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Ole Bent Samuelsen - One of the best experts on this subject based on the ideXlab platform.

  • pharmacokinetic data show that oxolinic acid and Flumequine are absorbed and excreted rapidly from plasma and tissues of lumpfish
    Frontiers in Veterinary Science, 2019
    Co-Authors: Gyri Teien Haugland, Bjorn Tore Lunestad, Karen Obrestad Kverme, Rita Hannisdal, Marielle Kallekleiv, Duncan J Colquhoun, Heidrun I Wergeland, Ole Bent Samuelsen
    Abstract:

    This study examined the uptake, tissue distribution and elimination of the antibacterial agents oxolinic acid and Flumequine in lumpfish (Cyclopterus lumpus L.) by use of LC-MS/MS following a single oral administration of 25 mg/kg fish given in feed. Lumpfish are increasingly used as cleaner fish for removal of sea lice on commercially farmed salmon. The production of lumpfish is successful, but there are challenges with bacterial infections and the number of antibacterial treatments has increased in recent years. As the lumpfish is a novel species to farming, there is a need for pharmacokinetic data and establishment of protocols for efficient antibacterial treatment. The current study describes the pharmacokinetic properties of oxolinic acid and Flumequine in lumpfish. Absorption of oxolinic acid was moderate and was characterised by a calculated peak plasma concentration (Cmax) of 2.12 µg/ml after 10.3 hours (Tmax) and an elimination half-life (t1/2) of 21 hours. Area under curve (AUC) and AUC from 0 to 24 hours (AUC0-24h) were calculated to be 60.9 and 34.0 h g/ml, respectively. For Flumequine, plasma Cmax was found to be 2.77 µg/ml after 7.7 h (Tmax) with t1/2 of 22 h. The area under the curve (AUC) and AUC from 0 to 24 hours (AUC0-24h) were calculated as 104.3 and 50.3 h g/ml, respectively. Corresponding Cmax values in muscle, liver and head-kidney for oxolinic acid were 4.01, 3.04 and 4.68 µg/g respectively and Tmax of 11.1, 9.2 and 10.0 h, respectively. For Flumequine, Cmax values of 4.16, 4.01 and 7.48 µg/g were obtained in muscle, liver and head kidney respectively, with corresponding Tmax values of 10.2, 10.3 and 6.0 h. Antimicrobial susceptibility values as determined by minimum inhibitory concentration (MIC) analyses against 28 isolates of Aeromonas salmonicida isolated from diseased lumpfish ranged from 0.06 to 15 µg/ml for oxolinic acid and 0.024 to 6.25 µg/ml for Flumequine. Bimodal distributions in susceptibility to both oxolinic acid and Flumequine were observed. The combination of pharmacokinetic properties and MIC data make possible calculation of efficient treatment doses, which are needed to improve the welfare of lumpfish and minimize development of antibiotic resistant bacteria.

  • efficacy of orally administered Flumequine in the treatment of vibriosis caused by listonella anguillarum in atlantic cod gadus morhua
    Diseases of Aquatic Organisms, 2005
    Co-Authors: Frode Todnem Vikmo, Oivind Bergh, Ole Bent Samuelsen
    Abstract:

    The efficacy of orally administered Flumequine in the treatment of experimentally induced vibriosis in Atlantic cod Gadus morhua was investigated. Cod (mean ± SD, 120 ± 30 g) were randomly distributed to twelve tanks and bath challenged for 1 h with Listonella anguillarum serotype O2α, strain HI-610, using a dose of 9.2 × 10 6 CFU ml -1 . At 3 d post-challenge, medication was introduced in 10 of the groups at doses of 2.5, 5, 10, 15 and 25 mg Flumequine kg -1 body weight d -1 in duplicate. The medication was administered on Days 1, 2, 4, 6, 8, and 10 after the initiation of treatment. In challenged unmedicated fish, mortality started on Day 4 post-challenge, reaching a final cumulative mortality of 82% at Day 18. In the medicated groups, mortality started on Days 3 to 5 post-challenge, reaching final cumulative mortalities of 42, 49, 37, 37 and 23% respectively for the fish treated with 2.5, 5, 10, 15 and 25 mg Flumequine kg -1 body weight d -1 . Survival of medicated fish in all groups was significantly greater than in challenged unmedicated fish (p < 0.001). Twenty-four h following the final medication, HPLC analysis found a linear relationship between doses and mean concentrations of the drug in plasma, muscle and liver.

