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At least 631 records · Page 35Linked to original sources
PubMed2002

Resolution of epithelial ingrowth in a patient treated with 5-fluorouracil.

PURPOSE: To report the effect of 5-fluorouracil on the outcome of a single case of epithelial ingrowth secondary to a wound leak after a complicated penetrating keratoplasty. DESIGN: Case report. METHODS: A 44-year-old man with extensive epithelial ingrowth after trauma and a penetrating keratoplasty received a fluid-gas exchange followed by two injections of 500 microg of 5-fluorouracil into the anterior chamber. RESULTS: Two weeks after receiving the 5-fluorouracil injections, complete disappearance of the epithelial ingrowth from the anterior chamber occurred. No evidence of recurrence was detectable at 5 months. CONCLUSION: Use of 5-fluorouracil is a potentially effective treatment of epithelial ingrowth, particularly in eyes with extensive involvement, in which the risks of traditional ablative therapeutic modalities are considerable.

Adult↗
PubMed1992

Results of intraoperative 5-fluorouracil supplementation on trabeculectomy for open-angle glaucoma.

The success rate of filtration surgery has been increased by the postoperative subconjunctival injection of 5-fluorouracil, a potent antimetabolite. However, the optimal route of administration has not been determined. Trabeculectomy was performed on one eye each of 14 patients. Topical 5-fluorouracil was applied intraoperatively (50 mg/ml for five minutes) and subconjunctival 5-fluorouracil was injected postoperatively (an average of 5.8 injections) (mean total dose, 29 mg). Seven of the 14 eyes had primary open-angle glaucoma, and seven eyes had open-angle glaucoma with either uveitis, aphakia, or previous failed trabeculectomy. Mean preoperative intraocular pressure was 24.7 mm Hg during treatment with an average of three antiglaucoma medications, and mean final intraocular pressure was 11.9 mm Hg during treatment with an average of 0.2 medication. Thirteen of 14 eyes (93%) had final intraocular pressure of 18 mm Hg or less. Mean follow-up was 6.4 months (range, four to nine months). No remarkable complications occurred. Visual acuity remained stable in 13 of 14 eyes (93%). Intraoperative 5-fluorouracil may be a helpful adjunct in achieving low final intraocular pressure after trabeculectomy.

Administration, Topical↗
PubMed1990

Adjunctive use of delayed and adjustable low-dose 5-fluorouracil in refractory glaucoma.

We used delayed 5-mg subconjunctival injections of 5-fluorouracil as an adjunct to filtering surgery in ten eyes with refractory glaucoma. The first 5-fluorouracil injection was made three to 15 days postoperatively and was used only when clinical signs suggested an impending bleb failure. These signs included flattening and localization of bleb, increased vascularity, early subconjunctival scarring, loss of microcystic conjunctival changes, and increased intraocular pressure. After a follow-up of ten to 17 months (mean, 13.7 months), an intraocular pressure of less than 21 mm Hg was attained in five eyes without medication and in four eyes with medication. The treatment failed in one eye. The average dose of 5-fluorouracil was 28 +/- 12 mg per eye. There were no conjunctival wound leaks. Six eyes developed transient corneal epithelial defects. The modified administration of 5-fluorouracil can result in fewer conjunctival wound leaks. Its use can be limited to those patients who show evidence of impending bleb failure.

Adolescent↗
PubMed1990

Needle revision with and without 5-fluorouracil for the treatment of failed filtering blebs.

Twelve patients with failed or failing filtering blebs were treated by transconjunctival needle revision of the bleb. Seven of these received 5-fluorouracil as an adjunct. Intraocular pressure decreased from 31.3 +/- 8.8 mm Hg (range, 20 to 47 mm Hg) to 17.0 +/- 3.7 mm Hg (range, 8 to 22 mm Hg). The length of follow-up ranged from two to 31 months. The results in 11 of 12 patients (91.6%) were satisfactory, defined by an intraocular pressure of 22 mm Hg or less, with or without antiglaucoma medications, and requiring no subsequent procedures for control of intraocular pressure. The success rates and overall pressure lowering effect of the seven patients receiving and the five patients not receiving 5-fluorouracil were similar. However, most patients receiving 5-fluorouracil were thought to be at higher risk for surgical failure. Complications of needle revision were minor and resolved without sequelae. We advocate the consideration of transconjunctival needle revision with or without the use of 5-fluorouracil as a useful therapeutic modality in the management of the failed or failing filtering bleb.

