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[Antibiotic prophylaxis for transurethral resection of the prostate--comparison of oral administration therapy with intravenous administration therapy].

To compare the prophylactic effect of oral and intravenous antibiotics against postoperative fever and urinary tract infection (UTI) after transurethral resection of the prostate (TUR-P), we conducted a multi-center prospective randomized study. The incidence of pyrexia over 38 degrees C was defined as the primary endpoint. One hundred and fifty patients with sterile urine before TUR-P were entered into this study. The patients were allocated randomly into the two arms; arm A cefotiam 4 g a day for 7 days, arm B tosufloxacin 300 mg a day for 7 days, based on the stratification into the 4 groups determined with/without preoperative indwelling catheters and with/without the history of preoperative UTI. Of these patients, 143 were eligible. We divided 124 patients without preoperative UTI and without indwelling catheters as the "low risk group", and the other 19 patients with preoperative UTI and/or with indwelling catheters as the "high risk group". In the low risk group, 9 patients out of 63 (14.3%) in arm A and 6 out of 61 (9.8%) in arm B had pyrexia during 7 postoperative days. The incidence of fever in arm B was 4.4% less than that in arm A and the 95% confidence limit was from -7% to 16%. In the high risk group, 4 out of 11 (36.4%) patients in arm A and none of 8 in arm B had fever but the difference was not significant. The incidence of post operative UTI in the low risk group on the 4 to 5, 9 to 12, 23 to 26 and 37 to 40 postoperative days was 8.3, 16.4, 25.0 and 23.9% in arm A and 6.7, 16.7, 29.6 and 36.7% in arm B, respectively. The prophylactic effect of oral administration of tosufloxacin is equivalent to that of the intravenous administration of cefotiam. The use of oral antibiotics is beneficial to reducing the cost of medication.

Administration, Oral↗

Studies on tumor necrosis factor (TNF)--I. Pharmacokinetics of human recombinant TNF in rabbits and monkeys after intravenous administration.

By intravenous (bolus) administration of human recombinant tumor necrosis factor (2.5 X 10(6) units) into rabbits and monkeys it has been possible to follow its decay in the plasma and to determine the pharmacokinetic parameters. After labelling TNF with 125I, simultaneous determination of protein-bound radioactivity and bioactivity was carried out with the result that radioactivity decays somewhat slower than bio-activity suggesting that the use of the former tracer alone may underestimate TNF catabolism. Simultaneous determination of 125I-TNF in rabbit plasma and lymph after intravenous and subcutaneous administration indicated a lymph to plasma TNF concentration ratio of about 0.1 and 1 or more for the two routes, respectively.

Animals↗

Treatment of atrial fibrillation in horses by intravenous administration of quinidine.

Intravenous administration of quinidine gluconate converted atrial fibrillation (AF) to sinus rhythm in 9 of 12 horses. Twelve horses that were diagnosed by ECG to have AF were administered up to 11 mg of quinidine gluconate/kg of body weight in 1.0- to 1.5-mg/kg bolus injections every 10 to 15 minutes. The total dose of quinidine administered IV ranged from 1.8 to 5.8 g. Increased ventricular rate, apprehension, and mild depression were observed during treatment. Other signs of toxicosis were not observed. One horse was successfully treated with IV administered quinidine gluconate on 3 occasions. Intravenous administration of quinidine is a safe and effective alternative for treatment of AF in some horses.

Animals↗

[Therapeutic effects of micronomicin on experimental infections in mice by intravenous administration].

Protective effects of intravenous administration of micronomicin (MCR) on mouse experimental infections were investigated. Mice were better protected by intravenous administration in S. marcescens T-55 experimental infection than subcutaneous administration. No remarkable differences were found between the two administrations in cases of P. aeruginosa BMH No. 1 and E. coli GN 2411-5 infections. Intravenous administrations of MCR, gentamicin (GM), dibekacin (DKB), amikacin (AMK) and sisomicin (SISO) protected the infection of P. aeruginosa BMH No. 1 in a similar extent. MCR was more effective intravenously than AMK; DKB and AMK; DKB, AMK and SISO in experimental infections of E. coli GN 2411-5; S. marcescens T-55; P. aeruginosa KY-8510 harboring aminoglycoside inactivating enzyme AAC(6')-4, respectively.

Aminoglycosides↗

Optimal timing for intravenous administration set replacement.

