I.m. Administration (i.m + administration)

Distribution by Scientific Domains


Selected Abstracts


Pharmacokinetics and pharmacokinetic/pharmacodynamic integration of orbifloxacin in Korean Hanwoo cattle

JOURNAL OF VETERINARY PHARMACOLOGY & THERAPEUTICS, Issue 3 2009
G. ELIAS
The pharmacokinetics and pharmacodynamics of orbifloxacin were studied in six clinically healthy Hanwoo cows after intravenous (i.v.) and intramuscular (i.m.) administration at a dose of 3 mg/kg. Orbifloxacin concentrations were determined by high performance liquid chromatography with fluorescence detection. Steady-state volume of distribution and clearance of orbifloxacin after i.v. administration were 0.92 L/kg and 0.24 L/hkg, respectively. Following i.m. administration, a slow and complete absorption with absolute bioavailability of 101.4%, and a maximum concentration (Cmax) of 1.17 ,g/mL at 1.04 h were observed. The in vitro serum protein binding was 14.76%. The in vitro antibacterial activity of orbifloxacin against a pathogenic strain of Mannheimia haemolytica (M. haemolytica), Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus) was determined. The ex vivo activity of orbifloxacin against M. haemolytica strain was also determined, and these data were integrated with the ex vivo bacterial counts to establish AUC24h/MIC values producing bacteriostatic action, bactericidal action and elimination of bacteria. Mean values were 32.7, 51.6 and 102.6 h, respectively. From these data, we predict that orbifloxacin, when administered i.m. at a dosage of 2.5,5 mg/kg once a day, would be effective against bovine pathogens, such as M. haemolytica. Additional studies may be needed to confirm its efficacy in a clinical setting, and to evaluate the penetration of the drug in diseased tissues. [source]


Characterization of the pharmacokinetic disposition of levofloxacin in stallions after intravenous and intramuscular administration

JOURNAL OF VETERINARY PHARMACOLOGY & THERAPEUTICS, Issue 5 2008
A. GOUDAH
The target of the present study was to investigate the plasma disposition kinetics of levofloxacin in stallions (n = 6) following a single intravenous (i.v.) bolus or intramuscular (i.m.) injection at a dose rate of 4 mg/kg bwt, using a two-phase crossover design with 15 days as an interval period. Plasma samples were collected at appropriate times during a 48-h administration interval, and were analyzed using a microbiological assay method. The plasma levofloxacin disposition was best fitted to a two-compartment open model after i.v. dosing. The half-lives of distribution and elimination were 0.21 0.13 and 2.58 0.51 h, respectively. The volume of distribution at steady-state was 0.81 0.26 L/kg, the total body clearance (Cltot) was 0.21 0.18 L/h/kg, and the areas under the concentration,time curves (AUCs) were 18.79 4.57 ,g.h/mL. Following i.m. administration, the mean t1/2el and AUC values were 2.94 0.78 h and 17.21 4.36 ,g.h/mL. The bioavailability was high (91.76% 12.68%), with a peak plasma mean concentration (Cmax) of 2.85 0.89 ,g/mL attained at 1.56 0.71 h (Tmax). The in vitro protein binding percentage was 27.84%. Calculation of efficacy predictors showed that levofloxacin might have a good therapeutic profile against Gram-negative and Gram-positive bacteria, with an MIC , 0.1 ,g/mL. [source]


Pharmacokinetic,pharmacodynamic integration of danofloxacin after intravenous, intramuscular and subcutaneous administration to rabbits

