Fluorouracil, topical

Dibucaine (Nupercainal) Doxepin, Topical (Zonalon, Prudoxin) Econazole (Spectazole) Efalizumab (Raptiva) Erythromycin, Topical (A/T/S, Eryderm, Erycette, T-Stat) Erythromycin Benzoyl Peroxide (Benzamycin) Finasteride (Propecia) Fluorouracil, Topical [5-FU] (Efudex) Gentamicin, Topical (Garamycin, G-Mycitin)... 

Fluorouracil/ Topical [5-FU] (Efudex) [Antineoplastic/ Antimetabollte] Uses Basal cell carcinoma actinic/solar k atosis Action Inhibits thymidylate S5mthetase (-1- DNA S5mth, S-phase specific) Dose 5% cream bid X 2-6 wk Caution [D, ] Irritant chemo Contra Component sensitivity Disp Cream, soln SE Rash, dry skin, photosens EMS See RuorouracU OD See RuorouracU... 

FLUOROURACIL (TOPICAL AND ORAL) PORFIMER t risk of photosensitivity reactions Attributed to additive effects Avoid exposure of skin and eyes to direct sunlight for 30 days after porfimer therapy... 

PORFIMER I. ACE INHIBITORS -enalapril 2. ANALGESICS -celecoxib, ibuprofen, ketoprofen, naproxen 3. ANTIARRHYTHMICS — amiodarone 4. ANTIBIOTICS -ciprofloxacin, dapsone, sulphonamides, tetracyclines 5. ANTICANCER AND IMMUNOMODULATING DRUGS -fluorouracil (topical and oral) 6. ANTIDIABETIC DRUGS-glipizide 7. ANTIMALARIALS -hydroxychloroquine, quinine 8. ANTIPSYCHOTICS -chlorpromazine, fluphenazine 9. CALCIUM CHANNEL BLOCKERS - diltiazem 10. DIURETICS -bumetanide, furosemide, hydrochlorothiazide II. PARA-AMINOBENZOIC ACID (TOPICAL) 12. RETINOIDS-acitretin, isotretinoin 13. SALICYLATES (TOPICAL) t risk of photosensitivity reactions Attributed to additive effects Avoid exposure of skin and eyes to direct sunlight for 30 days after porfimer therapy... 

Fluorouracil Topical antimitotic drug Telangiectasia bilateral cicatricial ectropion exacerbation of Herpes labialis pain, edema, livedo reticularis erosions (SEDA-7, 166) (SEDA-7, 166) (SEDA-5, 155)... 

ANTICANCER AND IMMUNOMODULATING DRUGS -fluorouracil (topical and oral)... 

Johnson MR, Hageboutros A, Wang K et al. life-threatening toxicity in a dihydropyrimidine dehydrogenase-deficient patient after treatment with topical 5-fluorouracil. Clin Cancer Res 1999 5 2006-2011. 

The reaction of XeF2 with uracil produces the 5-fluoro derivative, which can be applied topically for treating some types of skin diseases including some types of skin cancer. The reaction producing 5-fluorouracil can be shown as... 

K. B. Sloan, S. A. Koch, K. G. Silver, Mannich Base Derivatives of Theophylline and 5-Fluorouracil Syntheses, Properties and Topical Delivery Characteristics , Int. J. Pharm. 1984, 21, 251 - 264. 

Interferes w/ DNA synth Dose Adults. Anaerobic Infxns 500 mg IV q6-8h Amebic dysentery 750 mg/d PO for 5-10 d Trichomoniasis 250 mg PO tid for 7 d or 2 g PO X 1 C. difficile 500 mg PO or IV qSh for 7-10 d (PO preferred IV only if pt NPO) Vaginosis 1 applicator-full intravag bid or 500 mg PO bid for 7 d Acne rosacea/skin Apply bid Peds. 30 mg/ kg PO/IV/d q6H, 4 g/d max-s-. Amebic dysentery 35-50 mg/kg/24 h PO in 3 -s- doses for 5-10 d Rx 7-10 d for C. difficile-, in hepatic impair Caution [B, M] Avoid EtOH Contra 1st tri of PRO Disp Tabs, caps, IV, topical lotion, intravag gel, cream SE Disulfiram-like Rxn dizziness, HA, GI upset, anorexia, urine discoloration Interactions t Effects W/ cimetidine T effects OF carbamazepine, fluorouracil, Li, warfarin -1- effects W/ barbiturates, cholestyramine, colestipol, phenytoin EMS t Effects of anticoagulants concurrent EtOH use can cause disulfiram-like Rxn (tach, N/V, sweating, flushing, headache, blurred vision, confusion) may cause a metallic taste and discolored urine OD May cause N/V/D, numbness in hands and feet, Szs, and loss of coordination symptomatic and supportive... 

