Downey K M, Chaput de Saintonge D M
Br J Clin Pharmacol. 1986 Mar;21(3):295-9. doi: 10.1111/j.1365-2125.1986.tb05193.x.
Ten healthy normal volunteers received an intravenous infusion of erythromycin lactobionate over 60 min to a total dose of 800 mg (n = 9), and 524 mg (n = 1). Blood samples were collected at 10 min intervals for 100 min and gastric contents aspirated, via a nasogastric tube, from pre-dose to 105 min after start of infusion. Incidence and severity of three gastrointestinal symptoms (nausea, stomach discomfort and feelings of hunger), two CNS symptoms (dizziness and faintness) and a 'control' symptom (back pain) were measured using 100 mm visual analogue scales. Rate of infusion and plasma erythromycin concentration correlated with nausea (P less than 0.001) and stomach discomfort (P less than 0.001); plasma erythromycin concentration was also correlated with dizziness (P less than 0.05). Concentrations of active erythromycin in the aspirate were pH dependent. In one subject the concentration of erythromycin in the aspirate exceeded that in the plasma by 100 fold. Bile staining of samples containing the highest levels of microbiologically active erythromycin makes the origin of the erythromycin in these samples uncertain.
十名健康正常志愿者在60分钟内静脉输注乳糖酸红霉素,总剂量为800毫克(n = 9),以及524毫克(n = 1)。每隔10分钟采集血样,共采集100分钟,并通过鼻胃管在给药前至输注开始后105分钟抽吸胃内容物。使用100毫米视觉模拟量表测量三种胃肠道症状(恶心、胃部不适和饥饿感)、两种中枢神经系统症状(头晕和昏厥)以及一种“对照”症状(背痛)的发生率和严重程度。输注速率和血浆红霉素浓度与恶心(P < 0.001)和胃部不适(P < 0.001)相关;血浆红霉素浓度也与头晕相关(P < 0.05)。抽吸物中活性红霉素的浓度取决于pH值。在一名受试者中,抽吸物中红霉素的浓度比血浆中的浓度高出100倍。含有最高水平微生物活性红霉素的样本出现胆汁染色,使得这些样本中红霉素的来源不确定。