Serfontein W J, Mekel R
Res Commun Chem Pathol Pharmacol. 1979 Nov;26(2):391-411.
A survey of the leterature on bismuth toxicity in man in relation to blood level data, has revealed the necessity of distinguishing between lipid soluble and water soluble organic complexes of bismuth on the one hand and the simple inorganic salts of bismuth on the other hand. A characteristic feature of the former, illustrated by the water soluble bismuth complex triglycollamate, is the high bismuth levels (due to absorption of the complex as such) and the nephrotoxic properties of the compound in man. Bismuth absorption after administration of the simple inorganic salts of bismuth is postulated to occur in the form of ionic bismuth as such, low bismuth levels being characteristic features of such compounds. Bismuth blood and urine levels obtained from patients after administration of a new anti-ulcer drug (Bicitropeptide) in a well controlled clinical trial are discussed and suggest that that this bismuth containing drug behaves pharmacologically in a manner similar to the inorganic bismuth salts in man, low bismuth blood levels and the absence of toxic side effects being conspicuous features of the drug. Based on these considerations, it is proposed that the pharmacologically active bismuth compounds be divided into four different groups depending on structure, stability and solubility. The question as to what constitutes a "toxic bismuth blood level" can only be discussed in relation to the new proposed sub-division of bismuth compounds and is only meaningful if the term is defined to relate only to ionic bismuth (presumably bound to a large extent to blood proteins). Based on information gleaned from the literature and blood level values reported in the clinical trial referred to, it is suggested that bismuth blood level values below 50 micrograms/ml are highly unlikely to be associated with meaningful toxicity in man. Finally, attention is drawn to the reversibility of bismuth toxicity in man as reported by many authors irrespective of the type of bismuth compound concerned.
一项关于人体铋毒性与血药浓度数据关系的文献综述表明，有必要区分铋的脂溶性和水溶性有机络合物与铋的简单无机盐。前者的一个特征，以水溶性铋络合物三乙醇胺铋酸盐为例，是铋水平较高（由于该络合物本身被吸收）以及该化合物对人体具有肾毒性。服用铋的简单无机盐后，铋的吸收被假定以离子铋的形式发生，低铋水平是此类化合物的特征。文中讨论了在一项严格控制的临床试验中，患者服用一种新型抗溃疡药物（双环肽）后测得的铋血药浓度和尿药浓度，结果表明这种含铋药物在人体中的药理行为与无机铋盐相似，低铋血药浓度和无毒性副作用是该药物的显著特征。基于这些考虑，建议根据结构、稳定性和溶解性将具有药理活性的铋化合物分为四类。关于什么构成“毒性铋血药浓度”的问题，只能结合新提出的铋化合物分类来讨论，并且只有在该术语被定义为仅与离子铋（可能在很大程度上与血液蛋白结合）相关时才有意义。根据从文献中收集的信息以及上述临床试验报告的血药浓度值，建议铋血药浓度值低于50微克/毫升时，人体极不可能出现有意义的毒性反应。最后，许多作者报告指出无论涉及何种铋化合物，人体铋中毒都具有可逆性，提请注意这一点。
