Rhodotorulic acid--investigation of its potential as an iron-chelating drug

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 increa...

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Published inThe Journal of pharmacology and experimental therapeutics Vol. 209; no. 3; pp. 342 - 348
Main Authors Grady, R W, Peterson, C M, Jones, R L, Graziano, J H, Bhargava, K K, Berdoukas, V A, Kokkini, G, Loukopoulos, D, Cerami, A
Format Journal Article
LanguageEnglish
Published United States Elsevier Inc 01.06.1979
American Society for Pharmacology and Experimental Therapeutics
Subjects
Adult
Animals
Deferoxamine - pharmacology
Dogs
Female
Haplorhini
Humans
Hydroxamic Acids - administration & dosage
Hydroxamic Acids - adverse effects
Hydroxamic Acids - metabolism
Hydroxamic Acids - pharmacology
Hydroxybenzoates - pharmacology
Infusions, Parenteral
Injections, Intramuscular
Iron - metabolism
Iron Chelating Agents
Macaca fascicularis
Male
Mice
Piperazines - administration & dosage
Piperazines - adverse effects
Piperazines - metabolism
Piperazines - pharmacology
Rats
Rhodotorula
Thalassemia - metabolism
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Summary: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.
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ISSN:0022-3565
1521-0103
DOI:10.1016/S0022-3565(25)31674-5