Dosing & Uses
Dosage Forms & Strengths
intravenous injection: Schedule II
- 185 MBq/2.5mL
Dopamine Transporter Visualization
Radiopharmaceutical indicated for
- Striatal dopamine transporter visualization using single photon emission computed tomography (SPECT) brain imaging to assist in the evaluation of adults with suspected Parkinsonian syndromes (PS) or suspected dementia with Lewy bodies (DLB)
- Help differentiating essential tremor from tremor due to PS (idiopathic Parkinson disease, multiple system atrophy and progressive supranuclear palsy)
Dose
- Measure dose by a suitable radioactivity calibration system immediately before administering
- Administer thyroid-blocking agent (eg, potassium iodide oral solution, potassium perchlorate) at least 1 hr before dose
- Recommended dose is 111-185 MBq (3-5 mCi)
- Begin SPECT imaging 3-6 hr post-injection
-
Thyroid blockade
- Administer 1 hr before DaTscan dose
- Potassium iodide oral solution (or Lugol’s Solution) equivalent to 100 mg iodide, OR
- Potassium perchlorate 400 mg
Renal Impairment
Excreted by kidneys
Severe renal impairment may increase radiation exposure to patient and alter images
Safety and efficacy not established
In the 2 principal clinical studies, 45% of the subjects were aged 65 yr or older
There were no differences in response compared to younger subjects that would require a dose adjustment
Other reported clinical experience has not identified differences in responses between the elderly and younger patients
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (0)
Monitor Closely (18)
- amoxapine
amoxapine decreases effects of ioflupane I 123 by receptor binding competition. Use Caution/Monitor. Drugs that bind to dopamine transporter receptor with high affinity may interfere with the image following ioflupane I123 administration.
- benztropine
benztropine decreases effects of ioflupane I 123 by receptor binding competition. Use Caution/Monitor. Drugs that bind to dopamine transporter receptor with high affinity may interfere with the image following ioflupane I 123 administration.
- bupropion
bupropion decreases effects of ioflupane I 123 by receptor binding competition. Use Caution/Monitor. Drugs that bind to dopamine transporter receptor with high affinity may interfere with the image following ioflupane I 123 administration.
- buspirone
buspirone decreases effects of ioflupane I 123 by receptor binding competition. Use Caution/Monitor. Drugs that bind to dopamine transporter receptor with high affinity may interfere with the image following ioflupane I 123 administration.
- citalopram
citalopram decreases effects of ioflupane I 123 by receptor binding competition. Use Caution/Monitor. Drugs that bind to dopamine transporter receptor with high affinity may interfere with the image following ioflupane I 123 administration.
- cocaine topical
cocaine topical decreases effects of ioflupane I 123 by receptor binding competition. Use Caution/Monitor. Drugs that bind to dopamine transporter receptor with high affinity may interfere with the image following ioflupane I 123 administration.
- dextroamphetamine
dextroamphetamine decreases effects of ioflupane I 123 by receptor binding competition. Use Caution/Monitor. Drugs that bind to dopamine transporter receptor with high affinity may interfere with the image following ioflupane I 123 administration.
- escitalopram
escitalopram decreases effects of ioflupane I 123 by receptor binding competition. Use Caution/Monitor. Drugs that bind to dopamine transporter receptor with high affinity may interfere with the image following ioflupane I 123 administration.
- iodixanol
iodixanol decreases effects of ioflupane I 123 by unknown mechanism. Use Caution/Monitor. Administration of iodinated contrast agents may interfere with thyroid uptake of radioactive iodine (I-131 and I-123) and decrease therapeutic and diagnostic efficacy in patients with thyroid carcinoma. Decreased efficacy lasts for 6-8 weeks. .
- metformin
ioflupane I 123 increases toxicity of metformin by unspecified interaction mechanism. Modify Therapy/Monitor Closely. Administration of intravascular iodinated contrast agents in metformin-treated patients has led to rare cases of acute decrease in renal function and the occurrence of lactic acidosis. The American College of Radiology Guidelines (2018) recommend temporarily stopping metformin in patients with eGFR is <30 mL/min/1.73 m2 or who are undergoing arterial catheter studies that might result in emboli to the renal arteries. Continue to withhold metformin for 48 hr subsequent to the procedure and reinstituted only after renal function has been reevaluated and found to be normal. .
- methamphetamine
methamphetamine decreases effects of ioflupane I 123 by receptor binding competition. Use Caution/Monitor. Drugs that bind to dopamine transporter receptor with high affinity may interfere with the image following ioflupane I 123 administration.
- norepinephrine
norepinephrine decreases effects of ioflupane I 123 by receptor binding competition. Use Caution/Monitor. Drugs that bind to dopamine transporter receptor with high affinity may interfere with the image following ioflupane I 123 administration.
- paroxetine
paroxetine decreases effects of ioflupane I 123 by receptor binding competition. Use Caution/Monitor. Drugs that bind to dopamine transporter receptor with high affinity may interfere with the image following ioflupane I 123 administration.
- phentermine
phentermine decreases effects of ioflupane I 123 by receptor binding competition. Use Caution/Monitor. Drugs that bind to dopamine transporter receptor with high affinity may interfere with the image following ioflupane I 123 administration.
- selegiline
selegiline decreases effects of ioflupane I 123 by receptor binding competition. Use Caution/Monitor. Drugs that bind to dopamine transporter receptor with high affinity may interfere with the image following ioflupane I 123 administration.