JOURNAL OF VETERINARY PHARMACOLOGY & THERAPEUTICS, Issue 1 2007
E. FERNNDEZ-VARN
The pharmacokinetics of danofloxacin was studied following intravenous (i.v.), intramuscular (i.m.) and subcutaneous (s.c.) administration of 6 mg/kg to healthy rabbits. Danofloxacin concentration were determined by high-performance liquid chromatography assay with fluorescence detection. Minimal inhibitory concentrations (MICs) assay of danofloxacin against 30 strains of Staphylococcus aureus from several European countries was performed in order to compute pharmacodynamic surrogate markers. The danofloxacin plasma concentration versus time data after i.v. administration could best be described by a two-compartment open model. The disposition of i.m. and subcutaneously administered danofloxacin was best described by a one-compartment model. The terminal half-life for i.v., i.m. and s.c. routes was 4.88, 6.70 and 8.20 h, respectively. Clearance value after i.v. dosing was 0.76 L/kgh. After i.m. administration, the absolute bioavailability was mean (SD) 102.34 5.17% and the Cmax was 1.87 mg/L. After s.c. administration, the absolute bioavailability was mean (SD) 96.44 5.95% and the Cmax was 1.79 mg/L. Danofloxacin shows a favourable pharmacokinetics profile in rabbits reflected by parameters such as a long half-life and a high bioavailability. However, in consideration of the low AUC/MIC indices obtained, its use by i.m. and s.c. route against the S. aureus strains assayed in this study cannot be recommended given the risk for selection of first mutant subpopulations. [source]


Pharmacokinetics of erythromycin in nonlactating and lactating goats after intravenous and intramuscular administration

JOURNAL OF VETERINARY PHARMACOLOGY & THERAPEUTICS, Issue 1 2007
L. AMBROS
The objectives of this work were to compare the pharmacokinetics of erythromycin administered by the intramuscular (i.m.) and intravenous (i.v.) routes between nonlactating and lactating goats and to determine the passage of the drug from blood into milk. Six nonpregnant, nonlactating and six lactating goats received erythromycin by the i.m. (15 mg/kg) and the i.v. (10 mg/kg) routes of administration. Milk and blood samples were collected at predetermined times. Erythromycin concentrations were determined by microbiological assay. Results are reported as mean SD. Comparison of the pharmacokinetic profiles between nonlactating and lactating animals after i.v. administration indicated that significant differences were found in the mean body clearance (8.38 1.45 vs. 3.77 0.83 mL/kgh respectively), mean residence time (0.96 0.20 vs. 3.18 1.32 h respectively), area under curve from 0 to 12 h (AUC0,12) (1.22 0.22 vs. 2.76 0.58 ,gh/mL respectively) and elimination half-life (1.41 1.20 vs. 3.32 1.34 h); however, only AUC0,12 showed significant differences after the i.m. administration. Passage of erythromycin in milk was high (peak milk concentration/peak serum concentration, 2.06 0.36 and AUC0,12milk/AUC0,12serum,6.9 1.05 and 2.37 0.61 after i.v. and i.m. administrations respectively). We, therefore, conclude that lactation affects erythromycin pharmacokinetics in goats. [source]


Pharmacokinetics of cefepime administered by i.v. and i.m. routes to ewes

JOURNAL OF VETERINARY PHARMACOLOGY & THERAPEUTICS, Issue 6 2005
M. ISMAIL
The pharmacokinetics of cefepime were studied following i.v. and i.m. administration of 20 mg/kg in 10 ewes. Following i.v. administration of a single dose, the plasma concentration,time curves of cefepime were best fitted using a two-compartment open model. The elimination half-life (t1/2,) was 1.76 0.07 h, volume of distribution at steady-state [Vd(ss)] was 0.32 0.01 L/kg and total body clearance (ClB) was 2.37 0.05 mL/minkg. Following i.m. administration, the drug was rapidly absorbed with an absorption half-life (t1/2ab) of 0.49 0.05 h, maximum plasma concentration (Cmax) of 31.9 1.5 ,g/mL was attained at (tmax) 1.1 0.2 h and the drug was eliminated with an elimination half-life (t1/2el) of 2.06 0.11 h. The systemic bioavailability (F) after i.m. administration of cefepime was 86.8 7.5%. The extent of plasma protein binding measured in vitro was 14.8 0.54%. The drug was detected in urine for 36 h postadministration by both routes. [source]


Pharmacokinetics of ceftiofur in red deer (Cervus elaphus)

