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Ioflupane I 123

Pronunciation: EYE-oh-FLOO-pane
Class: Diagnostic aid

Trade Names

DaTscan
- Injection, solution 74 MBq (2 mCi) per mL at calibration

Pharmacology

In vitro, ioflupane binds reversibly to the human recombinant dopamine transporter (DaT). Autoradiography of postmortem human brain slices exposed to radiolabeled ioflupane shows concentration of the radiolabel in striatum (caudate nucleus and putamen). Following administration of ioflupane I 123 to humans, radioactive decay of the iodine 123 emits gamma radiation that can be detected externally using gamma detectors, allowing visualization of the brain striata through single-photon emission computed tomography (SPECT) imaging.

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Pharmacokinetics

Absorption

Only 5% of the administered radioactivity remained in whole blood at 5 minutes postinjection. Uptake in the brain reached approximately 7% of injected radioactivity at 10 minutes postinjection and decreased to 3% after 5 hours; striata to background ratios were relatively constant between 3 and 6 hours postinjection. Approximately 30% of the whole brain radioactivity was attributed to striatal uptake.

Elimination

By 48 hours postinjection, approximately 60% of the injected radioactivity has been excreted in the urine, with fecal excretion estimated to be approximately 14%.

Special Populations

Renal Function Impairment

No data available.

Hepatic Function Impairment

No data available.

Indications and Usage

For striatal dopamine transporter visualization using SPECT brain imaging to assist in the evaluation of adult patients with suspected parkinsonian syndromes.

Contraindications

Known hypersensitivity to the active substance or to any of the excipients, or to iodine.

Dosage and Administration

Brain imaging
Adults

IV 111 to 185 MBq (3 to 5 mCi).

General Advice

  • Radiopharmaceuticals should be used by or under the control of physicians who are qualified by specific training and experienced in the safe use and handling of radionuclides, and whose experience and training have been approved by the appropriate government agency authorized to license the use of radionuclides.
  • Encourage hydration prior to and following administration in order to permit frequent voiding. Encourage the patient to void frequently for the first 48 hours following administration.
  • Before administration, administer potassium iodide oral solution or Lugol solution (equivalent to iodide 100 mg) or potassium perchlorate (400 mg) to block uptake of iodine 123 by the patient's thyroid. Administer the blocking agent at least 1 hour before the dose of ioflupane I 123.
  • Use aseptic procedures and radiation shielding during preparation and administration.
  • Administer as a slow IV injection (administered over a period of not less than 15 to 20 seconds) via an arm vein.

Storage/Stability

Store between 68° and 77°F. Store within the original lead container or equivalent radiation shielding.

Drug Interactions

Amoxapine, amphetamine, benztropine, bupropion, buspirone, cocaine, methamphetamine, methylphenidate, phentermine, selegiline, and sertraline

Because ioflupane binds to the dopamine transporter, drugs that bind to the dopamine transporter with high affinity, such as amoxapine, may interfere with the image obtained following ioflupane I 123 administration.

Selective serotonin reuptake inhibitors (eg, citalopram, paroxetine)

May increase or decrease ioflupane binding to the dopamine transporter. It is not known whether discontinuation of these drugs prior to ioflupane I 123 administration may minimize the interference with an ioflupane I 123 image.

Adverse Reactions

CNS

Dizziness, headache, vertigo (1% or less).

GI

Dry mouth, nausea (1% or less).

Miscellaneous

Hypersensitivity reactions (eg, rash, pruritus), injection-site pain (postmarketing).

Precautions

Pregnancy

Category C . Radioactive iodine products cross the placenta and can permanently impair fetal thyroid function.

Lactation

Undetermined. Breast-feeding women may consider interrupting breast-feeding and pumping and discarding breast milk for 6 days after administration in order to minimize risks to a breast-feeding infant.

Children

Not indicated for use in children.

Hypersensitivity

Hypersensitivity reactions have been reported and have generally consisted of skin erythema and pruritus.

Renal Function

Patients with severe renal impairment may have increased radiation exposure and altered ioflupane I 123 images.

Thyroid accumulation

Ioflupane I 123 injection may contain up to 6% of free iodide (iodine 123). To decrease thyroid accumulation of iodine 123, block the thyroid gland before administration. Failure to block thyroid uptake of iodine 123 may result in an increased long-term risk for thyroid neoplasia.

Overdosage

Symptoms

Neoplasia.

Patient Information

  • Instruct patients to inform their physician or health care provider if they have reduced renal or hepatic function, are sensitive to ioflupane I 123, are sensitive to potassium iodide oral solution or Lugol solution, and/or may be pregnant, are trying to become pregnant, or are breast-feeding.
  • Instruct patients to increase their level of hydration prior to and after receiving ioflupane I 123, and to void frequently for the first 48 h following administration.

Copyright © 2009 Wolters Kluwer Health.

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