Oxiklorin

Quick links to important sections

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 Oxiklorin

Oxiklorin: What Type of Medicine is It?

This section provides a clear, authoritative definition of Oxiklorin, focusing on its composition, origin, and general classification, which is essential for understanding the drug's fundamental identity.

Property Description
Active ingredient Hydroxychloroquine sulfate
Form Oral tablets
Pharmacological class Antimalarial, Antirheumatic Drug
Common use Systemic autoimmune and parasitic conditions
Origin Synthetic derivative (of Chloroquine)

Oxiklorin: Identity, Classification, and Composition

Oxiklorin is a synthetic, prescription-only medication containing the active substance Hydroxychloroquine sulfate, which is supplied for oral administration in the form of tablets. It is formally classified as both an antimalarial drug and an antirheumatic agent, specifically categorized within the broader group of 4-aminoquinoline derivatives. Its classification as a derivative of Chloroquine reflects a chemically modified structure, which is clinically recognized for differing pharmacokinetic properties, supporting its long-term use in certain conditions.

The medicine is a single-component product where the active ingredient, Hydroxychloroquine sulfate, is supported by pharmacological studies for its intended therapeutic effects. As a prescription medicine, Oxiklorin is subject to regulatory oversight, ensuring its quality and consistency as an oral tablet formulation intended for patients requiring systemic treatment. The use of the sulfate salt form is standard for achieving optimal bioavailability.


The General Purpose and Therapeutic Role

Oxiklorin belongs to the class of Disease-Modifying Anti-Rheumatic Drugs (DMARDs), which are clinically recognized for their role in influencing the underlying disease process rather than just providing symptomatic relief.

The drug's primary general purpose is to act as an immunomodulator, helping to regulate and calm an overactive or misdirected immune response within the body, which is critical in certain autoimmune conditions. This means the drug works by stabilizing the disease process itself, offering a fundamental change in disease course. Simultaneously, it leverages its historical antiparasitic action against specific organisms, maintaining its dual therapeutic role in clinical practice, typically used in situations such as disease flares or as a long-term maintenance agent.

Regulatory References

  1. FDA DailyMed Label

What side effects are possible with Oxiklorin?

Possible Side Effects and Safety Information

The safety profile of Oxiklorin (Hydroxychloroquine sulfate) is structured by regulatory authorities to classify adverse reactions based on frequency and affected physiological systems. The most commonly documented adverse reactions involve the gastrointestinal system, such as nausea, vomiting, diarrhea, and abdominal pain, along with nervous system effects like headache and dizziness.


Documented Serious Safety Concerns

The official labeling emphasizes certain serious adverse reactions that are potentially life-altering or life-threatening. The most critical concerns are focused on the eyes and the heart, requiring specific safety protocols.

  • Ocular Toxicity: There is a documented risk of irreversible Retinal Toxicity (Maculopathy), which can lead to permanent visual field defects. This risk is explicitly tied to the cumulative dosage and duration of therapy, with risk increasing significantly after prolonged use.
  • Cardiotoxicity: The medicine is officially associated with the risk of potentially fatal Cardiomyopathy and disturbances in cardiac rhythm, including QT prolongation and Ventricular Arrhythmias.
  • Other Serious Risks: These also include severe cutaneous adverse reactions (e.g., SJS, DRESS), serious Hypoglycemia, and Neuropsychiatric Events, including psychosis and suicidal behavior, which have been reported in both acute and chronic treatment settings.

Population-Specific Safety Considerations

Official labeling includes specific safety considerations for certain patient populations. Caution is required for individuals with pre-existing conditions such as Psoriasis or Porphyria, as the medicine may exacerbate these disorders. Additionally, individuals with Renal or Hepatic impairment require cautious use due to the potential for drug accumulation and increased toxicity risk. The drug is contraindicated in patients with known hypersensitivity to 4-aminoquinoline derivatives.

Overdose and Emergency Response

Overdose and When to Seek Help

Overdose with Oxiklorin (Hydroxychloroquine) is a medical emergency that can rapidly become life-threatening. The most critical concerns involve severe effects on the cardiovascular and central nervous systems. Toxic effects, including symptoms of overdose, can manifest quickly, often within 1 to 3 hours after a toxic ingestion, and may be fatal.

Immediate medical attention is required if any signs of overdose are observed. If the person collapses, has a seizure, has trouble breathing, or cannot be awakened, immediately call emergency services.


Documented Overdose Manifestations

System Affected Clinical Manifestations (as per authoritative sources)
Cardiovascular Sudden and early cardiac arrest, severe hypotension, ventricular arrhythmias (including Torsades de Pointes), QRS and QT interval prolongation, and depressed myocardial contractility.
Central Nervous System Headache, drowsiness, convulsions (seizures), coma, depressed level of consciousness, and acute psychosis.
Other Symptoms Visual disturbances, hypokalemia (low potassium), and respiratory depression.

