Mepacrine

Quick links to important sections

Mepacrine

Treatment option:

Medically reviewed

Marina Burgos

Last updated on 10/01/2026

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

Overview of Mepacrine

What is Mepacrine? An Overview

Mepacrine is a medication known for its primary anti-parasitic properties and its ability to influence the immune system.

Property Description
Active ingredient Quinacrine
Form Oral tablet
Pharmacological class Antiprotozoal / Antimalarial
General purpose Combating parasitic infections; modulating immune response
Origin Synthetic Organic Compound

What Type of Medicine is Mepacrine?

Mepacrine, also known by its chemical name Quinacrine, is classified as an antiprotozoal agent, which means its main function is to target and eliminate single-celled organisms, such as certain parasites, that can cause infection in the body. Quinacrine is a synthetic organic compound, identifying it as a chemically manufactured substance rather than one directly derived from a natural source.

This drug is clinically recognized for its efficacy in environments where parasitic infections are endemic. As a pharmaceutical product, Mepacrine is typically supplied as an oral tablet for administration by mouth, acting as a systemically working medicine. It is a single active ingredient product, where Quinacrine is the sole component responsible for the therapeutic effects.


General Purpose of Mepacrine's Action

The main general purpose of Mepacrine is to combat parasitic infections and also to help moderate certain inflammatory processes. Mepacrine has an established use in treating parasitic infections, as the medicine is recognized as effective in fighting these specific internal invaders.

Beyond this anti-parasitic role, Mepacrine is valued for its distinct influence on the immune response. Quinacrine can act as an immunomodulator, meaning the medicine can help to stabilize or calm overactive signals from the body's immune system in chronic conditions. The medicine, therefore, serves a dual function: clearing foreign organisms and helping to regulate the body's defensive reactions.

Regulatory References

  1. NIH LiverTox

What side effects are possible with Mepacrine?

Possible Side Effects and Safety Information

Official regulatory documents classify the adverse effects of Mepacrine (Quinacrine) into frequency categories, spanning effects that are common and generally manageable to those that are rare but serious. The most common and expected reaction is the yellowing or discoloration of the skin, sclera, and nails, which is typically asymptomatic, harmless, and resolves after discontinuation.

Less severe but common reactions involve the Gastrointestinal System, presenting as nausea, abdominal cramping, or diarrhea, as well as minor effects on the Nervous System like headache and dizziness. These common reactions are often noted to improve with continued treatment or dose adjustment.

Serious adverse reactions, though rare, are officially documented and require specific safety awareness. These include aplastic anemia (a severe blood disorder) and hepatotoxicity (liver injury or hepatitis). Due to these risks, regulatory labels necessitate routine monitoring of blood counts and liver function.

System-Organ Class Affected Examples of Documented Effects
Skin and Subcutaneous Tissue Yellow discoloration, rashes, hyperpigmentation
Blood and Lymphatic System Aplastic anemia (rare), hemolytic anemia
Hepatobiliary Disorders Liver function enzyme elevation, hepatitis (rare)

Specific population safety constraints are also outlined. Mepacrine is typically avoided in individuals with G-6-PD deficiency due to the risk of hemolytic anemia and requires caution in those with severe hepatic impairment. Furthermore, use during pregnancy and lactation is generally advised against in official documentation.

Overdose and Emergency Response

Mepacrine Overdose and When to Seek Help

Regulatory documents define Mepacrine (Quinacrine) overdose as a serious event with the potential for severe and life-threatening outcomes, particularly affecting the central nervous system (CNS) and cardiovascular system.

Documented Overdose Manifestations

Official labeling describes overdose presentations that include seizures, convulsions, psychotic episodes, and excitement as primary CNS effects. Cardiovascular signs may include hypotension and cardiac arrhythmias, which can rapidly progress to cardiovascular collapse and respiratory arrest. Other documented effects include vomiting, stomach upsets, and the potential for permanent blindness or deafness.

