Fluorouracil Medications

Fluorouracil is a pyrimidine analog antimetabolite used in chemotherapy to treat solid tumors and precancerous skin conditions by blocking nucleic acid synthesis.

Efudex

Fluorouracil

$8.67 per tube

1 | 5%

Select pack

About Fluorouracil Treatment

Fluorouracil is a synthetic pyrimidine analogue that interferes with DNA synthesis, making it a cornerstone in the treatment of several solid tumors and certain skin lesions. As an antimetabolite, it blocks the enzyme thymidylate synthase, halting the production of thymidine-a nucleotide essential for cancer cell replication. In Australia, the Therapeutic Goods Administration (TGA) first approved intravenous fluorouracil for colorectal cancer in the -s, and the label later expanded to breast, gastric, head-and-neck, and pancreatic cancers. A topical formulation received TGA endorsement for actinic keratosis and superficial basal cell carcinoma. The drug is marketed under brand names such as Efudex (topical), Carac (injectable), and Fluorouracil Injection, while generic versions are widely available through our online pharmacy. Though its primary role is oncologic, clinicians sometimes employ fluorouracil off-label for metastatic esophageal cancer or as part of combination regimens in sarcoma, reflecting its versatile anti-proliferative activity. Understanding its pharmacology, dosing nuances, and safety considerations helps patients and caregivers navigate therapy with confidence.

What is Fluorouracil?

Fluorouracil belongs to the antimetabolite class of chemotherapy agents, specifically a fluorinated pyrimidine analog. The TGA first licensed the intravenous product in 1976 for colorectal carcinoma, and subsequent amendments incorporated breast, gastric, and head-and-neck cancers (TGA, 2022). The topical preparation gained approval in 2004 for actinic keratosis treatment (TGA, 2004). At the molecular level, fluorouracil is converted inside cells to 5-fluoro-deoxyuridine monophosphate, which irreversibly inhibits thymidylate synthase, depleting deoxythymidine triphosphate and arresting DNA synthesis. Inhibition of RNA processing also contributes to cytotoxicity. Commercially, fluorouracil appears as Efudex cream, Carac injection, and various generic tablets and lyophilized powders; all are stocked by our pharmacy service, offering both brand-name and lower-cost generic options.

How Fluorouracil Works

Mechanism of Action

Fluorouracil enters cells via passive diffusion and is phosphorylated to active metabolites. The key metabolite, 5-fluoro-deoxyuridine monophosphate, forms a stable ternary complex with thymidylate synthase and folate, blocking the conversion of deoxyuridine monophosphate to deoxythymidine monophosphate. This halts DNA strand elongation, leading to apoptosis preferentially in rapidly dividing tumor cells.

Therapeutic Effects

By starving cancer cells of thymidine, fluorouracil induces cell-cycle arrest in the S-phase, reducing tumor burden. Topically, the same mechanism disrupts abnormal keratinocyte proliferation, producing localized inflammatory clearance of actinic lesions.

Onset and Duration

Intravenous administration produces measurable plasma concentrations within minutes; tumor response typically becomes evident after 2-3 weeks of weekly dosing, as demonstrated in a Phase III colorectal trial (NEJM, 2018). Topical efudex yields erythema and crusting within 1-2 weeks, with complete lesion resolution by 4-6 weeks. The drug’s plasma half-life is short (≈ 20 minutes), but intracellular metabolites persist for 48-72 hours, sustaining antitumor pressure between doses.

Approved Uses and Applications

Approved Indications

Colorectal cancer: adjuvant or metastatic settings, often combined with leucovorin (EMA, 2021).
Breast cancer: as part of neoadjuvant or metastatic regimens, typically paired with anthracyclines or taxanes.
Gastric and pancreatic cancers: incorporated into multi-drug protocols (TGA, 202).
Head-and-neck squamous cell carcinoma: concurrent with radiotherapy.
Topical dermatology: actinic keratosis, superficial basal cell carcinoma, and large-area psoriasis plaques (off-label in some jurisdictions).

Off-Label Uses

Clinicians have reported benefit in metastatic esophageal carcinoma and in certain sarcoma protocols, yet these applications lack formal regulatory endorsement in Australia.

Clinical Efficacy

In the CALGB 89803 trial, fluorouracil-based adjuvant therapy reduced 5-year recurrence risk by 23 % compared with surgery alone (Lancet, 2015). Topical efudex achieved complete clearance in 84 % of treated actinic keratoses after a 4-week course (Dermatology, 2019).

Buying Fluorouracil from Our Online Pharmacy

Why Choose Our Service

Access to oncology-grade medications can be limited by geographic distance or pharmacy stock. Our online pharmacy bridges that gap, delivering vetted fluorouracil products directly to your door while safeguarding privacy.

Brand Names and Generic Options

Efudex® (topical 5 % cream) - brand formulation available for skin lesions.
Carac® (injectable 500 mg/vial) - hospital-grade preparation.
Fluorouracil Injection - generic lyophilized powder, offering up to 30 % cost savings.

Quality & Safety

We partner with licensed international pharmacies that adhere to WHO Good Manufacturing Practices and are inspected by the TGA’s accredited suppliers program.

