Metirel

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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 Metirel

Quick Facts

Property Description
Active ingredient Hydroxychloroquine sulfate
Form Oral tablet
Pharmacological class Antimalarial, Disease-Modifying Anti-Rheumatic Drug (DMARD)
Common use Immune system modulation and antimalarial defense
Origin Synthetic compound (4-Aminoquinoline derivative)

Metirel is a trade name for a synthetic prescription-only medication whose active component is Hydroxychloroquine sulfate. This drug is classified as a 4-Aminoquinoline compound, a class known for its established utility in the management of both certain parasitic diseases and chronic inflammatory autoimmune disorders. It is recognized as a key treatment option in health systems.


Hydroxychloroquine: A Dual-Class Antimalarial and DMARD

Metirel is an Rx-only medication recognized for its dual role as both an antimalarial and a Disease-Modifying Anti-Rheumatic Drug (DMARD). This dual classification signifies that the drug is clinically recognized for its ability to modify the underlying disease processes in chronic autoimmune conditions, differentiating it from medications that only manage symptoms.

Its general purpose is to provide systemic control over the inflammation and dysregulated immunity characteristic of disorders like systemic lupus erythematosus. As a synthetic derivative of chloroquine, Hydroxychloroquine is generally preferred for long-term use in rheumatic diseases because it is considered to have a lower risk profile concerning ocular toxicity compared to its predecessor. This preference for Hydroxychloroquine in long-term treatment relates to its specific physicochemical properties.

Composition and Physical Form of Metirel

The medicine is supplied for patient use as an oral solid dosage form, specifically a tablet, which is the prescribed route of administration. The active ingredient is Hydroxychloroquine sulfate, a synthetic compound. This single-ingredient tablet form delivers the active substance combined with necessary pharmaceutical excipients to ensure a stable and consistent oral preparation for systemic absorption. The medicine achieves a prolonged half-life due to its inherent pharmacological properties, which supports the steady therapeutic levels required for sustained immune system modulation.

What side effects are possible with Metirel?

Possible Side Effects and Safety Information

Metirel, which contains hydroxychloroquine sulfate, has an official safety profile focused on risks across several major organ systems, with specific emphasis on ocular and cardiac safety. This information is derived exclusively from governmental regulatory documents.


Officially Documented Adverse Reactions

The most frequently reported adverse effects include gastrointestinal issues, such as nausea, vomiting, diarrhea, and abdominal pain, as well as headache.

Serious adverse reactions are officially documented and include:

  • Ocular Toxicity: The primary safety concern is irreversible retinal damage (maculopathy). Regulatory documents note this risk is directly related to cumulative dosage and treatment duration, and visual changes may progress even after cessation of therapy.
  • Cardiotoxicity: The label highlights the risk of fatal and non-fatal cardiomyopathy and serious arrhythmias, including Torsades de pointes.
  • Hematological and Systemic Risks: Severe blood disorders, such as aplastic anemia and agranulocytosis, as well as severe cutaneous adverse reactions (e.g., SJS, TEN, DRESS syndrome) are documented.

Safety Constraints and Special Populations

Adverse effects are officially grouped by System-Organ Classes, covering the nervous system (e.g., seizure, dizziness), skin (e.g., rash, pigmentation changes), and musculoskeletal system (e.g., muscle myopathy).

Safety constraints include contraindication for individuals with a known hypersensitivity to 4-aminoquinoline compounds or pre-existing retinal changes caused by this drug class. Caution is noted for specific patient groups, including those with hepatic or renal impairment and those with G-6-PD deficiency (risk of hemolysis).

Overdose and Emergency Response

Overdose and when to seek help

Overdose of Metirel (hydroxychloroquine sulfate) is officially described as a severe, life-threatening emergency requiring immediate action. Acute ingestion of a massive dose may lead to rapid onset of toxic effects, often occurring within 30 minutes to two hours.

Documented Manifestations and Severe Outcomes: Official regulatory information notes that overdose may present with drowsiness, headache, visual disturbances, and vomiting. However, the primary risks involve the Cardiovascular System and Central Nervous System. Severe outcomes include ventricular arrhythmias, QRS and QT prolongation, severe hypotension, and progression to cardiovascular collapse and cardiac arrest. Convulsions (seizures), respiratory arrest, and significant hypokalemia are also documented consequences.

