Fluorouracil 5% Solution 10ml
It is used to treat a precancerous skin problem called actinic keratosis.It is used to treat a type of skin cancer called basal cell carcinoma. Only the 5% strength is for use to treat basal cell carcinoma.
Drug Class
Antineoplastic, Keratolytic
Pharmacologic Class
Antimetabolite
Pregnancy Category
Category X
FDA Approved
Mar 1970
DEA Schedule
Not Controlled
Overview
What is this medicine?
Fluorouracil topical solution is a medication applied to the skin to treat certain abnormal skin growths, such as actinic keratosis (pre-cancerous spots) and some types of skin cancer (superficial basal cell carcinoma). It works by causing the abnormal skin cells to become inflamed, blister, and eventually peel off, allowing new, healthy skin to grow in their place. It's important to apply it exactly as directed and to protect treated areas from the sun.
How to Use This Medicine
Using Your Medication Correctly
To use this medication safely and effectively, follow your doctor's instructions and the information provided below.
Apply this medication only to your skin, as directed by your doctor. Do not take it by mouth.
Avoid applying this medication to sensitive areas, including your eyes, eyelids, mouth, or nose, as it may cause irritation or ulcers.
Be careful not to let the medication accumulate in the skin folds around your eyes, nose, or mouth. If you accidentally get the medication in these areas, rinse them thoroughly with water.
Wash your hands before and after applying the medication, unless your hand is the treated area. In that case, do not wash your hand after application.
Before applying the medication, clean the affected area and dry it thoroughly. Wait 10 minutes after washing the area before applying the medication.
Apply a thin layer of the medication to the affected skin and gently rub it in. Unless instructed by your doctor, do not cover the treated area with bandages or dressings.
Avoid applying the medication to cuts, scrapes, eczema, or damaged skin. Only apply it to the affected skin, and not to healthy skin.
After applying the medication, avoid touching the treated skin to anyone else's skin.
Storing and Disposing of Your Medication
Store this medication at room temperature, away from freezing temperatures.
Keep the medication in a dry place, avoiding storage in a bathroom.
Store all medications in a safe location, out of the reach of children and pets.
What to Do If You Miss a Dose
If you miss a dose, apply it as soon as you remember.
If it is close to the time for your next dose, skip the missed dose and resume your regular schedule.
Do not apply two doses at the same time or take extra doses.
To use this medication safely and effectively, follow your doctor's instructions and the information provided below.
Apply this medication only to your skin, as directed by your doctor. Do not take it by mouth.
Avoid applying this medication to sensitive areas, including your eyes, eyelids, mouth, or nose, as it may cause irritation or ulcers.
Be careful not to let the medication accumulate in the skin folds around your eyes, nose, or mouth. If you accidentally get the medication in these areas, rinse them thoroughly with water.
Wash your hands before and after applying the medication, unless your hand is the treated area. In that case, do not wash your hand after application.
Before applying the medication, clean the affected area and dry it thoroughly. Wait 10 minutes after washing the area before applying the medication.
Apply a thin layer of the medication to the affected skin and gently rub it in. Unless instructed by your doctor, do not cover the treated area with bandages or dressings.
Avoid applying the medication to cuts, scrapes, eczema, or damaged skin. Only apply it to the affected skin, and not to healthy skin.
After applying the medication, avoid touching the treated skin to anyone else's skin.
Storing and Disposing of Your Medication
Store this medication at room temperature, away from freezing temperatures.
Keep the medication in a dry place, avoiding storage in a bathroom.
Store all medications in a safe location, out of the reach of children and pets.
What to Do If You Miss a Dose
If you miss a dose, apply it as soon as you remember.
If it is close to the time for your next dose, skip the missed dose and resume your regular schedule.
Do not apply two doses at the same time or take extra doses.
Lifestyle & Tips
- Wash hands thoroughly immediately after applying the solution.
- Avoid contact with eyes, nose, mouth, or other mucous membranes. If contact occurs, rinse thoroughly with water.
- Avoid prolonged exposure to sunlight or other ultraviolet light (e.g., tanning beds) during and immediately after treatment, as this can worsen skin reactions. Use protective clothing and sunscreen on treated areas.
- Do not cover the treated area with bandages or dressings unless specifically instructed by your doctor.
- Be aware that the treated skin will become red, inflamed, blistered, and may peel or crust. This is a normal and expected part of the treatment process, indicating the medication is working.
