Ioflupane I 123 is an intravenous, radioactive diagnostic agent indicated as an adjunct to other diagnostic evaluations for striatal dopamine transporter visualization using single photon emission computed tomography (SPECT) brain imaging in adults with suspected Parkinsonian syndromes or dementia with Lewy bodies. To block uptake of iodine-123 by the thyroid, premedication with potassium iodide oral solution or strong iodine solution (e.g., Lugol's solution) is necessary; failure to block thyroid uptake of iodine-123 may result in increased long-term risk for thyroid cancer. Hypersensitivity reactions have been reported within minutes of ioflupane I 123 administration and have either resolved spontaneously or after treatment with corticosteroids and antihistamines.
General Administration Information
For storage information, see the specific product information within the How Supplied section.
NOTE: Administer potassium iodide oral solution or strong iodine solution (e.g. Lugol's Solution) (equivalent to 100 mg iodide) at least 1 hour before ioflupane I 123 administration to block uptake of iodine-123 by the thyroid.
NOTE: Ensure patient is adequately hydrated by encouraging patient hydration before and after ioflupane I 123 administration. In addition, encourage frequent voiding for the first 48 hours after ioflupane I 123 administration.
NOTE: Ioflupane I 123 is a radioactive material. To assure minimum radiation exposure to occupational workers and to minimize radiation exposure to patients, observe appropriate precautions that are consistent with proper patient management. Radiopharmaceuticals are intended for use only by nuclear physicians and/or radiopharmacists who are qualified by training and experience in the safe use and handling of radioactive material, and whose experience and training have been approved by the appropriate governmental agency authorized to license the use of radiopharmaceuticals.
NOTE: Storage and disposal should be controlled in compliance with appropriate regulations of the governmental agency authorized to license the use of radiopharmaceuticals.
Route-Specific Administration
Injectable Administration
-To minimize radiation exposure, maintain adequate shielding during the life of the product.
-Visually inspect parenteral products for particulate matter and discoloration. The solution is clear and colorless; discard if vial contains particulate matter or if solution is discolored.
Intravenous Administration
-Immediately prior to administration, determine the dose based on radioactivity of the product using a suitable radioactivity calibration system.
-Using aseptic technique and radiation shielding, withdraw the recommended dose.
-Administer IV over at least 20 seconds.
-Initiate the single photon emission computed tomography (SPECT) scan 3 to 6 hours after ioflupane I 123 administration. Acquire images using a gamma camera fitted with high-resolution collimators and set to a photopeak of 159 keV with a +/- 10% energy window. At least 120 views should be obtained over 360 degrees.
-Storage: Discard any unused portion.
Dizziness, headache, and vertigo occurred in less than 1% of subjects receiving ioflupane I 123 during clinical trials. All adverse reactions were deemed mild to moderate in severity.
Nausea and xerostomia occurred in less than 1% of subjects receiving ioflupane I 123 during clinical trials. All adverse reactions were deemed mild to moderate in severity.
Injection site reaction (i.e., pain) and hypersensitivity reactions, including dyspnea, edema, rash, erythema and pruritus, have been reported after ioflupane I 123 administration. Hypersensitivity reactions usually occurred within minutes of ioflupane I 123 administration and resolved spontaneously or after treatment with corticosteroids and antihistamines.
Ioflupane I 123 is contraindicated in persons with known serious hypersensitivity to ioflupane I 123. Have hypersensitivity treatment measures available prior to ioflupane I 123 administration, and observe patients for signs and symptoms of a hypersensitivity reaction. Hypersensitivity reactions have generally occurred within minutes of ioflupane I 123 administration and have either resolved spontaneously or after treatment with corticosteroids and antihistamines.
Ioflupane I 123 is intended for use only by or under the control of physicians and/or radiopharmacists who are qualified by specific training and experience in the safe use and handling of radioactive materials, and whose experience and training have been approved by the appropriate governmental agency authorized to license the use of radionuclides. Take care to assure minimum accidental exposure of radiation to occupational workers, including use of effective shielding. Furthermore, take care to minimize radiation exposure to the patient by proper patient management before, during, and after the procedure. Advise patients to hydrate prior and subsequent to ioflupane I 123 administration, and instruct patients to void frequently for the first 48 hours after administration of ioflupane I 123 to minimize the radiation-absorbed dose to the bladder. To block uptake of iodine-123 by the thyroid, administer potassium iodide oral solution or strong iodine solution (e.g., Lugol's Solution) (equivalent to 100 mg iodide) at least 1 hour before ioflupane I 123 administration. Failure to block thyroid uptake of iodine-123 may result in increased long-term risk for thyroid cancer.