When Immediate Medical Help Is Required: Due to the risk of sudden cardiac and respiratory arrest, official regulatory documents state that an individual must seek immediate medical attention for any suspected overdose. Emergency services must be contacted immediately if the affected person has collapsed, had a seizure, is experiencing trouble breathing, or cannot be awakened.

Management and Monitoring: Regulatory guidance confirms there is no specific antidote for this overdose. Management must be prompt, symptomatic, and supportive. Procedures may include gastric decontamination with activated charcoal and the use of pharmacological support like epinephrine. Continuous cardiac monitoring (EKG) and laboratory assessment for electrolyte abnormalities are mandatory. The documents also note that children are especially sensitive to the toxic effects.

Therapeutic Uses of Metirel

What Metirel Treats: Main Uses and Benefits

Metirel (hydroxychloroquine sulfate) is commonly used across therapeutic domains involving chronic autoimmune disorders and parasitic infections. This medication is relevant for managing specific conditions, including Systemic Lupus Erythematosus (SLE), Rheumatoid Arthritis, and uncomplicated malaria. It is considered relevant in clinical settings that involve acute or disruptive symptom patterns, where it assists with maintaining functional stability.


Therapeutic Benefit and Symptom Focus

In chronic inflammatory conditions, Metirel supports the patient during difficult episodes by easing distress related to systemic inflammation and may assist with managing the frequency of symptomatic flares. It is used when groups of symptoms, such as joint swelling, stiffness, and persistent physical discomfort, appear suddenly or fluctuate. The application of this therapy is considered relevant in contexts involving heightened systemic burden, contributing to easing the overall symptom load.

For infectious disease management, the medication is applied in addressing the symptoms related to heightened physiological activity during acute malarial attacks. It is also commonly used for prophylactic prevention in situations requiring short-term symptomatic assistance when traveling to areas where malaria is common.

Quick Fact: Support for Symptoms Related to Inflammation
Therapeutic Focus Chronic systemic inflammation and joint symptoms
Benefit Supports day-to-day comfort and stability
Context Applied in conditions involving inflammatory or irritative processes

Regulatory References

  1. NIH MedlinePlus Drug Information

Eligibility and Restrictions for Use

Eligibility Map: Who Can and Cannot Use Metirel — Official Regulatory Information

This section outlines the official population eligibility and non-eligibility rules for Metirel (hydroxychloroquine sulfate) as defined by authoritative governmental regulatory bodies.

Category Official Regulatory Status (as stated in label)
Populations for whom use is allowed Adults for approved autoimmune conditions and uncomplicated malaria treatment/prophylaxis.
Populations for whom use is contraindicated Patients with known hypersensitivity to 4-aminoquinoline compounds.
Patients with pre-existing retinopathy or other serious maculopathy.
Age-related eligibility rules Pediatric: Use for chronic indications is generally not established or is contraindicated for long-term therapy. Use for malaria is not recommended in children below a specific body weight (e.g., 31 kg) due to the fixed tablet strength.
Geriatric: Use requires caution due to increased likelihood of reduced renal, hepatic, or cardiac function.
Condition-specific eligibility rules Use requires caution in patients with hepatic or renal impairment, psoriasis, porphyria, or existing blood disorders (e.g., G6PD deficiency).
Pregnancy and lactation eligibility status Pregnancy: Use is generally reserved for cases where the clinical benefit to the mother is determined to outweigh the potential risk to the fetus.
Lactation/Breastfeeding: Excreted into breast milk; use is often considered acceptable for a healthy infant by professional guidelines, but requires careful consideration.

Official Eligibility Statements:

  • Use is contraindicated in patients with a known allergy to any 4-aminoquinoline derivative.
  • The medicine is contraindicated if the patient has pre-existing damage to the retina or macula.
  • Use is limited by potential exacerbation of psoriasis or porphyria.

Connection to the overall eligibility profile: Regulatory bodies define eligibility by establishing absolute prohibitions based on hypersensitivity or pre-existing severe ocular disease. For populations not absolutely excluded, eligibility is often conditional, mandating caution or potential dosage adjustment when the patient has pre-existing hepatic, renal, or specific metabolic/skin conditions.

What should I know about interactions with other medicines?

Interactions with other medicines and products

When taking any medicinal product, including Metirel, it is essential to consider the potential for drug-drug, drug-food, or drug-substance interactions. Interactions can occur when one product affects the way the body handles another, changing its absorption, metabolism, or elimination. This can lead to increased or decreased levels of the medicine in the body, which may alter its effectiveness or the risk of side effects.