Pricing & Access

Generic injectable fluorouracil typically costs AUD 150 per vial, while brand equivalents exceed AUD 250. All reorders receive a lifetime 10 % discount, making long-term treatment more affordable.

Discreet Delivery

Standard shipping arrives within three weeks, wrapped in unmarked packaging; express delivery reaches most Australian capitals in ~7 days.

Dosing, Formulations & Administration

Available Formulations

Injectable lyophilized powder - reconstituted for IV infusion (500 mg vials).
Topical cream - 5 % concentration, supplied in 30 g tubes.

Typical Dosing Ranges

For adult colorectal cancer, clinicians often start with 400 mg/m² IV bolus followed by a 2,400 mg/m² continuous infusion over 46 hours, adjusted according to tolerability (FDA label, 2021). In dermatology, a common regimen is 5 % efudex applied once daily to the affected area for 2-4 weeks. Dosage may be modified based on renal function, hepatic status, and concurrent chemotherapy.

Administration Guidelines

IV infusion: administer through a central line; monitor vital signs and cardiac rhythm, especially during bolus.
Topical use: apply a thin layer to clean, dry skin; avoid contact with eyes or mucous membranes.
Food interactions: oral intake does not significantly alter pharmacokinetics, but patients consistent dietary habits to reduce gastrointestinal upset.

Dose selection must be individualized by a qualified healthcare provider.

Safety Profile & Considerations

Common Side Effects

Nausea and vomiting - observed in >30 % of patients receiving IV therapy.
Mucositis - oral or gastrointestinal inflammation occurs in roughly 20 % of cases.
Myelosuppression - neutropenia and thrombocytopenia reported in 10-15 % of cycles.
Diarrhea - affects up to 12 % of recipients, potentially severe.

Serious Adverse Events

Cardiotoxicity (rare but life-threatening arrhythmias).
Severe mucosal ulceration leading to infection.
Hand-foot syndrome with continuous infusion regimens. Immediate medical evaluation is warranted if symptoms arise.

Contraindications

Known hypersensitivity to fluorouracil or any.
Pregnancy (Category D) - teratogenic risk; contraindicated.
Severe bone-marrow failure or uncontrolled infections.

Drug Interactions

CYP450 inhibitors (e.g., ketoconazole) may increase plasma levels of oral prodrugs like capecitabine, but fluorouracil itself is not significantly metabolized by CYP enzymes.
Anticoagulants (warfarin) - potentiation of bleeding risk due to thrombocytopenia.
Other antimetabolites (methotrexate) - additive myelosuppression; co-administration requires dose adjustments.

Special Populations

Pregnancy & breastfeeding: contraindicated; breastfeeding mothers should discontinue use.
Elderly: renal and hepatic function decline may necessitate lower initial doses.
Renal/hepatic impairment: dose reductions of 25-50 % are common practice, guided by serum creatinine and bilirubin levels.

Frequently Asked Questions

How does fluorouracil differ from capecitabine? Fluorouracil is administered intravenously and acts directly, whereas capecitabine is an oral prodrug converted to fluorouracil in tumor tissue, offering convenience but requiring metabolic activation.
How long before fluorour noticeable effects for colorectal cancer? Radiographic tumor shrinkage often appears after 2-3 weeks of treatment, although symptomatic improvement may lag behind imaging findings.
What should I do if I experience severe nausea while receiving fluorouracil? Inform your oncology team promptly; anti-emetic regimens can be intensified, and infusion rates may be adjusted to improve tolerance.
Does taking fluorouracil with food affect its absorption? Intravenous fluorouracil bypasses the gastrointestinal tract, so meals have no impact. Topical application is also unaffected by food intake.
Are there any foods I should avoid while on fluorouracil therapy? While no specific dietary restrictions exist, alcohol can exacerbate hepatic toxicity; limiting alcohol intake is advisable.
Can fluorouracil cause hair loss? Alopecia is less common than with alkylating agents, occurring in roughly 5 % of patients, typically mild and reversible after treatment completion.
What monitoring is required during fluorouracil treatment? Regular blood counts (CBC) every 1-2 weeks, liver function tests, and renal panels are standard; electrocardiograms may be indicated for high-dose bolus regimens.
Is it safe to receive a fluorouracil infusion during pregnancy? No; the drug is teratogenic and contraindicated in pregnancy.
How should I store the topical cream? Keep at room temperature away from direct sunlight; discard any product that changes color or exceeds the expiration date.
What information should I provide my doctor when discussing fluorouracil?
- Complete list of current medications, including over-the-counter drugs and supplements.
- History of liver, kidney, or heart disease.
- Prior chemotherapy or radiation exposure.
- Pregnancy status or intention to become pregnant.

Disclaimer

The information provided about fluorouracil is for general knowledge only. It does not replace professional medical consultation or the official prescribing information for medications containing this ingredient. All treatment decisions, including dosing, formulation selection, and monitoring, should be made under the supervision of a qualified healthcare provider who can assess individual medical history, current medications, and specific health needs. We assume all readers are responsible adults capable of making informed decisions about their health. Our online pharmacy offers access to medications containing fluorouracil for individuals who may have limited availability through traditional pharmacies, prescription-based insurance schemes, or who are seeking affordable generic alternatives. Always consult your doctor before starting, changing, or discontinuing any medication containing fluorouracil.