DATSCAN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DATSCAN (DATSCAN).
Ioflupane I-123 is a cocaine analog that binds to the dopamine transporter (DAT) in the striatum, allowing visualization of dopaminergic neuron integrity via SPECT imaging.
| Metabolism | Hepatic metabolism via cytochrome P450 enzymes (minor); no major active metabolites. |
| Excretion | Primarily renal excretion of intact drug and metabolites; approximately 60% of the administered dose is excreted in urine within 48 hours, with about 15% in feces. |
| Half-life | The terminal elimination half-life of Ioflupane I-123 is approximately 30 hours. This long half-life allows for imaging up to 6 hours post-injection, but requires consideration of radiation exposure. |
| Protein binding | Approximately 70% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Ioflupane has a volume of distribution of about 13 L/kg, indicating extensive tissue distribution beyond plasma volume, consistent with its lipophilicity and CNS penetration. |
| Bioavailability | Not applicable; administered intravenously as a diagnostic radiopharmaceutical. Bioavailability is 100% by IV route. |
| Onset of Action | After intravenous injection, uptake in the striatum reaches peak levels within 30 minutes, with maximal contrast between striatum and background achieved at 3-6 hours. |
| Duration of Action | The diagnostic imaging window is 3-6 hours post-injection. The radioactivity remains detectable for up to 24 hours, but optimal imaging is within the specified window. |
3-5 mCi (111-185 MBq) of iodine-123 ioflupane administered as a single intravenous bolus injection over approximately 15-20 seconds.
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment required for renal impairment; iodine-123 ioflupane is not significantly renally eliminated. |
| Liver impairment | No specific dose adjustment guidelines; use caution in severe hepatic impairment as metabolism is hepatic. |
| Pediatric use | Not approved for use in pediatric patients; safety and efficacy not established. |
| Geriatric use | No specific dose adjustment; standard adult dose may be used in elderly patients based on clinical judgment. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for DATSCAN (DATSCAN).
| Breastfeeding | No data on ioflupane I 123 excretion in human milk. Radiopharmaceuticals may be excreted; advise temporary cessation of breastfeeding for at least 24-48 hours post-administration to reduce infant radiation exposure. M/P ratio unknown. |
| Teratogenic Risk | DATSCAN (ioflupane I 123) is a radiopharmaceutical. No human data on fetal risk; animal studies show no teratogenicity at clinically relevant doses. All radiopharmaceuticals pose potential fetal radiation risk; use in pregnancy only if clearly needed. First trimester: highest risk of radiation-induced fetal anomalies; consider alternative. Second/third trimester: lower risk but fetal thyroid uptake may occur. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to ioflupane or any excipient","Pregnancy (unless benefit outweighs radiation risk)"]
| Precautions | ["Hypersensitivity reactions including anaphylaxis","Radiation exposure risk (especially in pregnant women and children)","Image interpretation errors due to technical artifacts or patient movement","Interference from drugs affecting DAT (e.g., amphetamines, cocaine, methylphenidate)"] |
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| Fetal Monitoring | Maternal: Monitor for hypersensitivity reactions (rash, dyspnea). No specific fetal monitoring required; however, if used during pregnancy, consider fetal radiation dose estimation by medical physicist. Post-administration: Ensure adequate hydration to promote radionuclide excretion. |
| Fertility Effects | No known effects on fertility in humans. Animal studies at doses up to 58 times human exposure showed no impairment of fertility. |