Ueda C T, Beckmann P J, Dzindzio B S
Ther Drug Monit. 1984;6(1):43-9. doi: 10.1097/00007691-198403000-00009.
Saliva and serum quinidine concentrations were determined in six cardiac patients after twice-daily dosing with 324 or 648 mg quinidine gluconate and the relationship of these concentrations to the degree of suppression of ventricular premature beats (VPB) was evaluated. Mixed saliva and corresponding serum samples were obtained at various times after the 1st, 9th, and 19th doses. With serum quinidine concentrations ranging from 0.05 to 0.83 micrograms/ml after the first dose, the average saliva/serum ratios for quinidine varied between 0.25 and 1.35 (0.54 +/- 0.43). At steady state with the serum quinidine concentrations ranging between 0.36 and 3.35 micrograms/ml, the average saliva/serum ratios ranged from 0.27 to 1.79 (0.81 +/- 0.72) and from 0.19 to 1.84 (0.90 +/- 0.85) for the 9th and 19th doses, respectively. The interpatient variations in the saliva/serum ratio were large for the three doses (approximately 90%). On the other hand, the intrapatient variations were smaller and diminished with each succeeding sampled dose (from 31 to 18 to 12% for the 1st, 9th, and 19th doses, respectively). Moreover, the value for the quinidine saliva/serum ratio for a given patient was similar for all three doses. No significant correlation between the extent of VPB suppression and the concentrations of quinidine in the saliva or serum was observed. The data suggest that salivary quinidine concentrations may be clinically useful to monitor serum drug concentrations in a given patient. However, the relationship between saliva and serum quinidine concentrations and suppression of VPB measured by Holter monitoring is not clear-cut.
对6例心脏病患者每日两次服用324或648mg葡萄糖酸奎尼丁后,测定其唾液和血清中的奎尼丁浓度,并评估这些浓度与室性早搏(VPB)抑制程度之间的关系。在第1、9和19剂给药后的不同时间采集混合唾液和相应的血清样本。首次给药后血清奎尼丁浓度范围为0.05至0.83μg/ml,奎尼丁的平均唾液/血清比值在0.25至1.35之间(0.54±0.43)。在稳态下,血清奎尼丁浓度范围为0.36至3.35μg/ml,第9剂和第19剂的平均唾液/血清比值分别为0.27至1.79(0.81±0.72)和0.19至1.84(0.90±0.85)。这三剂药物的患者间唾液/血清比值变化很大(约90%)。另一方面,患者内变化较小,且随着后续采样剂量的增加而减小(第1、9和19剂分别从31%降至18%再降至12%)。此外,给定患者的奎尼丁唾液/血清比值在所有三剂药物中相似。未观察到VPB抑制程度与唾液或血清中奎尼丁浓度之间存在显著相关性。数据表明,唾液奎尼丁浓度在临床上可能有助于监测特定患者的血清药物浓度。然而,通过动态心电图监测测得的唾液和血清奎尼丁浓度与VPB抑制之间的关系并不明确。