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PubMed2002

Needling revision with subconjunctival 5-fluorouracil in failing filtering blebs.

BACKGROUND: 5-Fluorouracil, an antimetabolic agent, improves the success rate of trabeculectomies by inhibiting subconjunctival fibrosis. However, complications may be associated with early postoperative use. We investigated the outcome of needling revision with delayed subconjunctival 5-fluorouracil in failing filtering blebs after a trabeculectomy in patients with medically poorly controlled glaucoma. METHODS: We performed needling revision with subconjunctival 5-fluorouracil injection 5.0 +/- 4.0 weeks after trabeculectomy with failing filtering blebs in 25 eyes of 24 patients. The diagnoses of these patients were primary angle-closure glaucoma (4), primary open-angle glaucoma (4), post-cornea-graft glaucoma (8), traumatic glaucoma (5), neovascular glaucoma (3) and pseudophakic glaucoma (1). RESULTS: Total success was achieved in 21 eyes (84%) including complete success in 10 (40%) and qualified success in 11 (44%) after 3.2 +/- 1.2 needling revisions over an average 8.3 +/- 7.0-month follow-up period from the last needling revision. The mean intraocular pressure was 16.0 +/- 8.4 mmHg in the last visit compared with 26.0 +/- 8.1 mmHg before the procedure. Major complications were transient hypotony (1), transient corneal epithelial defect (13) and hyphema (3). CONCLUSIONS: This study supports the efficacy and safety of the delayed use of 5-fluorouracil with needling revision for managing failing filtering blebs following a trabeculectomy.

Adult↗
PubMed2002

[Changes of the heart conduction system after exposure to fluorouracil].

Using 20 male rats the electron microscopic study of conducting system of the heart was performed to assess the effect of fluorouracil--an antineoplastic drug belonging to antimetabolite group. A daily dose of 15 mg/kg of fluorouracil was injected intraperitoneally for 5 days; three courses of injections with the intervals of three weeks were performed. Toxic effect of fluorouracil is demonstrated after the first course of injections and is revealed as a predominant injury of pacemaker cells in sinoatrial and atrioventricular nodes. Latent pacemaker myocytes and Purkinje fibers undergo "calcium injury" during the second and the third courses of fluorouracil injections. The irreversible damage of contractile and specialized myocytes results in fibrosis which develops predominantly in the areas of atrioventricular bundle and its branches.

Animals↗
PubMed2002

Effective treatment of actinic keratosis with 0.5% fluorouracil cream for 1, 2, or 4 weeks.

New therapeutic options would benefit patients with actinic keratosis (AK), a precancerous condition that is a significant health concern. The efficacy and safety of a microsphere-based formulation of 0.5% fluorouracil cream were evaluated in a randomized, double-blind, multicenter, parallel-group study. Patients (N= 177) were randomized to receive 0.5% fluorouracil or vehicle once daily for 1, 2, or 4 weeks. Efficacy was assessed by lesion counts and clearance. Safety was evaluated by monitoring adverse events, including facial irritation. Significant improvements were seen from baseline to posttreatment follow-up in all efficacy variables for all fluorouracil regimens compared with vehicle. Patients treated for one week experienced significant improvements compared with vehicle, although efficacy increased with increasing treatment duration. Most patients experienced mild to moderate facial irritation of predictable onset and duration. Once-daily administration of 0.5% fluorouracil cream for 1, 2, or 4 weeks is safe and effective for the treatment of AKs.

Administration, Topical↗
PubMedDate not supplied

Weekly paclitaxel and 5-fluorouracil in pretreated patients with metastatic breast cancer: a phase I study.

