Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Diminazene”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 163 records · Page 9Linked to original sources
PubMed2002

Residual effect of antibabesial drugs on the live redwater blood vaccines.

It has been demonstrated that the attenuated organisms used in the unfrozen South African Babesia bovis and B. bigemina (redwater) vaccines are susceptible for longer periods to the residual effect of the anti-babesial drugs diminazene and imidocarb dipropionate than the virulent field strains. Reports of vaccine failures in some animals vaccinated with the frozen South African redwater vaccines after prophylactic treatment with imidocarb dipropionate have led us to reinvestigate the validity of the recommended prescribed waiting periods. Results indicated that waiting periods before administration of the frozen B. bovis and B. bigemina vaccines in animals that have been treated with diminazene at 3.5 mg/kg live weight, compare favorably with results initially obtained for the unfrozen vaccines at 4 and 8 weeks, respectively. However, the inhibitory effect of imidocarb dipropionate at 3.0 mg/kg live weight on the infectivity of both frozen B. bovis and B. bigemina vaccines is longer than previously anticipated and necessitated changing the minimum waiting periods before administration of these vaccines from 8 to 12 weeks and 16 to 24 weeks, respectively.

Animals↗
PubMed2001

Effect of clindamycin therapy on phagocytic and oxidative activity profiles of spleen mononuclear cells in Babesia rodhaini-infected mice.

Spleen weight, the number of spleen mononuclear cells, and their phagocytic activity in groups of Babesia rodhaini-infected mice treated with diminazene diaceturate and clindamycin increased significantly in the early stage of treatment, and then decreased in the final stage of treatment to approximately the pre-infection level. The number of F4/80-positive macrophages and their oxidative activity per mean whole-spleen weight also increased significantly during the course of treatment in comparison with the untreated group. The increases in the clindamycin-treated group were more prominent than those in the group treated with diminazene diaceturate, suggesting the effectiveness of clindamycin therapy for murine babesiosis.

Animals↗
PubMed2004

Transition models to assess risk factors for new and persistent trypanosome infections in cattle-analysis of longitudinal data from the Ghibe Valley, southwest Ethiopia.

The objective of this study was to apply transition models to distinguish between factors associated with both incident and persistent trypanosome infections. Data collected from 1561 cattle were analyzed from a long-term study involving 8 herds in which both trypanosome infections (a total of 56,931 cattle sampling-months) and tsetse (Glossina spp.) challenge were monitored monthly from March 1986 to March 1998. Both pour-on and insecticide-target tsetse control programs and mass treatment with diminazene aceturate before tsetse control were associated with significant decreases in both incidence and persistence of trypanosome infection relative to noncontrol periods, as were seasonal and sex effects. The magnitudes of the effects were, however, often different for new and persistent infections. For persistence of infection, there were 2 trends. In general, the duration of infection increased during the study, despite the regular treatment with diminazene aceturate. The transition model had 2 major benefits. The first was to identify an increasing duration of infections with time, taking into account other factors associated with increasing infection risk. The second was to highlight different patterns in the effects of certain factors on new and persistent trypanosome infections.

Age Factors↗
PubMed2004

Knowledge and attitudes of cattle owners regarding trypanosomosis control in tsetse-infested areas of Uganda.

A pilot survey using a structured questionnaire was conducted in Tororo and Busia districts of Uganda on the knowledge and attitudes of cattle owners regarding tsetse fly and trypanosomosis control, in order to understand factors that hindered their full participation. A total of 81 cattle owners was randomly selected and interviewed, of which 92.5% were aware of tsetse flies and trypanosomosis and 87.6% recognised animal trypanosomosis as a problem in the area. Most cattle owners were aware of tsetse fly trapping (76.5%), isometamidium chloride use (55.5%), diminazene aceturate use (48%) and pour-on applications (18.5%). However, knowledge did not coincide with the application of control measures. Despite the widespread awareness, tsetse fly trapping and pour-on applications were used by only a small percentage of cattle owners (7.5% applied tsetse fly trapping while 76.5% were aware of it; 1.2% applied pour-on insecticides while 18.5% were aware of them). Differences between awareness and application were highly significant for tsetse fly trapping (chi2 = 67.8, d.f. = 1, P < 0.001) and pour-on applications (chi2 = 10.8, d.f. = 1, P < 0.05), but not for isometamidium chloride use (chi2 = 0.08, d.f. = 1, P = 0.77) and diminazene aceturate use (chi2 = 0.00, d.f. = 1, P = 1.00). Most cattle owners (97.5%) were willing to participate in future control programmes, but preferred participating on a group basis (85.2%) rather than individually (14.8%). The 4 most favoured control options in order of importance were: fly traps supplied by the government and maintained by cattle owners; contribution of labour by cattle owners for trap deployment; self-financing of trypanocidal drugs and self-financing of pour-on insecticide. The control options that should be selected in order to elicit full participation by cattle owners are discussed.