  • Enzyme-Mediated Interactions: The liver contains enzymes, such as the cytochrome P450 (CYP) family, which are responsible for metabolizing many drugs. If Metirel is a substrate, inhibitor, or inducer of these enzymes, it may significantly affect the blood levels of other medicines that share the same metabolic pathway. This requires careful consideration when taken with other medicines known to be potent CYP enzyme modulators.
  • Common Interacting Classes: Interactions are often observed with products that affect the central nervous system (CNS), or those that alter the heart's electrical activity, such as certain anti-arrhythmics or anti-psychotics. Products that alter the body’s electrolyte balance, such as some diuretics, may also warrant caution.
  • General Guidance: Before starting Metirel, and throughout the course of treatment, patients should inform their healthcare provider and pharmacist about all prescription drugs, over-the-counter medicines, herbal supplements, and dietary products they are using. This comprehensive disclosure is the primary step to identify and manage any potential interactions. Do not start or stop any other medication without first consulting a healthcare professional.

Mechanism of Action

The action of Hydroxychloroquine sulfate is centered on two distinct but complementary immunomodulatory mechanisms that occur inside specific cells, modulating excessive immune signaling and altering internal cellular processes.


Intracellular pH Modulation and Antigen Presentation

The drug acts as a weak base, concentrating in and raising the pH of acidic cellular compartments (lysosomes and endosomes) within immune cells. This pH elevation interferes with the enzymatic activity required for proper antigen processing and subsequent presentation on MHC Class II molecules. This molecular cascade ultimately reduces the ability of T-cells to become fully activated, leading to a modulation of the adaptive immune response pathway.


Inhibition of TLR Signaling and Cytokine Release

Hydroxychloroquine directly targets and inhibits pattern recognition receptors, specifically Toll-like Receptor 7 ( TLR7) and TLR9, located inside endosomes. By blocking the binding of nucleic acid ligands to these receptors, the drug suppresses the innate immune signaling cascade, which, in turn, reduces the downstream production and release of pro-inflammatory mediators, such as Type I Interferons and certain cytokines. This interference restricts the systemic generation of inflammatory signals.


Interference with Parasite Detoxification

A separate mechanistic pathway is observed in malarial parasites: the drug concentrates in their food vacuole and inhibits heme polymerase. This action prevents the conversion of toxic heme into non-toxic hemozoin, leading to the accumulation of cytotoxic free heme and resulting in parasite cellular failure.

Dosage and Administration Information

Metirel, a trade name for hydroxychloroquine sulfate, is prescribed exclusively as an oral tablet and must be administered strictly by the oral route. To support gastrointestinal tolerance and absorption, the medication is consistently taken with a meal or a glass of milk. Dosing follows highly specific regimens defined by the reason for use, which dictates both the amount and frequency of administration.

For long-term conditions like systemic lupus erythematosus (SLE) and rheumatoid arthritis (RA), administration is typically a once-daily or twice-daily schedule, with maintenance doses generally ranging from 200 mg to 400 mg per day. The maximum dose for chronic use is rigidly constrained and should not exceed 6.5 mg/kg of body weight per day. Because Metirel's action is cumulative, a sustained duration of use over weeks or months is often required before the full effect is observed.

In contrast, the regimen for malaria prophylaxis requires a once-weekly 400 mg dose, beginning one to two weeks before entering an endemic area and continuing for four full weeks after departure. For the acute treatment of uncomplicated malaria, a short, three-day course totaling 2000 mg is followed, beginning with an 800 mg initial dose. Pediatric dosing is also weight-based, requiring careful calculation.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Metirel

This section provides a descriptive overview of the research available for Metirel (hydroxychloroquine sulfate) by detailing the study designs and the outcomes researchers monitored, without providing clinical advice or treatment recommendations. The evidence described highlights what has been observed so far in study groups, and these findings reflect the specific conditions under which the research was conducted.


Evidence for Use in Systemic Lupus Erythematosus (SLE)

Metirel has been evaluated in research exploring the long-term patterns of Systemic Lupus Erythematosus (SLE). Research exploring how symptoms change over time includes Randomized Controlled Trials (RCTs) and large, long-term observational cohort studies that monitor patient health for many years. These studies monitored specific outcomes, including overall survival, the accumulation of irreversible damage to organs, and the frequency of sudden symptom flare-ups.

