RADIOPHARMACEUTICALS

JAMES P. JIMENEZ, RPh

 RADIOACTIVITY
• Is the spontaneous transformation of one
nuclide into another nuclide with the emission
of energy in the form of radiation.
 RADIOACTIVITY
• Nuclides
– Distinct atom or nucleus characterized by a
specific number of protons and neutrons
• Isotopes – nuclides with the same number of protons
but different number of neutrons
– Stable
– Unstable
• Isotones
• Isobars
 RADIOPHARMACEUTICALS
• Is a preparation, intended for in vivo use, that
contains a radionuclide in the form of a simple
salt or complex
• Exists as solid, liquid, gas or a pseudogas
 TYPES OF RADIATION
• Alpha particles
– Heaviest and slowest and emitted only from
elements with atomic numbers higher than 82

• Beta particles – negatron or positron

– Same mass as an electron; faster than alpha
particle due to lower mass
– negatron and positron have similar properties
except for the charge
 TYPES OF RADIATION
• Gamma radiation
– has no mass and charge but has a very high energy;
photon/quanta of energy
– emitted as a result of nuclear deexcitation

• K-Capture/Electron Capture
– Produced by isotopes with an unstable proton:
neutron ratio but with insufficient energy to emit a
positron.
 ENERGY AND KINETICS
• Electron volt
– defined as the energy acquired by an electron
when accelerated through a potential of 1 volt
– 1 volt (1 Joule/Coulomb) X 1.602 x 10-19 Coulomb
 ENERGY AND KINETICS
• Decay Rate
– the time rate at which atoms undergo
disintegration
– The rate of disintegration may be expressed as
follows:
 ENERGY AND KINETICS
• Decay Rate
– Exponential Decay Law
 ENERGY AND KINETICS
• HALF LIFE
– the time required for ½ of a given number of
atoms to decay
– t1/2 = ln 2/λ (λ= disintegration/decay constant)
 UNITS OF RADIOACTIVITY
• CONVERSION EQUIVALENTS
– 1 Ci = 3.7 x 10^10 Bq = 3.7 x 10^4 MBq = 37 x
10^3 MBq
– 1 mCi = 37 MBq
– 1 µCi = 0.037 MBq
– 1 Bq = 2.7 x 10^-11 Ci
– 1 MBq = 10^6 Bq = 2.7 x 10^-5 Ci
= 2.7 x 10^-2 mCi = 0.027 mCi
= 27 µCi
 UNITS OF MEASUREMENT
• Roentgen (R)
– Quantity of x-ray or gamma radiation that will
produce sufficient ion pairs to have one
electrostatic unit (esu) of charge of either sign in 1
cc or air at STP

• Radiation Absorbed Dose (Rad)

– Measures the amount of energy transferred to a
particular medium.
 UNITS OF MEASUREMENT
• Roentgen Equivalent Man (rem)
– used to determine doses received by people
working on radioisotopes; RAD x RBE.
• α particle: 10 -20
• β particle, γ radiation: 1

• Gray (Gy)
– SI derived unit of absorbed radiation dose done by
1 Joule of ionizing radiation/Kg of matter
 UNITS OF MEASUREMENT
• Sievert (Sv)
– SI derived unit for the equivalent dose of
radiation; Gy X by a weighing factor
• α particle: 20
• β particle, γ radiation: 1
 BIOLOGICAL EFFECTS
• Biological effects are related to the
interactions of the radiation with molecules,
which results in the formation of abnormal
amounts of ions and free radicals.
 RADIONUCLIDE PRODUCTION
• Fission
– radioactive process in which a relatively heavy
nucleus splits into two nuclei of nearly equal size
with the simultaneous emission of two or three
neutrons

