5-Fluril IV Injection or Infusion

Introduction

5-Fluorouracil (5-FU) is a chemotherapy medication primarily used to treat various types of cancer, including colorectal, breast, stomach, and pancreatic cancers. It belongs to the class of antimetabolites and works by interfering with the synthesis of DNA and RNA in rapidly dividing cancer cells.

Uses

5-FU is widely used to treat solid tumors, especially colorectal cancer. It is also effective against breast, stomach, esophageal, and pancreatic cancers. In dermatology, topical 5-FU is used to treat actinic keratosis and superficial basal cell carcinoma.

Mechanism of Action

5-FU is a pyrimidine analog that inhibits thymidylate synthase, an enzyme required for DNA synthesis. It is converted into active metabolites that disrupt both RNA and DNA synthesis, leading to the inhibition of cell division and eventual cell death, particularly in rapidly dividing cancer cells.

How Long Does It Take to Work?

The effects of 5-FU vary depending on the type of cancer being treated, the method of administration, and individual patient factors. It may take several weeks to observe a clinical response. However, biochemical changes in cancer cells can begin shortly after treatment initiation.

Absorption

5-FU has poor oral bioavailability due to extensive first-pass metabolism, which is why it is primarily administered intravenously or topically. When given intravenously, it is rapidly absorbed into the bloodstream.

Route of Elimination

5-FU is primarily metabolized in the liver by the enzyme dihydropyrimidine dehydrogenase (DPD). It is excreted mainly via the kidneys as metabolites, with a small portion eliminated through the lungs as carbon dioxide.

Dosage

Intravenous Dosage (Cancer Treatment):

• Colorectal Cancer: The typical dose is 370-425 mg/m² per day as an IV bolus for 5 days in a row (Mayo Clinic regimen), or 400-600 mg/m² IV bolus on Day 1 followed by a continuous infusion of 2400-3000 mg/m² over 46 hours (FOLFOX regimen).
• Breast Cancer: Administered as part of combination therapy, a typical regimen may include 500 mg/m² intravenously on Days 1 and 8 of each 28-day cycle.
• Gastric Cancer: Typically dosed at 500-600 mg/m² IV on Day 1 of each cycle, usually in combination with other chemotherapy agents like cisplatin.

• Actinic Keratosis: Apply a thin layer of 5% cream to the affected area twice daily for 2-4 weeks.
• Superficial Basal Cell Carcinoma: Apply a thin layer of 5% cream to the lesion twice daily for 3-6 weeks or longer depending on the physician’s guidance.

• Dosage adjustments may be needed for patients with renal or hepatic impairment.
• Dosing can vary based on protocols and patient-specific factors such as performance status and prior treatment responses.

Administration

5-FU can be administered as an intravenous bolus, continuous intravenous infusion, or topically. Intravenous administration is the most common method in cancer treatment, either as a single agent or part of a combination regimen. Topical administration is used for skin conditions like actinic keratosis.

Side Effects

Common side effects include nausea, vomiting, diarrhea, mucositis, myelosuppression (low blood cell counts), and hand-foot syndrome (palmar-plantar erythrodysesthesia). More severe side effects may include cardiac toxicity, neurotoxicity, and hepatotoxicity.

Toxicity

Overdosing on 5-FU can lead to severe gastrointestinal toxicity, bone marrow suppression, neurotoxicity, and death. Symptoms of overdose include severe nausea, vomiting, diarrhea, bleeding, and infection due to immunosuppression. Immediate medical intervention is required.

Precautions

Patients with a deficiency of the enzyme dihydropyrimidine dehydrogenase (DPD) are at increased risk of severe toxicity from 5-FU. Pre-screening for DPD deficiency may be recommended. Caution is also advised in patients with pre-existing cardiac disease, liver dysfunction, or poor nutritional status.

