Drug Interaction:
Pharmacodynamic drug-drug interaction studies have not been performed in patients
to establish the effects
Within a clinical study of patients with a range of cognitive impairment, some
patients with probable AD were receiving the following medications: donepezil,
galantamine, memantine.
Mean cortical Standardized Uptake Value (SUV) ratios did not differ between the
patients taking or not taking these concomitant medications.
In in vitro tests, none of the drugs tested, including the acetylcholinesterase
inhibitors donepezil, galantamine, and tacrine, altered florbetapir F 18
binding to its target.
Indication:
Amyvid (Florbetapir F 18 Injection) for intravenous use
Initial U.S. Approval: 2012
Drug Name- Amyvid
Active Ingredient - Florbetapir 18
Used as radioactive diagnostic aid for Positron Emmission Tomography (PET)
imaging of the brain to estimate Beta-amyloid neuritic plaque in adults who are
being evaluated for Alzehimers disease(AD) and other causes for cognitive decline
Indication-
Used as radioactive diagnostic aid for Positron Emission Tomography (PET)
imaging of the brain to estimate Beta-amyloid neuritic plaque in adults who are
being evaluated for Alzehimers disease(AD) and other causes for cognitive decline
Approved by FDA on 6-4-2012 (Ref- FDA Approved List- 2012)
Adverse Reaction:
The most common reported adverse reaction was headache, occurring in
2% of patients, followed by musculoskeletal pain, blood pressure increased,
fatigue, nausea, and injection site reaction, all occurring in <1% of patients
Contra-Indications:
CONTRAINDICATIONS
None
WARNINGS AND PRECAUTIONS
Image interpretation errors (especially false negatives) have been observed (
Radiation risk: Amyvid, similar to all radiopharmaceuticals, contributes to a
patient’s long-term cumulative radiation exposure.
Ensure safe handling to protect patients and health care workers from
unintentional radiation exposure
Dosages/ Overdosage Etc:
Active Ingredient - Florbetapir 18
INDICATIONS AND USAGE
Amyvid is a radioactive diagnostic agent for Positron Emission Tomography (PET)
imaging of the brain to estimate â-amyloid neuritic plaque density in adult patients
with cognitive impairment who are being evaluated for Alzheimer’s Disease (AD)
and other causes of cognitive decline.
A negative Amyvid scan indicates sparse to no neuritic plaques, and is inconsistent
with a neuropathological diagnosis of AD at the time of image acquisition; a negative
scan result reduces the likelihood that a patient’s cognitive impairment is due to AD.
A positive Amyvid scan indicates moderate to frequent amyloid neuritic plaques;
neuropathological examination has shown this amount of amyloid neuritic plaque
is present in patients with AD, but may also be present in patients with other types
of neurologic conditions as well as older people with normal cognition.
Amyvid is an adjunct to other diagnostic evaluations
Limitations of Use
A positive Amyvid scan does not establish a diagnosis of AD or other cognitive disorder
Safety and effectiveness of Amyvid have not been established for:
Predicting development of dementia or other neurologic condition;
Monitoring responses to therapies
DOSAGE AND ADMINISTRATION
Use appropriate radiation safety handling measures
Administer 370 MBq (10 mCi) as a single intravenous bolus in a total volume
of 10 mL or less
Obtain 10-minute PET images starting approximately 30 to 50 minutes after
intravenous injection
Image interpretation: Refer to full prescribing information
The radiation absorbed dose from a 370 MBq (10 mCi) dose of Amyvid
is 7 mSv in an adult
DOSAGE FORMS AND STRENGTHS
10mL, 30 mL, or 50 mL multidose vial containing a clear, colorless injectable
solution at a strength of 500-1900 MBq/mL (13.5-51 mCi/mL) florbetapir
F 18 at End of Synthesis (EOS)
Patient Information:
PATIENT COUNSELING INFORMATION
Instruct patients to inform their physician or healthcare provider if they are pregnant
or breastfeeding.
Inform patients who are breastfeeding to use alternate infant nutrition sources
(e.g., stored breast milk or infant formula) for 24 hours (>10 half-lives of radioactive
decay for the F 18 isotope) after administration of the drug or avoid use of the drug.
Pharmacology/ Pharmacokinetics:
1. Mechanism of Action
Florbetapir F 18 binds to â-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 â-amyloid plaques, the dissociation
constant (K d) for florbetapir was 3.7 ± 0.3 nM.
2.Pharmacokinetics
Following the intravenous administration of 370 MBq (10 mCi) of florbetapir F 18
to healthy volunteers, the drug was distributed throughout the body with less
than 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.
The residual F 18 in circulation during the 30-90 minute imaging window was
principally in the form of polar F 18 metabolites.
Whole body scanning following the intravenous injection showed accumulation
of radioactivity in the liver within four minutes post-injection, followed by elimination
of the radioactivity predominantly through the biliary/gastrointestinal tract with much
lower radioactivity detected in the bladder. Essentially all radioactivity collected
in the urine was present as polar metabolites of florbetapir F 18.
Pregnancy and lactation:
USE IN SPECIFIC POPULATIONS
1. Pregnancy
Pregnancy Category C.
It is not known whether Amyvid can affect reproductive capacity
or cause fetal harm when administered to a pregnant woman.
Animal reproduction studies have not been conducted with Amyvid.
Amyvid should be administered to a pregnant woman only if clearly needed.
All radiopharmaceuticals, including Amyvid, have a potential to cause fetal harm.
Assess pregnancy status before administering Amyvid to a female of reproductive
potential.
2. Nursing Mothers
It is not known whether Amyvid is excreted in human milk.
Because many drugs are excreted into human milk and because of the potential
for radiation exposure to nursing infants from Amyvid, avoid use of the drug in
a breastfeeding mother or have the mother temporarily interrupt breastfeeding
for 24 hours (>10 half-lives of radioactive decay for the F 18 isotope)
after exposure to Amyvid.
If breastfeeding is interrupted, the patient should pump and discard her breast milk
and use alternate infant nutrition sources (e.g., stored breast milk or infant formula)
for 24 hours after administration of the drug.
3. Pediatric Use
Amyvid is not indicated for use in pediatric patients.
4. Geriatric Use
Of 496 patients in completed clinical studies of Am yvid, 307 patients were
.65 years old (203 patients were over 75 years of age).
No overall differences in safety or effectiveness were observed between these
subjects and younger subjects.
Manufacturer Details