Abstract:Following intravenous administration of an oxytetracycline-HC1 and an oxytetracycline-dihydrate formulation to dairy cows, no statistical difference could be found between the pharmacokinetic parameters, derived from the three-compartment model, of these preparations. Urinary recovery was continued for a period of 72 h following intravenous or intramuscular OTC administration. The recovery of OTC in the urine in the 72-h period was in the range of 73% to 96% of the available dose administered. The renal OTC cl… Show more
“…The pharmacokinetic parameters derived from the i.v. data of product F, presented in Table 2, were similar to those reported previously (13,14). The final elimination half-life (T1127) was 9.5 ± 2.1 h., the distribution volume (VDarea) 1.02 ± 0.16 litre/kg, and the total body clearance (C1B) 0.076 litre/kg/hr.…”
Section: Plasmasupporting
confidence: 73%
“…The renal OTC clearance was significantly correlated to urine flow and creatinine clearance, that of the unbound OTC being at least twice greater than the creatinine clearance (Table 4), which indicates that OTC is excreted by tubular secretion and glomerular filtration minus urogenital reabsorption (in distal tubulus and presumably from the bladder) (2,13). It is noteworthy that in pigs the renal clearances of the unbound OTC and creatinine are both 3 to 4 times higher than in cows (2,9).…”
SUMMARY Oxytetracycline (OTC) concentrations in plasma and milk dairy cows were determined following a single intramuscular injection offive oxytetracycline-20% formulations at a dosage of approximately 10 mg/kg. For obtaining pharmacokinetic reference parameters, one 10% OTC formulation was administered intravenously. The five 20% formulations were compared and evaluated pharmacokinetically with respect to absorption rate, peak plasma and milk OTC concentrations, biological half-life, and relative bioavailability. The mean maximum plasma OTC concentrations varied between 4.5 and 6.8 pg/m1 and were achieved between 5 and 10 h depending on the formulation involved. The mean maximum milk concentrations, ranging from I. 12 to 1.92 pg/ml, were achieved 12 to 24 h A plasma OTC concentration exceeding O. 5 pg/ml was maintained for 48 h to 70 h, and in milk for 33 to 49 h, depending on the formulation involved Formulations exhibiting the lowest clinically noticeable irritation showed the highest peak plasma OTC concentrations and the best bioavailability. Among the formulations the calculated withholding periods for milk were in the range of 3 to 4 days and for edible tissues of 9 to 14 days. The OTC and creatinine clearances were significantly correlated to each other and to the urinary flow. OTC was excreted predominantly by glomerular filtration, partly by tubular secretion minus urogenital (distal renal tubuli and bladder) reabsorption.
“…The pharmacokinetic parameters derived from the i.v. data of product F, presented in Table 2, were similar to those reported previously (13,14). The final elimination half-life (T1127) was 9.5 ± 2.1 h., the distribution volume (VDarea) 1.02 ± 0.16 litre/kg, and the total body clearance (C1B) 0.076 litre/kg/hr.…”
Section: Plasmasupporting
confidence: 73%
“…The renal OTC clearance was significantly correlated to urine flow and creatinine clearance, that of the unbound OTC being at least twice greater than the creatinine clearance (Table 4), which indicates that OTC is excreted by tubular secretion and glomerular filtration minus urogenital reabsorption (in distal tubulus and presumably from the bladder) (2,13). It is noteworthy that in pigs the renal clearances of the unbound OTC and creatinine are both 3 to 4 times higher than in cows (2,9).…”
SUMMARY Oxytetracycline (OTC) concentrations in plasma and milk dairy cows were determined following a single intramuscular injection offive oxytetracycline-20% formulations at a dosage of approximately 10 mg/kg. For obtaining pharmacokinetic reference parameters, one 10% OTC formulation was administered intravenously. The five 20% formulations were compared and evaluated pharmacokinetically with respect to absorption rate, peak plasma and milk OTC concentrations, biological half-life, and relative bioavailability. The mean maximum plasma OTC concentrations varied between 4.5 and 6.8 pg/m1 and were achieved between 5 and 10 h depending on the formulation involved. The mean maximum milk concentrations, ranging from I. 12 to 1.92 pg/ml, were achieved 12 to 24 h A plasma OTC concentration exceeding O. 5 pg/ml was maintained for 48 h to 70 h, and in milk for 33 to 49 h, depending on the formulation involved Formulations exhibiting the lowest clinically noticeable irritation showed the highest peak plasma OTC concentrations and the best bioavailability. Among the formulations the calculated withholding periods for milk were in the range of 3 to 4 days and for edible tissues of 9 to 14 days. The OTC and creatinine clearances were significantly correlated to each other and to the urinary flow. OTC was excreted predominantly by glomerular filtration, partly by tubular secretion minus urogenital (distal renal tubuli and bladder) reabsorption.