Overdose Risk Factors and Severity

Overdose has been described as potentially fatal, with toxicity associated with certain drug concentrations and critical signs like QRS prolongation greater than 120 milliseconds. Ingestion of the drug, even in relatively small quantities in children, has been associated with severe toxicity and death. Immediate, aggressive medical intervention is necessary due to the rapid onset and severity of cardiotoxicity and central nervous system effects. The toxic actions can lead to circulatory collapse and respiratory arrest.

Therapeutic Uses of Oxiklorin

What Oxiklorin Treats: Main Uses and Benefits

Oxiklorin (Hydroxychloroquine sulfate) is generally applied across domains where additional symptomatic support is needed in the context of systemic autoimmune disorders and specific parasitic infections. This medication is commonly used to help manage systemic inflammation and specific parasitic infections.

The relevant indications involve conditions where functional stability becomes affected, such as Systemic Lupus Erythematosus (SLE), Chronic Discoid Lupus Erythematosus (DLE), and Rheumatoid Arthritis (RA). Oxiklorin assists with managing symptoms related to physical discomfort and systemic imbalance, such as chronic joint pain, swelling, morning stiffness, and the skin rashes associated with Lupus flares. This long-term support helps maintain a sense of stability, which contributes to easing the overall symptom load during periods of heightened symptoms.

The medicine is also relevant in clinical settings that involve acute or disruptive symptom patterns, like the acute attacks of certain types of malaria. It is applied when short-term symptomatic assistance is needed to address symptoms related to fever and chills, or when prophylactic support is required in endemic areas.


Quick Fact: Relief for Inflammatory Symptoms Oxiklorin is generally used to provide long-term symptomatic support by easing chronic pain, stiffness, and systemic inflammation in conditions like Rheumatoid Arthritis and Lupus, which helps reduce functional strain.

Regulatory References

  1. NIH DailyMed overview

Eligibility and Restrictions for Use

Who Can and Cannot Use Oxiklorin

The eligibility to use Oxiklorin (Hydroxychloroquine sulfate) is determined strictly by regulatory guidelines that establish formal prohibitions and conditional use requirements.

Category Regulatory Eligibility Status
Contraindicated Populations Use is formally prohibited for patients with a known hypersensitivity to 4-aminoquinoline compounds or pre-existing maculopathy (retinal damage). Children below 6 years of age are contraindicated due to the risk of toxicity and difficulty in administering accurate doses with the available tablet strength. Long-term therapy is also contraindicated for all pediatric patients.
Conditional Use Populations Caution and professional monitoring are required for populations with impaired renal or hepatic function, cardiac disease or risk factors for QT interval prolongation, and Glucose-6-phosphate dehydrogenase (G6PD) deficiency. Patients with Psoriasis or Porphyria should use with caution, as these conditions may be exacerbated. Older adults are at increased risk of retinal toxicity.
Pregnancy and Lactation Use is generally avoided for non-malarial indications unless the treating physician determines the benefit outweighs the potential risk. The drug is transferred to breast milk, and the official label advises careful consideration of risk versus benefit.

This regulatory framework strictly defines the eligible population based on absolute exclusions and a set of conditions that necessitate extreme caution, all of which are documented in official prescribing information.

What should I know about interactions with other medicines?

Oxiklorin (hydroxychloroquine) can interact with a wide range of medicines, potentially altering the drug's effects, the effects of the co-administered drug, or increasing the risk of adverse reactions. It is crucial to inform your healthcare provider about all medicines, over-the-counter products, and supplements you are taking.

Potential Drug-Drug Interactions

Drug Class / Example Potential Interaction Recommendation
QT-prolonging medicines (e.g., amiodarone, azithromycin, certain antidepressants) Increased risk of severe heart rhythm abnormalities (QT prolongation). Combination should be avoided or used with very close cardiac monitoring.
Diabetes medicines (e.g., insulin, metformin, glipizide) Enhanced blood sugar-lowering effect, increasing the risk of hypoglycemia (low blood sugar). Careful blood sugar monitoring and potential dosage adjustment of diabetes medicine are required.
Antacids or Kaolin Can reduce the absorption and effectiveness of Oxiklorin. Take antacids at least 4 hours before or after Oxiklorin.
Antiepileptic medicines (e.g., phenytoin, carbamazepine) May decrease the effectiveness of Oxiklorin. Increased monitoring and possible dosage changes may be needed.
Digoxin Oxiklorin can increase the levels of Digoxin in the blood, leading to potential toxicity. Close monitoring of Digoxin blood levels is necessary.
Methotrexate May increase the risk of side effects from Methotrexate. Regular monitoring for toxicity is essential.
Cyclosporine Oxiklorin may increase Cyclosporine plasma concentrations. Close monitoring and dosage adjustments are recommended.

