Pharmacokinetics, bioavailability, plasma protein binding and disposition of nalidixic acid in Rainbow Trout (Oncorhynchus mykiss)

Jarboe, Herman H.; Toth, Bruce R.; Shoemaker, Kathy E.; Greenlees, Kevin J.; Kleinow, Kevin M.

doi:10.3109/00498259309057035

Cited by 13 publications

(3 citation statements)

References 19 publications

(21 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Previous pharmacokinetic studies of enrofloxacin in finfish have been limited to multiple temperature and dose administration trials in rainbow trout (Bowser et al, 1992). Other quinolone and fluoroquinolone antimicrobials subject to pharmacokinetic examination in finfish include nalidixic acid (Uno et al, 1992;Jarboe et al, 1993), oxolinic acid (Bjorklund & Byland, 1991;Hustvedt et al, 1991;Ishida, 1992;Kleinow et al, 1994), flumequine (Sohlberg et al, 1990;Rogstad et al, 1993), sarafloxacin (Martinsen et al, 1993a,b;Martinsen et al, 1994), and difloxacin (Elston et al, 1994).…”

mentioning

confidence: 99%

Multiple route and dose pharmacokinetics of enrofloxacin in juvenile Atlantic salmon

Stoffregen

Wooster

Bustos

et al. 1997

Vet Pharm & Therapeutics

View full text Add to dashboard Cite

The fluoroquinolone antibacterial family is a relatively recent group of bactericidal compounds, generally characterized by efficacy against a wide spectrum of bacterial organisms and exhibiting minimal adverse effects in treated patients. The fluoroquinolones are widely prescribed in both human and veterinary medicine, though in veterinary medicine in the USA there are currently only two approved compounds, enrofloxacin (Baytril, Bayer Animal Health, Shawnee Mission, KS) and sarafloxacin (SaraFlox, Abbott Laboratories, North Chicago, IL), both with limited species and disease label approvals. Currently, there are no approved fluoroquinolone antibacterials to treat bacterial infectious diseases in cultured fish species. Enrofloxacin was administered to juvenile Atlantic salmon as a single bolus via intraarterial (i.a.), intraperitoneal (i.p.), intramuscular (i.m.), or oral gavage routes of administration. The drug was administered via the first three routes to achieve a dose of 10 mg/kg, and via oral gavage to achieve both 10 (p.o.-10) and 5 (p.o.-5) mg/kg doses. Two-compartment model kinetics were observed with elimination of half-lives (t1/2) of 130.6, 34.32, 84.98, 105.11, and 48.24 h, area under the drug concentration-time curves (AUC) of 84.3, 75.31, 55.61, 41.68, and 38.81 micrograms x h/mL, and bioavailabilities (F) of 100, 89.34, 65.97, 49.44, and 46.04% (i.a., i.p., i.m., p.o.-10, p.o.-5, respectively). All administration routes at 10 mg/kg were found to yield comparable drug concentration-time curves for multiple tissue, indicating no distinct advantage of using one route over another from a kinetics perspective. Finally, the 5 mg/kg dose (p.o.-5) yielded comparable multiple tissue drug concentration-time curves to the 10 mg/kg dose (p.o.-10), providing pharmacokinetic evidence to justify therapeutic efficacy trials with the lower dose.

show abstract

mentioning

confidence: 99%

Multiple route and dose pharmacokinetics of enrofloxacin in juvenile Atlantic salmon

Stoffregen

Wooster

Bustos

et al. 1997

Vet Pharm & Therapeutics

View full text Add to dashboard Cite

show abstract

“…The three basic drugs tested (metoprolol, propranolol, venlafaxine) were overall more closely matched to human values, with a difference range of 1.7 to 3.3‐fold (Henneberger et al, 2022). Similarly, the antibiotic nalidixic acid is 74% unbound in the plasma of rainbow trout (Jarboe et al, 1983), but only 7% unbound in human plasma (Portmann et al, 1966). Although our data note a closer relationship between binding values for diltiazem in rainbow trout and human plasma, it is clear that extrapolating plasma protein binding values from mammalian studies may misrepresent the chemical partitioning characteristics in fish.…”

Section: Discussionmentioning

confidence: 99%

Factors Affecting the Binding of Diltiazem to Rainbow Trout Plasma: Implications for the Risk Assessment of Pharmaceuticals in Aquatic Systems

