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INTRODUCTION
Radiopharmaceuticals are the radioisotopes or radionuclides which are employed
in medicine for the diagnosis and treatment of certain diseases. These
compounds are used in trace amounts to produce radioactivity, that is essential
for the pharmacological effect. However, they are also liable to produce
hazardous effects when mishandled.
Radioactive compounds are so called, because they emit radiations or particles
(α, β and γ) by spontaneous decay to attain stability. This radioactive decay is
independent of temperature, pressure and concentration of a catalyst.
Different particles or rays emitted during radioactivity and their properties are
given in the below table.
Isotopes
Isotopes are the nuclides of an element with same number of protons (atomic
number “Z”), but different number of neutrons. They differ in nuclear masses,
thus differing in atomic weight or mass number (A) and also in certain physical,
chemical and nuclear properties. They are produced by chemical reactions of
atoms and molecules.
Radioactive isotopes undergo nuclear reactions with one another and with
neutrons to emit radioactive radiations (α, β and γ rays). Elements produced
after nuclear changes or rearrangements in the original nuclide (parent) are
called “daughter or decay nuclides”. This process of nuclear change is known as
“radioactive decay or disintegration”.
Stability of Isotopes
Naturally occurring nuclides of many elements possess a favourable ratio
of protons and neutrons. This ratio is responsible for the stability of
isotopes. For example, the stable ratio for potassium is 1:1.115. Any change in
this ratio i.e., either addition or removal of one or more neutrons alters the
atomic number, thereby disturbing the stability of the nuclide.
This can be exemplified by the instability caused due to a change in the number
of neutrons from the iodine nucleus.Many isotopes of the elements with Z ≤ 83
are considered to be stable isotopes with a few exceptions and isotopes
(naturally occurring or artificially prepared) of the elements with Z > 83 are
unstable.
2. RADIOACTIVITY
Radioisotopes or radionuclides undergo spontaneous decay or disintegration to
attain stability by emitting radioactivity
.
Types of Radionuclides
These radionuclides are of two types,
1. Natural Radionuclides
(a) High Atomic Weight Elements
There are about 40 elements emitting α, β and γ rays.
E.gs: Uranium-238, Radium-226
(b) Moderate Atomic Weight Elements
These include Potassium-40, Rubidium-87.
2. Artificial Radionuclides
They are prepared synthetically to produce the desired radioactivity.
Characteristics of Radioactivity
1. Types of Decay or Activity
Radioactivity may either be emission of α, β or γ-rays accompanied by neutron
particles or X-rays or only energy (characteristic of the wavelength of emitted
ray). This depends on the number of atoms of the radioisotope present.
2. Rate of Decay
It is expressed as t½. It is defined as the number of radioactive nuclei actually
disintegrating or decaying or mutating in a given time.
A radioisotope decays at the same rate emitting same radiations or
particles at any point of time or condition.
Half-Life (t½) of Radioactive Element
The rate and type of decay of individual nuclides of a radioactive element
varies significantly. Hence, it is not possible to study single nuclide for its
properties. So, to statistically determine the chances of transformation
(decay or disintegration or transmutation) by a certain number of nuclides
from a population of nuclides in a given time, a law
has been formulated, known as “decay law”, which is given as follows,
2. Cyclotron Irradiation
In this method, a particle accelerating equipment called “cyclotron” is used,
in which a target nuclide is bombarded with high energy sub-atomic particles
such as protons, α-particles or fast moving electrons
resulting in a nuclear reaction. This leaves the target nuclides unstable, which
therefore breaks, producing new radioisotopes or nuclides to achieve stability.
Examples
5. RADIOISOTOPES
Sodium Iodide (NaI131)
Sodium iodide is one of the most common diagnostic agent which is available as
capsules and as solutions. Although it does not find a mention in the Indian
Pharmacopoeia, it is official in the USP. It can be administered either by oral or
intravenous route and is generally used as a diagnostic aid in determining the
normal functioning of the thyroid gland and also in thyroid scanning procedures
to determine the size, position and presence of thyroid tumours.
The required amount of iodine-131 in sodium iodide I-131 solution should
not be less than 90% and not more than 110%. The quantity of iodine-131
present is expressed in the form of millicuries or microcuries. In case, if the
solution possesses any other chemical forms of radioactivity, then their
percentage should not exceed 5% of the total radioactivity.
Moreover, the solution is also required to be devoid of other radio nuclides.