Interaction

5-FU interacts with other chemotherapy agents, anticoagulants, and medications that affect liver function. Combining 5-FU with leucovorin enhances its effectiveness by stabilizing the binding of 5-FU to thymidylate synthase. It may also interact with radiation therapy, increasing radiation sensitivity in cancer cells.

Disease Interaction

Patients with a history of cardiac disease may experience increased cardiotoxicity with 5-FU. Additionally, those with liver or kidney dysfunction may require dose adjustments due to altered metabolism and clearance of the drug.

Drug Interaction

5-FU can interact with anticoagulants such as warfarin, increasing the risk of bleeding. It may also interact with other chemotherapy agents, immunosuppressants, and radiation therapy, enhancing both therapeutic and toxic effects.

Food Interactions

There are no major known food interactions with 5-FU, but patients are generally advised to maintain good nutrition to support overall health during chemotherapy. Alcohol may exacerbate side effects like nausea and liver toxicity.

Pregnancy Use

5-FU is classified as Category D for pregnancy, meaning there is positive evidence of risk to the fetus. It should not be used during pregnancy unless absolutely necessary, and effective contraception should be used during treatment.

Lactation Use

5-FU is contraindicated during lactation as it can be excreted into breast milk and may harm the nursing infant. Breastfeeding should be discontinued during treatment.

Acute Overdose

Acute overdose of 5-FU can result in severe gastrointestinal toxicity, myelosuppression, and even death. Immediate management may include supportive care, hydration, anti-nausea medications, and blood transfusions if necessary. In severe cases, the use of the antidote uridine triacetate can reduce the toxicity of 5-FU.

Contraindication

5-FU is contraindicated in patients with known hypersensitivity to the drug, DPD deficiency, and in pregnant or breastfeeding women. It should also be avoided in patients with severe bone marrow suppression.

Use Direction

5-FU should be administered by a healthcare professional in a hospital or clinic setting when used for cancer treatment. Topical forms should be applied according to the prescription, avoiding contact with the eyes and mucous membranes.

Storage Conditions

5-FU should be stored at controlled room temperature (20-25°C). Topical forms should be protected from light and moisture. Intravenous solutions should be used immediately after preparation and any unused portion discarded.

Volume of Distribution

5-FU has a moderate volume of distribution, allowing it to diffuse into various tissues, including tumors. It is widely distributed in the body but has limited penetration into the central nervous system.

Half Life

The half-life of 5-FU is approximately 10-20 minutes when given as a bolus injection due to rapid metabolism by the liver. Continuous infusion leads to a longer effective half-life and more sustained plasma levels.

Clearance

5-FU is primarily cleared by the liver through metabolism by DPD. A small fraction of the drug is excreted unchanged in the urine. The clearance rate may be significantly reduced in patients with DPD deficiency or liver dysfunction.

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Some Frequently Asked Questions About 5-Fluril IV Injection or Infusion 25 mg/ml

1. What is 5-Fluorouracil (5-FU)?

5-Fluorouracil (5-FU) is a chemotherapy drug used to treat various types of cancer by interfering with the growth of cancer cells.

2. What types of cancer is 5-FU used to treat?

It is commonly used to treat:

• Colorectal cancer
• Breast cancer
• Stomach cancer
• Pancreatic cancer
• Esophageal cancer
• Head and neck cancers
• Skin cancer (topical form)

3. How does 5-FU work?

5-FU inhibits DNA and RNA synthesis, preventing cancer cells from dividing and growing.

4. How is 5-FU administered?

It can be given as:

• Intravenous (IV) infusion
• Injection
• Topical cream (for skin cancer and precancerous lesions)

5. Can 5-FU be taken as a pill?

No, 5-FU is usually given as an IV infusion or a topical cream, not as an oral tablet.

6. How long does a course of 5-FU treatment last?

It varies depending on the cancer type and treatment plan, typically lasting from a few weeks to several months.

7. What are the common side effects of 5-FU?

Side effects may include:

• Nausea and vomiting
• Diarrhea
• Fatigue
• Mouth sores
• Low blood cell counts
• Hair thinning
• Skin reactions (if using topical 5-FU)

8. Can 5-FU cause hair loss?

It may cause hair thinning, but complete hair loss is uncommon.