Fluorouracil is a pyrimidine analogue (see Chapter 27, Section II.b.3). Topical application may be used for malignant and premalignant skin conditions, including actinic keratosis. Adverse effects include local inflammatory and allergic reactions. Photosensitivity reactions during and for up to 2 months after treatment may become manifest. 

Fluorouracil (Efudex, Fluoroplex) is an antimetabolite used for the topical treatment of actinic keratoses. It is also useful for the treatment of superficial basal cell carcinomas when conventional surgical modalities are impractical. Local inflammatory reactions characterized by erythema, edema, crusting, burning, and pain are common (and, some would argue, desirable) but may be minimized by reduced frequency of application or use in combination with a topical corticosteroid. 

Other routes of administration can be employed in certain situations. Methotrexate and cytarabine are given intrathecally or intraventricularly to prevent relapses in the meninges in acute lymphocytic leukemia and to treat carcinomatous meningitis. Thiotepa and bleomycin have been administered by intravesical instillation to treat early bladder cancers. Fluorouracil can be applied topically for certain skin cancers. 

Fluorouracil is used in several combination regimens in the treatment of breast cancer. It also has palliative activity in gastrointestinal adenocarcinomas, including those originating in the stomach, pancreas, liver, colon, and rectum. Other tumors in which some antitumor effects have been reported include carcinomas of the ovary, cervix, oropharynx, bladder, and prostate. Topical 5-fluorouracil cream has been useful in the treatment of premalignant keratoses of the skin and superficial basal cell carcinomas, but it should not be used in invasive skin cancer. 

Fluorouracil, a fluorinated pyrimidine antimetabolite is used topically for the treatment of multiple actinic keratoses and intralesionally for keratoacanthomas. 

Fluorouracil is a fluorinated pyrimidine antimetabolite that resembles uracil, with a fluorine atom substituted for the 5-methyl group. Its systemic pharmacology is described in Chapter 54. Fluorouracil is used topically for the treatment of multiple actinic keratoses. 

Approximately 6% of a topically applied dose is absorbed—an amount insufficient to produce adverse systemic effects. Most of the absorbed drug is metabolized and excreted as carbon dioxide, urea, and ct-fluoro-B-alanine. A small percentage is eliminated unchanged in the urine. Fluorouracil inhibits thymidylate synthetase activity, interfering with the synthesis of DNA and, to a lesser extent, RNA. These effects are most marked in atypical, rapidly proliferating cells. 

Fluoroplex 1% topical solution contains fluorouracil 1%, propylene glycol, sodium hydroxide or hydrochloric acid to adjust the pH, and purified water. 

Fluorouracil is normally given intravenously (Table 55-3) and has a short metabolic half-life on the order of 15 minutes. It is not administered by the oral route because its bioavailability is erratic due to the high levels of the breakdown enzyme dihydropyrimidine dehydrogenase present in the gut mucosa. Floxuridine (5-fluoro-2 -deoxyuridine, FUDR) has an action similar to that of fluorouracil, and it is only used for hepatic artery infusions. A cream incorporating fluorouracil is used topically for treating basal cell cancers of the skin. 

Therapeutic applications Fluorouracil is employed primarily in the treatment of slowly growing, solid tumors (for example, colorectal, breast, ovarian, pancreatic, and gastric carcinomas). Adjuvant therapy with levamisole, a veterinary anthelmintic agent, improves the survival of patients with colonic cancer. 5-FU is also effective for the treatment of superficial basal cell carcinom when applied topically. 

A useful derivative of this compound is 5-fluorouracil that is used as a topical ointment in the treatment of some types of skin cancer and other skin diseases. One preparation of the compound is by the fluorination of uracil with XeF2 ... 

Carbachol, topical cholinesterase inhibitors, and oral CAIs (e.g., aceta-zolamide) are used as last-resort options after failure of less toxic options. The optimal timing of laser or surgical trabeculectomy is controversial, ranging from initial therapy to after failure of third- or fourth-hue drug therapy. Antiproliferative agents such as fluorouracil and mitomydn C are used to modify the healing process and maintain patency. 

FLUOROURACIL TEMOPORFIN t risk of photosensitivity with topical fluorouracil Uncertain possibly additive effect (topical fluorouracil can cause local irritation, while temoporfin is a photosensitizer) Patients on temoporfin are advised to avoid direct sunlight for at least 15 days... 

Common causative organisms in adults with canaliculitis include Staphylococcus aureus and Actinomyces species. Primary herpetic infections (herpes simplex, varicella, and vaccinia) have a higher prevalence among patients younger than age 20 years and often present with cutaneous manifestations of the infectious disease. Chronic allergies may also be associated with canalicular obstruction. Occasionally, patients may suffer from canalicular obstruction as a result of topical antimetabolite treatment such as 5-fluorouracil or mitomycin C. 

Fluorouracil is specific to the S phase of the cell cycle. It is primarily used intravenously to treat carcinoma of the breast and adenocarcinomas of the gastrointestinal tract (1). In addition, topical fluorouracil is used to treat actinic keratoses. 

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