Blood–brain barrier transport of morphine in patients with severe brain trauma

Aims In experimental studies, morphine pharmacokinetics is different in the brain compared with other tissues due to the properties of the blood–brain barrier, including action of efflux pumps. It was hypothesized in this clinical study that active efflux of morphine occurs also in human brain, and...

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Bibliographic Details
Published in:British journal of clinical pharmacology 2004-04, Vol.57 (4), p.427-435
Main Authors: Ederoth, Per, Tunblad, Karin, Bouw, René, Lundberg, C. Johan F., Ungerstedt, Urban, Nordström, Carl‐Henrik, Hammarlund‐Udenaes, Margareta
Format: Article
Language:English
Subjects:
Adult
Analgesics
Analgesics, Opioid - pharmacokinetics
Anestesi och intensivvård
Anesthesiology and Intensive Care
Area Under Curve
Biological and medical sciences
blood-brain barrier
Blood-Brain Barrier - metabolism
Brain Injuries - metabolism
brain injury
Clinical Medicine
Drug Disposition
Female
Half-Life
human
Humans
Kirurgi
Klinisk medicin
Male
Medical and Health Sciences
Medical sciences
MEDICIN
Medicin och hälsovetenskap
MEDICINE
microdialysis
Middle Aged
morphine
Morphine - pharmacokinetics
Neurologi
Neurology
Neuropharmacology
pharmacokinetics
Pharmacology. Drug treatments
Surgery
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Summary:Aims In experimental studies, morphine pharmacokinetics is different in the brain compared with other tissues due to the properties of the blood–brain barrier, including action of efflux pumps. It was hypothesized in this clinical study that active efflux of morphine occurs also in human brain, and that brain injury would alter cerebral morphine pharmacokinetics. Methods Patients with traumatic brain injury, equipped with one to three microdialysis catheters in the brain and one in abdominal subcutaneous fat for metabolic monitoring, were studied. The cerebral catheter locations were classified as ‘better’ and ‘worse’ brain tissue, referring to the degree of injury. Morphine (10 mg) was infused intravenously over a 10‐min period in seven patients in the intensive care setting. Tissue and plasma morphine concentrations were obtained during the subsequent 3‐h period with microdialysis and regular blood sampling. Results The area under the concentration–time curve (AUC) ratio of unbound morphine in brain tissue to plasma was 0.64 (95% confidence interval 0.40, 0.87) in ‘better’ brain tissue (P 
ISSN:0306-5251
1365-2125
1365-2125
DOI:10.1046/j.1365-2125.2003.02032.x