Using Oxiklorin with other medicines that lower the seizure threshold (e.g., bupropion) or other antimalarial agents like mefloquine can increase the risk of seizures. The combined use of Oxiklorin and other hepatotoxic or nephrotoxic agents should also be approached with caution due to potential organ toxicity.

Mechanism of Action

How Oxiklorin Works

Oxiklorin (Hydroxychloroquine sulfate) acts as a weak base, targeting intracellular processes by altering the pH environment within specific organelles.


Modulation of Intracellular pH and Signaling

The drug primarily acts on acidic intracellular compartments, such as lysosomes and endosomes, raising their pH (alkalinization). This molecular change initiates a specific mechanistic cascade by inhibiting lysosomal acid hydrolases and blocking the activation of endosomal Toll-like Receptors ( TLR7/ TLR9). This suppression of innate immune signaling decreases the production of pro-inflammatory signaling molecules like Interferon-alpha ( IFN-alpha), leading to a systemic dampening of specific immune signaling.


Disruption of Antigen Processing

The altered pH further affects immune cell activity by impairing the process of antigen presentation. Specifically, the altered environment disrupts the loading of processed autoantigens onto Major Histocompatibility Complex ( MHC) Class II molecules. This interference modifies the molecular steps that shape systemic physiological outcomes by reducing T cell activation and MHC Class II loading.


Mechanistic Specificity

The drug's mechanism also includes a specific effect on parasites, where it concentrates in the food vacuole and inhibits heme polymerase, leading to the accumulation of a toxic byproduct. The drug's cellular mechanism is constrained by a slow, mechanism-dependent onset requiring weeks to months of tissue accumulation to achieve full pathway regulation.

Dosage and Administration Information

How Oxiklorin is Used: Official Administration Guidelines

Oxiklorin (200 mg tablets) is approved exclusively for oral administration, and its official use is governed by specific schedules. Following established guidelines for dosing, frequency, and administration context is essential to align with the drug's labeled instructions.


Administration Requirements

The tablets must be swallowed whole and are not to be crushed or divided. To ensure proper intake and absorption, each dose must be taken with a meal or a glass of milk.


Dosing and Frequency Patterns

Official dosing is based on the condition being addressed. The dose is calculated in terms of hydroxychloroquine sulfate, and the maximum daily dose for chronic use (Lupus or Rheumatoid Arthritis) should generally not exceed 400 mg or 6.5 mg/ kg of actual body weight, whichever is lower.

Condition Typical Adult Dosing & Frequency Course/Duration
Chronic Conditions 200 mg to 400 mg daily, taken as a single dose or divided into two doses. Action is cumulative and requires weeks to months for maximum effect.
Malaria Prophylaxis 400 mg once weekly, taken on the same day each week. Must be started 2 weeks before exposure and continued for 4 weeks after leaving the endemic area.
Acute Malaria Treatment Total dose of 2000 mg over 3 days, following a fixed schedule (800 mg initial dose, followed by 400 mg at 6, 24, and 48 hours). A short, fixed-time regimen.

Population Rules

  • Pediatric Dosing: Dosage for children in malaria is based on a calculation of 6.5 mg/ kg of body weight. The calculated dose must not exceed the maximum adult dose.

Recent Clinical Evidence

Research Evidence: Overview of Studies for Oxiklorin

Evidence for use in Systemic Lupus Erythematosus (SLE)

The research for Oxiklorin in Systemic Lupus Erythematosus (SLE) involves randomized controlled trials and large observational cohort studies. Researchers specifically examine measures of disease activity scores, the frequency of flares, and the accumulation of long-term organ damage over time. Observational studies report patterns where survival outcomes were measured and less accumulated organ damage was monitored in groups observed over many years. Research also described that discontinuing the drug was observed to be associated with a different frequency of disease flares compared to continued treatment.

Evidence for use in Rheumatoid Arthritis (RA)

For Rheumatoid Arthritis (RA), the evidence is rooted in double-blind, placebo-controlled randomized trials. Researchers monitored outcomes related to physical discomfort and daily functioning, specifically through measures such as tender and swollen joint counts and functional ability scores. Studies examined how average scores on clinical disease activity measurements compared between patient groups receiving the drug and those receiving placebo over the study duration. Research also indicates that the drug has explored its use in combination with other anti-rheumatic medicines.

Evidence Gaps and Special Populations

The full body of evidence includes studies on pediatric patients for malaria prophylaxis and specific cohorts of pregnant women with SLE, contributing to the available data for these groups. The research base for malaria also includes field studies, and findings indicate patterns related to the measurement of parasite clearance time in patients with susceptible infections. However, the comparative evidence is limited for head-to-head trials against newer classes of drugs across all autoimmune conditions. Data for long-term outcomes like the prevention of joint damage in RA are still emerging, and establishing a direct link between the drug and long-term organ protection in SLE remains challenging due to confounding factors in observational research.

