Sechi L A, Tedde R, Cassisa L, Marigliano A, Uneddu F, Melis A, Pala A
Hypertension Unit, University of Sassari, Italy.
J Cardiovasc Pharmacol. 1990 Feb;15(2):269-75. doi: 10.1097/00005344-199002000-00014.
Ketanserin, an antagonist of 5-HT2-serotonergic and alpha 1-adrenergic receptors, has come into use for the therapy of mild to moderate arterial hypertension. Quite recent observations have shown changes in transmembrane sodium (Na) transport after the acute administration of high doses of this drug to normal subjects. It is well known that some of these transport systems have an altered activity in essential hypertension. We evaluated the effects of long-term (3 months) administration of ketanserin (40-80 mg/day) on Na and potassium (K) intracellular concentrations and transmembrane fluxes in red blood cells (RBCs) from 12 essential hypertensive patients. In addition the present study describes the in vitro effects of two different concentrations of the drug (5 x 10(-8) and 5 x 10(-7) M) on erythrocytes in normal subjects. In the first study, both systolic and diastolic blood pressure were significantly lowered by the treatment with ketanserin (from 165/103 to 143/89; p less than 0.001). Na and K intraerythrocyte concentrations fell markedly during ketanserin administration (both p less than 0.001). A marked decrease in Na,K-pump activity (p less than 0.001) and an increase in Na,lithium(Li)-countertransport function (p less than 0.001) were observed. Na outward cotransport, Na leak, and K leak were not modified by the therapy. Direct correlation was found between the fall in mean blood pressure and in Na and K intraerythrocyte concentration (respectively, p less than 0.01 and p less than 0.05).(ABSTRACT TRUNCATED AT 250 WORDS)
酮色林是一种5-羟色胺2（5-HT2）-血清素能和α1-肾上腺素能受体拮抗剂，已用于治疗轻至中度动脉高血压。最近的观察结果表明，在给正常受试者急性大剂量服用该药后，跨膜钠（Na）转运发生了变化。众所周知，这些转运系统中的一些在原发性高血压中活性发生了改变。我们评估了长期（3个月）服用酮色林（40 - 80毫克/天）对12例原发性高血压患者红细胞（RBC）内钠（Na）和钾（K）浓度及跨膜通量的影响。此外，本研究描述了两种不同浓度的药物（5×10⁻⁸和5×10⁻⁷摩尔/升）对正常受试者红细胞的体外作用。在第一项研究中，酮色林治疗可使收缩压和舒张压显著降低（从165/103降至143/89；p＜0.001）。在服用酮色林期间，红细胞内Na和K浓度显著下降（均为p＜0.001）。观察到钠钾泵活性显著降低（p＜0.001），钠锂（Li）逆向转运功能增加（p＜0.001）。钠外向协同转运、钠泄漏和钾泄漏未因治疗而改变。发现平均血压下降与红细胞内Na和K浓度下降之间存在直接相关性（分别为p＜0.01和p＜0.05）。（摘要截选至250字）
