Piperazine Citrate Research Articles

In Vitro. Screening of Cleome Viscosa. Extract for Anthelmintic Activity

The crude alcohol and aqueous extracts of the seeds of Cleome viscosa. Linn. (Capparidaceae) were investigated for their anthelmintic activity against Pheretima posthuma. and Ascardia galli.. Various concentrations (10–100 mg/mL) of each extract were tested in the bioassay, which involved determination of time of paralysis and time of death of the worms. Both extracts exhibited considerable anthelmintic activity in a dose-dependent manner. The most significant activity was observed at the highest concentration of 100 mg/mL against both types of worms. Piperazine citrate (10 mg/mL) was included as standard reference and distilled water as control.

<i>In vitro </i> anthelmintic property of various seed oils against <i> Pheritima posthuma</i>

Seed oils of Gynandropsis gynandra, Impatiens balsamina, Celastrus paniculata, Embelia ribes and Mucuna pruriens were investigated for their anthelmintic property against Pheritima posthuma . Three concentrations (10, 50 and 100 mg/ml) of each oil were studied in a bioassay, which involved the determination of time of paralysis and time of death of the worm. All the oils exhibited moderate to significant anthelmintic activity. Embelia ribes showed the best anthelmintic activity in both the parameters. Piperazine citrate (10 mg/ml) was included in the assay as standard reference drug.

In Vitro Antihelmintic Property of Various Seed Oils

Seed oils of Passiflora edulis, Jatropa curucas, Tinospora cordifolia, Sesbania grandiflora and Sapindus laurifolia were investigated for their antihelmintic property against Pheritima pasthuma. Three concentrations (10, 50 and 100 mg/ml) of each oil were studied in the bioassay, which involved the determination of time of paralysis and time of death of the worm. Sesbania grandiflora showed the highly significant antihelmintic activity in both the parameters (paralysis and death), while Tinospora cordifolia showed significant effect in case of time of death. Piperazine citrate (10 mg/ml) was included in the assay as standard reference drug.

Electrocardiographic Profile of Oral Piperazine Citrate in Healthy Volunteers

The electrocardiographic (ECG) profile of oral piperazine citrate was determined in healthy volunteers. Piperazine caused reduction in heart rate in all the subjects. The highest percentage of change was 15.7. The average pretreatment (73.6+/-6.59 beats/min) when compared with the heart rate 1 hour after piperazine was administered (64.6+/-5.21 beats/min) was statistically significant (P=0.0054). The QT and JT intervals had average increases of 9.7% and 11.1%, respectively. In contrast, piperazine did not have any effect on the QRS complex following its administration. However, the average PR interval 1 hour after ingesting oral piperazine 2 g was significantly prolonged, 0.18+/-0.0063 seconds compared with a pretreatment average of 0.16+/-0.0098 seconds. The difference between the 2 values was statistically significant (P=0.0161). No dysrhythmic phenomena were seen. Sinus rhythm was maintained in all the volunteers, with every QRS-T complex preceded by a P wave. The direction and magnitude of the mean electric axis of QRS complex and T wave were not altered by piperazine. It is concluded that oral piperazine citrate induced some changes on the ECG profile of healthy human volunteers, typical of many potent antiarrhythmic agents.

Evaluation of Evolvulus alsinoides Linn. for Anthelmintic and Antimicrobial Activities

Objective: To study the anthelmintic and antimicrobial activities of the ethanolic extract of Evolvulus alsinoides Linn. Materials and methods: The anthelmintic activity was evaluated on adult Indian earthworm Pheretima posthuma due to its anatomical and physiological resemblance with the intestinal roundworm parasites of human beings. The antibacterial activity of the crude ethanolic extract was performed by agar cup plate method. Results: The ethanolic extract caused paralysis followed by death of the worms at all tested dose levels. It was observed that the ethanolic extract of Evolvulus alsinoides is more potent than the reference control piperazine citrate. Potency of the extract was inversely proportional to the time taken for paralysis/ death of the worms. The activity confirms the dose dependency nature of the extract. The results of antimicrobial activity revealed that the extract exhibited activity against Pseudomonas aeruginosa and Escherichia coli but inactive against Staphyloccus aureus and Candida albicans . None of test concentrations exhibited comparable activity with the reference control ampicillin trihydrate. Conclusion: The present study concludes that the plant is also endowed with potential anthelmintic property in addition to its other popular uses in the traditional system of medicine.

In vitro Anthelmintic Properties of Buchholzia coriaceae and Gynandropsis gynandra Extracts

Methanol extracts from the leaves and stems of Gynandropsis gynandra and Buchholzia coriaceae were investigated for their activity against Fasciola gigantica, Taenia solium and Pheritima pasthuma, respectively. Five concentrations (10–100 mg/ml) of each extract were studied in the bioassay, which involved determination of time of paralysis and time of death of the worms. All the extracts exhibited considerable anthelmintic activities, and the order of sensitivity of the extracts to the worms was P. pasthuma > F. gigantica > T. solium. The most active of the extracts were B. coriaceae and G. gynandra stem methanol extracts. Piperazine citrate (10 mg/ml) and distilled water were included in the assay as standard reference drug and control, respectively.

Anthelmintic Activity of a Root Extract ofRitchiea capparoides var. longipedicellata

The methanol extract of the roots of Ritchiea capparoides var. longipedicellata was evaluated for in vitro anthelmintic activity against tapeworms, earthworms and roundworms. The extract was more active on tapeworms and had the least effect on roundworms. The activity was 2-4 times lower than that of the reference compound, piperazine citrate.

Normal-Phase High Performance Liquid Chromatographic Method with Dansylation for the Assay of Piperazine Citrate in Dosage Forms

Abstract The assay of the anthelmintic agent piperazine citrate in dosage forms has been accomplished by normal-phase HPLC after converting the drug to a UV-absorbing dansyl (DNS) derivative. For this purpose, an aliquot of an aqueous extract or dilution from tablets, powders, effervescent granules or syrups was first mixed with a solution of 1-benzylpiperazine, the internal standard, and next with solutions of DNS-chloride and sodium carbonate. Sonication of the reaction mixture led to the formation of the DNS-derivatives, with bis-DNS-piperazine separating as a crystalline product. After extraction into chloroform, and dilution of the extract with mobile phase, the DNS derivatives were separated on a cyanopropyl column with hexane-isopropanol (85:15) as the mobile phase. At a flow rate of 1.5 mL/min and a detection wavelength of 335 nm, DNS-1-benzylpiperazine and bis-DNS piperazine eluted at 4.0 and 8.5 min, respectively. Detector responses were linearly related to on-column concentrations of piperazine citrate ranging from 8–50 μg. The recovery of analyte from synthetic formulations simulating the various dosage forms was in all cases > 99.0% (range 99.7–102.0%). Assay results by the proposed method agreed closely with those obtained by the gravimetric method of USP 23.

Piperazine neurotoxicity: Worm wobble revisited

Piperazine has been used to treat pinworm and roundworm infections for over 40 years. Piperazine-induced cerebellar ataxia, causing the dropping of objects, clumsiness, and gait abnormalities, has been infrequently reported, usually in the setting of overdose or renal insufficiency. The unusual case of an otherwise well child who developed ataxia following seven days of piperazine citrate therapy is reported.

SPECTROPHOTOMETRIC DETERMINATION OF PIPERAZINE USING 3,5-DIBROMO-2-METHYL-p-BENZOQUINONE

A spectrophotometric method is developed for the quantitative determination of piperazine either in bulk drug or in pharmaceutical dosage forms. The method is based on the formation of vinylamine of this drug by interaction with acetaldehyde. The resulting enamine interacts with 3,5-dibromo, 2-methyl-p-benzoquinone (DEMQ) forming an intense blue colored aminovinylquinone which can be estimated spectrophotometrically at lmax642 nm. DEMQ is prepared according to a modified oxidation procedure by treatment of 2,4,6 tribromo-3-methylphenol with chromic oxide in a mixture of acetic acid and acetonitrile (9:1). Beer-Lambert's Law was adhered to over the range of 2-8, 2-9, and 2-10 mg.ml-1 for piperazine hydrate, tartrate, citrate and phosphate respectively. The optimum reaction conditions and the effect of all variables have been studied. The proposed method is simple, rapid, sensitive, accurate, precise and has been applied successfully for the analysis of some pharmaceutical formulations of piperazine including tablets, effervescent granules and syrup with good recoveries. Results obtained are in good agreement with those obtained by the official methods.

A field evaluation of anthelmintics for control of cyathostomes of horses in Brazil

The anthelmintic efficacy of ivermectin (IVM), piperazine citrate (PPZ) and fenbendazole (FBZ) alone, and combinations of FBZ with varying dosages of PPZ, was evaluated for the control of strogyles of Mangalarga equids. In all cases of positive strongyle egg counts per gram of faeces (EPG) before and after treatment, pure populations of cyathostome larvae with eight gut cells were consistently observed in faecal cultures. The faecal egg count reductions (FECR) were evaluated between Day 7 and Day 56 post-treatment. Significant differences ( P⩽0.05) were found between Day 7 and Day 49 when comparing the mean EPG values of IVM with those of the other anthelmintics. PPZ alone and the combination of FBZ (7.5 mg kg −1) and PPZ (55 mg base kg −1) did not show significant differences during the trial; both groups exhibiting an FECR of > 90% between Day 7 and Day 30. Horses treated with the combinations of FBZ (7.5 mg kg −1) and PPZ at either 40 or 25 mg base kg −1, and with FBZ alone at either 7.5 or 15 mg kg −1, showed an FECR of <90% 2 weeks after treatment. The emergence of a degree of resistance of strongyles to FBZ and PPZ in a segment of the cyathostomes in this population is suggested.

