Radio-Pharmaceutics

Why we study radiopharmaceutics?.

The main responsibility of the Radiopharmacist or Radiopharmaceutical Scientist in nuclear medicine is the preparation of radiopharmaceuticals to ensure their safety and effi

The main responsibility of the Radiopharmacist or Radiopharmaceutical Scientist in nuclear medicine is the preparation of radiopharmaceuticals to ensure their safety and efficacy.
 Introduction
• Radiopharmacy: a discipline concerned with the preparation, dispensing and quality control
of radiopharmaceuticals.
• Radiopharmaceuticals: medicinal products that contain radionuclides (radioactive isotopes)
that may be used for diagnosis or treatment or sterilization. Also known as radiotracer or
radio diagnostic agent.
• They are administered parenterally, orally or by inhalation.
• Radionuclide : An unstable nuclide that decays spontaneously by the emission of particles
(alpha or beta particles) or photons (gamma rays or x-rays) to become stable.
• Radiation: Particles or waves coming from the nucleus of the atom (to be more stable)
• Nuclear radiation: The particles or photons derived from nucleus of the radioactive
element.
• Radiopharmaceuticals are regulated both as medicinal products (GMP regulations) and as
radioactive substances (safety regulations (nuclear energy legislation)).
 Types of Radiations
• A) Nonionizing radiation: Has low frequency and their energy do not remove electrons from atoms
• B) Ionizing radiation : Has high frequency and their energy can move electrons from atoms. The
energy released in form of of particles (alpha or beta particles) or photons (gamma rays or x-rays).
➢Consumer products that contain radioactive materials
• 1- Fertilizer: potassium (naturally radioactive), phosphorus and nitrogen.
• 2- Luminous clocks and watches or exit signs: tritium (hydrogen 3) or promethium 147 or radium
226
• 3- Smoke detectors: americium 241
 Naturally occurring
radioactive materials
• Potassium K 40 • Strontium 90
• Tritium H 3 • Technetium 99
• Iodine I 127 • Thorium
• Radium (Ra) • Plutonium
• Radon (Rn): radioactive • Cesium 137
gas found in soils, rock, • Tritium
and water. Radon causes
lung cancer and is a threat • Uranium
to health • Cobalt 60
• Americium 241
 Atom
• The atoms have orbitals and nucleus (Nuclide have a specific number of
neutrons and protons )
• The stability of the atom depends on the neutron to proton ratio in the
nucleus.
• Proton has a mass 1.800 times that of an orbital electron .
• Neutrons have an equivalent mass to the proton but carry no electrical
charge.
• In a stable atom, the number of electrons, which are negatively charged,
equals the number of protons.
• Mass number: the sum of the number of protons and neutrons.
• Atomic number: the number of protons which is also same as number
• of electrons in a neutral atom.
• Isotopes: are atoms of various mass number but have the same atomic
number.
• The chemical properties of an element are affected by the number of
electron rather than neutrons in the atom.
• Above atomic number 83, all elements are radioactive.
 Radioactive Decay
• Radioactive Decay: Spontaneous process in which an unstable radionuclide transforms to a
more stable (radio) nuclide releasing energy (ionizing radiation) in the form of particles (alpha
or beta particles) or photons (gamma rays).
• Ionizing radiation: is radiation composed of particles that carry enough energy to liberate
electrons from atoms or molecules without rising the temperature of the material.
• The rate of radioisotopes decay is indicated by the number of atoms of nuclide which are
disintegrating per unit time
• This number is proportional to the total number of radioactive atoms present in the sample
(first-order kinetics)
• Decay equation 𝑵 = 𝑵𝟎 𝒆−λ𝒕
• N number of atoms at elapsed time t 𝑵𝟎 number of atoms at time 0
• λ is the disintegration constant (decay constant) Half-life = 0.693/λ
Types of Radiopharmaceuticals
Decay
• 1- Alpha decay
• Occurs in heavy elements with atomic numbers
greater than 83
• Usually heavy nuclei such as radon, uranium,
neptunium, decay by α particle emission.
• Possess the largest mass (Travel a few inches though
air) and has largest charge of radiation (cause a great
damage to the immediate area by breaking down
DNA). have the highest ionization power
• Consisting of 2 proton and 2 neutrons (A helium
nucleus)
• As alpha particles losses energy its velocity decrease
then attract electrons and become helium ion.
 • Alpha decay
• Have positive charge and can be detected by strong
magnetic field
• Carry 2 positive charge (2 protons)
• The penetrating power of alpha particles is less as
compared to other emissions (cannot penetrate the tissue )
• Can be stopped with a sheet of paper.
