Efudex Package Insert

[Sherley]

Forwhich conditions is this drug approved? Fluorouracil is FDA approved for the treatment of the following conditions: anal cancer, cervical cancer, colon cancer, rectal cancer, breast cancer, stomach (gastric) cancer, head and neck cancer, bladder cancer, neuroendocrine tumors, hepatobiliary cancers, thymic cancers, and pancreatic cancer. Fluorouracil may also come in a topical form that is FDA approved for the treatment of superficial basal cell carcinoma. It is important for patients to remember that physicians have the ability to prescribe medication for conditions other than those for which the drug has been approved by the FDA. Patients who have received a prescription of this drug for a condition other than which it is approved may wish to discuss this issue with their physician.

What is the mechanism of action? Fluorouracil belongs to a class of agents called antimetabolites. Antimetabolites produce their anti-cancer effects by inhibiting the ability of a cell to produce or repair DNA, thereby making the cell unable to replicate or repair itself and ultimately causing cellular death.

How is fluorouracil typically given (administered)? Fluorouracil may be given intravenously (into a vein), and may be applied topically as a skin cream. The information on this sheet mainly covers the intravenous formulation. The dose depends on several factors, including the condition being treated, the size of the patient, the particular regimen being used, and the overall health of the patient.

How are patients typically monitored? Patients will usually have scheduled meetings with their healthcare provider while they are being treated with flourouracil. Typically, blood will be drawn to check levels of blood cells and to monitor functions of some organ systems, such as the kidneys or liver. Patients may also undergo physical examinations, scans or other measures to assess side effects and response to therapy. In addition, patients will have their heart function monitored, as treatment with fluorouracil may produce damage to the heart. Patients should notify their healthcare provider if they notice changes in heart rate or rhythm, or experience chest pain. Patients who are using the topical fluorouracil will also undergo skin assessments.

What are possible late side effects of treatment with fluorouracil? With the use of this drug, there is risk of developing damage to the heart after treatment is completed, although this is uncommon. Patients experiencing chest or jaw pain, difficulty breathing, sweating or noticeable changes in heart rate or rhythm should contact their healthcare provider immediately.

This is not a complete list of side effects. Some patients may experience other side effects that are not listed here. Patients may wish to discuss with their physician the other less common side effects of this drug, some of which may be serious.

Some side effects may require medical attention. Other side effects do not require medical attention and may go away during treatment. Patients should check with their physician about any side effects that continue or are bothersome.

What is a package insert? A package insert is required by the FDA and contains a summary of the essential scientific information needed for the safe and effective use of the drug for healthcare providers and consumers. A package insert typically includes information regarding specific indications, administration schedules, dosing, side effects, contraindications, results from some clinical trials, chemical structure, pharmacokinetics, and metabolism of the specific drug.By carefully reviewing the package insert, you will get the most complete and current information about how to safely use this drug. If you do not have the package insert for the drug you are using, your pharmacist or physician may be able to provide you with a copy.

The information provided above on the drug you have selected is provided for your information only and is not a substitute for consultation with an appropriate medical doctor. We are providing this information solely as a courtesy and, as such, it is in no way a recommendation as to the safety, efficacy, or appropriateness of any particular drug, regimen, dosing schedule for any particular cancer, condition, or patient nor is it in any way to be considered medical advice. Patients should discuss the appropriateness of a particular drug or chemotherapy regimen with their physician.

As with any printed reference, the use of particular drugs, regimens and drug dosages may become out-of-date over time, since new information may have been published and become generally accepted after the latest update to this printed information. Please keep in mind that health care professionals are fully responsible for practicing within current standards, avoiding use of outdated regimens, employing good clinical judgment in selecting drugs and/or regimens, in calculating doses for individual patients, and verifying all dosage calculations.

OMNI HEALTH MEDIA SPECIFICALLY DISCLAIMS AND EXCLUDES ALL EXPRESSED OR IMPLIED WARRANTIES, INCLUDING ANY IMPLIED WARRANTIES AS TO QUALITY, ACCURACY (INCLUDING TYPOGRAPHICAL ERRORS), MERCHANTABILITY, OR FITNESS FOR ANY PARTICULAR PURPOSE OF THE INFORMATION CONTAINED HEREIN. OMNI HEALTH MEDIA DISCLAIMS ALL LIABILITY OR DAMAGES ARISING FROM ANY USE OF THE INFORMATION.