JOURNAL OF VETERINARY PHARMACOLOGY & THERAPEUTICS, Issue 1 2004
Mark L. Drew
Twelve adult female red deer (Cervus elaphus) were given 250 mg of ceftiofur sodium by intramuscular injection (i.m.) and ballistic implant in a crossover design. Blood samples were taken from an in-dwelling jugular catheter prior to drug administration and at 0.25, 0.5, 1, 2, 4, 8, 12, 24, 36, 48, and 72 h postadministration of the drug. Samples were centrifuged and plasma kept frozen at ,70 C until analysis for ceftiofur and active metabolites using an HPLC method. The pharmacokinetics of ceftiofur and metabolites after i.m. dosing and following ballistic implant were quite different. Absorption after i.m. injection was rapid; whereas following ballistic implant there was a lag-time until concentrations were detectable in plasma. The maximum concentration reached in plasma was higher following injection compared with ballistic implant, however the AUC calculated after ballistic implant was almost identical to the mean AUC found after i.m. dosing. The results indicate that i.m. administration of ceftiofur maintains adequate plasma levels for most susceptible bacterial pathogens for at least 12 h; therefore twice daily administration is needed in red deer. Ballistic implants produced plasma concentrations above the MIC for most bacterial pathogens from 4 to 24 h in most animals after administration; however, absorption of the drug was variable and some did not maintain effective concentrations for more than a few hours. Ceftiofur is a useful drug in red deer and twice daily i.m. administration dosing should allow treatment for susceptible bacterial pathogens. [source]


Comparison of plasma pharmacokinetics and bioequivalence of ceftiofur sodium in cattle after a single intramuscular or subcutaneous injection

JOURNAL OF VETERINARY PHARMACOLOGY & THERAPEUTICS, Issue 5 2000
S. A. Brown
Ceftiofur sodium, a broad-spectrum cephalosporin, is active against gram-positive and gram-negative pathogens of veterinary importance. This study was designed to compare the bioequivalence of the sodium salt in cattle after a single intramuscular (i.m.) or subcutaneous dose (s.c.) of 2.2 mg ceftiofur equivalents/kg body weight. The criteria used to evaluate bioequivalence were (1) the area under the curve from time of injection to the limit of quantitation (LOQ) of the assay (AUC0-LOQ), and (2) time concentrations remained above 0.2 ,g/mL (t>0.2). Twelve crossbred beef cattle were enrolled in a three-period, two-treatment crossover trial, with a minimum 2-week washout period between doses of 2.2 mg ceftiofur equivalents/kg. Blood samples were collected serially for up to 72 h post-injection. Plasma samples were then analyzed using a validated assay that measures ceftiofur, and all desfuroylceftiofur-related metabolites, by high-performance liquid chromatography (HPLC) as the stable derivative, desfuroylceftiofur acetamide. A maximum plasma concentration (Cmax) of 13.93.55 ,g/mL was observed from 0.67,2.0 h after i.m. administration, whereas a Cmax of 13.63.85 ,g/mL was observed from 0.67,3.0 h after s.c. administration. The AUC0-LOQ was 10835.0 ,g h/mL after i.m. dosing, compared with 10529.8 ,g h/mL after s.c. dosing. The pre-established criterion for equivalence of the AUC0-LOQ for the i.m. and s.c. routes of administration was satisfied. The t>0.2 was 49.28.55 h after i.m. administration, compared with 47.09.40 h after s.c. administration. The pre-established criterion for equivalence of the t>0.2 for i.m. and s.c. administration was satisfied. The equivalence of AUC0-LOQ and t>0.2 for i.m. and s.c. administration of 2.2 mg ceftiofur equivalents (CE)/kg doses of ceftiofur sodium suggest similar therapeutic efficacy and systemic safety for the two routes of administration. [source]


Efficacy of Ovsynch Protocol with Antiprolactin Treatment for Timed Artificial Insemination During Non-breeding Seasons in Yaks (Poephagus grunniens L.)

