technetium Tc 99m exametazime (Rx)

Brand and Other Names:Ceretec, Drax Exametazime

Dosing & Uses


Dosage Forms & Strengths

multi-dose vial kit (Ceretec)

  • 5 multidose powder vials each containing 0.5 mg exametazime
  • 5 vials of methylene blue injection USP 1%
  • 5 vials of 0.003 M Monobasic Sodium

single-dose vial kit (Drax Exametazime)

  • 5 single-dose vials, each vial containing lyophilized mixture of 0.5 mg exametazime

Regional cerebral flow scintigraphy


  • Approved for Ceretec
  • Indicated for regional cerebral blood flow scintigraphy with or without methylene blue stabilization
  • Brain perfusion single-photon emission computed tomography (SPECT) imaging is a functional nuclear imaging technique performed to evaluate regional cerebral perfusion; technetium Tc 99m exametazime is injected into the patient; 3-dimensional (3D) representation of cerebral blood flow can be iterated using gamma detectors, allowing for interpretation


  • Recommended dose: 370-740 MBq (10-20 mCi) IV
  • Dynamic imaging: Administer <10 minutes prior to examination
  • Planar/tomographic imagining: Administer 15 minutes-6 hr prior to examination

Leukocyte-labeled scintigraphy


  • Indicated for leukocyte labeled scintigraphy as an adjunct in the localization of intra-abdominal infection and inflammatory bowel disease


  • Recommend dosage range for technetium Tc 99m exametazime labeled leukocytes: 259-925 IV MBq [7-25 millicuries (mCi)] IV
  • Administer at least 30 minutes prior serial pelvic and abdominal imaging
  • Complete procedures within 4 hr postinjection; see Administration

Dosage Modifications

Renal impairment

  • Technetium Tc 99m exametazime is substantially excreted by the kidneys, so excretion is decreased/delayed and therefore radiation exposure is greater in renally impaired patients; a reduction in administered Tc 99m can be considered provided an adequate number of labeled WBCs are administered

Dosing Considerations

To minimize radiation dose to the bladder, the patient should be encouraged to void when the examination is completed and as often thereafter as possible; adequate hydration should be encouraged to permit frequent voiding

Following the administration of Tc99m exametazime injection (Ceretec) with methylene blue stabilizer, urine discoloration may occur

Safety and efficacy not established

Dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal or cardiac function, and of concomitant disease or other drug therapy



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                    Adverse Effects

                    Frequency Not Defined

                    Hypersensitivity, including anaphylaxis

                    Postmarketing Reports

                    Cardiovascular: Transient blood pressure increase

                    Skin and subcutaneous tissue disorders: Rash, generalized erythema, urticaria, angioedema, pruritus

                    General disorders and administration site conditions: Facial edema, fever, asthenic conditions (eg, malaise, fatigue)

                    Nervous system disorders: Headache, dizziness, paresthesia

                    Vascular disorders: Flushing

                    Gastrointestinal disorders: Nausea, vomiting






                    Hypersensitivity reactions, including serious signs and symptoms of anaphylaxis, following administration of Tc 99m labeled leukocytes prepared using Tc 99m exametazime have been reported; monitor for hypersensitivity reactions and always have cardiopulmonary resuscitation equipment and personnel available

                    Image interpretation may be affected by presence of other pathophysiological processes within and outside of the abdominal cavity (eg, tumor, infarction, trauma, and other inflammatory conditions)

                    Technetium Tc 99m 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 and preparation reconstitution procedures to protect patients and health care workers from unintentional radiation exposure; encourage patients to drink fluids and void as frequently as possible after administration


                    Pregnancy & Lactation


                    Limited available data with technetium Tc 99m exametazime use in pregnant women are insufficient to inform a drug associated risk for major birth defects and miscarriage

                    Animal reproduction studies with technetium Tc 99m exametazime have not been conducted

                    Inform patients who are pregnant or may become pregnant about the potential for adverse pregnancy outcomes based on the radiation dose from technetium Tc 99m exametazime and the gestational timing of exposure

