Ioflupane
Encyclopedia
Ioflupane is the International Nonproprietary Name
of a phenyltropane
compound which is a neuro-imaging radiopharmaceutical drug, used by nuclear medicine
physicians for the diagnosis of Parkinson's disease
and the differential diagnosis of Parkinson's disease over other disorders presenting similar symptoms. It is injected into a patient and viewed with a gamma camera
in order to acquire SPECT images of the brain
with particular respect to the striatum, a subcortical region of the basal ganglia. The drug is sold under the tradename DaTSCAN and is manufactured by GE Healthcare
, formerly Amersham plc. It is not marketed outside of Europe
and the United States.
The iodine
introduced during manufacture is a radioactive isotope
, I-123
, and it is the properties of this isotope that makes the solution visible to a gamma camera. I-123 has a half life 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
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 neurones 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.
and a scan should not be performed with less than 111MBq.
Thyroid blocking via oral administration of 120 mg potassium iodide
is recommended to minimise unnecessary excessive uptake of radioiodine. One dose is given 2 hours before the injection and a further dose 24 hours later.
The most convenient way to administer the IV dose is via a peripheral intravenous cannula
. The scan is carried out 3 to 6 hours post injection.
. 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 4.35 mSv
. Pregnant patients should not undergo the test and breast feeding patients must cease since I-123 is secreted in breast milk.
International Nonproprietary Name
An International Nonproprietary Name is the official nonproprietary or generic name given to a pharmaceutical substance, as designated by the World Health Organization...
of a phenyltropane
Phenyltropane
Phenyltropanes were originally developed to reduce cocaine addiction and dependency. In general these compounds act as inhibitors of the plasmalemmal monoamine reuptake transporters. Although RTI holds a strong position in this field, they are not the only researchers that have prepared these...
compound which is a neuro-imaging radiopharmaceutical drug, used by nuclear medicine
Nuclear medicine
In nuclear medicine procedures, elemental radionuclides are combined with other elements to form chemical compounds, or else combined with existing pharmaceutical compounds, to form radiopharmaceuticals. These radiopharmaceuticals, once administered to the patient, can localize to specific organs...
physicians for the diagnosis of Parkinson's disease
Parkinson's disease
Parkinson's disease is a degenerative disorder of the central nervous system...
and the differential diagnosis of Parkinson's disease over other disorders presenting similar symptoms. It is injected into a patient and viewed with a gamma camera
Gamma camera
A gamma camera, also called a scintillation camera or Anger camera, is a device used to image gamma radiation emitting radioisotopes, a technique known as scintigraphy...
in order to acquire SPECT images of the brain
Brain
The brain is the center of the nervous system in all vertebrate and most invertebrate animals—only a few primitive invertebrates such as sponges, jellyfish, sea squirts and starfishes do not have one. It is located in the head, usually close to primary sensory apparatus such as vision, hearing,...
with particular respect to the striatum, a subcortical region of the basal ganglia. The drug is sold under the tradename DaTSCAN and is manufactured by GE Healthcare
GE Healthcare
GE Healthcare is a division of GE Technology Infrastructure, which is itself a division of General Electric . It employs more than 46,000 people worldwide and is headquartered in Little Chalfont, Buckinghamshire, United Kingdom. GE Healthcare is the first GE business segment to be headquartered...
, formerly Amersham plc. It is not marketed outside of Europe
Europe
Europe is, by convention, one of the world's seven continents. Comprising the westernmost peninsula of Eurasia, Europe is generally 'divided' from Asia to its east by the watershed divides of the Ural and Caucasus Mountains, the Ural River, the Caspian and Black Seas, and the waterways connecting...
and the United States.
Pharmacology
DaTSCAN is a solution of ioflupane (123I) for injection into a living test subject.The iodine
Iodine
Iodine is a chemical element with the symbol I and atomic number 53. The name is pronounced , , or . The name is from the , meaning violet or purple, due to the color of elemental iodine vapor....
introduced during manufacture is a radioactive isotope
Isotope
Isotopes are variants of atoms of a particular chemical element, which have differing numbers of neutrons. Atoms of a particular element by definition must contain the same number of protons but may have a distinct number of neutrons which differs from atom to atom, without changing the designation...
, I-123
Iodine-123
Iodine-123 is a radioactive isotope of iodine used in nuclear medicine imaging, including single photon emission computed tomography . The isotope's half-life is 13.22 hours; the decay by electron capture to tellurium-123 emits gamma radiation with predominant energies of 159 keV and 127 keV...
, and it is the properties of this isotope that makes the solution visible to a gamma camera. I-123 has a half life of approximately 13 hours and a gamma photon energy of 159 keV
Kev
Kev can refer to:*Kev Hawkins, a fictional character.*Kevin, a given name occasionally shortened to "Kev".*Kiloelectronvolt, a unit of energy who symbol is "KeV".* Krefelder Eislauf-VereinKEV can refer to:...
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
Dopamine is a catecholamine neurotransmitter present in a wide variety of animals, including both vertebrates and invertebrates. In the brain, this substituted phenethylamine functions as a neurotransmitter, activating the five known types of dopamine receptors—D1, D2, D3, D4, and D5—and their...
transporters (DAT
Dopamine transporter
The dopamine transporter is a membrane-spanning protein that pumps the neurotransmitter dopamine out of the synapse back into cytosol, from which other transporters sequester DA and NE into vesicles for later storage and release...
) in the brains of mammals, in particular the striatal
Striatum
The striatum, also known as the neostriatum or striate nucleus, is a subcortical part of the forebrain. It is the major input station of the basal ganglia system. The striatum, in turn, gets input from the cerebral cortex...
region of the brain. A feature of Parkinson's disease is a marked reduction in dopaminergic neurones 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 MBqBecquerel
The becquerel is the SI-derived unit of radioactivity. One Bq is defined as the activity of a quantity of radioactive material in which one nucleus decays per second. The Bq unit is therefore equivalent to an inverse second, s−1...
and a scan should not be performed with less than 111MBq.
Thyroid blocking via oral administration of 120 mg potassium iodide
Potassium iodide
Potassium iodide is an inorganic compound with the chemical formula KI. This white salt is the most commercially significant iodide compound, with approximately 37,000 tons produced in 1985. It is less hygroscopic than sodium iodide, making it easier to work with...
is recommended to minimise unnecessary excessive uptake of radioiodine. One dose is given 2 hours before the injection and a further dose 24 hours later.
The most convenient way to administer the IV dose is via a peripheral intravenous cannula
Cannula
A cannula or canula is a tube that can be inserted into the body, often for the delivery or removal of fluid or for the gathering of data...
. The scan is carried out 3 to 6 hours post injection.
Risks
Common side effects of ioflupane (123I) are headache, vertigo, increased appetite and formicationFormication
Formication is the medical term for a sensation that resembles that of insects crawling on the skin. It is one specific form of a set of sensations known as paresthesia, which also include the more common prickling, tingling sensation of "pins and needles"...
. Less than 1% of patients experience pain at the injection site.
The radiation risks are reported as low. The committed effective dose
Effective dose
Effective dose may refer to:*Effective dose the dose of pharmacologic agent which will have a therapeutic effect in some fraction of the population receiving the drug...
for a single investigation on a 70 kg individual is 4.35 mSv
MSV
mSv or MSV may refer to:*Medium Speed Vehicle, an administrative classification in certain jurisdictions for a 35MPH version of the NEV...
. Pregnant patients should not undergo the test and breast feeding patients must cease since I-123 is secreted in breast milk.