NUCMED
2. Radionuclide characteristic – the radionuclide must
2 General Components of RADIOPHARMACEUTICAL
 Radionuclide
 Pharmaceutical
RADIOPHARMACEUTICAL
 Are medicinal products designed for the use in the
investigation or treatment of human diseases.
 Contain “radionuclide” as an integral part of the
main ingredient.
 Are administered to a human subjects usually by
intravenous injection.
2 General Components
1. RADIONUCLIDE
 The atoms involved and the only nuclei that undergo
radioactive decay
 Emits gamma ray as it decays
 This is tagged to a radiopharmaceutical
2. PHARMACEUTICALS/TRACER
 Any chemical substances intended for use in medical
diagnosis, cure treatment or prevention of disease.
 Carries the radionuclide to the organ being examined.
 This is chosen in the basis of its preferential
localization or participation in the physiological
function of a given organ.
 Produces gamma-ray emission from within the organ
is being studied.
DESIGN CHARACTERISTICS OF
RADIOPHARMACEUTICALS
 The radionuclide decay should result in gamma
emissions of suitable energy (100-300 keV is ideal
for gamma cameras) and sufficient abundance of
emission of external detection.
 It should not contain particulate radiation (beta
emissions), which increases patient’s radiation dose
without adding diagnostic information.
 Beta emissions are suitable for therapeutic
radiopharmaceuticals.
 The effective half-life should only be longer
enough for the intended application, usually a few
hours.
 The specific activity should be high. (Tc-99m).
 The pharmaceutical component should be free of
any toxicity or secondary effects.
 Should be readily available or easily compounded
and should have a reasonable cost.
 The agent should rapidly and specifically localize
according to the intended application.
4 BASIC FACTORS INVOLVE IN THE CHOICE OF
RADIOPHARMACEUTICALS:
1. Biological behaviour - the radiopharmaceutical must
achieve a satisfactory distribution in the body or trace a
particular metabolic absorptive, excretory or other
pathway.
A “hot” lesion or “hot spot” produced with an area
increased radioactivity.
A “cold” lesion is detected with decreased
radioactivity.
The term “target” is used to denote the organ or the
volume which it is desired to concentrate the
radiopharmaceutical
have the suitable properties as regard radiation emitted
energy and abundance of gamma rays and half-life.
3. Radionuclide characteristic –the radionuclide must
have the suitable properties as regard radiation emitted
energy and abundance of gamma rays and half-life.
4. Pharmaceutical - most agent are injected
intravenously and must therefore be of high
pharmaceutical quality.
 Have a short half life
 Produce monochromatice gamma ray
 Minimizes production of particulate radiation
 Be non-toxic
 Localize in the organ or tissue of interest
To minimize radiation dose radiopharmaceuticals
should be the following:
MODES OF ADMINISTRATION OF
RADIOPHARMACEUTICAL:
 Injection – Most common
 Swallowing/Ingesting – Used in gastric emptying
study
 Inhalation – Used in a ventilation lung scan
 Instilling – Used for a cystogram
WHAT TO CONSIDER WHEN ADMINISTERING
RADIOPHARMACEUTICALS?
1. Patient need to be pyrogen free.
 Pyrogen
 Are products of microbial metabolism which produce
fever when injected to human subjects
 They are heat-stable and are not destroyed by normal
methods of sterilisation.
MECHANISM OF LOCALIZATION:
 Active Transport- Involves cellular metabolic
process that results in organ or tissue concentration
above plasma levels.
 Simple Diffusion- Involves movement of substance
from regions of higher concentration to a lower
concentration.
 Capillary blockade- Particles larger than RBC’s are
lodged at the first capillary bed it encounters.
 Phagocytosis- Involves the recognition and removal
of small foreign particles in the blood.
 Cell Sequestration- Process by the which the spleen
recognition and removes the damaged RBC’s and
cells nearing the end of heir life expectancy.
 Antigen- Antibody complexion. It is a tumor
localization
 Compartmental localization- Occurs when
radiopharmaceutical are introduced directly into well-
defined body compartments and remain there for a
time necessary for imaging.
PRINCIPAL SOURCES OF RADIONUCLIDES
1. Naturally Occurring Radionuclides
 Ra-226 – most famous naturally occurring
nuclide, was first used in treatment in 1903 (half-life
of 1620 years)
 K- 40 and C-14 – other significant naturally Technetium-99m
occurring radionuclides  The most commonly used radionuclide in nuclear
 0.012% of natural potassium is K-40, as the human medicine.
body contains about 190g of potassium, this  Most important radionuclide for visualization.
represents an activity of approximately 0.2uCi  The only desired radionuclide in Mo-Tc generator
 C-14 is produced in the upper atmosphere due to eluate.
the effect of cosmic radiation and becomes  Advantage: provides adequate time for the imaging
incorporated into plants and animals man. yet allows the target organ to decay background
radiation levels within 2 days.
2. Nuclear Reactor – produce radioactive substances  Modes of Decay: Isomeric Transition
 Particle accelerators or atom smasher.  Principal Photon energy: 140 KeV
 Neutron Bombardment- This is the most important  Produced in a generator system.
method of producing artificial radionuclides  Can be bound to biologically active compounds
or drugs to create radiopharmaceutical. (e.g. Tc-
 Fission Products 99 MAA)
 Radionuclide are normally obtained by neutron
bombardment of a uranium target (U-235) in Quality Control of Tc99-m Eluate
reactor splitting the uranium atom into two 1. 99Mo Breakthrough
radionuclides.  This is 99Mo contamination in the 99mTc-eluate and
 Process which uranium is bombardment with originates from the small quantity of 99Mo that may
neutron. be eluted with 99mTc.
 The US Pharmacopeia (USP 26) limit [also the
3. Cyclotron (Charged particle Bombardment) Nuclear Regulatory Commission (NRC) limit] is 0.15
 Important in PET facility mCi 99Mo/mCi (0.15 kBq/MBq) 99mTc per
 Expensive to run, usually only a single target can be administered dosage at the time of administration.
irriadiated at one time  measured by detecting 740-keV and 780-keV
 Products decay either by positron emission or photons of 99Mo in a dose calibrator or a NaI (Tl)
electron capture detector coupled to a pulse height analyzer.
I. Radionuclide Generator 2. Other Radionuclide Contamination
 Consist of a longer-lived parent and a shorter  In generators using fission-produced molybdenum, a
wavelength daughter. number of extraneous activities such as those of
 The daughter product will still have a useful half- 103Ru, 132Te, 131I, 99Zr, 124Sb, 134Cs, 89Sr,
life for clinical applications. 90Sr, and 86Rb may remain in the eluate as
 Molybdenum/Tc-99m Generator System – most contaminants.
important generator system NRC limits:
II. GENERATOR 131I:0.05 mCi/mCi (0.05 Bq/kBq) 99mTc
 A radionuclide generator is 103Ru : 0:05 mCi=mCi ð0:05 Bq=kBqÞ 99mTc
called a radioisotope 89Sr:0.0006 mCi/mCi (0.0006 Bq/kBq) 99mTc *the only
“cow”, which is a isotope that would be effectively shielded by a plastic
radioactive parent syringe.
decays a radioactive 90Sr:0.00006 mCi/mCi (0.00006 Bq/kBq) 99mTc
daughter b- and g-emitting radionuclides: not more than 0.01% of
all activity at the time of administration;
 Often colloquially gross a-particle impurity: not more than 0.001
referred to as “COWS” as nCi/mCi (0.001 Bq/MBq)99mTc
they are milked to  These contaminants can be checked by a
obtain radionuclide is multichannel pulse height analyzer
covered by lead (Pb) to
reduce radiation. 3. Aluminum Breakthrough
 The aluminum contamination originates from the
 Concept of generator was developed in the early alumina bed of the generator. The presence of
years of the century in order to provide a supply for aluminum in the 99mTc-eluate interferes with the
radon gas from Ra-226 preparation of 99mTc-sulfur colloid;
Process – elution  USP 26 limit is 10 ug Al/ml 99mTc for fission-
Saline Solution – produced 99Mo.
eluant  The presence of aluminum can be detected by the
Radioactive daughter colorimetric method using aurin tricarboxylic acid or
– eluate methyl orange, and can be quantitated by
Radioactive parent –
comparison with a standard solution of aluminum.
Mo-99 (half life of 66  -Excessive amounts of aluminum in the eluate
hours) produced by a indicate lack of
nuclear reactor  stability of the column.
generator and fission 4. pH
products comes a  The pH of the eluate should be between 4.5 and 7.5;
radioactive daughter this can be checked quantitatively with a pH meter or
– Tc-99m(half life 6 hrs) qualitatively with pH paper.

