Fluorouracil 2% 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, Antimetabolite
Pharmacologic Class
Pyrimidine Antimetabolite
Pregnancy Category
Category D
FDA Approved
Mar 1970
DEA Schedule
Not Controlled
Overview
What is this medicine?
Fluorouracil topical solution is a medicine applied to the skin to treat certain skin growths, like actinic keratosis (pre-cancerous spots) and some types of skin cancer. It works by targeting and destroying abnormal cells. You will likely experience a strong skin reaction (redness, crusting, soreness) where you apply it, which is a sign the medicine is working.
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 directed 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 area to someone else's skin.
Storing and Disposing of Your Medication
Store this medication at room temperature, away from freezing temperatures.
Keep it 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 directed 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 area to someone else's skin.
Storing and Disposing of Your Medication
Store this medication at room temperature, away from freezing temperatures.
Keep it 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
- Avoid prolonged sun exposure and use sunscreen/protective clothing during and immediately after treatment, as treated areas may be more sensitive to sunlight.
- Wash hands thoroughly after application.
- Avoid contact with eyes, nose, mouth, and other mucous membranes.
- Do not apply to open wounds or irritated skin.
- Do not cover treated areas with occlusive dressings unless directed by a doctor.
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 2-4 weeks. For Superficial Basal Cell Carcinoma: Apply to affected area twice daily for 3-6 weeks, up to 12 weeks.
Condition-Specific Dosing:
actinicKeratosis:
Apply twice daily for 2-4 weeks.
superficialBasalCellCarcinoma:
Apply twice daily for 3-6 weeks, 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; use with caution if extensive application on compromised skin.
Dialysis:
No specific adjustment needed 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; use with caution if extensive application on compromised skin.
Pharmacology
Mechanism of Action
Fluorouracil is a pyrimidine analog that acts as an antimetabolite. It is converted intracellularly to active metabolites, including 5-fluorodeoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP). FdUMP inhibits thymidylate synthase, thereby blocking the synthesis of thymidylate, a precursor of DNA. FUTP is incorporated into RNA, leading to the production of functionally defective RNA. These actions disrupt DNA and RNA synthesis, leading to cell death, particularly in rapidly proliferating cells like cancerous cells.
Pharmacokinetics
Absorption:
Bioavailability:
<0.1% (systemic from intact skin)
Tmax:
Not well-defined for topical systemic absorption due to minimal levels
FoodEffect:
Not applicable for topical formulation
Distribution:
Vd:
Not well-characterized for systemic distribution after topical application
ProteinBinding:
Not well-characterized for topical application
CnssPenetration:
Limited
Elimination:
HalfLife:
10-20 minutes (for systemically absorbed drug)
Clearance:
Rapid systemic clearance
ExcretionRoute:
Renal (as inactive metabolites)
Unchanged:
Not available
Pharmacodynamics
OnsetOfAction:
Visible reaction typically within 3-5 days of application
PeakEffect:
Most severe inflammatory reaction usually occurs within 2-3 weeks of treatment
DurationOfAction:
Healing may take 1-2 months after cessation of treatment
Confidence:
Medium
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Help Immediately
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention 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 unusual 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 may last for 2 weeks or longer after stopping the medication. If you experience a skin reaction that 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, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention 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 unusual 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 may last for 2 weeks or longer after stopping the medication. If you experience a skin reaction that 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, blistering, or ulceration beyond what is expected.
- Signs of infection (e.g., pus, fever, spreading redness).
- Unusual bleeding or bruising.
- Any signs of systemic reaction (e.g., severe nausea, vomiting, diarrhea, mouth sores, fever, chills) â though rare with topical use.
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 conditions to ensure safe treatment:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction you experienced, including any symptoms.
If you have a dihydropyrimidine dehydrogenase deficiency, a rare genetic disorder.
If you are pregnant or think you may be pregnant. This medication is not recommended during pregnancy, and you should not take it if you are pregnant.
If you are breastfeeding. You should not breastfeed while taking this medication.
If the patient is a child. This medication is not intended for children, and you should not give it to a child.
Additionally, it is crucial to discuss all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. This includes:
All your current medications, including dosages and frequencies.
* Any health problems you have, including pre-existing conditions and medical history.
Your doctor needs this information to assess potential interactions and ensure it is safe for you to take this medication. Do not start, stop, or change the dose of any medication without first consulting your doctor.
It is essential to inform your doctor about the following conditions to ensure safe treatment:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction you experienced, including any symptoms.
If you have a dihydropyrimidine dehydrogenase deficiency, a rare genetic disorder.
If you are pregnant or think you may be pregnant. This medication is not recommended during pregnancy, and you should not take it if you are pregnant.
If you are breastfeeding. You should not breastfeed while taking this medication.
If the patient is a child. This medication is not intended for children, and you should not give it to a child.
Additionally, it is crucial to discuss all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. This includes:
All your current medications, including dosages and frequencies.
* Any health problems you have, including pre-existing conditions and medical history.
Your doctor needs this information to assess potential interactions and ensure it is safe for you to take this medication. Do not start, stop, or change the dose 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 sunlight, 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 skincare products or medications on your skin.
Patients lacking the enzyme dihydropyrimidine dehydrogenase (DPD) are at a higher risk of experiencing severe and potentially life-threatening side effects. These may include mouth irritation or sores, diarrhea, low white blood cell counts, or nerve problems.