BACKGROUND: Administration of intravenous therapy is a common occurrence within the hospital setting. Routine replacement of administration sets has been advocated to reduce intravenous infusion contamination. If decreasing the frequency of changing intravenous administration sets does not increase infection rates, a change in practice could result in considerable cost savings. OBJECTIVES: The objective of this review was to identify the optimal interval for the routine replacement of intravenous administration sets when infusate or parenteral nutrition (lipid and non-lipid) solutions are administered to people in hospital via central or peripheral venous catheters. SEARCH STRATEGY: We searched The Cochrane Central Register of Controlled Trials (CENTRAL), MEDLINE, CINAHL, EMBASE: all from inception to February 2004; reference lists of identified trials, and bibliographies of published reviews. We also contacted researchers in the field. We did not have a language restriction. SELECTION CRITERIA: We included all randomized or quasi-randomized controlled trials addressing the frequency of replacing intravenous administration sets when parenteral nutrition (lipid and non-lipid containing solutions) or infusions (excluding blood) were administered to people in hospital via a central or peripheral catheter. DATA COLLECTION AND ANALYSIS: Two authors assessed all potentially relevant studies. We resolved disagreements between the two authors by discussion with a third author. We collected data for the outcomes; infusate contamination; infusate-related bloodstream infection; catheter contamination; catheter-related bloodstream infection; all-cause bloodstream infection and all-cause mortality. MAIN RESULTS: We identified 23 references for review. We excluded eight of these studies; five because they did not fit the inclusion criteria and three because of inadequate data. We extracted data from the remaining 15 references (13 studies) with 4783 participants. We conclude that there is no evidence that changing intravenous administration sets more often than every 96 hours reduces the incidence of bloodstream infection. We do not know whether changing administration sets less often than every 96 hours affects the incidence of infection. In addition, we found that there were no differences between participants with central versus peripheral catheters; nor between participants who did and did not receive parenteral nutrition, or between children and adults. AUTHORS' CONCLUSIONS: It appears that administration sets that do not contain lipids, blood or blood products may be left in place for intervals of up to 96 hours without increasing the incidence of infection. There was no evidence to suggest that administration sets which contain lipids should not be changed every 24 hours as currently recommended.

Bacterial Infections↗

Increase in peripheral blood flow by intravenous administration of prostaglandin E1 in patients with peripheral arterial disease, accompanied by up-regulation of hepatocyte growth factor.

Since endothelial damage is a trigger for the progression of atherosclerosis, we evaluated the clinical utility of prostaglandin E1 (PGE1) in relation to peripheral blood flow and regulation of hepatocyte growth factor (HGF), an angiogenic growth factor, in patients with peripheral arterial disease (PAD). Fourteen male patients with PAD who showed the characteristic symptoms of arteriosclerosis obliterans (Fontaine I: n=2; Fontaine II: n=4; Fontaine III: n=2; Fontaine IV: n=6), confirmed by angiography, were enrolled in this study. Patients were administrated synthetic PGE1 at a dose of 120 microg per day for 14 consecutive days. Measurement of peripheral blood flow and serum HGF concentration was performed before PGE1 treatment and after 14 days of administration. Interestingly, intravenous administration of PGE1 for 2 weeks significantly increased the blood flow as assessed by a laser Doppler imager (p<0.01). In patients with Fontaine III and IV, serum HGF concentration was significantly higher than that in patients with Fontaine I or II and normal subjects. Of importance, administration of PGE1 further increased serum HGF concentration as compared to that before treatment (p<0.01). The increase in circulating HGF might work as a compensatory mechanism to decrease local HGF expression in patients with PAD, since HGF acts as an angiogenic growth factor with anti-apoptotic actions on endothelial cells. Moreover, to confirm the stimulatory effect of PGE1 on HGF in vessels, we employed an in vitro culture system. PGE1 increased HGF production and the growth of human cultured vascular endothelial cells. The stimulatory effect of PGE1 on HGF production might be due to an increase in cAMP, since forskolin and 8-bromo-cAMP induced HGF production. In conclusion, we demonstrated that administration of PGE1 stimulated peripheral blood flow, accompanied by an increase in systemic HGF concentration. Also, our in vitro data suggested that PGE1 augmented not only the systemic HGF level, but also local HGF production, probably through cAMP accumulation, resulting in improvement of endothelial function and blood flow.

Aged↗

Decontamination of the bowel by intravenous administration of pefloxacin.