BACKGROUND: Recent studies have shown a good activity/tolerability for weekly paclitaxel and 5-fluorouracil in protracted continuous infusion (p.c.i.) in metastatic breast cancer patients pretreated with anthracyclines. MATERIALS AND METHODS: To define the MTD of weekly paclitaxel (days 1-8-15-22, every 4 weeks with a starting dose of 75 mg/m2 and subsequent dose escalation: 90 mg/m2 and 105 mg/m2) in combination with a fixed dose of 5-fluorouracil in p.c.i. (250 mg/m2/day for 3 weeks + 1 week of rest). RESULTS: Eleven patients were enrolled; on Step III two patients experienced DLT (1 G 3 mucositis and 1 febrile neutropenia). G 3-4 toxicities were: G 3 mucositis (2 out of 11), G 3-4 neutropenia (1 out of 11). CONCLUSION: The recommended schedule for phase II studies is: paclitaxel 90 mg/m2/w + 5-fluorouracil 250 mg/m2 in p.c.i. for 21 days. This is the first phase I trial with the combination of weekly paclitaxel and 5-fluorouracil p.c.i. in advanced breast cancer patients.

Aged↗
PubMedDate not supplied

Topical treatment of actinic keratosis with fluorouracil: is irritation associated with efficacy?

Actinic keratoses (AKs) are common dysplastic epidermal lesions that share clinical, histologic, and molecular features with squamous cell carcinoma. Therapeutic options include destructive modalities (i.e., cryosurgery, curettage) or topical fluorouracil treatment. The efficacy of topical fluorouracil for the treatment of widespread AK lesions has been demonstrated in multiple studies, but treatment is often associated with significant skin irritation. Various approaches to decrease irritation while maintaining efficacy have been attempted, including altered treatment regimens, combination therapies, and variations in vehicle formulations. Recently, a novel topical fluorouracil cream that contains 0.5% 5-fluorouracil in a microsphere vehicle has been approved for the treatment of AK. Data demonstrate that this low-dose formulation is effective in reducing AK lesions while maintaining a tolerable irritation profile.

Administration, Cutaneous↗
PubMed2004

[Case report of two colorectal cancer patients with liver metastasis showing favorable response to fluorouracil and l-leucovorin therapy].

We treated 2 patients with colorectal cancer accompanied by liver metastasis who showed favorable response to combined treatment with fluorouracil and l-Leucovorin. Case 1 was a 40-year-old man with rectal carcinoma (moderately differentiated adenocarcinoma; se, n1, p1, H0, stage IV). He underwent low anterior resection of the rectum and postoperatively showed an increase peritoneal dissemination and liver metastasis. The patient was given 600 mg/m2 fluorouracil and 250 mg/m2 l-Leucovorin concomitantly for 7 courses. At course 3, the liver metastasis showed partial response and, during the 18 months after the 7th course, his peritoneal dissemination and other lesions were well controlled. As of 30 months post-treatment the patient was alive. Case 2 was a 60-year-old man with rectal carcinoma (well differentiated adenocarcinoma; ss, n1, p0, H1, stage IV). He underwent low anterior resection and postoperatively was given 3 courses of fluorouracil and l-Leucovorin. At course 2, he showed complete response, and, at present 8 months after the 2 courses, the patient continues to show complete response. Adverse drug reactions in both patients were controlled on an outpatient basis. While in the past liver metastasis has been treated by hepatic arterial infusion chemotherapy, a combination therapy with fluorouracil and l-Leucovorin can be used on an outpatient basis and results in a favorable response. This suggests that this combination therapy has clinical significance.

Adenocarcinoma↗
PubMed2004

[Drug distribution in gastric cancer and adjacent tissues by preoperative intraperitoneal chemotherapy with Co-fluorouracil liposome].

