Pharmacokinetics and bone tissue concentrations of lincomycin following intravenous and intramuscular administrations to cats

Abstract

The pharmacokinetic properties and bone concentrations of lincomycin in cats after single intravenous and intramuscular administrations at a dosage rate of 10 mg/kg were investigated. Lincomycin minimum inhibitory concentration (MIC) for some gram-positive strains isolated from clinical cases was determined. Serum lincomycin disposition was best-fitted to a bicompartmental and a monocompartmental open models with first-order elimination after intravenous and intramuscular dosing, respectively. After intravenous administration, distribution was rapid (T(1/2(d)) = 0.22 ± 0.09 h) and wide as reflected by the volume of distribution (V((d(ss)))) of 1.24 ± 0.08 L/kg. Plasma clearance was 0.28 ± 0.09 L/h · kg and elimination half-life (T(1/2)) 3.56 ± 0.62 h. Peak serum concentration (C(max)), T(max), and bioavailability for the intramuscular administration were 7.97 ± 2.31 μg/mL, 0.12 ± 0.05 h, and 82.55 ± 23.64%, respectively. Thirty to 45 min after intravenous administration, lincomycin bone concentrations were 9.31 ± 1.75 μg/mL. At the same time after intramuscular administration, bone concentrations were 3.53 ± 0.28 μg/mL. The corresponding bone/serum ratios were 0.77 ± 0.04 (intravenous) and 0.69 ± 0.18 (intramuscular). Lincomycin MIC for Staphylococcus spp. ranged from 0.25 to 16 μg/mL and for Streptococcus spp. from 0.25 to 8 μg/mL.

Pharmacokinetics of lincomycin following intravenousadministration in febrile goats

“…The Cl  of lincomycin in present study was also lower than the Cl  of (0.50±0.02L/h/kg) in febrile calves and higher than Cl  (0.26L/h/kg) in sheep for florfenicol ( Dumka and Singh, 2013;Jianzhong et al, 2004).The high value of t 1/2 â in the present study (9.99±2.83 h), which was longer than the elimination half-life of 3.3 h in buffalo calves, 3.38 h in pigs, 4.2 h in cats and 3 h in calves for lincomycin (Gouri et al 2014;Albarellos et al 2012Albarellos et al , 2013Huimin et al 2012), indicated slow elimination of lincomycin during febrile condition in goats. This finding was comparable to the prolonged t 1/2  of florfenicol (3.08 ± 0.07 h) in febrile cross bred calves than that in healthy (2.76 ± 0.16 h) reported by Dumka and Singh, (2013).…”

“…(Dumka and singh, 2013). High distribution of lincomycin to various tissues and body fluids were reflected by large Vd area which was higher than the Vd area in calves with induced Pasteurella haemolytica pneumonia (1.2 L/kg), buffalo calves (1.15 L.kg -1 ), pigs (1.1 L.kg -1 ) cats (0.97-1.24 L.kg -1 ) and chicken (1.76 L.kg -1 ) for lincomycin (Burrows et al 1986;Nielsen and Gyrd-Hansen 1998;Albarellos et al 2012Albarellos et al , 2013Gouri et al 2014;El-Sayed et al 2015). In support of present result, Vd area of florfenicol in febrile calves (2.11± 0.18 L/kg) was reported by Dumka and Singh, (2013).…”

“…Minimum inhibitory concentration (MIC 90 ) lincomycin has been reported in the range of 0.06-2.0 µg.ml -1 against Streptococcus, Mycoplasma hyopneumoniae, and Staphylococcus spp. (Petinaki et al 2008;Albarellos et al 2012;Giguere 2013). The T>MIC was calculated for MIC S of 0.06, 0.1, and 0.6 g/mL.…”

“…Successful treatment of arthritis and pedal osteomyelitis usually associated with Trueperella pyogens (Arcanobacterium pyogens) has been reported with lincomycin in sheep (Giguere, 2013). Pharmacokinetics of lincomycin has been conducted in dairy cattle (Weber et al1981), calves (Burrows et al 1983(Burrows et al , 1986, buffalo calves (Gouri et al 2014), pigs (Chaleva and Nquyen 1987;Nielsen and Gyrd-Hansen 1998), cats (Albarellos et al 2012(Albarellos et al , 2013 and chickens (El-Sayed et al 2015). Further, disease conditions are known to alter the disposition of antimicrobials (Kumar et al 2010;Burrows 1986).…”

Degradation Efficiency and Characterization of Lincomycin by Electron Beam Irradiation

“…It is excreted in the urine as a mixture of the parent drug and its conjugated metabolite. 3,4 In recent years, a number of PPCPs have been detected in aqueous environmental systems, including rivers, lakes, and reservoirs. Among the 30 PPCPs surveyed in Korea, lincomycin was detected with relatively high concentration and frequency.…”