Required Emergency Actions

Immediate medical attention is required for all suspected overdoses. Regulatory guidance mandates that individuals contact emergency services immediately and seek urgent hospital treatment due to the high risk of delayed, severe complications. Management is officially documented as supportive because no specific antidote is known. Measures described include gastric lavage, administration of activated charcoal, and specialized cardiac monitoring.

Population-Specific Notes

The drug is noted to be less tolerated by children. Official labeling also documents that overdose may exacerbate pre-existing Psoriasis or Porphyria, or precipitate transitory psychosis in susceptible individuals.

Therapeutic Uses of Mepacrine

What Mepacrine Treats: Main Uses and Benefits

Mepacrine (Quinacrine) is considered relevant across therapeutic areas, including the management of certain infections and conditions involving systemic imbalance. Its clinical applications include managing certain infections and addressing chronic inflammatory conditions marked by heightened symptoms.


Symptom Management in Chronic Autoimmune Conditions

Mepacrine is applied in addressing symptoms related to inflammatory or irritative states typical of Systemic Lupus Erythematosus (SLE) and Cutaneous Lupus Erythematosus (CLE). It offers therapeutic support that may assist with the management of recurrent symptoms related to flare-ups and provides benefit in managing symptoms related to inflammatory or irritative states of the skin and discomfort.

Antiparasitic Management of Specific Infections

The medication is commonly used to help with antiparasitic management to treat the intestinal infection Giardiasis, which is caused by a protozoal parasite. It is relevant in clinical settings marked by the pathogen's presence and is used for managing symptoms that create noticeable physiological strain, and is applied in scenarios where additional management of discomfort is required. Symptoms addressed include persistent diarrhea and abdominal distress.

Support for Challenging Symptom Patterns

Mepacrine is considered relevant across therapeutic domains in clinical settings that involve acute or unstable symptom patterns where symptoms of connective tissue diseases are present, or is applied in settings where symptoms are challenging to manage. It is relevant for managing symptoms that interfere with daily comfort and create noticeable interference with daily stability, and provides support that helps ease the overall symptom burden and assists with maintaining functional stability.

Quick Fact: Relief for Inflammatory Symptoms
Mepacrine is commonly used to help with symptoms related to inflammatory or irritative states and provides support that helps ease the overall symptom burden in chronic conditions.

Eligibility and Restrictions for Use

Eligibility Map: Who Can and Cannot Use Mepacrine

Official regulatory documents define strict criteria for Mepacrine (Quinacrine) use based on population, age, and coexisting conditions.

Eligibility Classification Official Regulatory Status
Contraindicated Populations Patients with known hypersensitivity to acridine dyes and derivatives. Also contraindicated for concurrent use with Primaquine due to potentiated toxicity.
Avoidance and Mandatory Caution The medicine must be avoided in individuals with Glucose-6-Phosphate Dehydrogenase (G-6-PD) deficiency due to the risk of hemolytic anemia. Caution is required for patients with Porphyria, Psoriasis, a history of Psychosis, or signs of hepatic injury.
Reproductive Status Use in pregnant women and nursing mothers is officially not recommended or restricted, as the drug crosses the placenta and is excreted into breast milk.
Age-Group Rules Use is established primarily in adults without contraindications. Use in children requires caution due to decreased tolerability. Official data is insufficient regarding the drug's effects on the older adult population.

Regulatory documents define eligibility for Mepacrine by establishing absolute exclusions (contraindications), mandatory avoidance based on genetic and metabolic status, and conditional caution for certain pre-existing comorbidities (hepatic function). This framework strictly governs which patient groups may or may not use the drug.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Mepacrine (quinacrine) has documented interaction patterns that are classified based on official regulatory information, including pharmacokinetic effects and mandatory prohibitions.


Contraindicated Combination

Co-administration with Primaquine is strictly contraindicated and explicitly prohibited in regulatory labeling. This restriction is based on Mepacrine’s documented potential to increase the blood level of Primaquine, which raises the risk of toxicity.


