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PubMed1984

Chemoprophylaxis with diminazene aceturate in experimental Babesia bigemina infection in cattle.

Four-month-old fully susceptible cross bred calves were immunised against Babesia bigemina infection by treating them, during the prepatent period, with one or two doses of diminazene aceturate at 3 mg (kg bodyweight)-1. After 45 days the recovered calves were challenged with the homologous strain of B bigemina infected blood. The ensuing host responses, body temperature, parasitaemia, haemoglobin, packed cell volume, haemoglobinuria, capillary agglutinating antibodies and mortality, were studied. The four untreated control calves developed a severe form of the disease with classical symptoms and two died. Calves of both groups which recovered resisted the challenge infection with a mild relapse in the immunised group, thus indicating a state of premunition. The effect of one dose of diminazene was sufficient to suppress all the clinical effects of the disease.

Amidines↗
PubMed1983

A comparison of the efficacy of isometamidium, amicarbalide and diminazene against Babesia canis in dogs and the effect on subsequent immunity.

Isometamidium, amicarbalide and diminazene were used to treat experimentally induced canine babesiosis. Relapse parasitaemias developed after treatment in all groups of animals. The relapse interval, however, was shorter and more relapses occurred after treatment with amicarbalide than either of the other 2 drugs. Only half of the dogs treated with either isometamidium or diminazene relapsed to infection. Challenge with homologous parasites 62 days after initial infection resulted in severe babesiosis in all 3 animals which had not developed relapse infections. Of the 9 animals which had relapses after treatment only 1 developed severe babesiosis following homologous challenge.

Amidines↗
PubMed1999

Polymerase chain reaction and DNA probe hybridization to assess the efficacy of diminazene treatment in Trypanosoma brucei-infected cattle.

Four of eight Ankole longhorn cattle experimentally infected with Trypanosoma brucei were treated with 7 mg/kg diminazene aceturate (Berenil, Hoechst AG, Germany) at day 71 postinfection. The trypanocidal activity was monitored using polymerase chain reaction (PCR) and DNA probe hybridization. When extracted parasite DNA (without host DNA) was used, as little as 1 fg per reaction, which is equivalent to about 1-10% of the DNA in a single trypanosome, produced a specific product that was visible as a 177-bp band in an agarose gel. In infected cattle, specific PCR products could be amplified at as early as 1 day postinfection. PCR signals remained positive during infection, except in one sample, although aparasitemic phases occurred. In cases where treatment resulted in a significant clinical improvement, PCR signals disappeared at 3-4 days after the administration of the drug. By contrast, in cattle that showed clinical signs of CNS involvement after treatment, although aparasitemic, and died before the termination of the experiment, specific products could be amplified on several occasions following treatment. The PCR signals generated after treatment could be further enhanced by subsequent slot-blot hybridization with a T. brucei-specific DNA probe. We conclude that PCR coupled with DNA probe hybridization provides a highly sensitive tool for the assessment of therapeutic efficiency and disease progression in trypanosome infections, especially in chronic infections when the level of parasitemia is low or when trypanosomes are sequestered at cryptic sites.

Animals↗
PubMedDate not supplied

Diminazene aceturate residues in the tissues of healthy, Trypanosoma congolense and Trypanosoma brucei brucei infected dogs.

The tissue distribution and residue profile of diminazene aceturate was investigated in healthy dogs and in dogs infected with Trypanosoma congolense and Trypanosoma brucei brucei. The drug was administered at 3.5 mg/kg i.m. and tissue samples were taken post mortem from the animals at 48, 72, 120, 168 and 240 h after injection. The drug was distributed to various organs and tissues of the body with the highest concentrations occurring in liver and kidney. Higher drug levels were obtained in the tissues of healthy dogs compared with trypanosome infected animals except in the brain. The levels of residues in the healthy animals were significantly different (P less than 0.05) from those of the infected dogs. The drug residues were still detectable in the tissues of the animals 10 days after drug administration.

Animals↗
PubMed1988

Relapses in dogs experimentally infected with Trypanosoma brucei and treated with diminazene aceturate or isometamidium chloride.

Twenty dogs of mixed local East African breeds were used. Five of the dogs were uninfected controls and 15 were infected with T. brucei (ILRAD 273). Five of the infected dogs were untreated controls, five were treated with a high curative dose of diminazene aceturate, (7 mg kg-1 body weight (wt.), and five were given a subcurative dose of isometamidium chloride (1 mg kg-1 body wt.). The drugs, given at 8 days post infection (d.p.i..), led to apparent recovery. The antibody titres, however, remained high in both groups and at 42-49 d.p.i. there was at least one relapse in each treatment group. Parasite populations from relapsed animals were more resistant to the drugs than the original infecting populations. The implications of these findings are discussed.