Intravenous administration of pefloxacin 400 mg twice daily rapidly decontaminated the bowel from Gram-negative bacilli in ten healthy volunteers. The faecal concentrations of enterococci and yeasts did not change significantly. Further, pefloxacin did not facilitate colonization of the bowel by a highly resistant challenge strain (Klebsiella pneumoniae, MIC = 56 mg/l). The diffusible faecal concentration of pefloxacin was between 110 and 260 mg/l in all samples from day 3 of treatment onwards. It is concluded that parenteral administration of pefloxacin is very effective for decontamination of the bowel from Gram-negative bacilli and provides reliable prophylaxis against colonization of the bowel by highly resistant Gram-negative bacilli ingested with food.

Adult↗

[Comparative organ distribution of various sizes of liposomes during their intravenous administration].

Distribution after intravenous administration of unilamellar--0.025-0.030 micron, multilamellar--0.05-2.0 micron and large oligolayer--0.2-0.5 micron liposomes, 99mTc labelled in the lipid phase, was studied in mice tissues. Distinct correlation between clearance of the liposomes from circulation and the vesicles size was found. Large oligolayer liposomes were stored in spleen tissue 3-4 fold more effectively as compared with uni- and multilamellar liposomes; accumulation of the vesicles in spleen tissue depended also on concentration of the microemulsion administered.

Animals↗

Pharmacokinetics and pharmacodynamics of emepronium bromide (Cetiprin) after intravenous administration in man.

Intravenous doses of 1, 5, 10 and 15 mg of emepronium bromide were given to three healthy volunteers. Emepronium serum concentration declined in a triexponential manner with half-lives between 2.2-3.0 min., 1.0-1.6 hours and 5.1-13 hours, respectively. The initial dilution space (volume of the central compartment) varied between 4.1-7.5 l. The area under the serum concentration time curve increased linearly with dose, indicating constancy of total serum clearance (range: 24-38 l/hr) with dose. The renal clearance of emepronium varied with serum concentration; secretion in addition to glomerular filtration was evident. Tubular secretion of emepronium was half-saturated at serum concentrations of approximately 50 nmol/l. No obvious drug-related effect on blood pressure was noted, whereas salivary secretion decreased and heart rate increased with 10-15% at emepronium serum concentrations of about 200 nmol/l. ECG recordings were without abnormalities after slow intravenous injections of emepronium bromide in doses of up to 15 mg. Since no adverse effects were noted, intravenous administration of emepronium bromide may be an alternative in situations where the drug is now used intramuscularly e.g. severe tenesmus in the urinary bladder.

Administration, Oral↗

Plasma concentration of alpha-methyldopa and sulphate conjugate after oral administration of methyldopa and intravenous administration of methyldopa and methyldopa hydrochloride ethyl ester.

The plasma concentrations of free alpha-methyldopa and methyldopa sulphate conjugate were measured in 7 hypertensive patients with normal renal function following alpha-methyldopa (1 g) orally. Five of these patients subsequently received alpha-methyldopa ethyl ester (250 mg) (methyldopate) intravenously and two further patients received 250 mg of alpha-methyldopa intravenously. After oral administration a large amount of total plasma alpha-methyldopa was present as sulphate conjugate. There were wide interindividual differences in the ratio of free: conjugated alpha-methyldopa in plasma (ratio at 4 hours ranged from 3.73-0.83) suggesting that individual differences in the extent of sulphate conjugation may occur. There was no close correlation between the degree of conjugation and the fall in arterial pressure. At all time intervals examined, plasma concentrations were higher following intravenous alpha-methyldopa than alpha-methyldopate. The plasma concentration of alpha-methyldopa (free and esterified) 60 minutes after i.v. alpha-methyldopate was 1.7+/-0.3 mug/ml while at the same time after the same dose of methyldopa by the same route the mean concentration was 5.9 mug/ml. Although small amounts of sulphate conjugate were detected after i.v. alpha-methyldopate, insignificant quantities of conjugate were found after i.v. alpha-methyldopa. The average fall in mean arterial pressure was 27 mm/Hg following i.v. alpha-methyldopa but only 2.7 mm Hg following alpha-methyldopate. These results suggest that sulphate conjugation of alpha-methyldopa occurs in the gastrointestinal tract during absorption. Hydrolysis of alpha-methyldopa ethyl ester does not appear to be instantaneous and pharmacokinetic differences between the ester and free alpha-methyldopa have been demonstrated.

