Meglumine antimonate

The conditions described above were used by Figad re, Alami and coworkers" to prepare analogues of meglumine antimonate (Glucantime ), a product used in chemotherapy, from chloroenynes or chlorodienes (Scheme 21). The reaction was further extended to various chloroenynes (Scheme 22). 

Visceral (L donovani, L chagasi, L infantum) Sodium stibogluconate, 20 mg/kg/d IV or IM for 28 days Meglumine antimonate... 

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

Antimony is excreted in the urine. Peak concentrations are seen at about 1-2 hours after an intramuscular injection of meglumine antimonate. Serum concentrations faU to about 10% of peak concentrations after about 8 hours. There is some accumulation of antimony during continued treatment. On a weight for weight basis children require a higher dose and tolerate antimony better. Toxicity is more likely in patients with impaired renal function, as would be expected for a drug that is mainly excreted in the urine. 

Common adverse effects of meglumine antimonate are anorexia, nausea, vomiting, malaise, myalgia, headache, and lethargy. Muscle, bone, and joint pains have been described (SEDA-12, 710) (SEDA-13, 838) (20). Cardiac toxicity and electrocardiographic changes are dose-related. The general condition of the patient with visceral leishmaniasis probably plays a crucial role in these and other adverse effects. Malnutrition is common, the immune status often severely impaired, and patients are susceptible to intercurrent infections (SEDA-12, 710). 

Berbamine was evaluated in BALB/c mice infected with Letshmartia amazonensis (IFLA/BR/67/PH8 or MHOM/GF/84/CAY-H-142) or L. venezuelensis (VE/74/PM-H3). The treatments were initiated one day after parasitic infection at an alkaloid concentration of 100 mg/kg/day for fourteen days, and the reference compound (meglumine antimonate) at 200 mg/kg/day. Berbamine was found to be less potent than meglumine antimonate against L. amazonensis, and the alkaloid did not show significant activity against L. venezuelensis [334]. 

Berberine and 8-cyanodihydroberberine were found to exhibit significant activity (> 50% suppression of lesion size) against the lesions of Leishmania braziliensis panamensis in golden hamsters. Tetrahydroberberine (canadine) was more potent but less toxic than berberine against Leishmania donovani, but not as potent as meglumine antimonate, a standard drug utilized in the therapy of leishmaniasis [209]. 

Torrus D, Massa B, Boix V, et al. Meglumine antimonate-induced pancreatitis. Am J Gastroenterol 1996 91 820-821 [Letter]. 

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