Actikerall

Quick links to important sections

Actikerall

Selected form

Method of action: Antimetabolites, Keratolytic

Treatment option: Keratoses, Actinic Keratosis

Medically reviewed

Rosario Oropesa

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 Actikerall

Quick Facts

Property Description
Active Ingredients Fluorouracil (5-FU) and Sodium Salicylate
Form Film-forming Cutaneous Solution
Pharmacological Class Combination Cytostatic Agent and Keratolytic Agent
General Purpose Targeted management of specific hyperkeratotic skin lesions
Origin Synthetic

Actikerall: Identity, Classification, and Composition

Actikerall is a prescription-only medicine defined as a combination drug used for specific dermatological management, classifying it as both a Cytostatic Agent and a Keratolytic Agent.

This pharmaceutical identity is derived from its two distinct synthetic active ingredients: Fluorouracil (5-FU) and Sodium Salicylate. Fluorouracil provides the cytostatic effect by interfering with the proliferation of rapidly dividing cells, consistent with its classification as an antimetabolite. Concurrently, Sodium Salicylate provides the keratolytic effect by promoting the softening and exfoliation of thickened skin tissue. This dual mechanism—combining cell growth control with tissue softening—is a key factor in managing lesions with significant skin thickening.

Formulation and Synergistic Action

The physical form of Actikerall is a film-forming cutaneous solution intended solely for topical application directly onto the skin. This film-forming characteristic is essential, as it concentrates the active ingredients precisely on the target area, facilitating continuous, sustained exposure. The inclusion of the keratolytic agent is designed to enhance the ability of the cytostatic agent to penetrate the skin barrier.

The Fluorouracil and Sodium Salicylate work together synergistically by combining targeted cell growth control with tissue softening to enhance overall effectiveness. This integrated mechanism is intended to address both the proliferation of abnormal cells and the overlying obstruction, supporting the localized removal of the compromised skin area.

What side effects are possible with Actikerall?

Possible Side Effects and Safety Information

The official safety profile for Actikerall is defined by the medicine's topical application and the known actions of its active ingredients, Fluorouracil and Sodium Salicylate. Government regulatory documents classify adverse reactions based on their frequency of occurrence and the physiological system affected.

Local skin reactions at the application site are the most frequently documented adverse effects, and their appearance is considered part of the expected treatment response. These reactions are typically categorized as Very Common or Common in regulatory summaries.

Frequency-Classified Adverse Reactions

Frequency Examples of Officially Listed Reactions
Very Common Erythema (redness), Inflammation, Irritation, Pruritus (itching), Pain, Burning
Common Headache, Skin scaling (Exfoliation), Mild bleeding, Erosion, Scab formation
Uncommon Ulceration, Edema (swelling), Dermatitis, Dry eye, Increased lacrimation

Serious Adverse Reactions and Safety Constraints

The label addresses the potential for systemic toxicity linked to the active ingredients, which represents the most serious consideration. This risk is managed through explicit contraindications and application limits. The medicine is officially contraindicated for use during pregnancy and lactation, in patients with renal insufficiency, and in individuals with a complete deficiency of the Dihydropyrimidine Dehydrogenase (DPD) enzyme. The treated area must be protected from direct sunlight, and the product must not be used on bleeding lesions or near mucous membranes. Local irritation is noted to be more prominent at the initiation of therapy for the majority of patients.

Overdose and Emergency Response

The official documentation for Actikerall overdose addresses the risks associated with the systemic exposure of its two active ingredients, Fluorouracil and Salicylate. Accidental swallowing or ingestion mandates that immediate action be taken, requiring contact with a Poison Control Centre or hospital emergency department, even if the person is currently without symptoms. The regulatory text emphasizes that prompt medical assistance is required due to the potential for severe systemic complications.

If signs of high blood levels develop following topical overuse, individuals must stop the application, wash the area with warm water, and seek immediate medical help right away. Systemic toxicity from the fluorouracil component is documented to include gastrointestinal symptoms such as stomach pain, vomiting, diarrhea, or swelling and soreness of the mouth (mucositis). Signs of systemic salicylate toxicity include ringing in the ears (tinnitus), confusion, lethargy, or hyperventilation.