“…This fact may imply large differences in the pharmacokinetic behaviour and bioavailability between the formulations. Several factors have already been described which influence the OTC pharmacokinetics and OTC persistence in the body: age, injection site, irritation, composition and route of application, urine flow, and disease state of the animal (3,6,7,8,9). This report deals with the pharmacokinetics, bioavailability, and withdrawal time aspects of seven commercially available oxytetracycline-10% formulations and one experimental formulation.…”
SU MM A R Y In plasma and milk the oxytetracycline (OTC) concentrations were determined following a single intramuscular administration of eight 10%-formulations to dairy cows at a dose of approximately 5 mg/kg. Two of these formulations were injected intravenously to obtain reference values of the drug's pharmacokinetic parameters. The eight formulations were compared and evaluated pharmacokinetically with respect to absorption rate, peak plasma and milk OTC concentrations, biological half-life, and relative bioavailability. The mean maximum plasma OTC concentrations, ranging from 2.0 to 4. 1 pg/ml, were achieved between 4 and 12 hours post injection, depending on the formulation involved. The mean maximum milk OTC concentrations, in the range between 0.92 and 1.43 mg/ml, were achieved 12 to 24 h p. i. The OTC milk concentration-time profile ran parallel to the OTC plasma concentration-time profile. After intravenous administration the time for the appearance of OTC in milk was shorter (1-2 hours p.i.), the peak milk OTC concentration was higher (1.7-1.9 pg/ml) and achieved earlier (6-8 h p.i.). and the OTC persistence in milk shorter than after i.m. administration. Formulations exhibiting the lowest clinically noticeable irritation showed the most favourable pharmacokinetic characteristics: rapid absorption with the highest peak plasma OTC concentrations and good bioavailability. The plasma and milk protein binding for OTC was respectively 71.7± 7.4% and 84.8 ± 5.45%. Withdrawal times for milk and edible tissues are presented on the basis of preset tolerance or detection limits.
“…The half-life of elimination of oxytetracycline administered at this dosage in calves has been reported to be 6.4 ± 1.3 hour at 6 weeks of age (Burrows et al 1987). Oxytetracycline is mostly excreted by the kidney (85-86%) and mainly through glomerular filtration (Nouws et al 1985). …”
Tetracycline and related compounds are used extensively as broad spectrum antibiotics in the treatment of bacterial infections in ruminants. Tetracycline may cause acute pancreatitis which may result in increased serum amylase activity. However, it has been shown that administration of oxytetracycline in human results in decrease serum amylase activity. In this study changes in serum amylase activity were measured in 20 clinically healthy calves following intravenous injection of oxytetracycline hydrochloride at 10 mg/kg of body weight. Blood samples were collected at 30, 60, and 120 minutes after oxytetracycline injection. Serum amylase activity was measured using the amyloclastic assay. The activity of serum amylase was increased significantly (P < 0.05) at 30 (40.5%), 60 (35.1%), and 120 (39.3%) minutes after oxytetracycline hydrochloride administration. To the authors’ knowledge this is the first study on the acute effect of tetracycline administration on serum amylase activity in calves.
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