Disposition Kinetics of lincomycin following intravenous administration in hypothyroid goats

Author(s):  
Meemansha Sharma ◽  
Vinod Kumar Dumka ◽  
Saloni Singla ◽  
Rajdeep Kaur ◽  
Raushan Kumar Singh

Hypothyroidism is a common disorder of small ruminants and is expected to alter the pharmacokinetics of drugs. Hypothyroidism was induced by feeding thiourea at the dose rate 50 mg.kg-1 daily for 28 days to goats. Disposition of lincomycin, after intravenous administration at dose rate 10 mg/kg, was investigated in hypothyroid goats to determine the potential dosage regimen against susceptible microorganisms. Blood samples were collected from 1 min to 24 h of drug administration. The drug was detected in plasma up to 8 h and lincomycin was rapidly distributed from blood to the tissue, as evidenced by the high value of the distribution coefficient (mean ± SEM) 12.3±1.09 h-1. The large Vd (1.78±0.18 L/kg) indicated vast tissue distribution of lincomycin in goats. The elimination half life, AUC and total body clearance were 3.99± 0.25 h, 33.2±1.71 ìg.h/mL and 0.31±0.02 L/h/kg, respectively. Based on results, lincomycin in hypothyroid goats is suggested to be repeated at 12 h interval for organisms sensitive to lincomycin having MIC up to 0.1 µg.ml-1.

Author(s):  
Saber El Hanbally ◽  
Hanem El Gendy ◽  
Hanem El Gendy ◽  
Mohamed El Hewaity ◽  
Mohamed El Hewaity

Background: Nonsteroidal anti-inflammatory drugs and antibiotics are commonly prescribed together. We aimed to study the kinetic profile of cefquinome (2 mg/kg b.wt.) following intramuscular administration of it alone and co-administered with meloxicam (0.2 mg/kg b.wt.) in goats.Methods: Five Egyptian Baladi goats, each goat was injected intramuscularly at the dose rate of 2 mg/kg b.wt. Cefquinome into the deep gluteal muscle of hindquarter alone and then after fifteen days washout period, these animals also injected intramuscularly at the dose rate of 2 mg/kg b.wt. Cefquinome preceded with meloxicam at the dose rate of 0.2 mg/kg b.wt. The serum concentrations of cefquinome were detected by high performance liquid chromatography, two compartment model.Results: Following a single dose intramuscular administration of cefquinome alone, peak plasma concentration (1.71±0.0189 μg/ml) was obtained at 1.59±0.0038 h. The absorption half-life (t1/2ab), total body clearance (Cltot), elimination half-life (t1/2el) and area under curve (area under concentration (AUC(0-inf)) of cefquinome were 0.4±0.0028 h, 0.068±0.78 l/h/kg, 9.21±0.178h and 29.36±0.78 µg.h.ml-1, respectively. Following a single dose intramuscular co-administration of cefquinome and meloxicam, peak plasma concentration (1.60±0.0124 μg/ml) was obtained at 1.49±0.0092 h. The absorption half-life (t1/2ab), total body clearance (Cltot), elimination half-life (t1/2el) and area under curve (AUC(0-inf)) of cefquinome were 0.396±0.006 h, 0.094±0.25 l/h/kg, 6.5±0.221 h and 21.38±0.696 µg/h/ml, respectively. Non significant alters were reported in the parameters following co-administration of Cefquinome with meloxicam.Conclusions: From our results, may be concluded that intramuscular administration of meloxicam may be successfully co-administrated with cefquinome for combating bacterial infections with an inflammatory condition in goats without any antagonistic effect.


