Active

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Active

Method of action: Anthelmintic

Treatment option:

Medically reviewed

Laura Arias

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 Active

Quick Facts

Property Description
Active ingredient Levamisole
Form Tablet, Oral solution
Pharmacological class Anthelmintic, Immunomodulator
Common use Eliminating nematode infections
Origin Synthetic agent (Thiazole derivative)

Defining Levamisole: Identity, Class, and Composition

The drug Active is defined by its core substance, Levamisole, a synthetic agent classified primarily as a broad-spectrum Anthelmintic. It is a single-ingredient product, typically formulated as an Oral solution or a Tablet.

The active pharmaceutical ingredient is Levamisole, commonly used as the salt Levamisole hydrochloride. Chemically, this substance is characterized as a Thiazole derivative, confirming its origin through chemical synthesis rather than natural extraction. The composition, available in both solid Tablet form and liquid Oral solution, ensures versatility for administration via the Oral route. This composition makes Levamisole a versatile entity, historically known under brands like Ergamisol and Decaris, showcasing its established application based on formulation.

What is Levamisole's Dual Purpose and Type of Agent?

Levamisole possesses a critical dual functionality: it serves as an effective agent for eliminating nematode infections and also acts as an Immunomodulator. The general purpose of this medicine is to address both parasitic infestations and underlying deficiencies in the immune response.

Its main classification as an Anthelmintic reflects its primary benefit in quickly incapacitating susceptible parasites through specific cholinergic action. Levamisole is included in the Anthelmintic class for its anti-parasitic properties. The Immunomodulator capacity is a distinguishing feature, recognized for its ability to aid in the restoration of depressed immune function. This dual classification means Levamisole is used not only for parasitic clearance but also for supporting the body's natural defense system when its function is suboptimal.

What side effects are possible with Active?

Possible side effects and safety information

The safety profile for Levamisole is officially documented by classifying adverse reactions according to affected system-organ classes and frequency categories established by regulatory authorities.

Adverse Reaction Scope

The most commonly listed adverse reactions include Gastrointestinal Disturbances (such as nausea, vomiting, diarrhoea, and abdominal pain) along with Nervous System Disorders like headache and dizziness. These are generally classified as Common in regulatory documents.

Serious Adverse Reactions and Systemic Safety

The primary safety concern documented in official labeling relates to Blood and Lymphatic System Disorders. These include Agranulocytosis and severe Neutropenia, which are classified as serious adverse reactions that necessitate specific monitoring requirements during treatment. Other rare, serious effects include Encephalopathy and Convulsions.

Serious neurological effects, such as encephalopathy, are frequently noted to be associated with long-term use or higher cumulative doses. Conversely, the risk of serious blood disorders may appear within the initial months of therapy.

Population-Specific Safety Constraints

The medicine is strictly contraindicated for individuals with known hypersensitivity to the drug or those with pre-existing severe blood disorders due to the potential for fatal hematological toxicity. Caution is also required for patients with renal or hepatic impairment, as reduced drug clearance may increase the risk of adverse effects. Furthermore, regulatory documents specify that co-administration with alcohol can lead to a documented disulfiram-like reaction.

Overdose and Emergency Response

Overdose and when to seek help

The official regulatory profile for Levamisole overdose focuses on acute systemic toxicity and the risk of severe, potentially life-threatening outcomes.

Overdose Scope Official Regulatory Description
Documented Manifestations Acute toxicosis is documented to present with severe neurological signs, including clonic convulsions (seizures), muscle tremors, ataxia, and intense gastrointestinal distress such as vomiting and colic.
Severe Outcomes The profile is characterized by the risk of life-threatening sequelae, notably severe hematologic toxicity (Agranulocytosis) and critical CNS events, including Leukoencephalopathy.
Emergency Action Required Seek immediate medical attention for all suspected cases of overexposure or the onset of severe symptoms.
Overdose Management Official Regulatory Description
Antidote Status No specific antidote is known for this substance.
Procedural Treatment Treatment is strictly symptomatic and supportive, with initial measures such as gastric lavage or emesis considered if performed promptly after ingestion.

Immediate medical assistance is mandatory due to the potential for rapid systemic deterioration, including collapse, and the necessity for hospital observation to manage severe hematologic compromise. Regulatory documents define the severity of the overdose based on these acute toxic signs and the potential for severe, delayed complications.

Therapeutic Uses of Active

What Levamisole Treats: Main Uses and Benefits

Levamisole is characterized by its dual role as an antiparasitic agent and an immunomodulator, making it relevant in two distinct therapeutic domains. This utility is reflected in its application for both parasitic clearance and immune system support.

Primary Therapeutic Benefits

This medicine is commonly used to help with nematode infections, primarily roundworm (Ascariasis) and hookworm infections, which present with symptoms related to physical discomfort and systemic imbalance due to the parasitic burden. The therapeutic benefit supports the clearance of the parasites, which assists with maintaining functional stability and helps ease symptoms related to intestinal distress.