OBJECTIVE: To examine the distribution of fluorouracil in gastric cancer (CA), lymph node (LN), normal gastric mucosa (NG), peritoneum (PE), greater omentum (GO) and lesser omentum (LO) by preoperative intraperitoneal chemotherapy with Co-fluorouracil liposome (Co 5-Fu), and offer an experimental basis for clinic practice. METHODS: Ninety-six gastric cancer patients were divided into four groups: Co 5-Fu i.v. injection group (Co 5-Fu i.v.), Co 5-Fu intraperitoneal perfusion group (Co 5-Fu i.p.), 5-Fu i.v. injection group (5-Fu i.v.) and intraperitoneal perfusion group (5-Fu i.p.) given on day-2, day-1 and 60 minutes before operation. Fluorouracil concentration in all tissues collected during operation were examined by high performance liquid chromatography (HPLC). RESULTS: The fluorouracil concentration in the tissues in Co 5-Fu i.p. group was significantly higher than that in Co 5-Fu i.v. or 5-Fu i.p. group (P < 0.05 or P < 0.01), and that in 5-Fu i.p. group was greatly higher than that at 5-Fu i.v. group (P < 0.01). In Co 5-Fu i.p. group, the concentration of drug in LN, CA, PE, NG, GO and LO decreased gradually with the former 3 tissues significantly higher than the latter 3 tissues (P < 0.01), and adjacent lymph node was the highest. In Co 5-Fu i.v. group, the ranking was LN, CA, NG, PE, GO and LO with the former 3 tissues significantly higher than the latter 3 tissues (P < 0.01) and showing tumor tissues higher than the other tissues (P < 0.01). In 5-Fu i.p. group, the ranking was PE, LN, CA, NG, GO and LO with the former 2 tissues significantly higher than the latter tissues (P < 0.01). CONCLUSION: Co 5-Fu possesses drug targeting, slow release and long effect in gastric cancer tissues and adjacent lymph nodes. Preoperative chemotherapy with Co 5-Fu i.p. is more advantageous than 5-Fu given i.v. or 5-Fu i.p.

Aged↗
PubMed2004

Fluorouracil 5% and 0.5% creams for the treatment of actinic keratosis: equivalent efficacy with a lower concentration and more convenient dosing schedule.

Several formulations and concentrations of topical fluorouracil have received US Food and Drug Administration (FDA) approval for the treatment of actinic keratosis (AK). The most commonly used are the fluorouracil 5% and 0.5% creams. In clinical trials, these formulations have demonstrated a marked ability to partially and completely eradicate AK lesions. Application site irritation, erythema, and burning are common side effects of both formulations, but comparative data suggest that the fluorouracil 0.5% cream is more cost-effective and may be safer, more tolerable, and as efficacious as fluorouracil 5% cream.

Administration, Cutaneous↗
PubMed1992

Stability of fluorouracil, cytarabine, or doxorubicin hydrochloride in ethylene vinylacetate portable infusion-pump reservoirs.

The stability of fluorouracil, cytarabine, and doxorubicin hydrochloride in admixtures stored in portable infusion-pump reservoirs was investigated. Admixtures containing fluorouracil 50 or 10 mg/mL, cytarabine 25 or 1.25 mg/mL, or doxorubicin hydrochloride 1.25 or 0.5 mg/mL in 0.9% sodium chloride injection or 5% dextrose injection were placed in 80-mL ethylene vinylacetate drug reservoirs protected from light, and 1-mL quantities were withdrawn immediately after preparation and after storage for 1, 2, 3, 4, 7, 14, and 28 days at 4, 22, or 35 degrees C. For each condition, three samples from each admixture were tested for drug concentration by stability-indicating high-performance liquid chromatography. The admixtures were also monitored for precipitation, color change, and pH. Evaporative water loss from the containers was measured. Fluorouracil was stable at all temperatures for 28 days. Cytarabine was stable for 28 days at 4 and 22 degrees C and for 7 days at 35 degrees C. Doxorubicin hydrochloride was stable for 14 days at 4 and 22 degrees C and for 7 days at 35 degrees C. No color change or precipitation was observed, and pH values were stable. Loss of water through the reservoirs was substantial only at 35 degrees C for 28 days. When stored in ethylene vinylacetate portable infusion-pump reservoirs, fluorouracil, cytarabine, and doxorubicin hydrochloride were each stable for at least one week at temperatures up to 35 degrees C. Cytarabine and doxorubicin hydrochloride showed decreasing stability at longer storage times and higher temperatures.