This medication can be toxic and even fatal to pets. To ensure their safety, keep the container and treated skin areas out of reach of pets. Dispose of or thoroughly clean any cloths or applicators used to apply this medication. Avoid getting this medication on your clothes, carpet, or furniture. If a pet ingests the container, comes into contact with the medication, swallows it, licks the treated area, or exhibits symptoms such as vomiting or seizures, contact your veterinarian immediately.
There is a risk of harm to the unborn baby if you take this medication while pregnant. If you become pregnant or suspect you may be pregnant during treatment, notify your doctor right away.
To prevent pregnancy during treatment with this medication, use birth control. Your doctor may also advise you to continue using birth control for a period after your last dose. Discuss your birth control options with your doctor to determine the best approach for your situation.
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 sunlight, 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 skincare products or medications on your skin.
Patients lacking the enzyme dihydropyrimidine dehydrogenase (DPD) are at a higher risk of experiencing severe and potentially life-threatening side effects. These may include mouth irritation or sores, diarrhea, low white blood cell counts, or nerve problems.
This medication can be toxic and even fatal to pets. To ensure their safety, keep the container and treated skin areas out of reach of pets. Dispose of or thoroughly clean any cloths or applicators used to apply this medication. Avoid getting this medication on your clothes, carpet, or furniture. If a pet ingests the container, comes into contact with the medication, swallows it, licks the treated area, or exhibits symptoms such as vomiting or seizures, contact your veterinarian immediately.
There is a risk of harm to the unborn baby if you take this medication while pregnant. If you become pregnant or suspect you may be pregnant during treatment, notify your doctor right away.
To prevent pregnancy during treatment with this medication, use birth control. Your doctor may also advise you to continue using birth control for a period after your last dose. Discuss your birth control options with your doctor to determine the best approach for your situation.
Overdose Information
Overdose Symptoms:
- Exaggerated local reactions (severe erythema, erosion, ulceration, necrosis)
- Potential for systemic effects if applied to large areas or compromised skin (e.g., nausea, vomiting, diarrhea, stomatitis, bone marrow suppression - rare)
What to Do:
Discontinue use. Treat symptoms supportively. For suspected systemic overdose, seek immediate medical attention. Call 1-800-222-1222 (Poison Control).
Drug Interactions
Contraindicated Interactions
- Patients with known dihydropyrimidine dehydrogenase (DPD) deficiency (caution for topical, especially with extensive application)
Monitoring
Baseline Monitoring
Skin assessment of affected area
Rationale: To document initial lesion appearance, size, and extent prior to treatment.
Timing: Prior to initiation of treatment
Routine Monitoring
Local skin reaction (erythema, scaling, crusting, erosion, ulceration)
Frequency: Daily by patient, weekly/bi-weekly by clinician
Target: Expected inflammatory response indicating drug efficacy
Action Threshold: Excessive pain, severe ulceration, signs of infection (pus, fever, spreading redness), or unexpected systemic symptoms.
Symptom Monitoring
- Local irritation
- Pain
- Burning
- Itching
- Tenderness
- Crusting
- Erosion
- Ulceration
- Hyperpigmentation
- Scarring
Special Patient Groups
Pregnancy
Category D. Should not be used during pregnancy due to potential for fetal harm. Advise women of childbearing potential to use effective contraception.
Trimester-Specific Risks:
First Trimester:
Potential for teratogenicity
Second Trimester:
Potential for fetal harm
Third Trimester:
Potential for fetal harm
Lactation
Caution advised. It is not known if fluorouracil is excreted in human milk after topical application. Due to the potential for serious adverse reactions in breastfed infants, 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:
Potential for serious adverse reactions (e.g., bone marrow suppression, gastrointestinal toxicity) if significant systemic absorption occurs.
Pediatric Use
Safety and efficacy not established in pediatric patients. Not recommended for use in children.
Geriatric Use
No specific dose adjustments needed. Elderly patients may have more fragile skin, requiring careful monitoring of local reactions and skin integrity.
Clinical Information
Clinical Pearls
- Patients should be fully informed about the expected inflammatory reaction (erythema, scaling, crusting, erosion, ulceration) which indicates the drug is working. This reaction can be cosmetically unappealing and uncomfortable.
- Treatment duration varies based on the condition and individual response; complete healing may take weeks after stopping treatment.
- Strict adherence to application instructions (frequency, duration, amount) is crucial for efficacy and to minimize adverse effects.
- Sun protection is vital during and after treatment, as treated areas are highly sensitive to UV light.
- Avoid applying near eyes, nostrils, or mouth due to potential for severe irritation and systemic absorption.
Alternative Therapies
- Imiquimod cream (for actinic keratosis, superficial BCC)
- Ingenol mebutate gel (for actinic keratosis)
- Diclofenac gel (for actinic keratosis)
- Photodynamic therapy (PDT) (for actinic keratosis, superficial BCC)
- Cryotherapy (for actinic keratosis, superficial BCC)
- Surgical excision (for superficial BCC)
- Laser ablation (for actinic keratosis)
Cost & Coverage
Average Cost:
Varies widely (e.g., $100 - $500+) per 10ml solution
Generic Available:
Yes
Insurance Coverage:
Tier 2 or Tier 3 (varies by insurance plan)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor for further guidance. To ensure safe and effective treatment, 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 for more information. If you have any questions or concerns about your medication, don't hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.