Aherne G W, Piall E M, Twycross R G
Br J Clin Pharmacol. 1979 Dec;8(6):577-80. doi: 10.1111/j.1365-2125.1979.tb01047.x.
1 Venous blood was obtained from patients with far-advanced cancer receiving either diamorphine (diacetylmorphine, heroin) hydrochloride (65 samples) or morphine sulphate (24 samples) regularly by mouth in doses from 2.5 mg to 90 mg every 4 h. 2 Samples were obtained within 30 min of the 09.00 h drug round. 3 Serial samples were also obtained over a 4 h period from three patients receiving diamorphine hydrochloride. 4 Assay of serum 'morphine equivalents' was by radioimmunoassay using an antibody that cross reacts almost equally with diamorphine, 6-0 monoacetylmorphine and morphine. 5 The serum concentration of opiates expressed as 'morphine equivalents' ranged from 11 ng/ml to 1440 ng/ml. 6 A highly significant positive linear correlation exists between the dose administered and the serum concentration (P less than 0.001) with respect to both drugs. 7 There was no difference between the two drugs in relation to the serum concentration achieved per 10 mg of opiate administered. 8 Higher oral doses of both diamorphine and morphine are now being used when indicated rather than, as before, resorting to injections when an oral dose in excess of 40 mg is indicated.
从患有晚期癌症且正在定期口服盐酸二醋吗啡(二乙酰吗啡、海洛因)(65份样本)或硫酸吗啡(24份样本)的患者身上采集静脉血,每4小时口服剂量为2.5毫克至90毫克。
在上午9点给药后的30分钟内采集样本。
还从三名接受盐酸二醋吗啡的患者身上在4小时内采集了系列样本。
血清“吗啡等效物”的测定采用放射免疫分析法,使用的抗体与二醋吗啡、6-0单乙酰吗啡和吗啡的交叉反应几乎相同。
以“吗啡等效物”表示的阿片类药物血清浓度范围为11纳克/毫升至1440纳克/毫升。
就两种药物而言,给药剂量与血清浓度之间存在高度显著的正线性相关性(P小于0.001)。
每服用10毫克阿片类药物所达到的血清浓度,两种药物之间没有差异。
现在,当有指征时,会使用更高剂量的二醋吗啡和吗啡口服,而不是像以前那样,当口服剂量超过40毫克有指征时就采用注射方式。