  • dosage regime experiments with oxolinic acid and Flumequine in atlantic salmon salmo salar l held in seawater
    Aquaculture, 2002
    Co-Authors: Odd F Ellingsen, Astri Rogstad, Christian Syvertsen, Bjorn Midttun, Ole Bent Samuelsen
    Abstract:

    Abstract The absorption and distribution of the two antibacterial agents Flumequine and oxolinic acid were studied during multiple dosing in Atlantic salmon ( Salmo salar ) at two commercial fish farms in Western Norway. Oxolinic acid and Flumequine were administered as Apoxolon Akvaletter® Vet., 5 g/kg and Apoquin Akvaletter® Vet., 5 and 10 g/kg, respectively. Akvaletter® Vet. is a coextruded pellet with an outer layer of a modified fish feed, and a central core containing the active ingredient. In field trial 1, Akvaletter® Vet. were fed by appetite on consecutive days. In field trial 2, Akvaletter® Vet. were fed by appetite every second day on alternate days for 1 week. Commercial feed was fed on the intervening days. Highest mean concentration in plasma, muscle and liver were in the range 1.7–29,2 μg/ml (g). In the trials, Flumequine concentrations were found to be 2–9 times higher than for oxolininc acid. Based on calculated AUC values, it was found that both drugs were well distributed into muscle and liver. An increase in the dose of Flumequine administered led to a reduction in the AUC/dose ratio. Both drugs with both dosage regimes were found to secure high drug concentrations, and will definitely provide effective treatment against sensitive pathogens. The higher concentrations obtained with Flumequine, combined with its high bactericidal activity, should make it the drug of choice. Flumequine at 10 g/kg resulted in reduced appetite when dosed daily. Our recommendations are, therefore, that Flumequine dosed as Akvaletter® Vet. 5 g/kg should be preferred.

  • the efficacy of a single intraperitoneal injection of Flumequine in the treatment of systemic vibriosis in corkwing wrasse symphodus melops
    Journal of Aquatic Animal Health, 2000
    Co-Authors: Ole Bent Samuelsen, Lise Torkildsen, Susanna Husgard, Oivind Bergh
    Abstract:

    Abstract In this investigation, the efficacy of a single intraperitoneal injection of Flumequine in the treatment of systemic vibriosis in corkwing wrasse Symphodus melops was examined. In a population of corkwing wrasse that was experiencing daily mortality, the dominant bacterium cultivated from kidney samples of dead fish was tentatively classified as a species of Vibrio resembling V. splendidus. The infected fish were randomly divided into two groups, each of 60 individuals. Group 1 was treated with Flumequine (25 mg/kg of fish) administered by a single intraperitoneal injection, whereas the fish from group 2 were injected with saline. The mortality was observed daily for 21 d. The cumulative mortality was significantly (P < 0.005) higher in the control group (58%) compared with the medicated group (11%). Bacterial examination of kidneys from dead and surviving fish of both groups indicated the Vibrio to be quickly and effectively eliminated by the antibacterial agent.

  • minimum inhibitory concentrations of chloramphenicol florfenicol trimethoprim sulfadiazine and Flumequine in seawater of bacteria associated with scallops pecten maximus larvae
    Aquaculture, 2000
    Co-Authors: Lise Torkildsen, Ole Bent Samuelsen, Bjorn Tore Lunestad, Oivind Bergh
    Abstract:

    Abstract The purpose of this study was to find the minimum inhibitory concentrations (MIC) for the following antibacterial agents: chloramphenicol, florfenicol, Flumequine and the combination trimethoprim/sulfadiazine to bacteria associated with scallop ( Pecten maximus ) larvae. To evaluate possible effects of components in seawater to the antimicrobial activity of these agents, MIC values were established on Mueller Hinton agar dissolved in either distilled water added 2% NaCl or 25‰ seawater. For Flumequine and trimethoprim/sulfadiazine, the MIC values increased significantly using 25‰ seawater compared to 2% NaCl. Chloramphenicol and florfenicol did not show any significant increase in MIC values using 25‰ seawater compared to 2% NaCl. A significant increase in MIC values was found for chloramphenicol in the second egg group, using 25‰ seawater compared to 2% NaCl. It is concluded that Flumequine, trimethoprim/sulfadiazine and chloramphenicol are, to a varying degree, antagonised by components in seawater.