III. ELUTION
 Accomplished by OTHER RADIONUCLIDE GENERATOR:
placing a special 1. 113Sn–113mIn Generator
sterile vacuum vial on  the 113Sn has a half-life of 117 days and decays by
the exit or
collection port.
electron capture, and the daughter 113mIn decays
 Elution Volume: 5- 20 by 393-keV isomeric transition with a half-life of 100
mL min.
 The generator has a long shelf life due to the long
Molybdenum-99 half-life of 113Sn.
 The parent of Tc-99m  Common contaminants are 113Sn, 117mSn, and
 Half-life: 66 hours 125Sb
 Mode of Decay: Beta minus 2. 68Ge–68Ga Generator
 Principal Photon energies: 740 and 780 KeV  Germanium-68 decays by electron capture with a
 the most common radionuclide contaminant in the half-life of 271 days, and 68Ga, with a half-life of 68
generator eluate.
min, decays by positron emission and hence 511-
 keV annihilation radiations.

 68Ge is routinely used as standard sealed sources

for calibration of PET cameras
3. 82Sr–82Rb Generator (Cardiogen-82)
 Strontium-82 has a half-life of 25 days and decays to
82Rb by electron capture. Rubidium-82 decays by bþ
emission (95%) with a half-life of 75 s.
 Because of its short half-life,
 82Rb can be eluted repeatedly every 10 to 15 min
with maximum yield.
 administered to the patient using an infusion system
for myocardial perfusion imaging by the PET
technique.