Pharmacokinetics and skin concentrations of lincomycin after intravenous and oral administration to cats

Abstract

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

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).…”

“…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). This was further shown by the long MRT which was longer than the MRT of 4.32 h in buffalo calves, 5.5 h in cats and in 3.76 h in chicken after IV administration of lincomycin (Albarellos et al 2013;Gouri et al 2014;El-Sayed et al 2015). The MRT of lincomycin obtained in present study was also higher than the MRT of florfenicol (2.93±0.06 h) in febrile calves (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).…”

“…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).…”

Dynamic metabonomic and microbiological response of rats to lincomycin exposure: an integrated microbiology and metabonomics analysis

“…33,34 Additionally, on the basis of its poor systemic bioavailability, LM was selected at the dosage of 1.5 g kg À1 of body weight in our study to rapidly and completely remove the microbes from the gut. 35 We combined 16S rRNA sequencing and metabolomics to characterize the time-dependent microbiological and endogenous metabolic response to LM in urine and faeces. The data clearly indicated that LM exposure disturbed either the gut bacteria at the abundance level or the urinary/faecal metabolomic proles.…”