scholarly journals Comparative Pharmacokinetics of Levofloxacin in Healthy and Renal Damaged Muscovy Ducks following Intravenous and Oral Administration

2014 ◽  
Vol 2014 ◽  
pp. 1-6 ◽  
Author(s):  
Mohamed Aboubakr ◽  
Ahmed Soliman

The pharmacokinetics aspects of levofloxacin were studied in healthy and experimentally renal damaged Muscovy ducks after single intravenous (IV) and oral (PO) dose of 10 mg kg−1 bwt. Following IV administration, elimination half-life (t1/2(β)) and mean residence time (MRT) were longer in renal damaged ducks than in healthy ones. Total clearance(Cltot)in renal damaged ducks (0.20 L kg−1 h−1) was significantly lower as compared to that in healthy ones (0.41 L kg−1 h−1). Following PO administration, the peak serum concentration(Cmax)was higher in renal damaged than in healthy ducks and was achieved at maximum time(tmax)of 2.47 and 2.05 h, respectively. The drug was eliminated (t1/2(el)) at a significant slower rate (3.94 h) in renal damaged than in healthy ducks (2.89 h). The pharmacokinetic profile of levofloxacin is altered in renal damaged ducks due to the increased serum levofloxacin concentrations compared with that in clinically healthy ducks. Oral administration of levofloxacin at 10 mg kg−1 bwt may be highly efficacious against susceptible bacteria in ducks. Also, the dose of levofloxacin should be reduced in renal damaged ducks. Pharmacokinetic/pharmacodynamic integration revealed significantly higher values forCmax/MIC and AUC/MIC ratios in renal damaged ducks than in healthy ones, indicating the excellent pharmacokinetic characteristics of levofloxacin in renal damaged ducks.

Author(s):  
Gabriela A. Albarellos ◽  
Laura Montoya ◽  
Graciela A.A. Denamiel ◽  
Sabrina M. Passini ◽  
María F. Landoni

The aim of the present study was to describe the plasma pharmacokinetic profile and skin concentrations of lincomycin after intravenous administration of a 15% solution and oral administration of 300 mg tablets at a dosing rate of 15 mg/kg to cats. Susceptibility of staphylococci (n = 31) and streptococci (n = 23) strains isolated from clinical cases was also determined. Lincomycin plasma and skin concentrations were determined by microbiological assay using Kocuria rhizophila ATCC 9341 as test microorganism. Susceptibility was established by the antimicrobial disc diffusion test. Individual lincomycin plasma concentration–time curves were analysed by a non-compartmental approach. After intravenous administration, volume of distribution, body clearance and elimination half-life were 0.97 L/kg ± 0.15 L/kg, 0.17 L/kg ± 0.06 L/h.kg and 4.20 h ± 1.12 h, respectively. After oral administration, peak plasma concentration, time of maximum plasma concentration and bioavailability were 22.52 µg/mL ± 10.97 µg/mL, 0.80 h ± 0.11 h and 81.78% ± 24.05%, respectively. Two hours after lincomycin administration, skin concentrations were 17.26 µg/mL ± 1.32 µg/mL (intravenous) and 16.58 µg/mL ± 0.90 µg/mL (oral). The corresponding skin: plasma ratios were 2.08 ± 0.47 (intravenous) and 1.84 ± 0.97 (oral). The majority of staphylococci and streptococci tested in this study were susceptible to lincosamides (87.09% and 69.56%, respectively). In conclusion, lincomycin administered orally at the assayed dose showed a good pharmacokinetic profile, with a long elimination half-life and effective skin concentration. Therefore, it could be a good first option for treating skin infections in cats.


1970 ◽  
Vol 64 (2) ◽  
pp. 228-252 ◽  
Author(s):  
E. Gerhards ◽  
H. Röpke ◽  
P. E. Schulze ◽  
H. Hitze

ABSTRACT The metabolism and pharmacokinetics (biodynamics) of 1,2α-methylene-[14C]-6-chloro-pregna-4,6-dien-17α-ol-3,20-dione (Cyproterone; Cy) have been investigated in man following intravenous and oral administration. The principal metabolite in the plasma following the intravenous and oral administration is 1,2α-methylene-6-chloro-pregna-4,6-diene-17α,20α-diol-3-one (20α-OH-Cy). After a single oral dose of 100 mg Cy, the concentration of unchanged free Cy during the first 24 hours is about 1 μg/100 ml plasma. Of 100 mg Cy administered p. o., only about 40% was absorbed, 60% being eliminated in the faeces. In the urine, 20α-OH-Cy and 1,2α-methylene-6-chloro-androst-4,6-diene-3,17-dione(17-keto-Cy) were isolated and identified as the principal metabolites. About 60% of the radioactivity in the urine, following oral and intravenous administration of [14C]-Cy, is present in the form of watersoluble compounds (conjugates) which cannot be decomposed either with enzymes (β-glucuronidase, sulphatase) or by means of cold or hot acid hydrolysis. Decomposition by solvolysis with perchloric acid in ethyl acetate, however, is quantitative. On the basis of simulation performed with an analogue computer, the elimination half-life of the deep compartments following intravenous or oral administration of Cy would be between 3 and 5 days, on the basis of 14C-activity. 'Oral administration' of 100 mg Cy daily, as simulated on the analogue computer, is cumulative; an equilibrium in the deep compartment being reached only after about 28 days and that in the blood after about 14 days.