Endogenous formation of N-nitrosamines from piperazine and their urinary excretion following antihelmintic treatment with piperazine citrate

Antihelmintic treatment with piperazine (1,4-diazacyclohexane) for microfilarie parasitism results in the endogenous formation of piperazine-derived N-nitrosamines. The urinary excretion of these N-nitrosamines was determined by biochemical monitoring of 14 patients receiving 2 g piperazine citrate. The urinary excretion (mean +/- SD) of N-mononitrosopiperazine (MNPz) was 27.0 +/- 26.7 micrograms/day (range 0.6-96.0 micrograms/day). Trace levels of 0.73 +/- 0.92 micrograms/day N,N'-dinitrosopiperazine (DNPz) (range ND-2.8 micrograms/day) were also found in 7 of 14 urine samples. N-Nitroso-3-hydroxypyrrolidine (NHPYR), a metabolite of both MNPz and DNPz, was detected in 11 of 14 urine samples at a mean concentration of 1.74 +/- 1.72 micrograms/day (range ND-5.7 micrograms/day) and traces of N-nitrosodiethanolamine in two samples at levels of 0.3 and less than 0.1 micrograms/day. The results show that biochemical monitoring of urinary NHPYR may be a good indicator of endogenous MNPz formation. While DNPz was also detected in urine, conclusive validation for its endogenous formation could not be provided because no evidence was found for the presence of its major metabolite, N-nitroso-(2-hydroxyethyl)glycine in urine.

Anthelmintic treatment against Gyrodactylus sp. infecting rainbow trout Oncorhynchus mykiss

Various anthelmintics belonging to different pharmacological groups (ivermectin, clorsulon, closantel, netobimin, febantel, praziquantel, niclofolan, bithionol, trichlorfon, levamisole hydrochloride, piperazine citrate and dihydrochloride, nitroscanate), all of proven efficacy against certain helminths, were tested and compared for their in vivo and in vitro activity on a natural infection of Oncorhynchus mykiss by Gyrodactylus, probably G. salaris. The trout were also observed for signs of toxic reaction to the drugs. Complete efficacy (100 % reduction) with no toxic effects was achieved only by bithionol (20 mg I-') and nitroscanate (0.07 mg 1-l).

Mebendazole poisoning in infancy

Accidental mebendazole poisoning in an 8-week-old infant and respiratory arrest with tachyarrhythmia associated with continuous seizures is reported. Exchange transfusion was undertaken as a life-saving measure. Mebendazole, like piperazine citrate, has considerable neurotoxicity, especially in infancy, and we propose the use of exchange transfusion as a means of mebendazole elimination in infants.

Prevalence, incidence, intensity and associated morbidity of intestinal helminths in south Thailand

Prevalence, incidence, intensity and associated morbidity of intestinal helminths in South Thailand. International Journal for Parasitology 19: 217–228. Intensive surveys for Ascaris lumbricoides, Trichuris trichiura and hookworm were carried out in two villages in Phang Nga Province, southern Thailand, in order to measure prevalence, estimate incidence and determine the relation between intensity of infection and morbidity before and after chemotherapy. The study populations were a small upland village community (Nai Tone) and a grade school in a small coastal village (Boh Saen). About half of the Nai Tone villagers were given a broad spectrum antihelminthic (albendazole), and the Boh Saen students were all treated successively with three drugs: piperazine citrate to treat for Ascaris, pyrantel pamoate to treat for hookworm, and mebendazole to treat for Trichuris. Stool examinations were made using the quick Kato smear technique, questionnaires were administered concerning a variety of possible symptoms, and anthropometric and blood biochemical parameters were measured both before and after treatment. The prevalence of Ascaris was 31.0 and 22.6%, hookworm was 89.1 and 88.0% and Trichuris was 59.7 and 77.8% in the Nai Tone and Boh Saen study populations, respectively. Average intensity of Ascaris was highest in the 0–9 year age class (> 32,000 epg) in Nai Tone Village. Hookworm intensity of infection was higher in males than in females in all age classes, and in Nai Tone Village at least 25% of males and 20% of females had 8000 or more epg of faeces. Trichuris intensity of infection was highest between 5 and 10 years of age in both populations. The only signs or symptoms showing a significant ( P < 0.05) difference between high and low classes of intensity of infection and a significant improvement ( P < 0.01) after drug treatment, were headache and flatulance in the case of hookworm infection in Boh Saen School. The presence of multiple infections made testing of hypotheses concerning particular parasite species difficult.

Estudo comparativo da eficiência de Ivermectina, de Fenbendazole, de Mebendazole e de Mebendazole associado ao Citrato de Piperazina.no controle de ciatostomíneos de eqüinos da raça Mangalarga Paulista

The anthelmintic efficacy of Ivermectin, Fenbendazole, Mebendazole and Mebendazole combined with Piperazine Citrate for the control of cyathostomes of Mangalarga Paulista equids were analyzed. In all cases of positive eggs per gram (epg) counts before and after treatment, pure populations of cyathostome larvae with eight gut cells in faecal cultures were consistently observed. The percentages of efficacy were evaluated between the 7th and 72nd days post-treatment. Confronting the epg mean values of Ivermectin in respect of the others anthelmintics, significant differences were found between the 7th and 57th days; Fenbendazole and Mebendazole did not show significant differences during the experiment. The association of Mebendazole combined with Piperazine Citrate indicated a significantly higher efficacy than Fenbendazole and Mebendazole between the 7th and 30th days.

Antibodies to diethylcarbamazine cross-react with microfilariae of Wuchereria bancrofti

Antibodies directed against the microfilarial sheath have been instrumental in the immune elimination of circulating microfilariae in human lymphatic filariasis. We report here that antibodies to diethylcarbamazine (DEC, the most commonly used anti-filarial drug) cross-react with the sheath of Wuchereria bancrofti microfilariae. Antibodies with reactivity to DEC were raised in rabbits by immunization with a conjugate of methylpiperazine carboxylic acid (MPCA, an acid hydrolysis product of DEC) coupled to bovine serum albumin. The reactivity of these antibodies with microfilarial sheath of W. bancrofti was demonstrated by indirect immunofluorescent assay and indirect immunoperoxidase assay. This reactivity could be effectively inhibited by pre-incubation of the antisera with different haptens such as DEC, MPCA or piperazine citrate.

A comparison of the genetic activity of pyrvinium pamoate with that of several other anthelmintic drugs in Saccharomyces cerevisiae

Several anthelmintic drugs that are used routinely in oxyuriasis therapy were analyzed for genotoxicity in a diploid mitotic recombination and gene conversion assay (strain D5 of Saccharomyces cerevisiae), and in a haploid yeast reversion assay (strain XV185-14C). Piperazine citrate, piperazine adipate, mebendazole and thiabendazole did not appear to be genotoxic in either yeast strain. Pyrvinium pamoate induced the reversion of the missense, nonsense and frameshift alleles in strain XV185-14C, whereas pyrantel pamoate induced only the reversion of the frameshift allele. Pyrvinium pamoate was recombinogenic in strain D5, and there is an indication that pyrantel pamoate, at the lowest dose that was tested, might induce gene conversion or aneuploidy.

Mortality of captive tortoises due to viviparous nematodes of the genus Proatractis (Family Atractidae).

Between September 1982 and January 1984, verminous colitis was diagnosed post mortem in eight red-footed tortoises (Geochelone carbonaria) and three leopard tortoises (Geochelone pardalis) from the reptile collection of the National Zoological Park. This represented 69% of 16 tortoise necropsy accessions for that period. Etiology was determined to be a viviparous pinworm-like nematode of the genus Proatractis (Family Atractidae). Clinical signs were either nonspecific, consisting of anorexia, lethargy, and depression, or were absent. Limited trials with piperazine citrate and fenbendazole appeared to be ineffectual against the parasite and supportive therapy was unsuccessful. Post mortem examination revealed roughening and thickening of the mucosa of the cecum and colon, and in severe cases myriads of tiny (0.5-1.0 cm) nematodes were evident on the mucosal surface. In six tortoises, worms were found also in the small intestine. Histopathologic features in severe cases included mucosal necrosis with parasites and mixed inflammatory cells extending into the tunica muscularis. Focal to diffuse lymphoplasmacytic infiltrates were present consistently in the submucosa of the cecum and colon, and similar but milder lesions occasionally occurred in the small intestine.

The Anthelmintic Activity of Some Iraqi Plants of the Cucurbitaceae

The anthelmintic efficacy of four plants of the Cucurbitaceae against Hymenolepis nana (tapeworm) and Aspicularis tetraptera (pinworm) infections in mice was evaluated utilizing piperazine citrate ...