Activity of azithromycin against Leishmania major in vitro and in vivo.

Abstract

Abstract. Azithromycin, an azalide antibiotic of the macrolide family, concentrates in the tissues and especially in macrophages. Because Leishmania parasites reside in these cells, we tested this antibiotic for a possible antileishmanial activity in vitro and in vivo. Azithromycin decreased the Leishmania major promastigote count in cell-free cultures at log phase approximately 50-fold. In macrophage cultures infected with L. major amastigotes, azithromycin caused a significant decrease in parasite levels with an ED 50 of 12 g/ml. The activity in vivo was evaluated after infection of the footpads of susceptible BALB/cByJ mice and resistant C57BL/6J mice with L. major. Treatment of BALB/cByJ mice with azithromycin, 100 to 200 mg/kg/d, resulted in a significant decrease in lesion size and in the number of parasites per lesion, whereas no effect was seen in the treated C57BL/6J mice. Azithromycin has activity against L. major in vitro and in vivo. Given the severity of the disease and the limitations of the available therapeutic agents, azithromycin may have a significant role in the treatment of this group of diseases.

Failure of both azithromycin and antimony to treat cutaneous leishmaniasis in Manaus, AM, Brazil

“…In an experiment in-vitro and in-vivo model, azithromycin showed activity against Leishmania major (KROLEWIECKI et al, 2002). In an open trial in Brazil, it cured 16 out of 20 patients with cutaneous ulcers caused by Leishmania (Viannia) braziliensis, however, cure time, doses and cycles number presented high variability (PRATA et al, 2003).…”

Oral azithromycin versus its combination with miltefosine for the treatment of experimental Old World cutaneous leishmaniasis

“…As it concentrates in tissues and especially in macrophages, and may reach levels 100 to 200 times higher than those in serum (Gladue et al 1989) therefore, its potential role as antileishmanial agent was evaluated. Krolewiecki et al (2002) demonstrated that, azithromycin has antileishmanial activity following its subcutaneous adminstration in BALB\c mice infected with Leishmania major. Moreover, Sinagra et al (2007) reported significant activity of its oral adminstration against Leishmania (Viannia) braziliensis however, no activity against infections with Leishmania (Leishmania) amazonensis in golden hamsters could be observed.…”

O uso da associação azitromicina e N-metil glucamina no tratamento da leishmaniose cutânea causada por Leishmania (Leishmania) amazonensis em camundongos C57BL6

“…[5][6][7] A classe dos macrolídeos atua inibindo a síntese proteica, dissociando o peptídio do ribossomo. 6 Tem características como a de concentrarse nos tecidos, especialmente nos macrófagos, com níveis 100 a 200 vezes superiores do que no soro, tornando-a atrativa para o tratamento de infecções causadas por micro-organismos intracelulares.…”

“…Usando-a no tratamento de pacientes, foi demonstrada ação leishmaniostática com resposta terapêutica mais lenta do que a dos antimoniais. 5 Em experimentações in vitro, a azitromicina não contribuiu para a fagocitose da L. major, mas aumentou a taxa de morte intracelular das amastigotas. 8 Outra possibilidade é que a azitromicina tenha efeito imunomodulador, diminuindo-lhes o número e ativando neutrófilos e prevenindo a produção de mediadores e citocinas pró-inflamatórias.…”

“…8 Outra possibilidade é que a azitromicina tenha efeito imunomodulador, diminuindo-lhes o número e ativando neutrófilos e prevenindo a produção de mediadores e citocinas pró-inflamatórias. 5,9 In…”