Glover

Klaczek

Goss

et al. 2022

Enviro Toxic and Chemistry

View full text Add to dashboard Cite

The accumulation of organic toxicants in fish plasma, and how they partition between the bound and unbound fraction once absorbed, are important metrics in models that seek to predict the risk of such contaminants in aquatic settings. Rapid equilibrium dialysis of diltiazem, an ionizable weak base and important human pharmaceutical contaminant of freshwaters, was conducted with rainbow trout (Oncorhynchus mykiss) plasma. The effect of fed state, fish sex, fish strain/size, and dialysis buffer pH on the binding of radiolabeled diltiazem (9 ng ml −1 ) was assessed. In fed fish, 24.6%-29.5% of diltiazem was free, unbound to plasma proteins. Although starvation of fish resulted in a decrease in plasma protein, the bound fraction of diltiazem remained relatively constant. Consequently, the protein-bound concentration of diltiazem increased with length of starvation. In general, rainbow trout strain was a significant factor affecting plasma binding, although the two strains tested also differed markedly in size. Dialysis buffer pH significantly influenced plasma binding, with a higher unbound diltiazem fraction at pH 6.8 than pH 8.0. These data indicate that empirical measures of plasma binding in fish are important for accurate risk assessment and that the physiological status of a fish is likely to impact its sensitivity to toxicants such as diltiazem.

show abstract

“…Collections of experimental binding data and also predictive models are abundant for human plasma (Kratochwil et al 2002; Fasano et al 2005; Zhang et al 2012), but only a few studies have measured binding to fish plasma (Schmieder and Henry 1988; Jarboe et al 1993; Schultz et al 2001; Reimschuessel et al 2005; Fitzsimmons et al 2009; Escher et al 2011; Nichols et al 2013). Serum albumin determines the free fraction of the majority of drugs in human plasma (Fanali et al 2012), but binding to lipid components and glycoproteins can also contribute to plasma binding.…”

Section: Introductionmentioning

confidence: 99%

Trout and Human Plasma Protein Binding of Selected Pharmaceuticals Informs the Fish Plasma Model

Henneberger

Klüver

Mühlenbrink

et al. 2020

Enviro Toxic and Chemistry

View full text Add to dashboard Cite

Concerns are increasing that pharmaceuticals released into the environment pose a risk to nontarget organism such as fish. The fish plasma model is a read-across approach that uses human therapeutic blood plasma concentrations for estimating likely effects in fish. However, the fish plasma model neglects differences in plasma protein binding between fish and humans. Because binding data for fish plasma are scarce, the binding of 12 active pharmaceutical ingredients (APIs; acidic, basic, and neutral) to rainbow trout (Oncorhynchus mykiss) and human plasma was measured using solidphase microextraction (SPME). The plasma/water distribution ratios (D plasma/w ) of neutral and basic APIs were similar for trout and human plasma, differing by no more than a factor of 2.7 for a given API. For the acidic APIs, the D plasma/w values of trout plasma were much lower than for human plasma, by up to a factor of 71 for naproxen. The lower affinity of the acidic APIs to trout plasma compared with human plasma suggests that the bioavailability of these APIs is higher in trout. Read-across approaches like the fish plasma model should account for differences in plasma protein binding to avoid overor underestimation of effects in fish. For the acidic APIs, the effect ratio of the fish plasma model would increase by a factor of 5 to 60 if the unbound plasma concentrations were used to calculate the effect ratio. Environ Toxicol Chem 2020;00:1-10.

show abstract

Pharmacokinetics, bioavailability, plasma protein binding and disposition of nalidixic acid in Rainbow Trout (Oncorhynchus mykiss)

Cited by 13 publications

References 19 publications

Multiple route and dose pharmacokinetics of enrofloxacin in juvenile Atlantic salmon

Multiple route and dose pharmacokinetics of enrofloxacin in juvenile Atlantic salmon

Factors Affecting the Binding of Diltiazem to Rainbow Trout Plasma: Implications for the Risk Assessment of Pharmaceuticals in Aquatic Systems

Trout and Human Plasma Protein Binding of Selected Pharmaceuticals Informs the Fish Plasma Model

Contact Info

Product

Resources

About