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RADIOPHARMACEUTICALS

Presented by:
Ma. Isabelle S. Ramirez, RRT
January 6, 2015
RADIOPHARMACEUTICAL
◦ It is a radioactive compound used for the
diagnosis and therapeutic treatment of human
disease
◦ Other terms used are radiotracer,
radiodiagnostic agent and tracer.
◦ These are sterile and nonpyrogenic and can be
administered safely to humans.
RADIOPHARMACEUTICAL
◦ It has two components: a radionuclide and a
pharmaceutical.
◦ Radionuclide – radioactive component which
provides a signal for detection outside the body
◦ Pharmaceutical – a chemical moiety which
directs the radionuclide to the target organ or
system of interest
http://www.whatisnuclearmedicine.com/Whatis-61-
Radiopharmaceuticals?PHPSESSID=53ad4b66082c19fa4aca317f32d134fb
Characteristics of an Ideal
Radiopharmaceutical
◦ Easy Availability
◦ It should easily be produced, inexpensive and
readily available in any nuclear medicine facility
◦ Short Effective Half Life
◦ It should have a relatively short effective half life,
which should not be longer than the time required to
complete the study in question
Characteristics of an Ideal
Radiopharmaceutical
◦ Particle Emission
◦ Diagnostic Radiopharmaceuticals: γ-ray emitting
radionuclides are preferable
◦ Therapeutic Radiopharmaceuticals: α and β-
particle emission should be used because of
effective radiation damage to abnormal cells
Characteristics of an Ideal
Radiopharmaceutical

◦ Decay by Electron Capture or Isomeric


Transition
◦ Diagnostic Radiopharmaceuticals: should
decay by electron capture or isomeric
transition without any internal conversion
Characteristics of an Ideal
Radiopharmaceutical
◦ High Target-to-Nontarget Activity Ratio
◦ It is desirable that the radiopharmaceutical be
localized preferentially in the organ under study
since the activity from the nontarget areas can
obscure the structural details of the picture of the
target organ.
◦ Therefore, the target-to-nontarget activity ratio must
be high enough.
Mechanisms of
Radiopharmaceutical Localization
◦ Passive diffusion:
◦ 99mTc-DTPA in brain imaging, 99mTc-DTPA aerosol
and 133Xe in ventilation imaging, 111In-DTPA in
cisternography.
◦ Ion exchange:
◦ uptake of 99mTc-phosphonate complexes in bone.
Mechanisms of
Radiopharmaceutical Localization
Passive Diffusion:
(A) Following IV injection of
Tc-99m DTPA, dynamic
imaging shows poor
cerebral blood flow to an
area of stroke (arrows). (B)
Delayed imaging at 3 hours
after injection shows
increased accumulation of
Tc-99m DTPA in the same
area of stroke (arrow)
because of diffusion across
a disrupted BBB.
Mechanisms of
Radiopharmaceutical Localization

Passive diffusion
(A) Normal uptake of Tc-99m HMPAO in the brain of a living person.
(B) Absence of Tc-99m HMPAO uptake in the brain is consistent with
brain death. Also seen is normal uptake in lacrimal glands,
nasopharynx, thyroid, and lungs.
Mechanisms of
Radiopharmaceutical Localization
◦ Capillary blockage:
◦ 99mTc-macroaggregated albumin (MAA) particles
trapped in the lung capillaries.
◦ Phagocytosis:
◦ removal of 99mTc-sulfur colloid particles by the
reticuloendothelial cells in the liver, spleen, and
bone marrow.
Mechanisms of
Radiopharmaceutical Localization
Capillary Blockage
Tc-99m MAA perfusion lung
scan showing a classic wedge
shaped defect (arrow) in a
patient with pulmonary
embolism.
Mechanisms of
Radiopharmaceutical Localization
Phagocytosis
Tc-99m sulfur colloid
scan shows
normal uptake in liver
but lack of uptake in a
cavernous
hemangioma.
Mechanisms of
Radiopharmaceutical Localization
Phagocytosis
Tc-99m sulfur colloid scan in a
patient with severe alcoholic
cirrhosis demonstrating colloid
shift away from the liver (arrow)
to the spleen and marrow.
Mechanisms of
Radiopharmaceutical Localization
◦ Active transport:
◦ 131I uptake in the thyroid, 201Tl uptake in the
myocardium.
◦ Cell sequestration:
◦ sequestration of heat-damaged 99mTc-labeled
red blood cells by the spleen
Mechanisms of
Radiopharmaceutical Localization