Documented Drug–Drug Interactions

Mepacrine is a substrate of the Cytochrome P450 (CYP) 3A4/5 enzyme system and an inhibitor of CYP2E1.

  • CYP3A4/5 Inhibitors: Co-administration with inhibitors may enhance Mepacrine's toxicities by reducing its elimination and increasing plasma concentrations.
  • CYP3A4/5 Inducers: Co-administration with inducers may reduce Mepacrine's effectiveness (efficacy) by accelerating its metabolism.
  • CYP2E1 Substrates: Specific monitoring is required when Mepacrine is co-administered with substrates of CYP2E1 due to Mepacrine's inhibitory effect on this enzyme.

Drug–Substance Interaction and Specific Caution

The co-administration of Mepacrine with alcohol (ethanol) has been reported to produce a mild flushing reaction. Additionally, caution is officially advised for the use of Mepacrine in patients with severe liver disease, as this condition may increase the clinical significance of its metabolic interactions.

Mechanism of Action

DNA Intercalation and Replication Interference

Mepacrine operates within a mechanistic domain defined by its ability to intercalate directly into the DNA helix of rapidly dividing cells, particularly in susceptible parasitic organisms. This physical insertion disrupts the structural integrity of the DNA and interferes with crucial processes, including DNA replication and RNA transcription. The resulting physiological effect involves the inhibition of cellular growth and disruption of cellular division in the target organism, which shapes the compound's overall cellular-disrupting profile.


️ Phospholipase A2 Inhibition and Inflammatory Pathway Modulation

A separate mechanistic action involves the inhibition of the enzyme Phospholipase A2 (PLA2). This enzyme is required for releasing precursors of pro-inflammatory mediators from cell membranes. By inhibiting PLA2, Mepacrine modulates the inflammatory cascade, leading to a reduction in the overall output of inflammatory substances such as prostaglandins. This mechanism influences immune signaling pathways and contributes to the compound's mechanism-linked physiological profile.


Cellular and Lysosomal Membrane Targeting

Due to its weak-base properties, Mepacrine exhibits lysosomotropism, causing it to accumulate in and destabilize acidic cellular compartments like lysosomes. This intracellular concentration interferes with the normal integrity and function of these organelles, which supports the modulation of cellular processes driven by distinct signaling patterns.

Dosage and Administration Information

How to Use Mepacrine: Official Administration Guidelines

Mepacrine is generally supplied as a 100 mg oral tablet and must be administered by mouth for systemic effect. Compounding pharmacies in some regions may prepare this medicine for oral use.

To aid proper use and facilitate administration, the official instructions dictate that each dose of Mepacrine must be taken after a meal. This ingestion timing defines a key administration condition. The medicine may be taken with a full glass of water, tea, or juice. Furthermore, tablets may be crushed and mixed with food like jam or honey to assist patients who are unable to swallow them whole.

Dosing by Usage Context

Usage Scenario Standard Adult Dose Frequency and Duration
Maintenance Use (Chronic Conditions) 100 mg daily Typically once daily (q.d.). Onset of action may take 3 to 6 weeks.
Acute Treatment (e.g., Giardiasis) 100 mg Three times daily (TID) for a course lasting 5 to 7 days.

For pediatric patients requiring acute treatment, the dosage is calculated based on body weight, typically prescribed as 2 mg/kg three times daily (TID). In some long-term contexts, the 100 mg dose may be taken on alternate days as a modification to the standard daily regimen.

Recent Clinical Evidence

Mepacrine: Recent Clinical Evidence

Mepacrine (also known as quinacrine) is an acridine derivative originally developed as an antimalarial and antiprotozoal agent. While it has largely been replaced in those roles, recent clinical studies have focused on its anti-inflammatory and immunomodulatory properties, primarily in the context of autoimmune diseases.