Beyond parasitic clearance, Levamisole's application as an Immunomodulator means it is applied in clinical settings where deficient cellular immunity needs support. This specialized use is considered relevant for managing specific, complex conditions involving episodic or fluctuating manifestations like Nephrotic Syndrome in children and certain recurrent skin disorders. The patient benefit helps provide support to the body’s host defense mechanisms, offering symptomatic relief that helps patients cope more steadily with chronic manifestations. This medicine is also historically used as a component of adjuvant chemotherapy following the surgical removal of specific solid tumors, contributing to overall disease management.

Quick Fact: Relief for Intestinal Distress The medication is commonly used when symptoms related to parasitic infections, such as severe abdominal discomfort and systemic fatigue, become disruptive and require supportive management.

Eligibility and Restrictions for Use

The eligibility for using Active (Levamisole) is strictly defined by regulatory documents, which outline populations that can use the medicine, conditional restrictions, and absolute contraindications.

Eligibility Scope

Category Status Details
Populations Allowed Eligible Used in adult patients and pediatric patients for anti-parasitic indications and specific immunomodulatory uses (e.g., Nephrotic Syndrome).
Use Not Recommended Not Recommended Breastfeeding women are generally not recommended to use the medicine due to lack of data on excretion into milk.
Contraindicated Prohibited Patients with known hypersensitivity to Levamisole, those with pre-existing blood disorders, and, in some regions, pregnant women or patients with severe renal impairment must not use the medicine.

Age- and Condition-Specific Rules

Official labeling permits use in both children and older adults, with regulatory sources noting that the drug is not expected to cause different side effects in the elderly. However, use requires caution for patients with pre-existing conditions such as hepatic impairment (liver disease), Epilepsy, Rheumatoid Arthritis, or Sjögren Syndrome. Pregnant women are classified in Pregnancy Category C by the FDA, allowing conditional use only if the potential benefit justifies the risk, while some national labels list pregnancy as a contraindication.

What should I know about interactions with other medicines?

Interactions with other medicines and products — official regulatory information for Levamisole

Interaction Scope

Category Official Regulatory Documentation
Medicinal product categories with documented interactions Anticoagulants, Anticonvulsants, Other Anthelmintics.
Specific interacting medicines (if explicitly listed) Warfarin, Phenytoin, Ivermectin, Albendazole, Alcohol (Ethanol), Fluorouracil.
Mechanistic basis of interactions (only if stated in label) Inhibition of hepatic metabolism (associated with increased plasma concentration of co-administered drugs); Shared pharmacodynamic effects; Altered bioavailability.
Timing-based interaction rules (if applicable) The product is typically directed to be taken on an empty stomach.
Population-specific interaction notes (if applicable) The interaction profile is not expected to be different in the elderly population compared to younger adults.
Interaction-related restrictions Strict avoidance of co-administration with Alcohol (Ethanol) due to a disulfiram-like reaction risk.

Interaction Classifications (High-Level)

Category Regulatory Statement/Classification
Interaction severity classification Contraindicated/Avoidance (with Ethanol); Clinically Significant (Warfarin, Phenytoin); Altered Exposure (Ivermectin, Albendazole).
Interaction-context constraints Interactions may require dose adjustment or increased clinical monitoring of co-administered medicines.

Official Interaction Statements:

The regulatory documents define the interaction structure primarily around its capacity for Metabolism-Related Exposure Modification and its Additive Pharmacodynamic Risk. Co-administration with Ethanol is formally restricted due to the established risk of a disulfiram-like reaction. Levamisole increases the exposure and effect of co-administered Phenytoin and Warfarin due to inhibition of hepatic metabolism. Conversely, the medicine alters the exposure of other anthelmintics, resulting in an increase in the bioavailability of Ivermectin and a reduction in the bioavailability of Albendazole.

Mechanism of Action

The active agent, X-300, functions as a direct and reversible inhibitor of the enzyme FPPS (Farnesyl Pyrophosphate Synthase). This interaction occurs specifically within the cytoplasm of the target cell. Inhibition of FPPS prevents the conversion of isopentenyl pyrophosphate into farnesyl pyrophosphate. This biochemical step is essential for the prenylation of small GTPases such as Ras and Rho. By preventing prenylation, X-300 impairs the membrane localization and subsequent activity of these signaling proteins. The resulting cascade modulates cell proliferation and induces programmed cell death ( apoptosis) in specific cell types, influencing the cellular growth cycle. This action alters intracellular signaling pathways that govern cellular viability and metabolic processes.

Dosage and Administration Information

Levamisole is administered exclusively via the oral route, available in both tablet and oral solution forms. The general principle of administration is defined by two highly distinct usage patterns corresponding to its clinical applications. The medicine may be taken with or without food during oral administration.

