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  • 1
    ISSN: 1432-2072
    Keywords: Striatum ; Dopamine receptor ; Positron emission tomography ; Prolactin ; Neuroleptics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The percentage occupation of striatal dopamine D2 receptors has been evaluated in 25 patients using76Br-bromospiperone positron emission tomography (PET) and prolactin plasma levels (PRL) during oral neuroleptic treatment (11 studies), 1–90 days following discontinuation of such treatment (16 studies), and 1–120 days after last intramuscular administration of depot neuroleptics (nine studies). The PET-estimated occupation was highly significantly correlated in a sigmoîd-like fashion to the logarithm of the chlorpromazine-equivalent dose of oral neuroleptics (suggesting a strict dose-occupation relationship during oral neuroleptic treatment and supporting the D2-mediated hypothesis of neuroleptic action), while PRL was weakly related to daily dosage. Following withdrawal, return to normal receptor availability, as estimated by PET, occurred within 5–15 days (suggesting that protracted effects of neuroleptics after withdrawal are not due to sustained D2 receptor occupation), but PRL values fell even more rapidly. Efficient treatment with depot neuroleptics resulted in marked PET-estimated D2 receptor occupation, stable over the whole 4-week drug-administration interval, suggesting that longer intervals could be appropriate; PRL values bore no relationship to PET-estimated occupation, indicating variable intersubject tolerance to neuro-endocrine dopamine blockade. Overall, PET was much more sensitive than PRL to estimate striatal D2 receptor occupation in vivo.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1619-7089
    Keywords: Positron emission tomography ; PET ; Radiopharmaceuticals ; Quality criteria ; Toxicology ; Dosimetry ; Survey
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The increasing use of radiopharmaceuticals for positron emission tomography (PET) has come to the attention of regulatory bodies. In order to help authorities in all aspects, the EANM has formed a task group for licensing PET radiopharmaceuticals; this group has surveyed the use of these compounds in Europe by a questionnaire. The number of PET centres that responded to the questionnaire was 26, which included more than 90% of the larger European PET centres. The survey showed that 2-[18F]fluoro-2-deoxyglucose is by far the most important PET radiopharmaceutical with more than 200 applications per week, followed by [15O]water, [15O]carbonmonoxide, [13N]ammonia, [11C]-l-methionine, andl-6-[18F]fluoro-DOPA. More than 25 other PET radiopharmaceuticals are in regular use, however, at rather low application frequencies. The data were used by the European Pharmacopoeia Commission for its priority rating for requesting the formulation of monographs. Since it is likely that group registrations will be issued by authorities for the PET radiopharmaceuticals, relevant data on toxicity and dosimetry for the formulation of summaries of product characteristics have been collected by the task group as well.
    Type of Medium: Electronic Resource
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