Available Forms & Alternatives
Available Strengths:
- Fluorouracil 2% Solution 10ml
- Fluorouracil 5% Solution 10ml
- Fluorouracil 50mg/ml Inj, 50ml
- Fluorouracil 5% Cream 40gm
- Fluorouracil 2.5gm/50ml Inj, 1 Vial
- Fluorouracil 500mg/10ml Inj, 10ml
- Fluorouracil 1gm/20ml Inj 20ml
- Fluorouracil 2.5gm/50ml Inj, 50ml
- Fluorouracil 0.5% Cream 30gm
- Fluorouracil 1gm/20ml Inj 20ml
- Fluorouracil 2.5gm/50ml Inj, 50ml
- Fluorouracil 5gm/100ml Inj, 100ml
- Fluorouracil 500mg/10ml Inj 10ml
- Fluorouracil 50mg/ml Inj20ml
Dosing & Administration
Adult Dosing
Standard Dose:
For Actinic Keratosis: Apply to affected area twice daily for 2 to 4 weeks. For Superficial Basal Cell Carcinoma: Apply to affected area twice daily for 3 to 6 weeks, up to 12 weeks.
Condition-Specific Dosing:
Actinic Keratosis:
Apply a sufficient amount to cover the lesions twice daily. Treatment duration is typically 2 to 4 weeks. Complete healing may not be evident for 1 to 2 months after cessation of therapy.
Superficial Basal Cell Carcinoma:
Apply a sufficient amount to cover the lesions twice daily. Treatment duration is typically 3 to 6 weeks, but may extend up to 12 weeks.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment needed due to minimal systemic absorption.
Moderate:
No specific adjustment needed due to minimal systemic absorption.
Severe:
No specific adjustment needed due to minimal systemic absorption.
Dialysis:
No specific considerations due to minimal systemic absorption.
Hepatic Impairment:
Mild:
No specific adjustment needed due to minimal systemic absorption.
Moderate:
No specific adjustment needed due to minimal systemic absorption.
Severe:
No specific adjustment needed due to minimal systemic absorption.
Pharmacology
Mechanism of Action
Fluorouracil is an antimetabolite that interferes with DNA and RNA synthesis. It is converted intracellularly to active metabolites, including 5-fluorodeoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP). FdUMP inhibits thymidylate synthase, blocking the synthesis of thymidylate, a precursor of DNA. FUTP is incorporated into RNA, leading to faulty RNA synthesis. These actions preferentially affect rapidly proliferating cells, such as those found in actinic keratoses and superficial basal cell carcinomas, leading to their destruction.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 6% (systemic absorption from topical application)
Tmax:
Not well-defined for topical application due to minimal systemic absorption.
FoodEffect:
Not applicable for topical administration.
Distribution:
Vd:
Not significant systemically from topical application.
ProteinBinding:
Not significant systemically from topical application.
CnssPenetration:
Limited (due to minimal systemic absorption).
Elimination:
HalfLife:
10-20 minutes (if systemically absorbed)
Clearance:
Rapid (if systemically absorbed)
ExcretionRoute:
Primarily via respiratory excretion as CO2 and renal excretion of inactive metabolites (if systemically absorbed).
Unchanged:
Minimal (if systemically absorbed)
Pharmacodynamics
OnsetOfAction:
Visible inflammatory response typically begins within 3-5 days, progressing over 1-2 weeks.
PeakEffect:
Peak inflammatory reaction usually occurs during the 2nd or 3rd week of treatment.
DurationOfAction:
Therapeutic effects persist for weeks after cessation of therapy, with complete healing taking 1-2 months.
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Attention Immediately
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Stomach pain
Bloody diarrhea
Vomiting
Severe diarrhea
Changes in eyesight, eye pain, or severe eye irritation
Mouth irritation or mouth sores
Fever, chills, or sore throat
Unexplained bruising or bleeding
Feeling very tired or weak
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
Itching
Changes in skin color
Scarring
Skin reactions at the application site, including:
+ Burning
+ Dryness
+ Irritation
+ Redness
+ Pain
+ Swelling
* Note: Skin reactions are common and may last for 2 weeks or longer after stopping the medication. If a skin reaction bothers you, contact your doctor.