Overdose complications are officially classified as severe, necessitating hospital admission and close monitoring. The risks documented in regulatory sources include potential life-threatening outcomes such as seizures, severe acid-base abnormalities, or bone marrow depression. Management is primarily symptomatic and supportive, as no specific antidote is listed in the topical solution's prescribing information. Patients with a known Dihydropyrimidine Dehydrogenase (DPD) enzyme deficiency are noted to be at an increased risk for fluorouracil accumulation and associated severe toxicity.

Therapeutic Uses of Actikerall

What Actikerall Treats: Main Uses and Benefits

Actikerall is commonly used for the management of Actinic Keratosis (AK), a condition involving hyperkeratotic skin symptoms caused by chronic sun exposure. The medication is considered relevant for the management of mild to moderate intensity (Grade I/II) lesions in immunocompetent adult patients. The treatment is relevant for easing symptoms related to the thick, rough, and scaly patches typically found on highly exposed areas like the face, the forehead, or the balding scalp. The medication may be part of symptomatic management for conditions where lesions are present and carry a risk of malignant transformation.

This approach assists with managing the clinical presentation and the symptomatic cluster related to both abnormal cell growth and the physical symptom of thickened tissue, which often create noticeable physiological strain. This supports general well-being during symptomatic phases by contributing to easing the overall symptom load.


“It is an important therapeutic option for localized skin growths resulting from chronic sun damage.”

Quick Fact: Symptomatic Relief for Actinic Keratosis
Primary Indication Actinic Keratosis (Solar Keratosis)
Lesion Severity Mild to moderate intensity (Grade I/II)
Symptoms Managed Thick, rough, scaly, or crusty patches
Patient Benefit Supports lesion resolution and helps ease symptom burden

Eligibility and Restrictions for Use

Who Can and Cannot Use Actikerall?

Actikerall's population eligibility is strictly defined by government regulatory documents, focusing on immunocompetent adults with specific lesions. Use is permitted only for immunocompetent adult patients for hyperkeratotic actinic keratosis of the face, forehead, and balding scalp.


Official Eligibility Exclusions

The medicine is contraindicated and must not be used in the following populations and conditions:

  • Pregnancy and Lactation: Use is absolutely contraindicated during pregnancy and the lactation period.
  • Enzyme Deficiency: Patients with known Dihydropyrimidine Dehydrogenase (DPD) deficiency.
  • Organ Function: Patients with renal insufficiency (kidney problems).
  • Hypersensitivity: Individuals with a known allergy to fluorouracil, salicylic acid, other salicylates, or any formulation ingredient.
  • Concurrent Medication: Patients taking brivudine, sorivudine, or their analogues.

Age and Condition Limitations

The safety and efficacy of Actikerall have not been established in children and adolescents under 18 years of age, and its use is not recommended in this group. Patients with sensory disturbances (e.g., associated with diabetes) require close medical monitoring of the treatment area. The medicine is not to be used on bleeding lesions or for treating skin conditions other than the approved actinic keratosis.

What should I know about interactions with other medicines?

The documented interaction profile for Actikerall (Fluorouracil and Salicylic Acid) is defined by specific restrictions stemming from both its cytostatic and keratolytic components, as established in government regulatory documents.

The most critical restriction is the absolute contraindication with certain antiviral medicines. Co-administration of Brivudine, Sorivudine, or their analogues is prohibited because these substances interfere with the metabolic breakdown of Fluorouracil. This pharmacokinetic interaction involves inhibition of the Dihydropyrimidine Dehydrogenase (DPD) enzyme, leading to a drastic increase in Fluorouracil exposure and associated toxicity. A mandatory interval of at least four weeks must be observed between the use of these nucleoside analogues and Actikerall.

This metabolic constraint also leads to a population-specific contraindication: the medicine is prohibited for use in individuals with a known inherited DPD enzyme deficiency.

Interactions with other medicinal products are also documented regarding exposure modification. Co-administration may lead to elevated blood levels of Phenytoin, an anticonvulsant. The absorbed Salicylic Acid component may also interact with Methotrexate and antidiabetic agents such as Sulfonylureas. Lastly, a pharmacodynamic interaction exists with other dermatological treatments: the co-administration of skin products that cause irritation or drying may result in undesirable additive local effects on the skin.

