Bertaccini G, Coruzzi G
Scand J Gastroenterol Suppl. 1986;121:30-6.
Besides the main effect of the H2 antagonists--that is, the inhibition of gastric acid secretion--these drugs possess several other pharmacological activities, which in most cases may be evident only for doses higher than those required to produce the H2 blockade. The non-secretory activities of the H2 antagonists may be classified into true side effects--that is, those independent of the primary action, which may or may not depend on the primary action. They concern the central and autonomic nervous systems, cardiovascular and endocrine systems, digestive system (gut, liver, pancreas), immune system, and so forth. It is obvious that when the actions of the different H2 blockers are completely at variance with regard to the same factor (cimetidine increase the TSH response to TRH, whereas ranitidine decreases it; ranitidine stimulates gastrointestinal motility, whereas oxmetidine inhibits it; ranitidine increases the exocrine pancreatic response to cholecystokinin, whereas oxmetidine decreases it; metiamide and cimetidine increase the activity of histamine methyltransferase, whereas burimamide decreases it), this is a clear demonstration that we are dealing with non-specific effects rather than with H2-receptor blockade. All these effects may be of interest because sometimes they may be useful in potentiating the primary action, and sometimes they may represent adverse reactions. In any case, they characterize pharmacologically the individual molecules of the family.
除了H2拮抗剂的主要作用(即抑制胃酸分泌)外,这些药物还具有其他几种药理活性,在大多数情况下,只有在高于产生H2受体阻滞所需的剂量时,这些活性才可能明显。H2拮抗剂的非分泌活性可分为真正的副作用,即那些独立于主要作用的副作用,这些副作用可能与主要作用有关,也可能无关。它们涉及中枢和自主神经系统、心血管和内分泌系统、消化系统(肠道、肝脏、胰腺)、免疫系统等等。显然,当不同的H2阻滞剂对同一因素的作用完全不同时(西咪替丁增加促甲状腺激素对促甲状腺激素释放激素的反应,而雷尼替丁则降低该反应;雷尼替丁刺激胃肠蠕动,而奥美替丁则抑制胃肠蠕动;雷尼替丁增加外分泌胰腺对胆囊收缩素的反应,而奥美替丁则降低该反应;甲硫米特和西咪替丁增加组胺甲基转移酶的活性,而布立马胺则降低该活性),这清楚地表明我们处理的是非特异性效应,而不是H2受体阻滞。所有这些效应都可能令人感兴趣,因为有时它们可能有助于增强主要作用,有时它们可能代表不良反应。无论如何,它们在药理学上表征了该类药物的各个分子。