Bernini G, Taddei S, Graziadei L, Pedrinelli R, Salvetti A
J Hypertens Suppl. 1985 Nov;3(2):S117-9.
It has been reported that endogenous opioid antagonism through naloxone (NAL) blunts the hypotensive effect of captopril (CAP) in normal man. For this reason a study was carried out to determine whether NAL interacts with the antihypertensive effect of CAP in patients with mild-to-moderate essential hypertension (n = 6; age 22-43 years). Patients received, according to a randomized code, placebo (PL) during saline infusion, CAP (25 mg orally) during saline infusion, PL + NAL (0.4 mg as a bolus followed by a continuous infusion of 4.0 mg/h for 2 h) and CAP + NAL at the same doses. Three-day intervals elapsed between each phase of the study. Blood pressure (BP) and heart rate (HR) were recorded before (-20 to 0 min) and every 15 min for the next 2 h after drug administration. Blood samples for plasma renin activity (PRA), noradrenaline (NA) and aldosterone (ALD) were collected before (time 0) and 120 min after drug administration. Neither PL nor NAL changed any of the parameters examined, while CAP alone reduced mean BP to a highly significant extent. Naloxone did not change the hypotensive effect of CAP to any significant extent. Captropril, either alone or associated with NAL, tended to reduce plasma ALD and increase PRA (P less than 0.05) without changing HR or plasma NA. These data indicate that, at least under the experimental conditions used, endogenous opioid antagonism does not interfere with the haemodynamic and humoral effect of CAP in essential hypertensive man. This suggests that endogenous opioids do not mediate the pharmacological actions of CAP.
据报道,通过纳洛酮(NAL)进行内源性阿片拮抗可减弱卡托普利(CAP)对正常人的降压作用。因此,开展了一项研究,以确定NAL是否会与轻度至中度原发性高血压患者(n = 6;年龄22 - 43岁)中CAP的降压作用相互影响。患者根据随机编码,在输注生理盐水期间接受安慰剂(PL),在输注生理盐水期间接受CAP(口服25毫克),接受PL + NAL(静脉推注0.4毫克,随后以4.0毫克/小时的速度持续输注2小时)以及相同剂量的CAP + NAL。研究的每个阶段之间间隔三天。在给药前(-20至0分钟)以及给药后的接下来2小时内每15分钟记录一次血压(BP)和心率(HR)。在给药前(时间0)和给药后120分钟采集血样,检测血浆肾素活性(PRA)、去甲肾上腺素(NA)和醛固酮(ALD)。单独使用PL或NAL均未改变所检测的任何参数,而单独使用CAP可使平均血压显著降低。纳洛酮在任何显著程度上均未改变CAP的降压作用。卡托普利单独使用或与NAL联合使用时,倾向于降低血浆ALD并增加PRA(P < 0.05),而不改变HR或血浆NA。这些数据表明,至少在所使用的实验条件下,内源性阿片拮抗并不干扰CAP对原发性高血压患者的血流动力学和体液效应。这表明内源性阿片类物质并不介导CAP的药理作用。