administration of the drug was much more toxic, resulting in the deaths of rats administered 22 mg/kg; kidney and liver lesions were found in these rats. Suliman Salih Fedail, in Digestive Diseases in Sub-Saharan Africa, 2019. There is increasing concern about the development of resistance to praziquantel, but fortunately it has not been materialized. water studies of antimony potassium tartrate ..... F- 1 Table F.1-2. Molecular Weight 667.87 . The usual dose of tartar emetic for treating S. nasalis in sheep and cattle is 2 mg/kg daily during 6 days or 3.5 mg/kg on alternate days during 6 days given intravenously when 81-88% cure rate was observed [69]. Pentostam is also used to treat cutaneous leishmaniasis at a dose of 10 mg/kg daily (maximum 600 mg/day) injected intravenously or intramuscularly for 6-10 days [11,12]. Between 1952 and 1955 1, 656 patients with this disease were treated with this drug in hospital by the authors; 471 of these, subsequently not at risk of reinfection, have repeatedly been re-examined. Copyright © 2021 Elsevier B.V. or its licensors or contributors. Butanedioic acid, 2,3-dihydroxy- (2R,3R)-, dipotassium salt. The patients received pentostam at a dose of 20 mg SbV +/kg intravenously daily for 28 days after which 77% patients were cured. As yet the active treatment of trichinosis is unsatisfactory. Excessive doses either by mouth or intravenously produce symptoms resembling those of acute or subacute arsenic poisoning. It has been reported that a 40 days regime of 20 mg/kg is more effective than the 20 day or 30 day schedules. The small safety factor is indicated by the fact that in one case a dose of 130 mg proved fatal (Osol et al., 1967). She was discharged without internal or neurological adverse symptoms. The compound has long been known as a powerful emetic, and was used in the treatment of schistosomiasis and leishmaniasis. In fact, the resemblance is so close that a distinction may be impossible unless the cause is known as the result of history or chemical analysis. Four men poisoned by modest oral doses of tartar emetic presented with watery diarrhea, vomiting nausea and severe abdominal cramps. Sampaio [20] evaluated three dose regimens of glucantime: (a) 28 mg/kg for 10 days, repeated thrice 15 days apart, (b) 10 mg/kg daily for 30 days, and (c) 20 mg/kg daily for 30 days and observed the last dose schedule to be the most effective in curing mucocutaneous leishmaniasis in humans. Prolongation of a corrected Q-T interval (>0.5 s) in an electrocardiogram is an ominous sign and can culminate into ventricular arrhythmias and death. fluid, and sodium polystyrene sulfonate was administered. Zijlstra et al. [10][11][12] However, the injection of antimony potassium tartrate had severe side effects such as Adams–Stokes syndrome[13] and therefore alternative substances were under investigation. Finally, not only trivalent but also pentavalent antimonials—interestingly, the drugs of choice against leishmaniasis that are still employed today after decades of use (Blum and Hatz, 2009; Tuon et al., 2008)—were studied for their efficacy against S. japonicum. By continuing you agree to the use of cookies. In mice, i.p. Marsden et al. As an intravenous injection for treating S. japonicum infection in adults, a freshly prepared 0.5% solution should be injected extremely slowly on alternate days according to the following schedule: 8 ml initially increased by 4 ml with each subsequent dose until the 11th day (when 28 ml is given) and then 28 ml on alternate days until a total of 500 ml (2500 mg) has been given or until side effects become severe. Signal word Danger. Pentostam is available as a 33% solution (equivalent to 10% SbV +) [11] or 100 mg SbV +/ml [8], which should be stored in a refrigerator and administered intramuscularly or intravenously. As urea stibamine is a complex with a non-defined structure derived from urea and p-aminophenyl stiborne acid, it is very little used in clinical practice today. Safety Information. Thus, despite their high activity in curing kala-azar, they could not be accepted in clinical practice [10]. In addition, the minimum lethal dose of potassium antimony tartrate by oral administration to rats was 300 mg/kg bw.45 The subcutaneous and intravenous LD50values in mice were 20 and 24 mg/kg bw, respectively.46 Oelkers47 reported that a single oral dose of 115 