Research so far indicates that studies have consistently reported measurements tracking lower rates of these acute symptomatic changes. Furthermore, long-term observational data suggest an association with measurements reflecting overall survival rates and tracking lower rates of long-term organ damage accumulation in the observed populations.

️ Evidence for Use in Rheumatoid Arthritis (RA)

Metirel was studied for its use in Rheumatoid Arthritis (RA). The evidence base includes RCTs comparing the drug against placebo or other Disease-Modifying Anti-Rheumatic Drugs (DMARDs), as well as systematic reviews that combine these findings. These trials assessed short-term and intermediate symptom patterns, examining standardized indicators related to physical discomfort and systemic imbalance.

Clinical trials reported measurements indicating changes in disease activity scores and joint-related outcomes reflecting daily functioning. Studies monitored the evolution of symptoms over defined time intervals and described patterns related to the resolution of joint swelling and tenderness. However, evidence is limited regarding the drug's effect on preventing irreversible joint damage (radiographic progression) compared to other DMARDs where this outcome was studied.

What Remains Uncertain About Metirel Evidence

The existing evidence base contains several research gaps and uncertainties. Data for certain groups, such as specific ethnic populations or those with multiple complex health conditions, remain insufficient to draw broad conclusions. Furthermore, comparative evidence that directly contrasts Metirel against all newer treatment options is lacking in head-to-head trials. For the malaria indication, certainty remains low in areas where widespread drug resistance has been documented. The research provides context but not individual predictions; findings describe group patterns, not personal outcomes.

Frequently Asked Questions (FAQ)

Common questions about Metirel (FAQ)

Q: How quickly should Metirel start working?

A: For chronic autoimmune conditions, official information indicates that the full effect of the medicine is typically not seen right away. Initial signs of benefit may take several weeks to one or two months to become noticeable, and it can take up to six months of consistent use to achieve the complete therapeutic effect.

Q: What is the expected timeframe for feeling the effects of Metirel?

A: The therapeutic response to this medicine is often gradual due to its specific mechanisms of action. Studies and official documents show that measurable symptom relief may begin one to two months after starting treatment. The complete expected timeframe for feeling the full effects typically requires up to six months of continuous use.

Q: How long does one dose of Metirel stay active in the body?

A: The medicine is known to have a prolonged elimination half-life, which describes the time it takes for the body to clear the substance. According to official product information, the terminal half-life typically ranges from 32 to 50 days. This long duration supports the steady therapeutic levels required for treating chronic conditions.

Q: Can Metirel be taken with alcohol?

A: Regulatory documents do not list a direct, specific interaction with alcohol. However, official safety information indicates that this medicine can cause side effects like dizziness, nausea, or liver-related issues. Consuming alcohol may be associated with an increased occurrence or severity of these central nervous system and gastrointestinal effects.

Q: Is Metirel known to cause weight gain or weight loss?

A: Official adverse reaction listings report that weight loss or anorexia (decreased appetite) has been documented as a side effect. This is typically included among the common gastrointestinal or metabolic effects. Concerns about significant or unintentional weight change are typically addressed by a healthcare provider.

Q: Does Metirel affect sleep?

A: Yes, sleep-related issues and psychiatric effects have been reported in official product documents. These include reports of nervousness, irritability, and in very rare cases, nightmares. Changes in sleep patterns or mental state while using the medicine are often discussed with a healthcare provider.

Q: Is it normal to feel tired when starting Metirel?

A: Fatigue, or a lack of energy, is listed among the commonly reported mild side effects in official patient information. This feeling is often associated with other common adverse events such as headache or dizziness when treatment is first initiated.

Q: Can Metirel cause mood changes or depression?

A: Official safety information reports that psychiatric adverse reactions are possible with this medicine. These documented effects include nervousness, irritability, and in serious instances, psychosis, suicidal behavior, and severe mood or mental changes. The reporting of these effects often prompts close observation by a healthcare provider.

Q: Will I need ongoing blood tests while taking Metirel?

A: Official safety monitoring is standard due to documented risks associated with long-term use. Regulatory guidelines specify that patients should receive a baseline and then regular eye examinations to monitor for retinal damage. Monitoring for blood disorders is also typically indicated.

Q: Is Metirel a strong medicine?

