Trial reportClinical pharmacokinetics2006
Population pharmacokinetics of heroin and its major metabolites.
Trial report in Clinical pharmacokinetics, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
16 citing papers in PubMed, 71 citations in OpenAlex.
- Toxidromes.Nature reviews. Disease primers · 2026Review
- The relationship between injection status, cocaine use, overdose, and drug-related behaviors among people who use opioids.Drug and alcohol dependence reports · 2026Article
- Intranasal diamorphine population pharmacokinetics modeling and simulation in pediatric breakthrough pain.CPT: pharmacometrics & systems pharmacology · 2025Article
- The development of opioid vaccines as a novel strategy for the treatment of opioid use disorder and overdose prevention.The international journal of neuropsychopharmacology · 2025Review
- P-glycoprotein (MDR1/ABCB1) Restricts Brain Penetration of the Main Active Heroin Metabolites 6-monoacetylmorphine (6-MAM) and Morphine in Mice.Pharmaceutical research · 2023Article
- Heroin- and Fentanyl-Induced Respiratory Depression in a Rat Plethysmography Model: Potency, Tolerance, and Sex Differences.The Journal of pharmacology and experimental therapeutics · 2023Article
- Heroin and its metabolites: relevance to heroin use disorder.Translational psychiatry · 2023Review
- Novelty-induced locomotor behavior predicts heroin addiction vulnerability in male, but not female, rats.Psychopharmacology · 2022Article
- Pharmacokinetic Pharmacodynamic Modelling Contributions to Improve Paediatric Anaesthesia Practice.Journal of clinical medicine · 2022Review
- Identification and Characterization of Biomarkers and Their Role in Opioid Addiction by Integrated Bioinformatics Analysis.Frontiers in neuroscience · 2020Article
- Postmortem redistribution of the heroin metabolites morphine and morphine-3-glucuronide in rabbits over 24 h.International journal of legal medicine · 2016Article
- Transporter-Mediated Disposition of Opioids: Implications for Clinical Drug Interactions.Pharmaceutical research · 2015Review
- The effects of opioids on HIV reactivation in latently-infected T-lymphoblasts.AIDS research and therapy · 2014Article
- A vaccine strategy that induces protective immunity against heroin.Journal of medicinal chemistry · 2011Article
- Oral diacetylmorphine (heroin) yields greater morphine bioavailability than oral morphine: bioavailability related to dosage and prior opioid exposure.British journal of clinical pharmacology · 2008Article
- Endogenous opiates and behavior: 2006.Peptides · 2007Review
Corrections and comments
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Authors and funding
5 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundIn several European countries and in Canada, clinical trials are being conducted in which heroin-addicted patients are treated with pharmaceutically prepared heroin in order to reduce the destructive behaviour that is so often associated with this drug.
objectiveTo develop an integrated population pharmacokinetic model for heroin (diamorphine) and its pharmacodynamically active metabolites 6-acetylmorphine, morphine, morphine-3-glucuronide and morphine-6-glucuronide. Additionally, the influence on heroin pharmacokinetics of several covariates that are typical for this population was determined.
methodPlasma concentration data from 106 heroin-dependent patients in The Netherlands (74 heroin inhalers and 32 injectors) were obtained. The 'chasing the dragon' technique was used for inhalation, in which the fumes of heroin base, heated on aluminum foil, were inhaled. Heroin doses varied between 66 and 450 mg. Heroin, 6-acetylmorphine and morphine data were fitted simultaneously using sequential two-compartment models. Morphine-3-glucuronide and morphine-6-glucuronide data were fitted separately to one-compartment models. All data analysis was performed using nonlinear mixed-effect modelling.
resultsThe bioavailability of inhaled heroin was estimated to be 53% (95% CI 43.7, 62.3). The terminal half-lives of heroin and 6-acetylmorphine were estimated to be 7.6 and 21.8 minutes, respectively. The clearances of morphine and the morphine-glucuronides were estimated to be 73.6 L/h (95% CI 62.8, 84.4) and between 6 and 10 L/h, respectively. The terminal half-life of 6-acetylmorphine was 13% lower in cocaine users (p < 0.05). No other significant relationships between covariates and pharmacokinetic parameters were discovered.
conclusionsPharmacokinetic parameters of heroin and its five major metabolites were assessed simultaneously in one integrated model. Covariate analyses revealed that sex, bodyweight, benzodiazepine use and creatinine clearance (>60 mL/min) do not need to be taken into account in the medical prescription of pharmaceutically prepared heroin for the treatment of heroin dependency.
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