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1.
Mem. Inst. Oswaldo Cruz ; 112(4): 247-254, Apr. 2017. graf
Artigo em Inglês | LILACS | ID: biblio-841783

RESUMO

BACKGROUND Praziquantel has been cited as the only drug for treating schistosomiasis. However, concerns over drug resistance have encouraged the search for novel drug leads. The antimalarial drug primaquine possesses interesting anti-schistosmal properties. OBJECTIVES This study is the first to document the potential role of primaquine as a schistosomicide and the ultrastructural changes induced by primaquine on juvenile or adult male worms of Schistosoma mansoni. METHODS Ultrastructural alterations in the tegumental surface of 21-day-old juvenile and adult male worms of S. mansoni were demonstrated following primaquine treatment at different concentrations (2, 5, 10, 15, and 20 µg/mL) and incubation periods (1, 3, 6, 24, and 48 h) in vitro, using both scanning and transmission electron microscopy. FINDINGS At low concentrations (2, 5, and 10 µg/mL) both juvenile and adult male worms were alive after 24 h of incubation, whereas contraction, paralysis, and death of all worms were observed after 24 h of drug exposure at 20 µg/mL. The tegument of juvenile and adult male worms treated with primaquine exhibited erosion, peeling, and sloughing. Furthermore, extensive damage of both tegumental and subtegumental layers included embedded spines, and shrinkage of muscles with vacuoles. The in vitro results confirmed that primaquine has dose-dependent effects with 20 µg/mL as the most effective concentration in a short incubation period. MAIN CONCLUSIONS The schistosomicidal activity of primaquine indicates that this drug possesses moderate in vitro activity against juvenile and adult male worms, since it caused high mortality and tegumental alterations. This study confirmed that the antimalarial drug primaquine possesses anti-schistosomal activity. Further investigation is needed to elucidate its mechanism of action.


Assuntos
Animais , Masculino , Praziquantel/farmacologia , Schistosoma mansoni/efeitos dos fármacos , Schistosoma mansoni/ultraestrutura , Anti-Helmínticos/farmacologia , Fatores de Tempo , Microscopia Eletrônica de Varredura , Cricetinae , Relação Dose-Resposta a Droga
2.
Rev. Inst. Med. Trop. Säo Paulo ; 58: e7, 2016. tab, graf
Artigo em Inglês | LILACS | ID: lil-774566

RESUMO

Introduction: Schistosomiasis is a chronic disease caused by trematode flatworms of the genus Schistosoma and its control is dependent on a single drug, praziquantel (PZQ), but concerns over PZQ resistance have renewed interest in evaluating the in vitro susceptibility of recent isolates of Schistosoma mansoni to PZQ in comparison with well-established strains in the laboratory. Material and methods: The in vitro activity of PZQ (6.5-0.003 µg/mL) was evaluated in terms of mortality, reduced motor activity and ultrastructural alterations against S. mansoni. Results: After 3 h of incubation, PZQ, at 6.5 µg/mL, caused 100% mortality of all adult worms in the three types of recent isolates, while PZQ was inactive at concentrations of 0.08-0.003 µg/mL after 3 h of incubation. The results show that the SLM and Sotave isolates basically presented the same pattern of susceptibility, differing only in the concentration of 6.5 µg/mL, where deaths occurred from the range of 1.5 h in Sotave and just in the 3 h range of SLM. Additionally, this article presents ultrastructural evidence of rapid severe PZQ-induced surface membrane damage in S. mansoni after treatment with the drug, such as disintegration, sloughing, and erosion of the surface. Conclusion: According to these results, PZQ is very effective to induce tegument destruction of recent isolates of S. mansoni.


Assuntos
Animais , Feminino , Masculino , Praziquantel/farmacologia , Schistosoma mansoni/efeitos dos fármacos , Schistosoma mansoni/isolamento & purificação , Esquistossomicidas/farmacologia , Resistência a Medicamentos , Larva/efeitos dos fármacos , Larva/ultraestrutura , Testes de Sensibilidade Parasitária , Schistosoma mansoni/ultraestrutura
3.
Mem. Inst. Oswaldo Cruz ; 108(5): 600-604, ago. 2013. tab, graf
Artigo em Inglês | LILACS | ID: lil-680780

RESUMO

Current schistosomiasis control strategies are largely based on chemotherapeutic agents and a limited number of drugs are available today. Praziquantel (PZQ) is the only drug currently used in schistosomiasis control programs. Unfortunately, this drug shows poor efficacy in patients during the earliest infection phases. The effects of PZQ appear to operate on the voltage-operated Ca2+channels, which are located on the external Schistosoma mansoni membrane. Because some Ca2+channels have dihydropyridine drug class (a class that includes nifedipine) sensitivity, an in vitro analysis using a calcium channel antagonist (clinically used for cardiovascular hypertension) was performed to determine the antischistosomal effects of nifedipine on schistosomula and adult worm cultures. Nifedipine demonstrated antischistosomal activity against schistosomula and significantly reduced viability at all of the concentrations used alone or in combination with PZQ. In contrast, PZQ did not show significant efficacy when used alone. Adult worms were also affected by nifedipine after a 24 h incubation and exhibited impaired motility, several lesions on the tegument and intense contractility. These data support the idea of Ca2+channels subunits as drug targets and favour alternative therapeutic schemes when drug resistance has been reported. In this paper, strong arguments encouraging drug research are presented, with a focus on exploring schistosomal Ca2+channels.


Assuntos
Animais , Camundongos , Bloqueadores dos Canais de Cálcio/farmacologia , Nifedipino/farmacologia , Praziquantel/farmacologia , Schistosoma mansoni/efeitos dos fármacos , Esquistossomicidas/farmacologia , Testes de Sensibilidade Parasitária
4.
Salvador; s.n; 2013. 121 p. ilus.
Tese em Português | LILACS | ID: lil-710698

RESUMO

A esquistossomose é um grave problema de saúde pública causado pelo helminto Schistosoma mansoni, sendo uma das endemias parasitárias de maior prevalência no Brasil. Apresenta diversas formas clínicas passíveis de serem reproduzidas em modelos experimentais. A lesão renal da glomerulopatia esquistossomótica está associada ao antígeno parasitário que, em consequência da presença de hipertensão portal e formação da circulação colateral, permitem que complexos imunes sejam depositados em glomérulos renais, desencadeando um processo inflamatório progressivo. O objetivo do trabalho foi avaliar o comportamento das alterações renais em camundongos infectados pelo S. mansoni, antes e após o tratamento com praziquantel, a fim de observar a resposta à presença dos complexos imunes e ao processo inflamatório formado na glomerulopatia. Foram organizados 3 grupos de camundongos BALB/c de ambos os sexos: grupo controle intacto (10 animais), grupo de reinfectados tratados (35 animais) e grupo de reinfectados não tratados (35 animais). A avaliação da estrutura renal foi analisada através da microscopia óptica, observando a histologia glomerular com as colorações de HE, PAS e PIFG, através da imunofluorescência marcando IgG e antígeno de Nash, e da microscopia eletrônica de transmissão com emprego da morfometria para avaliar áreas de depósito de complexos imunes. Foram analisadas, também, a carga parasitária, o peso do fígado, a presença dos vermes nas veias mesentéricas e a estrutura física dos órgãos. Os resultados demonstraram significativa redução da carga parasitária, do peso do fígado, das alterações estruturais nas observações histológicas e dos depósitos de complexos imunes em área e marcação no tecido renal, após tratamento com praziquantel. O tratamento específico reverteu os processos iniciais de agressão renal na glomerulopatia do modelo experimental, embora em alguns poucos camundongos, após a quimioterapia, a doença se manteve. Os achados deste trabalho reforçam a possibilidade de que o estado normal de estrutura renal pode ser restabelecido com o tratamento antiparasitário, desde que ministrado logo que se instala a glomerulopatia esquistossomótica clínica.


Schistosomiasis is an important public health problem due to infection with the helminth Schistosoma mansoni, which is also one the parasitic diseases listed as highly prevalent in Brazil. It presents several clinical forms, which are susceptible of experimental reproduction in mice. The lesion involving the kidney – Schistosomal glomerulopathy – is related to the presence of circulating parasite antigens, which can be attached to circulating antibodies to form antigen-antibody complexes with glomerular deposition. However, in the presence of portal hypertension and collateral circulation, these antigen complexes, can bypass macrophage clearance and reach the systemic circulation, thus coming to be deposited within the renal glomeruli, starting a progressive inflammatory process. The aim of this research was to evaluate renal changes in mice infected with S. mansoni, before and after treatment with praziquantel, through the presence of immune complexes in the glomeruli, and its correlation with the glomerular changes shown. BALB/c mice infected, infected and treated mice and non-infected groups were evaluated. Besides the evaluation of the renal changes by optical microscopy (HE, PAS, PIFG), immunofluorescence (IgG and Nash antigen) and transmission electron microscopy, a morphometric study of the areas containing immune complexes was also attempted. Besides parasite burden, liver weigh, number of worm pairs within mesenteric veins, and organs physical structure, were also evaluated.