Administration, Oral↗

Fosfomycin levels in human aqueous humor after intravenous administration.

Following intravenous infusion of an 8 g single dose of the antibiotic agent fosfomycin, its penetration into human primary aqueous humor was investigated. 1-2 h after the start of infusion, peak values of 35 to 60 micrograms/ml were reached. These concentrations in the aqueous humor would inhibit a high percentage of gram-positive and gram-negative strains commonly causing bacterial endophthalmitis. The infusion of an 8 g dose of fosfomycin immediately preceding intraocular surgery thus constitutes effective peri-operative prophylaxis. Moreover, as a broad-spectrum antibiotic, fosfomycin is indicated as initial therapy in intraocular bacterial infections.

Aged↗

Acute hemodynamic effects and blood pool kinetics of polystyrene microspheres following intravenous administration.

The acute hemodynamic effect of intravenous administration of polystyrene microspheres was investigated and correlated with their distribution pattern and kinetics. Microspheres of three diameters (3.4, 7.4, and 11.6 micrometer) were administered. The 7.4- and 11.6-micrometer diameter microspheres were filtered by the pulmonary capillary network following intravenous administration, the majority during the first pass. There was no significant hemodynamic effect following administrations of the 7.4- and 11.6-micrometer diameter microspheres in doses as high as 3.0 X 10(9) and 6.1 X 10(8) respectively (total cross-sectional area of 1.3 X 10(11) and 6.4 X 10(10) micrometer2, respectively). Intravenous administration of 3.4-micrometer diameter microspheres produced significant dose-dependent systemic hypotension and depression of myocardial performance at dosages as slow as 1.0 X 10(10) (cross-sectional area of 9.1 X 10(10) micrometer2). These differences in acute hemodynamic effect from the 7.4- and 11.6-micrometer diameter microspheres may be due to the differences in distribution kinetics and fate of the 3.4-micrometer diameter microspheres, which readily pass through the lungs to the spleen. Although elimination of the smaller spheres from the blood during the first 6-8 min was rapid, i.e., t 1/2 = 1.62 and 1.72 min from the venous and arterial blood circulation, respectively, levels of 10(3) spheres/g of blood were present in the circulation for greater than 1 hr. These findings must be considered in the planning of intravenous administration of microspheres as a drug delivery system to target organs.

Animals↗

[Convulsion following the combination of single preoperative oral administration of enoxacine and single postoperative intravenous administration of flurbiprofen axetil].

We experienced a case of convulsion following the combination of single oral administration of enoxacine before an emergency operation and single postoperative intravenous administration of flurbiprofen axetil. The patient was an 87-year-old female referred to our hospital for severe abdominal pain. She was diagnosed as having the strangulation ileus, then underwent the emergent operation of partial resection of the necrotic small intestine under general anesthesia. Unfortunately we did not know that she had temporarily received oral enoxacine 200 mg, a new quinolone, administered by the previous doctor on the day before the operation. After the operation, flurbiprofen axetil 50 mg, a nonsteroidal anti-inflammatory drug, was given intravenously in thirty seconds due to postoperative pain. One minute after administration of the drug, she immediately developed a convulsive fit, severe disturbance of consciousness and apnea. We then administered at once, a single dose of diazepam intravenously for convulsion treatment, kept her airway open and controlled her ventilation. Convulsion disappeared in a minute and her condition improved gradually. We suspect that convulsive seizure may have been induced by the drug interaction between single oral dose of enoxacine before the operation and single intravenous dose of flurbiprofen axetil after the operation. We also suspect that the serum concentration of enoxacine was kept high because of metabolic disturbance and renal dysfunction resulting from her old age and dehydration. This case suggests that medication before the emergency operation must be considered in anesthetic management because of the possible side effect such as convulsion induced by the drug interaction between neuquinolones and anti-inflammatory drugs.

Administration, Oral↗

Continuous intravenous administration of 1-(2-tetrahydrofuryl)-5-fluorouracil [FT] by intravenous hyperalimentation (IVH)--stability of FT in IVH solution and tumor levels of 5-fluorouracil (5-FU).

