Fluorouracil 2.5gm/50ml Inj, 1 Vial

Fluorouracil (5-FU) is a pyrimidine analog antimetabolite. It acts by several mechanisms: 1. Inhibition of thymidylate synthase (TS): 5-FU is converted to 5-fluorodeoxyuridine monophosphate (FdUMP), which binds to and inhibits TS, an enzyme critical for DNA synthesis (specifically, the methylation of deoxyuridine monophosphate to deoxythymidine monophosphate). This leads to 'thymineless death' of rapidly dividing cells. 2. Incorporation into RNA: 5-FU is metabolized to 5-fluorouridine triphosphate (FUTP) and incorporated into RNA, interfering with RNA processing and protein synthesis. 3. Incorporation into DNA: 5-FU is metabolized to 5-fluorodeoxyuridine triphosphate (FdUTP) and can be incorporated into DNA, leading to DNA damage and fragmentation.

Urgent 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 immediate medical attention:

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
+ Difficulty breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of nervous system problems, including:
+ Changes in mood or behavior
+ Confusion
+ Fever
+ Numbness or tingling in the hands or feet
+ Stiff neck
+ Sensitivity to bright lights
+ Severe muscle weakness
Signs of infection, such as:
+ Fever
+ Chills
+ Severe sore throat
+ Ear or sinus pain
+ Cough
+ Increased or discolored sputum
+ Painful urination
+ Mouth sores
+ Wounds that won't heal
Signs of bleeding, including:
+ Vomiting or coughing up blood
+ Coffee ground-like vomit
+ Blood in the urine
+ Black, red, or tarry stools
+ Gum bleeding
+ Abnormal vaginal bleeding
+ Unexplained bruises or bruising that worsens
+ Uncontrollable bleeding
Feeling extremely tired or weak
Chest pain or pressure
Shortness of breath, significant weight gain, or swelling in the arms or legs
Abnormal heartbeat
Dizziness or fainting
Changes in vision
Redness or irritation on the palms of the hands or soles of the feet
Balance problems
Excessive sleepiness
Uncontrolled eye movements
Headache

Administration Site Reactions

This medication may cause irritation at the injection site. If the medication leaks from the vein, it can also cause irritation around the affected area. Inform your nurse if you experience any redness, burning, pain, swelling, or fluid leakage at the injection site.

Other Possible Side Effects

Like all medications, this drug can cause side effects. However, many people may not experience any side effects or only minor ones. If you're concerned about any of the following side effects or if they persist, contact your doctor:

Diarrhea
Upset stomach or vomiting
Decreased appetite
Mouth irritation or mouth sores
Hair loss
Dry skin
Changes in nail condition

This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.

Before Taking This Medication: Important Information to Share with Your Doctor

It is crucial 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 allergic reaction you experienced, including any symptoms.
Certain health conditions, such as:
+ Poor nutrition
+ Active infections
+ Bone marrow problems, including low white blood cell count, low platelet count, or low red blood cell count
+ Dihydropyrimidine dehydrogenase (DPD) deficiency
* If you are breast-feeding, as you should not breast-feed while taking this medication.

This list is not exhaustive, and it is essential to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine if it is safe 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 all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Regular blood work and laboratory tests, as directed by your doctor, are crucial to monitor your condition.

This medication can cause low blood cell counts, which may lead to bleeding problems, infections, or anemia. In severe cases, these complications can be life-threatening. If you have any questions or concerns, discuss them with your doctor. You may be more susceptible to infections, so it is vital to practice good hygiene, such as washing your hands frequently, and avoid close contact with people who have infections, colds, or flu.

Bleeding can occur more easily while taking this medication, so it is crucial to be cautious and avoid injuries. To minimize the risk of bleeding, use a soft toothbrush and an electric razor. If you experience stomach upset, vomiting, diarrhea, or loss of appetite, consult your doctor, as they may be able to suggest ways to alleviate these side effects.

If you have diarrhea or vomiting, it is essential to discuss this with your doctor to prevent dehydration and electrolyte imbalances. Certain patients who lack the enzyme dihydropyrimidine dehydrogenase (DPD) are at a higher risk of developing severe and potentially life-threatening side effects, including mouth irritation or sores, diarrhea, low white blood cell counts, or nerve problems.

This medication may also increase the risk of heart problems, such as heart attack, heart failure, or abnormal heartbeat, particularly in individuals with a history of heart disease. Consult your doctor to discuss this risk. Before receiving any vaccinations, inform your doctor, as some vaccines may not be effective or may increase the risk of infection when taken with this medication.

You may be more prone to sunburn while taking this medication, so take necessary precautions when exposed to the sun. If you experience excessive sunburn, inform your doctor. This medication may also affect fertility, leading to difficulties in becoming pregnant or fathering a child. If you plan to conceive, discuss this with your doctor before starting treatment.

Additionally, this medication may harm the unborn baby if taken during pregnancy. If you or your partner may become pregnant, it is essential to use birth control while taking this medication and for a specified period after the last dose. Your doctor will advise you on the duration of birth control use. If you or your partner becomes pregnant, notify your doctor immediately.