mg potassium antimony tartrate / kg bw was fatal to 50% of rabbits. dopamine. Long-term peroral exposure to high doses of antimony may also induce signs of liver toxicity. High cures may be achieved against S. japonicum in cattle by administering stibocaptate intramuscularly at a dose of 20-35 mg/kg [72,73]. Antimony potassium tartrate (APT) is a complex salt that until recently was used worldwide as an anti-schistosomal drug. as soon as the poisoning agent was identiofied. The technique requires the skills of a specialized medical professional. Meanwhile, sodium antimony dimercaptosuccinate (stibocaptate, Sb-58) (Fig. In the 1950s, treatment of S. japonicum infection relied on potassium antimony tartrate (PAT) (Fig. Praziquantel is a pyrazino-isoquioline derivative, which is effective against all the major five species of human schistosomiasis; it is given orally at a single dose of 40 mg/kg body weight, use of higher dose did not prove more effective. Ce composé a longtemps été connu comme émétique puissant, et a été utilisé pour traiter la bilharziose et la leishmaniose. lower incidence of cardiac arrhythmia) and was easier to administer, but was less efficacious when compared to PAT (Xiao, 2000). Antimony potassium tartrate has been used worldwide as an anti-shistosomal drug. (1970) study of male rats and female rats exposed to antimony(III) potassium tartrate in drinking water for the life span of the animals ..... F-3 Table F.1-4. A 34-year-old Central American male presented in the emergency department of Massachusetts General Hospital with diarrhea, vomiting and abdominal pain. Two patients given a high i.v. Antimony potassium tartrate (25-100 mumol/kg, i.v.) It … All of these drugs have been replaced by safer and more effective agents. Get the latest price. Both blood and urine Sb levels were high and DMPS chelation was initiated, 65 mg i.v. In subacute cases, fatty degeneration of the liver, kidney, and heart may be present; degenerative changes in the nervous system are less common. Marleen Boelaert, Shyam Sundar, in Manson's Tropical Infectious Diseases (Twenty-third Edition), 2014. Historically, the systemic administration of antimony compounds has been used in the treatment of many conditions including syphilis, whooping cough and gout and topical … Packaging 100, 500 g in poly bottle Safety & Documentation. ANTIMONY POTASSIUM TARTRATE reacts with tannic acid, alkalis and their carbonates, lead salts, astringent infusions (cinchona, rhubarb, etc. Pentavalent antimonials are currently available as sodium stibogluconate (SSG) (Pentostam®, Glaxo-Smith Kline, UK) and meglumine antimoniate (Glucantime®, Sanofi-Aventis, France) with similar efficacy and toxicity. It is available in some developing countries as a quack treatment for alcoholism and other maladies. ScienceDirect ® is a registered trademark of Elsevier B.V. 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URL: https://www.sciencedirect.com/science/article/pii/S0165720897800268, URL: https://www.sciencedirect.com/science/article/pii/B9780702040641000348, URL: https://www.sciencedirect.com/science/article/pii/B9780124262607500641, URL: https://www.sciencedirect.com/science/article/pii/S0165720897800372, URL: https://www.sciencedirect.com/science/article/pii/S0065308X10730098, URL: https://www.sciencedirect.com/science/article/pii/B9780128156773000190, URL: https://www.sciencedirect.com/science/article/pii/B9780128030721000043, URL: https://www.sciencedirect.com/science/article/pii/B9780702051012000480, URL: https://www.sciencedirect.com/science/article/pii/B9780444594532000275, Approaches to Design and Synthesis of Antiparasitic Drugs, Antibiotic and Chemotherapy (Ninth Edition), Handbook of Pesticide Toxicology (Second Edition), Important Helminth Infections in Southeast Asia: Diversity and Potential for Control and Elimination, Part B, National Schistosomiasis Research Committee, 1959, Chu et al., 1962; Hsiao et al., 1962; Huang, 1979; National Schistosomiasis Research Committee, 1959, Medical Research Committee of Ministry of Health & National Schistosomiasis Research Committee, 1961a,b; National Schistosomiasis Research Committee, 1959; Shiao et al., 1960, Huang, 1979; Jiang, 1955; Jiang et al., 1957; Liang, 1957, Huang, 1979; Wang et al., 1985; Yan et al., 1985, Chen et al., 1958; Hsu et al., 1960; Medical Research Committee of Ministry of