Autoimmune and Inflammatory Conditions

Research has explored mepacrine's use in various dermatological and systemic conditions, often in patients who have shown poor response to or intolerance of other antimalarial drugs like hydroxychloroquine.

  • Cutaneous Lupus Erythematosus (CLE): Mepacrine is frequently studied for the treatment of discoid lupus erythematosus and subacute cutaneous lupus erythematosus. Studies suggest it may be beneficial alone or as an add-on therapy. A review of cases reported that patients with otherwise refractory CLE showed improvement when treated with mepacrine.
  • Systemic Lupus Erythematosus (SLE): Clinical data from retrospective analyses and small trials have investigated the addition of mepacrine to existing SLE treatment regimens (including hydroxychloroquine). In patients with refractory joint and/or skin manifestations, the combination was associated with a reduction in disease activity scores.

Safety and Tolerability Profile

In studies involving autoimmune diseases, mepacrine is generally used at lower doses compared to its historical antimalarial use. Key observations regarding its safety profile include:

Observation Status in Clinical Studies
Yellow Discoloration Common, typically temporary, harmless yellowing of the skin and urine.
Retinal Toxicity Unlike other antimalarials, mepacrine has shown negligible risk of retinal toxicity.
Gastrointestinal Issues Nausea, vomiting, and abdominal pain are commonly reported side effects.
Neuropsychiatric Effects Rare but documented reports of dizziness, headache, confusion, and, in rare instances, psychosis.

Overall, while mepacrine remains unlicensed for many of its current uses in some regions, it is available through compounding pharmacies, and its usage is supported by case series and non-randomized studies primarily for refractory cutaneous manifestations of lupus.

Frequently Asked Questions (FAQ)

Common questions about Mepacrine (FAQ)


Q: What is the reported onset of action for Mepacrine?

Official regulatory documents indicate that when Mepacrine is used for chronic conditions, the time required for the full therapeutic effect or onset of action to be observed may take approximately 3 to 6 weeks. The timeframe for acute, short-term uses is generally not specified in the same regulatory context.


Q: Are there any long-term effects associated with taking Mepacrine for many years?

The most common expected effect during long-term treatment is a temporary yellow discoloration of the skin and urine, which is typically noted to be asymptomatic. Regulatory information also documents the potential for rare, serious effects like aplastic anemia (a severe blood disorder) and hepatotoxicity (liver injury). These risks are the reason for routine monitoring of blood counts and liver function.


Q: Are there specific foods or drinks to avoid while taking Mepacrine?

Administration instructions state that Mepacrine should be taken after a meal. Furthermore, the co-administration with alcohol (ethanol) has been reported in official documents to potentially cause a mild flushing reaction in some individuals.


Q: What type of medicine is Mepacrine (e.g., steroid, immunosuppressant)?

Mepacrine's primary classifications are antiprotozoal and antimalarial agent. However, due to its action on certain immune signals, it is also noted to have an effect as an immunomodulator, helping to moderate the immune response. It is chemically an acridine derivative and is not classified as a steroid medication.


Q: How long does Mepacrine stay in your system after you stop taking it?

The drug is known to accumulate in body tissues during treatment, leading to a slow process of elimination. The elimination half-life (the time it takes for the concentration to reduce by half) is reported to be in the range of 5 to 14 days, which reflects its tendency to be slowly released from tissues.


Q: What is the official caution regarding Mepacrine use in patients with a history of liver disease?

Regulatory documents advise caution when using Mepacrine in patients with severe liver disease or hepatic impairment. This caution is advised because liver function affects how the body metabolizes the drug, which could potentially increase the risk of liver injury (hepatotoxicity).


Q: What is the official caution regarding Mepacrine use in the older adult population?

Official data regarding the effects and safety of Mepacrine in the older adult (geriatric) population is noted in regulatory documents as insufficient. This lack of data often leads to heightened care when considering use in this age group.