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Stomach pain
Bloody diarrhea
Vomiting
Severe diarrhea
Changes in eyesight, eye pain, or severe eye irritation
Mouth irritation or mouth sores
Fever, chills, or sore throat
Unexplained bruising or bleeding
Feeling very tired or weak
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
Itching
Changes in skin color
Scarring
Skin reactions at the application site, including:
+ Burning
+ Dryness
+ Irritation
+ Redness
+ Pain
+ Swelling
* Note: Skin reactions are common and may last for 2 weeks or longer after stopping the medication. If a skin reaction bothers you, contact your doctor.
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe pain or discomfort that is intolerable.
- Excessive inflammation or skin reaction extending beyond the treated area.
- Signs of infection (e.g., pus, fever, spreading redness, warmth).
- Systemic symptoms such as nausea, vomiting, diarrhea, or mouth sores (rare with topical use, but seek medical attention if they occur, especially if you have a known DPD deficiency).
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the symptoms you experienced.
If you have a dihydropyrimidine dehydrogenase deficiency, a rare genetic condition.
If you are pregnant or think you may be pregnant. This medication is not recommended during pregnancy.
If you are breastfeeding. You should not breastfeed while taking this medication.
* If the patient is a child, as this medication is not intended for pediatric use.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health issues. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the symptoms you experienced.
If you have a dihydropyrimidine dehydrogenase deficiency, a rare genetic condition.
If you are pregnant or think you may be pregnant. This medication is not recommended during pregnancy.
If you are breastfeeding. You should not breastfeed while taking this medication.
* If the patient is a child, as this medication is not intended for pediatric use.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health issues. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
When using this drug to treat basal cell carcinoma, it is crucial to use the 5% strength. If you have been prescribed this medication for basal cell carcinoma but do not have the 5% strength, consult your doctor immediately.
If you have a peanut allergy, discuss this with your doctor before starting treatment.
You may not see the full effects of this medication for a few months. Additionally, your skin may appear worse before it starts to improve.
This medication can increase your risk of sunburn. To minimize this risk, avoid exposure to the sun, sunlamps, and tanning beds. However, if your doctor recommends it, you can apply a moisturizer or sunscreen 2 hours after applying this medication. Always check with your doctor before using any other skin products or medications.
Patients lacking the enzyme dihydropyrimidine dehydrogenase (DPD) are at a higher risk of severe and potentially life-threatening side effects, including mouth irritation or sores, diarrhea, low white blood cell counts, and nerve problems.
This medication can be toxic and even fatal to pets. To ensure their safety, keep the container and treated skin area out of reach of pets. Dispose of or thoroughly clean any cloths or applicators used to apply the medication. Avoid getting the medication on your clothes, carpet, or furniture. If a pet ingests the medication, comes into contact with the treated area, or shows signs of illness such as vomiting or seizures after exposure, contact your veterinarian immediately.
There is a risk of harm to the unborn baby if you take this medication during pregnancy. If you become pregnant or suspect you may be pregnant while taking this medication, notify your doctor right away.
To prevent pregnancy during treatment, use birth control as directed by your doctor. You may also need to continue using birth control for a period after your last dose. Consult your doctor to determine the necessary duration of birth control use after stopping this medication.
When using this drug to treat basal cell carcinoma, it is crucial to use the 5% strength. If you have been prescribed this medication for basal cell carcinoma but do not have the 5% strength, consult your doctor immediately.
If you have a peanut allergy, discuss this with your doctor before starting treatment.
You may not see the full effects of this medication for a few months. Additionally, your skin may appear worse before it starts to improve.
This medication can increase your risk of sunburn. To minimize this risk, avoid exposure to the sun, sunlamps, and tanning beds. However, if your doctor recommends it, you can apply a moisturizer or sunscreen 2 hours after applying this medication. Always check with your doctor before using any other skin products or medications.
Patients lacking the enzyme dihydropyrimidine dehydrogenase (DPD) are at a higher risk of severe and potentially life-threatening side effects, including mouth irritation or sores, diarrhea, low white blood cell counts, and nerve problems.
This medication can be toxic and even fatal to pets. To ensure their safety, keep the container and treated skin area out of reach of pets. Dispose of or thoroughly clean any cloths or applicators used to apply the medication. Avoid getting the medication on your clothes, carpet, or furniture. If a pet ingests the medication, comes into contact with the treated area, or shows signs of illness such as vomiting or seizures after exposure, contact your veterinarian immediately.
