5-fluorouracil [5-FU] (Fluoroplex, Efudex, Adrucel, Carac)
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Introduction
Topical: Tradenames: Fluoroplex, Efudex.
Indications
- topical
- multiple actinic keratosis
- superficial basal cell carcinoma
- prevention of squamous cell carcinoma skin in high-risk patients[9]
- condyloma accuminata
- verruca plana
- leukoplakia[7]
- actinic cheilitis[7]
- radiodermatitis[7]
- systemic chemotherapy for malignancy (Adrucel)
Dosage
Administration:
- topical
Cream: 1% (Fluoroplex), 5% (Efudex)
Solution: 1% (Fluroplex), 2% (Efudex), 5% (Efudex), 10 mL.
Pharmacokinetics
- widely distributed
- penetrates into CSF
- metabolized in liver
- eliminated in urine
- 1/2life is 10-15 minutes
Typical response (topical)
- erythema followed by scaling, tenderness, vesiculation, erosion, ulceration, necrosis, re-epithelialization
- therapy is continued until the erosion, ulceration, necrosis phase is reached
- normal skin should show little response to 5-FU
- initial combination therapy with tretinoin may be indicated
- complete healing may take 1-2 months & may be hastened by application of topical glucocorticoid after 5-FU has bee discontinued
elimination via liver
1/2life = 10-15 minutes
Adverse effects
- topical:
- no systemic toxicity reported
- one manufacturer lists leukopenia & thrombocytopenia
- local pain
- pruritus
- irritation
- photosensitivity
- systemic
- common (> 10%)
- not common (1-10%)
- uncommon (< 1%)
- shortness of breath, ataxia, paresthesias, cardiac arrhythmias, heart failure, hypotension, headache, hyperpigmentation of the skin, pruritic maculopapular rash, partial loss of fingernails &/or toenails, hyperpigmentation of fingernail &/or toenail bed, myelosuppression, hepatotoxicity, visual disturbances, photosensitivity
- other[3]
- severe reaction in patients with DPYD deficiency
- stomatitis, leukopenia, thrombocytopenia, hair loss, diarrhea, fever, marked weight loss, cerebellar ataxia, neurologic symptoms, progressing to semicoma
- heart failure (rare) from myocardial infarction during treatment[6]
- pseudo-porphyria cutanea tarda[6]
- cutaneous lupus erythematosus[6]
- hand-&-foot syndrome
- excessive lacrimation
- hyperpigmentation of palms[10] (image)
- severe reaction in patients with DPYD deficiency
- topical 5FU may be lethal if consumed by dog[8]
Drug interactions
Laboratory
Mechanism of action
- antimetabolite; inhibits thymidylate synthase
- interferes with DNA synthesis
- S-phase specific
Mechanism of drug resistance:
- increased activity of target enzyme thymidylate synthase
- alteration in target enzyme thymidylate synthase
More general terms
Additional terms
Component of
- 5 fluorouracil/salicylic acid
- 5 fluorouracil/diclofenac
- 5-fluorouracil/irinotecan/leucovorin/oxaliplatin (FOLFIRINOX)
- cyclophosphamide/methotrexate/5-fluorouracil (CMF)
- cyclophosphamide/doxorubicin (Adriamycin)/5-fluorouracil (CAF)
- cyclophosphamide/epirubicin/fluorouracil (CEF, FEC-100)
- 5-fluorouracil/oxaliplatin/leucovorin (FOLFOX)
References
- ↑ AHFS Drug Information, American Society of Health-System Pharmacists, Bethesda, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ 3.0 3.1 Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998 Department of Veterans Affairs, VA National Formulary
- ↑ Harrison's Principles of Internal Medicine, 14th ed. Fauci et al (eds), McGraw-Hill Inc. NY, 1998, pg 529, 533
- ↑ 5.0 5.1 ARUP Consult: 5-Fluorouracil Sensitivity deprecated reference
- ↑ 6.0 6.1 6.2 6.3 6.4 Medical Knowledge Self Assessment Program (MKSAP) 16, 17, 18. American College of Physicians, Philadelphia 2012, 2015, 2018
- ↑ 7.0 7.1 7.2 7.3 7.4 7.5 Deprecated Reference
- ↑ 8.0 8.1 FDA Animal & Veterinary Update. Jan 18, 2017 FDA Warns of Illnesses and Deaths in Pets Exposed to Prescription topical (human) cancer treatment: Fluorouracil; http://www.fda.gov/animalveterinary/newsevents/cvmupdates/ucm537434.htm
- ↑ 9.0 9.1 Harrison P 5-FU Cream Reduces Surgery in High-Risk SCC Patients Medscape - Jan 08, 2018. https://www.medscape.com/viewarticle/891047
- ↑ 10.0 10.1 Schaefer JK, Ramnath N Fluorouracil-Induced Hyperpigmentation N Engl J Med 2020; 382:e6. Jan 23 PMID: https://www.ncbi.nlm.nih.gov/pubmed/31971682 https://www.nejm.org/doi/full/10.1056/NEJMicm1909329