Assuntos
Animais , Camundongos , Antígenos/imunologia , Antígenos , Esquistossomose/complicações , Esquistossomose/diagnóstico , Esquistossomose/imunologia , Praziquantel/farmacologia , Esquistossomose/parasitologia
5.
Braz. j. pharm. sci ; 46(3): 473-481, July-Sept. 2010. ilus, tab
Artigo em Inglês | LILACS | ID: lil-564913

RESUMO

The solubility behavior of drugs remains one of the most challenging aspects in formulation development. Solid Dispersion (SD) has tremendous potential for improving drug solubility. Although praziquantel (PZQ) is the first drug of choice in the treatment of schistosomiasis, its poor solubility has restricted its delivery oral route. In spite of its poor solubility, PZQ is well absorbed in the gastrointestinal tract, but large doses are required to achieve adequate concentration at the target sites. The aim of this study was to improve the solubility and dissolution rate of PZQ and to evaluate its intestinal absorption. SDs were formulated with PEG-60 castor oil hydrogenated (CR-60) using a fusion and evaporation method. Pure PZQ and physical mixtures (PM) and PZQ-CR-60 (2:1; 1:1; 1:2 ratios) were compared as regards their solubility, dissolution and intestinal absorption. The experimental results demonstrated the improvement in the solubility, dissolution rate and intestinal absorption. In addition, the solubility behavior showed pH dependency and that the solubility of PZQ was slower in acidic medium than in neutral and basic mediums. The increase in PZQ solubility of the SD with the CR-60 could be attributed to several factors such as improved wettability, local solubilization, drug particle size reduction and crystalline or, interstitial solid solution reduction.


A solubilidade de fármacos ainda é um dos principais desafios no desenvolvimento de formulações farmacêuticas. As dispersões sólidas (DS) apresentam grande potencial para melhorar a solubilidade de fármacos. O praziquantel é o fármaco de primeira escolha no tratamento da esquistossomose, contudo a baixa solubilidade em água restringe seu uso à administração pela via oral. Apesar da baixa solubilidade, o PZQ é bem absorvido através do trato gastrintestinal, mas doses orais elevadas são requeridas para garantir concentrações suficientes de fármaco para o tecido alvo. O objetivo deste estudo foi melhorar a solubilidade, a dissolução e avaliar a absorção do PZQ. As DS foram formuladas com óleo de castor hidrogenado - PEG 60 (CR-60), pelo uso dos métodos de fusão e evaporação do solvente. PZQ puro, mistura física (MF) e DS de CR-60-PZQ (1:2; 1:1; 2:1) foram comparados quanto à solubilidade, dissolução e absorção intestinal. Os resultados experimentais mostraram aumento na solubilidade, na taxa de dissolução e na absorção intestinal do PZQ nas DS. A solubilidade do PZQ foi maior em meio ácido, mostrando uma dependência do pH. O aumento na solubilidade do PZQ nas DS com CR-60 foi atribuída a fatores como aumento da molhabilidade, solubilização local, redução granulométrica e redução da cristalinidade ou, ainda, a ocorrência de uma solução sólida intersticial.


Assuntos
Fenômenos Químicos/estatística & dados numéricos , Dissolução/métodos , Emulsificantes , Óleo de Rícino/análise , Praziquantel/farmacologia , Hidrogenação , Interpretação Estatística de Dados
6.
Rev. bras. parasitol. vet ; 18(1): 53-59, Mar. 2009. graf, tab
Artigo em Português | LILACS | ID: lil-606766

RESUMO

Neste trabalho, avaliou-se a eficácia antiparasitária do praziquantel, levamisol e diflubenzuron administrados via oral, adicionados à ração, para pacus (Piaractus mesopotamicus) infectados por Anacanthorus penilabiatus e Dolops carvalhoi. Foram utilizadas 19 caixas d'água de 300 L de capacidade, comportando 28 peixes cada. Os tratamentos foram feitos misturando os princípios ativos nas dietas. A intensidade parasitária e eficácia foram avaliadas 1 dia antes e 3, 7 e 15 dias após o início da alimentação com ração contendo diflubenzuron, levamisol e praziquantel isolados ou associados em diferentes concentrações por 7 dias. Os resultados da eficácia terapêutica sugerem que, isoladamente ou associado com levamisol e praziquantel, o diflubenzuron é eficiente contra o crustáceo D. carvalhoi, demonstrando que a eficácia dos tratamentos nos dias 3, 7 e 15 variou de 96,2 a 100 por cento. Contra os monogenóides, as drogas não apresentaram eficácia satisfatória. Os resultados sugerem o uso do diflubenzuron para o controle de D. cavalhoi em peixes de cativeiro e em condições de quarentenário.