9. Does 5-FU cause nausea?

Yes, nausea is a common side effect, but anti-nausea medications can help.

10. How long does 5-FU stay in the body?

It is rapidly metabolized, but its effects on cancer cells can last for days to weeks.

11. Can I eat normally while taking 5-FU?

Yes, but a balanced, nutritious diet is recommended to manage side effects.

12. Does 5-FU affect fertility?

Yes, it may temporarily or permanently affect fertility in both men and women.

13. Can I drink alcohol while on 5-FU?

Alcohol can worsen side effects, so it is best to avoid it during treatment.

14. Can 5-FU be used in combination with other chemotherapy drugs?

Yes, it is often combined with drugs like leucovorin, oxaliplatin, or irinotecan for better effectiveness.

15. How does 5-FU affect the immune system?

It can lower white blood cell counts, making patients more prone to infections.

16. Can I get vaccinated while on 5-FU?

Live vaccines should be avoided, but inactivated vaccines may be safe under doctor supervision.

17. Can 5-FU cause liver damage?

Yes, liver function should be monitored during treatment.

18. What precautions should be taken during 5-FU treatment?

Patients should:

• Stay hydrated
• Avoid crowded places (to prevent infections)
• Use sunscreen (for skin sensitivity)
• Monitor for signs of infection

19. Can 5-FU be used in children?

It is rarely used in children and only under strict medical supervision.

20. Is 5-FU used for skin conditions?

Yes, topical 5-FU is used for actinic keratosis and basal cell carcinoma.

21. Can 5-FU cause mouth sores?

Yes, mouth sores (stomatitis) are a common side effect.

22. Can 5-FU be used during pregnancy?

No, it can cause severe birth defects and is not safe during pregnancy.

23. Can breastfeeding mothers take 5-FU?

No, 5-FU can pass into breast milk and harm the baby.

24. Can 5-FU cause heart problems?

Rarely, it can cause chest pain or heart rhythm issues.

25. How should topical 5-FU be applied?

Apply a thin layer to the affected skin, as directed by a doctor.

26. Can 5-FU cause eye irritation?

Yes, it may cause eye redness and irritation, especially in topical form.

27. Can 5-FU interact with other medications?

Yes, it may interact with blood thinners, phenytoin, and other chemotherapy drugs.

28. Can I take vitamins or supplements while on 5-FU?

Some supplements may interfere with treatment. Always consult your doctor first.

29. Can 5-FU be given as a single dose?

No, it is usually given in cycles over weeks or months.

30. Does 5-FU cause fatigue?

Yes, fatigue is a common side effect during and after treatment.

31. What should I do if I miss a dose?

Contact your doctor immediately for guidance.

32. Can 5-FU cause weight loss?

Yes, due to nausea, vomiting, and reduced appetite.

33. Can 5-FU be used for lung cancer?

It is not commonly used for lung cancer but may be included in some regimens.

34. How should I store 5-FU?

Keep it in a cool, dry place away from direct sunlight.

35. Can 5-FU affect kidney function?

Yes, kidney function should be monitored during treatment.

36. Can I exercise while on 5-FU?

Light exercise is okay, but avoid strenuous activity.

37. Can 5-FU cause depression?

Yes, chemotherapy drugs can impact mood and mental health.

38. Can 5-FU cause dizziness?

Yes, dizziness and weakness are possible side effects.

39. Can I travel while taking 5-FU?

Yes, but consult your doctor and carry medical records.

40. Does 5-FU affect blood sugar levels?

It can, especially in diabetic patients.

41. Can I drive after receiving 5-FU?

If you feel weak or dizzy, avoid driving.

42. Can 5-FU cause skin darkening?

Yes, skin discoloration may occur as a side effect.

43. Can I stop 5-FU treatment early?

No, always follow the prescribed treatment plan.