2021 ◽  
Vol 8 ◽  
Author(s):  
Ricardo Videla ◽  
Carla Sommardahl ◽  
Joe Smith ◽  
Deanna M. W. Schaefer ◽  
Sherry Cox

This study aimed to determine the pharmacokinetics of prednisolone following intravenous and oral administration in healthy adult alpacas. Healthy adult alpacas were given prednisolone (IV, n = 4), as well as orally (PO, n = 6). Prednisolone was administered IV once (1 mg/kg). Oral administration was once daily for 5 days (2 mg/kg). Each treatment was separated by a minimum 4 month washout period. Samples were collected at 0 (pre-administration), 0.083, 0.167, 0.25, 0.5, 0.75, 1, 2, 4, 8, 12, and 24 h after IV administration, and at 0 (pre-administration), 0.25, 0.5, 0.75, 1, 2, 4, 8, 12, 24 after the first and 5th PO administration. Samples were also taken for serial complete blood count and biochemistry analysis. Prednisolone concentration was determined by high pressure liquid chromatography. Non-compartmental pharmacokinetic parameters were then determined. After IV administration clearance was 347 mL/kg/hr, elimination half-life was 2.98 h, and area under the curve was 2,940 h*ng/mL. After initial and fifth oral administration elimination half-life was 5.27 and 5.39 h; maximum concentration was 74 and 68 ng/mL; time to maximum concentration was 2.67 and 2.33 h; and area under the curve was 713 and 660 hr*ng/mL. Oral bioavailability was determined to be 13.7%. Packed cell volume, hemoglobin, and red blood cell counts were significantly decreased 5 days after the first PO administration, and serum glucose was significantly elevated 5 days after the first PO administration. In conclusion, serum concentrations of prednisolone after IV and PO administration appear to be similar to other veterinary species. Future research will be needed to determine the pharmacodynamics of prednisolone in alpacas.


DICP ◽  
1989 ◽  
Vol 23 (6) ◽  
pp. 451-455 ◽  
Author(s):  
Sally Usdin Yasuda ◽  
Karen J. Tietze

Nimodipine, a calcium-channel antagonist with a relatively selective vasodilatory effect on cerebral blood vessels, has recently been approved for improvement of neurologic deficits due to spasm following subarachnoid hemorrhage. Nimodipine has low oral bioavailability (2.7–27.9 percent), a short half-life (2 h), is highly protein bound (98–99 percent), and is hepatically metabolized. Clinical studies have evaluated topical, intravenous, and oral administration of nimodipine for the treatment of cerebral artery spasm associated with subarachnoid hemorrhage. These studies document some benefit of the drug in reducing the occurrence of severe neurologic deficit, although this effect is not universal. Few adverse effects have been noted. Further studies are necessary to evaluate the pharmacologic and pharmacokinetic characteristics, the appropriate dose and route of administration, adverse effects, drug interactions, and the therapeutic efficacy of nimodipine before routine use can be recommended.


2016 ◽  
Vol 4 (2) ◽  
pp. 150
Author(s):  
Mohamed El-Hewaity

The disposition kinetic of tilmicosin (25mg/kg) was studied following oral administration alone, pretreated with amprolium (240 ppm), pretreated with diclazuril (2.5 ppm) and pretreated with toltrazuril (25 ppm) in broiler chickens. The serum tilmicosin concentrations were determined by microbiological assay technique using Bacillus subtilis (ATCC 6633) as the test organism. Following oral administration of tilmicosin, the disposition curve was best described by two-compartment open model. The maximum serum concentration (Cmax) was 1.90 ± 0.11, 1.27 ± 0.13, 1.50 ± 0.14 and 1.41 ± 0.11µg/ml for tilmicosin alone and in the presence of amprolium, diclazuril and toltrazuril, respectively. The elimination half-life (T0.5 (el)) was significantly decreased (5.28 ± 0.30, 5.88 ± 0.33, 6.03 ± 0.25 h, respectively) in amprolium, diclazuril and toltrazuril pretreated broiler chicken compared to tilmicosin alone (7.30 ± 0.41 h). The outcomes illustrated a significant decrease in the interval between doses in amprolium, diclazuril and toltrazuril pretreated broiler chicken compared to tilmicosin alone. Amprolium diclazuril and toltrazuril, resulted in a significance decrease in AUC (12.02 ± 1.14, 15.50 ± 1.26 and 14.56 ± 1.46 µg.h.ml-1, respectively) compared to tilmicosin alone (21.98±1.83 µg.h.ml-1). It is concluded that the administration of amprolium, diclazuril and toltrazuril before tilmicosin would altered its pharmacokinetic profile in broiler chicken.


