Assuntos
Aminas/urina , Heptaminol/urina , Heptanos/urina , Administração Oral , Aminas/administração & dosagem , Aminas/metabolismo , Suplementos Nutricionais/análise , Heptaminol/metabolismo , Heptanos/administração & dosagem , Heptanos/metabolismo , Humanos , Masculino , Pessoa de Meia-Idade , Projetos Piloto , Detecção do Abuso de SubstânciasRESUMO
Heptaminol is an antihypotensive drug and is one of the stimulants banned in sport competitions. When heptaminol was fortified to a drug-free urine sample and subjected to solid-phase extraction, trifluroacetic anhydride derivatization, and gas chromatography-mass spectrometry analysis, the results indicated three chromatographic peaks, with one major peak [peak 1 (P1) as heptaminol-2TFA], appearing at retention time 7.17 min, and two minor peaks [peak 2 (P2) and peak 3 (P3) as heptaminol-TFA], appearing at RT 5.87 and 5.81 min, respectively. The characteristic ions of peak mass spectra were m/z 322, 224, and 140 for P1, m/z 223 (molecular ion), 208, 140, and 110 for P2, and m/z 208, 140, and 110 for P3. The urine samples collected from healthy male volunteers who orally ingested a single dose (100 mg) of heptaminol were similar to the analytical results shown in the heptaminol-spiked control urine samples. This result suggested that the unchanged heptaminol was the sole form found in urine. The unchanged parent compound was completely eliminated in urine within 24 h and an average of approximately 97% of the dose was excreted through the renal pathway.
Assuntos
Cardiotônicos/urina , Dopagem Esportivo , Cromatografia Gasosa-Espectrometria de Massas/métodos , Heptaminol/urina , Detecção do Abuso de Substâncias/métodos , Anidridos Acéticos , Administração Oral , Adulto , Cardiotônicos/administração & dosagem , Cardiotônicos/farmacocinética , Fluoracetatos , Heptaminol/administração & dosagem , Heptaminol/farmacocinética , Humanos , Masculino , Pessoa de Meia-Idade , Reprodutibilidade dos Testes , Ácido Trifluoracético/químicaRESUMO
In ten healthy volunteers the plasma and urine concentrations of heptaminol (Heptylon) were determined by high-performance liquid chromatography after intravenous administration of 250 mg heptaminol and oral intake of 2 x 150 mg heptaminol in tablet form, and the pharmacokinetic parameters were calculated. Heptaminol was rapidly and entirely absorbed following oral administration of heptaminol. Mean plasma peak concentrations of 1.6 mg/l were reached after 1.8 h, the area under the plasma concentration-time curve was equal to that after intravenous administration. The dominant terminal plasma half-life was 2.5-2.7 h. The total clearance amounted to 700 ml/min, and nearly all the dose given was recovered unchanged in urine within 24 h, indicating renal elimination by glomerular filtration and tubular secretion without metabolization.
Assuntos
Amino Álcoois/farmacocinética , Heptaminol/farmacocinética , Administração Oral , Adulto , Disponibilidade Biológica , Cromatografia em Camada Fina , Feminino , Meia-Vida , Heptaminol/sangue , Heptaminol/urina , Humanos , MasculinoRESUMO
Heptaminol was measured in plasma and urine following pre-column derivatisation with o-phthalaldehyde and reversed-phase high-performance liquid chromatography employing fluorescence detection. The limits of detection were sufficient for pharmacokinetic studies of the drug after clinically-used doses. Plasma concentrations of heptaminol reached peak levels (2.19 micrograms/ml) at 0.75 h after single oral doses (0.47 g of heptaminol) and declined with a half-life of 2.1 h (+/- 0.5 S.D.). Heptaminol was well absorbed and excreted rapidly, mainly unchanged in urine, 82% dose (+/- 10 S.D.).