                    Limited data describes technetium Tc 99m exametazime crossing the placental barrier and visualization of radioactivity in the fetal liver; no adverse fetal effects or radiation-related risks have been identified for diagnostic procedures involving less than 50 mGy, which represents less than 10 mGy fetal doses


                    Unknown if distributed in human breast milk

                    To decrease radiation exposure to the breastfed infant, advise a lactating woman to pump and discard breast milk after administration of technetium Tc 99m exametazime-labeled leukocytes for 12-24 hours, where the duration corresponds to the typical range of administered activity, 259-925 MBq (7-25 mCi)

                    Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug, and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition

                    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

                    The addition of technetium Tc 99m pertechnetate to exametazime in the presence of stannous reductant, a lipophilic technetium Tc 99m complex is formed; this lipophilic complex is the active moiety; lipophilic technetium Tc 99m exametazime complex is taken up and retained in leukocytes


                    <1 hr postinjection: Radioactivity is seen in lungs, liver, gall bladder, spleen, blood pool, bone marrow, kidneys, and bladder

                    First 1-6 hr postinjection: Tc 99m is visualized in the bowel

                    24 hr postinjection: Substantial colonic activity is seen; normal areas visualized in earlier scans are still visible


                    Half-life: Physical: ~6 hr

                    Excretion: Urine and kidneys (~40%); Feces (~50%)



                    Technetium Tc 99 Exametazime Preparation

                    Contents of vial are sterile and pyrogen free; vial contains no bacteriostatic preservative; follow the directions carefully and adhere to strict aseptic procedures during preparation of the radiopharmaceutical; see full prescribing information for detailed instructions

                    0.37 – 2 GBq (10 - 54 mCi) technetium Tc99m may be added to the vial

                    Before reconstitution the technetium Tc99m generator eluate may be adjusted to the correct radioactive concentration to a volume of 5 mL by dilution with preservative-free, nonbacteriostatic 0.9% sodium chloride for injection

                    Use only eluate from a technetium Tc99m generator which was previously eluted within 24 hr; generator eluate >2 hr old should not be used; for the highest radiochemical purity reconstitute with freshly eluted technetium Tc99m generator eluate

                    Radiochemical purity testing must be performed prior to patient administration; radiochemical purity >80% is necessary for product acceptance

                    Do not use the final radiopharmaceutical preparation more than 30 minutes after the time of reconstitution; discard any unused material

                    Ceretec preparation

                    • When reconstituting a vial of Ceretec with 31-54 mCi, generator eluate more than 30 minutes old should not be used
                    • Do not use methylene blue stabilizer for leukocyte labeling procedure

                    Administration for Leukocyte Labeled Scintigraphy

                    Use strict aseptic procedures throughout preparation and handling

                    Visually inspect reconstituted technetium Tc 99m exametazime solution for particulate matter and discoloration prior to radiolabeling of white blood cells

                    Do not use the reconstituted solution if there is evidence of particulate matter or discoloration

                    Follow the directions of drug preparation carefully to ensure efficient leukocytes labeling

                    Measure patient dose with a suitable radioactivity calibration system immediately prior to administration

                    Instruct patients to hydrate, after administration of technetium Tc 99m exametazime labeled white blood cells and void frequently to minimize radiation dose to the kidneys and bladder

                    Storage for All Formulations

                    Unopened kit

                    • Store in original packaging at controlled room temperature 15-25°C (59-77°F)

                    Reconstituted product

                    • Store reconstituted injection at 20-25°C (68-77°F) using appropriate radiation shielding
                    • Expiration of radiolabeled product
                      • Ceretec with methylene blue stabilizer: 4 hr post-preparation
                      • Ceretec without methylene blue stabilizer: 30 minutes post-preparation Drax Exemestane: 4 hr post-preparation


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                    Patient Handout

                    A Patient Handout is not currently available for this monograph.


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