• Brivudine (and other antiviral nucleoside analogues like sorivudine) - severe and potentially fatal toxicity due to inhibition of DPD, leading to increased 5-FU exposure.

• Leucovorin (folinic acid): Enhances the cytotoxic effect of fluorouracil by stabilizing the binding of FdUMP to thymidylate synthase, but also increases toxicity (e.g., myelosuppression, mucositis, diarrhea).
• Capecitabine: Prodrug of fluorouracil; concurrent use leads to additive toxicity.
• Live vaccines: Increased risk of infection due to immunosuppression.
• Myelosuppressive agents (e.g., other chemotherapy, radiation therapy): Additive myelosuppression.
• Cimetidine, Metronidazole: May increase 5-FU plasma concentrations and toxicity.
• Warfarin: Increased anticoagulant effect (increased INR/bleeding risk).

• Phenytoin: May increase phenytoin levels and toxicity.
• Allopurinol: May reduce the efficacy of fluorouracil by interfering with its activation (though some studies suggest it may reduce toxicity without compromising efficacy in certain settings).
• Thiazide diuretics: May increase myelosuppression.

• Not available

• Signs of myelosuppression (fever, chills, sore throat, unusual bleeding/bruising, fatigue)
• Gastrointestinal toxicity (severe diarrhea, mucositis/stomatitis, nausea, vomiting, abdominal pain)
• Hand-foot syndrome (palmar-plantar erythrodysesthesia: redness, swelling, pain, blistering on palms/soles)
• Neurological symptoms (ataxia, confusion, lethargy, headache, visual disturbances)
• Cardiac symptoms (chest pain, shortness of breath, arrhythmias)
• Skin reactions (rash, photosensitivity)
• Hair loss (alopecia)

Fluorouracil is contraindicated in pregnancy (Pregnancy Category D). It 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 during treatment and for at least 6 months after the last dose.

Fluorouracil is contraindicated during breastfeeding (Lactation Risk L5). It is unknown if fluorouracil is excreted in human milk, but due to the potential for serious adverse reactions in the breastfed infant, breastfeeding should be discontinued during therapy and for at least 1 month after the last dose.

Fluorouracil is used in pediatric oncology for specific indications, but dosing is highly individualized based on body surface area and specific treatment protocols. Pediatric patients may be more susceptible to certain toxicities. Close monitoring is essential.

Elderly patients (≥65 years) may be at increased risk of severe toxicity (e.g., myelosuppression, gastrointestinal toxicity, neurotoxicity) due to decreased organ function, comorbidities, and polypharmacy. Careful monitoring, dose adjustments, and supportive care are crucial. Consider starting with a lower dose and titrating based on tolerance.

• DPD deficiency is a critical risk factor for severe, potentially fatal toxicity. Consider DPD testing, especially in patients with early or unusually severe toxicity.
• Leucovorin is often co-administered with fluorouracil to enhance its cytotoxic effect, but this also increases toxicity. The dose and schedule of leucovorin are crucial.
• Hand-foot syndrome (palmar-plantar erythrodysesthesia) is a common and often dose-limiting toxicity. Patient education on prevention (e.g., avoiding friction/heat, moisturizing) and early recognition is important.
• Severe diarrhea and mucositis are common and can be life-threatening. Aggressive supportive care, including antidiarrheals and pain management, is essential.
• Cardiac toxicity (e.g., angina, MI, arrhythmias) is rare but can occur, especially in patients with pre-existing cardiac disease. Monitor for cardiac symptoms.
• Neurotoxicity, though less common, can range from mild (e.g., lethargy, confusion) to severe (e.g., ataxia, seizures).
• Fluorouracil is a vesicant/irritant; ensure proper IV access and monitor for extravasation.

• Capecitabine (oral prodrug of 5-FU)
• Other antimetabolites (e.g., Gemcitabine, Pemetrexed, Cytarabine)
• Other classes of chemotherapy agents (e.g., platinum agents, taxanes, topoisomerase inhibitors)
• Targeted therapies (e.g., EGFR inhibitors, VEGF inhibitors)
• Immunotherapy (e.g., PD-1/PD-L1 inhibitors)

If your symptoms or health problems do not improve or worsen over time, it is essential to contact your doctor for further evaluation and guidance.

To ensure safe use, do not share your medication with others, and never take someone else's medication. Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion.

Proper disposal of unused or expired medications is crucial. Do not flush medications down the toilet or pour them down the drain unless specifically instructed to do so by your pharmacist or healthcare provider. If you are unsure about the best method for disposing of medications, consult with your pharmacist, who can provide guidance on safe disposal practices. Additionally, you may want to inquire about potential drug take-back programs in your area.

Some medications may come with an additional patient information leaflet. If you have any questions or concerns about your medication, it is recommended that you consult with your doctor, nurse, pharmacist, or other healthcare provider.

In the event of a suspected overdose, immediately contact your local poison control center or seek emergency medical attention. Be prepared to provide detailed information about the overdose, including the type and amount of medication taken, as well as the time it occurred, to ensure prompt and effective treatment.