Adrucil

Name: Adrucil

Fluorouracil Dosage

Fluorouracil is injected into a vein through an IV. A healthcare provider will give you this injection.

Your first dose of fluorouracil will be given in a hospital setting where you can be closely watched in case the medication causes serious side effects.

Fluorouracil injections are usually given daily for 3 or 4 days in a row, and then every other day for another 3 or 4 days. This treatment cycle may be repeated once a month. You may also receive a weekly dose. Follow your doctor's instructions.

How often you need fluorouracil injections will depend on many factors, including side effects and how your body responds to the medication. Try not to miss any appointments for your fluorouracil injections.

Fluorouracil can lower blood cells that help your body fight infections and help your blood to clot. Your blood will need to be tested often. Your cancer treatments may be delayed based on the results of these tests.

Tell your caregivers if you feel any burning, pain, or swelling around the IV needle when the medicine is injected.

Since this medication is given by a healthcare professional in a medical setting, an overdose is unlikely to occur.

Contact your doctor if you miss an appointment for your fluorouracil injection.

Adrucil Overview

Fluorouracil injectable is a prescription medication used to treat certain types of cancer. Fluorouracil is in a class of medications called antimetabolites. It works by slowing or stopping the growth of cancer cells in your body.

Fluorouracil cream and topical solution are prescription medications used to treat a skin condition on the face and front part of the scalp known as actinic keratosis (also called solar keratosis). Actinic keratosis is a precancerous condition marked by scaly, crusty patches of skin. It is caused by long term exposure to the sun. Fluorouracil (Efudex) 5% strength topical formulation is also useful in the treatment of superficial basal cell carcinomas. This is a slow-growing form of skin cancer.

Fluorouracil is in a class of drugs known as antimetabolites. It interferes with DNA and RNA production, causing fast-growing cells (like cancer cells or cells in actinic keratoses) to die.

This medication is available in an injectable form to be given directly into a vein (IV) by a healthcare professional.

This medication is also available as a cream and topical solution that are applied directly to the affected areas of the skin. It is usually used once a day for 2 to 4 weeks.

Common side effects of fluorouracil injectable include inflammation of the mouth, nausea, vomiting, diarrhea, and loss of appetite.

Common side effects of fluorouracil cream and topical solution include skin and eye irritation.

Adrucil Dosage

Injectable:

  • The starting dose is typically 12 mg/kg are given intravenously (into the vein) once daily for 4 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.
  • 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.
    • When toxic effects from the first course of therapy have subsided, maintenance dosage of 10 to 15 mg/kg/week as a single dose is recommended. Do not exceed 1 gram per week.
  • Dose and duration of use may be adjusted if you are in poorer health or if you experience certain toxic side effects.

Topical:

  • Cream
    • Refer to your specific cream product and your doctor's prescribed directions for use. There are different cream formulations with different directions.
  • Topical solution
    • Apply topical solution twice daily in an amount sufficient to cover the lesions.
    • The usual duration of therapy is from 2 to 4 weeks if treating for actinic or solar keratoses.
    • The usual duration of therapy is from 3 to 6 weeks if treating for basal cell carcinoma. Therapy may be required for as long as 10 to 12 weeks.

Adrucil FDA Warning

It is recommended that fluorouracil 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 fluorouracil.

Adrucil Pharmacokinetics

Distribution

Extent

Distributed into tumors, intestinal mucosa, bone marrow, liver, and other tissues.205 a

Readily crosses the blood-brain barrier (despite limited lipid solubility), and distributes into CSF and brain tissue.205 a

Usually higher concentration of fluorouracil or metabolites in tumor than in surrounding tissue or in corresponding normal tissue, and persists longer in some tumors than in the normal host tissues, perhaps due to impaired uracil catabolism; suggests some tumor specificity.a

Crosses the placenta in rats.205 Not known whether fluorouracil is distributed into human milk.205

Elimination

Metabolism

A small portion is anabolized in tissues to 5-fluoro-2′-deoxyuridine, then to active metabolite (5-fluoro-2′-deoxyuridine-5′-monophosphate).a

The major portion is degraded in the liver, to inactive metabolites (e.g., CO2, urea, α-fluoro-β-alanine, α-fluoro-β-guanidopropionic acid, and α-fluoro-β-ureidopropionic acid).a

Elimination Route

7–20% is excreted unchanged in urine within 6 hours; >90% of this in the 1st hour.a 205

Inactive metabolites are excreted as respiratory CO2 and (in urine) as urea, α-fluoro-β-alanine, α-fluoro-β-guanidopropionic acid, and α-fluoro-β-ureidopropionic acid.a

Half-life

About 16 minutes (range: 8–20 minutes) and is dose dependent; no intact drug is detected in plasma after 3 hours.205 a

Advice to Patients

  • Advise patients about expected toxic effects, especially oral manifestations.205 a

  • Advise patients that alopecia is possible, but usually transient.205

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs as well as any concomitant illnesses.205 a

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.205 a

  • Importance of informing patients of other important precautionary information. 205 (See Cautions.)

Commonly used brand name(s)

In the U.S.

  • Adrucil

Available Dosage Forms:

  • Injectable
  • Solution

Therapeutic Class: Antineoplastic Agent

Pharmacologic Class: Antimetabolite

Precautions While Using Adrucil

It is very important that your doctor check your progress at regular visits to make sure that this medicine is working properly and to check for unwanted effects.

While you are being treated with fluorouracil, and after you stop treatment with it, do not have any immunizations (vaccinations) without your doctor's approval. Fluorouracil may lower your body's resistance and there is a chance you might get the infection the immunization is meant to prevent. In addition, other persons living in your household should not take oral polio vaccine since there is a chance they could pass the polio virus on to you. Also, avoid persons who have taken oral polio vaccine within the last several months. Do not get close to them and do not stay in the same room with them for very long. If you cannot take these precautions, you should consider wearing a protective face mask that covers the nose and mouth.

Fluorouracil can temporarily lower the number of white blood cells in your blood, increasing the chance of getting an infection. It can also lower the number of platelets, which are necessary for proper blood clotting. If this occurs, there are certain precautions you can take, especially when your blood count is low, to reduce the risk of infection or bleeding:

  • If you can, avoid people with infections. Check with your doctor immediately if you think you are getting an infection or if you get a fever or chills, cough or hoarseness, lower back or side pain, or painful or difficult urination.
  • Check with your doctor immediately if you notice any unusual bleeding or bruising; black, tarry stools; blood in urine or stools; or pinpoint red spots on your skin.
  • Be careful when using a regular toothbrush, dental floss, or toothpick. Your medical doctor, dentist, or nurse may recommend other ways to clean your teeth and gums. Check with your medical doctor before having any dental work done.
  • Do not touch your eyes or the inside of your nose unless you have just washed your hands and have not touched anything else in the meantime.
  • Be careful not to cut yourself when you are using sharp objects such as a safety razor or fingernail or toenail cutters.
  • Avoid contact sports or other situations where bruising or injury could occur.

What do I need to tell my doctor BEFORE I take Adrucil?

  • If you have an allergy to fluorouracil or any other part of Adrucil (fluorouracil (systemic)).
  • If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.
  • If you have any of these health problems: An infection, low blood cell counts, or poor diet.
  • If you are breast-feeding. Do not breast-feed while you take this medicine.

This is not a list of all drugs or health problems that interact with Adrucil.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take this medicine with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

Dosage Forms and Strengths

Adrucil (fluorouracil injection USP) is supplied as:

• a single-dose vial containing 500 mg/10 mL (50 mg/mL) fluorouracil

Overdosage

Administer uridine triacetate within 96 hours following the end of fluorouracil infusion for management of fluorouracil overdose.

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

Carcinogenicity studies have not been performed with fluorouracil. Fluorouracil was mutagenic in vitro in the bacterial reverse mutation (Ames) assay and induced chromosomal aberrations in hamster fibroblasts in vitro and in mouse bone marrow in the in vivo mouse micronucleus assay.

Administration of fluorouracil intraperitoneally to male rats at dose levels equal to or greater than 1.7-fold the human dose of 12 mg/kg induced chromosomal aberrations in spermatogonia and inhibition of spermatogonia differentiation resulting in transient infertility. In female rats, intraperitoneal administration of fluorouracil during the pre-ovulatory phases of oogenesis at dose levels equal to or greater than 0.33 times a human dose of 12 mg/kg resulted in decreased incidence of fertile matings, increased pre-implantation loss, and fetotoxicity.

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