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| Clinical data | |
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| Trade names | Datscan, Striascan, Celsunax |
| Other names | Ioflupane (FPCIT); [I-123] N-ω-fluoropropyl- 2β-carbomethoxy- 3β-(4-iodophenyl) nortropane |
| AHFS/Drugs.com | Professional Drug Facts |
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| Routes of administration | Intravenous |
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| Pharmacokinetic data | |
| Bioavailability | N/A |
| Excretion | Kidney and fecal |
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| Chemical and physical data | |
| Formula | C18H23FINO2 |
| Molar mass | 431.290 g·mol−1 |
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Ioflupane (123I) is theinternational nonproprietary name (INN) of acocaine analogue which is a neuro-imagingradiopharmaceutical drug, used innuclear medicine for the diagnosis ofParkinson's disease and the differential diagnosis of Parkinson's disease over other disorders presenting similar symptoms. During theDaT scan procedure it is injected into a patient and viewed with agamma camera in order to acquireSPECT images of thebrain with particular respect to thestriatum, a subcortical region of thebasal ganglia.[7] The drug is sold under the brand nameDatscan and is manufactured byGE Healthcare, formerly Amersham plc.
Datscan is a solution of ioflupane (123I) for injection into a living test subject.[7]
Theiodine introduced during manufacture is a radioactiveisotope,iodine-123, and it is thegamma decay of this isotope that is detectable to a gamma camera.123I has ahalf-life of approximately 13 hours and a gamma photon energy of 159keV making it an appropriate radionuclide for medical imaging. The solution also contains 5% ethanol to aid solubility and is supplied sterile since it is intended for intravenous use.[7]
Ioflupane has a high binding affinity for presynapticdopamine transporters (DAT) in the brains of mammals, in particular thestriatal region of the brain. A feature of Parkinson's disease is a marked reduction indopaminergic neurons in the striatal region. By introducing an agent that binds to the dopamine transporters a quantitative measure and spatial distribution of the transporters can be obtained.
The Datscan solution is supplied ready to inject with a certificate stating the calibration activity and time. The nominal injection activity is 185 MBq[7] and a scan should not be performed with less than 111 MBq.
Thyroid blocking via oral administration of 120 mgpotassium iodide is recommended to minimize unnecessary excessive uptake of radioiodine.[8] This is typically given 1–4 hours before the injection.[7][9]
The most convenient way to administer the IV dose is via a peripheral intravenouscannula. The scan is carried out 3 to 6 hours post injection.[8][9]
Blood clearance of the radionuclide is rapid in healthy volunteers.[10] Radioactivity was 4.5% of the injected amount 5 min after injection of ioflupane (123I), falling to 2.2% at 30 min, 1.9% at 5 h, and declining to 1.3% at 24 h and 1.1% at 48 h after injection. Values were similar in both whole blood and plasma. Excretion was primarily renal.
Common side effects of ioflupane (123I) are headache, vertigo, increased appetite andformication. Less than 1% of patients experience pain at the injection site.[7]
The radiation risks are reported as low. The committedeffective dose for a single investigation on a 70 kg individual is 4.6 mSv.[11] Pregnant patients should not undergo the test. It is not known if123I-ioflupane is secreted in breast milk however it is recommended that breastfeeding be interrupted for three days after administration.[7]