Key Studies & References

  1. Efficacy and Safety of Hydroxychloroquine Therapy for Systemic Lupus Erythematosus Patients Depend on Administration Dose (PubMed)

Frequently Asked Questions (FAQ)

Common questions about Oxiklorin (FAQ)

Q: What happens if I miss taking a dose of Oxiklorin?

Official guidance for the active ingredient describes the instruction to take a missed dose as soon as it is remembered. However, if it is almost time for the next scheduled dose, the instruction is to skip the missed dose. Regulatory documents consistently state that a patient should not take two doses at the same time to make up for a missed dose.


Q: Are there any common foods or drinks that interact with Oxiklorin?

Official documents advise caution regarding certain common foods. The official labeling advises caution or limitation of grapefruit or grapefruit juice consumption, as it may significantly increase the medicine's level in the blood. This effect is noted because elevated drug levels could potentially result in an irregular heart rate.


Q: Does Oxiklorin cause weight gain or weight loss?

Weight loss is listed as a potential side effect in post-marketing reports for the active ingredient. Official prescribing information does not commonly list weight gain as an adverse event.


Q: Does Oxiklorin have a 'Black Box Warning' in official documents?

The drug’s official US Prescribing Information does include prominent warnings for serious risks, such as irreversible retinal toxicity and cardiotoxicity. While these warnings are critical and legally mandated, the specific term 'Black Box Warning' is not always used in the highest-level formatting of the public highlights.


Q: Will Oxiklorin show up on a standard drug test?

Official reports indicate that the active ingredient and related compounds may interfere with or show up on certain common urine chemistry tests. This interference has been noted primarily in situations where high concentrations of the medication are present, such as in situations such as overdose.


Q: Does alcohol consumption present a risk when taking Oxiklorin?

Regulatory guidance states that it is generally permissible to consume alcohol while taking this medication. However, because the drug is processed (metabolized) by the liver, regulatory documents note that caution may be advised in patients with pre-existing liver conditions or a history of alcoholism.


Q: Can I drive or operate machinery while taking Oxiklorin?

Official guidance includes a recommendation that patients evaluate their own ability to safely operate machinery. This is due to the potential for known side effects, such as dizziness or changes in vision, which could impair motor function and judgment.


Q: Are there any known interactions with herbal supplements like St. John's Wort?

Regulatory interaction data indicates that St. John's Wort may interact with the active ingredient. This herbal supplement is described as potentially causing the blood levels of Oxiklorin to decrease, which might reduce its intended effects. Official sources emphasize the importance of disclosing all supplements to a healthcare provider.


Q: Does Oxiklorin affect blood pressure?

The official label describes associations between this drug and serious heart conditions, including heart rhythm abnormalities and cardiotoxicity. However, blood pressure changes (either high or low) are not typically listed as a primary adverse reaction in the official US label.


Q: What type of monitoring (like blood tests) is sometimes needed while on Oxiklorin?

Due to the documented risk of retinal toxicity, official requirements describe the need for regular ophthalmological (eye) examinations, often including a baseline test and follow-up tests. For patients on long-term therapy, official documents also indicate that specialists may require periodic blood tests (full blood counts) and electrocardiograms (ECGs) to check for cardiotoxicity.


Q: Is the medication known to interact with contraceptives?

Regulatory interaction data suggests the medication could potentially increase the blood levels of certain components found in some oral contraceptives. For example, increased levels of the component drospirenone could elevate the risk of high potassium levels.


Q: What kind of specialist typically prescribes Oxiklorin?

Based on the drug's primary approved uses for systemic conditions, official information indicates the drug is often prescribed by medical specialists in areas dealing with systemic inflammation. These specialists typically include rheumatologists and dermatologists.

How should Oxiklorin be stored and disposed of?

Oxiklorin (Hydroxychloroquine Sulfate) must be stored and handled according to specific regulatory requirements to maintain the product's quality and ensure safety.

Storage Requirements

Item Requirement
Storage Temperature Store at 25 C (77 F), which is Controlled Room Temperature. Excursions are permitted between 15 C and 30 C (59 F to 86 F).
Container & Protection Dispense in a tight, light-resistant container and protect from light.
Child Protection KEEP THIS AND ALL DRUGS OUT OF THE REACH OF CHILDREN; accidental ingestion can be fatal.

Disposal Instructions

Item Regulatory Rule
Environmental Rule Do not flush this medication down the toilet to prevent it from entering the water supply.
Recommended Method Dispose of via an approved medicine take-back program.

These instructions define how the drug must be kept to protect its stability and how unused portions must be discarded according to federal guidelines for safety and environmental protection.

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

Available in countries:

Equivalent of Oxiklorin found in:

A-Z Index: