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At least 19 recordsLinked to original sources
PubMed1988

Arsenical and mercurial inhibition of tyrosine transport by the flounder intestine.

The effects of mercurials and arsenicals on tyrosine absorption by the winter flounder Pseudopleuronectes americanus were studied using isolated intestinal strips mounted in Ussing chambers. The mercurials mercuric chloride (HgCl2), p-chloromercuriphenyl sulfonic acid (PCMBS), and phenylmercuric acetate (PMA) and the arsenicals oxophenylarsine and arsenamide were chosen for their different chemical properties. The transmural absorptive fluxes (mucosa to serosa, M----S) were inhibited by mucosal additions of 0.1 mM HgCl2 (64% inhibition), 1.0 mM PCMBS (41% inhibition), and 0.25 mM oxophenylarsine (48% inhibition). Tyrosine tissue accumulation was inhibited 68% by 0.1 mM HgCl2, 42% by 1.0 mM PCMBS, and 62% by 0.25 mM oxophenylarsine. Serosal addition of 1.0 mM PCMBS inhibited M----S flux by 45%. Transepithelial potential (TEP) was measured to monitor changes in ionic gradients across the epithelial membrane. Mucosal addition of 0.1 mM HgCl2, and of 0.25 and 0.05 mM oxophenylarsine significantly changed the TEP. Serosal additions of 0.1 mM HgCl2, 1.0 mM PCMBS, and 0.25 mM oxophenylarsine also altered the TEP significantly. These results indicate that Na+-dependent tyrosine uptake is inhibited by arsenicals and mercurials, but it is unclear whether the Na+-tyrosine cotransport system or the transmembrane ionic gradients were affected by these heavy metals.

4-Chloromercuribenzenesulfonate↗
PubMed1969

Chemotherapeutic reactions of Chandlerella hawkingi, the filarial parasite of the Indian jungle crow, Corvus macrorhynchos (Agler).

1. A high percentage of Indian jungle crows (Corvus macrorhynchos Wagler), found in and around Lucknow, harbour a natural filarial infection Chandlerella hawkingi. The microfilariae of this species are sheathed and show nocturnal periodicity.2. Fourteen compounds active against other kinds of filariae, especially against Litomosoides carinii, were tested against Ch. hawkingi in jungle crows to find whether this infection would be suitable for routine filarial chemotherapy. This is apparently the first report of systematic screening of antifilarial compounds against an avian filariasis.3. Tartar emetic (10 mg/kg intravenously, daily for 6 days) and arsenamide (5 mg/kg intraperitoneally, daily for 6 days) proved to be effective in killing adult worms. Trivalent tryparsamide, though effective, was toxic in the doses tried. Diethylcarbamazine and other compounds tested were ineffective.4. The chemotherapeutic susceptibilities of Ch. hawkingi differ considerably from those of L. carinii and Wuchereria bancrofti.

Animals↗
PubMed1986

Electronic spreadsheet program for estimating two-compartment intravenous pharmacokinetic parameters by least squares linear regression analysis.

A microcomputer program using an electronic spreadsheet program was developed to calculate pharmacokinetic values of thiacetarsamide sodium, a drug used to kill the adult heartworm (Dirofilaria immitis) parasite of the dog. A least squares, semilogarithmic regression analysis was done on data using a two compartment intravenous model. The data entered includes the time after injection and the drug concentration at that time. A graph of the points can be viewed or plotted, with the time on the x-axis, and the natural log of the drug concentration on the y-axis. The program was developed on a Televideo (512 kbytes) microcomputer. The spreadsheet used was Lotus 123 with the pharmacokinetics program occupying 16 kbytes of memory (720 cells) out of the 400 kbytes available with Lotus.

Animals↗
PubMed1996

Thiacetarsamide depresses relaxation of canine pulmonary artery in vitro.

Little information is available on the primary pharmacological effects of thiacetarsamide on mammalian systems, particularly on blood vessels. The effects of thiacetarsamide on arterial responses was studied in isolated rings from canine pulmonary artery. Vessels were exposed to thiacetarsamide and dose-response relationships were applied to methacholine and nitroglycerin. To rule out non-specific effects of antihelmintics, the effects of two other antifilarial drugs, diethylcarbamazine and ivermectin, were also tested. Thiacetarsamide significantly depressed relaxation of canine pulmonary artery to both methacholine and nitroglycerin, and significantly enhanced constriction to norepinephrine. Neither diethylcarbamazine nor ivermectin altered vascular response. These direct effects of thiacetarsamide on arterial responsiveness may be responsible, in part, for acute pulmonary complications observed in dogs infected with Dirofilaria immitis after adulticide treatment.

Animals↗
PubMed2006

Influence of sulfide (S2-) on preservation and speciation of inorganic arsenic in drinking water.

Generally, H2SO4, HNO3, HCl or the combination of ethylenediaminetetraacetate with acetic acid (EDTA-HAc) have been used to preserve arsenite and arsenate species prior to analysis. When these acidic preservatives are added in sulfidic water, instantaneous precipitation of poorly crystalline orpiment, As2S3(am), occurs, thereby lowering the total arsenic, As(Tot), analysis. A new method for the determination of As(Tot) was developed in which acid-preserved sulfidic water samples were oxidized with NaOCl, converting As2S3(am) and thioarsenic species to arsenate. A new method was also developed for the separation of uncharged arsenite and charged thioarsenic species in fresh, unpreserved sulfidic water by adsorbing the charged thioarsenic species while allowing uncharged arsenite to pass through a strong-base resin unhindered. The adsorbed thioarsenic species could be eluted efficiently with 0.16 M NaOCl solution.

Adsorption↗
PubMed2001

Chronic fatigue syndrome in horses: diagnosis and treatment of 4 cases.

A report from England has suggested that Chronic Fatigue Syndrome exists in equines and constitutes an emerging veterinary problem. Preliminary epidemiological studies seem to confirm the zoonotic implications of CFS. An arsenical drug, sodium thiacetarsamide, was administered to four horses with a diagnosis of Chronic Fatigue Syndrome (CFS), already treated unsuccessfully with different medications. The CFS-like lethargy, with accompanying symptoms and signs, of the four animals obtained a complete remission after intravenous treatment with this drug at low dosage (0.1 mg/kg/day). No adverse side effects were ever noticed. This clinical response was associated with recovery from anaemia and decrease of muscular enzyme values in two of the four horses. In all patients, micrococci-like bacteria found before treatment adhering to the outer surface of many red blood cells, disappeared at post-treatment controls. Considerations are made on the possible action of an arsenical drug, used in isolation, in the treatment of CFS.

Animals↗
PubMed2001

Chronic Fatigue Syndrome (CFS) in 15 dogs and cats with specific biochemical and microbiological anomalies.

A great deal of controversy and speculation surrounds the etiology of Chronic Fatigue Syndrome (CFS) in human patients and the existence of a similar illness in animals. To evaluate the association with a presumptive staphylococcal infection and bacteremia, seven dogs and eight cats diagnosed with CFS (two meeting the CDC working case definition) were submitted to rapid blood cultures and fresh blood smears investigations. Nine out of 15 blood cultures proved Staph-positive and four isolates were specified as S. xilosus (3) and S. intermedius (1). The presence of micrococci-like organisms in the blood was of common observation among these subjects, in association with fatigue/pain-related symptoms and biochemical abnormalities suggestive of a myopathy. Following treatment with a low dosage arsenical drug (thiacetarsamide sodium, Caparsolate, i.v., 0.1 ml/kg/day) all patients experienced complete remission. Micrococci disappeared from the blood at post-treatment controls made 10-30 days later. The outcomes were compared with those of five healthy controls and five 'sick with other illness' patients showing significant difference.

Animals↗
PubMed1985

Pulmonary manifestations of heartworm disease.

