Subject(s)
Amines/urine , Heptaminol/urine , Heptanes/urine , Administration, Oral , Amines/administration & dosage , Amines/metabolism , Dietary Supplements/analysis , Heptaminol/metabolism , Heptanes/administration & dosage , Heptanes/metabolism , Humans , Male , Middle Aged , Pilot Projects , Substance Abuse DetectionABSTRACT
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.
Subject(s)
Cardiotonic Agents/urine , Doping in Sports , Gas Chromatography-Mass Spectrometry/methods , Heptaminol/urine , Substance Abuse Detection/methods , Acetic Anhydrides , Administration, Oral , Adult , Cardiotonic Agents/administration & dosage , Cardiotonic Agents/pharmacokinetics , Fluoroacetates , Heptaminol/administration & dosage , Heptaminol/pharmacokinetics , Humans , Male , Middle Aged , Reproducibility of Results , Trifluoroacetic Acid/chemistryABSTRACT
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.
Subject(s)
Amino Alcohols/pharmacokinetics , Heptaminol/pharmacokinetics , Administration, Oral , Adult , Biological Availability , Chromatography, Thin Layer , Female , Half-Life , Heptaminol/blood , Heptaminol/urine , Humans , MaleABSTRACT
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.).