The effect of renal disease on ioflupane I 123 imaging has not been established. Ioflupane I 123 is renally excreted, and patients with severe renal impairment may have increased radiation exposure and altered ioflupane I 123 imaging.
Radioactive iodine crosses the placenta and can permanently impair fetal thyroid function. Advise pregnant women of the potential risks of fetal exposure to radiation doses with the administration of ioflupane I 123. Administration of an appropriate thyroid blocking agent is recommended before ioflupane I 123 use to protect the woman and fetus from I 123 accumulation. There are no data regarding the use of ioflupane I 123 during pregnancy to determine the drug-associated risk for major birth defects, miscarriages, or adverse maternal or fetal outcomes. However, all radiopharmaceuticals have the potential to cause fetal toxicity, with the likelihood of harm depending on the stage of fetal development and the radiopharmaceutical dose. Administration of ioflupane I 123 185 MBq (5 mCi) results in an absorbed radiation dose to the uterus of 0.3 rad (3 mGy). Radiation doses more than 15 rad (150 mGy) have been associated with congenital anomalies but doses less than 5 rad (50 mGy) generally have not.
Iodine 123 (I 123), the radionuclide in ioflupane I 123, is excreted in human breast milk. There is no information on the effects of iofluplane I 123 on the breast-fed infant or on milk production. To minimize radiation exposure to a nursing infant, advise a lactating woman to interrupt breast-feeding and pump and discard breast milk for at least 6 days after ioflupane I 123 exposure.
It is unknown if ioflupane I 123 is associated with reproductive risk. Females of childbearing age should undergo pregnancy testing prior to administration of ioflupane I 123.
For radiographic examination in persons with suspected Parkinsonian syndromes or dementia with Lewy bodies as an adjunct to other diagnostic evaluations for striatal dopamine transporter visualization using single photon emission computed tomography (SPECT) brain imaging:
NOTE: This drug is a radiopharmaceutical and should be administered by individuals specifically trained in the handling of radioactive material.
NOTE: Dosage measured in megabecquerels (MBq) and millicuries (mCi)
NOTE: To block uptake of iodine-123 by the thyroid, administer potassium iodide oral solution or strong iodine solution (e.g. Lugol's Solution) (equivalent to 100 mg iodide) at least 1 hour before ioflupane I 123 administration.
Intravenous dosage:
Adults: 111 to 185 MBq (3 to 5 mCi) IV as a single dose. Begin SPECT imaging 3 to 6 hours after administration.
Maximum Dosage Limits:
-Adults
185 MBq (5 mCi) IV per procedure.
-Geriatric
185 MBq (5 mCi) IV per procedure.
-Adolescents
Safety and efficacy have not been established.
-Children
Safety and efficacy have not been established.
-Infants
Safety and efficacy have not been established.
-Neonates
Safety and efficacy have not been established.
Patients with Hepatic Impairment Dosing
Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.
Patients with Renal Impairment Dosing
Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.
*non-FDA-approved indication
Acetaminophen; Codeine: (Major) Hold codeine for 1 day, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Codeine binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Amoxapine: (Moderate) Amoxapine binds to the dopamine transporter and may interfere with dopamine transporter (DAT) imaging that utilizes radiolabeled ioflupane.
Amphetamine: (Major) Hold amphetamines for 7 days, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Amphetamines bind to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Amphetamine; Dextroamphetamine: (Major) Hold amphetamines for 7 days, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Amphetamines bind to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Amphetamines: (Major) Hold amphetamines for 7 days, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Amphetamines bind to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Armodafinil: (Major) Hold armodafinil for 3 days, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Armodafinil binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Aspirin, ASA; Carisoprodol; Codeine: (Major) Hold codeine for 1 day, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Codeine binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Benzphetamine: (Major) Hold amphetamines for 7 days, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Amphetamines bind to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Benztropine: (Moderate) Benztropine binds to the dopamine transporter and may interfere with dopamine transporter (DAT) imaging that utilizes radiolabeled ioflupane.