This assay evaluated the control efficacy of diflubenzuron, praziquantel and levamisole added to the diet of pacu (Piaractus mesoptamicus) infected with Anacanthorus penilabiatus and Dolops carvalhoi. 19 water tanks of 300 L capacity were utilized with 28 fish in each one. The treatments were made by mixing the active principles in the diet. The experiment was evaluated in four harvests done 1 day before and 3, 7 and 15 days after the treatment. The medicated feeding was applied for 7 days. The results of efficacy suggest that the diflubenzuron alone or associated with levamisole and praziquantel was efficient against the crustacean D. carvalhoi and the efficacy in the 3, 7 and 15 days evaluations ranged from 96,2 to 100 percent. Against the monogenean the drugs did not present efficacy. The results suggest the use of diflubenzuron for the control of D. carvalhoi in captive fishes in special conditions.


Assuntos
Animais , Anti-Helmínticos/farmacologia , Antinematódeos/farmacologia , Arguloida/efeitos dos fármacos , Controle de Doenças Transmissíveis , Diflubenzuron/farmacologia , Peixes/parasitologia , Helmintos/efeitos dos fármacos , Levamisol/farmacologia , Praziquantel/farmacologia
7.
Mem. Inst. Oswaldo Cruz ; 103(8): 781-785, Dec. 2008. ilus, tab
Artigo em Inglês | LILACS | ID: lil-502298

RESUMO

The antischistosomal activity of clonazepam, when administered alone or in association with oxamniquine and praziquantel, was experimentally evaluated in mice infected with Schistosoma mansoni. The animals were treated 45 days post-infection with a single dose, by oral route, according to three treatment schedules: clonazepam 25 mg/kg and sacrificed 15 min, 1h or 4 h after treatment; clonazepam 1.0, 2.5 or 10.0 mg/kg and sacrificed 15 days post-treatment or with the dose of 10 mg/kg in association with oxamniquine 50 mg/kg or praziquantel 200 mg/kg, single dose, orally, every schedule with a control group. The efficacy of the drugs in vivo was assessed by means of worm counts and their distribution in mesentery and liver, mortality and oogram changes. In the chemotherapeutic schedules used, clonazepam did not present antischistosomal activity and the result of the association of this drug with oxamniquine or praziquantel was not significantly different from the one obtained when these two last drugs were administered alone. In the in vitro experiments, the worms exposed to 0.6 mg/mL clonazepam remained motionless throughout the 8-day-period of observation, without egg-laying, whereas the worms of the control group showed normal movements, egg-laying and hatching of miracidia on the last day of observation. The results obtained in the present study confirm the action of clonazepam on S. mansoni adult worm, in vitro, causing total paralysis of males and females. However, no additive or synergistic effects were observed when clonazepam were used in association with oxamniquine or praziquantel.


Assuntos
Animais , Feminino , Masculino , Camundongos , Clonazepam/farmacologia , Schistosoma mansoni/efeitos dos fármacos , Esquistossomose mansoni/tratamento farmacológico , Esquistossomicidas/farmacologia , Clonazepam/administração & dosagem , Avaliação Pré-Clínica de Medicamentos , Quimioterapia Combinada , Fígado/parasitologia , Mesentério/parasitologia , Oxamniquine/administração & dosagem , Oxamniquine/farmacologia , Praziquantel/administração & dosagem , Praziquantel/farmacologia , Esquistossomicidas/administração & dosagem , Fatores de Tempo
8.
Indian J Exp Biol ; 2007 Sep; 45(9): 791-801
Artigo em Inglês | IMSEAR | ID: sea-55865

RESUMO

With a view to clarify the induction of the "Crabtree consequence" in liver cells of S. mansoni infected mice, the curative effect of oil extract of C. longa was tested and compared to praziquantel (PZQ) the effective drug against all schistosome species occurring in man. Protein, glucose, glucose-6-phopsphatase, AMP-deaminase, adensoine deaminase, urea concentration, pyravate kinase (PK), phosphoenol pyruvate carboxykinase (PEPCK) and PK/PEPCK ratio were estimated. In addition, worm burden and ova count in mice infected with S. mansoni were elucidated. The result showed that C. longa normalized the concentration of protein, glucose, AMP-deaminase and adenosine deaminase, which were changed by infection. Moreover, it lowered pyruvate kinase level, while PZQ-treatment induced more elevation of this enzyme. PZQ was more effective in lowering worm burden while C. longa extract was more potent in reducing egg count.