• Neutron Reaction
 RADIONUCLIDE PRODUCTION
• Accelerator/Cyclotron
– bombard the target nucleus with particles that
have been accelerated to a high velocity
 RADIOLABELLING METHODS
• Introduction of a foreign Label
• Isotope Exchange
• Labeling with Bifunctional Chelates
• Biosynthesis
DESIGN OF RADIOPHARMACEUTICALS
• STRUCTURE – DISTRIBUTION RELATIONSHIPS
– used to optimize target site delivery of the
candidate radiopharmaceutical
 DIAGNOSTICS
• Contrast Media
– a substance that is used to enhanced the contrast
between the structures or fluids within the body,
especially in medical imaging

• X-rays and CT Scans

– atoms or molecules that have a large number of
electrons, increasing the chance of stopping x-rays
 DIAGNOSTICS
• MRI (Magnetic Resonance Imaging)
– Compounds that alter the relaxation times of
atoms within body tissues.

• SPECT and PET

– Gamma and beta emitters that allow visualization
of tissues.
SPECT AND PET
 RADIOPHARMACEUTICALS AND
CONTRAST MEDIA
• Barium Sulfate
– Barium Sulfate Paste
– Barium Sulfate Suspension/ for Suspension
– Barium Sulfate Tablets
 RADIOPHARMACEUTICALS AND
CONTRAST MEDIA
• Diatrizoate Meglumine
– Provides contrast enhancement of the bladder

• Iodipamide
– Used for visualization of the gallbladder & biliary
ducts
 RADIOPHARMACEUTICALS AND
CONTRAST MEDIA
• Gadopentate Dimeglumine
– Used as a contrast agent in MRI for visualization of
brain, blood vessels, spinal and other disorders
 RADIOPHARMACEUTICALS AND
CONTRAST MEDIA
• Ferumoxides
– a sterile colloidal suspension of superparamagnetic iron oxide
associated with dextran in Water for Injection

• Chromium Cr-51 Edetate Injection

– determination of GFR

• Cyanocobalamin (Co-57 or Co-58)

– diagnosis of pernicious anemia

• Ferrous Fe-59 Citrate

– iron metabolism and RBC formation
 TECHNETIUM
RADIOPHARMACEUTICALS
• Most commonly used metal atom in
radiopharmaceuticals
• Has a 6-hour half life and a 140KeV gamma
photon that is emitted with high abundance
and it lacks particulate alpha and beta
emissions
• Versatile chemistry that allows it to be
chelated with a variety of compounds (but not
all)
 TECHNETIUM
RADIOPHARMACEUTICALS
RADIOPHARMACEUTICAL
99mTc Albumin Aggregated Injection
99mTc Sulfur Colloid Injection
99mTc Labeled RBC
99mTc Methylene Diphosphate
99mTc Pyrophosphate
99mTc Sestamibi
99mTc Sulfur Colloid cooked in scrambled
eggs
99mTc - bicirumab
USE
Lung scanning
Imaging areas of functioning
reticuloendothelial cells
Cardiac pool pumping
Bone imaging
Cardiac infarct imaging
Imaging of myocardial perfusion, breast
tumor
Gastric emptying imaging
Deep vein thrombosis
OTHER RADIOPHARMACEUTICALS
RADIOPHARMACEUTICAL
Cyanocobalamin Co 57 Capsules
125I Serum Albumin Injection
Iodohippurate 131I Injection
Sodium Chromate Cr 51 Injection
Sodium Iodide 131I Capsules/Solution
Sodium pertechnate 99mTc Injection
Sodium Phosphate 32P Solution
USE
Pernicious anemia
Blood volume determination
Renal function
Blood volume determination
Thyroid function, thyroid inhibitor
Brain and thyroid scanning
Ocular tumor localization &
antipolycythemia
COMPLETE LIST OF ALL AVAILABLE
RADIOPHARMACEUTICALS
COMPLETE LIST OF ALL AVAILABLE
RADIOPHARMACEUTICALS
COMPLETE LIST OF ALL AVAILABLE
RADIOPHARMACEUTICALS
COMPLETE LIST OF ALL AVAILABLE
RADIOPHARMACEUTICALS
 THANK YOU FOR LISTENING =)
END OF PHCH 121

STUDY REALLY HARD FOR THE 3 RD

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