Pentamidine isethionate salt

BACKGROUND: ;Cutaneous leishmaniasis is an endemic disease in Surinam. The disease was treated until the early 1970s with pentavalent antimony. Pentamidine mesylate was introduced by Niemel in 1973 for the treatment of cutaneous leishmaniasis in Surinam.;MATERIALS AND METHODS: ;In this retrospective study, we evaluate the results of treatment with pentamidine mesylate in 235 patients and with pentamidine isethionate in 80 patients.;RESULTS: ;In the pentamidine mesylate- and pentamidine isethionate-treated groups, a cure rate (healing without relapse) of nearly 90% was found. Relapses were seen in approximately 10% of patients in both groups. Minor side-effects, such as pain at the injection site, bitter taste, and nausea, were seen with both drugs in about 65% of patients. Complaints of the respiratory tract were seen in less than 10% of patients in the pentamidine isethionate-treated group, but were uncommon in the pentamidine mesylate-treated group.;CONCLUSIONS: ;Pentamidine mesylate and isethionate have similar safety, efficacy, and side-effect profiles in the treatment of cutaneous leishmaniasis in Surinam.

Iodopentamidine isethionate was heated for 70 min with [I-123]- or [I-125]-sodium iodide and ammonium sulphate in the absence of solvent at 140 degrees C. The product, [I-123]- or [I-125]-iodopentamidine isethionate, was purified by ion exchange chromatography. It was stable at room temperature in aqueous solution over several days, in human blood in vitro for at least 24 h (showing no binding to either cells or proteins), in urine over at least 15 h, and during nebulization in both ultrasonic and jet nebulizers.

The chemistry, antiprotozoal activity, pharmacology, clinical efficacy, adverse effects, dosage, administration, and hospital formulary considerations of pentamidine isethionate are reviewed. Pentamidine, an aromatic diamidine, has been used since the 1940s to treat a variety of protozoal infections. It is now most commonly administered in the treatment of Pneumocystis carinii pneumonia (PCP). It is generally not metabolized, and it is stored or bound to tissue and excreted slowly as the parent compound. Pentamidine is clearly effective in the treatment of PCP; however, the high incidence of adverse reactions associated with the drug led to the use of trimethoprim-sulfamethoxazole (TMP-SMX) as the first-line agent for PCP. Recent studies have reported a high incidence of adverse reactions, including leukopenia and hepatotoxicity, associated with the use of TMP-SMX therapy for PCP in patients with the acquired immunodeficiency syndrome (AIDS). The severity and frequency of these reactions suggest a possible new role for pentamidine in patients with AIDS who have PCP. The recommended intramuscular and intravenous dosage of pentamidine isethionate for adults and children is 4 mg/kg/day for 14 days.