1992 ◽  
Vol 26 (1) ◽  
pp. 8-10 ◽  
Author(s):  
David E. Nix ◽  
J. Michael Spivey ◽  
Allyn Norman ◽  
Jerome J. Schentag

OBJECTIVE: To assess the pharmacokinetics and tolerance of ciprofloxacin after the administration of single intravenous doses of 200, 300, and 400 mg. DESIGN: Double-blind, three-period, randomized, crossover trial. SETTING: Private, university-affiliated, hospital-based, clinical research center. PATIENTS: Normal healthy male volunteers, 18–40 years of age. INTERVENTIONS: Subjects received 200-, 300-, and 400-mg single intravenous doses of ciprofloxacin via 30-minute infusions in random sequence. MAIN OUTCOME MEASURES: Serum ciprofloxacin concentrations were determined by HPLC after each dose and the results were used to derive pharmacokinetic parameters. Tolerance was assessed by reported and observed adverse events, urine microscopic examinations for crystals, and examination of intravenous infusion sites. RESULTS: The mean area under the time curve (AUC) values displayed linearity with respect to the administered dose. No statistical differences were observed in total body clearance, steady-state volume of distribution, or elimination half-life with respect to dose administered. The mean total body clearance, steady-state volume of distribution, or elimination half-life ranged from 36 to 41 L/h, 146 to 169 L, and 3.5 to 3.7 h for the 200-, 300-, and 400-mg doses, respectively. Adverse effects, including venous irritation (four subjects) and crystalluria (two subjects), were mild and did not require withdrawal of any subject from the study. CONCLUSIONS: Intravenous ciprofloxacin in doses ranging from 200 to 400 mg demonstrated linear pharmacokinetics. These single doses were well tolerated, although cases of transient venous irritation and crystalluria were observed.


2011 ◽  
Vol 2011 ◽  
pp. 1-5
Author(s):  
Harshad B. Patel ◽  
Shailesh K. Mody ◽  
Hitesh B. Patel ◽  
Vipul A. Patel ◽  
Urvesh D. Patel

The present study was carried out to investigate disposition kinetics of moxifloxacin following single-dose intravenous (i.v.), intramuscular (i.m.), and subcutaneous (s.c.) administration at a dose rate of 5 mg/kg of body weight (b.wt.) in goats. Plasma samples collected after treatments were analyzed for drug concentration using high-performance liquid chromatography (HPLC). After i.v. administration, distribution of the drug was rapid and wide as reflected by high steady-state volume of distribution. Drug elimination was relatively faster with a total body clearance of 0.59±0.03 L/h/kg. Following i.m. injection, the drug has shown the rapid and near-to-complete absorption with bioavailability of 98.20±3.96 per cent. The maximum plasma drug concentration (Cmax) of 1.21±0.04 μg/mL was attained at 1 h (Tmax). The drug was widely distributed as reflected by high apparent volume of distribution. The elimination half-life (t1/2β) of the drug was 6.26±0.08  h. Following s.c. administration, the drug was rapidly absorbed (Cmax: 1.16±0.02 μg/mL; tmax: 1 h) and slowly eliminated from the body. The elimination half-life and total body clearance (ClB) were 5.61±0.10 h and 0.60±0.03 L/h/kg, respectively. The bioavailability of moxifloxacin following s.c. administration was 90.44±3.96 per cent.


2011 ◽  
Vol 1 (1) ◽  
pp. 4
Author(s):  
Yongqing Wang ◽  
Hongwen Zhang ◽  
Ling Meng ◽  
Nana Tang ◽  
Hongyu Yuan ◽  
...  

To investigate the pharmacokinetics and bioavailability of rabeprazole administrated by intravenous infusion and oral administration in healthy Chinese volunteers. A total of 20 male subjects were recruited and randomly assigned at the beginning of the study to receive a single dose of rabeprazole (20 mg) administrated either intravenously or orally. Following a 7-day washout period, all subjects received another 20mg dose via the alternate route. Intravenous dose was given in constant infusion over 30 min, and the oral dose was given in two 10mg tablets. Intravenous administration yielded the following measurements: the terminal half-life was (62.4±10.7) min; the Cmax was (1308.6±266.4) ng·ml-1; the total body clearance was (0.21±0.05) L·min-1; the AUC0-τ and AUC0-∞ were (99.6±21.9) mg∙min∙L-1 and (102. 4±23.3) mg∙min∙L-1, respectively. Oral administration yielded the following measurements: the half-life was (64.2±15.5) min; the Cmax was (508.3±180.2) ng·ml-1; Tmax was attained at about 229.5 min; the total body clearance was (0.31±0.10) L·min-1; the AUC0-τ and AUC0-∞ were (69.5±20.0) mg∙min∙L-1 and (70.6±20.2) mg∙min∙L-1, respectively. The bioavailability of rabeprazole was estimated to be 70.1% in healthy Chinese volunteers. The total body clearance after oral administration was significantly higher than that measured following intravenous administration (P <0.01).


