Dosing & Uses
Dosage Forms & Strengths
injectable solution
- 50-5000 MBq/mL (1.4-135 mCi/mL) in 30 mL multi-dose vials
- At time of administration, 300 MBq (8.1 mCi) are contained in up to 10 mL solution for injection
Beta-Amyloid Plaque Estimation
Radioactive, adjunctive diagnostic agent indicated 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 those with other types of neurologic conditions, as well as in older people with normal cognition
Dosage
- 300 megabecquerels (MBq), ie, 8.1 millicuries (mCi) IV bolus administered by slow IV bolus (1 mL/6 seconds) in a total volume of up to 10 mL
- Follow injection with an IV flush of 10 mL of 0.9% NaCl
Image Display & Interpretation
A 15 to 20-minute PET image should be acquired starting 45-130 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 used
Display
- Display images in the transaxial orientation using gray scale or inverse gray scale
- Sagittal and coronal planes may be used for additional orientation purposes
- CT or MR images may be helpful for anatomic reference purposes; however, visual assessment should be performed using the axial planes according to the recommended reading methodology
Interpretation
- Visually compare the activity in cortical gray matter with activity in adjacent white matter Regions displayed in the PET images which ‘anatomically’ correspond to white matter structures (eg, the cerebellar white matter or the splenium) should be identified to help the readers orient themselves
- View and assess images in a systematic manner, starting with the cerebellum and scrolling up through the lateral temporal and frontal lobes, the posterior cingulate cortex/precuneus, and the parietal lobes
- For a gray matter cortical region to be assessed as showing "tracer uptake" the majority of slices from the respective region must be affected
- For each patient, the PET image assessment is categorized as either beta-amyloid-positive or beta-amyloid-negative
- Beta-amyloid negative: Tracer uptake (ie, signal intensity) in gray matter is lower than in white matter in all 4 brain regions (no beta-amyloid deposition)
- Beta-amyloid positive: Smaller area(s) of tracer uptake equal to or higher than that present in white matter extending beyond the white matter rim to the outer cortical margin involving the majority of the slices within at least 1 of the 4 brain regions (moderate beta-amyloid deposition), or a large confluent area of tracer uptake equal to or higher than that present in white matter extending beyond the white matter rim to the outer cortical margin and involving the entire region, including the majority of slices within at least 1 of the 4 brain regions (pronounced beta-amyloid deposition)
- See figures of PET images in the prescribing information for further information
Not indicated
Adverse Effects
1-10%
Injection site pain (3.9%)
Injection site erythema (1.7%)
Injection site irritation (1.2%)
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, flutemetamol F18 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 healthcare workers from unintentional radiation exposure
Pregnancy & Lactation
Pregnancy
There are no available data on pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes
Animal data
- Animal reproduction studies have not been conducted; all radiopharmaceuticals, have a 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 in human milk, effects on breastfed infant, or on milk production; exposure to a breastfed infant can be minimized by temporary discontinuation of breastfeeding
Developmental and health benefits of breastfeeding should be considered along with mother's clinical need for drug and any potential adverse effects on breastfed child from drug from underlying maternal condition
To decrease radiation exposure to breastfed infant, advise a lactating woman to 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
F18-labeled stilbene derivative that binds to beta-amyloid plaques in the brain which produces a positron signal that is detected by a PET scanner
Distribution
10 minutes after IV bolus injection of 300 MBq, ~6% of the injected radioactivity was distributed to the brain
Plasma concentrations declined by ~75% at 20 minutes postinjection, and by ~90% at 50 minutes
The F18 in circulation during the 45 to 130-minute imaging window was principally associated with polar metabolites of florbetaben
Protein bound: 98.5%
Metabolism
Predominantly catalyzed by CYP2J2 and CYP4F2
Elimination
Half-life: 1 hr
Excretion: Primarily via hepatobiliary route; 30% urine (mostly as polar metabolites)
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 by whose experience and training have been approved by the appropriate governmental agency authorized to license the use of radiopharmaceuticals
IV Administration
The injection must be IV in order to avoid irradiation as a result of local extravasation, as well as imaging artifacts
Verify patency of the indwelling catheter by a saline test injection prior to administration
Inject IV bolus (6 sec/mL) into a large vein in the arm, followed by a saline flush of approximately 10 mL
Storage
Store at room temperature 25ºC (77°F); excursions permitted to 2-42°C (36-108°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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