A: Metirel is classified as a Disease-Modifying Anti-Rheumatic Drug (DMARD) and is included on the World Health Organization’s List of Essential Medicines. The official label includes specific warnings regarding serious, life-threatening risks, such as irreversible retinal and cardiac damage, which provides context on the seriousness of its therapeutic actions.

Q: Why do doctors prescribe Metirel for [a common secondary/off-label symptom]?

A: The medicine is only officially approved by regulatory bodies for use in specific, labeled conditions, which include systemic lupus erythematosus, rheumatoid arthritis, and malaria. Use outside of these approved conditions is not described in the official regulatory prescribing information.

Q: Can Metirel be stopped suddenly, or does it require a taper?

A: Regulatory information indicates that discontinuation is typically managed under the supervision of a healthcare professional. Abrupt cessation may lead to a relapse or worsening of the underlying condition. The drug’s long half-life means the body may take an extended period to adjust to decreasing levels.

Q: Is it true that Metirel is only for severe cases?

A: The medicine is approved for the treatment of both rheumatoid arthritis and systemic lupus erythematosus. While its mechanism modifies the underlying disease, it is often used for the long-term control of chronic disease, not solely for acute, severe interventions. The decision to use the medicine depends on a clinical assessment of the individual’s specific condition.

Q: What if I forget to take a dose of Metirel?

A: Official patient information provides specific instructions to take the dose if remembered immediately, unless it is nearly time for the next scheduled dose. If that is the case, the missed dose is skipped. The guidance specifies that two doses should not be taken to compensate for a single missed dose.

Q: Do the side effects of Metirel usually go away after a while?

A: According to patient information, common and mild side effects, such as gastrointestinal upset, often lessen or disappear after the first few days or weeks of treatment as the body adjusts. However, it is essential to note that serious side effects, such as ocular toxicity, may be irreversible and can progress even after the medicine is stopped.

Q: Are there any long-term safety concerns with taking Metirel?

A: Official regulatory warnings highlight specific long-term safety risks that necessitate ongoing management. These risks include irreversible retinal damage (maculopathy), which is linked to the cumulative dose taken over time, and potential cardiotoxicity, which requires regular monitoring.

Q: Is Metirel available as a generic drug?

A: Yes, regulatory records confirm that the original drug has generic alternatives available. The FDA has approved generic versions of Metirel (hydroxychloroquine sulfate) that are available in the same strength as the brand-name product.

Q: Does Metirel affect the ability to drive or operate machinery?

A: Official safety documents caution that the medicine may cause dizziness, visual disturbances, or other central nervous system effects. Regulatory documents caution that functional abilities should be confirmed prior to driving or operating machinery.

Q: Is it better to take Metirel in the morning or at night?

A: Official dosage instructions state that the medication should be taken with a meal or a glass of milk to support its absorption and reduce stomach upset. The instructions do not specify a time of day, as long as the intake aligns with the prescribed schedule (once or twice daily) and the administration conditions are met.

Q: What should I do if Metirel stops working?

A: If the medicine appears to stop working or if the condition worsens, official regulatory guidance indicates that non-response or worsening condition often leads to a therapeutic response assessment by a healthcare provider. If no improvement is seen after a defined period, the prescriber may consider discontinuing the treatment.

Q: What is the typical time frame before a healthcare provider reviews the use of Metirel?

A: The official safety guidelines mandate a structured review process. This includes an initial baseline eye examination, and for patients without major risk factors, annual eye exams are typically recommended to start after five years of treatment. This implies a structured and regular long-term review process for the use of the medicine.

How should Metirel be stored and disposed of?

How to Store and Dispose of Metirel?

Metirel (hydroxychloroquine sulfate) must be stored according to specific regulatory requirements to maintain product stability and safety. The official labeled temperature for storage is controlled room temperature, 25 C (77 F), with permitted short-term temperature excursions up to 30 C (86 F). The tablets must be kept in the original, tightly closed, light-resistant container, away from excess heat and moisture, such as the bathroom.

Storage Mandate Requirement
Temperature 25 C (77 F), protected from excess heat.
Environment Cool, dry place; keep container tightly closed.
Child Safety Keep this and all drugs out of the reach and sight of children.

Disposal must adhere to official guidelines. Metirel is not recommended for disposal by flushing down the toilet or sink. The preferred method is using a drug take-back program. If this is unavailable, unused or expired medication should be mixed with an unappealing substance, sealed in a container, and discarded in the household trash.

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

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