Fluorouracil 0.5% Cream 30gm
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 Analog
Pregnancy Category
Category X
FDA Approved
Jan 1970
DEA Schedule
Not Controlled
Overview
What is this medicine?
Fluorouracil cream is a medication applied to the skin to treat certain abnormal skin growths, like rough, scaly patches (actinic keratoses) or some types of skin cancer (superficial basal cell carcinoma). It works by stopping the growth of these abnormal cells. When you use it, your skin will likely become red, inflamed, and may even form scabs or sores. This is a normal and expected part of the treatment process, indicating the medicine is working. After treatment, the skin usually heals completely.
How to Use This Medicine
Proper Use of This Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. This medication is for topical use only, meaning it should be applied directly to the affected area of skin. Avoid applying it to your eyes, eyelids, mouth, or nose, as it may cause irritation or ulcers. Be cautious not to let the medication accumulate in the skin folds around these areas. If you accidentally get the medication in these sensitive areas, rinse them thoroughly with water.
Before applying the medication, wash your hands. If the affected area is on your hand, you can wash your hand before applying the medication, but avoid washing it afterwards. Clean the affected area before use and make sure it is completely dry. Wait 10 minutes after washing the affected area before applying the medication. Apply a thin layer to the affected skin and gently rub it in.
Important Application Guidelines
- Do not cover the treated area with bandages or dressings unless your doctor instructs you to do so.
- Avoid applying the medication to cuts, scrapes, eczema, or damaged skin.
- Do not apply the medication to healthy skin.
- After applying the medication, avoid letting the treated skin come into contact with another person's skin.
Storage and Disposal
Store this medication at room temperature, away from freezing temperatures. Keep it in a dry place, avoiding storage in a bathroom. Ensure all medications are kept in a safe location, out of the reach of children and pets.
Missed Dose Instructions
If you miss a dose, apply it as soon as you remember. However, if it is close to the time for your next scheduled dose, skip the missed dose and continue with your regular dosing schedule. Do not apply two doses at once or use extra doses to make up for a missed dose.
To use this medication correctly, follow your doctor's instructions and read all the information provided. This medication is for topical use only, meaning it should be applied directly to the affected area of skin. Avoid applying it to your eyes, eyelids, mouth, or nose, as it may cause irritation or ulcers. Be cautious not to let the medication accumulate in the skin folds around these areas. If you accidentally get the medication in these sensitive areas, rinse them thoroughly with water.
Before applying the medication, wash your hands. If the affected area is on your hand, you can wash your hand before applying the medication, but avoid washing it afterwards. Clean the affected area before use and make sure it is completely dry. Wait 10 minutes after washing the affected area before applying the medication. Apply a thin layer to the affected skin and gently rub it in.
Important Application Guidelines
- Do not cover the treated area with bandages or dressings unless your doctor instructs you to do so.
- Avoid applying the medication to cuts, scrapes, eczema, or damaged skin.
- Do not apply the medication to healthy skin.
- After applying the medication, avoid letting the treated skin come into contact with another person's skin.
Storage and Disposal
Store this medication at room temperature, away from freezing temperatures. Keep it in a dry place, avoiding storage in a bathroom. Ensure all medications are kept in a safe location, out of the reach of children and pets.
Missed Dose Instructions
If you miss a dose, apply it as soon as you remember. However, if it is close to the time for your next scheduled dose, skip the missed dose and continue with your regular dosing schedule. Do not apply two doses at once or use extra doses to make up for a missed dose.
Lifestyle & Tips
- Apply only to the affected areas as directed by your doctor. Avoid contact with eyes, nose, mouth, and other mucous membranes.
- Wash hands thoroughly immediately after applying the cream.
- Do not cover the treated area with occlusive dressings unless specifically instructed by your doctor.
- Avoid prolonged exposure to sunlight or artificial UV light (e.g., tanning beds) during and immediately after treatment, as this can worsen skin reactions.
- Use sunscreen and protective clothing when outdoors.
- Do not use other topical medications on the treated area unless approved by your doctor.
- Expect a significant inflammatory reaction (redness, scaling, crusting, erosion, pain) in the treated area. This is a sign 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:
Apply a thin film to affected area once daily or twice daily, depending on indication and product concentration.
