flutemetamol F 18 (Rx)

1-10%

Flushing (2%)

Increased blood pressure (2%)

Headache (1%)

Nausea (1%)

Dizziness (1%)

Contraindications

Contraindicated in patients with a history of hypersensitivity reaction, polysorbate 80, or any other inactive ingredient

Cautions

Hypersensitivity reactions (eg, flushing and dyspnea) have been observed within minutes following administration; these reactions may occur in patients with no history of prior exposure

Before initiating therapy, ask patients about prior reactions to drugs, especially those containing polysorbate

Resuscitation equipment and trained personnel should be immediately available

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 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

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.

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 flutemetamol was 6.7 nM

Distribution

Rapidly distributed throughout body

The time-activity curves for flutemetamol F 18 in the brain of subjects with positive scans shows continual signal increases from time zero through 30 minutes post administration, with stable values thereafter up to at least 120 minutes post-injection

Elimination

Excretion: 37% renal; 52% hepatobiliary

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 with 5-15 mL of 0.9% NaCl IV flush

Storage

Store at 2-30ºC (36-86°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