Lack of Methemoglobinemia with Flutamide

Schulz, Martin; Schmoldt, A.; Donn, F.; Becker, H.

doi:10.1345/1542-6270(2001)035<0021:lomwf>2.0.co;2

Cited by 4 publications

(5 citation statements)

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“…However, by looking at the literature, it can be observed that the effective concentrations in in vitro studies do vary, depending on the methodology used. Furthermore, the effective concentrations are within those expected in vivo during anti-inflammatory therapy with APA NSAIDs, 2,31) at least for HO˙. HO˙ is one of the most reactive radicals formed at the inflammation sites.…”

Section: Discussionmentioning

confidence: 68%

Antioxidant Activity and Inhibition of Human Neutrophil Oxidative Burst Mediated by Arylpropionic Acid Non-steroidal Anti-inflammatory Drugs

Costa

Moutinho

Lima

et al. 2006

Biological & Pharmaceutical Bulletin

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Section: Discussionmentioning

confidence: 68%

Antioxidant Activity and Inhibition of Human Neutrophil Oxidative Burst Mediated by Arylpropionic Acid Non-steroidal Anti-inflammatory Drugs

Costa

Moutinho

Lima

et al. 2006

Biological & Pharmaceutical Bulletin

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“…1C and data not shown). A useful comparator for the efficacy of tested antibiotics in curing the infected worms is the therapeutic human blood plasma concentration of these compounds, which is 2-20 g͞ml ampicillin, 2.4-4 g͞ml ciprofloxacin, 2.4-4 g͞ml tetracycline, and 5-10 g͞ml vancomycin (24). Thus, for three of the four antibiotics (ciprofloxacin being the exception), the concentrations that promoted nematode survival are equivalent to the desired plasma levels.…”

Section: Resultsmentioning

confidence: 99%

“…In contrast, the effective dose in the C. elegans curing assay of all of the known antibiotics that we tested was severalfold higher than the in vitro MIC. The effective dosage in the nematode model is similar to the therapeutic concentration of most antibiotics in human blood serum, which is typically 5-to 20-fold higher than the MIC (24). Possible explanations for the discovery of highly effective in vivo compounds with the nematode model include the possibilities that (i) the screen selects for compounds that are concentrated in the worm gut, (ii) the C. elegans immune system makes the bacteria more susceptible to inhibition, or (iii) the compounds weaken the integrity of the bacteria so that they are more readily digested.…”

Section: Compounds With a Lower Effective Dose In Vivo Than In Vitromentioning

confidence: 99%

Identification of novel antimicrobials using a live-animal infection model

Moy

Ball

Anklesaria

et al. 2006

Proc. Natl. Acad. Sci. U.S.A.

255

246

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The alarming increase of antibiotic-resistant bacterial pathogens points to the need for novel therapeutic approaches to combat infection. To discover novel antimicrobials, we devised a screen to identify compounds that promoted the survival of the model laboratory nematode Caenorhabditis elegans infected with the human opportunistic pathogen Enterococcus faecalis. E. faecalis colonizes the nematode intestinal tract, forming a persistent lethal infection. Infected nematodes were rescued by antibiotic treatment in a dose-dependent manner, and antibiotic treatment markedly reduced the number of bacteria colonizing the nematode intestine. To facilitate high throughput screening of compound libraries, we adapted a previously developed agar-based C. elegans-E. faecalis infection assay so that it could be carried out in liquid medium in standard 96-well microtiter plates. We used this simple infection system to screen 6,000 synthetic compounds and 1,136 natural product extracts. We identified 16 compounds and 9 extracts that promoted nematode survival. Some of the compounds and extracts inhibited E. faecalis growth in vitro, but, in contrast to traditional antibiotics, the in vivo effective dose of many of these compounds was significantly lower than the minimum inhibitory concentration needed to prevent the growth of E. faecalis in vitro. Moreover, many of the compounds and extracts had little or no affect on in vitro bacterial growth. Our findings indicate that the whole-animal C. elegans screen identifies not only traditional antibiotics, but also compounds that target bacterial virulence or stimulate host defense.antibiotic resistance ͉ chemical genetics ͉ Enterococcus faecalis ͉ antiinfectives

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“…3 It is toxic from 5 to 10 μg mL -1 and its fatal concentration is above 50 μg mL -1 . 4 Therefore, it is important to develop simple and sensitive methods for the determination of this drug.…”

Section: Introductionmentioning

confidence: 99%

Chemiluminescence Determination of Local Anaesthetic Mepivacaine in Human Plasma and Pharmaceuticals

Mokhtari¹

2016

ACSi

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In this study, a new method has been developed for the simple determination of mepivacaine (carbocaine). The method is based on the enhancement effect of mepivacaine in the chemiluminescence (CL) reaction of tris(1,10 phenanthroline)ruthenium(II) with cerium(IV). A mechanism for the CL reaction has been proposed on the basis of UV-Vis, fluorescent and CL spectra. Under optimum conditions, the CL intensity was proportional to the concentration of the drug in solution over the range 0.45-226.25 μg mL -1 (R 2 = 0.9996). The LOD was 0.34 μg mL -1 (S/N = 3). LOD was about 10 times lower than the therapeutic concentration of mepivacaine. The percent of relative standard deviation for determination of 11 replicates at level of 9.05 μg mL -1 and 90.50 μg mL -1 of mepivacaine were 1.8 and 3.7%, respectively. The proposed method was applied successfully for the determination of mepivacaine in human plasma and injectable solutions.

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Lack of Methemoglobinemia with Flutamide

Cited by 4 publications

References 0 publications

Antioxidant Activity and Inhibition of Human Neutrophil Oxidative Burst Mediated by Arylpropionic Acid Non-steroidal Anti-inflammatory Drugs

Antioxidant Activity and Inhibition of Human Neutrophil Oxidative Burst Mediated by Arylpropionic Acid Non-steroidal Anti-inflammatory Drugs

Identification of novel antimicrobials using a live-animal infection model

Chemiluminescence Determination of Local Anaesthetic Mepivacaine in Human Plasma and Pharmaceuticals

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