Condition-Specific Dosing:
Actinic Keratosis (0.5% cream):
Apply a thin film to the entire face or other affected area once daily for up to 4 weeks, or until the inflammatory response reaches the erosion stage, then discontinue. Maximum treatment duration is 4 weeks.
Superficial Basal Cell Carcinoma (5% cream):
Apply a thin film to the lesion twice daily for 3 to 6 weeks. Treatment may be continued for up to 10 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 a pyrimidine analog that acts as an antimetabolite. It interferes with DNA and RNA synthesis by inhibiting thymidylate synthase (TS), an enzyme crucial for DNA replication and repair. It is converted intracellularly to active metabolites, including 5-fluorodeoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP). FdUMP inhibits TS, leading to 'thymineless death' of rapidly dividing cells. FUTP is incorporated into RNA, disrupting RNA function. This selective toxicity targets rapidly proliferating cells, such as those found in actinic keratoses and superficial basal cell carcinomas.
Pharmacokinetics
Absorption:
Bioavailability:
Less than 10% (systemic absorption from topical application)
Tmax:
Not applicable for local effect; systemic Tmax is variable and low if absorbed.
FoodEffect:
Not applicable for topical formulation.
Distribution:
Vd:
Not applicable for topical local effect; systemic Vd is not clinically relevant for topical use.
ProteinBinding:
Not available (systemic binding is low)
CnssPenetration:
Limited (not clinically relevant for topical use)
Elimination:
HalfLife:
Not applicable for local effect; systemic half-life is short (10-20 minutes) if absorbed.
Clearance:
Rapid systemic clearance if absorbed.
ExcretionRoute:
Renal (as inactive metabolites) and respiratory (as CO2) if systemically absorbed.
Unchanged:
Less than 10% (systemically)
Pharmacodynamics
OnsetOfAction:
Local inflammatory response typically begins within 3-5 days of treatment.
PeakEffect:
Peak inflammatory response (erythema, erosion, crusting) usually occurs within 2-3 weeks.
DurationOfAction:
Therapeutic effect persists for the duration of treatment; resolution of lesions and healing occurs weeks after treatment cessation.
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Help Right Away
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 immediately:
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 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 immediately:
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 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 or discomfort that is unmanageable with over-the-counter pain relievers.
- Excessive inflammation or redness extending far beyond the treated area.
- Signs of infection: pus, fever, increasing warmth, or spreading redness.
- Allergic reaction: rash, hives, swelling of face/lips/tongue, difficulty breathing.
- Unexpected systemic symptoms (e.g., severe diarrhea, vomiting, mouth sores, fever, chills) - though rare with topical use, seek immediate medical attention if these occur.
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, such as foods or drugs. Describe the allergic reaction you experienced, including the symptoms that occurred.
If you have a condition called dihydropyrimidine dehydrogenase deficiency.
If you are pregnant or think you might be pregnant. Do not take this medication 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 should not be given to them.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health issues with your doctor and pharmacist. They will help determine if it is safe for you to take this medication with your other medications and health conditions. Never start, stop, or change the dose 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, such as foods or drugs. Describe the allergic reaction you experienced, including the symptoms that occurred.
If you have a condition called dihydropyrimidine dehydrogenase deficiency.
If you are pregnant or think you might be pregnant. Do not take this medication 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 should not be given to them.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health issues with your doctor and pharmacist. They will help determine if it is safe for you to take this medication with your other medications and health conditions. Never 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.
Note that only the 5% strength of this medication is approved for treating basal cell carcinoma. If you have been prescribed this medication for basal cell carcinoma and do not have the 5% strength, consult your doctor immediately.
If you have a peanut allergy, discuss this with your doctor before using this medication.
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 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 their reach. Store the medication in a secure location, dispose of or clean any cloths or applicators used to apply the medication, and avoid getting the medication on your clothes, carpet, or furniture. If your pet ingests the medication, comes into contact with the treated area, or shows signs of illness such as vomiting or seizures, 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 are planning to become pregnant while taking this medication, notify your doctor right away.
To prevent pregnancy during treatment with this medication, use effective birth control methods. Your doctor may also advise you to continue using birth control for a period after your last dose, so be sure to discuss this with them.
Note that only the 5% strength of this medication is approved for treating basal cell carcinoma. If you have been prescribed this medication for basal cell carcinoma and do not have the 5% strength, consult your doctor immediately.
If you have a peanut allergy, discuss this with your doctor before using this medication.
