The influence of age on the pharmacokinetics of aditoprim in pigs after intravenous and oral administration

Riond, J.‐L.; Müller, P; Wanner, M.

doi:10.1007/bf01839185

Cited by 11 publications

(13 citation statements)

References 24 publications

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“…ADP has excellent pharmacokinetic characteristics. Previous studies have shown that ADP has longer elimination half lives (3.3~14.8 h) and higher distribution volumes (4.6~10.4 L/kg) than those of TMP in pig, calf, monkey, sheep and some other animal species 5 6 7 8 9 10 11 12 13 14 15 16 17 , and a similar pattern is observed for ADP where the distribution volume is about four times higher than that of TMP. For the poor pharmacokinetics 18 and the development of antibacterial resistance 19 20 21 , TMP is often used in combination with sulfonamides as antibacterial synergist for the treatment and prevention of bacterial infections in veterinary and human medicine 22 .…”

supporting

confidence: 56%

The antibacterial activities of aditoprim and its efficacy in the treatment of swine streptococcosis

Cheng

Zhu

et al. 2017

Sci Rep

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Aditoprim (ADP) has potential use as an antimicrobial agent in animals. However, its pharmacodynamic properties have not been systematically studied yet. In this study, the in vitro antibacterial activities of ADP and its main metabolites were assayed, and the in vivo antibacterial efficacy of ADP for the treatment of swine streptococcosis was evaluated. It was shown that Salmonella and Streptococcus from swine, Escherichia coli and Salmonella from chickens, E. coli, Streptococcus, Mannheimia, Pasteurella from calves, Streptococcus and Mannheimia from sheep, and E. coli, Flavobacterium columnare, Acinetobacter baumannii and Yersinia ruckeri from fishes were highly susceptible to ADP. Haemophilus parasuis from swine, Staphylococcus aureus, Aeromonas punctate, Mycobacterium tuberculosis, Streptococcus agalactiae from fishes, and Klebsiella from calves and sheep showed moderate susceptibility to ADP, whereas E. coli, Actinobacillus pleuropneumonia, Pasteurella, S. aureus, Clostridium perfringens from swine, S. aureus, C. perfringens from chickens, and S. aureus from calves were resistant to ADP. The main metabolites of ADP showed equal activity to that of their parent compound, and the prevention and therapeutic dosages of ADP recommended for swine streptococcosis were 10 and 20~40 mg/kg b.w., respectively. This study firstly showed that ADP had strong antibacterial activity and had potential to be used as a single drug in the treatment of bacterial infectious diseases.

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confidence: 56%

The antibacterial activities of aditoprim and its efficacy in the treatment of swine streptococcosis

Cheng

Zhu

et al. 2017

Sci Rep

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“…The pharmacokinetics of aditoprim, a reversible dihydrofolate reductase inhibitor in the preclinical study phase, have already been documented in cattle (Ludwig et ah, 1985;Jordan et ah, 1987;Lohuis et al, 1992;Sutter et al, 1993), sheep (Hanni et al, 1987), goats (Knoppert et al, 1988), pigs (Ludwig et al, 1985;Riond et al, 1992), horses (von Fellenberg et al, 1990), and dogs (Sutter et al, 1991). In these species, aditoprim is characterized by a long plasma elimination half-life ranging from 6.7 to 12.5 h and a volume of distribution larger than 4.4 L/kg.…”

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confidence: 99%

Research Note: Pharmacokinetics of Aditoprim in Turkeys After Intravenous and Oral Administration

1993

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The pharmacokinetics of aditoprim, a not yet commercialized selective reversible inhibitor of dihydrofolate reductase, were determined in turkeys after intravenous (5 mg/kg BW) and oral (5.46 +/- .44 mg/kg BW) administration. The mean (+/- SD) total body clearance of 26.9 +/- 2.3 mL/min per kg BW was high when compared with that determined for other species, presumably a consequence of the higher metabolic rate of birds. Consequently, mean aditoprim elimination half-life was relatively short (3.3 +/- .2 h). As determined in mammalian species, the apparent volume of distribution at steady state was large. Aditoprim in drinking water (100 and 300 mg/L water) provided plasma concentrations between .08 and .19 micrograms/mL. Circadian rhythms with highest concentrations in the late afternoon and lowest concentrations in the morning were observed. Despite its short elimination half-life, aditoprim may still be a valuable antimicrobial for use in avian medicine pending safety, efficacy, and residue depletion studies.

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“…It is reported that this compound is particularly active against Enterobacteriaceae , Haemophilus , Staphylococcus , Streptococcus , Vibrio , and Aeromonas 2 . Moreover, ADP provides significant pharmacokinetic advantages, including long half-lives (6.1–11.9 h) and high tissue distribution volume (4.4–12.2 L/kg) in various animal species such as sheep 3 4 5 , cattle 6 7 8 9 , pig 10 , horse 11 , turkey 12 , dog 13 , and monkey 14 . These earlier studies have shown that ADP had a good efficacy when administered alone or combined with sulfonamides in a one-day dose for the treatment of respiratory and gastro-intestinal infections.…”

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Metabolism and Disposition of Aditoprim in Swine, Broilers, Carp and Rats

Wang

Huang

Pan

et al. 2016

Sci Rep

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Aditoprim (ADP) is a newly developed antibacterial agent in veterinary medicine. The metabolism and disposition of ADP in swine, broilers, carp and rats were investigated by using a radio tracer method combined with a radioactivity detector and a liquid chromatography/ion trap/time-of-flight mass spectrometry. After a single oral administration, more than 94% of the dose was recovered within 14 d in the four species. The urine excretion was dominant in swine and rats, making up 78% of the dose. N-monodesmethyl-ADP, N-didesmethyl-ADP, and 10 new metabolites were characterized. These metabolites were biotransformed from the process of demethylation, α-hydroxylation, N-oxidation, and NH2-glucuronidation. After an oral dose for 7 d, ADP-derived radioactivity was widely distributed in tissues, and high concentrations were especially observed in bile, liver, kidney, lung, and spleen. The radioactivity in the liver was eliminated much more slowly than in other tissues, with a half-life of 4.26, 3.38, 6.69, and 5.21 d in swine, broilers, carp, and rats, respectively. ADP, N-monodesmethyl-ADP, and N-didesmethyl-ADP were the major metabolites in edible tissues. Notably, ADP was detected with the highest concentration and the longest duration in these tissues. These findings indicated that ADP is the marker residue and the liver is the residue target tissue.

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The influence of age on the pharmacokinetics of aditoprim in pigs after intravenous and oral administration

Cited by 11 publications

References 24 publications

The antibacterial activities of aditoprim and its efficacy in the treatment of swine streptococcosis

The antibacterial activities of aditoprim and its efficacy in the treatment of swine streptococcosis

Research Note: Pharmacokinetics of Aditoprim in Turkeys After Intravenous and Oral Administration

Metabolism and Disposition of Aditoprim in Swine, Broilers, Carp and Rats

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