Ziv G, Creveld C V, Ben-Zvi Z, Glickman A, Yagil R
Ministry of Agriculture, Kimron Veterinary Institute, Bet-Dagan, Israel.
J Vet Pharmacol Ther. 1995 Aug;18(4):299-305. doi: 10.1111/j.1365-2885.1995.tb00594.x.
The disposition kinetics of tylosin tartrate administered intravenously (i.v.) at 10 mg/kg and intramuscularly (i.m.) at 20 mg/kg were studied in normal camels and in the same camels at the end of a 14 day water-deprivation period. After i.v. treatment, serum tylosin concentrations in the water-deprived camels were significantly higher, rate of drug elimination was slower, the volume of distribution was significantly smaller, and total body clearance was significantly slower than in the normal camels. On the other hand, serum drug concentrations were lower in the water deprived camels after i.m. dosing, the mean absorption time was significantly shorter and the i.m. availability was significantly smaller than in the normal camels. Water-deprivation was thought to cause reduced rate of tylosin elimination by the liver, as was shown for antipyrine--a drug which is eliminated from the body exclusively by the liver. Redistribution of tylosin in tissues concomitant with a greater proportion of drug in blood and extracellular fluid of water-deprived camels was suggested as a partial explanation for the higher serum drug levels seen after i.v. dosing. The low i.m. availability observed in the water-deprived camels implies that i.v. is the route of choice for tylosin administration to ill, dehydrated camels.
研究了在正常骆驼以及处于14天禁水期结束时的同一批骆驼中,静脉注射(i.v.)10 mg/kg和肌肉注射(i.m.)20 mg/kg酒石酸泰乐菌素的处置动力学。静脉注射治疗后,禁水骆驼的血清泰乐菌素浓度显著更高,药物消除速率更慢,分布容积显著更小,全身清除率也显著慢于正常骆驼。另一方面,肌肉注射给药后,禁水骆驼的血清药物浓度更低,平均吸收时间显著更短,肌肉注射的药物利用度显著低于正常骆驼。禁水被认为会导致肝脏对泰乐菌素的消除速率降低,就像安替比林那样——一种仅通过肝脏从体内消除的药物。有人提出,禁水骆驼组织中泰乐菌素的重新分布以及血液和细胞外液中药物比例的增加,是静脉注射给药后血清药物水平较高的部分原因。在禁水骆驼中观察到的低肌肉注射药物利用度意味着,对于生病、脱水的骆驼,静脉注射是泰乐菌素给药的首选途径。