Abstract | INTRODUCTION: METHODS: The study was designed as an open-label PK study in 2 cohorts: n = 5 with once daily 60 mg and n = 7 with once daily 30 mg SR oral dexamphetamine. Five days of blood plasma dexamphetamine concentrations measured with liquid chromatography-mass spectrometry with PK parameter estimates using noncompartmental analysis. RESULTS: Twelve cocaine-dependent plus heroin-dependent patients in heroin-assisted treatment were included. The initial cohort 1 dose of 60 mg once daily was adjusted to 30 mg after mild to moderate adverse events. After oral administration, tmax values (coefficient of variation %) were 6.0 (17.0%) and 6.3 (16.3%) hours and t1/2 were 11 (24.6%) and 12 (25.4%) hours for 60 mg and 30 mg SR dexamphetamine, respectively. At steady state, CSSmax values were reached at 100 (27.5%) ng/mL and 58.4 (14.4%) ng/mL, whereas CSSmin values were 39.5 (38.9%) ng/mL and 21.8 (19.8%) ng/mL for 60 mg and 30 mg, respectively. CONCLUSIONS: The investigated SR formulation of dexamphetamine showed favorable slow-release characteristics in cocaine and heroin-dependent patients. A dose-proportional steady-state concentration was achieved within 3 days. These findings support the suitability of the SR formulation in the treatment of cocaine dependence.
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Authors | Maikel Herbrink, Masha Nuijten, Bastiaan Nuijen, Alwin D R Huitema, Jos H Beijnen, Vincent M Hendriks, Peter Blanken, Amin Janmohamed, Wim van den Brink |
Journal | Journal of clinical psychopharmacology
(J Clin Psychopharmacol)
Vol. 38
Issue 3
Pg. 212-217
(Jun 2018)
ISSN: 1533-712X [Electronic] United States |
PMID | 29620701
(Publication Type: Clinical Trial, Phase I, Journal Article)
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Chemical References |
- Central Nervous System Stimulants
- Delayed-Action Preparations
- Dextroamphetamine
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Topics |
- Administration, Oral
- Adult
- Central Nervous System Stimulants
(administration & dosage, adverse effects, pharmacokinetics)
- Chromatography, Liquid
- Cocaine-Related Disorders
(rehabilitation)
- Cohort Studies
- Delayed-Action Preparations
- Dextroamphetamine
(administration & dosage, adverse effects, pharmacokinetics)
- Dose-Response Relationship, Drug
- Female
- Half-Life
- Heroin Dependence
(rehabilitation)
- Humans
- Male
- Mass Spectrometry
- Middle Aged
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