The continuous intravenous administration of 1-(2-tetrahydrofuryl)-5-fluorouracil (FT) to colorectal cancer patients was studied in regard to the stability of FT in intravenous hyperalimentation (IVH) solutions and tumor levels of 5-fluorouracil (5-FU). FT was very compatible with IVH solutions, because the decomposition of FT in IVH solution was very low, 3%. High levels of 5-FU, which is an active metabolite of FT, were obtained in the tumors, averaging 0.369 mcg/g. The ratios of 5-FU levels in the tumor to those in serum and normal tissues were 13.6 and 3.7, respectively. The difference in 5-FU levels between normal tissues and the tumors was statistically significant (P less than 0.01). Therefore, continuous intravenous administration of FT should be widely used to treat patients with colorectal cancer, as the method of administration of antitumor agents.

Colonic Neoplasms↗

A preparation of modified immune serum globulin (human) suitable for intravenous administration. Further characterization and comparison with pepsin-treated intravenous gamma globulin.

Numerous methods have been used in previous attempts to prepare a human gamma globulin solution suitable for intravenous administration. These include fractionation schemes, enzyme digestion, manipulations of pH, and various combinations of these methods. The selective reduction and alkylation process that we have developed for Gamimune causes a controlled and reproducible modification of a limited number of disulfide bonds in the hinge region of IgG, resulting in a functional antibody molecule of undiminished molecular weight and possessing complement-binding properties suitable for intravenous administration. Subtle changes in molecular structure or properties that may be caused by trace enzyme hydrolysis or extremes of pH and temperature are avoided. The biochemical characterization of immune globulin intravenous (Gamimune) is described herein, and the attributes of this chemically modified IgG are compared with some of the other intravenous gamma globulin preparations.

Chemical Phenomena↗

Pharmacokinetic study of all-trans-retinoyl-beta-D-glucuronide in Sprague-Dawley rats after single and multiple intravenous administration(s).

All-trans-retinoyl-beta-D-glucuronide (RAG) is an endogenous active metabolite of all-trans-retinoic acid (ATRA). In the present study, the pharmacokinetics of RAG was examined after the administration of a single intravenous does (5, 10, or 15 micromol/kg) and of multiple daily intravenous doses (5 micromol/kg) to rats for 8 days. The plasma concentrations of RAG and ATRA were measured by a reverse-phase HPLC method. A rapid distribution phase of approximately 1 h was observed in all of the rats after single or multiple doses. Thereafter, RAG was eliminated through a first-order process, in accord with a typical two-compartment first order pharmacokinetic profile. After single intravenous doses, the AUC of RAG increased proportionally with the dose and the clearance remained unchanged within the tested doses. There was no statistical significant difference in distribution rate constants from central compartment to peripheral compartment (K(12)) and from peripheral compartment to central compartment (K(21)) between different doses. However, as the dose increased from 5 micromol/kg to 10 micromol/kg, the volume of distribution at the steady state (V(ss)) and the volume of peripheral compartment (V(p)) decreased significantly (p < 0.05) from 1.290 +/- 0.269, 0.928 +/- 0.232. L/kg to 0.961 +/- 0.149, 0.647 +/- 0.107 L/kg, respectively. V(ss) and V(p) at a dose of 15 micromol/kg (0.924 +/- 0.187, 0.698 +/- 0.165 L/kg) were not significantly different from that at 10 micromol/kg. Thus, RAG might saturate the tissue-binding sites at higher doses. ATRA was detected as a metabolite of RAG at low levels (usually < 0.05 microM) only in the first 2 h after intravenous administration. RAG clearly was not extensively hydrolyzed to ATRA in our study. After multiple daily intravenous administration of RAG, the clearance (Cl) and the elimination rate constant (K(10)) remained unchanged (p > 0.05), indicating that long-term daily administration of RAG did not induce its accelerated metabolism. However, K(12), V(p), and V(ss) declined significantly (p < 0.05) from 1.67 +/- 0.54 h(-1), 0.928 +/- 0.232 L/kg, and 1.290 +/- 0.269 L/kg to 0.96 +/- 0.48 h(-1), 0.494 +/- 0.147 L/kg, and 0.818 +/- 0.187 L/kg, respectively. Therefore, long-term daily dosing of RAG seemed to decrease its distribution profile. Although the AUC of RAG did not change significantly after multiple dosing, the AUC of ATRA after RAG dosing significantly declined (p < 0.05) from 0.032 +/- 0.019 microM x h to 0.010 +/- 0.006 microM x h. The decline in the AUC of ATRA might reflect an increase in its uptake by tissue and/or in its metabolism. Because enhanced clearance is not associated with RAG after multiple administrations, RAG could be considered as an alternate to ATRA in appropriate clinical applications.

Animals↗