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Black Box Warning
See full prescribing information for complete Boxed Warning.
It is recommended that ADRUCIL Injection be given only by or under the supervision of a 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.
Overview
Fluorouracil (injection) is a that is FDA approved for the {{{indicationType}}} of carcinoma of the colon, rectum, breast, stomach and pancreas.. There is a Black Box Warning for this drug as shown here. Common adverse reactions include .
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
Condition1
ADRUCIL Injection is effective in the palliative management of carcinoma of the colon, rectum, breast, stomach and pancreas.
Dosing Information
General Instructions
ADRUCIL Injection should be administered only intravenously, using care to avoid extravasation. No dilution is required.
All dosages are based on the patient's actual weight. However, the estimated lean body mass (dry weight) is used if the patient is obese or if there has been a spurious weight gain due to edema, ascites or other forms of abnormal fluid retention.
It is recommended that prior to treatment each patient be carefully evaluated in order to estimate as accurately as possible the optimum initial dosage of ADRUCIL.
Dosage
Twelve mg/kg are given intravenously once daily for four successive days. The daily dose should not exceed 800 mg. If no toxicity is observed, 6 mg/kg are given on the 6th, 8th, 10th and 12th days unless toxicity occurs. No therapy is given on the 5th, 7th, 9th or 11th days. Therapy is to be discontinued at the end of the 12th day, even if no toxicity has become apparent.
Poor risk patients or those who are not in an adequate nutritional state should receive 6 mg/kg/day for three days. If no toxicity is observed, 3 mg/kg may be given on the 5th, 7 th and 9 th days unless toxicity occurs. No therapy is given on the 4 th, 6 th or 8 th days. The daily dose should not exceed 400 mg.
A sequence of injections on either schedule constitutes a "course of therapy."
Maintenance Therapy
In instances where toxicity has not been a problem, it is recommended that therapy be continued using either of the following schedules:
Repeat dosage of first course every 30 days after the last day of the previous course of treatment.
When toxic signs resulting from the initial course of therapy have subsided, administer a maintenance dosage of 10 to 15 mg/kg/week as a single dose. Do not exceed 1 g per week.
The patient's reaction to the previous course of therapy should be taken into account in determining the amount of the drug to be used, and the dosage should be adjusted accordingly. Some patients have received from 9 to 45 courses of treatment during periods which ranged from 12 to 60 months.
Handling and Disposal
Procedures for proper handling and disposal of anticancer drugs should be considered. Several guidelines on this subject have been published.1–7 There is no general agreement that all of the procedures recommended in the guidelines are necessary or appropriate.
Note: Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit. If a precipitate occurs due to exposure to low temperatures, resolubilize by heating to 140°F and shaking vigorously; allow to cool to body temperature before using.
Directions for proper use of pharmacy bulk package
(Not for Direct Infusion)
The 50 mL and 100 mL Pharmacy Bulk Packages are for use in a Pharmacy Admixture Service only. They should be inserted into a plastic hanging device and suspended as a unit in a laminar flow hood. Use only if clear and seal is intact and undamaged.
Use of this product is restricted to a suitable work area, such as a laminar flow hood. Use only if clear and seal is intact and undamaged. Prior to entering the vial, remove the flip-off seal and cleanse the rubber closure with a suitable antiseptic agent. The container closure may be penetrated only one time, utilizing a suitable sterile transfer device or dispensing set which allows measured distribution of the contents. The date and time the vial was initially opened should be recorded in the space provided on the vial label. Transfer individual dose(s) to appropriate intravenous infusion solutions. Use of a syringe with a needle is not recommended. Multiple entries increase the potential of microbial and particulate contamination.
The withdrawal of container contents should be accomplished without delay using aseptic technique.However, should this not be possible, a maximum time of 4 hours from initial closure entry is permitted to complete fluid transfer operations. It is recommended that the transferred fluids be used promptly.
Recommended Storage Conditions After Opening
Keep under laminar flow hood at room temperature.
Condition2
Dosing Information
Dosage
Condition3
Dosing Information
Dosage
Condition4
Dosing Information
Dosage
Off-Label Use and Dosage (Adult)
Guideline-Supported Use
Condition1
Developed by:
Class of Recommendation:
Strength of Evidence:
Dosing Information
Dosage
Condition2
There is limited information regarding Off-Label Guideline-Supported Use of Fluorouracil (injection) in adult patients.
Non–Guideline-Supported Use
Condition1
Dosing Information
Dosage
Condition2
There is limited information regarding Off-Label Non–Guideline-Supported Use of Fluorouracil (injection) in adult patients.
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
Condition1
Dosing Information
Dosage
Condition2
There is limited information regarding FDA-Labeled Use of Fluorouracil (injection) in pediatric patients.
Off-Label Use and Dosage (Pediatric)
Guideline-Supported Use
Condition1
Developed by:
Class of Recommendation:
Strength of Evidence:
Dosing Information
Dosage
Condition2
There is limited information regarding Off-Label Guideline-Supported Use of Fluorouracil (injection) in pediatric patients.
Non–Guideline-Supported Use
Condition1
Dosing Information
Dosage
Condition2
There is limited information regarding Off-Label Non–Guideline-Supported Use of Fluorouracil (injection) in pediatric patients.
Contraindications
Condition1
Warnings
See full prescribing information for complete Boxed Warning.
It is recommended that ADRUCIL Injection be given only by or under the supervision of a 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.
Description
Precautions
Description
Adverse Reactions
Clinical Trials Experience
There is limited information regarding Clinical Trial Experience of Fluorouracil (injection) in the drug label.
Body as a Whole
Cardiovascular
Digestive
Endocrine
Hematologic and Lymphatic
Metabolic and Nutritional
Musculoskeletal
Neurologic
Respiratory
Skin and Hypersensitivy Reactions
Special Senses
Urogenital
Miscellaneous
Postmarketing Experience
There is limited information regarding Postmarketing Experience of Fluorouracil (injection) in the drug label.
Australian Drug Evaluation Committee (ADEC) Pregnancy Category
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Fluorouracil (injection) in women who are pregnant.
Labor and Delivery
There is no FDA guidance on use of Fluorouracil (injection) during labor and delivery.
Nursing Mothers
There is no FDA guidance on the use of Fluorouracil (injection) with respect to nursing mothers.
Pediatric Use
There is no FDA guidance on the use of Fluorouracil (injection) with respect to pediatric patients.
Geriatic Use
There is no FDA guidance on the use of Fluorouracil (injection) with respect to geriatric patients.
Gender
There is no FDA guidance on the use of Fluorouracil (injection) with respect to specific gender populations.
Race
There is no FDA guidance on the use of Fluorouracil (injection) with respect to specific racial populations.
Renal Impairment
There is no FDA guidance on the use of Fluorouracil (injection) in patients with renal impairment.
Hepatic Impairment
There is no FDA guidance on the use of Fluorouracil (injection) in patients with hepatic impairment.
Females of Reproductive Potential and Males
There is no FDA guidance on the use of Fluorouracil (injection) in women of reproductive potentials and males.
Immunocompromised Patients
There is no FDA guidance one the use of Fluorouracil (injection) in patients who are immunocompromised.
Administration and Monitoring
Administration
Oral
Intravenous
Monitoring
There is limited information regarding Monitoring of Fluorouracil (injection) in the drug label.
Description
IV Compatibility
There is limited information regarding IV Compatibility of Fluorouracil (injection) in the drug label.
Overdosage
Acute Overdose
Signs and Symptoms
Description
Management
Description
Chronic Overdose
There is limited information regarding Chronic Overdose of Fluorouracil (injection) in the drug label.
Pharmacology
There is limited information regarding Fluorouracil (injection) Pharmacology in the drug label.
Mechanism of Action
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 a 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 a 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 a more rapid rate.
Structure
ADRUCIL® Injection (fluorouracil injection, USP) an antineoplastic antimetabolite, is a colorless to faint yellow aqueous, sterile, nonpyrogenic injectable solution available in a 50 mL and 100 mL Pharmacy Bulk Package for intravenous administration. Each mL contains 50 mg fluorouracil in water for injection, USP, pH is adjusted to 8.6 to 9.4 with sodium hydroxide.
Chemically, fluorouracil, a fluorinated pyrimidine, is 5-fluoro-2,4 (1H,3H)-pyrimidinedione. It is a white to practically white crystalline powder which is sparingly soluble in water. The structural formula is:
A Pharmacy Bulk Package is a container of a sterile preparation for parenteral use that contains many single doses. The contents are intended for use in a pharmacy admixture program and are restricted to the preparation of admixtures for intravenous infusion.
Pharmacodynamics
There is limited information regarding Pharmacodynamics of Fluorouracil (injection) in the drug label.
Pharmacokinetics
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 to twenty percent of the parent drug is excreted unchanged in the urine in six 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 α-fluoro-ß-alanine) which are inactive. The inactive metabolites are excreted in the urine over the next 3 to 4 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 a range of 8 to 20 minutes, and is dose dependent. No intact drug can be detected in the plasma 3 hours after an intravenous injection.
Nonclinical Toxicology
There is limited information regarding Nonclinical Toxicology of Fluorouracil (injection) in the drug label.
Clinical Studies
There is limited information regarding Clinical Studies of Fluorouracil (injection) in the drug label.
How Supplied
Storage
There is limited information regarding Fluorouracil (injection) Storage in the drug label.
Images
Drug Images
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