Mechanism of Action

Cytostatic Mechanism: Targeted Inhibition of Cellular Replication

This domain covers the action of Fluorouracil (5-FU), an antimetabolite that targets the cell's synthetic machinery. 5-FU is converted within the cell to an active form that irreversibly inhibits the enzyme Thymidylate Synthase, which is essential for synthesizing the DNA building blocks necessary for cell division. This mechanism halts DNA synthesis and triggers apoptosis (programmed cell death) in actively proliferating cells, resulting in localized cytostatic effect.


Keratolytic Mechanism: Disruption of the Skin Barrier

This domain focuses on the action of Salicylic Acid (SA), a keratolytic agent that acts chemically on the skin's surface. SA breaks down the intercellular cement substance and weakens the structural bonds (desmosomes) holding together the cells of the thickened outer layer of skin (stratum corneum). This disruption results in epidermal exfoliation, representing the physiological loosening of the corneocyte structure.


Mechanistic Synergy: Enhanced Bioavailability

The combination of the two ingredients yields a critical synergistic effect. The keratolytic action of Salicylic Acid removes the physical barrier of the thickened skin, facilitating the local transdermal access and concentration of the cytostatic 5-FU to the actively dividing cells situated beneath the surface. This ensures the necessary local drug concentration is achieved to facilitate the function of the growth inhibition mechanism.

Dosage and Administration Information

Administration Scope

Category Instruction
Route of administration The solution is strictly for topical application onto the skin and must not be used on the eyes or mucous membranes.
Dosing schedule Actikerall is applied once daily to the targeted lesion and a surrounding rim of healthy skin, limited to a maximum of 0.5 cm beyond the lesion edge. The total area treated must not exceed 25 cm² (5 cm x 5 cm) simultaneously.
Preparation requirements (if applicable) The medication must be applied to clean, dry skin. Before each new application, the previously formed film must be removed, typically by gently peeling it off.
Age-group administration rules Older adults (65 years) do not require specific dose adjustment. Use in pediatric patients (lt 18 years) is not established.

Instruction Classifications (High-Level)

Category Classification
Administration method type Topical (liquid film-forming solution)
Frequency pattern Daily application (with provision for reduction)
Basis of application Pharmacological and clinical standards
Use-context constraints Maximum 12-week duration; Limited total treatment area; Daily film removal.

Resulting Procedural Structure

Step sequence:

  • Prepare the site: Ensure the application area is clean, dry, and free of the previous film layer.
  • Apply the dose: Use the applicator once daily, covering the lesion and the prescribed surrounding rim of skin.
  • Observe the course: Continue application until the lesion is cleared, or for a period not exceeding 12 weeks.
  • Adjust frequency: The frequency may be reduced to three times per week if severe local skin reactions occur.

Connection to the overall use protocol (2–4 sentences): This protocol defines a controlled usage pattern by mandating the topical route and setting specific limits on the treatment area and the simultaneous number of lesions. The once daily frequency and required daily removal of the film ensure continuous, targeted exposure over the defined treatment duration.

Recent Clinical Evidence

Actikerall: Recent Clinical Evidence


Evidence for Use in Actinic Keratosis

The core evidence regarding this combination solution was studied for Actinic Keratosis (AK), a skin condition characterized by abnormal growths due to sun exposure. The primary research conducted was evaluated in a series of double-blind, Randomized Controlled Trials (RCTs). These studies primarily included immunocompetent adult patients whose AK lesions were located on sun-exposed areas like the face, forehead, or balding scalp.

The main outcomes that researchers examined included assessments of histological clearance (the confirmed removal of the abnormal tissue) and clinical response (visual and physical assessments of clearance). The studies also monitored the total number of lesions present on the skin surface. Studies was evaluated in comparison to a placebo (vehicle) as well as to other existing topical agents.

Studies reported measurements showing that the combination solution group and the placebo group achieved different proportions of clearance. Research highlights changes measured during the study period related to lesion counts. These findings contribute to understanding patterns observed in the specific populations and under the defined conditions that the research explored.