Alanine Transaminase↗
PubMed1997

Long-term occurrence of Trypanosoma congolense resistant to diminazene, isometamidium and homidium in cattle at Ghibe, Ethiopia.

Ten trypanosome isolates were collected at random from cattle at Ghibe, Ethiopia, in February 1993 and all shown to be savannah-type Trypanosoma congolense. When inoculated into naïve Boran (Bos indicus) calves, all 10 isolates were resistant to diminazene aceturate (Berenil), isometamidium chloride (Samorin) and homidium chloride (Novidium) at doses of 7.0 mg/kg body weight (b.w.), 0.5 mg/kg b.w. and 1.0 mg/kg b.w., respectively. In order to determine whether this multiple-drug resistance was expressed by individual trypanosomes, clones were derived from two of the isolates and characterised in mice for their sensitivity to the three compounds; by comparison to drug-sensitive populations, the two clones expressed high levels of resistance to all 3 trypanocides. In experiments to characterise the uptake kinetics of [14C]-Samorin, the maximal rates of uptake (Vmax) for 4 Ghibe isolates ranged from 9.2 to 15.0 ng/10(8) trypanosomes/min. In contrast, Vmax for the isometamidium-sensitive clone T. congolense IL 1180 was 86.7 +/- 8.6 ng/10(8) trypanosomes/min. Lastly, molecular karyotypes were determined for eight isolates: seven different chromosome profiles were observed. These data indicate that in February 1993 there was a high prevalence of drug-resistant trypanosome populations with different chromosome profiles in cattle at Ghibe. Since a similar situation existed at the same site in July 1989, this suggests that the drug-resistance phenotype of trypanosomes at Ghibe had not altered over a 4 year period.

Animals↗
PubMed1998

A trypanosome oligopeptidase as a target for the trypanocidal agents pentamidine, diminazene and suramin.

African trypanosomes contain a cytosolic serine oligopeptidase, called OP-Tb, that is reversibly inhibited by the active principles of three of the five most commonly used trypanocidal drugs: pentamidine, diminazene and suramin. OP-Tb was inhibited by pentamidine in a competitive manner, and by suramin in a partial, non-competitive manner. The inhibition of OP-Tb by a variety of suramin analogues correlated with the trypanocidal efficacy of these analogues (P=0.03; by paired Student's t-test). Since intracellular (therapeutic) concentrations of pentamidine and suramin are reported to reach approximately 206Ki and 15Ki respectively, we suggest that these drugs may exert part of their trypanocidal activity through the inhibition of OP-Tb.

Animals↗
PubMed2001

Validation of a polymerase chain reaction assay for monitoring the therapeutic efficacy of diminazene aceturate in trypanosome-infected sheep.

The diagnostic performance of a polymerase chain reaction assay (PCR) for monitoring the effectiveness of aceturate diminazene treatment was compared with those of an antibody-detection ELISA test and the buffy-coat technique using sheep experimentally infected with either savannah-type or forest-type Trypanosoma congolense or T. vivax. Within the period of infection, the PCR using specific savannah-type T. congolense primers showed a significant higher diagnostic sensitivity (p<0.05) than the buffy-coat technique. Both techniques gave closed results for detecting forest-type T. congolense or T. vivax infections. Following trypanocidal treatment, the PCR showed that specific product disappeared definitively 1 or 2 days later in animals in which a decrease of the antibody level and a significant improvement of the red packed cell volume were observed. The occurrence of relapse infection was detected by the PCR in one animal infected by T. vivax on day 19 post-treatment and confirmed by the persistence and increasing antibody level whereas the buffy-coat technique detected parasites 42 days later. Then, the PCR signals remained positive on several occasions while parasitaemia was detected only two times.The application of PCR combined with the antibody detection appeared to provide a useful tool as compared to the buffy-coat technique for monitoring the effectiveness of trypanocidal treatment.

Animals↗
PubMed1982

The efficacy of berenil (diminazene aceturate) against Trypanosoma evansi infection in mice.

The efficacy of berenil (diminazene aceturate) was studied in experimental Trypanosoma evansi infection in albino mice. The criteria used for the assessment of the anti-trypanosomal effect of berenil included the examination of the blood and tissues for T. evansi and the clinical, pathological and enzyme histochemical changes seen in the lungs, heart, liver, kidney and spleen at intervals after treatment. Single doses of 10 and 20 mg/kg of berenil given intraperitoneally or intramuscularly to infected mice produced a complete elimination of the protozoon and caused a slow tissue recovery mirrored in the persistence of lesions in different organs. Single doses of 3.5 mg/kg of berenil were less effective and none of the three dose levels of the drug used induced toxic effects in albino mice.

