Early pharmacokinetics and clinical effects of oral d-amphetamine in normal subjects

• Published in: Biological psychiatry (1969) Vol. 22; no. 11; pp. 1357 - 1368
• Main Authors: Angrist, Burt, Corwin, June, Bartlik, Barbara, Cooper, Thomas
• Format: Journal Article
• Language: English
• Published: New York, NY Elsevier Inc 01.11.1987; Elsevier Science
• Subjects: Administration, Oral; Adult; Arousal - drug effects; Biological and medical sciences; Dextroamphetamine - pharmacokinetics; Dextroamphetamine - pharmacology; Dose-Response Relationship, Drug; Female; Humans; Male; Medical sciences; Middle Aged; Neuropharmacology; Pharmacology. Drug treatments; Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease); Psychology. Psychoanalysis. Psychiatry; Psychopharmacology; Human; CNS stimulant; Oral administration; Normal; Pharmacokinetics; Food drug interaction; Blood plasma
• ISSN: 0006-3223; 1873-2402
• DOI: 10.1016/0006-3223(87)90070-9

Seven normal subjects received 0.25 mg/kg D-amphetamine orally, both after an overnight fast and again after a standard breakfast. Plasma levels, subjective and cardiovascular effects, and observer-rated activation were assessed hourly for 5 hr. Food did not affect amphetamine levels. Plasma levels peaked at 2–3 hr. Maximum cardiovascular effects generally occurred at 1 hr, whereas maximum behavioral and subjective effects occurred at 2 hr. Subjective and behavioral effects declined thereafter, in spite of substantial amphetamine levels. A separate group of 8 subjects received 0.5 mg/kg D-amphetamine orally. Plasma levels, subjective and cardiovascular effects, and activation ratings were assessed hourly for 4 hr. Maximum plasma levels were approximately twice those seen in the first group. In this case, plasma levels peaked at 3–4 hr; blood pressure and subjective and behavioral effects were all maximal at 2–3 hr and were declining by 4 hr, in spite of stable or rising plasma levels.