Bupropion: (Major) Hold bupropion for 8 days, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Bupropion binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Bupropion; Naltrexone: (Major) Hold bupropion for 8 days, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Bupropion binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Buspirone: (Moderate) Buspirone binds to the dopamine transporter and may interfere with dopamine transporter (DAT) imaging that utilizes radiolabeled ioflupane.
Butalbital; Acetaminophen; Caffeine; Codeine: (Major) Hold codeine for 1 day, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Codeine binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Butalbital; Aspirin; Caffeine; Codeine: (Major) Hold codeine for 1 day, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Codeine binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Chlorpheniramine; Codeine: (Major) Hold codeine for 1 day, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Codeine binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Citalopram: (Moderate) Selective serotonin reuptake inhibitors (SSRIs) may interfere with dopamine transporter (DAT) imaging that utilizes radiolabeled ioflupane. Observed changes in striatal tracer binding have generally been small and inconsistent. These changes are unlikely to affect the interpretation of visual assessments in routine clinical practice but may be relevant in the research setting.
Cocaine: (Major) Allow at least 2 days to elapse before performing dopamine transporter (DAT) imaging with radiolabeled ioflupane in patients who used cocaine or have received cocaine anesthesia. Cocaine binds the dopamine transporter. Acute cocaine ingestion may interfere with striatal tracer binding and increase the risk for a false-positive scan. Chronic cocaine use may have a more complex effect on dopamine transporter expression which may impact imaging interpretation.
Codeine: (Major) Hold codeine for 1 day, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Codeine binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Codeine; Guaifenesin: (Major) Hold codeine for 1 day, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Codeine binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Codeine; Guaifenesin; Pseudoephedrine: (Major) Hold codeine for 1 day, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Codeine binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Codeine; Phenylephrine; Promethazine: (Major) Hold codeine for 1 day, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Codeine binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Codeine; Promethazine: (Major) Hold codeine for 1 day, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Codeine binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Dexmethylphenidate: (Major) Hold methylphenidate and methylphenidate derivatives for 7 days, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Methylphenidate binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Dextroamphetamine: (Major) Hold amphetamines for 7 days, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Amphetamines bind to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Dextromethorphan; Bupropion: (Major) Hold bupropion for 8 days, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Bupropion binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Ephedrine: (Major) Hold ephedrine for 1 day, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Ephedrine binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Ephedrine; Guaifenesin: (Major) Hold ephedrine for 1 day, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Ephedrine binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Escitalopram: (Moderate) Selective serotonin reuptake inhibitors (SSRIs) may interfere with dopamine transporter (DAT) imaging that utilizes radiolabeled ioflupane. Observed changes in striatal tracer binding have generally been small and inconsistent. These changes are unlikely to affect the interpretation of visual assessments in routine clinical practice but may be relevant in the research setting.
Fentanyl: (Major) Hold fentanyl for 5 days, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Fentanyl binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Fluoxetine: (Moderate) Selective serotonin reuptake inhibitors (SSRIs) may interfere with dopamine transporter (DAT) imaging that utilizes radiolabeled ioflupane. Observed changes in striatal tracer binding have generally been small and inconsistent. These changes are unlikely to affect the interpretation of visual assessments in routine clinical practice but may be relevant in the research setting.
Fluvoxamine: (Moderate) Selective serotonin reuptake inhibitors (SSRIs) may interfere with dopamine transporter (DAT) imaging that utilizes radiolabeled ioflupane. Observed changes in striatal tracer binding have generally been small and inconsistent. These changes are unlikely to affect the interpretation of visual assessments in routine clinical practice but may be relevant in the research setting.
Haloperidol: (Major) Hold haloperidol for 5 days, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Haloperidol binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Isoflurane: (Major) Allow at least 1 day to elapse prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane in patients who have received isoflurane. Isoflurane binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Ketamine: (Major) Hold ketamine for 1 day, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Ketamine binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Lisdexamfetamine: (Major) Hold amphetamines for 7 days, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Amphetamines bind to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Methamphetamine: (Major) Hold amphetamines for 7 days, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Amphetamines bind to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Methylphenidate Derivatives: (Major) Hold methylphenidate and methylphenidate derivatives for 7 days, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Methylphenidate binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Methylphenidate: (Major) Hold methylphenidate and methylphenidate derivatives for 7 days, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Methylphenidate binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Modafinil: (Major) Hold modafinil for 3 days, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Modafinil binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Olanzapine; Fluoxetine: (Moderate) Selective serotonin reuptake inhibitors (SSRIs) may interfere with dopamine transporter (DAT) imaging that utilizes radiolabeled ioflupane. Observed changes in striatal tracer binding have generally been small and inconsistent. These changes are unlikely to affect the interpretation of visual assessments in routine clinical practice but may be relevant in the research setting.