T.e. Horsberg - One of the best experts on this subject based on the ideXlab platform.

  • Disposition of 14C-Flumequine in sea bream (Sparus auratus) after single intraperitoneal administration
    Food Control, 2017
    Co-Authors: A. Ben Mansour, M.j. Bakke, H. Guerbej, Z. Berriche, M. Samaali, B. Shaikh, J. Sasanya, T.e. Horsberg
    Abstract:

    Abstract This study was conducted to evaluate the pharmacokinetics of Flumequine following intraperitoneal administration of 14 C-Flumequine (12 mg/kg, 100 μCi/kg) in sea bream ( Sparus auratus ). Three fish (147 ± 29 g) were collected at various time points ranging from 0.5 h to 144 h post administration. Absorption, distribution and elimination were studied using whole body autoradiography and liquid scintillation counting whereupon the concentration of Flumequine equivalent versus time was evaluated in major organs and tissues (liver, bile, heart, brain, blood, kidney, intestine, spleen, red and white muscle). An agreement between the data obtained from whole body autoradiography and liquid scintillation counting was observed. A rapid and extensive distribution of Flumequine to the major organs 0.5 h after dosing was recorded. The main route of elimination appeared to be biliary excretion due to the high concentration of radioactivity in the bile and the prolonged elimination phase compared to others tissues. The elimination of Flumequine from the blood followed a two compartmental model with half life of the first phase and second phase being 0.98 h and 21.4 h respectively. The maximum Flumequine recorded in blood (C max ) was 9.09 mg/kg at 0.78 h (T max ). Only traces of drugs were observed in the major tissues of the fish 72 h after administration. Based on the current results and the elimination in edible tissues in particular, Flumequine seems to be an excellent treatment candidate for sea bream.

  • single dose pharmacokinetics of Flumequine in cod gadus morhua and goldsinny wrasse ctenolabrus rupestris
    Journal of Veterinary Pharmacology and Therapeutics, 2000
    Co-Authors: M K Hansen, T.e. Horsberg
    Abstract:

    Knowledge of the pharmacokinetic properties of drugs to combat bacterial infections in cod (Gadus morhua) and wrasse (Ctenolabrus rupestris) is limited. One antimicrobial agent likely to be effective is Flumequine. The aim of this study was to investigate the pharmacokinetic properties of Flumequine in these two species. Flumequine was administered intravenously to cod (G. morhua) at a dose of 5 mg/kg bodyweight and wrasse (C. rupestris) at a dose of 10 mg/kg. Flumequine was also administered orally to both species at a dose of 10 mg/kg body weight, and as a bath treatment at a dose of 10 mg/L water for 2 h. Identical experimental designs were used otherwise. The study was performed in seawater with a salinity of 3.2% and a temperature of 8.0±0.2 °C (cod) and 14.5±0.4 °C (wrasse). Pharmacokinetic modelling of the data showed that Flumequine had quite different pharmacokinetic properties in cod and wrasse. Following intravenous administration, the volumes of distribution at steady-state (Vss) were 2.41 L/kg (cod) and 2.15 L/kg (wrasse). Total body clearances (Cl) were 0.024 L/h.kg (cod) and 0.14 L/h.kg (wrasse) and the elimination half-lives (t1/2 λ z) were calculated to be 75 h (cod) and 31 h (wrasse). Mean residence times (MRT) were 99 h (cod) and 16 h (wrasse). Following oral administration, the t1/2 λ z were 74 h (cod) and 41 h (wrasse). Maximal plasma concentrations (tmax) were 3.5 mg/L (cod) and 1.7 mg/L (wrasse), and were observed 24 h post-administration in cod and 1 h post-administration in wrasse. The oral bioavailabilities (F) were calculated to be 65% (cod) and 41% (wrasse). Following bath administration, maximal plasma concentrations were 0.13 mg/L (cod) and 0.09 mg/L (wrasse), and were observed immediately after the end of the bath.