• Special precautions are taken to ensure that alpha emitters
are not inhaled , ingested or injected.
• Give reason: elements which emit alpha rays do not find
use in biological application.
 Types of Radiopharmaceuticals
Decay
• 2- Beta decay (-ß) (negatrons)
• Occurs in neutron rich nuclei
• One neutron converted to proton then the negative electron
(- beta particle) ejected from radioactive nuclei
• The β decay may be followed by γ ray emission , if the
daughter nuclide is in an excited state.
• Greater penetrating power than alpha rays
• not as destructive as alpha particles
• Because of the associated mass and charge of the particle,
beta particles are not as penetrating as gamma radiation
• Same charge and mass of electron
• Can be stopped by glass plate, Aluminium foil or block of
wood
Types of Radiopharmaceuticals
Decay
• 3- Electron capture (neutrino)
• When a proton from the atomic nucleus attracts an
electron from the innermost orbit, the negatively
charged electron, and the positively charged proton
combines together to form a neutron.
• As a result of this process, an electron neutrino is
released. When an element reduces its atomic number
by 1 and becomes an entirely different element, the
process is known as beta decay
Types of Radiopharmaceuticals
Decay
• 4- Beta decay (+ß) Positron decay
• Occurs in proton rich nuclei.
• One proton converted to neutron then the positron (+ beta
particle) ejected from radioactive nuclei.
• It will combine with any electron and annihilates forming
gamma ray photons
• Greater penetrating power than alpha rays
• have a range of more than 100 feet in air and up to about 1
mm in tissue. - not as destructive as alpha particles
• Because of the associated mass and charge of the particle,
beta particles are not as penetrating as gamma radiation
• Same size as electron but with positive charge
• Can be stopped by glass plate (Perspex) , Aluminium foil or
block of wood
Types of Radiopharmaceuticals
Decay
• 5- Gamma decay
• Is an emission of nuclear photon from excited
nucleus.
• The unstable nucleus has excess of energy. It expels
this energy as gamma ray to be stable.
• The nuclide retain its identity
• Are electromagnetic radiation with high frequency
• traveling at the speed of light
• Have no mass - no charge
• Most penetration (short wavelength- high energy)
• Can be stopped by 1 m thick concrete, or several cm
thick sheet of lead
 • Auger electrons originate from the orbital electrons rather than
from the nucleus.
• an electron from a higher orbital falls down into that lower
6- X-ray orbital, and the difference in energy between the two orbitals is
emitted in the form of a characteristic x ray.
• auger electron, possesses similar properties to a beta particle
except that it has much less energy, typically only tens to
hundreds of electron volts.
 A Decay series
• After the parent nuclide decays, the daughter nuclide produced can also be radioactive. In this
way, a single nuclide can undergo several radioactive decay processes, one after the other in a
chain.
 Half-lives of radiopharmaceuticals
The time required for a radionuclide to decay to 50% of its original activity
Radionuclides range widely in their half-life; for 𝐂𝟏𝟒 , it is 5,730 years, whereas for 𝐍𝐚𝟐𝟒 , it is 15
hours, and for 𝐊𝐫 𝟖𝟏 , it is 13 seconds.
• Physical half-life
• The amount of time necessary for the radioactive atoms to decay to one-half their original number.
Each radionuclide is characterized by a specific half-life that is a physical constant.
• Biological half-life
• The amount of time required for the body to metabolize or eliminate one-half of the administered
dose of any substance through biological processes.
• Effective half-life
• The time required for an administered radiopharmaceutical dose to be reduced by one-half as a result
of both physical decay and biological mechanisms.

• Where Te is the effective half-life, Tp is the physical half-life, and Tb is the biological half-life
 Radioactivity measurement
• The Curie (Ci): The amount of any radioactive material which decay at rate of 3.700 X 𝟏𝟎𝟏𝟎
disintegrating atom per second( 1 gm of radium).
• Becquerel (Bq) : 1 Becquerel is equivalent to one disintegration per second.
• 1 Ci = 3.700 X 𝟏𝟎𝟏𝟎 Bq
• Roentgen: amount of x or gamma radiation that produce ionization of one electrostatic unit (+ -) per
cubic centimetre.
• Rad: (the unit of absorbed dose) The amount of radiation absorbed by body tissue in which a
radioactive substance resides. (1 rad = 100 ergs of energy absorbed by 1 g of tissue) (0.01 j/kg)
• The gray (Gy): equal to 1 J of energy absorbed in 1 Kg of tissue( 1 Gy = 100 rad)
• REM: used to equate the difference in biological responses produced by different radiations
• REM = Rad X Relative Biological Effectiveness