Tissue distribution of residual antimony in rats treated with multiple doses of meglumine antimoniate
Meglumine antimoniate (MA) and sodium stibogluconate are pentavalent antimony (SbV) drugs used since the mid-1940s. Notwithstanding the fact that they are first-choice drugs for the treatment of leishmaniases, there are gaps in our knowledge of their toxicological profile, mode of action and kinetic...
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| Format: | Article |
| Language: | English |
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Fundação Oswaldo Cruz (FIOCRUZ)
2014-07-01
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| Series: | Memorias do Instituto Oswaldo Cruz |
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| Online Access: | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0074-02762014000400420&lng=en&tlng=en |
| _version_ | 1827842588794683392 |
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| author | Deise Riba Coelho Elaine Silva Miranda Tatiana Dillenburg Saint?Pierre Francisco José Roma Paumgartten |
| author_facet | Deise Riba Coelho Elaine Silva Miranda Tatiana Dillenburg Saint?Pierre Francisco José Roma Paumgartten |
| author_sort | Deise Riba Coelho |
| collection | DOAJ |
| description | Meglumine antimoniate (MA) and sodium stibogluconate are pentavalent antimony (SbV) drugs used since the mid-1940s. Notwithstanding the fact that they are first-choice drugs for the treatment of leishmaniases, there are gaps in our knowledge of their toxicological profile, mode of action and kinetics. Little is known about the distribution of antimony in tissues after SbV administration. In this study, we evaluated the Sb content of tissues from male rats 24 h and three weeks after a 21-day course of treatment with MA (300 mg SbV/kg body wt/d, subcutaneous). Sb concentrations in the blood and organs were determined by inductively coupled plasma-mass spectrometry. In rats, as with in humans, the Sb blood levels after MA dosing can be described by a two-compartment model with a fast (t1/2 = 0.6 h) and a slow (t1/2 >> 24 h) elimination phase. The spleen was the organ that accumulated the highest amount of Sb, while bone and thyroid ranked second in descending order of tissues according to Sb levels (spleen >> bone, thyroid, kidneys > liver, epididymis, lungs, adrenals > prostate > thymus, pancreas, heart, small intestines > skeletal muscle, testes, stomach > brain). The pathophysiological consequences of Sb accumulation in the thyroid and Sb speciation in the liver, thyroid, spleen and bone warrant further studies. |
| first_indexed | 2024-03-12T08:11:51Z |
| format | Article |
| id | doaj.art-4daa606f70cd484f819ade5735569e22 |
| institution | Directory Open Access Journal |
| issn | 1678-8060 |
| language | English |
| last_indexed | 2024-03-12T08:11:51Z |
| publishDate | 2014-07-01 |
| publisher | Fundação Oswaldo Cruz (FIOCRUZ) |
| record_format | Article |
| series | Memorias do Instituto Oswaldo Cruz |
| spelling | doaj.art-4daa606f70cd484f819ade5735569e222023-09-02T19:06:39ZengFundação Oswaldo Cruz (FIOCRUZ)Memorias do Instituto Oswaldo Cruz1678-80602014-07-01109442042710.1590/0074-0276140030S0074-02762014000400420Tissue distribution of residual antimony in rats treated with multiple doses of meglumine antimoniateDeise Riba CoelhoElaine Silva MirandaTatiana Dillenburg Saint?PierreFrancisco José Roma PaumgarttenMeglumine antimoniate (MA) and sodium stibogluconate are pentavalent antimony (SbV) drugs used since the mid-1940s. Notwithstanding the fact that they are first-choice drugs for the treatment of leishmaniases, there are gaps in our knowledge of their toxicological profile, mode of action and kinetics. Little is known about the distribution of antimony in tissues after SbV administration. In this study, we evaluated the Sb content of tissues from male rats 24 h and three weeks after a 21-day course of treatment with MA (300 mg SbV/kg body wt/d, subcutaneous). Sb concentrations in the blood and organs were determined by inductively coupled plasma-mass spectrometry. In rats, as with in humans, the Sb blood levels after MA dosing can be described by a two-compartment model with a fast (t1/2 = 0.6 h) and a slow (t1/2 >> 24 h) elimination phase. The spleen was the organ that accumulated the highest amount of Sb, while bone and thyroid ranked second in descending order of tissues according to Sb levels (spleen >> bone, thyroid, kidneys > liver, epididymis, lungs, adrenals > prostate > thymus, pancreas, heart, small intestines > skeletal muscle, testes, stomach > brain). The pathophysiological consequences of Sb accumulation in the thyroid and Sb speciation in the liver, thyroid, spleen and bone warrant further studies.http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0074-02762014000400420&lng=en&tlng=enpentavalent antimonialsthyroidliverleishmaniasesGlucantimepharmacokinetics |
| spellingShingle | Deise Riba Coelho Elaine Silva Miranda Tatiana Dillenburg Saint?Pierre Francisco José Roma Paumgartten Tissue distribution of residual antimony in rats treated with multiple doses of meglumine antimoniate Memorias do Instituto Oswaldo Cruz pentavalent antimonials thyroid liver leishmaniases Glucantime pharmacokinetics |
| title | Tissue distribution of residual antimony in rats treated with multiple doses of meglumine antimoniate |
| title_full | Tissue distribution of residual antimony in rats treated with multiple doses of meglumine antimoniate |
| title_fullStr | Tissue distribution of residual antimony in rats treated with multiple doses of meglumine antimoniate |
| title_full_unstemmed | Tissue distribution of residual antimony in rats treated with multiple doses of meglumine antimoniate |
| title_short | Tissue distribution of residual antimony in rats treated with multiple doses of meglumine antimoniate |
| title_sort | tissue distribution of residual antimony in rats treated with multiple doses of meglumine antimoniate |
| topic | pentavalent antimonials thyroid liver leishmaniases Glucantime pharmacokinetics |
| url | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0074-02762014000400420&lng=en&tlng=en |
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