Adult↗
PubMed1999

Noninfectious crystalline keratopathy after postoperative subconjunctival 5-fluorouracil.

PURPOSE: To describe a case of transient, noninfectious crystalline keratopathy after postoperative subconjunctival 5-fluorouracil. METHOD: Case report. Slit-lamp biomicroscopic examinations were performed during serial office examinations. RESULTS: A 69-year-old woman underwent an uncomplicated trabeculectomy with adjunctive sponge 5-fluorouracil application for 5 minutes in her left eye. Postoperative treatment included topical prednisolone acetate, ciprofloxacin, and scopolamine. She was initially examined with intrastromal corneal crystalline deposits 5 days after her first postoperative subconjunctival injection of 5-fluorouracil. The deposits completely disappeared 4 days later without addition to or change in treatment. CONCLUSION: Transient, noninfectious, crystalline, intrastromal corneal deposits may develop after adjunctive subconjunctival 5-fluorouracil administration.

Aged↗
PubMed1988

Preoperative irradiation and 5-fluorouracil suppository for carcinoma of the rectum.

For prevention of local recurrence of rectal carcinoma postoperatively, we attempted to use preoperative irradiation, 5-fluorouracil suppository, or both. When 5-fluorouracil was employed, it produced a remarkably high drug concentration in the rectum and regional lymph nodes. 5-fluorouracil suppository alone did not increase the 5 year postoperative survival rate. Preoperative irradiation combined with 5-fluorouracil suppository (combined treatment group) produced shrinkage of tumor size in 18 of 23 patients, including tumor disappearance in 2 patients, whereas irradiation alone produced shrinkage of tumor size in 13 of 24 patients. Cancer invasions to the external wall of the rectum and lymph node metastases, which were the most influential factors on local rectal recurrence postoperatively, were significantly reduced by preoperative combined treatment.

Aged↗
PubMed2003

Apoptosis, 5-fluorouracil sensitivity and expression of apoptotic proteins in a human ectocervical cell carcinogenesis model using different media.

Apoptosis has received widespread attention for its essential roles in biology, medicine and cancer. We previously found that normal, human papillomavirus (HPV) 16-immortalized and their transformed endocervical cells were increasingly resistant to apoptosis induced by a cancer therapeutic drug. Here, analogously, another common anticancer drug, 5-fluorouracil, in an ectocervical cell carcinogenesis model induced apoptosis in primary human ectocervical cells (HEC), whereas HPV18-immortalized HEC (HEC-18) and transformed HEC-18 (HEC-18T) were more resistant. Growth in serum/low density lipoprotein (LDL)-containing medium reversed resistance to 5-fluorouracil-induced apoptosis, particularly in HEC-18T. Cell viability results confirmed these findings. Using Western blots to compare protein levels with those of HEC not treated with 5-fluorouracil, the fold changes in HEC-18 and HEC-18T in LDL-free medium were 1.6-6.1-fold lower for pro-apoptotic p53, Bak and Bax. Four anti-apoptotic proteins were altered -2.1 to+14.6-fold for Bcl-2 and BAG-1 isoform p33 and p29. For BAG-1 p50 and p46, HEC-18 were weakly expressed and HEC-18T were moderately higher. Grown in LDL-containing medium, the differences in pro-apoptotic protein levels were mostly reversed. Expression was 1.4-32-fold higher in HEC-18 and HEC-18T of p53, Bax, BAG-1 p29, BAG-1 p33 and total BAG-1. These results showed that HEC carcinogenesis results in resistance to 5-fluorouracil-induced apoptosis, associated with reduced expression during carcinogenesis of pro-apoptotic proteins and increased expression of specific anti-apoptotic proteins.

Adenocarcinoma↗
PubMed1998

Regulation of the PepT1 peptide transporter in the rat small intestine in response to 5-fluorouracil-induced injury.