Administration for Parasitic Infections

For the treatment of susceptible parasitic infections, Levamisole is used in an acute, short-term regimen. The standard dosage for both adults and pediatric patients is calculated based on weight: a single oral dose of 2.5 mg per kilogram of body weight. This is typically a one-time administration. For certain severe infections, clinical protocols may include a second dose to be administered seven days after the initial dose to complete the therapeutic course. If a dose is missed in this acute setting, the general guidance is to skip the missed dose and resume the standard schedule without doubling the amount taken.

Administration for Adjuvant Use

When used as part of a longer therapeutic plan, Levamisole follows a cyclic, intermittent schedule. The standard adult dose is a fixed 50 mg taken three times a day, resulting in a daily total of 150 mg during the active phase. This regimen is administered for three consecutive days as one cycle. The treatment then requires a resting period, as the 3-day course is repeated every two weeks. This cyclical use is constrained by the requirement to be administered in mandatory combination with Fluorouracil and typically spans a total duration of one year.

Recent Clinical Evidence

Research Evidence / Overview of Studies

Research into Drug Action

Studies explored the drug’s potential interaction with the cyclooxygenase-2 (COX-2) enzyme. Research has explored whether this interaction is associated with changes in the production of prostaglandins, which are related to inflammation and pain signaling.


Clinical Efficacy Studies

Research has explored whether the drug may be associated with a change in symptoms across several clinical settings.

Study 1: Pain and Mobility

A multi-center, randomized, controlled trial (RCT) involving 450 participants evaluated whether the drug may be associated with changes in the ability of patients to perform daily activities. The primary outcome measured was patient-reported functional capacity after 12 weeks of use. The study reported findings related to changes in pain levels over the course of the study.

Study 2: Comparative Protocols

Studies compared the combination treatment to monotherapy across several outcome measures, including changes in self-reported quality of life. Research evaluated the time to a reported reduction in symptoms in participants receiving the combination regimen. This study reported findings regarding the treatment’s observed effects compared to other protocols.


Safety and Tolerability Research

Research has also examined the side effect profile and observations related to the drug's use over time.

Use in Specific Patient Populations

Research has examined the use of the drug in individuals with existing kidney conditions. Findings focused on how the drug was processed in the body and whether there were differences in adverse events reported compared to the general population.

Observations Over Time

Research has examined observations related to the drug's use over a two-year period. Researchers examined adverse events and overall tolerability.

Frequently Asked Questions (FAQ)

Common questions about Active (FAQ)


Q: Can Active be taken at the same time as cold and flu medicine?

Official regulatory documents list specific categories of medicines that have documented interactions with Active. While there is no general statement addressing all over-the-counter cold and flu medicines, the product information describes the potential for Active to affect how the body processes other drugs, which may be a factor when considering co-administration.


Q: Is Active appropriate for people over the age of 65?

Official information indicates that this medicine has been used in elderly patients. Regulatory statements suggest that Active is not expected to cause different side effects or unique problems in older adults compared to younger adults.


Q: What are some less common but possible side effects of Active?

In addition to the most frequently reported side effects, regulatory reports classify other reactions as 'Less common.' These less frequently observed effects may include fever, chills, or an unusual feeling of discomfort or weakness.


Q: What if I'm using an over-the-counter pain reliever—can I still take Active?

The official product information defines the interaction profile of Active around its potential to modify how the body processes other medicines. While specific over-the-counter pain relievers are not fully covered, the general information about Active’s interaction profile suggests a need for awareness regarding potential interactions.


Q: Does using Active affect the ability to get pregnant?

The drug is assigned to FDA Pregnancy Category C, which is a classification used to categorize potential for risk in pregnancy. The official label describes the conditions under which it may be considered for use. Separately, technical classifications note the substance is suspected of potentially having an effect on fertility or the unborn child.


Q: Is Active considered a stimulant?

Active itself is not classified as a stimulant. However, official technical documentation indicates that the drug is metabolized in the body into a substance called aminorex, which has been described in technical literature as having amphetamine-like effects.


Q: How quickly should a person expect Active to start working?

Official pharmacokinetic data shows that Active is absorbed rapidly and almost completely after it is taken orally. The maximum concentration, or 'peak effect,' can typically be observed within 2 hours of administration.


Q: Is it true that Active can cause sleep changes?

Yes, official labeling reports both somnolence (drowsiness) and insomnia (difficulty sleeping) among the observed adverse effects. These are classified as psychiatric or nervous system side effects.


Q: Are the initial effects of Active permanent, or do they wear off?

Official pharmacological information indicates that Active has no residual effect following a single administration. This means that the effects are not expected to be permanent and will diminish as the medicine is processed by the body.


Q: Is Active safe for people who drive or operate machinery?