Animal Husbandry↗
PubMed1988

The relapse of Trypanosoma brucei brucei infections after chemotherapy in rabbits.

Infections of T. brucei in the rabbit were found to relapse after chemotherapy. The results indicated that 25 mg/kg diminazene aceturate given 3 days after infection resulted in a complete cure but if given 7 days after infection relapses frequently occurred. However, treatment was apparently successful if delayed until 14 or 21 days. Six of the rabbits originally treated with diminazene aceturate on day 7 were treated with suramin 21 days later; in 3 rabbits the infections relapsed. In all rabbits in which drug treatment was not curative, the clinical condition nevertheless improved. An attempt to locate a cryptic focus of infection in rabbits was unsuccessful.

Amidines↗
PubMed1987

The sensitivity to trypanocidal drugs of Trypanosoma vivax isolated in Kenya and Somalia.

The drug sensitivity of seven Trypanosoma vivax-isolates from Kenya and Somalia was examined. With the exception of diminazene aceturate all commercially available trypanocidal drugs failed to effect a cure. The results suggest the existence of multiple drug resistance of T. vivax-strains, geographically widely distributed along the East African Coast. The isolates were resistant to the recommended dose rates of isometamidium, homidium and quinapyramine. Isometamidium showed no prophylactic properties when tested against one of the isolates. All were sensitive to diminazene aceturate.

Animals↗
PubMed1996

Inhibition of the protease activity in tracheobronchial aspirates of horses with chronic obstructive pulmonary disease.

OBJECTIVES: To clarify the role of proteolytic enzymes in the pathogenesis of chronic obstructive pulmonary disease (COPD) in horses, and to investigate new possibilities for treatment of this disease by interfering in the proteolytic process. DESIGN: Effect of antiproteolytic activity of selected protease inhibitors on tracheal aspirates was studied in vitro, and the inhibition profiles were compared with those of purified proteases. SAMPLE POPULATION: Respiratory tract secretions with antiproteolytic activity from 9 horses with COPD. PROCEDURE: Caseinolytic agar-diffusion assay. RESULTS: The protease-inhibition profile of tracheal aspirates differed from horse to horse. The profiles did not resemble that of any of the pure proteases. Acetylcysteine, pentamidine, and diminazene were most effective in inhibiting proteolytic activity in tracheal aspirates in vitro. CONCLUSIONS: A mixed type of proteolytic activity is present in the respiratory tract secretions of horses with COPD. CLINICAL RELEVANCE: Acetylcysteine, pentamidine, and diminazene seem to have potential to be used in vivo to protect the lungs of horses with COPD from proteolytic damage.

Acetylcysteine↗
PubMed1997

The role of the polyamine inhibitor eflornithine in the neuropathogenesis of experimental murine African trypanosomiasis.

The treatment of late-stage human African trypanosomiasis is complicated by a post-treatment reactive encephalopathy, also referred to as a 'reactive arsenical encephalopathy', that may be fatal. This study used a well established experimental mouse system to assess the use of the trypanostatic drug, eflornithine, in the management of this post-treatment reaction. Female CD-1 mice infected with an eflornithine-resistant trypanosome stabilate and treated with the trypanocidal compound diminazene aceturate on or after day 21 post-infection develop a reactive encephalopathy and relapsing parasitaemia. If these animals are re-treated with diminazene aceturate, a severe encephalopathy develops histologically comparable with that of human cases and characterized by a severe meningoencephalitis and astrogliosis. Histopathological and immunocytochemical examination shows that administration of eflornithine before or after the development of this reactive encephalopathy prevented or ameliorated the inflammatory reaction. Since an eflornithine resistant stabilate was used, this effect appears to be independent of the drug's trypanostatic action and illustrates an important, previously unrecognized, pharmacological property of eflornithine. Consideration can now be given to the use of eflornithine for the management of human trypanosomiasis cases, even where trypanosome resistance to eflornithine exists.

