Jantzen J P, Erdmann K, Hilley D, Klein A M
Anaesthesist. 1985 Jul;34(7):346-51.
Ketamine 25 mg/kg was administered to five foxhounds by the intravenous, intramuscular or rectal route. Plasma concentrations were measured by gas-chromatography and analgesia was tested by two techniques. Intravenous application gave reliable analgesia and well reproducible plasma levels in all subjects. Distribution and elimination half lives were found to be 6 min and 55 min, respectively. Intramuscular injection resulted in peak-plasma levels around the twentieth minute, elimination half life was fifty-two minutes, bioavailability 90%. Analgesia proved satisfactory in four out of the five subjects and lasted longer than after intravenous injection. The rectal route produced a wide range of peak-plasma levels, the average peak appearing after 40 min. We found an elimination halflife of 43 min and a bioavailability of 30%. Analgesia was poor in four out of the five subjects. The low plasma levels following rectal application are due to the poor bioavailability and this appears to be the reason for the unsatisfactory results with this route of administration. Bioavailability depends on the site of application (drainage mainly through the vena cava or portal vein) and the pH of the rectum.
将25毫克/千克的氯胺酮通过静脉、肌肉或直肠途径给予五只猎狐犬。通过气相色谱法测量血浆浓度,并通过两种技术测试镇痛效果。静脉给药在所有受试动物中均产生可靠的镇痛效果和可良好重现的血浆水平。分布半衰期和消除半衰期分别为6分钟和55分钟。肌肉注射导致血浆峰值水平出现在第20分钟左右,消除半衰期为52分钟,生物利用度为90%。在五只受试动物中有四只的镇痛效果令人满意,且持续时间比静脉注射后更长。直肠途径产生的血浆峰值水平范围较广,平均峰值出现在40分钟后。我们发现消除半衰期为43分钟,生物利用度为30%。在五只受试动物中有四只的镇痛效果较差。直肠给药后血浆水平较低是由于生物利用度差,这似乎是该给药途径效果不理想的原因。生物利用度取决于给药部位(主要通过腔静脉或门静脉引流)以及直肠的pH值。