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 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 their reach. Store the medication in a secure location, dispose of or clean any cloths or applicators used to apply the medication, and avoid getting the medication on your clothes, carpet, or furniture. If your pet ingests the medication, comes into contact with the treated area, or shows signs of illness such as vomiting or seizures, 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 are planning to become pregnant while taking this medication, notify your doctor right away.
To prevent pregnancy during treatment with this medication, use effective birth control methods. Your doctor may also advise you to continue using birth control for a period after your last dose, so be sure to discuss this with them.
Overdose Information
Overdose Symptoms:
- Exaggerated local skin reactions (severe erythema, erosion, ulceration, pain)
- Systemic toxicity is highly unlikely with topical overdose due to minimal absorption, but theoretical risks include bone marrow suppression, gastrointestinal toxicity (diarrhea, stomatitis), and neurotoxicity if massive amounts are ingested or absorbed.
What to Do:
For topical overdose, discontinue use and manage local skin reactions symptomatically. For accidental ingestion, contact a poison control center immediately (e.g., 1-800-222-1222 in the US) or seek emergency medical attention. Management would be supportive, focusing on potential systemic effects.
Drug Interactions
Monitoring
Baseline Monitoring
Skin assessment of affected area
Rationale: To document baseline appearance of lesions and surrounding skin.
Timing: Prior to initiation of treatment.
Routine Monitoring
Local skin reactions (erythema, erosion, crusting, pain, burning, itching)
Frequency: Daily by patient; weekly by clinician or as needed.
Target: Expected inflammatory response leading to erosion.
Action Threshold: Severe pain, excessive inflammation extending beyond treated area, signs of infection (pus, fever, spreading redness).
Lesion resolution
Frequency: At end of treatment period and follow-up visits.
Target: Complete clearance of lesions.
Action Threshold: Persistent or worsening lesions after appropriate treatment duration.
Symptom Monitoring
- Local skin irritation (redness, dryness, scaling, burning, stinging, itching, tenderness)
- Erosion or ulceration of treated skin
- Crusting or scabbing
- Pain at application site
- Signs of secondary infection (pus, warmth, fever, spreading redness)
Special Patient Groups
Pregnancy
Contraindicated in 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 and to use effective contraception.
Trimester-Specific Risks:
First Trimester:
High risk of major birth defects and fetal death due to potent teratogenic effects.
Second Trimester:
Risk of fetal toxicity and growth restriction.
Third Trimester:
Risk of fetal toxicity and growth restriction.
Lactation
Contraindicated during breastfeeding (L5). It is not known whether fluorouracil is excreted in human milk. 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:
High risk of serious adverse effects due to potential for systemic absorption and toxicity.
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Use is generally not recommended.
Geriatric Use
No specific dose adjustments are required for elderly patients. However, elderly patients may have more fragile skin and should be monitored closely for severe local skin reactions and potential for secondary infection.
Clinical Information
Clinical Pearls
- Patient education is crucial: Explain that the expected inflammatory reaction (redness, crusting, erosion) is a sign the medication is working and is temporary.
- Advise patients to apply the cream thinly and evenly to the entire affected area, not just individual lesions, as actinic keratoses are often subclinical.
- Treatment duration varies; patients should be prepared for a visible skin reaction lasting several weeks, followed by a healing period.
- Avoid applying to open wounds, mucous membranes, or near the eyes.
- Sun protection is vital during and after treatment to prevent worsening of reactions and recurrence of lesions.
- If severe pain or excessive inflammation occurs, temporary discontinuation or reduction in frequency may be necessary, under medical guidance.
Alternative Therapies
- Imiquimod cream (for actinic keratosis, superficial basal cell carcinoma)
- Ingenol mebutate gel (for actinic keratosis)
- Diclofenac sodium gel (for actinic keratosis)
- Cryotherapy (liquid nitrogen)
- Photodynamic therapy (PDT)
- Surgical excision (for basal cell carcinoma)
- Curettage and electrodessication
Cost & Coverage
Average Cost:
$150 - $500+ per 30gm tube (0.5% or 5%)
Generic Available:
Yes
Insurance Coverage:
Tier 2 or Tier 3 (often preferred generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. 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 is a good idea to check with your pharmacist. If you have any questions or concerns about this medication, consult 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 detailed information about the overdose, including the medication taken, the amount, and the time it occurred.