  • Single‐dose pharmacokinetics of Flumequine in cod (Gadus morhua) and goldsinny wrasse (Ctenolabrus rupestris)
    Journal of Veterinary Pharmacology and Therapeutics, 2000
    Co-Authors: M K Hansen, T.e. Horsberg
    Abstract:

    Knowledge of the pharmacokinetic properties of drugs to combat bacterial infections in cod (Gadus morhua) and wrasse (Ctenolabrus rupestris) is limited. One antimicrobial agent likely to be effective is Flumequine. The aim of this study was to investigate the pharmacokinetic properties of Flumequine in these two species. Flumequine was administered intravenously to cod (G. morhua) at a dose of 5 mg/kg bodyweight and wrasse (C. rupestris) at a dose of 10 mg/kg. Flumequine was also administered orally to both species at a dose of 10 mg/kg body weight, and as a bath treatment at a dose of 10 mg/L water for 2 h. Identical experimental designs were used otherwise. The study was performed in seawater with a salinity of 3.2% and a temperature of 8.0±0.2 °C (cod) and 14.5±0.4 °C (wrasse). Pharmacokinetic modelling of the data showed that Flumequine had quite different pharmacokinetic properties in cod and wrasse. Following intravenous administration, the volumes of distribution at steady-state (Vss) were 2.41 L/kg (cod) and 2.15 L/kg (wrasse). Total body clearances (Cl) were 0.024 L/h.kg (cod) and 0.14 L/h.kg (wrasse) and the elimination half-lives (t1/2 λ z) were calculated to be 75 h (cod) and 31 h (wrasse). Mean residence times (MRT) were 99 h (cod) and 16 h (wrasse). Following oral administration, the t1/2 λ z were 74 h (cod) and 41 h (wrasse). Maximal plasma concentrations (tmax) were 3.5 mg/L (cod) and 1.7 mg/L (wrasse), and were observed 24 h post-administration in cod and 1 h post-administration in wrasse. The oral bioavailabilities (F) were calculated to be 65% (cod) and 41% (wrasse). Following bath administration, maximal plasma concentrations were 0.13 mg/L (cod) and 0.09 mg/L (wrasse), and were observed immediately after the end of the bath.

  • comparative single dose pharmacokinetics of four quinolones oxolinic acid Flumequine sarafloxacin and enrofloxacin in atlantic salmon salmo salar held in seawater at 10 degrees c
    Antimicrobial Agents and Chemotherapy, 1995
    Co-Authors: B Martinsen, T.e. Horsberg
    Abstract:

    Quinolones are currently the most commonly used group of antimicrobial agents in Norwegian aquaculture. The aims of this study were to examine and compare the pharmacokinetic properties of the quinolones oxolinic acid, Flumequine, sarafloxacin, and enrofloxacin after intravascular and oral administration to Atlantic salmon (Salmo salar) by using identical experimental designs. The study was performed in seawater at 10.2 +/- 0.2 degree C with Atlantic salmon weighing 240 +/- 50 g (mean +/- standard deviation). The bioavailability varied considerably among the four quinolones. Following oral administration of medicated feed, the bioavailabilities of oxolinic acid, Flumequine, sarafloxacin, and enrofloxacin were 30.1, 44.7, 2.2, and 55.5%, respectively. Taking the different dosages (25 mg/kg of body weight for oxolinic acid and Flumequine and 10 mg/kg for sarafloxacin and enrofloxacin) into account, enrofloxacin showed the highest maximum concentration in plasma, followed by Flumequine, oxolinic acid, and sarafloxacin. Following intravenous administration, the volumes of distribution at steady state of oxolinic acid, Flumequine, sarafloxacin, and enrofloxacin were 5.4, 3.5, 2.3, and 6.1 liters/kg, respectively. Hence, all the quinolones showed good tissue penetration in Atlantic salmon. The elimination half-life of three of the quinolones, oxolinic acid, Flumequine, and sarafloxacin, was less than or equal to 24 h, with oxolinic acid showing the shortest (18.2 h). On the other hand, the elimination half-life of enrofloxacin was estimated to be 34.2 h, almost twice that of oxolinic acid. This study showed that Flumequine and enrofloxacin had better pharmacokinetic properties, compared with those of oxolinic acid, in Atlantic salmon held in seawater.

Irena M Choma - One of the best experts on this subject based on the ideXlab platform.