There is a risk of harm to the unborn baby if you take this medication during pregnancy. If you become pregnant or suspect you may be pregnant while taking this medication, notify your doctor right away.
To prevent pregnancy during treatment, use birth control as directed by your doctor. You may also need to continue using birth control for a period after your last dose. Consult your doctor to determine the necessary duration of birth control use after stopping this medication.
Overdose Information
Overdose Symptoms:
- Exaggerated local inflammatory reactions (severe erythema, blistering, erosion, ulceration).
- Increased pain and discomfort at the application site.
- Systemic toxicity (extremely rare with topical use, but could include nausea, vomiting, diarrhea, stomatitis, bone marrow suppression) if applied over large areas or to compromised skin, or in individuals with DPD deficiency.
What to Do:
Discontinue use immediately. Cleanse the affected area. Symptomatic and supportive care. For suspected systemic toxicity, seek emergency medical attention. Call 1-800-222-1222 (Poison Control).
Drug Interactions
Monitoring
Baseline Monitoring
Skin examination of affected area
Rationale: To assess the extent and nature of the lesions prior to treatment.
Timing: Prior to initiation of therapy.
Patient education on expected inflammatory response
Rationale: To prepare the patient for the anticipated local skin reactions and ensure adherence.
Timing: Prior to initiation of therapy.
Routine Monitoring
Local skin reaction (erythema, blistering, erosion, crusting, necrosis)
Frequency: Daily by patient, periodically by clinician (e.g., weekly or bi-weekly)
Target: Expected inflammatory response indicating drug efficacy.
Action Threshold: Excessive or unexpected severe reactions, signs of infection, or lack of response may require re-evaluation or discontinuation.
Patient comfort and pain level
Frequency: Daily by patient, periodically by clinician
Target: Tolerable discomfort.
Action Threshold: Severe pain or discomfort may require symptomatic treatment or temporary cessation.
Symptom Monitoring
- Local irritation
- Burning sensation
- Pain
- Itching
- Tenderness
- Photosensitivity
- Crusting
- Erosion
- Ulceration
- Hyperpigmentation
- Hypopigmentation
Special Patient Groups
Pregnancy
Contraindicated during pregnancy (Pregnancy Category X). Fluorouracil can cause fetal harm when administered to a pregnant woman. Women of childbearing potential should be advised to avoid becoming pregnant during therapy.
Trimester-Specific Risks:
First Trimester:
High risk of teratogenicity and fetal harm.
Second Trimester:
Risk of fetal harm.
Third Trimester:
Risk of fetal harm.
Lactation
Contraindicated during lactation. It is not known whether fluorouracil is excreted in human milk. Because of the potential for serious adverse reactions in nursing infants from fluorouracil, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Infant Risk:
High risk of serious adverse reactions.
Pediatric Use
Safety and efficacy in pediatric patients have not been established. Use is generally not recommended.
Geriatric Use
No specific dose adjustments are typically required. However, geriatric patients may have more fragile skin and may experience more pronounced local reactions. Use with caution and monitor closely.
Clinical Information
Clinical Pearls
- Patients must be thoroughly educated on the expected inflammatory response (redness, blistering, crusting, erosion) as this is a sign the medication is working and is often mistaken for an allergic reaction or infection.
- Treatment duration is crucial; patients should complete the full course as prescribed, even if lesions appear to clear sooner.
- Complete healing of the treated area may take 1-2 months after the cessation of therapy.
- Strict adherence to sun protection measures (sunscreen, protective clothing, avoiding peak sun hours) is essential during and immediately after treatment to prevent exacerbation of skin reactions.
- Avoid applying the solution to healthy skin surrounding the lesions to minimize irritation.
- The solution should be applied with a non-metallic applicator or gloved finger, and hands should be washed immediately after application.
Alternative Therapies
- Imiquimod cream (for actinic keratosis and superficial basal cell carcinoma)
- Ingenol mebutate gel (for actinic keratosis)
- Diclofenac sodium gel (for actinic keratosis)
- Cryotherapy (liquid nitrogen)
- Photodynamic therapy (PDT)
- Surgical excision
- Laser resurfacing
- Radiation therapy (for basal cell carcinoma)
Cost & Coverage
Average Cost:
Variable (e.g., $100 - $500+) per 10ml solution or 25g cream
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (often covered by most plans, generic preferred)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide information about the medication taken, the amount, and the time it happened.