Long-Term Studies and Follow-up Durations

Research explored short-term symptom changes and followed patients for a defined time interval to understand the duration of the observed responses. While the maximum treatment duration was studied for up to 12 weeks, the primary assessments for clearance were conducted eight weeks after the treatment ended.

Studies monitored outcomes related to lesion recurrence for up to 12 months following the end of the treatment period. This evidence contributes to understanding symptom patterns over an intermediate duration. However, the available research does not provide information for long-term outcomes, meaning that the full trajectory of the condition or any long-term effects are not fully established beyond the one-year follow-up period.


Evidence in Specific Patient Groups

The principal clinical trials were evaluated in a specific and narrow patient population. The research was studied for immunocompetent adults presenting with AK lesions of mild to moderate intensity.

Due to the design of the key regulatory trials, the results apply only to the populations studied. Data for certain groups remain insufficient, and there is limited information, for instance, for patients who are immunocompromised or for populations where comorbidities may have been present. Subgroup findings regarding different levels of disease severity are uncertain beyond the Grade I/II lesions that research examined.


Research Gaps and Areas of Uncertainty

Evidence highlights what is known — and what is still uncertain — regarding this solution. One key limitation identified by researchers is that the comparative evidence is lacking for direct, high-quality comparisons against alternative procedures, such as cryosurgery.

Furthermore, data are still emerging regarding the effectiveness of retreatment. The existing studies provide limited insight into how the solution was evaluated in patients who experience recurrence or those who require additional courses of treatment. As the follow-up durations were limited to approximately 12 months, the research does not determine whether an individual will respond similarly over many years, particularly regarding the long-term risk of potential disease progression.

Key Studies & References

  1. Clinical Trial Discussion and Evidence Gaps for Topical Fluorouracil-Salicylic Acid Solution
  2. Fluorouracil and Salicylic Acid (Actikerall): Scottish Medicines Consortium Public Assessment Summary (Regulatory Document)

Frequently Asked Questions (FAQ)

Common questions about Actikerall (FAQ)


Q: How is Actikerall different from a topical treatment that only contains 5-Fluorouracil (5-FU)?

Official product information indicates that Actikerall is a combination treatment. It contains a lower concentration of fluorouracil (5-FU) than topical 5-FU monotherapies often use. The inclusion of salicylic acid is designed to soften the thickened skin, which helps improve the penetration of the 5-FU into the targeted lesion.


Q: Is Actinic Keratosis considered a form of skin cancer?

According to regulatory documents, Actinic Keratosis (AK) is not cancer, but it is classified as a precancerous lesion. There is a risk that these abnormal skin growths may progress into a type of skin cancer known as squamous cell carcinoma if they are not treated.


Q: What is the expected timeframe for the skin to fully heal after the treatment course is finished?

Studies and official product information indicate that the final assessment of the treated area is typically made some time after treatment stops. While improvement may be seen earlier, the skin may take up to eight weeks after the treatment course is completed to fully heal.


Q: Is the redness and inflammation at the application site a sign that Actikerall is working?

The appearance of local skin reactions, such as mild to moderate redness and inflammation, is a common and expected occurrence. Official product information notes that these reactions happen in the majority of patients and are considered part of the expected treatment response.


Q: How can I tell the difference between a normal expected side effect and a serious adverse reaction?

Official product information separates local skin reactions (like irritation and redness) from serious systemic reactions. For very serious effects—such as persistent nausea, vomiting, mouth sores, fever, or chills—regulatory guidance advises discontinuing use and seeking immediate medical attention.


Q: What are the reported signs of a systemic reaction related to the fluorouracil component?

Serious systemic reactions, which are related to the fluorouracil component, are listed in regulatory documents. These signs can include persistent nausea, vomiting, diarrhea, mouth sores, or systemic issues such as fever, chills, and unusual bleeding or bruising.


Q: Can Actikerall cause permanent changes to skin color or texture?

Official product information lists skin discoloration and scarring at the application site as possible side effects. This means that while rare, there is a potential for changes to the color or texture of the treated skin.


Q: Is it normal for the treated area to bleed slightly during the process of crust removal?