BACKGROUND & AIMS: The oligopeptide transport system of the small intestine is resistant to mucosal injury. The mechanism of this resistance was investigated by examining the activity level and expression of the peptide transporter PepT1 in the intestine of rats treated with 5-fluorouracil. METHODS: The expression and localization of PepT1 were examined by immunoblot analysis of brush border membrane vesicles and immunohistochemical analysis of intestinal sections with PepT1-specific rabbit polyclonal antibodies. Also, Northern blot analysis was used for the expression of PepT1 messenger RNA (mRNA). RESULTS: Although the amounts of sucrase and an Na+-dependent glucose transporter protein in intestinal vesicles decreased markedly after 5-fluorouracil treatment, the amount of PepT1 protein remained largely unaffected. Immunohistochemical analysis also showed that the PepT1 immunoreactivity level was preserved in the brush border membrane of the remaining villi of 5-fluorouracil-treated rats. Levels of amino acid, glucose, and phosphate transporter mRNAs were profoundly depressed in 5-fluorouracil-treated animals, whereas the level of PepT1 mRNA conversely increased. CONCLUSIONS: The resistance of intestinal peptide transport to tissue injury may be attributable to increased synthesis of PepT1 rather than to a change in the kinetic properties of the residual absorbing cells.

Animals↗
PubMed1982

Oral administration of 5-fluorouracil: renal clearance and urinary concentration in man.

The pharmacokinetics of 5-fluouracil were studied in 9 patients with a history of bladder malignancies. A single dose of 250 mg. 5-fluorouracil was given orally and the renal clearance of active 5-fluorouracil was approximately 40 ml. per minute. The maximum serum (1,100 ng./ml. serum) and urinary concentrations (49,000 ng./ml. urine) of 5-fluorouracil occurred 20 and 40 minutes after administration, respectively. The urinary concentration per se is highly cytotoxic, whereas the short-lasting serum concentration previously has been proved to be without general cytotoxic effects even after continuous use of the drug for years. Although high concentrations of 5-fluorouracil are noted in the urine the antitumor effects of this treatment must be investigated further.

Administration, Oral↗
PubMed1982

Cyclophosphamide, methotrexate and 5-fluorouracil combination chemotherapy versus chloroethyl-cyclohexy-nitrosourea in the treatment of metastatic prostatic cancer.

In a prospective, randomized study the effect of cyclophosphamide, methotrexate and 5-fluorouracil combination chemotherapy was compared to the single agent, chloroethyl-cyclohexy-nitrosourea, in the treatment of hormonally refractive metastatic prostatic carcinoma. All patients could be evaluated and were followed for at least 2 years or until death. Responses were defined by the National Prostatic Cancer Project criteria. Of 20 patients who received cyclophosphamide, methotrexate and 5-fluorouracil 3 (15 per cent) had partial (median duration of 2.5 months), 4 (20 per cent) had stable (median duration of 5 months) and 13 had progression of the disease. Of 20 patients who received chloroethyl-cyclohexy-nitrosourea none had a partial response, 6 (30 per cent) had stability (median duration of 6.2 months) and 13 had progression of the disease. The over-all response rate for patients receiving cyclophosphamide, methotrexate and 5-fluorouracil was 35 per cent (stable plus partial regressions) and it was 30 per cent for those receiving chloroethyl-cyclohexy-nitrosourea (stable only). Subjective improvement was noted in all 7 patients who responded to combination chemotherapy and in 3 of the 6 patients who responded to the single agent. After 2 courses resistant patients were crossed over to the opposite regimen and none had an objective, stable or subjective response. Although the duration of response was short (2 to 6 months) patients with partial regressions or stabilized disease survived longer (p less than 0.05) than patients whose disease progressed (52 versus 24 weeks, respectively). The mean interval from diagnosis to chemotherapy (lead time) was 40 months for patients who responded to chemotherapy compared to 19 months for those with progression, which suggested a slower growing pattern of disease in those who did respond. There was no improvement in cohort survival with either treatment regimen. Over-all response rates to cyclophosphamide, methotrexate and 5-fluorouracil were not superior to reported responses to cyclophosphamide alone, and both treatment regimens appeared to be only marginally effective in the treatment of endocrine-resistant, advanced prostatic cancer.

Aged↗
PubMed1978

General resorption of intravesically instilled 5-fluorouracil.

To evaluate the resorption of intravesically instilled 5-fluorouracil a single dose of 250 or 1,000 mg. was injected into the empty bladder for 3 hours in 17 patients. The concentration of 5-fluorouracil in serum during instillation was recorded. A microbiologic agar plate method was used for the assay. No measurable 5-fluorouracil concentrations were recorded in the systemic blood of patients with undamaged bladder mucosa and low levels (less than 100 ng./ml. serum) of 5-fluorouracil were found in the systemic circulation of patients with mucosal lesions.

