Antimony compounds, pentavalent

In 1912, however, (201) it was discovered that espundia (American mucocutaneous leishmaniasis) can be cured by tartar emetic. It was soon learned that kala-a2ar (visceral leishmaniasis) and oriental sore (a cutaneous form of the disease occurring in the Middle East) also respond to antimonial therapy, especially when compounds of pentavalent antimony are employed. Treatment of leishmaniasis with the latter type of antimonials is safe and effective in over 90% of the cases (202). In 1918, it was demonstrated that tartar emetic is of value in the treatment of schistosomiasis (203). Pentavalent antimonials proved to be less effective. The introduction of antimony compounds for the treatment of parasitic diseases is undoubtedly one of the important milestones in the history of therapeutics (see Antiparasitic agents). 

Antimony compounds have been used to treat leishmaniasis ever since tartar emetic (antimony potassium tartrate) was discovered early in the 20th century to have efficacy against the mucocutaneous form of the disease. The cutaneous form has been treated with tartar emetic formulated in an ointment. Many side effects have been seen with this trivalent antimonial, some of which can be ascribed to the difficulty of obtaining pure antimony for its manufacture. These side effects include toxicity to the heart, Hver, and kidneys. Other promising trivalent antimonials have been abandoned in favor of pentavalent antimonials with lower toxicity. 

Pentavalent antimony compounds, 20 56 Pentavalent plutonium cations, 19 692 Pentavalent tungsten, 25 386 Pentavalent vanadium aqueous, 25 533... 

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. 

A. Liposomal amphotericin B was approved by the US. Food and Drug Administration to treat visceral leishmaniasis. Pentavalent antimony compounds, pentamidine, amphotericin B, and aminosi-dine (paromomycin) have all been demonstrated efficacious here. The liposomal amphotericin appears to be better taken up by the reticuloendothelial system, where the parasite resides, and partitions less in the kidney, where amphotericin B traditionally manifests its toxicity. In addition to being better tolerated by patients, it has proved to be very effective in India, where resistance to antimony drugs is widespread. This patient appears to have acquired his infection there, where many infected patients develop darkening of the skin, hence the name kala-azar, or black sickness. Albendazole, an anthelmintic, has no role here. Atovaquone, a naphthoquinone, is used to treat malaria, babesiosis, and pneumocystosis. Pyrimethamine-sulfadoxine is used to treat malaria and toxoplasmosis. Proguanil inhibits the dihydrofolate reductase of malaria parasites and is used in combination with atovaquone. 

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 . 

Antimony, which is considered a nonessential element, is comparable in its toxicological behavior to arsenic and bismuth. In analogy to arsenic, trivalent antimony compounds generally are more toxic than the pentavalent compounds. Poisoning with antimony and its compounds can result from acute and chronic exposure, especially from exposure to... 

Stibocaptate is a trivalent antimony compound, whose toxic effects, especially its acute adverse effects, are similar to those of the pentavalent compounds. 

Normally, antimony is absorbed slowly when ingested or administered orally. Many antimony compounds are gastrointestinal irritants. The emetic antimony potassium tartrate is easily absorbed and, within 24 h, 50% is excreted in the urine (hamsters). Antimony can concentrate in lung tissue, the thyroid gland, the adrenal glands, the kidneys, and the liver. The trivalent compounds of antimony concentrate in the red blood cells and liver and the pentavalent compounds concentrate in the blood plasma. Both forms are excreted in feces and urine, but generally. 

This test identifies the substance to be examined as a salt of antimony(III), Sb +, or antimony(V), Sb +. Antimony(III) and antimony(V) were formerly used in the oral treatment of intestinal worms and topically in the treatment of infections of protozoan parasites in the skin. But since especially tetrava-lent antimony is poisonous, they have generally been replaced by less toxic alternatives. At present, there are no monographs of antimony compounds in the European Pharmacopoeia. Antimony forms both tetra- and pentavalent ions, but the pentavalent is mainly found in oxides containing the antimonate ion, Sb04. Antimony(III), on the other hand, can be found as the free dissociated ion, Sb +, but, as also for example bismuth, since it reacts with water at neutral pH, forming antimonate. 

The interest in the elaboration of oxirans to cyclic carbonates is exemplified by three papers which have appeared this year. The conversion of (106) -> (107) is well known using elevated temperatures and pressures. Various catalysts have been employed and the range has been extended to include pentavalent organo-antimony compounds. " Good yields under much milder conditions have been achieved using a metal halide and a Lewis-base catalyst. The cyclic carbonate... 

Sodium stibogluconate is a pentavalent antimony compound and the antimony is determined as for the total antimony in sodium antimonylgluconate. 

Bismuth forms trivalent and pentavalent compounds. The trivalent compounds are more common. Many of its chemical properties are similar to other elements in its group namely, arsenic and antimony. 

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