5-Fluorouracil Pharmacology

5-Fluorouracil

About 5-Fluorouracil
Antimetabolite (Pyrimidine Analog), Antineoplastic
Mechanism of Action of 5-Fluorouracil
In the body the drug is converted into both flurodeoxy uridinemonophosphate and deoxyuridinetriphosphate. These flurodeoxyuridine monophosphates inhibit thymidylate synthetase which prevents the thymidine synthesis, an essential substrate for DNA synthesis. This thymidine nonavailability causes DNA synthesis failure. This drug itself incorporated into nucleic acid and produces its cytotoxic effect.5-Flurouracil also inhibit the synthesis of RNA..
Pharmacokinets of 5-Fluorouracil
Absorption-Absorbed rapidly after intravenous administration
Distribution- Widely distributed in the body.8 to 12% bound to the plasma proteins. It crosses the blood brain barrier.
Metabolism- It is metabolized in liver and in cell to its active and inactive metabolites.5-fluro-2-deoxyuridine monophosphate is its active metabolite.
Excretion- It is excreted through lungs. A small amount is excreted as unchanged form via feces.
Onset of Action for 5-Fluorouracil
N/A
Duration of Action for 5-Fluorouracil
N/A
Half Life of 5-Fluorouracil
Its plasma half life is about 10 to 20 minutes.
Side Effects of 5-Fluorouracil
1. Nausea
2. Vomiting
3. Lowered resistance to infection
4. Bruising or unusual bleeding
5. Anemia
6. Weakness
7. Sore in mouth
8. Taste changes
9. Diarrhea
10. Loss of appetite
11. Visual changes
12. Black, tarry stools
13. Blood in urine or in stool
14. Cough or hoarseness
15. Fever
16. Chills
17. Myelosuppression
18. Mucositis
19. Dermatitis
20. Angina
21. Heart attack
22. Alopecia
23. Conjunctivitis
24. Cardiac arrhythmias
25. Hyper pigmentation
26. Breathlessness
27. Euphoria
28. Ataxia
29. Nystagmus
30. Leucopenia
31. Thrombocytopenia
32. Anaphylaxis
33. Agranulocytosis
34. Myocardial ischemia
Contra-indications of 5-Fluorouracil
1. Hypersensitivity to the drug
2. Bone marrow suppression
3. Serious infections
4. Have had surgery within the previous month
5. Thrombocytopenia
6. Poor nutritional status
7. Dihydropyramidine dehydrogenase enzyme deficiency
8. The exposure to sunlight after topical application is contraindicated
Special Precautions while taking 5-Fluorouracil
1. Cardiac diseases
2. Hepatic or renal insufficiency
3. Recent radiation on pelvic
4. Previous treatment with alkylating agent.
Pregnancy Related Information
N/A
Old Age Related Information
Use with caution.
Breast Feeding Related Information
N/A
Children Related Information
Use with caution.
Indications for 5-Fluorouracil
1. Colon cancer
2. Breast cancer
3. Stomach cancer
4. Hepatoma
5. Cancer in pancreas
6. Ovarian cancer
7. Cervix cancer
8. Cancer in Urinary bladder
9. Cancer in Head
10. Cancer in Neck
11. Basal cell carcinoma
12. Disseminated superficial porokeratosis & linear keratosis

Interactions for 5-Fluorouracil
Cimetidine: Increased plasma fluorouracil concentration.
Other Bone marrow depressants, Immunosuppressive agents, Irradiation: Additive adverse effects.
Leucovorin calcium: Toxicity of fluorouracil enhanced.
Metronidazole: Enhanced toxicity.
Lab Tests: Elevation in alkaline phosphatase, serum transaminase, serum bilirubin and lactic dehydrogenase may occur.
Typical Dosage for 5-Fluorouracil
Adult-
Intravenous-
10 to15mg/ kg/day for 5 days followed by 5 to7.5mg/ kg on alternate days. Daily dose should not exceed 800mg.This course of therapy repeated every 30 days after the last day of the previous course.
Topical-
Apply the cream once a day for 4 weeks.
Schedule of 5-Fluorouracil
N/A
Storage Requirements for 5-Fluorouracil
Stored at 15 to 30 degree Celsius. Protect from light.
Effects of Missed Dosage of 5-Fluorouracil
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of 5-Fluorouracil
Transfuse the blood components. Induce emesis and gastric lavage.Give symptomatic and supportive treatment.

Home Delivery for 5-Fluorouracil in Your City

Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including 5-fluorouracil.

However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for 5-fluorouracil and other medicines and health products. Home delivery services for 5-fluorouracil may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take 5-fluorouracil only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for 5-fluorouracil before they complete the sale. You can get this information while placing the order for 5-fluorouracil with the pharmacy.

5-Fluorouracil is a generic medicine name and there are several brands available for it. Some of the brands for 5-fluorouracil might be better known than 5-fluorouracil itself. If the pharmacy that's willing to deliver medicines to your home doesn't have 5-fluorouracil in stock, you can ask for one of the branded alternatives for 5-fluorouracil.