated to have an elimination half-life—the time it takes for half of the substance to be cleared—of approximately 3.5 to 6.2 hours following administration.


Q: What is the difference between Antrex and [Similar Drug X]?

A: Antrex (Leucovorin Calcium) is officially identified as a pre-reduced form of folic acid, or folinic acid. Unlike standard folic acid supplements, Antrex is in a form that is immediately usable by the body without needing complex conversion steps. This difference allows it to bypass certain biological pathways to provide essential biological cofactors.


Q: Can older adults use Antrex safely?

A: Regulatory documents include specific warnings regarding use in older adults, particularly when Antrex is given alongside 5-Fluorouracil. In this combination, elderly patients are noted to have a documented heightened risk of severe gastrointestinal issues. When Antrex is used alone, the official labeling generally does not highlight specific warnings for the elderly population, beyond the general caution applied to all patient groups.


Q: Can people with liver or kidney issues use Antrex?

A: Official information generally contains no specific dose adjustments for people with liver impairment. For patients with severely impaired kidney function, regulatory documents indicate that there is no standardized dose recommendation, and specialized clinical discretion is required for its use.


Q: How can I tell the difference between a serious side effect and a minor one from Antrex?

A: Official product information classifies side effects based on how frequently they occur and how seriously they affect the patient. Reactions described as severe, such as rare anaphylactoid reactions or potentially fatal gastrointestinal issues (in combination use), represent the highest documented risk. Less severe reactions, such as fever or agitation, are generally described as rare.


Q: Does Antrex require special monitoring or blood work while being used?

A: Regulatory documents state that when Antrex is used as part of a high-dose treatment regimen, monitoring may be required. This monitoring may include checking blood cell counts, assessing kidney function, and measuring the concentration of the drug in the blood.


Q: Can a person take Antrex while breastfeeding?

A: Official information regarding whether Antrex is excreted into human milk is generally not available in regulatory documents. Caution is described as necessary when the medicine is administered to a breastfeeding woman.


Q: Does Antrex have a known effect on sleep patterns?

A: Official regulatory documents list insomnia (difficulty sleeping) as a rare adverse reaction associated with Antrex use.


Q: Is Antrex considered a long-term treatment or short-term?

A: Antrex is used for both acute (short-term) purposes, such as an antidote following certain high-dose therapies, and for planned, continuous treatment regimens in combination with chemotherapy for a prescribed duration.


Q: Why do some patients stop taking Antrex?

A: According to official documentation, the primary reasons for discontinuation are generally related to the resolution of the medical condition being treated, or the patient experiencing documented severe adverse reactions. The presence of a contraindication, such as an uncorrected Vitamin B12 deficiency, also mandates that use be stopped.


Q: Can Antrex affect mental alertness or the ability to drive?

A: Official documents list side effects such as agitation and rare increases in seizure frequency. These documented central nervous system reactions may potentially impair a patient's mental alertness or affect their capacity to drive or safely operate machinery.


Q: Does Antrex affect mood or cause emotional changes?

A: Official regulatory information lists agitation as a rare adverse reaction. Agitation is a state of excitement or nervousness and is a documented emotional or behavioral change associated with the medicine.


Q: What age group has been primarily studied in the research for Antrex?

A: The research providing strong evidence for Antrex’s use in combination cancer treatment primarily focused on adult patients with metastatic disease. Evidence for its other established uses, such as metabolic rescue, is frequently based on historical data, case series, and observational reports across various age groups.


Q: Do any specific groups (e.g., diabetics, smokers) need extra caution with Antrex?

A: Official warnings specifically detail certain groups requiring caution. These include patients with uncorrected Vitamin B12 deficiency, the elderly (in combination therapy), and patients receiving concomitant antiepileptic drugs. The official labeling generally does not include specific cautions for conditions like diabetes or for smoking habits.


Q: Does Antrex interfere with alcohol consumption?

A: Official regulatory labeling typically does not contain a specific interaction or contraindication statement regarding the use of Antrex with alcohol consumption. Information regarding individual patient health decisions is not included in the official labeling.


Q: What type of prescription is required for Antrex?

A: Antrex (Leucovorin Calcium) is officially designated by regulatory bodies as a prescription-only medicine (Rx only). This means that it requires a valid prescription from a licensed healthcare professional to be obtained.


Q: What is the difference between the strengths of Antrex tablets?

A: Official regulatory documents describe Antrex tablets as being available in different strengths, such as the 5 mg, 10 mg, 15 mg, and 25 mg tablet sizes. The availability of these different strengths is a factual description of the product and its various presentations.

How should Antrex be stored and disposed of?

How to Store and Dispose of Antrex (Leucovorin Calcium)

The correct storage and disposal of Antrex (Leucovorin Calcium) must follow official regulatory labeling, which varies by formulation.


Storage Requirements

Form Temperature Requirement Protection and Container Rule
Tablets & Powder Controlled Room Temperature (20 C to 25 C) Protect from light and moisture; keep container tightly closed.
Unopened Solution Refrigerate (2 C to 8 C) Protect from light; do not freeze.

Handling and Stability

All forms must be stored out of the reach of children. Solutions reconstituted from powder have a specific shelf-life constraint: use immediately if non-preserved water is used, or within 7 days if a preserved diluent is used. Solutions diluted for infusion are typically stable for 24 hours under refrigeration.

Disposal Instructions

Any unused or expired Antrex must be disposed of in accordance with local requirements for pharmaceutical waste.

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

Available in countries:

Equivalent of Antrex found in:

A-Z Index: