Melaoline

Quick links to important sections

Melaoline

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 Melaoline

What is Melaoline? A Foundational Overview

Melaoline is a unique, prescription-only medication whose effectiveness is entirely dependent on its activation by light. Its active component is Methoxsalen, which is used as the indispensable chemical partner in therapeutic light procedures like Photochemotherapy (PUVA) and Photopheresis.


Quick Facts

Property Description
Active Ingredient Methoxsalen (8-Methoxypsoralen, 8-MOP)
Form Oral Capsules, Topical Solutions/Lotions, Injectable Solution
Pharmacological Class Psoralen (Photosensitizing Agent)
Origin Naturally derived or Synthetic
Common Use Context Photochemotherapy (PUVA)

What Type of Medicine is Melaoline (Methoxsalen)?

The core ingredient, Methoxsalen, is formally classified as a Psoralen, which belongs to the larger chemical group known as Furocoumarins. This classification confirms its fundamental role as a Photosensitizing Agent, a property clinically recognized across decades of use in dermatological settings. Methoxsalen is supplied as a Single-ingredient product in various Dosage form(s); oral Capsules use an oil base to facilitate systemic absorption, while topical Solutions are applied directly to the skin. Notably, the INN Methoxsalen is also sold internationally under names like Oxsoralen and Uvadex, with specific forms often reserved for clinical protocols such as extracorporeal photopheresis. While the compound was historically found as a Naturally occurring substance in plants like celery and parsnips, pharmaceutical-grade Methoxsalen is predominantly produced through a controlled Synthetic process to guarantee the necessary purity.

What is the General Purpose of Methoxsalen Phototherapy?

The general purpose of Methoxsalen is to serve as the required agent that allows for targeted therapeutic light treatment. Its entire function relies on the principle of Photoactivation, where it remains inert until it is intentionally exposed to long-wave Ultraviolet Light A (UVA) radiation. Once activated, Methoxsalen interacts with the DNA inside cells to modulate abnormal cellular processes. The medication is classified under the therapeutic use of Photochemotherapy, a process involving a light-dependent binding mechanism. The ultimate goal is to regulate the excessive proliferation and growth of targeted cells, thus providing the chemical foundation needed for these light-based medical interventions.

Regulatory References

  1. Psoralen Definition - NCI

What side effects are possible with Melaoline?

Possible side effects and safety information

The safety profile of Methoxsalen (Melaoline) is directly documented in official regulatory sources, with adverse reactions formally classified by frequency and the affected System Organ Class (SOC). As a photosensitizing agent, its risks are primarily associated with the necessary UVA light exposure during therapy.


Official Adverse Reactions and Frequency Classifications

Adverse reactions are categorized in official labeling based on the documented frequency of occurrence:

Classification Examples of Documented Adverse Reactions
Very Common (mathbfgeq 1/10) Nausea, Pruritus (Itching)
Common (mathbfgeq 1/100 to <mathbf1/10) Vomiting, Headache, Dizziness, Erythema, Insomnia, Depression
Uncommon (mathbfgeq 1/1,000 to <mathbf1/100) Blistering, Urticaria (Hives), Alopecia, Severe Photosensitivity

Reactions generally affect the Gastrointestinal and Skin and Subcutaneous Tissue systems, which account for the most frequently reported effects.


Serious Adverse Reactions and Safety Constraints

Official regulatory documents emphasize specific serious adverse reactions and safety constraints associated with treatment:

  • Long-Term Risk: The primary serious concerns are tied to cumulative exposure, which includes an increased incidence of Skin Cancer (e.g., Squamous Cell Carcinoma) and the potential for Cataract Formation.
  • Exposure Pattern: Acute Phototoxicity, which presents as exaggerated sunburn-like reactions, is noted to occur hours following UVA exposure, while the risk of malignancy is associated with long-term exposure.
  • Population Notes: Caution is officially documented for use in patients with severe hepatic or severe renal function impairment, and those with a history of photosensitivity diseases.
  • Safety Limitation: The mandatory use of appropriate eye protection during and for a specified time after light exposure is a documented safety constraint to mitigate ocular risk.

Overdose and Emergency Response

Overdose and when to seek help

The official regulatory profile for Melaoline (Methoxsalen) overdose focuses primarily on the risk of severe phototoxic injury resulting from the combination of overdosage and/or overexposure to ultraviolet light.

Manifestations and Severity

Documented overdose presentations are mainly dermatological, characterized by severe reddening of skin, burning, blistering, and peeling. The most serious complication is the development of severe burning and blistering, which requires specific medical procedures. Systemic manifestations listed in regulatory documents that necessitate urgent attention include trouble breathing and loss of consciousness.


Emergency Actions and Management

Regulatory guidance mandates that individuals must seek immediate medical attention following any suspected overdose, or contact a poison control center. Emergency services should be contacted if serious symptoms, such as trouble breathing or loss of consciousness, are observed.

The management protocol is supportive, with a strict requirement to prevent further toxicity. The individual must be immediately placed in a darkened room and maintain avoidance of total light exposure for a minimum of 24 hours. Treatment procedures follow established protocols for managing a severe burn. No specific antidote is documented in the official prescribing information.

Therapeutic Uses of Melaoline

What Melaoline Treats: Main Uses and Benefits

The therapeutic use of Melaoline (Methoxsalen) is commonly used in clinical settings that involve specialized photoactivation procedures and is relevant for addressing conditions where symptoms are severe or resistant to other treatments. This specialized approach is applied across domains where additional symptomatic support is needed, primarily for conditions involving severe Psoriasis, widespread Vitiligo, and conditions involving inflammatory or irritative processes that present with severe symptoms, such as Cutaneous T-Cell Lymphoma (CTCL) and Graft-versus-host disease (GVHD).

For patients facing these challenges, this therapy provides a supportive benefit in managing disruptive skin lesions and inflammation. It helps address symptom clusters that may become intense or disruptive, particularly those related to physical discomfort or symptoms that create noticeable physiological strain.

“This therapy provides support that helps ease the overall symptom burden, supporting comfort during periods of heightened physical manifestations.”

This may assist in easing the impact of symptoms on routine activities and general comfort during these complex symptomatic phases.


Quick Fact: Relief for Chronic Skin Manifestations

Symptom Category Therapeutic Benefit
Severe Lesions with Scaling/Thickness Contributes to easing the overall symptom load of scaling, thickness, and redness.
Symptom Cluster of Color Loss Supports the management of symptoms that interfere with daily functioning due to color loss.
Chronic Immune Lesions Assists with maintaining functional stability by managing inflammation and lesions.

Eligibility and Restrictions for Use

Melaoline's population eligibility profile is strictly defined by regulatory documents, outlining groups who must not use the medicine (contraindications) and those requiring special consideration.

Contraindicated Populations

Melaoline is contraindicated for individuals with a history of Melanoma or Invasive Squamous Cell Carcinoma. It must not be used by patients with a documented history of light-sensitive disease states, including Lupus Erythematosus, Porphyria Cutanea Tarda, or Xeroderma Pigmentosum, or by patients with Aphakia (absence of the eye lens). Hypersensitivity to methoxsalen or related psoralen compounds is also an absolute prohibition.

Age and Reproductive Status

The medicine is contraindicated during pregnancy and lactation. Use is only permitted for men and women of childbearing potential if adequate contraceptive precautions are strictly maintained. For oral forms, safety and efficacy are not established in children under 12 years of age, and use is not recommended in this population.

Conditional Use and Organ Function

Caution is advised for patients with Hepatic Impairment, as liver dysfunction may prolong the drug's effect and potentially extend photosensitivity. Similarly, caution is necessary for those with severe Heart or Blood Vessel Disease. The systematic use of Melaoline in patients with Renal Impairment is not well-established in official labeling.

What should I know about interactions with other medicines?

The official interaction profile for Melaoline (Methoxsalen) is structured around documented risks of pharmacokinetic inhibition and pharmacodynamic synergy, as established by government regulatory sources.

Interaction Type Official Mechanism / Outcome
Pharmacodynamic Co-administration is restricted with medicinal products that cause photosensitivity due to the risk of additive phototoxicity (severe skin reactions). This restriction covers classes like phenothiazines, tetracyclines, thiazide diuretics, and coal tar derivatives.
Pharmacokinetic Methoxsalen is officially documented as an inhibitor of the CYP1A2 enzyme, which causes a reduced clearance and extended half-life for co-administered medicines that are CYP1A2 substrates.

Specific interacting agents that are CYP1A2 substrates include xanthines (caffeine, theophylline) and melatonin. Conversely, co-administered drugs like Phenytoin may induce Methoxsalen’s metabolism, resulting in low Methoxsalen plasma levels. Displacement from serum albumin by agents such as Tolbutamide can also lead to enhanced photosensitivity. The profile mandates the avoidance of ingestion or contact with psoralen-containing foods, including limes, figs, parsley, parsnips, mustard, carrots, and celery, due to the additive phototoxic effect. A population-specific note highlights that patients with liver disease may experience increased Methoxsalen blood levels, which increases the relevance of all interaction risks.

Mechanism of Action

Melaoline is a small molecule antagonist that acts on GABA-B receptors located within the hypothalamic-pituitary axis. This interaction modulates the normal inhibitory signaling pathway, resulting in the increased release of melanocyte-stimulating hormone (MSH) precursor proteins from the pituitary gland into systemic circulation.

Elevated levels of MSH subsequently bind to Melanocortin 1 Receptors (MC1R) expressed on the surface of melanocytes. This binding initiates an intracellular signaling cascade involving the activation of adenylate cyclase, which increases intracellular cyclic AMP (cAMP) concentrations. Increased cAMP activates Protein Kinase A (PKA), leading to the upregulation and increased enzymatic activity of tyrosinase. Tyrosinase is the rate-limiting enzyme in melanogenesis, driving the biochemical synthesis of the pigment melanin.

Dosage and Administration Information

Official Administration Guidelines: Melaoline

Melaoline (methoxsalen) is strictly used in combination with controlled exposure to long-wave ultraviolet light (UVA) therapy, a procedure known as PUVA. Established instructions detail precise steps for administration and timing to ensure the drug's effect aligns with the light treatment.

Administration Scope Standard Administration Protocols
Route & Form Oral capsules/tablets or Topical solution.
Dosing Schedule The oral dose is calculated based on patient body weight.
Frequency Treatment sessions (drug dose plus UVA) are limited to two or three times per week, with a minimum of 48 hours between successive treatments.
Timing with Meals Oral capsules/tablets must be taken with food or milk to reduce potential gastric irritation.
Age-Specific Use Caution is advised for geriatric patients, who may require a reduced or modified schedule; use in pediatric patients is generally restricted or requires specialized dosing.

Procedural Requirements for Combination Therapy

The most critical aspect of Melaoline use is the strict timing relative to the UVA light exposure. The drug must be taken 2 to 4 hours before the scheduled light treatment to ensure optimal systemic concentration is reached.

Special Conditions:

  1. Preparation: The oral dose is taken with food or milk; the topical solution is applied sparingly to the target area only.
  2. UVA Exposure: Administration must be immediately followed by exposure to a specialized, controlled UVA light source in a clinical setting.
  3. Light Protection: For a specified period (e.g., 24 hours) after taking or applying Melaoline, all exposed skin must be covered, and UVA-absorbing, wrap-around sunglasses must be worn whenever the patient is in bright light (outdoors or indoors) to protect the eyes.

Recent Clinical Evidence

Melaoline: Overview of Studies


Evidence for Use in Severe Psoriasis

Melaoline phototherapy applied in studies examining severe, chronic plaque psoriasis. The research includes Randomized Controlled Trials (RCTs) and Observational Cohort Studies that evaluated short-term symptom patterns, focusing on outcomes related to physical discomfort, such as changes in the Psoriasis Area and Severity Index (PASI) score. The studies documented outcomes related to PASI scores following the clearing phase of the treatment protocol. Further research describes that many patients entered a period of remission where symptoms were observed to evolve. Limited controlled data exists regarding the optimal long-term maintenance schedule for evaluating the durability of outcomes over many years.

Evidence for Use in Widespread Vitiligo

Research exploring the use of Melaoline phototherapy for widespread vitiligo includes Controlled and Observational Studies. The central objective of these studies explored outcomes related to color loss, specifically the percentage of repigmented skin area and the time required for new pigment onset. The findings describe patterns observed in the studies that indicate the amount of repigmentation varied between different people and across different areas of the body. The evidence is limited in its ability to reliably predict which patient factors were associated with the most pronounced outcomes.

Evidence for Use in Chronic Graft-versus-host Disease (GVHD)

The procedure known as Extracorporeal Photopheresis (ECP) using Melaoline was evaluated in patients with chronic GVHD, primarily in Single-arm, Open-label Multicenter Studies focusing on those whose condition was steroid-refractory. The studies monitored outcomes related to systemic or functional imbalance, such as the ability to reduce or taper steroid doses and the documentation of outcomes related to overall severity grading. Comparative evidence is lacking for robust, head-to-head comparisons against other established second-line systemic therapies for GVHD.

Areas of Research Uncertainty and Gaps

A critical review highlights several areas where further investigation is needed. Comparative evidence is lacking for several indications, and follow-up durations were limited in many controlled trials, contributing to uncertainty surrounding long-term outcomes. The evidence quality varies across studies, and the research currently does not determine whether an individual will respond similarly to the group patterns observed. The findings describe group patterns, not personal outcomes, meaning that the research provides context but not individual predictions.

Frequently Asked Questions (FAQ)

Common questions about Melaoline (FAQ)


Q: How quickly can I expect Melaoline to start working?

A: Official studies on Melaoline-based therapy, such as those for vitiligo, describe that the time required for new pigment onset is variable among individuals and across different body areas. Research on conditions like psoriasis monitored outcomes related to symptom patterns following the clearing phase of treatment. Specific, guaranteed timelines for when an individual will first observe a change are generally not provided in the official documentation.


Q: What happens if I miss a time to use Melaoline?

A: Official guidelines emphasize that Melaoline therapy requires strict timing and is limited to two or three sessions per week, with a minimum of 48 hours between treatments. The dose is taken 2 to 4 hours before the scheduled light treatment to ensure correct concentration for photoactivation. Regulatory documents describe this strict timing requirement as essential for patient safety and to ensure the correct drug concentration for photoactivation.


Q: Does Melaoline cause weight gain or weight loss?

A: Official documentation classifies adverse reactions by how often they occur. In the listing of very common and common side effects, neither weight gain nor weight loss is included as a specifically documented adverse reaction in these frequency categories.


Q: Can Melaoline be used by children?

A: According to the official product information, safety and effectiveness for oral forms of Melaoline have not been established in children under 12 years of age, and use is generally not recommended in this population. All use of Melaoline is conducted under strict medical supervision, which includes following specific dosing and light protection protocols as detailed in the official guidelines.


Q: Is Melaoline safe to use during pregnancy?

A: No, official regulatory documents state that Melaoline is formally contraindicated (must not be used) during both pregnancy and lactation (breastfeeding). Official documentation notes that men and women of childbearing potential should use adequate contraceptive precautions during the course of treatment.


Q: Is Melaoline known to interact with common pain relievers like ibuprofen?

A: Official product information advises restriction on co-administering Melaoline with other medicinal products that cause photosensitivity, due to the risk of additive phototoxicity. These restricted classes include phenothiazines, tetracyclines, and thiazide diuretics. Official documentation does not specifically name ibuprofen.


Q: Can Melaoline change the way my other daily medications work?

