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Radiopharmaceuticals

Radioactivity
Phenomenon by which one nuclide is
spontaneously transformed into another nuclide
with the emission of energy in the form of
radiation
During decay/spontaneous transformation, ratio
of neutrons to protons changes
After one or more decay, a NEW nucleus is
formed

Concepts on Radiopharmacy

Half-life
Time required for number of
radioactivity to decrease to onehalf the original number

t1/2 = 0.693/k

Atoms of a particular
radioisotope will ALWAYS
disintegrate in the same way and
rate
The amount of radioisotopes will
decrease with time at a constant
rate of disintegration

K = rate constant or the


fraction of radioatoms
disintegrating per unit
time

Drugs that possess the property of being


radioactive
Chemicals containing radioactive isotope for
us in human
Preparations intended for in-vivo use that
contains radionuclide in a form of an
element, simple salt or complex

Radioactive isotope
Non-reactive complex (ligand)
Affinity to organ of choice

General use

Diagnostic application
For treatment

Production of Radioisotopes

Nuclear Reactor
Accelerator Produced Isotopes with the use
of cyclotron
Generator Produced Isotopes

Methods of Measurement
Ionization chamber (electroscope)
The Geiger-Muller counter
The Scintillation Counter
Autoradiograph method

Forms of Radiation
Alpha Decay
Least penetrating
Can be blocked by paper

Beta Decay
Medium penetrating
Can be blocked by aluminum

Gamma Ray Decay


Most penetrating
Can be blocked by heavy metals

X-ray vs. Gamma Ray

Differ only in their origin

___ arises outside the nucleus while ___


arises within the nucleus

Units of Measurements

Currie (Ci) - in millicurie or microcurie


Roentgen (R) - ergs
RAD (Radiation Absorbed Dose) - ergs

Nuclear Medicine

Aim

Provide a detailed morphologic structure of


the organ
Testing of their physiologic function through
the accumulation of the radiopharmaceutical

Properties of a good radiotracer


Gamma emitter
Short half life
Can be detected
High organ specificity

Technicium - 99m
Metastable isomer of Technecium 99
Gamma emitter
Short phsyical half life - 6hrs
Short biological half life - 1 day

Parent Isotope Source

Fusion of enriched Uranium-235 to form


Molybdenum-99

Tc-99m
Generator

Examples of Radioactive
Isotopes

Functional Brain Imaging

Tc99m-HMPAO
(hexamethyl propylene amine oxime)
Must be injected

Bone scan

Sodium
Pertechnetate

Tc99m-medronate

Myocardial perfusion

Tc99m-sestamibi or Tc99m-tetrofosmin

Sentinel Node Identification

Tc99m-isosulfan
blue

Immuno-scintigraphy

Tc99m-monoclonal
antibody

Blood Pool Labeling

Tc99m-Sn

Heart Scan

Tc99m-pyrophosphate

Spleen Scan

Tc99m-sulfur colloid

Meckel's Scan
Tc99m-technetate

Half-life
1. Ga67

2. Au198

3. Kr81m

4. K42

K43

Generic Name

Use

Gallium citrate
Ga67 inj

Lesions of lungs,
breast, sinuses,
liver tumor bones

Gold Au198 inj

For neoplastic
suppressant and
liver scanning

13 seconds

Krypton Kr81m

Lung function,
ventilation and
perfusion;
radiocardiology

12.4 hours

Tumor
Potassium
localization and
Chloride K42 inj
renal blood flow

22 hours

Potassium
Heart imaging
Chloride K43 inj

78 hours

2.7 days

5. Se75
6. Na22
7. F18
8. Sr85
9. Tl201
10. Xe127
Xe133

120days

Selenomethionine
Se75 inj

Scintigraphy of
pancreas and
parathyroid glands

2.6 years

Sodium Na22
inj

Detection of circulatory
time, Na space and total
exchangeable Na

1.7 hours

Sodium
Fluoride F18 inj

Bone
metabolism

64 days

Strontium Sr85
inj

Bone
metabolism

73 hours

Thallium Tl201
Myocardial
Chloride inj perfusion imaging

36.4hours

Xenon Xe127
gas

For lung imaging check for alveolar


blockage

5.27days

Xenon Xe133
inj

For lung imaging check for alveolar


blockage

BRAIN

BLOOD

BONES

Hg197/203
In113m
Tc99m

Cr51 - RBC volume


I125/131 - RBC
Tc99m
K42
Fe59

In113m
F18
Sr85
Tc99m
Ga67