Pharmacokinetic parameters and milk concentrations of ketoprofen after administration as a single intravenous bolus dose to lactating goats

Musser, Jeffrey M.B.; Anderson, Kevin L.; Tyczkowska, Krystyna

doi:10.1046/j.1365-2885.1998.00148.x

Cited by 14 publications

(5 citation statements)

References 21 publications

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“…The KTP in beetal goats can be repeated after 12 hours because the drug was not detected in plasma at 12 th hour. The results of this study are in line with previous findings, that 2.47mg/kg BW dosage is appropriate in goats (Banting et al, 2008;Singh et al, 2009;Riviere and Papich, 2017) and can be repeated after 12 hours (Musser et al, 1998;Landoni et al, 1999;Arifah et al, 2003).…”

Section: Discussionsupporting

confidence: 92%

“…The pharmacokinetic parameters calculated in this study were maximum concentration (Cmax) 13.64±0.98µg/ml, clearance (Cl) 0.325±0.02 L/h/kg, Volume of distribution (VD) 1.40±0.132L/kg, Steady state volume of distribution (VDss) 0.50±0.09L/kg, half-life (t1/2) 3.10±0.37hrs and Elimination constant (Kel) 2.09±0.292L/hr. These results are similar and comparable with Musser et al (1998) who determined the pharmacokinetic parameters of Ketoprofen after single IV administration at the dosage of 2.2 mg/kg of BW in Toggenburg goats.…”

Section: Discussionsupporting

confidence: 90%

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Pharmacokinetic Evaluation and Dosage Optimization of Ketoprofen in Healthy Beetal Goats

Rehman¹

2019

PVJ

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Section: Discussionsupporting

confidence: 92%

Section: Discussionsupporting

confidence: 90%

Pharmacokinetic Evaluation and Dosage Optimization of Ketoprofen in Healthy Beetal Goats

Rehman¹

2019

PVJ

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“…The higher and earlier C max of (S)-(+)-KTP than MLX, shown in Figure 3, suggests that KTP may be of more bene¢t in the treatment of the acute in£ammatory disorders, although the e¡ects of the NSAIDs are not directly related to the plasma concentrations (Lascelles et al,1998;Musser et al,1998). If MLX is the drug of choice for other reasons, it should be given by the subcutaneous or intramuscular routes, which are signi¢cantly better than the oral route with respect to time of onset of action (Busch et al, 1998;Eullar-Ziegler et al, 2001).…”

Section: Discussionmentioning

confidence: 99%

A Pharmacokinetic Comparison of Meloxicam and Ketoprofen following Oral Administration to Healthy Dogs

et al. 2004

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Ketoprofen (KTP) and meloxicam (MLX) are non-steroidal anti-inflamatory drugs used extensively in veterinary medicine. The pharmacokinetics of these drugs were studied in eight dogs following a single oral dose of 1 mg/kg of KTP as a racemate or 0.2 mg/kg of MLX. The concentrations of the drugs in plasma were determined by high-performance liquid chromatography (HPLC). There were differences between the disposition curves of the KTP enantiomers, confirming that the pharmacokinetics of KTP is enantioselective. (S)-(+)-KTP was the predominant enantiomer; the S:R ratio in the plasma increased from 2.58 +/- 0.38 at 15 min to 5.72 +/- 2.35 at 1 h. The area under the concentration time curve (AUC) of (S)-(+)-KTP was approximately 6 times greater than that of (R)-(-)-KTP. The mean (+/- SD) pharmacokinetic parameters for (S)-(+)-KTP were characterized as Tmax = 0.76 +/- 0.19 h, Cmax = 2.02 +/- 0.41 microg/ml, t1/2el = 1.65 +/- 0.48 h, AUC = 6.06 +/- 1.16 microg.h/ml, Vd/F = 0.39 +/- 0.07 L/kg, Cl/F = 170 +/- 39 ml/(kg.h). The mean (+/- SD) pharmacokinetic parameters of MLX were Tmax = 8.5 +/- 1.91 h, Cmax = 0.82 +/- 0.29 microg/ml, t1/2lambda(z) = 12.13 +/- 2.15 h, AUCinf = 15.41 +/- 1.24 microg.h/ml, Vd/F = 0.23 +/- 0.03 L/ kg, and Cl/F = 10 +/- 1.4 ml/(kg.h). Our results indicate significant pharmacokinetic differences between MLX and KTP after therapeutic doses.

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“…To our knowledge, there are no published pharmacokinetic data after administration of the separate KTP enantiomers in the goat and only one publication on pharmacokinetics after administration of the racemate (Musser et al ., 1998), which, however, reported only ‘total drug’ concentrations and pharmacokinetic variables derived from these concentrations. The use of total drug concentrations fails to recognize that racemates are mixtures of two drugs that almost invariably differ in pharmacokinetic and pharmacodynamic properties.…”

Section: Introductionmentioning

confidence: 99%

Pharmacodynamics, chiral pharmacokinetics and PK–PD modelling of ketoprofen in the goat

Arifah¹,

Landoni²,

Lees³

2003

Vet Pharm & Therapeutics

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There have been few studies of the pharmacodynamics of nonsteroidal antiinflammatory drugs (NSAIDs) using PK-PD modelling, yet this approach offers the advantage of defining the whole concentration-effect relationship, as well as its time course and sensitivity. In this study, ketoprofen (KTP) was administered intravenously to goats as the racemate (3.0 mg/kg total dose) and as the single enantiomers, S(+) KTP and R(-) KTP (1.5 mg/kg of each). The pharmacokinetics and pharmacodynamics of KTP were investigated using a tissue cage model of acute inflammation. The pharmacokinetics of both KTP enantiomers was characterized by rapid clearance, short mean residence time (MRT) and low volume of distribution. The penetration of R(-) KTP into inflamed (exudate) and noninflamed (transudate) tissue cage fluids was delayed but area under the curve values were only slightly less than those in plasma, whereas MRT was much longer. The S(+) enantiomer of KTP penetrated less readily into exudate and transudate. Unidirectional inversion of R(-) to S(+) KTP occurred. Both rac-KTP and the separate enantiomers produced marked inhibition of serum thromboxane B2 (TxB2) synthesis (ex vivo) and moderate inhibition of exudate prostaglandin E2 (PGE2) synthesis (in vivo); pharmacodynamic variables for S(+) KTP were Emax (%) = 94 and 100; IC50 (microg/mL) = 0.0033 and 0.0030; N = 0.45 and 0.58, respectively, where Emax is the maximal effect, IC50 the plasma drug concentration producing 50% of Emax and N the slope of log concentration/effect relationship. The IC50 ratio, serum TxB2:exudate PGE2 was 1.10. Neither rac-KTP nor the individual enantiomers suppressed skin temperature rise at, or leucocyte infiltration into, the site of acute inflammation. These data illustrate for KTP shallow concentration-response relationships, probable nonselectivity of KTP for cyclooxygenase (COX)-1 and COX-2 inhibition and lack of measurable effect on components of inflammation.

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Pharmacokinetic parameters and milk concentrations of ketoprofen after administration as a single intravenous bolus dose to lactating goats

Cited by 14 publications

References 21 publications

Pharmacokinetic Evaluation and Dosage Optimization of Ketoprofen in Healthy Beetal Goats

Pharmacokinetic Evaluation and Dosage Optimization of Ketoprofen in Healthy Beetal Goats

A Pharmacokinetic Comparison of Meloxicam and Ketoprofen following Oral Administration to Healthy Dogs

Pharmacodynamics, chiral pharmacokinetics and PK–PD modelling of ketoprofen in the goat

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