RESUMO
The possible influence of sex, race and of postprandial administration conditions (either immediately after the end of meal or one hour later) on the plasma concentrations of amocarzine and its N-oxide metabolite, CGP 13 231, was investigated. 71 Ecuadorian patients (48 males and 23 females) of two different races (Indio and Negro) infected with Onchocerca volvulus participated in the study. The concentrations were measured on day 3 at times 3 and 6 h after postprandial administration in the morning of a treatment with either a dose of 5 mg/kg of amocarzine once daily (12 patients) or 3 mg/kg twice daily (59 patients) for 3 days. The concentrations of unchanged drug and of CGP 13 231 measured after the 5 mg/kg treatment were in the low range of those expected from dose proportionality by the comparison with the 3 mg/kg. After the 3 mg/kg dose, no significant difference in concentration of both compounds were detected between the male and female patients between Indio and Negro patients, between the administration immediately after food intake and one hour later. The only detected difference (P = 0.05) was that between Indio and Negro patients for the concentrations of CGP 13 231 at time 3 h. This difference was not confirmed at time 6 h. Therefore, the administration of amocarzine either immediately or one hour after food intake appeared to produce reproducible absorption conditions which were not influenced by sex and race.
Assuntos
Filaricidas/farmacocinética , Alimentos , Oncocercose/metabolismo , Piperazinas/farmacocinética , Absorção , Administração Oral , População Negra , Esquema de Medicação , Equador , Feminino , Filaricidas/administração & dosagem , Filaricidas/sangue , Humanos , Indígenas Sul-Americanos , Masculino , Oncocercose/tratamento farmacológico , Piperazinas/administração & dosagem , Piperazinas/sangue , Caracteres SexuaisRESUMO
Ten Sudanese patients with Onchocerca volvulus infection were treated with a single oral dose of 150 micrograms/kg of ivermectin. Plasma samples were collected before treatment, 0.5, 1, 3, 4, 6, 12 hours and 1, 2, 3, 7, and 30 days. Four patients were selected for nodulectomies and skin biopsies at 6, 18 and 30 hours and 3 days post treatment. Using these samples O. volvulus worm fragments were dissected free of host nodular tissues for ivermectin extraction. Ivermectin was present in the nodular tissue at 6 hr and persisted for 3 days. It was also detected in an individual worm tissue extract at a concentration similar to the nodule, but in subcutaneous fascial tissue higher concentrations were sometimes found. Ivermectin was detected by radioimmunoassay in the plasma of all patients at 1 hr and peak concentrations were reached in an average of 5.6 hr. The drug persisted at detectable levels for 7 days in 70% of the studied patients. Plasma samples were also collected from 16 treated Mexican onchocerciasis patients before ivermectin treatment and 4 hr treatment and from six individuals who served as controls. The Mexican patients had concentrations of ivermectin in their plasma similar to those in the Sudanese patients.
Assuntos
Ivermectina/farmacocinética , Oncocercose/tratamento farmacológico , Humanos , Ivermectina/uso terapêutico , México , Oncocercose/metabolismo , Radioimunoensaio , Sudão , Distribuição TecidualRESUMO
Guatermalan volunteers with onchocerciasis were given a dose of diethylcarbamazine to learn if this caused migration of microfilariae of Onchocerca volvulus into urine, blood, and sputum. In 5 of the 10 volunteers, the num0ers of microfilariae in the urine increased considerably following the drug. In the same 5, relatively large numbers of microfilariae were observed in the blood and sputum specimens. Response in the remaining 5 was negligible. Four controls given a placebo did not respond. Interestingly, however, 2 control subjects had onchocercal microfilariae in their concentrated blood specimens and 3 control subjects had microfilariae in the sputum. Therefore, we believe that microfilariae, if searched for, may be found in other parts of the patient not normally associated with the infection.