Fluorouracil 2.5gm/50ml Inj, 50ml

Fluorouracil is a pyrimidine analog that acts as an antimetabolite. It is converted intracellularly to active metabolites: fluorodeoxyuridine monophosphate (FdUMP), fluorouridine triphosphate (FUTP), and fluorodeoxyuridine triphosphate (FdUTP). FdUMP inhibits thymidylate synthase, thereby blocking the synthesis of thymidylate, a pyrimidine nucleotide essential for DNA synthesis. FUTP and FdUTP are incorporated into RNA and DNA, respectively, leading to dysfunctional nucleic acids and inhibition of cell growth and proliferation.

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 bruising 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. Many people may not experience any side effects or may only have mild 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 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.
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 crucial 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 tests and other laboratory assessments, 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 by washing your hands frequently and avoiding 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 individuals who lack the enzyme dihydropyrimidine dehydrogenase (DPD) may be at a higher risk of 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 an 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 DPD inhibitors): Concomitant use can lead to severe, potentially fatal toxicity due to inhibition of fluorouracil metabolism.

• Leucovorin (folinic acid): Enhances the cytotoxic effects of fluorouracil, but also increases toxicity (e.g., myelosuppression, GI toxicity).
• Allopurinol: May decrease the efficacy of fluorouracil by interfering with its activation.
• Capecitabine: A prodrug of fluorouracil; concomitant use leads to additive toxicity.
• Other myelosuppressive agents: Increased risk of severe myelosuppression.
• Live vaccines: Increased risk of infection due to immunosuppression.

• Warfarin: May increase the anticoagulant effect of warfarin, leading to increased INR and bleeding risk.
• Phenytoin: May increase phenytoin levels, leading to toxicity.
• Metronidazole: May increase fluorouracil toxicity by reducing its clearance.
• Cimetidine: May increase fluorouracil toxicity.

• Not many specific minor interactions are clinically significant or well-documented beyond general additive toxicities.

• Fever (especially >38°C or 100.4°F)
• Chills
• Severe diarrhea (more than 4-6 stools/day above baseline)
• Mouth sores or painful swallowing (stomatitis/mucositis)
• Nausea and vomiting (uncontrolled)
• Unusual bleeding or bruising
• Severe fatigue or weakness
• Redness, swelling, pain, or blistering on palms of hands or soles of feet (Hand-Foot Syndrome)
• Chest pain, shortness of breath, palpitations
• Confusion, dizziness, ataxia, headache (signs of neurotoxicity)

Fluorouracil is classified as Pregnancy Category D. It can cause fetal harm when administered to a pregnant woman. It is embryotoxic, teratogenic, and fetotoxic in animals. Avoid use during pregnancy. If used during pregnancy, the patient should be apprised of the potential hazard to the fetus.

Fluorouracil is contraindicated during breastfeeding. It is unknown whether fluorouracil is excreted in human milk, but 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.

Safety and effectiveness in pediatric patients have not been established for all indications. However, fluorouracil is used in specific pediatric oncology protocols (e.g., for medulloblastoma, some sarcomas). Dosing is highly protocol-specific and requires careful monitoring due to potential for severe toxicity.

Geriatric patients (≥65 years) may be at increased risk of toxicity, particularly myelosuppression, gastrointestinal toxicity (e.g., diarrhea, stomatitis), and hand-foot syndrome. Close monitoring for adverse effects and potential dose reductions are often necessary, especially in those with comorbidities or impaired organ function.

• DPD (Dihydropyrimidine Dehydrogenase) deficiency is a critical pharmacogenomic consideration. Patients with partial or complete DPD deficiency are at significantly increased risk of severe, potentially fatal fluorouracil toxicity. Pre-screening for DPD deficiency is recommended by some guidelines (e.g., NCCN, ESMO) before initiating fluoropyrimidine therapy.
• Leucovorin (folinic acid) is frequently co-administered with fluorouracil to enhance its cytotoxic effects by stabilizing the binding of FdUMP to thymidylate synthase, thereby increasing the duration of thymidylate synthase inhibition.
• The toxicity profile of fluorouracil varies with the administration schedule: continuous infusion regimens are generally associated with less myelosuppression but a higher incidence of mucositis and hand-foot syndrome compared to bolus regimens.
• Cardiotoxicity (e.g., angina, myocardial infarction, arrhythmias, cardiomyopathy) is a rare but serious and potentially fatal adverse effect of fluorouracil, occurring in 1-10% of patients. Patients with pre-existing cardiac disease should be monitored closely.
• Patients should be educated on the importance of reporting any signs of toxicity promptly, especially fever, severe diarrhea, or mouth sores, as these can be life-threatening.

• Other antimetabolites (e.g., Gemcitabine, Pemetrexed, Methotrexate) depending on the specific cancer type and treatment guidelines.
• Other classes of chemotherapy agents (e.g., platinum agents, taxanes, topoisomerase inhibitors) often used in combination with or as alternatives to fluorouracil in various cancer regimens.
• Targeted therapies or immunotherapies, depending on tumor biology and specific indications.

If your symptoms or health problems persist or worsen, it is essential to contact your doctor for further guidance. To ensure safe use, never share your medication with others, and do not take medication prescribed for someone else. Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion. Dispose of unused or expired medications properly. Unless instructed to do so by a healthcare professional, do not flush medications down the toilet or drain. If you are unsure about the correct disposal method, consult your pharmacist, who can also inform you about potential drug take-back programs in your area. Some medications may come with an additional patient information leaflet, which your pharmacist can provide. If you have any questions or concerns about your medication, discuss them 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 medical attention. Be prepared to provide information about the medication taken, the amount, and the time of ingestion.