REPRODUCTION IN DOMESTIC ANIMALS, Issue 3 2010
M Sarkar
Contents An attempt was undertaken to investigate the efficacy of Ovsynch protocol for timed artificial insemination (TAI) with or without Norprolac (antiprolactin) treatment during non-breeding season (winter months) in yaks (n = 25). During non-breeding season, plasma prolactin profile has been reported high due to cold and nutritional stress. The Norprolac dose of i.m. administration was standardized for prolactin suppression. Three different doses viz. 2.5, 5.0 and 7.5 mg were attempted and the dose of 7.5 mg Norprolac i.m. per animal was found to be suitable for suppression of prolactin levels up to 30 h. Ovsynch treatment with Norprolac induced more number of oestrous symptoms per animal (4.8 vs 2.1), higher LH peak concentration (24.01 vs 16.16 ng/ml), longer duration of LH surge (6.8 vs 5.2 h) and higher conception rate (70 vs 30%) in Ovsynch plus Norprolac treated animals compared with animals treated with Ovsynch alone. Therefore, this study clearly indicates the opportunity for practical application of the Ovsynch plus Norprolac protocol for TAI in yaks during non-breeding seasons. [source]


Pharmacokinetics and bioavailability of imidocarb dipropionate in swine

JOURNAL OF VETERINARY PHARMACOLOGY & THERAPEUTICS, Issue 4 2007
D. SU
A two-way crossover study was performed in eight healthy young pigs to determine the pharmacokinetics of imidocarb dipropionate (IMDP) following intravenous (2 mg/kg b.w.) and intramuscular (2 mg/kg b.w.) administrations. Each animal received one intravenous and one intramuscular injection with a 30-day washout period between the two-treatments. Plasma concentrations were measured by high-performance liquid chromatography (HPLC) assay with UV detector at regular intervals for up to 24 h post-injection. Intravenous plasma concentration profiles best fit a three-compartmental model yielding a mean system clearance (Cl(s)) of 558 mL/kgh and a mean half-life of 13.91 h. Mean imidocarb AUC(0,,) (,gh/mL), Vc (L/kg), Vd(area)(L/kg) and MRT(0-t) (h) values were 3.58, 0.11, 14.36 and 1.46, respectively. Compartmental modeling of imidocarb, after intramuscular administration produced best fit for two-compartmental model yielding mean K, (h,1), Cmax (,g/mL), tmax (h), and bioavailability (%) of 3.89, 2.02, 0.54, and 86.57 for the 2 mg/kg dose level. The present studies showed that IMDP was rapidly absorbed, widely distributed, and slowly eliminated. No adverse effects were observed in any of the pigs after i.v. and i.m. administrations of IMDP. The favorable PK behavior, such as the long half-life, acceptable bioavailability indicated that it is likely to be effective in pigs. [source]


Pharmacokinetics of erythromycin in nonlactating and lactating goats after intravenous and intramuscular administration

JOURNAL OF VETERINARY PHARMACOLOGY & THERAPEUTICS, Issue 1 2007
L. AMBROS
The objectives of this work were to compare the pharmacokinetics of erythromycin administered by the intramuscular (i.m.) and intravenous (i.v.) routes between nonlactating and lactating goats and to determine the passage of the drug from blood into milk. Six nonpregnant, nonlactating and six lactating goats received erythromycin by the i.m. (15 mg/kg) and the i.v. (10 mg/kg) routes of administration. Milk and blood samples were collected at predetermined times. Erythromycin concentrations were determined by microbiological assay. Results are reported as mean SD. Comparison of the pharmacokinetic profiles between nonlactating and lactating animals after i.v. administration indicated that significant differences were found in the mean body clearance (8.38 1.45 vs. 3.77 0.83 mL/kgh respectively), mean residence time (0.96 0.20 vs. 3.18 1.32 h respectively), area under curve from 0 to 12 h (AUC0,12) (1.22 0.22 vs. 2.76 0.58 ,gh/mL respectively) and elimination half-life (1.41 1.20 vs. 3.32 1.34 h); however, only AUC0,12 showed significant differences after the i.m. administration. Passage of erythromycin in milk was high (peak milk concentration/peak serum concentration, 2.06 0.36 and AUC0,12milk/AUC0,12serum,6.9 1.05 and 2.37 0.61 after i.v. and i.m. administrations respectively). We, therefore, conclude that lactation affects erythromycin pharmacokinetics in goats. [source]