Cytarabine↗
PubMed2005

Activity and toxicity of oxaliplatin and bolus fluorouracil plus leucovorin in pretreated colorectal cancer patients: a phase II study.

The aim of the current study was to evaluate the activity and toxicity of a combination of oxaliplatin with bolus fluorouracil and leucovorin in colorectal cancer (CRC) patients pretreated for advanced disease with various schedules including continuous fluorouracil infusion. Thirty consecutive patients with pretreated advanced CRC received oxaliplatin 130 mg/m2 by 2-h infusion dl, leucovorin 100 mg/m2 by 1-h infusion followed by fluorouracil 425 mg/m2 i.v. bolus from day 1 to 3 every 3 weeks for a maximum of 6 cycles. The best overall response rate in an intent-to-treat analysis was 13% (2 complete responses and 2 partial responses) (95% CI, 1.2-25.5%) and 37% of patients obtained stable disease with a tumor growth control rate of 50% (95% CI, 32.1-67.9%). The median progression-free survival was 4.0 months (95% CI, 1.4-6.5 months) and median overall survival was 12.0 months (95% CI, 9.9-14.1 months). The independent prognostic factors for improved overall survival were a good performance status and a response/stabilization of disease to chemotherapy. Severe neutropenia was quite common (43.3% of patients and 14.4% of cycles), although complicated by fever only in one case (3.3% of patients). There was one toxic death. In conclusion, the study combination showed an interesting rate of tumor growth control in a cohort of patients previously treated for advanced disease with various schedules including continuous fluorouracil infusion.

Adult↗
PubMedDate not supplied

[The trypanocidal action of fluorouracil on Crithidia oncopelti in the presence of lipid metabolic modifiers].

Effect of fluorouracil in combination with ascorbate and L-valin, modifiers of lipid metabolism was studied in cultured protozoa Crithidia oncopelti. The inhibitory effect of preparation in a concentration of 100 mcg/ml gradually decreased in the course of cultivation. Its readdition to a 96-hour culture did not increase its effect on protozoa cells. Combined addition of fluorouracil and modifiers (100 mcg/ml each) resulted in insignificant decrease of the cell accumulation in the culture as compared with the effect of fluorouracil alone. When fluorouracil and modifiers were readded to the 96-hour culture, the trypanostatic effect of preparation was 2.5 times enhanced. This enhancement was confirmed by destructive alterations in cell morphology and by the culture lysis by 192 h of protozoa cultivation.

Animals↗
PubMed1991

In vivo measurements of intratumoral metabolism, modulation, and pharmacokinetics of 5-fluorouracil, using 19F nuclear magnetic resonance spectroscopy.

In vivo 19F nuclear magnetic resonance spectroscopy was used to monitor and measure 5-fluorouracil and some of its cytotoxic anabolites directly in rats bearing the Walker 256 adenocarcinoma by using a 4.7-T horizontal bore magnet. A two-compartment subsystem model was used to estimate intratumoral transfer parameters. The apparent rate of formation of the nucleosides/tides in the tumor, K21, changed following methotrexate pretreatment, from a value of 6.4 +/- 2.4 to 15.5 +/- 5.0. These values were statistically significant to P less than 0.01. This 2-compartment model was validated by excising the tumors and measuring the 19F content of the acid soluble and the RNA fractions. The increase of the mean K21 value (2.4) estimated in vivo correlated favorably with the increase of the levels of the fluorinated nucleosides/nucleotides (2.2) observed by in vitro analysis. The in vitro measurements also revealed that the increase in the fluorinated nucleosides was accompanied with a similar increase in 5-fluorouracil incorporation into the RNA fraction, which suggests that increases or decreases in the relative intensity of the fluorinated nucleoside/nucleotide signals observed in vivo could be indicative of similar changes of the nuclear magnetic resonance invisible fluorinated RNA. The present study documents that it is now possible to estimate the pharmacokinetic behavior of 5-fluorouracil and of its active metabolites at its target site, tumor tissue, by using noninvasive measurements. Such measurements may provide useful means of assessing, during treatment, the possible effect of 5-fluorouracil on the tumor, and its response to treatment, both when used by itself as well as a function of biochemical modulation.