According to regulatory documents, mild bleeding is listed as a common reaction at the application site. Since the medication requires the daily removal of the film layer, this mild bleeding may be observed during that process.


Q: Why must patients avoid sun exposure while using Actikerall?

Official warnings state that the medicine should not be used with simultaneous exposure to sun. Regulatory warnings advise that sun exposure is to be avoided because the treated area of skin will be more sensitive to sunlight, increasing the risk of an exaggerated sunburn reaction.


Q: How long after discontinuing treatment must a person continue to limit sun exposure?

Official information notes that the treated area is more sensitive to sun exposure, though it does not specify a precise duration for post-treatment sun protection. Regulatory information suggests that the patient continue to protect the treated area from excessive sunlight and use sun protection (SPF 15 or higher) following the treatment course.


Q: Does Actikerall interact with common over-the-counter pain relievers or anti-inflammatories?

Regulatory documents note that the medicine may interact with other drugs containing salicylates (like aspirin), or certain medications used to treat diabetes. Official information advises that interactions with other medications, including common over-the-counter products, be reviewed by a healthcare professional.


Q: Is it necessary to use a specific type of moisturizer or skin product on the treated area?

Official information does not specify a necessary type of moisturizer. However, it warns that the co-administration of other skin products in the treatment area may result in undesirable additive local effects on the skin, such as increased irritation.


Q: Why is Actikerall classified as flammable and what are the specific storage precautions?

The solution is officially classified as flammable due to the composition of its ingredients. Regulatory instructions state that, due to flammability, the medicine is to be kept away from fire or flames at all times, including during application.


Q: Why does the solution sometimes cause permanent stains on clothing or acrylic surfaces?

Official warnings state that the solution may cause permanent stains on clothing, fabric, and certain surfaces, such as acrylics. Warnings note that contact with these materials is to be avoided during application.


Q: Are there any known risks of using Actikerall if a person has existing nerve damage, like diabetic neuropathy?

According to official product information, patients who have a reduced ability to sense touch, pain, or temperature (such as those with diabetic neuropathy) require close medical monitoring during the use of this medicine.


Q: What happens if a person forgets to apply a dose of Actikerall?

Official information describes the procedure for a forgotten application. Regulatory documents indicate that the missed application is typically skipped, and the regular daily schedule is continued, with instructions that a double application should not be used to compensate.


Q: Can the intensity of the treatment be monitored by a doctor, and if so, how?

Treatment intensity is monitored based on the patient's local skin reaction. The frequency of application may be adjusted by a healthcare professional—for example, by reducing the application to three times a week—if severe local skin reactions occur.


Q: Can Actikerall affect the ability to drive or operate machinery?

According to regulatory information, the medicine is applied topically to the skin. There are no reported side effects in the official documents that would be expected to impair a patient's ability to drive or operate machinery.


Q: Are there different formulations or strengths of Actikerall available?

Official regulatory filings confirm that the medicine is formulated as a single strength cutaneous solution. This solution contains 0.5% fluorouracil and 10% salicylic acid.


Q: Why is it advised not to apply the solution to hairy areas of the skin?

Official instructions note that application to hairy areas of the skin may cause the hair to become stuck together. This sticking can make it difficult to perform the required daily removal of the dried film before the next application.

How should Actikerall be stored and disposed of?

Storage and Disposal Requirements for Actikerall

Actikerall cutaneous solution requires specific conditions to maintain product stability and ensure safety, as mandated by regulatory labeling.


Storage and Stability

  • Temperature and Environment: The medicine must be stored at a temperature not exceeding 25 C; it must not be refrigerated or frozen. The solution is flammable and must be kept away from fire or flames.
  • Container and Integrity: The bottle must be kept tightly closed. If the solution dries up or crystals occur, the product must be discarded and no longer used.
  • Shelf-Life: The stability period after the bottle is first opened is 3 months.
  • Child Safety: Keep this medicine out of the sight and reach of children.

Disposal Instructions

Unused product or waste material must be disposed of in accordance with local requirements. The medicine must not be thrown away via wastewater or common household waste.

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

Available in countries:

Equivalent of Actikerall found in:

A-Z Index: