Gruen P H, Sachar E J, Langer G, Altman N, Leifer M, Frantz A, Halpern F S
Arch Gen Psychiatry. 1978 Jan;35(1):108-16. doi: 10.1001/archpsyc.1978.01770250110011.
The prolactin response to neuroleptics can serve as an index of dopamine blockade in humans. Plasma prolactin increments to single doses of chlorpromazine, and prolactin decrements to single doses of levodopa, were similar in normal and schizophrenic subjects. Antischizophrenic drugs of all chemical classes stimulated prolactin release,while chemically related drugs and other psychotropic agents ineffective in schizophrenia did not. The prolactin response to neuroleptic therapy occurred in all patients, and tolerance did not develop. Within subjects, prolactin responses were graded according to neuroleptic dose, but the upper limit of sensitivity of the response curve was achieved at doses below the therapeutic range. Relative prolactin-stimulating potency in humans of chlorpromazine, thioridazine, trifluoperazine, butaperazine, and haloperidol correlated well with their relative clinical potencies.
催乳素对抗精神病药物的反应可作为人体多巴胺阻断的指标。正常受试者和精神分裂症患者对单剂量氯丙嗪的血浆催乳素升高以及对单剂量左旋多巴的催乳素降低情况相似。所有化学类别的抗精神分裂症药物均刺激催乳素释放,而与化学结构相关但对精神分裂症无效的药物及其他精神药物则无此作用。所有患者均出现了催乳素对抗精神病药物治疗的反应,且未产生耐受性。在个体内部,催乳素反应根据抗精神病药物剂量分级,但反应曲线的敏感性上限在低于治疗范围的剂量时即已达到。氯丙嗪、硫利达嗪、三氟拉嗪、丁酰拉嗪和氟哌啶醇在人体中的相对催乳素刺激效力与其相对临床效力密切相关。