Q: Does Mepacrine cause any mood changes or mental fog?

Official product information notes that Mepacrine can be associated with central nervous system effects. Documented effects range from common ones like dizziness to rare but serious occurrences such as confusion, headache, and in very rare instances, psychosis.


Q: What do regulatory documents state about the use of Mepacrine in children?

Regulatory documents state that use in children requires caution due to a tendency for decreased tolerability compared to adults. Administration guidelines mention that Mepacrine tablets have been mixed with foods like jam or honey to help with consumption.


Q: What is the information regarding Mepacrine’s potential effects on vision?

Studies suggest that Mepacrine carries a negligible risk of retinal toxicity (damage to the retina at the back of the eye) when compared to other antimalarial drugs. Due to its structural relationship to other compounds, general visual disturbances may occasionally be noted.


Q: How does Mepacrine actually stop malaria from developing?

The drug works by physically inserting itself (intercalating) into the DNA helix of the targeted organism. This physical insertion disrupts the structure of the DNA and interferes with vital processes like DNA replication and cellular division, thereby inhibiting the organism's growth.


Q: Why do some doctors still prescribe Mepacrine when newer drugs exist?

Mepacrine is primarily studied for use as an alternative or add-on therapy, particularly for autoimmune skin conditions like Cutaneous Lupus Erythematosus (CLE). It may be considered for patients who have shown a poor response to or intolerance of other similar antimalarial drugs.


Q: Are there different brand names for the drug Mepacrine?

Yes, the active ingredient in Mepacrine is also known by its chemical name, Quinacrine. Historically, the drug has also been marketed under various trade names, including Atabrine or Atebrin.


Q: Can Mepacrine be used alongside psychiatric medications?

Due to the potential for rare but serious neuropsychiatric effects such as confusion and psychosis, the concurrent use with psychiatric medications is noted to require careful consideration and close monitoring.


Q: Why does Mepacrine have a bad taste or aftertaste for some people?

Official sources indicate that Mepacrine has a notable bitter taste. Administration guidelines mention that Mepacrine tablets have been mixed with foods like jam or honey to help with consumption and mask the unpleasant taste.


Q: How does the body break down Mepacrine after ingestion?

The metabolism and elimination of Mepacrine are carried out by the liver’s enzyme systems. Specifically, Mepacrine is a substrate of the Cytochrome P450 (CYP) 3A4/5 enzyme system, which plays a major role in how the body processes the drug.


Q: Are there specific genetic factors that affect how people respond to Mepacrine?

Yes, official safety guidelines state that Mepacrine must be avoided in individuals with a genetic condition called Glucose-6-Phosphate Dehydrogenase (G-6-PD) deficiency. This is due to a heightened risk of developing a severe blood condition known as hemolytic anemia.


Q: What scientific studies support Mepacrine’s anti-inflammatory properties?

The anti-inflammatory effects of Mepacrine are supported by clinical evidence showing its use in autoimmune conditions like Cutaneous Lupus Erythematosus (CLE). Its mechanism of action in this context involves the inhibition of Phospholipase A2 (PLA2), which is an enzyme involved in reducing the production of inflammatory mediators.

How should Mepacrine be stored and disposed of?

Storage Conditions

Mepacrine (quinacrine) must be stored at Controlled Room Temperature, which is generally defined as 15 C to 30 C (59 F to 86 F). The product must be protected from light and protected from moisture due to its light-sensitive and hygroscopic nature. It is a strict handling requirement that the medicine must not be frozen.

For product integrity, the container must be kept tightly closed and stored in its original container.

Child Safety and Disposal

To prevent accidental ingestion, the medicine must be stored strictly out of the sight and reach of children.

Disposal of unused or expired Mepacrine must be performed according to local regulations for pharmaceutical waste. Unless specific official instructions are given to flush, the product must not be poured down a sink or toilet to prevent environmental contamination.

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

Equivalent of Mepacrine found in:

A-Z Index: