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At least 919 records · Page 51Linked to original sources
PubMed1997

Recombinant interferon-alpha2a plus 5-fluorouracil for the treatment of metastatic melanoma.

The therapy of metastatic melanoma is limited by poor responses to known chemotherapeutic agents. The report of Mulder et al. (Proc ASCO 1992; 11: 347) raised the possibility of the known interaction between 5-fluorouracil and interferon-alpha2a improving response rates in melanoma. This study was designed to examine the effects of 5-fluorouracil plus interferon-alpha2a alone without the confounding effects of dacarbazine. Doses were chosen based on the earlier study rather than the higher doses used in colon cancer. Therapy for metastatic melanoma with 5-fluorouracil and interferon-alpha2a is manageable in terms of toxicity. The major toxicities were lethargy, nausea/anorexia and flu-like symptoms. These were thought to be primarily attributable to interferon-alpha2a. Only one case of severe diarrhoea occurred. The response rate of 14% is similar to the reported results of interferon-alpha2a treatment alone. On these data, there is no evidence of synergy using this dose and schedule.

Adult↗
PubMed2005

Needle revision of failed filtering blebs using 5-Fluorouracil and a combined ab-externo and ab-interno approach.

PURPOSE: To evaluate a surgical technique to revise a failed filtering bleb using subconjunctival 5-Fluorouracil with a combined ab-externo and ab-interno approach. PATIENTS AND METHODS: This study is a retrospective review of the outcome of 77 consecutive bleb revisions, with greater than 6-month follow-up, performed by a single glaucoma surgeon (MW). All eyes had previously functioning filtering blebs with currently inadequately controlled intraocular pressures (IOP) prior to the bleb revisions. All surgery was performed in the operating room, using a retrobulbar injection and a microscope. Visco-elastic was injected into the anterior chamber. 5-Fluorouracil (0.1 mL; 50 mg/ml) was infiltrated around the bleb. A 30-gauge needle was used to lyse subconjunctival fibrosis and episcleral scar tissue binding down the scleral flap, and elevate the scleral flap. Through an inferior paracentesis, a cyclodialysis spatula was used to confirm and enlarge the communication with the subconjunctival space. The main outcome measurements were IOP and number of glaucoma medications. A successful outcome was defined as a 20% reduction from baseline IOP and a maximum IOP of 18 mm Hg, with or without medications, and a minimal follow-up of 6 months. RESULTS: 52% of patients achieved success after one revision with an average follow-up of 29.6 +/- 14.4 months. In successful cases, the mean IOP decreased from 22.7 +/- 4.5 mm Hg to 11.3 +/- 3.5 mm Hg and medications were reduced from an average of 2.2 +/- 1.1 to 0.4 +/- 0.7. Kaplan-Meier survival analysis calculated a success of 77% at 1 year, 68% at 2 years, and 58% at 3 years. CONCLUSIONS: In failed filtering blebs, needle revision with 5-Fluorouracil and a combined ab-externo and ab-interno approach results in high success and low complication rates. The outcome of this procedure compares favorably with previously reported revision techniques.

Aged↗
PubMed1981

Differentiation between the genera Mycobacterium, Rhodococcus and Nocardia by susceptibility to 5-fluorouracil.

A test for susceptibility to 5-fluorouracil was useful for differentiating between species of rapidly growing mycobacteria, and for differentiating the genus Rhodococcus from the genus Nocardia. The majority of rhodococci tested were susceptible to 5-fluorouracil (20 micrograms ml-1), whereas the majority of nocardiae tested were resistant to it. Strains of Nocardia asteroides sensu stricto could be divided into two subgroups by their reaction to 5-fluorouracil.

Fluorouracil↗
PubMed1966

Effect of purine and pyrimidine analogues on growth and RNA metabolism in the soybean hypocotyl-the selective action of 5-fluorouracil.

The effects of several base analogues and cycloheximide on RNA synthesis, protein synthesis, and cell elongation were studied in excised soybean hypocotyl. None of the pyrimidine analogues tested affected growth or protein synthesis; only 5-fluorouracil appreciably inhibited RNA synthesis. 8-Azaguanine and 6-methylpurine markedly inhibited RNA and protein synthesis and cell elongation. Cycloheximide effectively inhibited both cell elongation and protein synthesis. The results show that 5-fluorouracil selectively inhibited ribosomal and soluble RNA synthesis without affecting the synthesis of D-RNA. These results indicate that the requirement for RNA synthesis to support continued protein synthesis and cell elongation is restricted to the synthesis of D-RNA.5-Fluorouracil was incorporated into all classes of RNA in a form believed to be 5-fluorouridylic acid. Cycloheximide markedly inhibited the accumulation of ribosomal RNA, but the results indicate that CH did not inhibit, per se, the synthesis of ribosomal RNA. The accumulation of newly synthesized D-RNA was only slightly affected by cycloheximide. These results show that the inhibition of cell elongation by cycloheximide correlates with the inhibition of protein synthesis, but not with the effect on RNA metabolism.

Cycloheximide↗
PubMed1989

Antitumor activity of BOF-A2, a new 5-fluorouracil derivative.

A compound containing both CNDP (3-cyano-2,6-dihydroxypyridine), an inhibitor of 5-fluorouracil (5-FU) degradation, and EM-FU (1-ethoxymethyl-5-fluorouracil), a masked form of 5-FU, was synthesized and named BOF-A2 (3-[3-(6-benzoyloxy-3-cyano-2-pyridyloxycarbonyl)benzoyl]-1-ethoxy methyl-5- fluorouracil). The antitumor activity of BOF-A2 was investigated in sarcoma-180-bearing mice and Yoshida sarcoma-bearing rats. The ED50 (the dose for 50% inhibition) values of BOF-A2 were 25 mg/kg against sarcoma-180 and 15 mg/kg against Yoshida sarcoma. In vitro studies showed that BOF-A2 was rapidly degraded to EM-FU and CNDP in homogenates of the liver and small intestine of mice and rats, and in sera of mice, rats and human, and the conversion of EM-FU to 5-FU occurred only in the microsomal fraction of rat liver in the presence of NADPH. After oral administration of BOF-A2 at 15 mg/kg to Yoshida sarcoma-bearing rats, BOF-A2 was hydrolyzed to EM-FU, CNDP and 5-FU, and their maximum concentrations in the blood were 2000 ng/ml, 300 ng/ml and 40 ng/ml, respectively. Moreover when BOF-A2 was given at the same dose to tumor-bearing mice and rats, the 5-FU levels in the tumor tissue increased much more than those in the blood and persisted for more than 8 h, whereas those in the blood decreased more rapidly. This accumulation and maintenance of a high level of 5-FU in the tumor tissue are concluded to be related to the high antitumor activity of BOF-A2.

Administration, Oral↗
PubMed1976

A sensitive assay of 5-fluorouracil in plasma by gas chromatography-mass spectrometry.

1 A gas chromatographic-mass spectrometric method was developed for determining 5-fluorouracil in plasma, using methylated thymine as an internal standard. 2 5-fluorouracil was extracted from plasma by a novel procedure which removed plasma components interferring with the sensitivity of the assay. The method included heating the plasma, washing with ether and extracting the drug under optimum conditions. 3 The sensitivity of the assay was 10 ng/ml plasma, sufficient to determine the low concentrations of 5-fluorouracil found in plasma during continuous infusion of the drug in patients receiving chemotherapy for cancer.

Chromatography, Gas↗
PubMed1979

Ocular side effects with 5-fluorouracil.

The concentrations of 5-fluorouracil in tears and plasma were studied in eight patients receiving the drug for carcinoma of the colon. The drug was measured by a gas liquid chromatographic method and found to be present only in the tears of patients with excessive lacrimation. In three patients with watery eyes the peak concentration in tears (16-23.8 micrograms/ml) occurred 15 minutes after IV administration and this corresponded with the end of the distribution (alpha) phase in the plasma when the plasma levels ranged from 18-26 micrograms/ml. In five patients without eye symptoms the drug was undetectable in the lacrimal fluid even though they had similar plasma levels (15-25 micrograms/ml) of 5-fluorouracil. The volumes of distribution and plasma clearance rates were similar in the two groups [being 0.2-0.52 (mean = 0.33) 1/kg and 612-978 (mean = 850) ml/min respectively in patients with excessive lacrimation and 0.13-0.79 (mean = 0.36) 1/kg and 435-1138 (mean = 831) ml/min respectively in the five patients without symptoms.]. It appears that 5-fluorouracil produces irritation of the lacrimal apparatus in about 30% of patients on the drug and in association with this appears in the tears where it may be responsible for the reported irritation and fibrosis of the tear duct.

Chromatography, Gas↗
PubMed2005

Double-blind randomised trial comparing 5-fluorouracil plus leucovorin to placebo for metastatic colorectal carcinoma.

OBJECTIVE: Previous randomised trials of chemotherapy for metastatic colorectal cancer have not concealed the allocation of treatment from participants. Most of these unblinded trials showed improved survival with chemotherapy. This trial used a double-blind design to test the hypothesis that there is no difference between the effect of 5-fluorouracil plus leucovorin and the effect of placebo on the survival of subjects with metastatic colorectal cancer. PATIENTS AND METHODS: In one hospital, 147 subjects with metastatic colorectal cancer were studied from 1989 to 2001. 73 were allocated chemotherapy with 5-fluorouracil plus leucovorin. 74 were allocated placebo. The primary end point was survival after randomization. Secondary end points were performance score, quality of life, serum level of carcinoembryonic antigen (CEA) and toxicity of treatment. RESULTS: One hundred and forty-two patients were followed up until death. The median survival time in the chemotherapy group was 8.7 months (95% confidence interval (CI) 6.9-11.0 months) compared to 6.7 months in the placebo group (95% CI 5.3-7.9 months). Chemotherapy did not affect performance status but slowed the rise of CEA and caused appreciable toxicity. CONCLUSIONS: In this double-blind trial, chemotherapy with 5-fluorouracil plus leucovorin did not improve survival, did not impair performance, but caused appreciable toxicity.

Antineoplastic Combined Chemotherapy Protocols↗
PubMed2004

Intralesional 5-fluorouracil, lidocaine and epinephrine mixture for the treatment of verrucae: a prospective placebo-controlled, single-blind randomized study.

BACKGROUND: The treatment of viral warts remains challenging. A variety of treatment modalities have been used with a range of success. Fluorouracil has been shown to be effective in treating warts but the method of its delivery directly onto the affected tissue has been of little efficacy. We evaluated the safety and efficacy of intralesional 5-fluorouracil in the treatment of verrucae. METHODS: Seventy-six patients with a total 315 verrucae were randomized to receive either a 5-fluorouracil, lidocaine and epinephrine (5-FU + LE) mixture or serum saline injection into the paired verrucae in the same patient. The mixture of 5-FU (4 cm(3), 50 mg/mL), lidocaine (1 cm(3), 20 mg/mL) and epinephrine (0.0125 mg/mL) was injected into the base of the wart using a mantoux needle. Each lesion was infiltrated with either of the solutions once a week for up to a maximum of 4 weeks, and the patients were followed up for 6 months. RESULTS: Complete response was noted in an average of 70% of the verrucae treated with the 5-FU + LE mixture and in 29% of those in the placebo group (P < 0.001). No clinically significant systemic and local adverse effects occurred. Pain and burning were noted as an immediate injection pain. Recurrence rates were evaluated and no statistically significant difference between the two groups was found. CONCLUSIONS: The results demonstrate that treatment of verrucae with 5-FU + LE mixture is safe and effective.

Adolescent↗
PubMed1985

Topical 5-fluorouracil in the treatment of vaginal intraepithelial neoplasia.

The effectiveness of 5-fluorouracil (Efudix) in the treatment of vaginal intraepithelial neoplasia was assessed in 14 patients diagnosed with the condition between January 1980 and December 1982. All patients received a standard dose of 2.5 g 5-fluorouracil cream once weekly for at least 10 consecutive weeks; mean duration of treatment was 12 weeks (range 10-20 weeks). The vaginal lesion was associated with a major dysplastic lesion of the cervix in all patients. The duration of follow-up ranged from 4 to 42 months (mean 15 months). Thirteen patients had complete resolution both colposcopically and cytologically. One patient still had colposcopic evidence of intraepithelial neoplasia (aceto-white epithelium) but a vaginal smear has been negative. This patient has since been lost to follow-up. We conclude that in the regimen described 5-fluorouracil is an effective treatment for vaginal intraepithelial neoplasia.

Administration, Topical↗
PubMed2004

Intermittent topical 5-fluorouracil is effective without significant irritation in the treatment of actinic keratoses but prolongs treatment duration.

BACKGROUND: Controversy exists as to whether treatment of actinic keratoses with intermittent doses of topical 5-fluorouracil is effective in the absence of significant irritation. OBJECTIVE: To evaluate the efficacy and degree of irritation of 5-fluorouracil as a function of its application frequency. METHODS: A total of 85 actinic keratoses in 53 patients were treated, initially with four applications per week for the first week. After this first week, if intolerable irritation arose, patients were instructed to reduce application frequency to two times per week for the rest of the treatment period. RESULTS: Treatment was completed for 95.4% of the lesions included, with healing of 88.6% of them. The mean time to healing was 7.4 weeks (with four applications weekly) and 10.2 weeks (with two applications). The healing rate was similar in the two groups. Significant correlations (p<0.001) were observed between application frequency and time to healing. CONCLUSION: Intermittent 5-fluorouracil treatment is effective without causing significant irritation, but time to healing increases with declining application frequency.

Administration, Topical↗
PubMed2004

Combined 5-fluorouracil and Er:YAG laser treatment in a case of recurrent giant keratoacanthoma of the lower leg.

BACKGROUND: Keratoacanthomas are fast-growing squamous tumors, which usually show spontaneous regression. The development of giant variants with an aggressive behavior has been described. Although surgical excision remains the treatment of choice for very large keratoacanthomas, other therapeutic options including laser surgery and topical chemotherapy may be superior in special situations. OBJECTIVE: The objective was to evaluate the efficacy of Er:YAG laser surgery combined with topical 5-fluorouracil treatment in a case of recurrent giant keratoacanthoma. METHODS: A 64-year-old woman presented for evaluation and treatment of recurrent tumors in her face and extremities. Despite repeated invasive surgical removal of these lesions, recurrence of fast-growing giant keratoacanthomas developed in the pretibial region of her left lower leg. Owing to recurrence after conventional surgery and the tumor size, a novel treatment method using ablative Er:YAG laser combined with topical 5-fluorouracil was performed. RESULTS: After four treatments with excellent patient compliance, histologic analysis of punch biopsies revealed tumor-free ulcerations. Complete epithelization was obtained after 9 weeks. Six months after the treatment, no recurrence was observed. CONCLUSION: The combined use of ablative Er:YAG laser and topical 5-fluorouracil chemotherapy may be considered as an effective treatment option in cases of giant keratoacanthoma when conventional surgery is not indicated.

Administration, Cutaneous↗
PubMed1980

Extravascular phagocytosis of proerythrocytes following 5-fluorouracil.

Amongst the perturbations induced in mouse bone marrow by 5-fluorouracil are the retention and phagocytosis of proerythrocytes within the extravascular compartment. Reasons for the latter response have been sought using electron microscopy. Proerythrocytes undergo normal maturation after 5-fluorouracil, judged by loss of mitochondria and vesicles, but fail generally to attain a biconcave shape. Most proerythrocytes have lost their organelles before phagocytosis occurs. Quantitative light microscopy shows a rise in the number of proerythrocytes 1 d after 5-fluorouracil which is attributable to maturation of orthochromatic erythroblasts. Thereafter the population size declines concomitantly with increased engulfment and phagocytosis by macrophages, activity which is maximal on days 4-5. Extravascular loss of proerythrocytes is also observed when marrow is rendered hypocellular by x-irradiation, or hydroxyurea. It is suggested that excessive maturation of proerythrocytes in the extravascular compartment can lead to their phagocytosis.

Animals↗
PubMed1977

Methodological aspects of an agar plate technique for determination of biologically active 5-fluorouracil in blood, urine and bile.

A microbiological agar plate technique for estimation of 5-fluorouracil concentrations in blood, urine and bile from man, dog and pig was evaluated. Different bacterial test strains, media modifications and techniques for inoculation were studied. The strain Streptococcus faecalis ATCC 8043, recommended previously by Clarkson et al., was found to be the most suitable. The influence of prediffusion, dilution, antibiotics and chemotherapeutic agents and their antagonists, as well as the effect of storage of samples containing 5-fluorouracil were examined. A detailed methodological description is presented. The method seems to be sufficiently sensitive and practical for routine determination of cytotoxic compounds from 5-fluorouracil in serum, plasma and urine.

Agar↗
PubMed1966

Morphogenesis in Trichoderma: suppression of photoinduction by 5-fluorouracil.

Sporulation in the fungus Trichoderma viride is inducible with a short light pulse. 5-Fluorouracil applied prior to photoinduction and removed thereafter suppressed sporulation without greatly aflecting growth. This compound also halved the rate of incorporation of uracil-C(14) into RNA but did not change the ratio of uridylic to cytidylic acid. The effect of 5-fluorouracil was counteracted by uracil but not by thymidine. This supports the hypothesis that 5-fluorouracil affects RNA rather than DNA.

Carbon Isotopes↗
PubMed1977

Prevention of 5-fluorouracil-caused growth inhibition in Sordaria fimicola.

Growth (dry weight accumulation) of Sordaria fimicola in standing liquid culture (sucrose-nitrate-salts-vitamins) is inhibited by the presence of 5 muM 5-fluorouracil in the medium. This inhibition is completely prevented by uracil, deoxyuridine, and 5-bromouracil, partly prevented (40 to 90% of growth observed without 5-fluorouracil) by uridine, thymidine, and 5-bromodeoxyuridine, and slightly prevented by trifluorothymine, cytosine, cytidine, deoxycytidine, and 5-methylcytosine (all at 0.5 to 1 mM). Thymidine and thymine riboside were without any apparent effect. Growth is also inhibited by 0.2 mM 6-azauracil, and this inhibition was completely prevented by uracil and uridine, partly prevented by deoxyuridine, 5-bromouracil, cytidine, and 5-methylcytosine, and slightly prevented by thymine, thymidine, 5-bromodeoxyuridine, cytosine, and deoxycytidine. The data suggest that the observed inhibition of growth by 5-fluorouracil is due to inhibition of both ribonucleic acid and deoxyribonucleic acid synthesis. The data also allow inferences concerning pyrimidine interconversions in S. fimicola; i.e., thymine can be anabolized to thymidylic acid without first being demethylated, although demethylation appears to occur also.

Ascomycota↗
PubMed1967

Postirradiation cell division in 5-fluorouracil-pre-treated Escherichia coli.

The correlation between 5-fluorouracil-induced resistance to ultraviolet (UV) light and the ability of bacterial cells to repair irradiation damage was investigated in various strains of Escherichia coli. Preincubation with 5-fluorouracil did not influence the dark-repair mechanism. It affected, however, the UV light-induced damage of cell division in filament-forming strains. It is suggested that the delay in postirradiation macromolecular synthesis of 5-fluorouracil-pretreated bacteria plays a decisive role in the recovery process leading to cross cell wall-forming ability in the damaged strains.

Cell Division↗
PubMed1993

Preoperative irradiation and fluorouracil chemotherapy for locally advanced rectosigmoid carcinoma: phase I-II study.

From June 1988 to July 1991, 20 patients with locally advanced rectal or rectosigmoid cancer were treated prospectively with a strategy of combining preoperative irradiation and fluorouracil chemotherapy before surgical resection. The preoperative radiation dose was 5,000 cGy, and fluorouracil chemotherapy was administered on the first and last 3 days of irradiation in an intravenous bolus dose of 500 mg/m2. In a median follow-up of 25 months, the local regional failure rate was 10%. The 3-year actuarial overall survival and disease-free survival were 92% and 82%, respectively. Twenty percent of the surgical specimens showed no residual tumor, and only 10% showed positive lymph nodes. Significant leukopenia occurred in 10% of patients. Preoperative irradiation and fluorouracil chemotherapy increased surgical downstaging and improved local regional control. The overall toxicity was acceptable. The results of this particular multimodality approach was encouraging and warrant further investigation in phase III trials.

Adult↗