Association of oxamniquine praziquantel and clonazepam in experimental Schistosomiasis mansoni

Araújo, Neusa; Mattos, Ana Carolina Alves de; Coelho, Paulo Marcos Zech; Katz, Naftale

doi:10.1590/s0074-02762008000800007

Cited by 15 publications

(18 citation statements)

References 11 publications

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“…The failure of imatinib treatment cannot yet be explained, since the dosage of imatinib administered was very high, over 50 times higher than the clinical dose for daily treatment. Again, the discrepancy between the results obtained when comparing antischistosomal agents in vitro and in vivo has already been described (Araújo et al 2008). Although in vitro studies are useful to generate knowledge, they are obviously limited.…”

Section: Discussionmentioning

confidence: 99%

Imatinib activity on Schistosoma mansoni

Katz¹,

Couto

Araújo

2013

Mem. Inst. Oswaldo Cruz

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Imatinib, a drug used for treatment of human chronic myeloid leukaemia, due to its activity against protein kinases, has been also evaluated in vitro against Schistosoma mansoni showing high schistosomicidal activity. In the present experiments imatinib activity in vitro was confirmed at the doses of 25 µM, 50 µM and 100 µM. The first drug activity observed with the lower dose was interruption of egg-laying and with the higher dosages was the death of the worms. In mice infected with S. mansoni no activity was found even with 1,000 mg/kg/day, 500 mg/kg/day, single oral dose or when administered for three consecutive days. This is another example of the difference of results related to in vitro and in vivo trials using S. mansoni worms.

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Section: Discussionmentioning

confidence: 99%

Imatinib activity on Schistosoma mansoni

Katz¹,

Couto

Araújo

2013

Mem. Inst. Oswaldo Cruz

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“…We also evaluated the in vitro effect of an association of C/E and PZQ on S. mansoni adult worms, because chemotherapy with a combination of different drugs has been used for the treatment of infectious disease in order to delay or prevent an increase in drug resistance. [43][44][45] The methodology was modified from that proposed by Araujo and co-workers. 44 After thirty minutes of adaptation of the parasites, a solution of C/E in methanol (5.0 mg/mL) and PZQ solubilized in RPMI-1640 (0.8 mg/mL) was added to the cultures.…”

Section: Introductionmentioning

confidence: 99%

“…[43][44][45] The methodology was modified from that proposed by Araujo and co-workers. 44 After thirty minutes of adaptation of the parasites, a solution of C/E in methanol (5.0 mg/mL) and PZQ solubilized in RPMI-1640 (0.8 mg/mL) was added to the cultures. For this purpose, we used associations of PZQ:C/E in the following proportions (lg/mL): 0.5:23.8, 0.5:11.9, 0.5:6.0; 0.25:23.8, 0.25:11.9, 0.25:6.0.…”

Section: Introductionmentioning

confidence: 99%

In vitro evaluation of the schistosomicidal effect of the extracts, fractions and major 3-hydroxy-2,6-dialkyl-substituted piperidine alkaloids from the flowers of Senna spectabilis (Fabaceae)

Castro

Silva

et al. 2016

Bioorganic & Medicinal Chemistry Letters

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In this work, we present the in vitro schistosomicidal activity evaluation of the most active dichloromethane fraction (FDm) (ED50=83.5μg/mL) and of a mixture of the major alkaloids ((-)-cassine/(-)-spectaline, C/E) (ED50=37.4μg/mL) from the flowers of Senna spectabilis against adult worms and cercariae. We also demonstrate other toxic effects including paralysis of the adult worms, inhibition of the secretory activity, tegument lesions and cercaricidal activity. In the association test of Praziquantel (PZQ)-C/E, we observed up to 80% mortality of Schistosoma mansoni in comparison to PZQ monotherapy. Due to the diversity of the toxic effects, the schistosomicidal activity of C/E is likely a result of a multitarget mechanism involving the tegument, secretory system and neuromotor action.

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“…Recently there have been reports of the emergence of schistosome phenotypes that are resistant to PZQ chemotherapy [50]. Other therapeutic drugs include clonazepam and oxamniquine and their positive effects were reported [51,52].…”

Section: Treatment Of Ph Secondary To Schistosomiasismentioning

confidence: 99%

Pulmonary vascular disease associated with schistosomiasis

Kolosionek

Crosby

Harhay

et al. 2010

Expert Review of Anti-infective Therapy

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In this article we focus on the pathogenesis and clinical characteristics of schistosomiasis infection on the lung vasculature. Overall, the basic biology and understanding of Schistosoma immune responses and their effect on the cardiopulmonary system is limited in both animal and human models, which hinders clinical care and drug development. The inflammatory response to the eggs in the lung appears to contribute to the remodeling of the pulmonary vessels. Portal hypertension caused by parasitemia also appears to contribute to the development of pathophysiologic alterations of the pulmonary vascular bed. Antischistosomal therapy, praziquantel, used for pulmonary hypertension secondary to schistosomiasis usually has no effect, but it is given to prevent further progression of disease. Currently, there are no clinical trials for the treatment of pulmonary vascular disease secondary to schistosomiasis. Specialty drugs such as phosphodiesterase type 5 or tyrosine kinase inhibitors exhibit some interesting activity, yet are prohibitively expensive, lack safety and efficacy studies in schistosomiasis endemic populations, and tend to be limited by safety, efficacy, route of administration and compliance problems.

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Association of oxamniquine praziquantel and clonazepam in experimental Schistosomiasis mansoni

Cited by 15 publications

References 11 publications

Imatinib activity on Schistosoma mansoni

Imatinib activity on Schistosoma mansoni

In vitro evaluation of the schistosomicidal effect of the extracts, fractions and major 3-hydroxy-2,6-dialkyl-substituted piperidine alkaloids from the flowers of Senna spectabilis (Fabaceae)

Pulmonary vascular disease associated with schistosomiasis

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