Paroxetine: (Moderate) Selective serotonin reuptake inhibitors (SSRIs) may interfere with dopamine transporter (DAT) imaging that utilizes radiolabeled ioflupane. Observed changes in striatal tracer binding have generally been small and inconsistent. These changes are unlikely to affect the interpretation of visual assessments in routine clinical practice but may be relevant in the research setting.
Phentermine: (Major) Hold phentermine for 5 days, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Phentermine binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Phentermine; Topiramate: (Major) Hold phentermine for 5 days, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Phentermine binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Selective serotonin reuptake inhibitors: (Moderate) Selective serotonin reuptake inhibitors (SSRIs) may interfere with dopamine transporter (DAT) imaging that utilizes radiolabeled ioflupane. Observed changes in striatal tracer binding have generally been small and inconsistent. These changes are unlikely to affect the interpretation of visual assessments in routine clinical practice but may be relevant in the research setting.
Selegiline: (Moderate) Selegiline may bind to the dopamine transporter and interfere with dopamine transporter (DAT) imaging that utilizes radiolabeled ioflupane.
Serdexmethylphenidate; Dexmethylphenidate: (Major) Hold methylphenidate and methylphenidate derivatives for 7 days, or at least 5 medication half-lives, prior to performing dopamine transporter (DAT) imaging with radiolabeled ioflupane. Methylphenidate binds to the dopamine transporter which may interfere with striatal tracer binding and increase the risk for a false-positive scan.
Sertraline: (Moderate) Selective serotonin reuptake inhibitors (SSRIs) may interfere with dopamine transporter (DAT) imaging that utilizes radiolabeled ioflupane. Observed changes in striatal tracer binding have generally been small and inconsistent. These changes are unlikely to affect the interpretation of visual assessments in routine clinical practice but may be relevant in the research setting.
After intravenous administration, ioflupane I 123 selectively binds to dopamine transporters (DaT) located in the striatum of the brain, thereby resulting in drug accumulation within the putamen and caudate nucleus. After administration, iodine 123 begins to decay and emits gamma radiation that can be detected by a gamma camera during single photon emission computed tomography (SPECT) imaging. In patients with non-Parkinsonian syndrome tremor, images obtained by the SPECT scan show 2 regions of activity within the striatum that are symmetrical, comma- or crescent-shaped, and distinct from surrounding brain tissue. In patients with Parkinsonian syndrome, images show 1 of the following: asymmetrical activity (i.e., activity in the putamen of 1 hemisphere while absent or reduced in the other); absent activity in the putamen of both hemispheres; absent activity in the putamen of both hemispheres and greatly reduced activity in 1 or both caudate nuclei. Results of ioflupane I 123 SPECT scans are intended to be used only as an adjunct to other diagnostic tests.
Ioflupane I 123 is administered intravenously. Ioflupane I 123 rapidly distributes throughout the body with only 5% of the radioactivity remaining in the blood at 5 minutes after administration. Brain uptake reaches approximately 7% of the injected radioactivity at 10 minutes after administration and decreases to 3% after 5 hours. Striata to background ratios remain relatively constant between 3 and 6 hours after administration; striatal uptake accounts for about 30% of the whole brain radioactivity. Approximately 60% of the injected radioactivity is excreted in the urine and 14% excreted in the feces by 48 hours post-injection.
Affected cytochrome P450 isoenzymes and drug transporters: none
-Route-Specific Pharmacokinetics
Intravenous Route
The estimated total body radiation absorbed dose from ioflupane I 123 is 11.3 microGy/MBq, assuming bladder emptying at intervals of 4.8 hours and appropriate thyroid blocking. The effective dose from 185 MBq (5 mCi) of ioflupane I 123 is 3.94 mSv in an adult.