title: Effects of the glucantime on the kinetic of biodistribution of radiopharmaceuticals in Wistar rats.
abstract: There are evidences that some drugs used for the human diseases can modify the biodistribution of radiopharmaceuticals. The N-methyl meglumine antimoniate, commercially known as glucantime (Rhodia, Brazil), is the elected drug for the treatment of all the clinical forms of leishmaniasis. As therapeutic drugs can present important toxic effects, we studied the effects of the glucantime on the kinetic of biodistribution of radiopharmaceuticals. To study the glucantime effect on the biodistribution of technetium-99m-methylenediphosphonic acid (99mTc-MDP), glucantime IM (80 mg/kg/day) was administered into male Wistar rats (3 months old age) in single dose during 7 days. 99mTc-MDP was injected 1 hr after the last dose. The animals (n = 24) were divided into two groups: treated (n = 12) and control (n = 12) and they were rapidly sacrificed, respectively, in 3 periods (5, 30 and 120 min) after administration of the 99mTc-MDP. The organs were isolated (brain, heart, thyroid, lungs, kidneys, testis, stomach, intestines, pancreas, spleen, liver, muscle, bone and bladder) and the percentages of radioactivity (%ATI) in each organ were calculated. The results were analyzed by the Wilcoxon test (p < 0.05). The analysis of the results has shown a significant increase of the %ATI after 5 min administration of the 99mTc-MDP in spleen, kidneys, testis, heart, liver and a reduction of %ATI in bladder. Thirty minutes after administration of the 99mTc-MDP, the analysis ofthe results reveals a significant reduction of the %ATI in femur, kidneys, thin bowel, lungs, heart, liver and an increase in abdominal muscle and stout bowel. One hundred-twenty min after administration of the 99mTc-MDP, the analysis of the results shows a significant reduction of the %ATI in spleen, thyroid, blood, femur, kidneys, liver and an increase in bladder, pancreas and lungs. Biochemical dosages were also performed before (control group, n = 12) and after (treated group, n = 12) treatment with glucantime. There was a significant (p < 0.05) decrease to the biochemical levels after the treatment with glucantime in following dosages: blood urea nitrogen, creatinine, alkaline phosphatase, lactic dehydrogenase, aspartate amino transferase, total creatine kinase, total protein, globulin and albumin. These results were compared with the control group, without glucantime, and statistical analyses were performed (t-student test, p < 0.05). These results could be associated with the biological effects and/or metabolization of the studied drug.
authors.affiliation: Universidade Federal do Rio Grande do Norte, Centro de Biociências, Departamento de Microbiologia e Parasitologia, Av. Salgado Filho, 3000, 59078-970, Natal, RN, Brazil. cechol@ufrnet.br
authors.forename: C M C
authors.initials: CM
authors.lastname: Xavier Holanda
authors.forename: R L
authors.initials: RL
authors.lastname: Cavalcanti Jales
authors.forename: M T J
authors.initials: MT
authors.lastname: Almeida Catanho
authors.forename: R C
authors.initials: RC
authors.lastname: Holanda Leite
authors.forename: L M
authors.initials: LM
authors.lastname: Lopes de Brito
authors.forename: L H
authors.initials: LH
authors.lastname: Jales-Junior
authors.forename: K C
authors.initials: KC
authors.lastname: Brandao
authors.forename: L F
authors.initials: LF
authors.lastname: Amorim
authors.forename: G G
authors.initials: GG
authors.lastname: de Brito Tiago
authors.forename: M L
authors.initials: ML
authors.lastname: Gomes
authors.forename: M
authors.initials: M
authors.lastname: Bernardo-Filho
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000633:toxicity; D004347:Drug Interactions; D006801:Humans; D007896:Leishmaniasis / Q000188:drug therapy; D008297:Male; D008536:Meglumine / Q000633:toxicity*; D000077485:Meglumine Antimoniate; D009942:Organometallic Compounds / Q000633:toxicity*; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar; D013669:Technetium Tc 99m Medronate / Q000493:pharmacokinetics*; D014018:Tissue Distribution
chemical_list: D000981:Antiprotozoal Agents; D009942:Organometallic Compounds; D019275:Radiopharmaceuticals; D008536:Meglumine; D000077485:Meglumine Antimoniate; D013669:Technetium Tc 99m Medronate