  • comparison of deproteinization methods used before tlc db and hplc analysis of Flumequine residues in milk
    Medicinal Chemistry, 2012
    Co-Authors: Irena M Choma, Edyta M Grzelak, Barbara Majer
    Abstract:

    Seventeen various extraction procedures based on precipitation of proteins in milk samples spiked with Flumequine were tested. Several criteria were taken into account, when choosing the most effective. The supernatants were analyzed by thin-layer chromatography – direct bioautography (TLC-DB) and high performance liquid chromatography (HPLC-UV). The results obtained from both methods indicate as the best the same deproteinization procedure. The addition of acetonitrile to milk in 1:1 volume proportions gave the highest concentration of Flumequine in supernatant and prompt coagulation of proteins in milk samples.

  • isocratic reversed phase high performance liquid chromatographic separation of tetracyclines and Flumequine controlled by a chaotropic effect
    Journal of Chromatography A, 2004
    Co-Authors: Karol Pilorz, Irena M Choma
    Abstract:

    Abstract Fast isocratic reversed-phase high-performance liquid charomatographic (RP-HPLC) separation of four tetracyclines and Flumequine was obtained using a Zorbax SB-C 18 column. Baseline resolution was achieved in 11 min. The peaks were narrow, well separated and without any tails although there was no chelating agents added to the mobile phase. Due to the chaotropic effect, the addition of potassium perchlorate allowed controlling the tetracyclines retention while the retention of Flumequine was almost constant.

  • determination of Flumequine in milk by thin layer chromatography bioautography
    Journal of Liquid Chromatography & Related Technologies, 2002
    Co-Authors: Irena M Choma, A Choma, K Staszczuk
    Abstract:

    ABSTRACT Fluoroquinolones are synthetic antibiotics widely used in human and animal medical treatment. Flumequine, belonging to this group, is often used in medical treatment and prevention in livestock. It is also added to feed or water to obtain better weight gain. Many physicochemical techniques have been reported for the assay of fluoroquinolones. Thin-layer chromatography (TLC) is a method of choice for analysis because it is cheap and simple, provides high sample throughput, and requires limited sample pre-treatment. Thin-layer chromatography-bioautography (TLC-B) is the screening technique, which combines TLC with microbiological detection resulting in enhanced sensitivity. In this paper, a simple TLC-B method for determination of Flumequine in milk is described. The sample pre-treatment is performed directly on the plate. Microbiological detection directly on the plate allows for enhanced sensitivity of the method.

J H Boon - One of the best experts on this subject based on the ideXlab platform.

  • influence of Flumequine on in vivo mitogen responses of european eel anguilla anguilla l 1758 lymphoid cells
    Veterinary Immunology and Immunopathology, 1995
    Co-Authors: M H T Van Der Heijden, G H R Booms, M W T Tanck, J H W M Rombout, J H Boon
    Abstract:

    Abstract The influence of Flumequine on mitogen induced lymphoid cell proliferation in European eels ( Anguilla anguilla L., 1758) was studied. For this purpose an in vivo test, using peroral drug administration followed by successive intraperitoneal injections with concanavalin A (ConA) or bacterial lipopolysaccharides (LPS) and 5-bromo-2′-deoxyuridine, was applied. Direct counting of proliferated cells in blood smears revealed that Flumequine possesses mitogenic properties. A synergistic and an antagonistic effect of the drug was observed after LPS and ConA stimulation, respectively. Flow cytometric analysis of peripheral blood lymphoid cells showed a significant reduction of the mean proportion surface immunoglobulin positive cells in the Flumequine-treated animals. It is concluded that Flumequine enhances proliferation of lymphoid cells (probably surface immunoglobulin negative cells) in eel under the present experimental conditions.

  • plasma disposition of Flumequine in common carp cyprinus carpio l 1758 african catfish clarias gariepinus burchell 1822 and european eel anguilla anguilla l 1758 after a single peroral administration
    Aquaculture, 1994
    Co-Authors: M H T Van Der Heijden, H J Keukens, W H F X Van Den Nieuwboer, M J B Mengelers, J H Boon
    Abstract:

    Abstract The disposition of perorally administered Flumequine in plasma was compared between common carp ( Cyprinus carpio L., 1758), African catfish ( Clarias gariepinus Burchell, 1822) and European eel ( Anguilla anguilla L., 1758) respectively, at a dose of 18 mg·kg −1 body weight. All species showed rapid absorption followed by biphasic plasma depletion. Significant interspecies differences were observed for most of the determined pharmacokinetic parameters. Mean highest plasma Flumequine concentrations were 6136 ng·ml −1 in carp, 4074 ng ml −1 in eel and 1179 ng·ml −1 in catfish. Mean distribution and elimination half-lives were 3.4 and 104.3 h for carp, 7.3 and 59.5 h for catfish and 56.7 and 451.2 h for eel. To achieve equivalent drug efficacy and to minimize the probability of residues as a result of medication, dosage regimes and withdrawal periods should be adapted for each species.