2020 ◽  
Vol 19 (8) ◽  
pp. 1735-1758
Author(s):  
Ifeanyi G. Eke ◽  
Ukamaka U. Eze ◽  
Aruh O. Anaga ◽  
Kennedy F. Chah ◽  
Boniface M. Anene ◽  
...  

Purpose: To evaluate the disposition kinetics of ceftriaxone (CFZ) in dogs with a view to determining its therapeutic dose and dosing frequency.Methods: Twelve (12) Basenji dogs (n = 4), divided into 3 groups (A, B and C), were used for the study. Ceftriaxone was administered intramuscularly at doses of 12.5, 25, and 50 mg/kg once to groups A, B and C respectively. Plasma CFZ concentration was determined by agar well diffusion assay at 0.25, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, and 24 h post-treatment, and the pharmacokinetic parameters were determined.Results: Intramuscular injection of CFZ to dogs resulted in rapid absorption, distribution and elimination (p < 0.05). The elimination half-life was short and did not change significantly with increase in dose. Serum concentration of CFZ changed significantly (p < 0.05) with increase in dose of CFZ. The maximum serum concentration (Cmax, 15.00 ± 1.18, 141.37 ± 15.87 and 259 ± 5.21 μg/mL) for groups A, B and C respectively were significantly (p < 0.05) different. The steady state CFZ concentrations; 0.94, 8.81 and 16.19 μg/mL for groups A, B and C, respectively, were significantly (p < 0.05) different. However, there was no significant difference in the time to reach steady state concentrations (Tmax, 00±0.021, 4.00±0.10 and 4.30±0.12 for groups A, B and C respectively). The therapeutic dose of CFZ was therefore determined to be 25 – 50 mg/kg every 4 h.Conclusion: Ceftriaxone undergoes rapid elimination in dogs with a short elimination half-life, thus making it an inconvenient prescription for out-patients in veterinary clinics. Keywords: Ceftriaxone, Pharmacokinetic profile, Dogs, Therapeutic dose, Veterinary clinic


Author(s):  
Shashwati Mathurkar ◽  
Preet Singh ◽  
Kavitha Kongara ◽  
Paul Chambers

The pharmacokinetics of salicylic acid (SA) in sheep was evaluated following intravenous (IV) and oral administration of sodium salicylate (sodium salt of salicylic acid) at different doses. Six healthy sheep were administered sodium salicylate (SS) IV at doses of 10, 50, 100 and 200 mg/kg body weight and another six sheep were drenched with 100 and 200 mg/kg of SS orally. Both studies were randomised crossover trials. A one-week washout period between each treatment was allowed in both studies. Blood samples were collected at 0, 15, 30 minutes and 1, 2, 4 and 6 hours after IV and oral SS administrations. Plasma SA concentrations were determined using high performance liquid chromatography with diode array detection method. Pharmacokinetic variables were calculated in a non-compartmental model. The elimination half-life (T1/2 el) of SA after IV administration of 200 mg/kg SS was 1.16 &plusmn; 0.32 hours. Mean bioavailability of SA was 64%, and mean T1/2 el was 1.90 &plusmn; 0.35 hours, after 200 mg/kg of oral SS. The minimum plasma SA concentration (16.8 &micro;g/mL) required to produce analgesia in humans was achieved after IV administration of 100 and 200 mg/kg SS in sheep for about 0.17 hour in this study. Experiments on pharmacokinetic-pharmacodynamics modelling are required to determine the actual effective plasma concentration range of SA in sheep.


Haematologica ◽  
2021 ◽  
Author(s):  
Soracha E. Ward ◽  
Jamie M. O’Sullivan ◽  
Alan B. Moran ◽  
Daniel I. R. Spencer ◽  
Richard A. Gardner ◽  
...  

Terminal sialylation determines plasma VWF half-life. A role for macrophage galactose lectin (MGL) in regulating hyposialylated VWF clearance has recently been proposed. In this study, we show that MGL influences physiological plasma VWF clearance. MGL inhibition was associated with a significantly extended mean residence time and 3-fold increase in endogenous plasma VWF:Ag levels (p


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