Active Transport
(A) Normal uptake of Tc-99m pertechnetate in thyroid (and salivary glands).
(B) Absent thyroid uptake (arrow) of Tc-99m pertechnetate in a patient who
was administered iodinated x-ray contrast media a few days before.
Mechanisms of
Radiopharmaceutical Localization

Cell Sequestration
Imaging with heat-damaged Tc-99m RBCs in a post-splenectomy patient shows
uptake in an accessory spleen (arrows). Also seen is normal retention in blood pool
(heart, liver, and major blood vessels).
Mechanisms of
Radiopharmaceutical Localization
◦ Metabolism:
◦ 18F-FDG uptake in myocardial and brain tissues.
◦ Compartmental localization:
◦ 99mTc-labeled red blood cells used in the gated
blood pool study.
◦ Receptor binding:
◦ 11C-dopamine binding to the dopamine
receptors in the brain.
Mechanisms of
Radiopharmaceutical Localization
Compartmental
localization:
Increased concentration
of Tc-99m RBCs in a
hemangioma near the
right knee (arrows).
Mechanisms of
Radiopharmaceutical Localization
Receptor Binding
In-111 capromab pendetide
image shows uptake in a
prostate cancer metastasis in
the right lung (arrow). Also
seen is normal retention in
blood pool and normal
uptake in liver, spleen, and
marrow.
Mechanisms of
Radiopharmaceutical Localization
◦ Antigen–antibody complex formation:
◦ 131I-, 111In-, and 99mTc-labeled antibody to
localize tumors.
◦ Chemotaxis:
◦ 111In-labeled leukocytes to localize infections.
List of Pharmaceuticals
◦ BIDA – Parabutyl Imino Diacetic Acid
◦ DISIDA – Diisopropyl Imino Diacetic Acid
◦ DMSA – Dimercaptosuccinic Acid
◦ DPD – Dicarboxypropyldiphosphonate
◦ DTA – Diethylynytriaminepentaacetic Acid
◦ EDTA – Ethylenediaminetetraacetic Acid
List of Pharmaceuticals
◦ EDTMP – Ethylenediaminetetraacetic Acid
◦ FHMA – Ferric Hydroxide Macroaggregates
◦ GH/GHA – Glucoheptanoic Acid
◦ HEDP – Hydroxy Ethylidene Diphosphonate
◦ HIDA – Phenylcarbarmoylmethyldiaminoacetic
Acid
◦ HMDP – Hydroxymethylene Diphosphonate
List of Pharmaceuticals
◦ IDA – Iminodiacetic Acid
◦ MAA – Macroaggregated Albumin
◦ MAG3 – Mercaptoacetylglycylglycylglycine
◦ MDP – Methylene Diphosphonate
◦ MIBG – Meta-Iodobenzylguanidine
◦ PAH – Para-Aminohippuric Acid
List of Pharmaceuticals
◦ PIPIDA – Paraisopropyl Iminodiacetic Acid
◦ PYP – Pyrophosphate
◦ BATO – Boronic Acid Technetium Oxide
Radiopharmaceuticals:
Technetium
◦ 99mTc-MAA – used for lung perfusion imaging and
venography for detecting deep vein thrombi in LE.
◦ 99mTc-Phosphonate – suitable for bone imaging
◦ 99mTc-MDP – bone imaging
◦ 99mTc-PYP – bone imaging
◦ 99mTc-DTPA – used for renal flow study, GFR
measurement, aerosol preparation in lung ventilation
studies
Radiopharmaceuticals:
Technetium
◦ 99mTc-IDA – commonly used as hepatobiliary agents to
evaluate hepatic function, biliary duct patency and
mainly in cholescintigraphy
◦ 99mTc-Sestamibi – myocardial perfusion imaging agent
and detection of breast tumors
◦ 99mTc-MAG3 – assessment of renal function, particularly
in renal transplants
◦ 99mTc-DMSA – used in renal cortical imaging
Radioiodinated
Radiopharmaceuticals
◦ 131I-Sodium Iodide – measurement of thyroid uptake
and imaging after oral administration, also for the
treatment of thyroid diseases
◦ 123I-Sodium Iodide – measurement of thyroid uptake
and imaging
◦ 123I/131I-MIBG – detection of pheochromocytoma
◦ 125I-Sodium Iothalamate – GFR measurement
Miscellaneous
Radiopharmaceuticals
◦ 111In-DTPA – used for cisternography
◦ 133Xe Gas – used primarily for ventilation studies of the
lungs and assessment of cerebral blood flow
◦ 201Tl-Thallous Chloride – used for myocardial perfusion
imaging
◦ 89Sr-Strontium Chloride – indicated for relief of pain
with skeletal metastases
◦ 18F-FDG – study of metabolism in brain and heart
END OF LECTURE