Ross C E, Toon S, Rowland M, Murray G H, Meya U
Medeval Ltd., Manchester, GB.
Pharmacopsychiatry. 1988 Sep;21(5):222-5. doi: 10.1055/s-2007-1021946.
Rolipram is an antidepressant with a novel mechanism of action: enhanced noradrenaline (first messenger) synthesis and release, and inhibition of cAMP (second messenger) breakdown. This study was aimed at objectively assessing potential anticholinergic effects of rolipram in healthy elderly volunteers by measurement of saliva production and pupil size. Eight male volunteers between 67 and 77 years of age first received in a randomized manner either a single dose of 50 mg amitriptyline or a placebo control. After a minimum washout period of seven days, they then received a multiple dosing regimen of a) 0.75 mg and b) 1.5 mg rolipram given every eight hours over a 5-day period with a two day washout between a) and b). Whereas no changes at all in pupil size could be observed, amitripyline significantly reduced salivary flow. Rolipram however had no effect on saliva production after either single or repeated administration of 0.75 or 1.5 mg. The results are discussed in connection with pharmacokinetic parameters obtained in the study.
增强去甲肾上腺素（第一信使）的合成与释放，并抑制环磷酸腺苷（第二信使）的分解。本研究旨在通过测量唾液分泌量和瞳孔大小，客观评估咯利普兰对健康老年志愿者的潜在抗胆碱能作用。8名年龄在67至77岁之间的男性志愿者首先以随机方式接受单剂量50毫克阿米替林或安慰剂对照。经过至少7天的洗脱期后，他们接着接受多剂量给药方案：a）0.75毫克和b）1.5毫克咯利普兰，在5天内每8小时给药一次，a）和b）之间有2天的洗脱期。虽然未观察到瞳孔大小有任何变化，但阿米替林显著减少了唾液分泌量。然而，无论是单次还是重复给予0.75毫克或1.5毫克咯利普兰后，其对唾液分泌均无影响。结合研究中获得的药代动力学参数对结果进行了讨论。