Aged↗
PubMed2003

Intrahepatic arterial versus intravenous fluorouracil and folinic acid for colorectal cancer liver metastases: a multicentre randomised trial.

BACKGROUND: The liver is the most frequent site for metastases of colorectal cancer, which is the second largest contributor to cancer deaths in Europe. We did a randomised trial to compare an intrahepatic arterial (IHA) fluorouracil and folinic acid regimen with the standard intravenous de Gramont fluorouracil and folinic acid regimen for patients with adenocarcinoma of the colon or rectum, with metastases confined to the liver. METHODS: We randomly allocated 290 patients from 16 centres to receive either intravenous chemotherapy (folinic acid 200 mg/m2, fluorouracil bolus 400 mg2 and 22-h infusion 600 mg/m2, day 1 and 2, repeated every 14 days), or IHA chemotherapy designed to be equitoxic (folinic acid 200 mg/m2, fluorouracil 400 mg/m2 over 15 mins and 22-h infusion 1600 mg/m2, day 1 and 2, repeated every 14 days). The primary endpoint was overall survival, and analysis was by intention to treat. FINDINGS: 50 (37%) patients allocated to IHA did not start their treatment, and another 39 (29%) had to stop before receiving six cycles of treatment because of catheter failure. The IHA group received a median of two cycles (0-6), compared with 8.5 (6-12) for the intravenous group. 45 (51%) IHA patients who did not start or did not receive six cycles switched to intravenous treatment. In both groups, grade 3 or 4 toxicity was uncommon. Median overall survival was 14.7 months for the IHA group and 14.8 months for the intravenous group (hazard ratio 1.04 [95% CI 0.80-1.33], log-rank test p=0.79). Similarly, there was no significant difference in progression-free survival. INTERPRETATION: Our results showed no evidence of an advantage in progression-free survival or overall survival for the IHA group; thus continued use of this regimen cannot be recommended outside of a clinical trial.

Adenocarcinoma↗
PubMed1984

5-fluorouracil and glaucoma filtering surgery: I. An animal model.

Failure of a glaucoma filtering procedure commonly results from scarring at the surgical site. Fibroblasts play an important role in the scarring process. 5-fluorouracil is an antimetabolite capable of inhibiting fibroblast proliferation. We tested the ability of 5-fluorouracil to inhibit cicatrization at the filtering site in an experimental model. Posterior lip sclerectomies were performed in each eye of ten normal owl monkeys. Postoperatively, one eye of each animal received subconjunctival injections of fluorouracil and the fellow eye received saline injections in a randomized, masked fashion. Two animals died of undetermined causes. None of the control eyes developed blebs, but six of the eight treated eyes in surviving animals developed blebs. The difference between intraocular pressures in fluorouracil-treated and control eyes was statistically significant (P less than 0.05). Signs of ocular toxicity included persistent corneal epithelial defects and delayed healing of the conjunctival incision. These results are considerably more favorable than those previously reported with experimental filtering procedures in non-human primates. Pharmacologic modulation of wound healing may decrease the risk of failure of filtering operations.

Animals↗
PubMed1987

Weekly psoriasis therapy using intralesional fluorouracil.

We report the use of weekly intralesional fluorouracil for treatment of entire psoriatic papules and portions of larger psoriatic plaques. Eleven patients participated and responded, with an average of 4.2 cm2 clearing about the injection site in the treated lesions, in comparison with no improvement in the control lesions. We injected 1 ml of fluorouracil (50 mg/ml) to form an intradermal wheal of about 0.8 cm2. Each patient received one to three injections at 1- to 2-week intervals, with an average of two injections per patient. The earliest signs of improvement occurred at 2 weeks; maximum clearing was achieved usually about 4 weeks after treatment began. At 3-month follow-up, four of the nine patients who had favorable response to treatment remained substantially in remission. Toxic effects were limited to local hyperpigmentation in seven patients, slight irritation in two patients, and moderate irritation in one patient. No systemic toxic effects were shown. Weekly pulse doses of fluorouracil given intralesionally instead of topically can greatly speed up response to therapy and can produce similarly good results. Intralesional administration of fluorouracil is locally effective, is often of long-term benefit, and can be tolerated well.

Administration, Topical↗
PubMed1997

High-performance liquid chromatographic assay of 5-fluorouracil in human erythrocytes, plasma and whole blood.

