Antimony sodium stibogluconate

Leishmaniasis is successfully treated with the pentavalent antimonial, sodium stibogluconate 6.21). Given intramuscularly, it has displaced all earlier forms of antimony treatment. Intramuscular pentamidine 10.27) provides an alternative treatment. 

Valproic acid/salts Losartan Meglumine antimoniate Piroxicam Procainamide Salicylates Sodium stibogluconate Zalcitabine... 

Sodium stibogluconate is a pentavalent antimo-nial compound. It is a prodrug as the pentavalent an-timonial has to be reduced to a divalent antimony compound. Sodium stibogluconate is used to deal leishmaniasis and is only available for adminisda-tion by injection. It is excreted in the urine. In general it is tolerated fairly well. Adverse effects include pain at the injection site and gasdointestinal complaints. Cardiac arrhythmias can occur and renal and hepatic function should be monitored. 

No pentavalent antimonial is licensed for use, but sodium stibogluconate is available from the Parasitic Disease Drug Service of the Centers for Disease Control (CDC) for treatment of leishmaniasis. While the pentavalent antimony compounds can be given intravenously or intramuscularly, local infiltration of the lesion in cutaneous leishmaniasis is highly effective. Because of the lower toxicity of liposomal amphotericin B, this drug is considered a first-line choice for vis-cerotropic leishmaniasis rather than the antimonials. 

Pentamidine is an alternative to sodium stibogluconate in the treatment of visceral leishmaniasis, with similar efficacy, although resistance has been reported. The drug has been successful in some cases that have failed therapy with antimonials. The dosage is 2-4 mg/kg intramuscularly daily or every other day for up to 15 doses, and a second course may be necessary. Pentamidine has also shown success against cutaneous leishmaniasis, but it is not routinely used for this purpose. 

C.N. Chunge, et al., Visceral leishmaniasis unresponsive to antimonial drugs Successful treatment using a combination of sodium stibogluconate plus allopurinol. Trans R. Soc. Trop. Med. Hyg. 79 715-718, 1985. 

Meglumine antimonate is a pentavalent antimony compound, similar to sodium stibogluconate. 

Sodium stibogluconate (Pentostam) is an organic pentavalent antimony compound it may cause anorexia, vomiting, coughing and substemal pain. Used in mucocutaneous leishmaniasis, it may lead to severe irrflammation around pharyngeal or tracheal lesions which may require corticosteroid administration to control. Meglumine antimoniate is similar. 

The pentavalent antimony compound, sodium stibogluconate, is used as an anti-parasitic drug. Treatment of Leishmania braziliensis has been reported to be successful with sodium stibogluconate whereas in Leishmania mexicana, the response was lower and the preferred drug for this disease was ketoconazole . 

Meglumine antimoniate is a pentavalent antimonial chemically similar to sodium stibogluconate and is considered to have similar efficacy and toxicity. Meglutamine antimoniate solution contains pentavalent antimony 8.5% and stibogluconate 10%. 

Sodium stibogluconate is a pentavalent antimonial that contains pentavalent antimony 10%. 

In a prospective, open trial, conventional treatment with sodium stibogluconate (n = 69) was compared with meglumine antimoniate (n = 58) for cutaneous Leishmania braziliensis (13). The trial was too small and of too short a duration to compare efficacy rehably, but... 

There has been a further comparison of meglumine antimoniate (n = 47) and sodium stibogluconate (n = 64) (14). The trial was too small to examine the efficacy of the two drugs, but there were more adverse events with sodium stibogluconate, with a greater proportion with raised transaminase and amylase activities. There were no differences in electrocardiographic abnormalities between the two groups. 

Saldanha AC, Romero GA, Merchan-Hamann E, Magalhaes AV, Macedo V de O. Estudo comparativo entre estibogluconato de sodio BP 88R e antimoniato de meglumina no tratamento da leishmaniose cutanea I. Eficacia e seguranca. [A comparative study between sodium stibogluconate BP 88R and meglumine antimoniate in the treatment of cutaneous leishmaniasis. I. The efficacy and safety.] Rev Soc Bras Med Trop 1999 32(4) 383-7. 

The pentavalent sodium stibogluconate (12b) is obtained by treating an aqueous solution of gluconic acid (47) with moist Sb205 the resulting mixture is neutralised with sodium hydroxide to get sodium antimony (V) gluconate (12b) with antimony content ranging form 28-29.5% [45]. 

The introduction of tartar emetic (1) in 1912 for the treatment of mucocutaneous leishmaniasis heralded a new era in the treatment of the disease, which was followed by the investigation of a number of other antimonials for clinical efficacy in leishmaniasis. This led to the discovery of a number of fivevalent antimony compounds, that have laboratory and clinical efficacy and are better tolerated than tartar emetic. These included sodium stibogluconate (2), meglumine antimoniate (3), derivatives of stibanilic acid (stibamine, 4), stibacetin (5), ethyl stibamine (a mixture of 4, 5, antimonic acid and Et2NH in a molar ratio of 1 2 1 3 with 41-44% of fivevalent antimony content) and urea stibamine (6) have been used to treat kala-azar, cutaneous and mucocutaneous leishmaniasis in man. 

All three forms of leishmaniasis are treated with stibogluconate sodium (antimony sodium gluconate-pentavalent antimony, Pentostam), which is obtained from the CDC. In adults, both... 

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