1991 ◽  
Vol 11 (1) ◽  
pp. 59-63 ◽  
Author(s):  
Paul Nikolaidis ◽  
Scott E. Walker ◽  
Nicholas Dombros ◽  
Achilleas Tourkantonis ◽  
Tom W. Paton ◽  
...  

Seven adult patients on continuous ambulatory peritoneal dialysis (CAPD) received one dose of pefloxacin, a novel quinolone antibiotic, orally and intravenously on two separate occasions to characterize the pharmacokinetics and metabolism of the drug. Concentrations of both pefloxacin and its active metabolite N-desmethylpefloxacin (norfloxacin) were measured in serum and dialysate by HPLC. Half-life, total body clearance and peritoneal clearance were determined. The overall elimination half-life was 19.9h. Relative to the IV dose the bioavailability following oral administration of pefloxacin was 76%. The mean serum and dialysate concentrations were similar up to 24 h after the oral or IV dose. After a 6 h dwell time the dialysate concentration of pefloxacin was 2.24 mg/L which is above the MICgo for most bacteria responsible for peritonitis in CAPD patients. The peritoneal clearance of pefloxacin averaged 2.5 mL/min. Serum concentrations of the metabolite norfloxacin were less than 0.5 mg/L during the 24 h study period. We conclude that pefloxacin might be equally effective in the treatment of peritonitis of CAPD after oral or IV administration. Since the peritoneal clearance contributes insignificantly to the elimination of pefloxacin during CAPD, the proposed maintenance regimen of an oral or IV 400 mg dose/day seems to be a reasonable therapy for infections in CAPD patients.


2009 ◽  
Vol 53 (8) ◽  
pp. 3266-3268 ◽  
Author(s):  
Kook-Hwan Oh ◽  
Chiweon Kim ◽  
Hankyu Lee ◽  
Hajeong Lee ◽  
Ji Yong Jung ◽  
...  

ABSTRACT The pharmacokinetic characteristics of piperacillin sodium were studied in five volunteers undergoing on-line hemodiafiltration (HDF). The subjects were given 2 g of piperacillin sodium intravenously over 1 min and placed on on-line HDF for 4 h starting at 60 min after the piperacillin infusion. Noncompartmental models were employed for estimation of the pharmacokinetic parameters, and intradialytic piperacillin clearance was calculated by the recovery method. The mean volume of distribution and the elimination half-life were 0.27 ± 0.13 liter/kg (mean ± standard deviation) and 1.1 ± 0.6 h, respectively. The total body clearance of piperacillin was 0.19 ± 0.08 liter/h/kg. Piperacillin clearance through on-line HDF was 0.11 ± 0.06 liter/h/kg. The mean serum piperacillin concentration was 4.0 ± 1.9 μg/ml at the end of the 4-h on-line HDF session. The concentration of infused piperacillin recovered in the dialysate was 527 ± 236 mg (26.3% ± 11.8%). We suggest the replacement of 500 mg of piperacillin after each on-line HDF session.


