Haegeli Laurent, Brunner-La Rocca Hans Peter, Wenk Markus, Pfisterer Matthias, Drewe Jürgen, Krähenbühl Stephan
Department of Cardiology, University Hospital, Basel, Switzerland.
Br J Clin Pharmacol. 2007 Dec;64(6):804-9. doi: 10.1111/j.1365-2125.2007.03035.x. Epub 2007 Sep 13.
In patients with decompensated heart failure, absorption of orally administered furosemide may be delayed, possibly leading to impaired pharmacodynamic effects. Sublingual administration may represent an alternative in such situations.
In a crossover study including 11 healthy men, 20 mg furosemide was administered intravenously, orally and sublingually on three different days. Pharmacokinetics and pharmacodynamics were assessed from repeated blood and urine samples.
Compared with oral administration, sublingual administration was associated with 43% higher C(max)[difference 215 ng ml(-1), 95% confidence interval (CI) 37, 392], a higher urinary recovery (8.9 vs. 7.3 mg, difference 1.6 mg, 95% CI 0.3, 2.9), an 28% higher AUC (difference 328 ng h(-1) ml(-1), 95% CI 24, 632) and a higher bioavailability of furosemide (59 vs. 47%, difference 12.0%, 95% CI -1.2, 25.2). Sodium excretion was higher after sublingual compared with oral administration (peak excretion rate 1.8 vs. 1.4 mmol min(-1), P < 0.05), whereas urine volume did not differ significantly between the two application modes. In comparison, intravenous administration showed the expected more rapid and intense response.
Sublingually administered furosemide tablets differ in certain kinetic and dynamic properties from identical tablets given orally. Sublingual administration of furosemide may offer therapeutic advantages in certain groups of patients.
在失代偿性心力衰竭患者中，口服速尿的吸收可能会延迟，这可能导致药效学效应受损。在这种情况下，舌下给药可能是一种替代方法。
在一项包括11名健康男性的交叉研究中，在三个不同的日子分别静脉内、口服和舌下给予20mg速尿。通过重复采集血液和尿液样本评估药代动力学和药效学。
与口服给药相比，舌下给药的C(max)高43%[差异215ng/ml，95%置信区间(CI)37,392]，尿回收率更高(8.9对7.3mg，差异1.6mg，95%CI0.3,2.9)，AUC高28%[差异328ng·h/ml，95%CI24,632]，速尿的生物利用度更高(59%对47%，差异12.0%，95%CI -1.2,25.2)。舌下给药后的钠排泄量高于口服给药(峰值排泄率1.8对1.4mmol/min，P<0.05)，而两种给药方式之间的尿量没有显著差异。相比之下，静脉给药显示出预期的更快和更强的反应。
舌下给药的速尿片在某些动力学和动态特性上与口服相同片剂不同。舌下给予速尿可能在某些患者群体中具有治疗优势。