Assuntos
Animais , Curcuma/química , Humanos , Fígado/efeitos dos fármacos , Masculino , Camundongos , Contagem de Ovos de Parasitas , Fitoterapia , Extratos Vegetais/farmacologia , Praziquantel/farmacologia , Schistosoma mansoni/efeitos dos fármacos , Esquistossomose mansoni/tratamento farmacológico , Esquistossomicidas/farmacologia
9.
Rev. ciênc. farm. básica apl ; 28(2): 209-214, 2007. tab
Artigo em Português | LILACS | ID: lil-486512

RESUMO

A esquistossomose mansônica é causada pelo trematódeo digenético intravascular Schistosoma mansoni. Para o tratamento dessa enfermidade o praziquantel (PZQ) e a oxamniquina (OXA) são os fármacos escolhidos. Noentanto, esses fármacos apresentam limitações quanto à ação e casos de resistência ou tolerância já foram relatados. Por esse motivo, são necessários os estudos de novas alternativas que visam melhorar os fármacos já existentes, como a incorporação desses em lipossomas. Este estudo verificou a ação do praziquantel incorporado a lipossomas (lip.PZQ) sobre os ovos de S. mansoni, linhagem BH em camundongos Mus musculus (Swiss-SPF). Para tanto, foram testadas quatro doses de PZQ elip.PZQ (47; 60; 250 e 300mg/kg) sendo que parte dos camundongos foi tratada após 30 dias de infecção e outra após 45 dias. A análise do o ograma mostrou que a dose lip.PZQ 300mg/kg administrada no 45º dia de infecção foi mais eficaz, pois reduziu a oviposição pelas fêmeas de S. mansoni.


Assuntos
Animais , Camundongos , Anti-Helmínticos/uso terapêutico , Antígenos de Helmintos/farmacologia , Praziquantel/farmacologia , Schistosoma mansoni , Lipossomos
10.
Mem. Inst. Oswaldo Cruz ; 101(supl.1): 283-287, Oct. 2006. ilus
Artigo em Inglês | LILACS | ID: lil-441260

RESUMO

Praziquantel (PZQ) is effective against all the evolutive phases of Schistosoma mansoni. Infected Biomphalaria glabrata snails have their cercarial shedding interrupted when exposed to PZQ. Using primary in vitro transformed sporocysts, labeled with the probe Hoechst 33258 (indicator of membrane integrity), and lectin of Glycine max (specific for carbohydrate of N-acetylgalactosamine membrane), we evaluated the presence of lysosomes at this evolutive phase of S. mansoni, as well as the influence of PZQ on these acidic organelles and on the tegument of the sporocyst. Although the sporocyst remained alive, it was observed that there was a marked contraction of its musculature, and there occurred a change in the parasite's structure. Also, the acidic vesicles found in the sporocysts showed a larger delimited area after contact of the parasites with PZQ. Damages to the tegument was also observed, as show a well-marked labeling either with Hoechst 33258 or with lectin of Glycine max after contact of sporocysts with the drug. These results could partially explain the interruption/reduction mechanism of cercarial shedding in snails exposed to PZQ.


Assuntos
Animais , Camundongos , Anti-Helmínticos/farmacologia , Lisossomos/efeitos dos fármacos , Oocistos/efeitos dos fármacos , Praziquantel/farmacologia , Schistosoma/efeitos dos fármacos , Schistosoma/citologia , Schistosoma/crescimento & desenvolvimento
11.
Mem. Inst. Oswaldo Cruz ; 101(supl.1): 293-298, Oct. 2006. ilus
Artigo em Inglês | LILACS | ID: lil-441262

RESUMO

We have been able to label the excretory system of cercariae and all forms of schistosomula, immature and adult worms with the highly fluorescent dye resorufin. We have shown that the accumulation of the resorufin into the excretory tubules and collecting ducts of the male adult worm depends on the presence of extracellular calcium and phosphate ions. In the adult male worms, praziquantel (PZQ) prevents this accumulation in RPMI medium and disperses resorufin from tubules which have been prelabelled. Female worms and all other developmental stages are much less affected either by the presence of calcium and phosphate ions, or the disruption caused by PZQ. The male can inhibit the excretory system in paired female. Fluorescent PZQ localises in the posterior gut (intestine) region of the male adult worm, but not in the excretory system, except for the anionic carboxy fluorescein derivative of PZQ, which may be excreted by this route. All stages of the parasite can recover from damage by PZQ treatment in vitro. The excretory system is highly sensitive to damage to the surface membrane and may be involved in vesicle movement and damage repair processes. In vivo the adult parasite does not recover from PZQ treatment, but what is inhibiting recovery is unknown, but likely to be related to immune effector molecules.