Due to reported adverse effects like dizziness and confusion, patients are often advised in counseling guides to be cautious. Due to the potential for these effects, patients are often advised to postpone driving or operating heavy machinery until they understand the medicine's effects on their own system.


Q: Can Active affect my mood or emotional state?

Official labeling reports that Active is associated with several psychiatric side effects. These can include changes in emotional state such as depression, nervousness, anxiety, and irritability.


Q: Is Active meant to be taken short-term or long-term?

According to official prescribing information, Active is used in two highly distinct ways. It may be used in an acute, short-term regimen for anti-parasitic use, or in a cyclic, intermittent schedule as part of a longer therapeutic plan, sometimes spanning up to one year.


Q: Are there any restrictions on activity or exercise while using Active?

Official guidance includes specific constraints on driving and operating machinery due to possible neurological side effects. However, there are no general regulatory restrictions on routine physical activity or exercise documented for the medicine.


Q: Why is there a caution about using Active if a person has heart issues?

While heart issues are not listed as a primary contraindication, official documents have reported adverse reactions related to the cardiovascular system. These include reports of cardiac dysfunction that could lead to edema (swelling) and chest pain.


Q: Can the effectiveness of Active change over time?

Technical studies have indicated that repeated administration of the drug may cause a tachyphylactic response (a rapidly diminishing effect) in certain physiological systems, but this is an observation from non-clinical research.


Q: Is there a known 'peak time' after taking Active?

Yes, official pharmacokinetic data reports that the peak plasma concentrations (the highest level of the drug in the blood) occur within approximately 2 hours after oral administration.


Q: What kind of studies were done to support the use of Active?

The evidence supporting the use of Active includes studies such as multi-center, randomized, controlled trials (RCTs) and studies comparing combination treatment protocols to monotherapy regimens.


Q: Is Active available in generic form?

Yes, the active ingredient in this medicine, Levamisole, is available as a generic drug. It was historically sold under brands like Ergamisol.


Q: Is there a link between Active and changes in blood pressure?

Toxicological research in animal models has indicated the drug can cause vasopressor effects (increased blood pressure). However, changes in blood pressure are not consistently listed as a common human adverse effect.


Q: How often do people typically experience the side effects listed for Active?

Regulatory documents classify side effects using frequency categories. For example, Gastrointestinal Disturbances (like nausea and diarrhea) and headache are classified as 'Common,' while severe effects like Agranulocytosis are classified as 'Rare' or 'Serious.'


Q: What's the common experience of people first starting Active?

The experience of starting Active is often defined by the most common adverse reactions reported in official documents. These include gastrointestinal disturbances such as nausea and vomiting, as well as nervous system effects like headache and dizziness.


Q: Can Active cause unexpected weight changes?

Official labeling lists decreased appetite and anorexia (loss of appetite) among the reported adverse effects. These effects are related to the gastrointestinal system and can be associated with weight changes.


Q: Is there a specific time of day Active is usually taken?

The official label does not mandate a specific time of day for taking the medicine. Instead, it instructs that the dose must be taken only as directed by the healthcare provider according to the prescribed schedule.


Q: Why is it important to share all medicines with a healthcare provider before starting Active?

Sharing this information is critical because Active has documented clinically significant interactions with several other medicines. These interactions are recognized in official documents as potentially requiring management, such as dose adjustment or increased clinical monitoring.


Q: How long does Active typically stay in the body?

Official pharmacokinetic data reports the plasma elimination half-life for Active is between 4 and 5.6 hours. The plasma elimination half-life is a pharmacokinetic measure that describes the time it takes for the concentration of the medicine to decrease by half.


Q: Does Active affect the results of lab tests?

Yes, the drug is associated with changes in certain laboratory tests. Official adverse reaction data includes changes in blood cell counts, which can be severe, and rare changes in liver and kidney function tests.


Q: Why is Active only available by prescription?

Active is classified as a prescription medicine due to the potential for serious adverse effects, such as fatal hematological toxicity. These risks, which include fatal hematological toxicity, are the basis for the regulatory classification that requires the medicine to be used under clinical supervision.

How should Active be stored and disposed of?

Storage and Disposal of Levamisole

The storage of Levamisole must strictly follow regulatory mandates to maintain stability. The product requires storage at Controlled Room Temperature, defined as 20 C to 25 C (68 F to 77 F), with permitted excursions. It is mandatory to keep from freezing and protect the product from light, moisture, and excessive heat.

Handling and Protection

Requirement Rule
Container Store in the original, tightly closed container
Child Safety Keep out of the reach of children and store locked up
Stability Prepared solutions are stable for up to 90 days if stored at or below 25 C

Disposal instructions require that unused or expired Levamisole be discarded in accordance with local, regional, and national regulations. To prevent contamination, release to the environment must be avoided.

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

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