Dosing & Uses
Dosage Forms & Strengths
IV injection
- 0.1-19mcg/mL (florbetapir) and 13.5-51mCi/mL (florbetapir F 18)
Beta-Amyloid Plaque Estimation
Radioactive, adjunctive diagnostic agent for PET brain imaging to estimate beta-amyloid neuritic plaque density in adult patients with cognitive impairment who are being evaluated for Alzheimer Disease (AD) and other causes of cognitive decline
A negative scan indicates sparse to no neuritic plaques, and is inconsistent with a neuropathological diagnosis of AD as a cause of cognitive impairment; whereas, a positive scan indicates moderate-to-frequent amyloid neuritic plaques
Moderate-to-frequent amyloid plagues are found in patients with AD, but may also be present in with other types of neurologic conditions as well as older people with normal cognition
Dosage
- 370 MBq (10 mCi) as a single IV bolus injection in a total volume of 10 mL or less; follow bolus injection 0.9% NaCl IV flush
- Not to exceed 50 mcg mass dose
- Inject through a short IV catheter (~1.5 inches or less) to minimize the potential for adsorption of the drug to the catheter
Limitations of use
- Positive scan does not establish a diagnosis of AD or other cognitive disorder
- Safety and effectiveness have not been established for: 1) predicting development of dementia or other neurologic condition; 2) monitoring responses to therapies
Image Display & Interpretation
A 10-minute PET image should be acquired starting 30-50 minutes after IV injection
The patient should be supine; position head to center the brain, including the cerebellum, in the PET scanner field of view
Reduce head movement with tape or other flexible head restraints may be employed
Image reconstruction should include attenuation correction with resulting transaxial pixel sizes between 2 and 3 mm
Display
- Display images in the transaxial orientation with access as needed to the sagittal and coronal planes
- In reviewing the images, include all transaxial slices of the brain using a black-white scale with the maximum intensity of the scale set to the maximum intensity of all the brain pixels
- Initially locate the brain slice with the highest levels of image contrast (highest radioactivity signals for florbetapir uptake) and adjust the contrast appropriately
- Start image interpretation by displaying slices sequentially from the bottom of the brain to the top
- Periodically refer to the sagittal and coronal plane image display, as needed to better define the radioactivity uptake and to ensure that the entire brain is displayed
Interpretation
- Image interpretation is based upon the distribution of radioactive signal within the brain; clinical information is not a component of the image assessment
- Images are designated as positive or negative by comparing the radioactivity in cortical gray matter with activity in the adjacent white matter; this determination is made only in the cerebral cortex; the signal uptake in the cerebellum does not contribute to the scan interpretation (for example, a positive scan may show retained cerebellar gray-white contrast even when the cortical gray-white contrast is lost)
- Negative scans show more radioactivity in white matter than in gray matter, creating clear gray-white contrast
- Positive scans show cortical areas with reduction or loss of the normally distinct gray-white contrast; these scans have one or more areas with increased cortical gray matter signal which results in reduced (or absent) gray-white contrast
- Specifically, a positive scan will have either: a) 2 or more brain areas (each larger than a single cortical gyrus) in which there is reduced or absent gray-white contrast; this is the most common appearance of a positive scan, OR b) 1 or more areas in which gray matter radioactivity is intense and clearly exceeds radioactivity in adjacent white matter
- See figures of PET images in the prescribing information for further information
Not indicated
Adverse Effects
1-10%
Headache (1.8%)
<1%
Musculoskeletal pain (0.8%)
Fatigue (0.6%)
Nausea (0.6%)
Anxiety (0.4%)
Back pain (0.4%)
Increased blood pressure (0.4%)
Claustrophobia (0.4%)
Feeling cold (0.4%)
Insomnia (0.4%)
Neck pain (0.4%)
Warnings
Contraindications
None
Cautions
Risk for image misinterpretation
- Errors may occur in the estimation of brain neuritic plaque density during image interpretation; perform image interpretation independently of the patient’s clinical information
- Other errors may be due to extensive brain atrophy that limits the ability to distinguish gray and white matter on the scan as well as motion artifacts that distort the image
Radiation risk
- Similar to other radiopharmaceuticals, florbetapir F 18 contributes to a patient’s overall long-term cumulative radiation exposure; long-term cumulative radiation exposure is associated with an increased risk of cancer
- Ensure safe handling to protect patients and health care workers from unintentional radiation exposure
Pregnancy & Lactation
Pregnancy
There are no available data on use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes
All radiopharmaceuticals, have potential to cause fetal harm depending on stage of fetal development, and magnitude of radiopharmaceutical dose
If considering administration to a pregnant woman, inform patient about potential for adverse pregnancy outcomes based on radiation dose from drug and gestational timing of exposure
Lactation
There are no data on presence of drug or metabolites in human milk or effects on breastfed infant or milk production
Exposure to a breastfed infant can be minimized by temporary discontinuation of breastfeeding
The developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed child from drug or from underlying maternal condition
To decrease radiation exposure to breastfed infant, advise a lactating woman to interrupt breastfeeding, and pump and discard breast milk for 24 hours after administration of drug
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Binds to beta-amyloid plaques and the F 18 isotope produces a positron signal that is detected by a PET scanner
In in vitro binding studies using postmortem human brain homogenates containing beta-amyloid plaques, the dissociation constant (Kd) for florbetapir was 3.7± 0.3 nM
Distribution
Rapidly distributed throughout body
<5% of the injected F 18 radioactivity present in the blood by 20 minutes following administration, and less than 2% present by 45 minutes after administration
Elimination
Half-life: 109.77 minutes (F 18)
Excretion: Principally via feces (GI and bile), small amount in urine
Administration
IV Preparation
Must not be diluted
Inspect the radiopharmaceutical dose solution prior to administration and do not use it if it contains particulate matter or is discolored
Use aseptic technique and radiation shielding to withdraw solution
Assay the dose in a suitable dose calibrator prior to administration
Radiation safety
- Radioactive drug; handle with appropriate safety measures to minimize radiation exposure during administration
- Use waterproof gloves and effective shielding, including lead-glass syringe shields when handling
- Radiopharmaceuticals should only be used by or under the control of physicians 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 radiopharmaceuticals
IV Administration
Inject through a short IV catheter (~1.5 inches or less) to minimize the potential for adsorption of the drug to the catheter
Portions of the dose may adhere to longer catheters
Administer as single IV bolus injection in a total volume of 10 mL or less; follow bolus injection 0.9% NaCl IV flush
Not to exceed 50 mcg mass dose
Storage
Store at 25ºC (77°F); excursions permitted to 15-30ºC (59-86°F)
The product does not contain a preservative
Store within the original container or equivalent radiation shielding
This preparation is approved for use by persons under license by the Nuclear Regulatory Commission or the relevant regulatory authority of an Agreement State
Images
Formulary
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