1988 ◽  
Vol 7 (2) ◽  
pp. 175-178 ◽  
Author(s):  
M. Egfjord ◽  
J.A. Jansen ◽  
H. Flachs ◽  
J.S. Schou

A mixture containing 3 g of boric acid and 300 mg of cinchocaine chloride prescribed due to painful dental protrusion was accidentally ingested by a 12-month-old girl. She developed violent vomiting and coughing. Irritability, tremor, seizures and a delirious reaction. She was treated with diazepam, intubated, sedated and ventilated. Her diuresis was stimulated with furosemide and fluid. Within the first 24 h she was treated with haemodialysis twice on femoral catheters. Her renal function was unaffected. In two days she fully recovered. The maximum measured levels of boric acid and cinchocaine chloride approximately 6 h after ingestion were 26 μg/ml and 71 ng/ml respectively. The plasma half-life of boric acid was 7.0 h and decreased to 3.6 and 4.4 h during the two haemodialyses. The total body clearance of boric acid increased correspondingly from 21 ml/min to 41 and 34 ml/min. The in vitro clearance of boric acid of the dialyser was later determined to be 18 ml/min. It is concluded that haemodialysis is valuable in the treatment of boric acid intoxication because it increases the elimination of the drug even in patients without any sign of renal toxicity.


1982 ◽  
Vol 28 (1) ◽  
pp. 204-206 ◽  
Author(s):  
R Jagenburg ◽  
C G Regårdh ◽  
S Rödjer

Abstract We studied the kinetics of intravenously administered L-phenylalanine with respect to the effect of age and sex, using a two-compartment model. We found that the volume of the peripheral compartment and total body clearance decrease with age. The sex-related influence was less obvious when distribution volumes and total body clearance were corrected for differences in body size. We emphasize the necessity of having age-matched control subjects in kinetic studies.


1996 ◽  
Vol 30 (10) ◽  
pp. 1106-1109 ◽  
Author(s):  
Alicia CM Alexander ◽  
Adam Akers ◽  
Gary R. Matzke ◽  
Francesca T. Aweeka ◽  
Donald S. Fraley

OBJECTIVE: To report the disposition of foscarnet in a patient undergoing peritoneal dialysis. CASE SUMMARY: A 34-year-old man with AIDS received foscarnet for the treatment of esophageal cytomegalovirus. We characterized the clearance of foscarnet in this patient during continuous cyclic peritoneal dialysis (CCPD) and continuous ambulatory peritoneal dialysis (CAPD). DISCUSSION: The foscarnet half-lives during CCPD and CAPD were 41.4 and 45.8 hours, respectively. These values are significantly greater than the half-life of 4.5 hours observed in patients with normal renal function and about half that reported in anuric patients undergoing hemodialysis during the interdialytic period. The CCPD and CAPD clearances of foscarnet were 5.8 and 4.5 mL/min, respectively; the CAPD clearances of creatinine and urea nitrogen were 4.1 and 6.0 mL/min, respectively. The patient's estimated total body clearance values of foscarnet during CCPD and CAPD were 9.8 and 8.8 mL/min, respectively. Thus, CCPD and CAPD augmented the patient's residual clearance of foscarnet by 145% and 105%, respectively. CONCLUSIONS: Since incremental increases in residual clearance of 30% or more generally will result in clinically significant changes in a drug's serum concentration, foscarnet dosage needs to be individualized for patients receiving peritoneal dialysis.


1986 ◽  
Vol 20 (9) ◽  
pp. 704-707 ◽  
Author(s):  
Maria J. Otero ◽  
Miguel Barrueco ◽  
Eduardo L. Marino ◽  
Francisco Gomez ◽  
Alfonso Dominguez-Gil

The influence of age on the disposition of theophylline was studied in 95 adult patients (nonsmokers) with bronchial asthma requiring oral theophylline therapy: 17 patients age ≥39 years, 50 patients age 40–59 years, and 28 patients < 60 years. A decrease was observed in total body clearance together with an increase in the elimination half-life of theophylline parallel to the advance in age of the patients. The apparent volume of distribution of theophylline was similar in the three groups of patients. According to the results obtained, recommendations are made regarding the dosage regimens of theophylline in elderly patients.


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