Animals↗
PubMed1986

The cytotoxicity of 5-fluorouracil is due to its incorporation into RNA not its inhibition of thymidylate synthase as evidenced by the use of a mouse cell mutant deficient in thymidylate synthase.

The biochemical basis for the cytotoxicity of 5-fluorouracil is still controversial; it is not clear whether the mechanism involves interference with DNA metabolism or incorporation of the drug into RNA. To distinguish between these two possibilities, we took advantage of a mutant strain of the mouse mammary tumor cell line FM3A that is deficient in thymidylate synthase, which is widely believed to be the target of 5-fluorouracil. We demonstrated that the target of the cytotoxicity of 5-fluorouracil was not thymidylate synthase; instead, the cytotoxicity was positively correlated with drug incorporation into RNA under conditions where thymidine increased the incorporation of 5-fluorouracil into RNA concentration-dependently.

Animals↗
PubMed1988

[Elaboration of the combination of antitumor preparations bleomycetin + 5-fluorouracil + cisplatin].

Clinical trials on efficacy and toxicity of combined use of bleomycetin, 5-fluorouracil and cisplatin in patients with disseminated tumor processes were conducted. Two regimens were applied. Regimen I included intravenous administration of cisplatin in a dose of 100-150 mg/m2 on day 1, intramuscular administration of bleomycetin in a dose of 10 mg on days 2-4 and intravenous jet injection of 5-fluorouracil in a dose of 400 mg/m2 on days 2-4. Regimen II consisted of intramuscular administration of bleomycetin in a dose of 10 mg on days 1-3, intravenous jet injection of 5-fluorouracil in a dose of 400 mg/m2 on the same days and intravenous administration of cisplatin in a dose of 100-150 mg/m2 on day 4. The intervals between the courses amounted to 4 weeks. Complete regression of cervical carcinoma relapsing was observed in 1 patient. In 5 patients i.e. 1 with small-cell lung cancer, 3 with squamous cell lung cancer and 1 with metastases of low-differentiated cancer from an undetected focus to supraclavicular lymph nodes the effect was partial. Long-term stabilization of the disease at the background of the treatment for 6-7 months was stated in 3 patients. On the whole the objective response was in 6 out of 22 patients or in 27 per cent. 7 of them were treated with cisplatin in a dose of 150 mg/m2. The regimens of the combined use of 5-fluorouracil, bleomycetin and cisplatin were low toxic. The therapeutic effect showed that the combination was of practical value.

Antineoplastic Combined Chemotherapy Protocols↗
PubMed1989

Phase I and II studies of the combination of recombinant human interferon-gamma and 5-fluorouracil in patients with advanced colorectal carcinoma.

Based on the in vitro and in vivo data suggesting synergistic cytolysis by the combination of 5-fluorouracil and interferon-gamma against a variety of malignant cell lines including a human colon carcinoma cell line (HT-29), we initiated studies in patients with advanced colon or rectal carcinoma. Forty-six patients received 5-fluorouracil as an intravenous injection on days 1-5 and recombinant human interferon-gamma as an intramuscular injection on days 1-14, followed by a rest period of 14 days; courses were repeated every 28 days. In the phase I study, cohorts of two patients received a stepwise dose level increase to achieve the maximum tolerated dose (MTD), at which a total of six patients were studied. The dose levels constituting the MTD were as follows: 5-fluorouracil (500 g/m2/day) and recombinant gamma-interferon (0.5 mg/m2/day). Four patients achieved a partial response in the phase I study. In the phase II study, 30 patients received therapy at the MTD. Among 29 evaluable patients in the phase II study, two patients achieved a partial response. Common toxicities included malaise, fever, anorexia, nausea and vomiting, and diarrhea. Transient severe myelosuppression was common but did not result in significant morbidity. Our data suggest that the combination of 5-fluorouracil and recombinant gamma-interferon did not have the same antitumor effect in patients as it had in the preclinical experiments.

