Source: European Medicines Agency (EU) Revision Year: 2021 Publisher: Pinax Pharma GmbH, Lausitz Mühlenweg 5, 04924 Bad Liebenwerda, Germany
Pharmacotherapeutic group: Diagnostic radiopharmaceuticals, central nervous system
ATC code: V09AB03
At the chemical concentrations used for diagnostic examinations, Celsunax does not appear to have any pharmacodynamic activity.
Ioflupane is a cocaine analogue. Studies in animals have shown that ioflupane binds with high affinity to the presynaptic dopamine transporter and so radiolabelled ioflupane (123I) can be used as a surrogate marker to examine the integrity of the dopaminergic nigrostriatal neurons. Ioflupane also binds to the serotonin transporter on 5-HT neurons but with lower (approximately 10-fold) binding affinity.
There is no experience in types of tremor other than essential tremor.
In a pivotal clinical study including evaluation of 288 subjects with dementia with Lewy bodies (DLB) (144 subjects), Alzheimer’s disease (124 subjects), vascular dementia (9 subjects) or other (11 subjects), the results of an independent, blinded visual assessment of the ioflupane (123I) images were compared to the clinical diagnosis as determined by physicians experienced in the management and diagnosis of dementias. Clinical categorisation into the respective dementia group was based on a standardised and comprehensive clinical and neuropsychiatric evaluation. The values for the sensitivity of ioflupane (123I) in determining probable DLB from non-DLB ranged from 75.0% to 80.2% and specificity from 88.6% to 91.4%. The positive predictive value ranged from 78.9% to 84.4% and the negative predictive value from 86.1% to 88.7%. Analyses in which both possible and probable DLB patients were compared with non-DLB dementia patients demonstrated values for the sensitivity of ioflupane (123I) ranging from 75.0% to 80.2% and specificity from 81.3% to 83.9% when the possible DLB patients were included as non-DLB patients. The sensitivity ranged from 60.6% to 63.4% and specificity from 88.6% to 91.4% when the possible DLB patients were included as DLB patients.
Ioflupane (123I) is cleared rapidly from the blood after intravenous injection; only 5% of the administered activity remains in whole blood at 5 minutes post-injection.
Uptake in the brain is rapid, reaching about 7% of injected activity at 10 minutes post-injection and decreasing to 3% after 5 hours. About 30% of the whole brain activity is attributed to striatal uptake.
At 48 hours post-injection, approximately 60% of the injected radioactivity is excreted in the urine, with faecal excretion calculated at approximately 14%.
Non-clinical data for ioflupane reveal no special hazard for humans based on conventional studies of safety pharmacology, single and repeated dose toxicity and genotoxicity.
Studies on reproductive toxicity and to assess the carcinogenic potential of ioflupane have not been performed.
After use, all materials associated with the preparation and administration of radiopharmaceuticals, including any unused medicinal product and its container, should be decontaminated or treated as radioactive waste and disposed of in accordance with the conditions specified by the local competent authority. Contaminated material must be disposed of as radioactive waste via an authorised route.
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