Animals↗
PubMed1992

Correlation of autoantibody titres with central nervous system pathology in experimental African trypanosomiasis.

CD-1 mice infected with the protozoan parasite Trypanosoma brucei brucei developed few signs of central nervous system pathology associated with the invasion of the central nervous system by these parasites and did not survive beyond 5-6 weeks with deaths common before this time point. However, use of the trypanocidal drug diminazene aceturate (40 mg/kg), which fails to cross the blood-brain barrier, on day 21 post-infection led to the development of central nervous system pathology similar to that seen in the fatal post-treatment reactive encephalopathies that can occur in human African trypanosomiasis. Enzyme-linked immunosorbent assays were used to measure autoantibody titres to double-stranded DNA, myelin basic protein and to the myelin-specific galactocerebrosides and gangliosides in groups of infected mice, with or without the post-treatment reaction, on day 30 post-infection and compared with uninfected controls. Infection with T. brucei brucei raised the titres of all of these autoantibodies. Treatment of infected mice with diminazene aceturate resulted in elevated levels of all of these autoantibodies compared to the untreated animals. There was a strong positive correlation between the central nervous system pathology and the levels of autoantibodies to myelin basic protein, galactocerebrosides and gangliosides, but not to double-stranded DNA. The elevated titres observed may be a consequence of the polyclonal B cell activation that is believed to occur in African trypanosomiasis, parasite epitopes that are cross-reactive with these central nervous system (CNS)-specific antigens or result from the CNS damage associated with sub-curative chemotherapy.

Animals↗
PubMed2005

Identification of anti-babesial activity for four ethnoveterinary plants in vitro.

A commonly available Babesia caballi culture system was utilized for anti-babesial screening of four commonly used ethnoveterinary plants, Rhoiscissus tridentata, Elephantorrhiza elephantina, Aloe marlothii and Urginea sanguinea, in vitro. Well-established B. caballi cultures were initially incubated with either imidocarb diproprionate and diminazene aceturate to validate the model, where after the studies were performed on the four plants. Effectivity was established as the degree of inhibition using a colour change method as well as by evaluating percentage parasitized cells on thin culture smears and calculating the degree of residual infectivity. The model was effective in demonstrating the in vitro efficacy of the well known anti-babesial drugs imidocarb and diminazene indicating an EC50 value of 0.08 and 0.3 microg/ml, respectively. Only the E. elephantina rhizomes acetone extracts were effective at a concentration of 100 microg/ml. It was also shown that the colour change method of evaluation was not very sensitive for determining activity of crude plant extracts.

Aloe↗
PubMed2001

The incidence of new and the prevalence and persistence of recurrent trypanosome infections in cattle in southwest Ethiopia exposed to a high challenge with drug-resistant parasites.

A method is described for calculating new infection incidence from monthly field data collected between April 1994 and February 1998 from an average of 770 Ethiopian Highland Zebu cattle maintained under traditional management in the Ghibe valley, southwest Ethiopia and exposed to a high challenge with drug-resistant parasites. Each month cattle with a packed cell volume (PCV)<26% and detected as parasitaemic, or cattle showing clinical signs of trypanosomosis, were treated with diminazene aceturate at 3.5 mg/kg body weight. An infection was defined as a new infection if it was preceded by 2 previous months in which both samples had a PCV>/=26% and were not detected with trypanosomes. Using this definition the average monthly incidence of infections of Trypanosoma congolense in cattle over 36 months of age was 13.3%, and the prevalence of recurrent infections 13.0%. Assuming that an animal had recovered from infection when PCV again returned to 26% without parasites being detected, mean persistence of infection was 3.8 months (median between 2 and 3 months). In contrast, T. vivax infections were susceptible to diminazene. The incidence of T. vivax infections in adults was lower than for T. congolense (2.8%), and they were less pathogenic (mean reduction of 3.1% units of PCV due to T. vivax infection compared with 4.6% units for T. congolense). Also, fewer cases were treated. Calves were first detected parasitaemic at an average age of 8.8 months and their infections persisted longer than those in adults. The effect of age on incidence of infection was not significant beyond 15 months of age. Adult male cattle appeared to be more susceptible to T. congolense infection than adult female cattle.