A HPLC assay method was modified and validated for the determination of 5-fluorouracil in human red blood cells, plasma and whole blood with a two-fold increased sensitivity (detection limit=10 ng/ml). The assay was linear from 25 to 1500 ng/ml and the accuracy ranged from 96.7 to 103.2% at 25 ng/ml, 94.8 to 99.4% at 500 ng/ml, and 98.9 to 99.5% at 1500 ng/ml. Intra-assay and inter-assay coefficients of variation were less than 8% over the range of concentrations and less than 8% over 10 days of analysis. After intravenous bolus and infusion of 5-fluorouracil in patients with colorectal cancer, the concentrations of 5-fluorouracil in whole blood were 108-111% of plasma concentrations, while packed red blood cells levels were 8-15% of plasma concentrations in the five patients studied. By utilising basic analytical hardware, this represents an accurate, precise, reproducible and affordable method for 5-fluorouracil pharmacokinetics investigation and therapeutic drug monitoring.

Antimetabolites, Antineoplastic↗
PubMed1999

Concomitant and controlled release of dexamethasone and 5-fluorouracil from poly(ortho ester).

A viscous bioerodible and hydrophobic poly(ortho ester) has been developed as a biocompatible, sustained drug release system for an ophthalmic application in intraocular proliferative disorders. The combination of wound healing modulators such as 5-fluorouracil and dexamethasone is a major advantage since these drugs act at different stages of these diseases. Since 5-fluorouracil is an acidic, water-soluble compound and dexamethasone exists in three chemical forms, i.e. the water-insoluble base, the highly hydrophobic acetate ester or the basic phosphate salt, it was of interest to investigate whether the physicochemical properties of the drugs have an influence on their release rates, and whether a concomitant and sustained release of both 5-fluorouracil and dexamethasone could be achieved. It has been found that lipophilicity and acidobasicity play a major role in controlling drug release rates and polymer degradation. The combination of 5-fluorouracil and dexamethasone phosphate allows a sustained and concomitant release of both drugs, due to the basic characteristics of the corticosteroid which stabilize the polymer. This system appears to be promising for concomitant and controlled drug delivery aimed at the pharmacological treatment of intraocular proliferative disorders.

Anti-Inflammatory Agents, Non-Steroidal↗
PubMed1999

Ultrasound-enhanced diffusion into coupling gel during phonophoresis of 5-fluorouracil.

PURPOSE: To investigate the competitive transport across skin and back-diffusion of 5-fluorouracil into coupling gel under the influence of ultrasound, heat-alone and Azone enhancement. METHODS: The ultrasound effect on 5-fluorouracil penetration through whole rat skin was investigated in modified diffusion cells using a commercial ultrasound generator which was calibrated with a bilaminar membrane hydrophone. RESULTS: Ultrasonic dosimetry measurements demonstrated that the skin membrane was subjected to a complex and unpredictable standing wave field which induced physiologically acceptable heating of the tissue. Surprisingly, ultrasonication produced a decrease in percutaneous drug penetration. Quantification studies indicated that this effect was due to the diffusive loss of the hydrophilic substance 5-fluorouracil from the skin surface into the overlying volume of coupling gel. This phenomenon could be duplicated by the application of conductive heating, indicating that the thermal effects of ultrasound were probably responsible for accelerated 5-fluorouracil diffusion through the gel. CONCLUSION: This study acutely demonstrates how formulation design of the donor vehicle/coupling gel may radically affect therapeutic efficacy in phonophoretic systems.

Animals↗
PubMed2002

Determination of the 5-fluorouracil and N1(2'-furanidyl)uracil in the presence of tegafur by zero-crossing first derivative spectrometry.

A first derivative spectrometric method has been developed for the determination of the 5-fluorouracil and N1(2'-furanidyl)uracil related substances and degradation products of tegafur. The wavelengths selected for the determination of 5-fluorouracil and N1(2'-furanidyl)uracil were 298 and 288 nm, respectively. At this wavelength, the calibration graphs between the amplitude of the signals and the concentration of each compound were linear up to 24.75 mg l(-1) for 5-fluorouracil and up to 20.20 mg l(-1) for N1(2'-furanidyl)uracil. The detection limits were 0.40 and 0.050 mg l(-1) for 5-fluorouracil and N1(2'-furanidyl)uracil, respectively. The method is simple and rapid and does not require any preliminary treatment of the sample. The method was validated.

Fluorouracil↗