Amidines↗
PubMed1976

Pharmacokinetic investigations on diminazene and rolitetracycline in comparison to a combination of both.

Serum level tests were carried out on healthy cows with a combination drug of one part Berenil and two parts Reverin. When compared with the commercial preparations Berenil (Diminazene) and Reverin (Rolitetracycline), the kinetic behaviour of Reverin in the combination preparation was identical. In the case of Berenil, administered in the form of the combination drug, the second slow elimination phase with a 63 hour half-life, as found after the administration of Berenil only, could not be observed. Eight hours after administration of the combination only minimal Berenil serum levels were detectable, after 24 hours the levels were lower than the limit of detection. This has a practical bearing on the question of residues.

Amidines↗
PubMed1991

Immunological changes in Babesia rodhaini infected BALB/c mice after treated with anti-babesial drug; diminazene diaceturate.

A model system capable of investigating immunological changes was first established in Babesia rodhaini infected mice with an aid of a drug, diminazene diaceturate (DD). Intraperitoneal (ip) inoculation with B. rodhaini resulted in acute death in euthymic (nu/+) and athymic (nu/nu) BALB/c mice. Treatment with DD at an early stage of infection saved both mice from acute death. Parasitemia recurred in some of them but resulted in death only in nu/nu mice. A re-challenge with 10(5) parasitized erythrocytes (PE) on the surviving mice on day 28 post infection revealed resistance in nu/+ but not in nu/nu mice. The results suggested a participation of the thymus in the protective mechanisms. Immunological changes were then observed on nu/+ and nu/nu mice which were inoculated ip with 10(4)PE and treated with the drug, and then challenged with 10(5)PE ip on day 28. An antibody response was measured with immediate reaction by footpad injection of a soluble antigen of B. rodhaini and by ELISA of serum antibody using the antigen and protein A, on day 10 and later, and further a pronounced response was detected after re-challenge in nu/+ mice. No response was detected by ELISA in nu/nu mice. Delayed footpad reaction was seen in nu/+ mice by day 14 and later but it was suppressed after the re-challenge.(ABSTRACT TRUNCATED AT 250 WORDS)

Acute Disease↗
PubMed2004

Protective efficacy of isometamidium chloride and diminazene aceturate against natural Trypanosoma brucei, Trypanosoma congolense and Trypanosoma vivax infections in cattle under a suppressed tsetse population in Uganda.

The protective efficacy of isometamidium chloride (ISMM) and diminazene aceturate (DIM) against Trypanosoma brucei, Trypanosoma congolense and Trypanosoma vivax infections in cattle under a suppressed tsetse population was assessed in southeast Uganda. A total of 66 and 57 trypanosome-infected cattle were treated with ISMM and DIM, respectively together with 177 trypanosome-free animals not treated were followed for 12 months, checked every 4 weeks. There was no statistical difference in the mean time to infection with any trypanosome species in animals treated with ISMM or DIM. However, the mean time to trypanosome infection was significantly longer for treated animals than controls. The mean time to infection with each of the three trypanosome species differed significantly, with the average time to T. vivax infection the lowest, followed by T. congolense and then T. brucei. The protective efficacy of DIM was as good as that of ISMM; implying curative treatments against trypanosomosis are sufficient for combination with tsetse control. Isometamidium chloride or DIM had the highest impact on T. brucei and T. congolense infections in cattle.

Animals↗
PubMed1999

The formation of DNA interstrand cross-links by a novel bis-[Pt2Cl4(diminazene aceturate)2]Cl4.4H2O complex inhibits the B to Z transition.

We present data demonstrating that the cytotoxic compound [Pt2Cl4(diminazene aceturate)2]Cl4.4H2O (Pt-berenil) circumvents cisplatin resistance in ovarian carcinoma cells. The analysis of the interaction of Pt-berenil with linear and supercoiled DNA indicates that this compound induces the formation of a large number of covalent interstrand cross-links on DNA and that this number is significantly higher than that produced by cis-diamminedichloroplatinum(II) (cis-DDP). Renaturation experiments, interstrand cross-link assays, and electron microscopy indicate that the kinetics of DNA interstrand cross-link formation caused by Pt-berenil binding is faster than that caused by cis-DDP at similar levels of platinum bound to DNA. Furthermore, the number of DNA interstrand cross-links in Pt-berenil-DNA complexes is influenced by supercoiling. Circular dichroism experiments show that Pt-berenil strongly inhibits the B-DNA-to-Z-DNA transition of poly(dG-m5 dC). poly(dG-m5dC) at salt concentrations (3 mM MgCl2) at which the native methylated polynucleotide readily adopts the Z-DNA conformation, which suggests that the induction of interstrand cross-links by Pt-berenil inhibits the Z-DNA transition. On the basis of these results, we propose that bis(platinum) compounds with structure similar to Pt-berenil may act as blockers of DNA conformational changes and may also display activity in cisplatin-resistant cells.

Animals↗
PubMedDate not supplied

Liquid chromatographic determination of diminazene diaceturate (Berenil) in raw bovine milk.

A simple liquid chromatographic (LC) method is presented for the determination of diminazene (DZ) in raw bovine milk. DZ is extracted from raw milk by chilled aqueous centrifugation and is isolated from milk components on a cyano solid-phase extraction column. DZ is eluted by using a methanol-ion pairing reagent. A Phenomenex LUNA CN column and an acetonitrile-buffered mobile phase with a counter ion are used for gradient LC. The LC effluent is monitored at a detection wavelength of 372 nm by using a deuterium lamp. Under the parameters described, the retention time of DZ is 8-10 min with a peak area response of 6.5 mAU/ng. The method demonstrated excellent precision over all levels tested (25-400 ppb) with an overall average recovery of 90.4 +/- 14.5%. The method is applicable to the monitoring of milk for DZ residues at the 25 ppb level with a limit of quantitation of 10 ppb.

Animals↗
PubMed2005

Comparative application of wavelet approaches to absorption and ratio spectra for the simultaneous determination of diminazene aceturate and phenazone in veterinary granules for injection.

A comparison of two wavelet approaches, Daubechies and reverse Biorthogonal, is described for the quantitative resolution of a binary mixture of diminazene aceturate (DIMA) and phenazone (PHE) in veterinary granules for injection without any chemical separation. These two approaches were specified as db4 (a = 180) and rbior3.7 (a = 125) respectively, after testing the signal analysis parameters for the overlapping absorption spectra and ratio spectra. In the first step db4 (a = 180) was applied to the original absorbance data vector of DIMA and PHE. In the second step rbio3.7 (a = 125) was applied to the ratio spectra data vectors of DIMA using the divisor PHE. The same approach was also subjected to the ratio spectra of PHE using the divisor DIMA. The db4 (a = 180) and rbior3.7 (a = 125) calibration graphs were constructed using the transformation values obtained in the wavelet domain. In the method validation, the wavelet calibration functions were tested using synthetic mixtures and the standard addition technique. The simultaneous quantitative analysis of DIMA and PHE in the commercial veterinary preparation was achieved by the elaborated methods. The assay results were compared with each other and good agreement was observed.

Algorithms↗
PubMed1987

Ejaculate characteristics of sheep infected with Trypanosoma brucei and T vivax: changes caused by treatment with diminazene aceturate.

The effect of Trypanosoma brucei and T vivax on the ejaculate of sheep and the rate of recovery with diminazene aceturate treatment was investigated. Animals were made to ejaculate once a week before infection, during infection and after treatment. Parameters studied were semen volume, semen colour, sperm motility and concentration, percentage dead spermatozoa and sperm morphology. Both infections severely affected the quality of the ejaculate although in T vivax infection there was no appreciable change in semen volume and sperm concentration. There was a reduction in sperm motility and concentration, an increase in the percentage of dead spermatozoa and in abnormal sperm morphology. Treatment led to improvement in all parameters but recovery was faster in T vivax than in T brucei infection. Ejaculate with few primary abnormalities was not obtained until 19 weeks after treatment.

Animals↗
PubMed1982

Delay in resolution of trypanosome-induced genital lesions in male rabbits infected with Trypanosoma brucei and treated with diminazene aceturate.

The effects of drug therapy on the resolution of the genital lesions accompanying systemic Trypanosoma brucei infection was investigated using male California White rabbits. Infected animals were treated with diminazene aceturate two to 13 days after the onset of gross scrotal lesions; they were killed at different intervals after treatment to determine the histological evidence of healing of the genital lesions. It was found that, although parasites disappeared soon after treatment, regeneration of seminiferous epithelium depended on the severity of the initial lesions. Only mildly afflicted rabbits had fully recovered within 141 days.

Amidines↗