Injection: clear, colorless solution containing 37 MBq/mL to 1,480 MBq/mL (1 mCi/mL to 40 mCi/mL) of Fluorodopa F 18 Injection, at calibration time in a multiple-dose glass vial.
Fluorodopa F 18 Injection use contributes to a patient’s overall long-term radiation exposure, which is associated with an increased risk of cancer. Use the smallest dose necessary for imaging and ensure safe handling to protect the patient and health care worker [see Dosage and Administration (2.1, 2.2)].
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. No adverse reactions have been reported for Fluorodopa F 18 Injection based on an open-label clinical trial in 68 patients [see Clinical Studies ( 14)] and additional clinical experience in 53 patients.
The following adverse reactions have been identified during post approval of use of Fluorodopa F 18 Injection outside of the United States. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
General Disorders and Administration Site Conditions: Pain
Aromatic L-amino acid decarboxylase (AADC) inhibitors
Prior to Fluorodopa F 18 Injection administration, use of AADC inhibitors (e.g. carbidopa, benserazide etc.) may increase Fluorodopa F 18 bioavailability to the brain by inhibiting peripheral decarboxylase activity and restricting peripheral Fluorodopa F 18 metabolism [see Dosage and Administration (2.3)].
Dopamine agonists, dopamine reuptake inhibitors, dopamine releasing agents (DRAs), peripheral catechol-O-methyltransferase (COMT) inhibitors, and monoamine oxidase (MAO) inhibitors
Therapy for Parkinson’s syndromes includes dopamine agonists, dopamine reuptake inhibitors, dopamine releasing agents (DRAs) such as psychostimulants of the amphetamine class, peripheral catechol-O-methyltransferase (COMT) inhibitors, and monoamine oxidase (MAO) inhibitors. Whether discontinuation of these drugs prior to Fluorodopa F 18 administration may minimize the interference with a Fluorodopa F 18 image is not fully known; however, if use of these drugs can be safely suspended, discontinue use 12 hours before administration of Fluorodopa F18 Injection [see Dosage and Administration (2.3)].
There are no available data on Fluorodopa F 18 Injection use in pregnant women. Additionally, animal reproductive and developmental toxicity studies have not been conducted with Fluorodopa F 18 Injection. However, all radiopharmaceuticals, including Fluorodopa F 18 Injection, have a potential to cause fetal harm depending on the stage of fetal development, and the magnitude of the radiation dose. If considering Fluorodopa F 18 Injection administration to a pregnant woman, inform the patient about the potential for adverse pregnancy outcomes based on the radiation dose from the drug and the gestational timing of exposure.
The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risks of major birth defects and miscarriage in clinically recognized pregnancies are 2 to 4% and 15 to 20%, respectively, regardless of drug exposure.
No data are available regarding the presence of Fluorodopa F 18 Injection in human milk, the effects of the drug on the breastfed child, or the effects of the drug on milk production. Exposure of Fluorodopa F 18 Injection to a breast fed infant can be minimized by temporary discontinuation of breastfeeding [see Clinical Considerations]. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for Fluorodopa F 18 Injection and any potential adverse effects on the breastfed child from Fluorodopa F 18 Injection or from the underlying maternal condition.
The body of scientific information related to radioactivity decay, drug tissue distribution and drug elimination shows that less than 0.01% of the radioactivity administered remains in the body after 24 hours.
Clinical ConsiderationsTo decrease radiation exposure to a nursing infant, advise a lactating woman to pump and discard breastmilk for at least 24 hours (12 half-lives) after administration of Fluorodopa F 18 Injection.
The safety and effectiveness of Fluorodopa F 18 Injection for visualization of dopaminergic neurons in the striatum has not been established in pediatric patients.
Fluorodopa F 18 Injection is a radioactive diagnostic agent used in PET imaging. The active ingredient 6-[18 F] Fluoro-L-3, 4-dihydroxyphenylalanine has the molecular formula of C9 H10 FNO4 with a molecular weight of 214.18, and has the following chemical structure:
Fluorodopa F 18 Injection is a sterile, pyrogen-free, clear, colorless solution. Each mL contains between 37 MBq/mL to 1,480 MBq/mL (1 mCi/mL to 40 mCi/mL) of no-carrier added Fluorodopa F 18 (6-[18 F] Fluoro-L-3, 4-dihydroxyphenylalanine) at the end of synthesis (EOS). There is 40.88 mg Na-EDTA, 140 mg ascorbic acid, and 663 mg ethanol in 28 mL ±1 mL sodium phosphate buffer. The pH of the solution is between 3 and 5.
Fluorine F 18 is a cyclotron produced radionuclide that decays by positron emission to Oxygen O 18 (stable) and has a physical half-life of 109.7 minutes. The principal photons useful for imaging are the dual 511 keV gamma photons, which are produced and emitted simultaneously in opposite direction following positron-electron annihilation (Table 2).
|Radiation/Emission||% Per Disintegration||Mean Energy|
* Produced by positron annihilation
The point source air-kerma coefficient for F 18 is 3.75 × 10-17 Gy m2 / (Bq s). The half-value layer (HVL) for the 511 keV photons is 5 mm lead (Pb). The range of attenuation coefficients for this radionuclide as a function of lead shield thickness is shown in Table 3. For example, the interposition of a 9 mm thickness of Pb, with a coefficient of attenuation of 0.25, will decrease the external radiation by 75%.
|Shield thickness (Pb) mm||Coefficient of Attenuation|
For use in correcting for physical decay of this radionuclide, the fractions remaining at selected intervals after calibration are shown in Table 4.
|Time Since Calibration||Fraction Remaining|
* Calibration time
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