Fluorouracil (5-FU, 5-fluorouracil), sold under the brand name Adrucil among others, is a cytotoxic chemotherapy medication used to treat cancer.[3] By intravenous injection it is used for treatment of colorectal cancer, oesophageal cancer, stomach cancer, pancreatic cancer, breast cancer, and cervical cancer.[3] As a cream it is used for actinic keratosis, basal cell carcinoma, and skin warts.[4][5]

Side effects of use by injection are common.[3] They may include inflammation of the mouth, loss of appetite, low blood cell counts, hair loss, and inflammation of the skin.[3] When used as a cream, irritation at the site of application usually occurs.[4] Use of either form in pregnancy may harm the fetus.[3] Fluorouracil is in the antimetabolite and pyrimidine analog families of medications.[6][7] How it works is not entirely clear, but it is believed to involve blocking the action of thymidylate synthase and thus stopping the production of DNA.[3]

Fluorouracil was patented in 1956 and came into medical use in 1962.[8] It is on the World Health Organization's List of Essential Medicines.[9] In 2021, it was the 281st most commonly prescribed medication in the United States, with more than 800,000 prescriptions.[10][11]

Fluorouracil has been given systemically for anal, breast, colorectal, oesophageal, stomach, pancreatic and skin cancers (especially head and neck cancers).[12] It has also been given topically (on the skin) for actinic keratoses, skin cancers and Bowen's disease[12] (a type of cutaneous squamous-cell carcinoma), and as eye drops for treatment of ocular surface squamous neoplasia.[13] Other uses include ocular injections into a previously created trabeculectomy bleb to inhibit healing and cause scarring of tissue, thus allowing adequate aqueous humor flow to reduce intraocular pressure.

Fluorouracil is contraindicated in patients who are severely debilitated and in patients with bone marrow suppression due to either radiotherapy or chemotherapy.[14] It is likewise contraindicated in pregnant or breastfeeding women.[14] Non-topical use, i.e. administration by injection, should be avoided in patients who do not have malignant illnesses.[14]

The United States package insert warns that acute cerebellar syndrome has been observed following injection of fluorouracil and may persist after cessation of treatment. Symptoms include ataxia, nystagmus, and dysmetria.[23]

There is very little difference between the minimum effective dose and maximum tolerated dose of 5-FU, and the drug exhibits marked individual pharmacokinetic variability.[24][25][26] Therefore, an identical dose of 5-FU may result in a therapeutic response with acceptable toxicity in some patients and unacceptable and possibly life-threatening toxicity in others.[24] Both overdosing and underdosing are of concern with 5-FU, although several studies have shown that the majority of colorectal cancer patients treated with 5-FU are underdosed based on today's dosing standard, body surface area (BSA).[27][28][29][30] The limitations of BSA-based dosing prevent oncologists from being able to accurately titer the dosage of 5-FU for the majority of individual patients, which results in sub-optimal treatment efficacy or excessive toxicity.[27][28]

Numerous studies have found significant relationships between concentrations of 5-FU in blood plasma and both desirable or undesirable effects on patients.[31][32] Studies have also shown that dosing based on the concentration of 5-FU in plasma can greatly increase desirable outcomes while minimizing negative side effects of 5-FU therapy.[27][33] One such test that has been shown to successfully monitor 5-FU plasma levels and which "may contribute to improved efficacy and safety of commonly used 5-FU-based chemotherapies" is the My5-FU test.[29][34][35]

It may increase the INR and prothrombin times in people on warfarin.[14] Fluorouracil's efficacy is decreased when used alongside allopurinol, which can be used to decrease fluorouracil induced stomatitis through use of allopurinol mouthwash.[36]

The dihydropyrimidine dehydrogenase (DPD) enzyme is responsible for the detoxifying metabolism of fluoropyrimidines, a class of drugs that includes 5-fluorouracil, capecitabine, and tegafur.[37] Genetic variations within the DPD gene (DPYD) can lead to reduced or absent DPD activity, and individuals who are heterozygous or homozygous for these variations may have partial or complete DPD deficiency; an estimated 0.2% of individuals have complete DPD deficiency.[37][38] Those with partial or complete DPD deficiency have a significantly increased risk of severe or even fatal drug toxicities when treated with fluoropyrimidines; examples of toxicities include myelosuppression, neurotoxicity and hand-foot syndrome.[37][38]

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