Adenocarcinoma↗
PubMed1989

[The development of myocardial infarct in a patient treated with 5-fluorouracil].

The authors describe the first case of myocardial infarction in their department which occurred during 5-fluorouracil treatment. In a 37 year-old patient two years before the infarction an epidermoid carcinoma of the lower lip was found. The patient was subjected to operation and radiotherapy. Because of a relapse of the process after one year the patient was re-operated with subsequent chemotherapy (vincristine, methotrexate, cis-platinum). Because the effect was not satisfactory, after another year 5-fluorouracil treatment was started (i.v. infusion of 3000 mg in two days). In the course of the infusion the patient developed the clinical picture of a non-transmural infarction of the anterior wall. The course was uncomplicated. The ECG returned to normal on the 9th day after discontinuation of 5-fluorouracil treatment. The effect of 5-fluorouracil on the heart is explained by a coronary vascular spasm. The authors recommend therefore administration of calcium blockers.

Adult↗
PubMed1987

5-Fluorouracil augmentation of dihydrofolate reductase RNA containing contiguous exon and intron sequences in KB7B cells.

Quantitative S1 nuclease mapping studies were performed with uniformly labeled RNA probes, containing contiguous dihydrofolate reductase exon and intron sequences, and total RNA isolated from KB7B cells exposed to 5-fluorouracil for 5 days. Dihydrofolate reductase RNA containing both exon 1 and intron I, or exon 5 and a portion of intron V, increased up to 5-fold in cells grown in the presence of 2.0 to 3.0 microM 5-fluorouracil. Dihydrofolate reductase RNA containing exon 1 or exon 5, but lacking intron I or intron V, respectively, increased 2-fold in cells grown in the presence of 0.65 to 3.0 microM 5-fluorouracil. Primer extension analysis and S1 mapping studies revealed two major transcriptional start sites at positions -72 and -69 and minor start sites upstream from position -183, for dihydrofolate reductase RNA isolated from methotrexate-resistant KB7B cells. The results of these studies demonstrate that 5-fluorouracil alters the metabolism of dihydrofolate reductase precursor mRNA and/or processing intermediates.

Endonucleases↗
PubMed1988

Viability of microorganisms in fluorouracil and cisplatin small-volume injections.

The ability of various microorganisms to survive in cisplatin injection or fluorouracil injection in small-volume containers was assessed. Inoculum suspensions of Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Pseudomonas cepacia, Candida albicans, or Aspergillus niger were injected into polyvinyl chloride minibags containing 20 mL of either fluorouracil injection 50 mg/mL or cisplatin injection 1 mg/mL in 0.9% sodium chloride injection. All minibags were stored at 25 degrees C for 28 days. Three minibags containing only the sodium chloride solution and 18 minibags containing the sodium chloride solution inoculated with microorganisms served as negative and positive controls, respectively. Samples (1 mL) were obtained within 30 minutes of inoculation and again on days 1, 2, 4, 7, 14, 21, and 28. All microbial species lost viability in both the cisplatin and the fluorouracil admixtures over the study period. In most instances, this loss was more pronounced than that in the positive control solution. Whether the pH of the solutions contributed to this loss of viability was not determined. Under the conditions of this study, admixtures containing cisplatin and fluorouracil did not support rapid growth of microorganisms when stored at room temperature for up to 28 days.

Bacteria↗