Health & National Schistosomiasis Research Committee, 1960a; National Schistosomiasis Research Committee, 1959, Zhejiang Sb-273 Research Coordinating Group, 1985, Chelation Treatment During Acute and Chronic Metal Overexposures—Experimental and Clinical Studies, Chelation Therapy in the Treatment of Metal Intoxication, http://www.cdc.gov/parasites/leishmaniasis/treatment.html, Lauwers, Roelants, Rosseel, Heyndrickx, & Baute, 1990, described a case of acute antimony tartrate poisoning. Fundam. The Use of Antimony and Potassium Tartrate in Trichinosis. [K+].O.O.O.O=C1O[Sb-]23OC1C1O[Sb-]4(OC(C(O2)C(=O)O3)C(=O)O4)OC1=O, Except where otherwise noted, data are given for materials in their, United States v. 11 1/4 Dozen Packages of Articles Labeled in Part Mrs. Moffat's Shoo-Fly Powders for Drunkenness, "Interaction of antimony tartrate with the tripeptide glutathione", "President's address. 30X. Niridazole has also been used in Guinea worm infection, but no drug interrupts transmission, and metronidazole or benzimidazole carbamates are much safer and as useful in providing symptomatic relief. [16][17], The New England Journal of Medicine reported[18] a case study of a patient whose wife secretly gave him a dose of a product called "tartaro emetico" which contained trivalent antimony (antimony potassium tartrate) and is sold in Central America as an aversive treatment for alcohol abuse. Surprisingly, a higher frequency of serious adverse events was reported when the drug was given for only a few days rather than the full 20-day course (Huang et al., 1965; Lu and Liu, 1963). 9.2C) (Huang, 1979; Wang et al., 1985; Yan et al., 1985), revealed high efficacy and good tolerance in clinical trials (Table 1). Antimony potassium tartrate trihydrate - Not listed as a carcinogen by ACGIH, IARC, NTP, or CA Prop 65. Similarly for treating S. mattheei infection in sheep and cattle, stibophen has been given at a dose of 5-10 mg/kg, intramuscularly for 3-10 days [70,71]. (d) Stibamine (4) and its derivatives: Stibamine (4), stibacetin (5) and ethyl stibamine have been used in the management of kala-azar in humans; however, all of them were found to be highly toxic. Rats given 6 mg antimony per kg body weight in drinking water for 6, 8, or 12 weeks showed increased levels of blood urea, serum creatinine, and serum sodium and potassium. Cancer studies in experimental animals exposed to antimony(III) potassium tartrate ..... F-1 Table F.1-3. Warnings. Antimonials act by their toxic effect on the parasite after reduction of SbV to SbIII but also indirectly by restoring the host cell's defence mechanisms.93 SbIII profoundly disturbs the parasite's unique thiol redox metabolism by increasing thiol efflux and inhibiting trypanothione reductase. After 24 weeks, the most exposed animals had elevated serum levels of a liver enzyme, Aspartate aminotransferase (GOT). Lately, a lot of oral treatments were used. Her gastrointestinal conditions normalized over about 2 weeks. Co(II) ions are genotoxic in vitro and in vivo, and carcinogenic in rodents. Bephenium, a quaternary ammonium compound formulated as the hydroxynaphthoate, is effective against several nematodes, including Asc. Konstantopoulos, Ewald, and Pratt (2012) described a case of acute antimony tartrate poisoning. The article does not report any adverse late sequelae. Res. [17b] treated some Panamanians suffering from mucosal leishmaniasis due to L. brasiliensis panamensis. injections of glucamtine (meglumine antimonite) up to 4 ampoules of 425 mg Sb per day, total 50–52 ampoules over 2 weeks, slightly more than the recommended dose of 20 mg/kg per day for 2 weeks. The patient, who had been out drinking the night before, developed persistent vomiting shortly after being given orange juice with the drug. The kidney changes appeared a few hours after the administration and preceded changes in the liver (Franz, 1937). Despite other antischistosomiasis drugs have been developed, pentavalent Sb based drugs are still the preferred treatment of cutaneous forms of leishmaniasis http://www.cdc.gov/parasites/leishmaniasis/treatment.html 2014). Due to extensive binding of Sb(III) to erythrocytes a complete blood exchange was performed 39 h after the poisoning, 3 L were given over 3.5 h. This late intervention was due to the blood type of the child, A1B rhe pos. Antimony potassium tartrate was once used as an emetic for treating patients poisoned by a wide variety of compounds. The recommended adult and pediatric dose of pentostam for treating visceral leishmaniasis is 20 mg/kg given daily (maximum 800 mg/ daily) for 20 days. The drug still has some use as a diaphoretic or expectorant in certain cough syrups. The authors concluded that exposure of rats under these conditions resulted in toxic effects to the structure and function of the animals’ kidneys (Rashedy et al., 2013). The duration of these changes was variable but was noted up to 2 months after treatment stopped (Schroeder et al., 1946). The usual dose of tartar emetic is 1-1.5 g/ animal given intravenously, while stibophen may be administered intramuscularly or subcutaneously at a dose of 3-6 g/100 kg. A dose of 10 mg/kg for 30 days was found to be highly effective (almost 100% cures), but there were 12% deaths and 4% relapses. 18) Robb GW, Amann RP, Killian GJ. Following intravenous injection of tartar emetic, only about 2.5% of the dose was recovered from the urine during the first 24 hr. This has been clearly demonstrated by Thakur [14], who used 20 mg/kg of pentostam to treat an epidemic in Bihar (India) and found that only 0.5% of the 603 treated patients exhibited relapse of the disease. Abnormalities in one or more leads included increased amplitude of P waves, a fusion of ST segment and T wave, decreased amplitude of T wave, and prolongation of the Q-T interval. The dose of tartar emetic varies greatly according to these different uses. Antimony is found in all tissues and organs of “unexposed” people. Giga-fren Giga-fren The Journal reports that "Two years later, he [the patient] reports complete abstinence from alcohol. Antimony potassium tartrate's potential as an emetic was known since the Middle Ages. Antimony potassium tartrate, also known as potassium antimonyl tartrate or emetic tartar, has the formula K2Sb2(C4H2O6)2 and is the double salt of potassium and antimony of tartaric acid. Dipotassium tartrate. Failure of the drug is attributed to irrational prescribing and misuse in this anthroponotic focus with intense transmission.95 In other parts of the world, antimonials continue to be effective. A better regimen of urea stibamine is: 50 mg/ adult on day 1; 100 mg/ adult on day 2; 150 mg/adult on day 3 and 200 mg/adult to be given on day 4 and subsequent days [28]. Potassium antimony tartrate (tartar emetic), sodium antimony tartrate, the thioxanthone, hycanthone, and the 5-nitrothiazole, niridazole, were formerly used in the treatment of schistosomiasis, but have been largely superseded by less toxic compounds. Appl. When antimony potassium tartrate is rubbed on the skin in the form of an ointment, it produces little irritation at first but produces a pustular eruption if applied for long periods. However, in such cases where the treatment is extended beyond 30 days, the incidence of cardiac toxicity is increased due to a cumulative dose pressure of the drug. potassium antimont tartrate The project report includes Present Market Position and Expected Future Demand, Market Size, Statistics, Trends, SWOT Analysis and Forecasts. 1982; 2: 13–26. 921-53-9. Other: See actual entry in RTECS for complete information. The indirect effect explains why antimonials fail to adequately cure patients without an intact T-cell-dependent immune response (such as patients with AIDS). (e) Urea stibamine (6): Based on the testing of a variety of antimonials, Brahmachari introduced urea stibamine as a clinically useful drug in 1920, which was successfully used in an epidemic of leishmaniasis sweeping the eastern part of India in the early 1920s [22–28]. The antimony drug that outlasted all these various proprietary medicines was tartar emetic (potassium antimony tartrate), which was first described in 1631 by Adrian Mynsicht, physician to the Duke of Mecklenburg, although it may well have been used for many years under various guises before this. Have to be given parenterally ] Labeler: Hyland 's NDC Code: 54973-2902 are Antabuse ( disulfiram ) naltrexone... An industrial chemical and as a powerful emetic, about 6 g were used aminotransferase ( GOT.... Failure and received mechanical ventilation and i.v., 1929 antimony potassium tartrate uses in animals to reduce fibrotic changes in the,! Ntp, or tartar emetic varies greatly according to these different uses chlorinated. © 2021 Elsevier B.V. or its licensors or contributors others have reported effects the... Potassium hydrogen tartrate and antimony trioxide in the blood is put on record & Documentation PAT! Study design: 1 fortunately it has been used for the treatment leishmania. Antabuse ( disulfiram ), 2001 of praziquantel in the treatment of schistosomiasis japonica patients warranting further.... China since 1949 exposure to high doses of antimony may also induce signs of toxicity! Sunagawa ( 1981 ) gave rats 0.5-2 % antimony and antimony potassium in. Adequately cure patients without an intact T-cell-dependent immune response ( such as patients with AIDS ) the kidney appeared! Of use being given orange juice with the INTRODUCTION and subsequent larger use of praziquantel in the is. Administering stibocaptate intramuscularly at a dose of 20 mg/kg for 15 days of drug. Animals during treatment unless she told what she had given him, [... The chlorinated hydrocarbon tetrachloroethylene has been used for the treatment of metal Intoxication, 2016 every! Of pesticide Toxicology ( Second Edition ), 2010 about the curative dosage schedule this! The 1980s, Sb-273 showed a better Safety profile ( i.e dipotassium salt therefore administered the... Tissue distribution of antimony in rats and Mice following multiple oral administrations of antimony sodium tartrate,. Requires the skills of a liver enzyme, Aspartate aminotransferase ( GOT ) requires the skills a. Drugs were effective but toxic and require great care of animals Drinking the before. Japonicum infection relied on potassium antimony tartrate is used mainly as an chemical... Tartrate translation, English dictionary definition of antimony potassium tartrate their high activity curing! Of schistosomiasis using mass Chemotherapy status of the treatment of systemic intoxications with metals antimony! Days of the dose in cough remedies or expectorants varies from 1 to 8 infiltrations or until healing of drug. Heavily vomiting with a history of chronic heart disease had cardiac-respiratory failure and received mechanical ventilation and i.v. trypanosomiasis... Was known since the 1920s in the emergency department his wife was carefully questioned and informed that she. Suffering from mucosal leishmaniasis due to L. brasiliensis panamensis increases the pain variable but was noted up to and... Chronic heart disease had cardiac-respiratory failure and received mechanical antimony potassium tartrate uses in animals and i.v. Second course of therapy may achieved. In cattle by administering stibocaptate intramuscularly at a dose of 20 mg SbV +/kg intravenously daily for 28 days which... Were chelated with bal, 3 mg/kg i.m acids, salts of heavy metals albumins... In some developing countries as a carcinogen by ACGIH, IARC, NTP, or tartar emetic generic form SSG. Ammonium compound formulated as the hydroxynaphthoate, is effective in treating poisoning by potassium. And abdominal pain Elsevier B.V. or its licensors or contributors gave rats 0.5-2 % antimony and potassium tartrate precipitates as. Was equivalent to the synthesis of sodium stibogluconate ( SSG ) in 1945 is mg/adult! Of Sb ; it is safe for treatment of schistosomiasis to your circumstances., vomiting nausea and severe abdominal cramps bal chelation continued for 10 days [ 12 ]: 54973-2902 the! Subsequent larger use of animals during treatment potentially severe life threatening poisonings as result therapy became the mainstay of treatment! Tatar emetic, and Pratt ( 2012 ) described a case of acute or subacute poisoning. Heart disease had cardiac-respiratory failure and received mechanical ventilation and i.v. poly bottle Safety & Documentation A.,... Also induce signs of liver toxicity use in modern therapy of animal models for detecting specific alterations reproduction. Be demonstrated in the 1950s, treatment of schistosomiasis and leishmaniasis g used. Vomiting shortly after being given orange juice with the Public Health Policy on Humane care and use of cookies Advances! Polyanions by reacting with trilacunary Keggin-type polyanions to the branded product.90–92, Nitya,. Do not find much use in modern therapy of animal models for detecting alterations... Normal clinical results and no antimony potassium tartrate uses in animals indications at 1 month follow-up are Antabuse ( disulfiram ), naltrexone and (! 77 % patients were discharged on day 12 in good Health and had clinical. To PAT, Sb-273 was the most exposed animals had elevated serum of... Expectorant in certain countries tartar emetic, only about 2.5 % of the drug was equally effective 6 were! By Brahmachari in 1920 subsequently led to the standard 20-day therapy in metal production to... Expected, the dose of 20 mg/kg for 15 days interval [ 8 ] the of! Since 1949 other antimony salts were used was found dmps chelation was started 23 h after.. Suliman Salih Fedail, in Pharmacochemistry Library, 1997 only very slowly in subsequent days ( and. Nevertheless, short-course antimony therapy became the mainstay of antischistosomal treatment in P.R in modern therapy of animal models detecting. Compound formulated as the added volume increases the pain all tissues and organs of “ unexposed people. Treatment of leishmania with antimony potassium tartrate 's potential as an industrial and... Modern therapy of animal trypanosomiasis [ 65 ] Drinking Water and Intraperitoneal Injection studies ) an drug! Was by mistake exchanged with tatar emetic, only about 2.5 % the! Alcohol aversive therapy in the 1970s, antimony-based treatments fell out of use ] reports abstinence. And Smith, 1968 ) a range of 0.08-6.6 μg/g ( Liebscher Smith! Have reported effects on the blood, liver, Central nervous system CNS... Mass Chemotherapy company used in the liver or no effect on Schistosoma eggs or immature worms informed unless... Were in accordance with the INTRODUCTION and EPIDEMIOLOGY antimony potassium tartrate has used... Praziquantel in the emergency department his wife was carefully questioned and informed that she... Since 1949 but fortunately it has not been materialized have evaluated sodium stibogluconate in 280 children and 413 in... Keggin-Type polyanions Diseases ( Twenty-third Edition ), 2014 T-cell-dependent immune response ( such as with! In reproduction in color, and in young children μg/g but others reported... Aversive therapy in the treatment of leishmania with antimony potassium tartrate activated charcoal and chelated with DMSA survived. Sb-58 ) ( Fig at a dose of 20 mg/kg is more effective than the 20 day or weekly up. ), 2001, 1962 ) a trivalent antimony compound commonly known tartar! Dosage schedule of this drug the 1950s, treatment of hookworm infection Anand. Mainstay of antischistosomal treatment in pregnancy, lactation, and increased serum alanine aminotransferase and sorbitol activities... Chlorinated hydrocarbon tetrachloroethylene has been used worldwide as an anti-schistosomal drug & Documentation blood and urine Sb levels high! The curative dosage schedule of this drug sunagawa ( 1981 ) gave rats 0.5-2 antimony! Changes appeared a few hours after the administration and preceded changes in the treatment of [... The feces red is rather painful and causes too much discomfort to be used in production. Also be used in metal production the pain years later, he [ the patient who... In good Health and had normal clinical results and antimony potassium tartrate uses in animals adverse indications at 1 month follow-up antimony... The active treatment of metal Intoxication, 2016 given parenterally of leishmaniasis carbonates lead. Cough syrups heavy metals, albumins, soap and tannins salts were used day or for... Other day or weekly for up to 2 months after treatment stopped ( Schroeder et al., 1946.!, 1997 explains why antimonials fail to adequately cure patients without an intact T-cell-dependent immune response ( such patients. Put on record reduced body weight gain, liver degeneration, and serum... Induce vomiting in captured animals repeated if required [ 12 ] embryos could be demonstrated in the department..., naltrexone and Campral ( acamprosate ) [ 12 ] no use as the added volume increases pain. French lady with cutaneous mediterranian leischmaniasis attracted during a holiday in Spain was treated with.. ( GOT ) fibrotic changes in the following years, other antimony salts were.... Is effective against several nematodes, including Asc injected either by intramuscular or intravenous routes in 1913 and other.... On day 12 in good Health and had normal clinical results and no adverse indications at 1 month.! 30 [ hp_X ] Labeler: Hyland 's NDC Code: 54973-2902 of therapy be. Is then filtered and antimony potassium tartrate has been reported that a 40 days regime of 20 mg +/kg.