Florbetapir F 18 is an intravenous, radioactive, diagnostic agent used to estimate beta-amyloid neuritic plaque density. It is approved for use with Positron Emission Tomography (PET) brain imaging to evaluate adults for Alzheimer's Disease (AD) or other causes of cognitive decline. A positive PET scan is indicated by the presence of moderate (6-19) to frequent (>= 20) beta-amyloid plaques; a negative scan indicates sparse (1-5) to no plaques. A study has shown that readers undergoing special training were able to interpret the scans with 92% sensitivity and 100% specificity. Florbetapir F 18 PET imaging is only intended for use as an adjunct to other diagnostic tests and does not establish a diagnosis of AD or other cognitive disorders. Additionally, the images cannot be used to predict development of neurologic conditions nor response to therapy. Florbetapir F 18 was approved by the FDA in April 2012.
General Administration Information
For storage information, see the specific product information within the How Supplied section.
-NOTE: Florbetapir F 18 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 should only be used 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
-For intravenous (IV) use only.
-To minimize radiation exposure, vials are shipped in a shielded container; maintain adequate shielding, including lead-glass syringe shields, during the life of the product.
-Use waterproof gloves during the entire handling and administration process.
-Visually inspect parenteral products for particulate matter and discoloration. The solution is clear and colorless; discard if the vial contains particulate matter or if the solution is discolored.
-Do not dilute.
-Do not use after the expiration date on the container label.
Intravenous Administration
-Using aseptic technique and radiation shielding, withdraw the appropriate dose immediately prior to administration.
-Assay the dose in a suitable dose calibrator.
-Administer via bolus injection through a short IV catheter (1.5 inches or less). Due to drug adsorption, long catheters are not recommended.
-Initiate the positron emission tomography (PET) scan 30-50 minutes after drug administration.
No serious adverse reactions were observed following use of florbetapir F 18 during clinical trials. The most frequently reported reactions were headache (1.8%), musculoskeletal pain (0.7%), hypertension or increased blood pressure (0.7%), nausea (0.7%), fatigue (0.5%), and injection site reaction (bleeding, irritation, pain; 0.5%). Adverse events occurring in 0.4% of the drug recipients included anxiety, back pain, claustrophobia, chills or feeling cold, dizziness, insomnia, and neck pain. Cases of infusion site rash (unspecified), pruritus, urticaria, flushing, and dysgeusia also occurred; however, the frequency was not reported by the manufacturer.
Florbetapir F 18 positron emission tomography (PET) images are to be interpreted independent of the patients clinical features by individuals who have successfully completed a special training program provided by the manufacturer. Use of clinical information may lead to misinterpretations. Errors may also result from extensive brain atrophy and motion artifacts. In cases where there is uncertainty, readers are advised to use a computerized tomography (CT) image, if available, to clarify location of PET radioactivity to the gray matter anatomy. Florbetapir F 18 PET images are to be used as an adjunct to other diagnostic tests. Additionally, the images will not predict development of neurologic conditions nor response to therapy.
Florbetapir F 18 should be used only by nuclear physicians and/or radiopharmacists who are qualified by 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. Care should be taken to assure minimum accidental exposure of radiation to occupational workers, including use of waterproof gloves and effective shielding. Furthermore, care should be taken to minimize radiation exposure to the patient by proper patient management before, during, and after the procedure.
Florbetapir F 18 is not approved for use in neonates, infants, children, or adolescents.
There are no available data on florbetapir F 18 use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. Animal reproduction studies have not been conducted with florbetapir F 18 to evaluate its effect on female reproduction and embryofetal development. All radiopharmaceuticals, including florbetapir F 18, have the potential to cause fetal harm depending on the stage of fetal development and the magnitude of the radiopharmaceutical dose. If considering florbetapir F 18 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.