Assuntos
Animais , Feminino , Masculino , Anti-Helmínticos/farmacologia , Polilisina/farmacologia , Praziquantel/farmacologia , Schistosoma mansoni/efeitos dos fármacos , Corantes Fluorescentes , Oxazinas , Schistosoma mansoni/fisiologia
12.
Journal of the Egyptian Society of Parasitology. 2006; 36 (1): 197-220
em Inglês | IMEMR | ID: emr-78289

RESUMO

The effect of cyclooxygenase-2 [COX-2] inhibitor, such [as meloxicam, and pyocyanin pigment of Pseudomonas aeruginosa] with and without praziquantel [PZQ] on worms, ova count, bone marrow and blood cells in 7 groups of Schistosoma mansoni infected mice was studied. The results revealed significant decrease of worm burden and ova count in all treated groups as compared to the infected untreated group, while those with combined treatment of PZQ and meloxicam or pyocyanin showed complete eradication of the worm with the highest reduction in the tissue egg load. EM showed extensive swelling and vesiculation of the tegument, completely implanted spines that overlie degenerated muscle layer were obvious in groups treated with either meloxicam or pyocyanin. Hematological study revealed significant increase [P < 0.05] of total leucocytic count of PZQ treated group while that treated with either meloxicam or pyocyanin showed significant decrease [P < 0.05], but in combination of PZQ with meloxicam or pyocyanin no significant difference as compared to the infected untreated group. The neutrophil was the main cell affected in groups treated with neither meloxicam nor pyocyanin alone with significant decrease [P < 0.05], but with significant increase [P < 0.05] in combination with PZQ as compared to the infected untreated group. Those treated with PZQ plus meloxicam showed significant increase as compared to that plus pyocyanin. Eosinophil count showed significant decrease [P < 0.05] in all treated groups as compared to the infected untreated group. Inverse correlation between serum level of sFas and peripheral neutrophil count was detected. Ultrastructural study of the bone marrow explained the results as groups treated with meloxicam revealed dissociation between nuclear and cytoplasmic development in the neutophils with cytoplasm maintaining primitive appearance despite maturation of the nucleus that is manifested by the persistent production of immature granules and the still orientation of Golgi cternae and the centriole around the nucleus. Groups treated with pyocyanin pigment revealed many abnormalities in neutophils as hypogranularity or early apoptotic morphology changes as intense pen- nuclear chromatin aggregation or nucleus fragmentation.In peripheral blood apoptotic morphology changes was detected in both groups treated with meloxicam or pyocyanin while most of cells of mice treated with PZQ were in an active state. Consequently, it is preferable to give meloxicam with PZQ for a short period of time [less side-effect] to eradicate S. mansoni worm completely but with continuous observation of the peripheral neutrophil count and function


Assuntos
Animais de Laboratório , Inibidores de Ciclo-Oxigenase , Pseudomonas aeruginosa/efeitos dos fármacos , Praziquantel/farmacologia , Doenças Parasitárias em Animais , Camundongos , Combinação de Medicamentos , Microscopia Eletrônica , Contagem de Leucócitos , Receptor fas
13.
Egyptian Journal of Schistosomiasis and Infectious and Endemic Diseases. 2005; 27: 25-37
em Inglês | IMEMR | ID: emr-70364

RESUMO

Mirazid [myrrh] is a new herbal extract [oleo gum resin from the stem of the plant Commiphora molmol with claimed antibilharzial activity. LD16, LD50, and LD84 of Mirazid were determined in albino mice and were found to be 1984, 3138, and 4963 mg/kg respectively. The antibilharzial efficacy of Mirazid, administered orally at a dose of 250X5 mg/kg, in comparison to the schistosomicidal drug of choice praziquantel [PZQ], administered orally at a dose of 250X2 mg/kg, was evaluated in S. haematobium infected hamsters. Treatment was conducted 90 days post infection. Parasitological parameters expressing cure and hepatic histopathological changes were evaluated 4 weeks after treatment. Praziquantel treatment completely eradicated S.haematobium worms, caused disappearance of immature and mature egg stages, with 100% dead eggs. Hepatic and intestinal tissue egg loads were reduced by 79.2% and 99.7% respectively. Mirazid failed to induce any significant change in total number of worms, but induced significant reduction in the 1[st], 2[nd], and 3[rd] immature egg stages with increase in the number of the fourth stage, but this change was not reflected on the total number of immature eggs. Mirazid did not affect tissue egg load. The hepatic histopathological changes induced by S. haematobium infection were improved in praziquantel treated hamsters with reduction in granuloma number and size. Ova degeneration with regression of granulomatous inflammatory reaction was more manifested when compared to infected untreated controls. Mirazid did not results in evident regression of hepatic schistosomal pathology. In conclusion, praziquantel is still the drug of choice for treatment of S. haematobium, while Mrazid cannot substitute PZQ in the treatment of S. haematobium. Further trials using modified preparations may result in better antibilharzial efficacy of this novel herbal extract preparation