Method of Preparation
I131having a half-life of about 8.08 days is separated in the form
of sodium iodide from the products obtained due to uranium fission or when
tellurium is subjected to neutron irradiation. The solution also exhibits the
presence of sodium thiosulphate or any other reducing agent. Preparation of
capsules involve the evaporation of alcoholic solution of sodium iodide I131
directly on the inner walls of the gelatin capsules.
Properties
1. NaI131 solution is clear and colourless. It is mixed with physiological
saline solution so as to make it isotonic.
2. Iodine is oxidized to volatile I2 by air and radiolytic free radicles, which can be
hazardous. Such air oxidation can be prevented by maintaining the solution at an
alkaline pH (7.5-9) and adding sodium ascorbate or thiosulfate.
3. b-radiations are responsible for rendering both the solution as well as the
container dark in colour with time.
Assay
Sodium iodide-I131 can be assayed using a suitable counting equipment.
Since the compound emits both b-particles and g-rays during its decay, it is
necessary that the counting equipment is well equipped with an electronic
sealing device as well as a suitable sensing unit, which can either be a
Geiger-Muller counter or a scintillation detector. Activity
of the compound can be determined by comparing it with a standardized
I-131 solution or using an instrument which has been calibrated using the
standardized solution.
Uses
As already stated, sodium iodide-I131 is used as a diagnostic aid to
determine the normal functioning of the thyroid gland and is also used in
scanning the thyroid gland.
Examples
(a) Radioactive Cyanocobalamin(57Co)
(i) It is employed for measuring glomerular filtration rate (GFR).
(ii) It is also used to study defects in absorption of vitamin B12 through
intestine of the patient.
(b) Radiolabelled Gold (198Au)Colloidal gold injection is
administered to study blood circulation in liver.
(c) Radiolabelled Iodine (131I)
(i) Sodium iodide injection is used for the diagnosis of thyroid dysfunction.
(ii) Iodinated human serum albumin is administered for the diagnosis of
cardiovascular diseases.
(iii) Sodium iodohippurate injection is administered to diagnose any renal
dysfunction.
(iv) Sodium rose bengal injection finds use in the investigation of liver function.
(d) 18F (or) Tc-99m is employed in the diagnosis of brain tumours or
lesions.
These radioactive isotopes are taken up by the organs and thus measured by
scintillation counters, which are setup over the organs.
Positron Emission Tomography (PET)
Positron emission tomography is a popular diagnostic technique that uses
radioisotopes which emit low radiation positrons. These radionuclide
preparations
are administered into the body and the fate of these nuclides is determined using
suitable devices.
For example, radiolabelled nitrogen, oxygen and carbon dioxide gases are
used to detect pulmonary diseases.
Although PET is gaining importance, availability of radionuclides ultimately
depends on the presence of acceleration facilities i.e., cyclotron (particle
accelerator) and/or linear accelerator.
Limitations of PET
1. Half life of these nuclides is very short.
2. These nuclides cannot be transported.
3. Cyclotrons used are expensive to install and run.
2. Radioisotopes in Therapy
Radioisotopes that are used therapeutically ionize the atoms in their path with
the emission of radiations. The strength or energy of these emitted
radiations
(α, β or γ-rays) is measured as millions of electron volts called MeV
HAZARDS OF RADIOACTIVITY
The hazardous/harmful effects due to radiation exposure are of various
types.
1. Radiation exposure may lead to gene mutations, therefore disturbing the
genetic make-up.
2. It mainly effects continuously and rapidly dividing tissues or cells such as
bone marrow, mucosa of gut, gonads, foetus etc.
3. Skin and soft tissues are affected on exposure to high energy radiations.
4. Bone marrow is highly damaged due to radiation exposure and results in
leukaemia.
5. Certain organs like colon, urinary bladder, liver etc., are significantly
damaged, whereas other organs are less effected.
Hence, personnel working with radioactive substances are recommended to
protect themselves by lead shielding.When a radioactive isotope (source) is
ingested, it remains in the body for a long time, before getting excreted and
continuously emits radiation which gets absorbed by
the surrounding tissues or organs. The radiation produced may get reduced at
constant rate and stops only when the radiation source has been completely
eliminated from the body. Thus, excretion of a radioisotope is important, which
depends on the biochemical and physiological properties of the chemical, but not
the radionuclide.
Committed Dose
It represents the total dose of radiation absorbed from a source during a period
of 50 years. It is so called because
it cannot be separated from the body easily. This dose does not effect or cause
damage to the person, if it is within the specified limits