There are no data on the presence of florbetapir F 18 in human milk, the effects on the breast-fed infant, or the effects on milk production. Lactation studies have not been conducted in animals. Exposure of florbetapir F 18 to a breast-fed infant can be minimized by temporary discontinuation of breast-feeding; advise a breast-feeding woman to pump and discard breast milk for 24 hours (more than 10 half-lives of radioactive decay for the F 18 isotope) after administration of florbetapir F 18. Consider the developmental and health benefits of breast-feeding along with the mother's clinical need for florbetapir F18 and any potential adverse effects on the breast-fed child from florbetapir F 18 or the underlying maternal condition.
Florbetapir F 18 may be associated with reproductive risk. Assess pregnancy status of any female of reproductive potential by pregnancy testing before administering florbetapir F 18.
For use during positron emission tomography (PET) imaging of the brain to estimate beta-amyloid plaque density in adults being evaluated for Alzheimer's Disease and other causes of cognitive decline:
NOTE: Not indicated to predict the development of a neurologic condition nor for monitoring response to therapy.
NOTE: This drug is a radiopharmaceutical and should only be administered by individuals specifically trained in the handling of radioactive material. Must be dispensed from a radiopharmacy to the imaging center within several hours, because the drug looses over half its radioactivity every two hours.
NOTE: Dosage measured in megabecquerels (MBq) and millicuries (mCi).
Intravenous dosage:
Adults: 370 MBq (10 mCi) by a single IV bolus injection followed by 0.9% sodium chloride flush. Initiate a 10 minute PET image scan 30-50 minutes after the bolus injection. The images should only be interpreted by readers who have successfully completed a special training program provided by the manufacturer of florbetapir F18. In a study involving 59 terminally ill patients (29 with Alzheimer's Disease, 13 with other dementing disorder, 12 with no cognitive impairment, 5 with mild cognitive impairment), 5 trained readers interpreted florbetapir F 18 PET images of the brain with 92% sensitivity (95% CI: 78%-98%) and 100% specificity (95% CI: 80%-100%).
Children and Adolescents: Not indicated.
Maximum Dosage Limits:
-Adults
370 MBq (10 mCi) IV per procedure.
-Geriatric
370 MBq (10 mCi) IV per procedure.
-Adolescents
Safety and efficacy have not been established.
-Children
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
There are no drug interactions associated with Florbetapir F 18 products.
Florbetapir F 18 is a radiopharmaceutical used to estimate beta-amyloid plaque density in the brain. Following intravenous administration, the drug diffuses across the blood-brain barrier and binds to beta-amyloid aggregates, if present. Any areas of the brain that contain beta-amyloid plaques will retain the drug; in all other areas, the drug is remove by cerebral perfusion. Once bound, the F 18 isotope produces a positron signal (for up to at least 90 minutes post-injection) that can be detected by a positron emission tomography (PET) scan. A positive scan indicates moderate (6-19) to frequent (>= 20) neuritic plaque counts and a negative scan indicates none to sparse (1-5) counts. These scans, in conjunction with other diagnostic tests, are used to evaluate patients for Alzheimer's Disease and other causes of cognitive decline.
Florbetapir F 18 is administered intravenously. Once administered, the drug rapidly distributes throughout the body with < 5% remaining in the serum after 20 minutes and < 2% remaining by 45 minutes. The majority of the drug that remains in circulation is a polar F 18 metabolite. The drug crosses the blood-brain barrier and, unless bound to beta-amyloid plaques, is subsequently removed by cerebral perfusion. It also accumulates in the liver within 4 minutes of administration, and is mainly eliminated by the biliary/gastrointestinal tract; limited amounts are excreted in the urine as the polar metabolite.
-Route-Specific Pharmacokinetics
Intravenous Route
The amount of radiation absorbed following exposure to the recommended florbetapir F 18 dose is 7 mSv; use of a computerized tomography (CT) scan increases exposure to 9 mSv. The products radioactive half-live is 109 minutes.