Assuntos
Animais de Laboratório , Praziquantel/farmacologia , Commiphora , Mesocricetus , Fígado/patologia , Extratos Vegetais , Histologia , Schistosoma haematobium/efeitos dos fármacos
14.
Journal of the Egyptian Society of Parasitology. 2005; 35 (3): 1037-1050
em Inglês | IMEMR | ID: emr-72390

RESUMO

Mirazid [MZ], an oleo-resin extract derived from Myrrh was reported in several experimental and clinical trails to be safe and effective against other trematodes like schistosomiasis and fascioliasis. This experimental work aimed at investigating the possible efficacy of MZ against heterophyids [Pygidiopsis genata], using praziquantel as a therapeutic control. Results showed that MZ in emulsion form is a promising drug for the treatment of heterophyidiasis, as proved by significant reduction of worm count, overt surface tegumental changes like deformity and erosion of tegumental spines observed by scanning electron microscope [SEM]. The effective dose regimen was 500 mg/kg/d for 3 successive days, produced 100% reduction in worm load. The proved efficacy of the drug, together with reported low toxicity, relative to praziquantel, favours its use as a natural new alternative therapy for the treatment of human heterophyidiasis


Assuntos
Animais de Laboratório , Commiphora/efeitos dos fármacos , Praziquantel/farmacologia , Microscopia Eletrônica de Varredura , Peixes , Ciclídeos
15.
Southeast Asian J Trop Med Public Health ; 2003 Jun; 34(2): 274-80
Artigo em Inglês | IMSEAR | ID: sea-34524

RESUMO

To determine the genetic basis of the resistance of Schistosoma mansoni to praziquantel (PZQ) and to understand whether the resistance is dominant or recessive trait, a schistosome cross was undertaken between a PZQ-susceptible and a PZQ-resistant isolate using infections of the single-sex cercariae which were identified by a direct W1-specific PCR technique. The resistances of F1 and F2 generation to PZQ were evaluated using in vitro egg, miracidial and cercarial tests. The F1 hybrid progeny from crosses between the susceptible and resistant isolates were resistant to PZQ. The resistant phenotype reappeared in the F2 progeny. It can thus be considered that the PZQ resistance behaves like a dominant trait.


Assuntos
Animais , Resistência a Medicamentos/genética , Feminino , Masculino , Camundongos , Praziquantel/farmacologia , Schistosoma mansoni/efeitos dos fármacos , Esquistossomicidas/farmacologia , Caramujos/parasitologia
16.
Journal of the Egyptian Society of Parasitology. 2003; 33 (2): 391-6
em Inglês | IMEMR | ID: emr-62852

RESUMO

The effect of eight chemicals; vinegar, Allium sativum [crude garlic], Acacia auriculiformis, lemon juice, praziquantel, pumpkin, perosan and yomesan on the viability of cysticerci of Taenia saginata in vitro was investigated. The minimum exposure times required for cysticerci to be non-evaginable for the eight chemicals were 5, 10, 25, 40, 55, 75, 90 and 105 minutes, respectively. The best one was vinegar and the least effective was yomesan


Assuntos
Animais de Laboratório , Cysticercus/efeitos dos fármacos , Acetatos , Praziquantel/farmacologia
17.
Journal of the Egyptian Society of Parasitology. 2002; 32 (1): 201-18
em Inglês | IMEMR | ID: emr-59717