The clinical signs associated with heartworm disease are the result of changes in the pulmonary arterial system. These clinical signs are the result of either pulmonary hypertension or lung parenchymal disease associated with vascular changes. An increase in pulmonary arterial pressure produces an increase in right ventricular afterload, which may lead to exercise intolerance, syncope, and right-sided congestive heart failure. Coughing, dyspnea, and hemoptysis are the results of pulmonary parenchymal disease.

Adrenal Cortex Hormones↗
PubMed2005

Novel thioarsenic metabolites in human urine after ingestion of an arsenosugar, 2',3'-dihydroxypropyl 5-deoxy-5-dimethylarsinoyl-beta-D-riboside.

The presence of arsenic-containing carbohydrates, arsenosugars, in many seafoods raises questions of human health concerning the ingestion and metabolism of these compounds. A previous study investigating the metabolites in human urine after the ingestion of a common arsenosugar 2',3'-dihydroxypropyl 5-deoxy-5-dimethylarsinoyl-beta-d-riboside (oxo-arsenosugar) showed that the arsenic was rapidly excreted in the urine and was present as at least 12 metabolites, only three of which could be identified. In this repeat study with oxo-arsenosugar and using high-performance liquid chromatography/inductively coupled plasma mass spectrometry, we report the identification of seven arsenic metabolites, which together accounted for 88% of the total urinary arsenic collected over 61 h. The metabolites included previously reported human urinary arsenicals dimethylarsinate (DMA), oxo-dimethylarsenoethanol (oxo-DMAE), and trimethylarsine oxide, in addition to new human metabolites oxo-dimethylarsenoacetate (oxo-DMAA), thio-dimethlyarsenoacetate (thio-DMAA), thio-dimethylarsenoethanol (thio-DMAE), and the thio-arsenosugar. Cytotoxicity testing of the major metabolites DMA, oxo-DMAE, thio-DMAE, oxo-DMAA, and thio-DMAA showed that they were nontoxic even at 10 mM, except for DMA, which showed some toxic effects at 1 mM.

Adult↗
PubMed2001

Chronic fatigue and immune dysfunction syndrome associated with Staphylococcus spp. bacteraemia responsive to thiacetarsamide sodium in eight birds of prey.

Chronic fatigue and immune dysfunction syndrome (CFIDS) is a recognized human illness with zoonotic implications that is rarely described in animals. Eight birds of prey examined between 1992 and 1995 and sharing common symptoms (asthenia, inability to fly, poor appetite and emaciation) underwent laboratory tests revealing immunodeficiency, anaemia, high creatine kinase levels and low serum magnesium levels. Diagnosis of CFIDS was based upon these features. The effectiveness of an arsenic-based medication, thiacetarsamide sodium, administered intravenously for 2-3 days at low dosages (0.1 ml/kg/day) has been demonstrated by checks carried out 10, 20 and 30 days after therapy. The symptoms and the immune and haematological dysfunctions disappeared within 2-4 weeks of treatment. In all patients, micrococcus-like organisms found adhering to the outer surface of many red blood cells, had disappeared at post-treatment controls. Two of five blood cultures were positive for Staphylococcus spp. (S. intermedius and S. xilosus). Consideration is given to the pharmacological activity of an arsenic-based drug in animal illnesses resembling CFIDS.

Animals↗
PubMedDate not supplied

Validation of deconvolutional analysis for the measurement of hepatic function in dogs with toxic-induced liver disease.

The extraction of the hepatobiliary radiopharmaceutical 99mTc-mebrofenin (Choletec) by the liver can be used to evaluate the severity of hepatocellular disease. The hepatic parenchymal cells extract mebrofenin from the blood by the same active transport mechanism as bilirubin. The ability of the liver to extract 99mTc-mebrofenin is a measure of hepatic parenchymal cell function. In this study, we induced hepatocellular disease by administration of a hepatotoxic drug and compared a direct method of determining the hepatic extraction of 99mTc-mebrofenin to hepatic extraction fraction derived from deconvolutional analysis. We also compared both methods of calculating the hepatic extraction of 99mTc-mebrofenin to liver histopathology. Hepatic extraction fraction derived from deconvolutional analysis correlated very well to the direct measurement technique (R=0.922, p < 0.001). Both methods of determining hepatic extraction correlated well to quantitative histopathology, having the same correlation coefficient and p values. (R=-0.833, p=0.003). As the hepatic extraction 99mTc-mebrofenin decreased, the severity of the histopathologic lesions of the liver increased in a linear fashion. There was a significant correlation of the hepatic excretion T1/2 to quantitative histopathology (R=0.949, p < 0.001). The hepatic excretion T1/2 increased as the severity of the histopathologic lesions of the liver increased. Hepatic extraction (HEF) and excretion of 99mTc-mebrofenin are good predictors of the severity of hepatocellular damage in toxic induced liver disease. This study helps validate the premise that HEF derived from deconvolutional analysis is a good predictor of the actual first pass hepatic extraction of 99mTc-mebrofenin.

Aniline Compounds↗
PubMedDate not supplied

Evaluation of plasma time-activity curves of technetium-99m-mebrofenin for measurement of hepatic function in dogs.

In this study, plasma time-activity curves of 99mTc-mebrofenin were used to quantify hepatic function in dogs before and after induction of hepatic damage using a hepatotoxic agent. Nine dogs were determined to be healthy on the basis of physical examination, laboratory data and hepatic imaging. Plasma samples were collected 1, 3, 5, 7, 9, 15, 20, 30, 40, 50, and 60 minutes following a peripheral venous injection of 111-222 MBq (3-6 mCi) of 99mTc-mebrofenin. The area under the plasma time-activity curve (AUC) was calculated using two different methods and compared to direct measurement of the hepatic extraction efficiency. First pass hepatic extraction efficiency of 99mTc-mebrofenin was calculated from differential equation analysis of a two-compartment model following mesenteric venous injection of the radiopharmaceutical. In 7 of the original 9 dogs and 2 additional healthy dogs, plasma clearance and hepatic extraction efficiency determination were repeated following induction of hepatic injury by thiacetarsamide (3 mg/kg IV twice daily for 1 day). In one additional dog, hepatic injury was induced using carbon tetrachloride (0.3 ml/kg IP). Plasma time-activity curves of 99mTc-mebrofenin had kinetics of a two compartment model. Area under the curve was highly correlated with hepatic extraction efficiency. The AUC integrated from 1-60 minutes (AUC60) had the best correlation with hepatic extraction efficiency (r2 = 0.978, p < 0.001). A formula for calculation of hepatic extraction efficiency was derived using linear regression analysis: hepatic extraction efficiency = 105.583 - 3.099 x 10(5) x AUC60. Plasma clearance of a peripheral venous injection of 99mTc-mebrofenin is a simple, non-invasive, convenient method to quantify hepatic function which can be performed without a gamma camera.

Algorithms↗
PubMed1975

Levamisole as a microfilaricidal agent in the control of canine dirofilariasis.

The effectiveness of levamisole hydrochloride as a microfilaricidal agent when used 3 weeks after thiacetarsamide sodium therapy for canine dirofilariasis, was studied in 6 experimental dogs and 20 clinical cases. The drug, when administered orally in gelatine capsules daily, cleared microfilariae from the circulation in the experimental dogs in 7 to 11 days. A dose rate of 10mg/kg appeared as effective as 15mg/kg. In the clinical group 70% of dogs had zero microfilarial counts after 4 to 8 doses at 10mg/kg daily. Vomiting, diarrhoea and inappetence were observed in some animals, but were not a significant problem. Elevations in plasma GPT and AP levels were recorded during the administration of levamisole in some dogs while GOT levels rose in 1 dog only. Urea and creatinine levels were unaffected in all dogs. The only haematological parameter affected was the eosinophil count which rose during levamisole administration. All levamisole-treated animals, were successfully commenced on daily DEC, as a prophylactic measure, while an anaphylactic-type reaction occurred when this drug was administered to 1 of the 2 control animals.

Alanine Transaminase↗