Animals↗
PubMed2005

Anti-babesial compounds from Curcuma zedoaria.

Anti-babesial activity was confirmed in an extract of the bark of Curcuma zedoaria. The active ingredients were isolated, and their chemical structures were determined to be zedoalactones A, B, and C based on spectral data. Zedoalactone C is a hitherto unreported compound. The IC50 vales of these active compounds against Babesia gibsoni were compared with a standard drug, diminazene aceturate. The IC50 value of diminazene aceturate was 0.6 microg/mL, while those of zedoalactones A, B, and C were 16.5, 1.6 and 4.2 microg/mL, respectively.

Animals↗
PubMed2006

Fumagillin, a new P-glycoprotein-interfering agent able to modulate moxidectin efflux in rat hepatocytes.

We have tested the ability of two compounds licensed in veterinary medicine: fumagillin and diminazene diaceturate to increase intracellular moxidectin quantity in rat hepatocytes. These compounds significantly increased the quantity of 14C-moxidectin (expressed as area under the time curve concentrations) in cultured rat hepatocytes by 44% and 65% for diminazene and fumagillin treatments respectively. In addition, we have tested these drugs for their interference with P-glycoprotein (P-gp) function in porcine kidney epithelial cells transfected with murine mdr1a (Mdr1a-LLCPK1). We examined the intracellular accumulation of rhodamine 123 (Rho 123) as a functional test to evaluate the effects of these two drugs on P-gp activity. In this model, only fumagillin led to a marked intracellular accumulation of Rho 123. After transforming the data to express the results as a percentage of the accumulation in the presence of the P-gp inhibitor valspodar (VSP), the maximal Rho 123 accumulation was 47% of that with VSP for 100 microm fumagillin. The EC50, the concentration needed to determine 50% of the maximal effect was 34 microm. Fumagillin interacts with P-gp function and appears as a promising compound among registered drugs available, which may optimize the therapeutic use of macrocyclic lactones (MLs).

ATP Binding Cassette Transporter, Subfamily B, Mem↗
PubMed1987

Trypanocidal activity of a 5-substituted 2-nitroimidazole compound (Ro 15-0216) in mice.

The trypanocidal activity of a 5-substituted 2-nitroimidazole compound (Ro 15-0216, 2-(dimethylamino)-4'-[(1-methyl-2-nitroimidazole-5-yl) methoxy] acetanilid) was tested in stocks of T.b. brucei, T.b. evansi, T. vivax, and T. congolense. The trypanosome stocks showed different sensitivities, the Trypanozoon group was most sensitive followed by T. vivax and T. congolense. Administration of the compound in the drinking water was superior to single intraperitoneal injections. A T.b. brucei stock with reduced sensitivity to Mel B and insensitive to diminazene aceturate was cured by a dose 13 times greater than that necessary for the drug-sensitive T.b. brucei stock, administered in the drinking water. Quinapyramine- and quinapyramine/suramin-resistant stocks of T.b. evansi were eliminated with doses of 63 and 160 mg/kg i.p., respectively; to eliminate the drug-sensitive T.b. brucei stock, 250 mg/kg i.p. were required. The combination of Ro 15-0216 with suramin showed a synergistic effect in suramin-sensitive and in suramin-resistant stocks of T.b. evansi, although high doses of suramin were applied in the latter. Synergism of Ro 15-0216 with diminazene aceturate was demonstrated in T. congolense-infected mice.

Acetanilides↗
PubMed1984

[The hypotensive effect of aromatic amidines and imidazolines].

