Grady R W, Peterson C M, Jones R L, Graziano J H, Bhargava K K, Berdoukas V A, Kokkini G, Loukopoulos D, Cerami A
J Pharmacol Exp Ther. 1979 Jun;209(3):342-8.
The use of rhodotorulic acid (RA) as an iron-chelating drug was suggested by experiments in hypertransfused rats in which urinary and fecal iron excretion were significantly enhanced in response to RA. The toxicity of the drug appears to be minimal at a parenteral dose less than 250 mg/kg. An increased excretion of zinc was the only notable side effect of the drug at the doses used. When administered i.v. to humans, RA was only 16% more effective than desferrioxamine (DF). Pharmacokinetic studies showed that RA persisted in the bloodstream of dogs 6 times longer than desferrioxamine after an intravenous injection. Accordingly RA was evaluated as a potential repository drug. While animal experiments were encouraging, human subjects experienced a painful local reaction to RA administered either i.m. or s.c. as a suspension in physiological saline. Accordingly it appears that RA is best looked at as a second line drug, unless a means can be found to obviate local inflammatory reactions.
在多次输血的大鼠实验中发现，给予红酵母氨酸（RA）后，尿铁和粪铁排泄显著增加，这提示RA可作为一种铁螯合剂药物。当非肠道给药剂量小于250mg/kg时，该药物的毒性似乎最小。在所使用的剂量下，药物唯一显著的副作用是锌排泄增加。静脉注射给人类时，RA的疗效仅比去铁胺（DF）高16%。药代动力学研究表明，静脉注射后，RA在犬类血液中的持续时间比去铁胺长6倍。因此，RA被评估为一种潜在储存型药物。虽然动物实验结果令人鼓舞，但人类受试者皮下或肌肉注射生理盐水混悬液形式的RA时会出现疼痛的局部反应。因此，除非能找到消除局部炎症反应的方法，否则RA似乎最好被视为二线药物。