RESUMO

Four-five weeks old rats were included in this study and divided into two experimental groups received single or split doses of praziquantel [PZQ] as well as two control groups, one infected untreated and the other normal healthy rats. The effect of infection on rat growth as well as the jejunal and duodenal architecture was histopathologically studied after H and E staining. The jejunal ultrastructure was examined by SEM and TEM. The effect of PZQ was evaluated using the same techniques. It was observed that infected as well as infected treated animals had less weight than the healthy controls. The intensity of infection decreased gradually after treatment. The cure rate was 100% after split dose and 80% after a single dose. Altered villus height and cryptic depth were the characteristic changes in the architecture of the duodenum and jejunum, more pronounced in the latter. The split dose of PZQ revealed a more improvement of the histopathological findings than the single dose. By SEM, circular imprints representing defects in the villi were observed in the jejunum. By TEM deformation of microvillar architecture was observed together with organellar changes in the RER and the mitochondria after PZQ treatment


Assuntos
Animais de Laboratório , Praziquantel/farmacologia , Jejuno/patologia , Duodeno/patologia , Microscopia Eletrônica , Resultado do Tratamento , Ratos , Animais de Laboratório , Giardíase/tratamento farmacológico
18.
Journal of the Egyptian Society of Parasitology. 2002; 32 (1): 219-28
em Inglês | IMEMR | ID: emr-59718

RESUMO

V. Nana was frequently associated with Schistosoma mansoni and Fasciola spp. This study was conducted to investigate and compare the effects of praziquantel and triclabendazole on V. nana worms after in vitro exposure to 1 and 2 mug/ml of each of praziquantel or triclabendazole. All the worms were put under observation for 30 minutes. The worm mortality rates were recorded and the topographic tegumental changes were studied by scanning electron microscopy. The results demonstrated that praziquantel showed comparatively superior effect on adult V. nana worms than triclabendazole. The latter still revealed an anthelmintic effect


Assuntos
Animais de Laboratório , Praziquantel/farmacologia , Helmintos , Mebendazol/farmacologia , Microscopia Eletrônica , Resultado do Tratamento , Camundongos , Animais de Laboratório
19.
Rev. méd. Chile ; 127(1): 75-7, ene. 1999.
Artigo em Espanhol | LILACS | ID: lil-243762

RESUMO

We report a 26 years old asymptomatic female that expelled spontaneously a 39 proglottid strobila. The taxonomic study of proglottids and eggs found in the stool examination concluded that the patient was infected by Diphyllobothrium pacificum. This infection was probably acquired by the ingestion of raw fish (Sciaena deliciosa) with lemon in a traditional plate called "cebiche". She was treated with a single dose of praziquantel in a dose of 10 mg/kg body weight. After 24 h of treatment there were no scolices on feces. The patient did not have anemia. All eight family members studied, did no have the infection. A follow up stool examination three months later remained negative


Assuntos
Humanos , Feminino , Adulto , Difilobotríase/etiologia , Diphyllobothrium/patogenicidade , Praziquantel/farmacologia , Costa , Difilobotríase/diagnóstico , Difilobotríase/dietoterapia , Difilobotríase/tratamento farmacológico , Diphyllobothrium/isolamento & purificação , Diphyllobothrium/efeitos dos fármacos , Doenças Transmitidas por Alimentos/parasitologia , Contagem de Ovos de Parasitas
20.
Southeast Asian J Trop Med Public Health ; 1998 Jun; 29(2): 246-9
Artigo em Inglês | IMSEAR | ID: sea-31180

RESUMO

The study was carried out from September to November 1997 in Phrae Province of northern Thailand. A total of 95 adult patients with Opisthorchis-like ova in their stools were randomly treated with two different manufactured Praziquantels. Group 1, consisting of 49 patients, received a single dose of 40 mg per kg Praziquantel manufactured by the Thai Government Pharmaceutical Organization. Group 2 (46 patients) received Biltricide at the same dosage. Haplorchis taichui, H. yokogawai, Echinostome spp., O. viverrini, Taenia saginata and Enterobius vermicularis were expelled in the stools after treatment. Minute intestinal flukes were detected in 64% of patients. O. viverrini was found in lower proportion of 17%. By formalin-ether concentration examination one stool specimen from each patient, the cure rate in both groups on the 30th day of treatment was 100%. The side effects of the two different Praziquantel treatments were mild with no significant difference. Praziquantel, regardless of its manufacture, proved effective against O. viverrini and other minute intestinal flukes (H. taichui, H. yokogawai and Echinostome spp).


Assuntos
Adolescente , Adulto , Idoso , Animais , Antiplatelmínticos/farmacologia , Feminino , Humanos , Enteropatias Parasitárias/tratamento farmacológico , Masculino , Pessoa de Meia-Idade , Opistorquíase/tratamento farmacológico , Opisthorchis/isolamento & purificação , Praziquantel/farmacologia , Resultado do Tratamento
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