WARNING
It is recommended that ADRUCIL Injection be given only by or under the supervision of qualified physician who is experienced in cancer chemotherapy and who is well versed in the use of potent antimetabolites. Because of the possibility of severe toxic reactions, it is recommended that patients be hospitalized at least during the initial course of therapy. These instructions should be thoroughly reviewed before administration of ADRUCIL. ADRUCIL? (fluorouracil injection USP), an antineoplastic antimetabolite, is sterile, nonpyrogenic injectable solution for intravenous administration. Each 10 mL contains 500 mg fluorouracil, USP; pH is adjusted to 8.6 to 9.4 with sodium hydroxide. Chemically, fluorouracil, USP, fluorinated pyrimidine, is 5-fluoro-2,4 (1H,3H)-pyrimidinedione. It is white to practically white crystalline powder which is sparingly soluble in water. The structural formula is: C4H3FN2O2 M.W. 130.08 Close CLINICAL PHARMACOLOGY There is evidence that the metabolism of fluorouracil in the anabolic pathway blocks the methylation reaction of deoxyuridylic acid to thymidylic acid. In this manner, fluorouracil interferes with the synthesis of deoxyribonucleic acid (DNA) and to lesser extent inhibits the formation of ribonucleic acid (RNA). Since DNA and RNA are essential for cell division and growth, the effect of fluorouracil may be to create thymine deficiency which provokes unbalanced growth and death of the cell. The effects of DNA and RNA deprivation are most marked on those cells which grow more rapidly and which take up fluorouracil at more rapid rate. Following intravenous injection, fluorouracil distributes into tumors, intestinal mucosa, bone marrow, liver and other tissues throughout the body. In spite of its limited lipid solubility, fluorouracil diffuses readily across the blood-brain barrier and distributes into cerebrospinal fluid and brain tissue. Seven percent to 20% of the parent drug is excreted unchanged in the urine in hours; of this over 90% is excreted in the first hour. The remaining percentage of the administered dose is metabolized, primarily in the liver. The catabolic metabolism of fluorouracil results in degradation products (e.g., CO2, urea and ?-fluoro-?-alanine) which are inactive. The inactive metabolites are excreted in the urine over the next to hours. When fluorouracil is labeled in the six carbon position, thus preventing the 14C metabolism to CO2, approximately 90% of the total radioactivity is excreted in the urine. When fluorouracil is labeled in the two carbon position approximately 90% of the total radioactivity is excreted in expired CO2. Ninety percent of the dose is accounted for during the first 24 hours following intravenous administration. Following intravenous administration of fluorouracil, the mean half-life of elimination from plasma is approximately 16 minutes, with range of to 20 minutes, and is dose dependent. No intact drug can be detected in the plasma hours after an intravenous injection. Close INDICATIONS AND USAGE ADRUCIL (fluorouracil injection USP) is effective in the palliative management of carcinoma of the colon, rectum, breast, stomach and pancreas. Close CONTRAINDICATIONS(What is this?) ADRUCIL injection therapy is contraindicated for patients in poor nutritional state, those with depressed bone marrow function, those with potentially serious infections or those with ... WARNINGS (see boxed WARNING) THE DAILY DOSE OF ADRUCIL INJECTION IS NOT TO EXCEED 800 MG. IT IS RECOMMENDED THAT PATIENTS BE HOSPITALIZED DURING THEIR FIRST COURSE OF TREATMENT. ADRUCIL ... PRECAUTIONS General Fluorouracil is highly toxic drug with narrow margin of safety. Therefore, patients should be carefully supervised, since therapeutic response is ... ADVERSE REACTIONS Stomatitis and esophagopharyngitis (which may lead to sloughing and ulceration), diarrhea, anorexia, nausea and emesis are commonly seen during therapy. Leukopenia usually follows ... OVERDOSAGE The possibility of overdosage with fluorouracil is unlikely in view of the mode of administration. Nevertheless, the anticipated manifestations would be nausea, vomiting, diarrhea ... DOSAGE AND ADMINISTRATION General Instructions ADRUCIL injection should be administered only intravenously, using care to avoid extravasation. No dilution is required. All dosages are ... HOW SUPPLIED For intravenous use. ADRUCIL? (fluorouracil injection USP) is available as follows: SINGLE DOSE VIALS NDC Number ... REFERENCES 1. Recommendations for the Safe Handling of Parenteral Antineoplastic Drugs. Washington, DC, U.S. Government Printing Office (NIH Publication No. 83-2621) ... SPL UNCLASSIFIED SECTION TEVA PHARMACEUTICALS USA, INC. North Wales, PA 19454 Rev. 11/2015 Package/Label Display Panel(What is this?) Adrucil? (fluorouracil injection USP) 50 mg/mL, 10 10 mL Single Dose Vial Carton Label Text NDC 0703 ... INGREDIENTS AND APPEARANCE Product info.