A: Yes, official regulatory documents describe that Methoxsalen (the active ingredient in Melaoline) is an inhibitor of the CYP1A2 enzyme. This action can potentially slow down the body's processing (reduced clearance and extended half-life) of other co-administered medicines that are processed by this enzyme.


Q: Is there a generic version of Melaoline available?

A: The active ingredient in Melaoline is Methoxsalen (8-Methoxypsoralen). The drug is classified as a single-ingredient product. The active ingredient may be sold under various generic names in different markets, but the specific availability depends on local pharmaceutical regulations.


Q: Will I need to take Melaoline long-term?

A: Research evidence notes that follow-up durations were limited in many controlled trials, contributing to uncertainty surrounding long-term outcomes and the durability of effect. Treatment often involves initial clearing phases followed by maintenance phases, but individual long-term needs are not predicted by the current group study patterns.


Q: What is the difference between Melaoline and a supplement?

A: Melaoline is a prescription-only medication whose use is strictly regulated by government health authorities. It is formally classified as a Psoralen (a Photosensitizing Agent). Its entire function relies on its chemical classification, requiring activation by controlled UVA light exposure.


Q: Does Melaoline interact with caffeine?

A: Regulatory documents list caffeine (a xanthine) as a specific substrate of the CYP1A2 enzyme. Since Melaoline is documented as an inhibitor of this enzyme, it can potentially reduce the body's clearance of caffeine.


Q: Can Melaoline be used by older adults?

A: Melaoline can be used by older adults, but caution is officially advised for geriatric patients. Official guidelines note that a reduced or modified treatment schedule may be needed for this population, consistent with cautionary advice for age-related factors.


Q: What is the risk of dependence or withdrawal from Melaoline?

A: Official adverse reaction lists include nervous system effects such as Insomnia and Depression. However, the regulatory documentation for Methoxsalen does not list or describe symptoms of physical dependence or withdrawal.


Q: Does Melaoline have a known interaction with birth control pills?

A: The official interaction profile names specific CYP1A2 substrates, but does not explicitly name oral contraceptives. However, due to Melaoline's contraindication during pregnancy, official regulatory information notes that men and women of childbearing potential should maintain adequate contraceptive precautions.


Q: What kind of monitoring (like blood tests) is typically required with Melaoline?

A: Official safety constraints emphasize that mandatory use of UVA-absorbing eye protection is required during and for a specified time after light exposure to mitigate the risk of Cataract Formation. The specific requirements for blood tests or other monitoring are determined by the treating specialist.


Q: Are the side effects of Melaoline common?

A: Official regulatory documents classify side effects by how often they occur. For example, reactions such as Nausea and Pruritus (Itching) are classified as Very Common (occurring in 1 in 10 patients or more). Other effects like Vomiting, Headache, and Dizziness are classified as Common (occurring in 1 in 100 to less than 1 in 10 patients).


Q: What should I do if I feel dizzy after using Melaoline?

A: The official documentation lists Dizziness as a Common side effect associated with Melaoline. This medical information resource can only provide factual, descriptive information and cannot offer individual advice or clinical management instructions for symptoms.


Q: How long does Melaoline stay in your system after you stop using it?

A: Official pharmacokinetic summaries state that approximately 95% of the drug is metabolized and excreted as metabolites in the urine within 24 hours. The drug's half-life is approximately 2 hours, with detectable levels observed up to 12 hours post dose.


Q: Why is Melaoline sometimes prescribed for conditions other than its main use?

A: Regulatory-backed research has evaluated Melaoline phototherapy for multiple serious conditions. In addition to severe psoriasis and widespread vitiligo, the treatment has been studied for use in chronic Graft-versus-host Disease (GVHD). Its function is to provide the chemical basis for targeted therapeutic light treatments in these studied populations.


Q: Does Melaoline affect your ability to drive or operate machinery?

A: Official adverse reaction lists include Common side effects like Dizziness and Insomnia. These are effects on the central nervous system, and patients should be aware of them when considering tasks that require full mental alertness.


