Department of Pediatric Nephrology, University Hospitals Leuven, Herestraat 49, 3000 Leuven, Belgium.
Mol Genet Metab. 2012 Sep;107(1-2):234-6. doi: 10.1016/j.ymgme.2012.06.017. Epub 2012 Jul 6.
Halitosis due to dimethylsulfide (DMS) generation is a major side effect of cysteamine in the treatment of cystinosis. Recently, an enteric coated formulation of cysteamine bitartrate (RP103) administered twice daily was demonstrated to be non-inferior for lowering WBC cystine levels compared to the non-enteric coated formulation (Cystagon®), administered 4 times per day. Since both formulations had different pharmacokinetic profiles, we compared DMS breath levels after administration of either RP103 or Cystagon® in four cystinosis patients. Although cysteamine areas under the curve (AUCs) were comparable, AUC of DMS was lower after the administration of RP103 compared to Cystagon®. This observation is of importance in cystinosis patients, since halitosis hampers compliance with cysteamine therapy.
由于二甲基硫(DMS)的产生而导致的口臭是半胱胺治疗胱氨酸病的一个主要副作用。最近,每日两次给予包衣的柠檬酸半胱胺(RP103)的制剂在降低白细胞胱氨酸水平方面与每日四次给予非包衣制剂(Cystagon®)相比显示出非劣效性。由于这两种制剂具有不同的药代动力学特征,我们比较了 4 例胱氨酸病患者接受 RP103 或 Cystagon®后的 DMS 呼气水平。尽管半胱胺的曲线下面积(AUC)相似,但 RP103 给药后的 DMS AUC 低于 Cystagon®。这一观察结果在胱氨酸病患者中很重要,因为口臭会影响对半胱胺治疗的依从性。