  • disposition of Flumequine in plasma of european eel anguilla anguilla after a single intramuscular injection
    Aquaculture, 1991
    Co-Authors: J H Boon, M H T Van Der Heijden, G H R Booms, J M F Nouws, M Degen
    Abstract:

    Abstract The plasma disposition and the excretion of Flumequine, a second generation quinoline derivative, was studied in eel after a single intramuscular administration of 9 mg kg−1. Pharmacokinetic analysis of the plasma concentrations showed that the Flumequine formulation exhibited an extended absorption and elimination half-life of about 33 and 255 h respectively. Slow rates of absorption and tissue distribution, and the absence of biotransformation and active excretion may explain the long drug persistence. This must have consequences for the determination of a proper withdrawal time after treatment of consumable eels with Flumequine.

Henning Gjelstrup Kristensen - One of the best experts on this subject based on the ideXlab platform.

  • bioavailability of Flumequine after oral administration to atlantic salmon salmo salar l
    Aquaculture, 1995
    Co-Authors: Michiel Onne Elema, Kjell Arne Hoff, Henning Gjelstrup Kristensen
    Abstract:

    Abstract The bioavailability of Flumequine was investigated in Atlantic salmon ( Salmo salar L.) in seawater at 6–8 °C. Four types of commercially available medicated fish feed containing Flumequine (5 g kg −1 ) were administered to different groups of salmons (dose: 25 mg kg −1 body weight). The drug was also given as an intravascular bolus injection (dose: 10 mg kg −1 b.w.) and in form of a suspension in water, fish oil or corn oil (dose: 25 mg kg −1 b.w.). Elimination half-lives of 30–40 h were found. The bioavailability of all the tested products was around 40%. Neither the absorption rate, the absorption pattern, nor the presence of feed seemed to have any influence on the bioavailability. The in vitro Flumequine release from the medicated feed pellets was tested using a flow-through apparatus as described in the European Pharmacopoeia. A clear difference in dissolution profile among the four products was seen.

  • multiple dose pharmacokinetic study of Flumequine in atlantic salmon salmo salar l
    Aquaculture, 1994
    Co-Authors: Michiel Onne Elema, Kjell Arne Hoff, Henning Gjelstrup Kristensen
    Abstract:

    Abstract Medicated feed pellets containing Flumequine (5 g/kg) were given to a group of sea-water-adapted Atlantic salmon ( Salmo salar L.). The pellets contained small glass X-ray-dense beads. The fish were offered a fixed quantity of medicated feed during a period of 6 or 8 consecutive days. A control group received non-medicated pellets. Feed intake was assessed by counting the number of beads on X-ray pictures taken of the sampled fish. The results show that almost all the offered feed was eaten by the fish. No difference in appetite could be detected between the medicated and non-medicated feed groups. Plasma samples were taken each day of the medication period and for 8 days following medication. Tissue samples (liver, muscle and skin) were taken every 2nd day. A steady-state level of Flumequine in plasma, liver and muscle tissue was achieved on the 3rd day of medication. The estimated elimination half-life in plasma, liver and muscle tissue was about 21 h. Half-life in skin tissue was approx. 33 h, and therefore it took longer to reach a steady-state level. Skin tissue data show an accumulation of Flumequine during the medication period ranging from 14 μg/g on the 2nd day to 26 μg/g on the 8th day. The highest Flumequine concentrations were observed in skin tissue and liver tissue. Flumequine level in muscle tissue was approx. half that found in skin tissue. Water temperature remained approx. 8°C during the whole experiment. The Flumequine concentrations observed should give good protection against the most common pathogenic bacteria in European fish farming, which can be concluded by comparison with minimal inhibitory concentrations (MICs) as listed in literature.