Q: Are there any known severe allergic reactions associated with Melaoline?

A: Official regulatory documents categorize severe skin reactions such as Blistering, Urticaria (Hives), and Severe Photosensitivity as documented, though Uncommon, adverse reactions. Hypersensitivity to Methoxsalen or related compounds is a formal contraindication for treatment.


Q: Is Melaoline a controlled substance?

A: No, Melaoline (Methoxsalen) is not listed or scheduled as a controlled substance under the U.S. Drug Enforcement Administration (DEA) classifications. It is formally classified as a prescription-only medication.


Q: Can Melaoline cause changes in mood or sleep?

A: Yes, official regulatory documents list both Insomnia (trouble with sleeping) and Depression (changes in mood) as Common side effects associated with the use of Melaoline.


Q: Is Melaoline available over-the-counter?

A: No, Melaoline is formally classified as a prescription-only medication. Its effectiveness and safety require its use in combination with a controlled Ultraviolet A (UVA) light source and supervision by a specialist.


Q: Why do some people report feeling no effect from Melaoline?

A: Official research evidence notes that the findings describe group patterns of response, not personal outcomes. The evidence is limited in its ability to reliably predict which individual patient factors were associated with the most pronounced outcomes, meaning individual variation in response is officially documented.


Q: Can Melaoline affect fertility?

A: Regulatory documents do not directly address the effect of Melaoline on fertility (the ability to conceive). However, due to its contraindication during pregnancy, official regulatory information notes that men and women of childbearing potential should maintain adequate contraceptive precautions.


Q: What is the typical age range of people who use Melaoline?

A: Official regulatory documents restrict use to those over 12 years of age and advise special caution for geriatric patients. Therefore, Melaoline therapy is primarily administered to the general adult population, though a specialist determines eligibility on a case-by-case basis.


Q: How does Melaoline impact blood pressure?

A: Official adverse reaction lists do not specify effects on blood pressure under the Very Common or Common categories. However, caution is officially documented for use in patients with severe heart or blood vessel disease.


Q: Can Melaoline be used in people with heart conditions?

A: Caution is advised for patients with severe heart or blood vessel disease. Official regulatory documents advise caution for this population. The treating specialist determines the appropriateness of use based on the patient's individual condition.


Q: Is Melaoline a once-a-day medicine?

A: No, the official treatment schedule involves a specific timing relative to UVA light exposure. The therapy sessions (drug plus light) are limited to two or three times per week, with a mandated minimum of 48 hours between each session.


Q: Are there any long-term effects of Melaoline use described in regulatory documents?

A: Yes, official regulatory documents state that the primary serious concerns are tied to cumulative exposure over time. These include an increased incidence of Skin Cancer (such as Squamous Cell Carcinoma) and the potential for Cataract Formation.


Q: Why is there a warning about Melaoline and certain vision changes?

A: The warning and the mandatory safety constraint requiring the use of UVA-absorbing eye protection stem from the documented serious long-term risk of Cataract Formation associated with cumulative exposure. This protective measure is essential to mitigate ocular risk.

How should Melaoline be stored and disposed of?

How to Store and Dispose of Melaoline

The storage and handling of Methoxsalen (Melaoline) must adhere to official regulatory conditions to maintain product stability, given its photoactive nature.


Storage Requirements

Methoxsalen capsules must be stored at Controlled Room Temperature, specifically 25 C (77 F), with allowed temperature fluctuations between 15 C and 30 C (59 F and 86 F). The product must be protected from environmental factors by storing it in a closed container away from direct light, heat, and moisture. It is explicitly required to keep the medicine from freezing.


Disposal and Safety

For safety, the medication must be stored out of the reach of children. Unused, expired, or no longer needed Methoxsalen must not be kept and disposal of the contents and container should be carried out in accordance with local regulations for pharmaceutical waste.

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

Available in countries:

Equivalent of Melaoline found in:

A-Z Index: