Disease relevance of meglumine

• Glucantime-resistant visceral leishmaniasis in immunocompromised patients [1].
• Quinolines 1, 2, 3, and 7 reduced by 80 to 90% the parasite burdens in the lesion, whereas N-methylglucamine antimoniate (Glucantime), administered by subcutaneous injections at 100 mg [28 mg Sb(V)] per kg of body weight daily, reduced the parasite burdens by 98% [2].
• Clinical resistance to pentavalent antimonials, in the form of pentostam (sodium stibogluconate) or glucantime (N-methylglucamine antimoniate), has long been recognized as a problem in Leishmaniasis [3].
• Two hundred twenty-six consecutive adult patients with cutaneous leishmaniasis in Colombia were treated with Glucantime and 81% were cured [4].
• In previous studies of the treatment of localized cutaneous leishmaniasis (LCL) we demonstrated that the therapeutic efficiency of immunotherapy (BCG plus promastigotes of Leishmania mexicana) is equal to that of chemotherapy (Glucantime), without causing the serious side-effects of the drug treatment [5].

High impact information on meglumine

• Glibenclamide reduced the rate of lesion growth in BALB/c mice infected with Leishmania (Leishmania) mexicana, the effect was dose dependent, and the highest dose proved more effective than glucantime [6].
• We report that amastigotes of Leishmania infantum cultured under axenic conditions were poorly susceptible to meglumine [Glucantime; an Sb(V)], unlike those growing inside THP-1 cells (50% inhibitory concentrations [IC50s], about 1.8 mg/ml and 22 microg/ml, respectively) [7].
• The effect of camptothecin, an inhibitor of topoisomerase, and additive-free meglumine antimoniate (Glucantime) on the stabilization of cleavable DNA-protein complexes associated with the inhibition of topoisomerase was assessed in the human promonocytic cell line U-937, promastigotes of L [8].
• Sinefungin was significantly suppressive against both L. donovani and L. braziliensis panamensis infections in hamsters when compared with meglumine antimonate (Glucantime) [9].
• The resistance to glucantime was reverted by buthionine sulfoximine (BSO) and chlorambucil (CLB); however, thiol analyses by HPLC of wild-type and GLU-R10 cell lines, in the presence or absence of the drug, showed no differences between these two cell lines [3].

Chemical compound and disease context of meglumine

• In this study, Glucantime was more effective than pentamidine for treatment of L. braziliensis cutaneous leishmaniasis in Peru based on parasitologic as well as clinical criteria [10].
• The effect of intravenous or subcutaneous administration of meglumine antimonate (Glucantime) in dogs with leishmaniasis. A randomized clinical trial [11].
• OBJECTIVE: Evaluating the efficacy of pentoxifylline plus glucantime in the treatment of cutaneous leishmaniasis [12].

Biological context of meglumine

• The resistant cell lines were partially characterized by their in vitro response to glucantime, the stability of resistance phenotype, cross resistance to a range of drugs, and also by the analysis of total DNA fragments generated by restriction endonucleases and blot hybridization [13].
• A gene amplification from a glucantime-resistant Leishmania (Viannia) guyanensis cell line was characterised in an attempt to understand the mechanism of metal resistance in this pathogenic species [14].
• The 50% effective dose (ED50) of pharmaceutical and additive-free formulations of Glucantime were determined based on the kinetics of the response of Leishmania Viannia to SbV in vitro [15].
• During GLUCANTIME-treatment the following adverse reactions could be observed: general weakness, reduced food intake up to anorexia, vomiting and diarrhoea [16].
• CONCLUSIONS: By itself, increased access to Glucantime is unlikely to increase usage of the drug and to reduce its frequent premature discontinuance unless public health planners accommodate the health and illness world views of local populations [17].

Anatomical context of meglumine

• Elimination of the parasite burden by glucantime therapy restored responsiveness of lymphocytes to parasite antigens [18].
• We also studied the capacity of CP-elicited peritoneal macrophages of C57Bl/6 mice cultured alone or in combination with Glucantime and/or lymphokine to eliminate intracellular L. donovani amastigotes [19].
• Glucantime inhibited the growth of Leishmania cultured in complex medium but did not affect parasite growth when added to cells cultured in defined or semi-defined media [20].
• A significant increase in alphabeta T cells was seen in glucantime-treated patients (62.4% +/-7.6), when compared to the untreated patients (55.7% +/-5.5) and controls (55.1% +/-9.6) [21].
• Our data represent evidence for the reversibility of the abnormal HLA-DR expression by keratinocytes in ACL after Glucantime therapy or spontaneous scar formation, demonstrating that this expression is restricted to the period of active lesions [22].

Associations of meglumine with other chemical compounds

• The T-500 strain exhibited a Mdr phenotype; it was also resistant to other unrelated drugs like vinblastine, adriamycin and the commonly used antimonial drugs pentostam and glucantime [23].
• Specific serum antibody levels in Leishmania infantum-infected dogs treated with a combination of glucantime and allopurinol were estimated by indirect immunofluorescence and Western blotting [24].
• RESULTS: The results indicated that treatment by intraperitoneal administration of 8Brguo (150 mg/kg once daily for 1 week and thereafter once weekly for 1 month) diluted in Tween-80 produces an effect similar to that of treatment with the classical antimonial drug, Glucantime, in Leishmania amazonensis-infected CBA/J mice [25].
• Drug reference control groups received five doses of 200 mg/kg pentavalent antimony (Glucantime) or three doses of free pentamidine (0.17 mg/kg or 2.28 mg/kg) [26].

Gene context of meglumine

• In contrast, glucantime therapy led to a Th2-type response in the control group with a lower level of IL-2 [27].
• However, a combination of garlic and glucantime treatment was more effective than either treatment alone, and resulted in a Th1-type response similar to that which developed with garlic treatment [27].
• Likewise, the pattern of immunoblot change after the patients were treated and apparently cured with meglumine antimoniate (Glucantime) was studied by evaluating sera pretreatment and 1 year posttreatment [28].
• AIM: To evaluate the efficacy of combined cryotherapy and intralesional meglumine antimoniate (MA) (Glucantime, Specia, Paris, France) for the treatment of CL [29].
• Immunopathology of American cutaneous leishmaniasis. Modulation of MHC class II gene products by keratinocytes before and after glucantime therapy [22].

Analytical, diagnostic and therapeutic context of meglumine

• Control groups consisted of untreated mice and mice treated with a pentavalent antimonial (Glucantime) [30].
• Patients were treated with conventional chemotherapy by using pentavalent antimonium salts (Glucantime) for 3 weeks [31].
• In mice, it was found that immunostimulation of animals prophylactically, therapeutically, or both enhanced the effects of the antimonial drug (Glucantime) administered more than 1 week after a challenge of BALB/c and C57BL/6 mice [32].
• Its efficacy by oral administration was approximately four to eight times that by intramuscular administration and four times that of the positive control drug Glucantime by intramuscular administration [33].
• After glucantime therapy, immunoblotting profiles with LCL sera were reduced both in intensity and in the range of antigens detected; a 104-kDa antigen was newly detected with post-treatment LCL sera [34].

References