- selegiline transdermal
selegiline transdermal decreases effects of ioflupane I 123 by receptor binding competition. Use Caution/Monitor. Drugs that bind to dopamine transporter receptor with high affinity may interfere with the image following ioflupane I 123 administration.
- sertraline
sertraline decreases effects of ioflupane I 123 by receptor binding competition. Use Caution/Monitor. Drugs that bind to dopamine transporter receptor with high affinity may interfere with the image following ioflupane I 123 administration.
- voclosporin
voclosporin, ioflupane I 123. Either increases toxicity of the other by nephrotoxicity and/or ototoxicity. Modify Therapy/Monitor Closely. Coadministration with drugs associated with nephrotoxicity may increase the risk for acute and/or chronic nephrotoxicity.
Minor (0)
Adverse Effects
<1%
Headache
Nausea
Dizziness
Vertigo
Xerostomia
Postmarketing Reports
Immune system disorders: Hypersensitivity, including dyspnea, edema, rash, erythema, and pruritus
General disorders and administration site conditions: Injection site pain
Warnings
Contraindications
Hypersensitivity to active substance, excipients, or iodine
Cautions
May cause hypersensitivity reactions depicted by skin erythema and pruritus; these reactions have generally occurred within minutes of administration and have either resolved spontaneously or following administration of corticosteroids and antihistamines; contraindicated with known hypersensitivity to ioflupane I 123; have treatment measures available and monitor patients for symptoms or signs of a hypersensitivity reaction
Thyroid accumulation of iodine-123 may occur; to decrease thyroid accumulation of Iodine-123, block the thyroid gland (eg, potassium iodide) before administration of therapy; failure to block thyroid uptake of I-123 may result in an increased long-term risk for thyroid neoplasia
Radiation risk
- Contributes to patient’s overall long-term cumulative radiation exposure and its associated increased risk for cancer
- Ensure safe handling to minimize radiation exposure to patients and clinicians
-
Bladder protection
- Minimize radiation dose to bladder by encouraging hydration before and following administration
- Encourage patient to void frequently for first 48 hr following administration
Drug interaction overview
- Drugs that bind to dopamine transporter with high affinity may interfere with image
- Effects of dopamine agonists and antagonists on ioflupane I 123 imaging have not been established
-
Drugs that may interfere with ioflupane binding include
- Amoxapine, amphetamine, armodafinil, benztropine, bupropion, buspirone, cocaine, mazindol, methamphetamine, methylphenidate, norephedrine, phentermine, phenylpropanolamine, selegiline, and sertraline
-
Drugs that may increase or decrease ioflupane binding include
- Citalopram and paroxetine
Pregnancy & Lactation
Pregnancy
Radioactive iodine products cross the placenta and can permanently impair fetal thyroid function; administration of an appropriate thyroid blocking agent is recommended before use in a pregnant woman to protect the woman and fetus from accumulation of iodine
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; advise pregnant women of potential risks of fetal exposure to radiation doses with administration of product
Animal data
- Animal reproduction studies have not been conducted with ioflupane I 123; all radiopharmaceuticals have the potential to cause fetal harm depending on fetal stage of development and magnitude of radiation dose; administration at a dose of 185 MBq (5 mCi) results in an absorbed radiation dose to uterus of 0.3 rad (3.0 mGy)
- Radiation doses >15 rad (150 mGy) have been associated with congenital anomalies but doses under 5 rad (50 mGy) generally have not
Lactation
Iodide 123 (I 123), the radionuclide, is present in human milk; there is no information on effects on breastfed infant or on milk production; advise a lactating woman to interrupt breastfeeding and pump and discard breastmilk for at least 6 days (>10 physical half-lives) after administration in order to minimize radiation exposure to a breastfed infant
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.Pharmacology
Mechanism of Action
Binds reversibly to the human recombinant dopamine transporter (DaT) (Ki = 0.62 nM; IC50 = 0.71 nM)
Following administration, radioactive decay of the iodine123 emits gamma radiation which can be detected externally using gamma detectors, allowing visualization of the brain striata through SPECT imaging
Pharmacokinetics
Half-Life: 13.2 hr
Brain uptake: 7% of injected radioactivity at 10 min post-injection; decreased to 3% at 5 hr post-injection
Onset: ~7% of radioactivity in brain within 10 min
Metabolism: Decays to 123Te by electron capture
Excretion: feces (14% by 48 hr), urine (60% by 48 hr)
Administration
IV Preparation
IV injection: Use aseptic procedures and radiation shielding during preparation and administration
Inspect vial before administering and discard if vial contains particulate matter or discoloration
IV Administration
Slow IV injection (administer over at least 15-20 seconds) via an arm vein
Have medications and medical support to respond to anaphylaxis readily available
Storage
Store within original lead container or equivalent radiation shielding
Do not use after expiration date and time stated on label
Emits radiation and must be handled with safety measures to minimize radiation exposure to clinical personnel and patients
Images
Patient Handout
ioflupane I 123 intravenous
NO MONOGRAPH AVAILABLE AT THIS TIME
USES: Consult your pharmacist.
HOW TO USE: Consult your pharmacist.
SIDE EFFECTS: Consult your pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Consult your pharmacist.
DRUG INTERACTIONS: Consult your pharmacist.Keep a list of all your medications with you, and share the list with your doctor and pharmacist.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.
NOTES: No monograph available at this time.
MISSED DOSE: Consult your pharmacist.
STORAGE: Consult your pharmacist.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.
Information last revised July 2016. Copyright(c) 2023 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
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