Some amidine, diamidine and diimidazoline derivatives were tested on their ability to lower the blood pressure of the rat. Except for 5-amidino-2-phenylindole (271/179) all substances led to a short-lasting hypotension, the dose relationship of some of which was investigated. The biscationic character was a prerequisite for a strong hypotensive action. The predominantly peripheral origin of the blood pressure lowering action was shown for the substances pentamidine, diminazene, 6-amidino-2- (4-amidinophenyl)-indole (102/198), 5-amidino-2-(4-amidinophenyl) - benzofurane (150/49) and 2,6-diamidinoindole (261/115). A parasympathomimetic and histaminic efficiency could be excluded. The pressor effect of norepinephrine (noradrenaline) was reduced under the influence of pentamidine, diminacene and 102/198. With the dog 102/198 and 261/115 showed a diminution of heart rate and force as well as a vasodilatory effect. Using the rat, different cardiovascular parameters behaved analogous. Pentamidine, diminazene, 102/198 and 261/115 increased the force of contraction of the isolated rat atrium. Toxic effects were observed in doses as high as 0,5 mmol/l and l mmol/l. Pentamidine reduced the heart rate of the isolated atrium in a dose-dependent manner. Taking into account the in vitro results, the heart effects were interpreted as being reflectory. In the isolated rat aorta preparation the aforementioned substances in low doses shifted the dose-response curves of norepinephrine to the right, whereas higher doses also reduced the maximum contraction. Considering the results on the intact animal, a direct action of the diamidines on vascular smooth muscle was discussed.

Amidines↗
PubMed1997

Trypanosoma brucei: lack of cross-resistance to melarsoprol in vitro by cymelarsan-resistant parasites.

We have examined cross-resistance between trypanocidal drugs using a well-characterised drug-sensitive line, 247, and its cymelarsan-resistant derivative, 247melCyR. The cymelarsan-resistant line was cross-resistant to trimelarsen and melarsen oxide, and partially cross-resistant to two diamidines, pentamidine and berenil (diminazene aceturate). It was cross-resistant to lipid-soluble melarsoprol in vivo but to only a trivial degree in two in vitro assays. The potential role of adenosine transport in arsenical-induced killing of parasites was investigated. Adenosine, adenine, and the diamidines, but not inosine, were able to inhibit killing of drug-sensitive STIB 247 trypanosomes by cymelarsan and melarsen oxide in a concentration-dependent manner. These results are consistent with the view that these arsenical compounds enter trypanosomes via an adenosine-specific transporter. Melarsoprol-induced killing of trypanosomes was unaffected, however, by either purine and to only a slight degree by the diamidines. These data suggest that melarsoprol can enter trypanosomes by a route other than through an adenosine transporter and that there may be two mechanisms contributing to arsenical resistance in this drug-resistant line of trypanosomes.

Adenine↗
PubMed1983

The use of the 2 substituted 5-nitroimidazole, Fexinidazole (Hoe 239) in the treatment of chronic T. brucei infections in mice.

Relapse of chronic T. brucei infections was completely prevented by treating with either diminazene aceturate (Berenil) at 40 mg/kg or suramin (Germanin) at 20 mg/kg followed by four doses of the 2-substituted 5-nitroimidazole (Fexinidazole) (Hoe 239). None of these drugs administered singly elicited 100% permanent cures although a high percentage of the mice were cured with four doses of Fexinidazole at 250 mg/kg. A single dose of 20 mg/kg suramin followed by four daily doses of 30 mg/kg Fexinidazole will effectively eliminate all the trypanosomes from the brains of chronically infected mice.

Animals↗
PubMed1982

Relapse of monomorphic and pleomorphic Trypanosoma brucei infections in the mouse after chemotherapy.

Infections in mice were initiated with trypomastigotes from two lines of Trypanosoma brucei derived from the same primary isolated. Infections with one line were initiated by inoculation of metacyclic trypomastigotes from infected tsetse flies and the resulting infections were pleomorphic. The other line had been passaged 32 times in rodents and inoculation of bloodstream trypomastigotes gave rise to monomorphic infections. In both infections there were high levels of parasitaemia until death up to 4 weeks later if the infection was untreated. It was shown that after chemotherapy with 40 mg/kg diminazene aceturate (Berenil) relapses occurred in both types of infection after an aparasitaemic period of 2--3 weeks. Further, it was shown that 3 days after chemotherapy, brain tissue but neither spleen, liver nor blood was capable of transferring infection to normal recipient mice. There were two major differences in the response of the two infections to chemotherapy. First, treatment of the pleomorphic infection as soon as day 6 after infection resulted in a subsequent relapse while the monomorphic infection had to be at least 12 days old at the time of treatment before occurred. Second, following treatment of the pleomorphic, but not of the monomorphic infection there was an early transient recrudescence of low numbers of trypanosomes which were found to be non-infective to recipient mice. The early transient relapse was followed by a further aparasitaemic period and then the late continuous relapse characterised by large numbers of infective trypanosomes.

Amidines↗