Ioflupane (
123I) is the
international nonproprietary name (INN) of a
cocaine analogue which is a neuro-imaging
radiopharmaceutical drug, used in
nuclear medicine
Nuclear medicine or nucleology is a medical specialty involving the application of radioactive substances in the diagnosis and treatment of disease. Nuclear imaging, in a sense, is "radiology done inside out" because it records radiation emitting ...
for the diagnosis of
Parkinson's disease
Parkinson's disease (PD), or simply Parkinson's, is a long-term degenerative disorder of the central nervous system that mainly affects the motor system. The symptoms usually emerge slowly, and as the disease worsens, non-motor symptoms becom ...
and the differential diagnosis of Parkinson's disease over other disorders presenting similar symptoms. During the
DaT scan procedure it is injected into a patient and viewed with a
gamma camera
A gamma camera (γ-camera), also called a scintillation camera or Anger camera, is a device used to image gamma radiation emitting radioisotopes, a technique known as scintigraphy. The applications of scintigraphy include early drug development ...
in order to acquire
SPECT
Single-photon emission computed tomography (SPECT, or less commonly, SPET) is a nuclear medicine tomographic imaging technique using gamma rays. It is very similar to conventional nuclear medicine planar imaging using a gamma camera (that is, ...
images of the
brain
A brain is an organ that serves as the center of the nervous system in all vertebrate and most invertebrate animals. It is located in the head, usually close to the sensory organs for senses such as vision. It is the most complex organ in a v ...
with particular respect to the
striatum
The striatum, or corpus striatum (also called the striate nucleus), is a nucleus (a cluster of neurons) in the subcortical basal ganglia of the forebrain. The striatum is a critical component of the motor and reward systems; receives glutamate ...
, a subcortical region of the
basal ganglia
The basal ganglia (BG), or basal nuclei, are a group of subcortical nuclei, of varied origin, in the brains of vertebrates. In humans, and some primates, there are some differences, mainly in the division of the globus pallidus into an extern ...
.
The drug is sold under the brand name Datscan and is manufactured by
GE Healthcare
GE HealthCare is a subsidiary of American multinational conglomerate General Electric incorporated in New York and headquartered in Chicago, Illinois. As of 2017, it is a manufacturer and distributor of diagnostic imaging agents and radiopharma ...
, formerly Amersham plc.
Pharmacology
Datscan is a solution of ioflupane (
123I) for injection into a living test subject.
The
iodine
Iodine is a chemical element with the symbol I and atomic number 53. The heaviest of the stable halogens, it exists as a semi-lustrous, non-metallic solid at standard conditions that melts to form a deep violet liquid at , and boils to a vi ...
introduced during manufacture is a radioactive
isotope
Isotopes are two or more types of atoms that have the same atomic number (number of protons in their nuclei) and position in the periodic table (and hence belong to the same chemical element), and that differ in nucleon numbers (mass numbers) ...
,
iodine-123, and it is the
gamma decay
A gamma ray, also known as gamma radiation (symbol γ or \gamma), is a penetrating form of electromagnetic radiation arising from the radioactive decay of atomic nuclei. It consists of the shortest wavelength electromagnetic waves, typically sh ...
of this isotope that is detectable to a gamma camera.
123I has a
half-life
Half-life (symbol ) is the time required for a quantity (of substance) to reduce to half of its initial value. The term is commonly used in nuclear physics to describe how quickly unstable atoms undergo radioactive decay or how long stable ato ...
of approximately 13 hours and a gamma photon energy of 159
keV making it an appropriate radionuclide for medical imaging. The solution also contains 5% ethanol to aid solubility and is supplied sterile since it is intended for intravenous use.
Ioflupane has a high binding affinity for presynaptic
dopamine
Dopamine (DA, a contraction of 3,4-dihydroxyphenethylamine) is a neuromodulatory molecule that plays several important roles in cells. It is an organic compound, organic chemical of the catecholamine and phenethylamine families. Dopamine const ...
transporters (
DAT) in the brains of mammals, in particular the
striatal region of the brain. A feature of Parkinson's disease is a marked reduction in
dopaminergic neurons
Dopaminergic cell groups, DA cell groups, or dopaminergic nuclei are collections of neurons in the central nervous system that synthesize the neurotransmitter dopamine. In the 1960s, dopaminergic neurons or ''dopamine neurons'' were first ident ...
in the striatal region. By introducing an agent that binds to the dopamine transporters a quantitative measure and spatial distribution of the transporters can be obtained.
Method of administration
The Datscan solution is supplied ready to inject with a certificate stating the calibration activity and time. The nominal injection activity is 185
MBq and a scan should not be performed with less than 111 MBq.
Thyroid blocking via oral administration of 120 mg
potassium iodide is recommended to minimize unnecessary excessive uptake of radioiodine.
This is typically given 1–4 hours before the injection.
The most convenient way to administer the IV dose is via a peripheral intravenous
cannula
A cannula (; Latin meaning 'little reed'; plural or ) is a tube that can be inserted into the body, often for the delivery or removal of fluid or for the gathering of samples. In simple terms, a cannula can surround the inner or outer surfaces ...
. The scan is carried out 3 to 6 hours post injection.
Risks
Common side effects of ioflupane (
123I) are headache, vertigo, increased appetite and
formication
Formication is the sensation resembling that of small insects crawling on (or under) the skin when nothing is actually there. It is one specific form of a set of sensations known as paresthesias, which also include the more common prickling, tin ...
. Less than 1% of patients experience pain at the injection site.
The radiation risks are reported as low. The committed
effective dose for a single investigation on a 70 kg individual is 4.6
mSv
mSv or MSV may refer to:
* Maize streak virus, a plant disease
* Medium-speed vehicle, US category
* Medium Systems Vehicle, a class of fictional artificially intelligent starship in The Culture universe of late Scottish author Iain Banks
* Mill ...
.
Pregnant patients should not undergo the test. It is not known if
123I-ioflupane is secreted in breast milk however it is recommended that breastfeeding is interrupted for three days after administration.
See also
*
List of cocaine analogues
References
External links
*
{{DEFAULTSORT:Ioflupane (123i)
Radiopharmaceuticals
Neuroimaging
Medical physics
Tropanes
Dopamine reuptake inhibitors
Stimulants
Organofluorides
Iodoarenes
Extrapyramidal and movement disorders
Parkinson's disease