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1.

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,

Half-life (t½) is defined as the time required by a sample of nuclide to decay


or the radioactivity to reduce by half of its original value.
t½ is characteristic of a particular nuclide and describes the radionuclides. It
varies widely for different radio nuclides.
Units of Radioactivity
1. Curie (Ci)
The radioactivity (A) of a radionuclide is determined by counting the number of
such nuclides present at the time of measuring (Nt) and the decay constant (λ)
specific to that nuclide. It can be given in the form of an equation as,
A= λNt
It is expressed as “curie per gram (Ci/g) or millicurie per gram(mCi/g) or
microcurie per gram (μCi/g) of the material”.
One curie is the amount of radionuclide, whose rate of decay is 3.7×10 10
disintegrations per second.
2. Bequerel (Bq)
It is also a unit of radioactivity, but fairly smaller
compared to curie. Bq is the quantity of radionuclide
undergoing 1 disintegration per second.
1 Ci = 3.7×1010
Bq (or)
1 Bq = 2.7×10–11Ci
3. Roentgen (R)
It measures the amount of exposure to radioactivity.
1R = 2.58×10–4
C/kg (C = Coulomb).
4. Radiation Absorbed Dose (RAD)
RAD indicates the actual dose of radiation absorbed by the body. Unlike the units
of radioactivity (Ci and Bq), RAD clearly states the actual amount of radiation
absorbed.
1 RAD = 100 ergs/g or 10–2 J/kg
It can also be expressed in eV (electron volts) as 1 J = 6200 billion MeV
Energy absorption equivalents of 1R in various media are given below,
(a) Air: 1R (in air) = 0.87 RAD
(b) Water: 1R (water) = 0.97 RAD
(c) Tissues: 1R (tissue) = 0.93 RAD
5.
Radiation Equivalent in Man (REM) or Grays (Gy)Earlier, REM was the unit of
equivalent dose of the radiation. However, now its use is limited, since it
has been replaced by an SI unit “Gray” (Gy), which is more practical in
demonstrating pharmaceutical dosage form in terms of RAD. It is given by,
REM = Dose in RADs × Quality factor × Distribution factor
1 Gy = 100 RADs = 1 J/kg.
6. Quality Factor (QF) or Radiation Weighing Factor (Wr)
Since all the radiations are not quantitatively equal and it is not possible for “Gy”
to accurately describe actual effect of the absorbed radiation (which is
numerically
related to energy), an arbitary factor was developed.
It was previously called as Quality Factor (QF) and used along with REM.
However, now it has been replaced with Radiation Weighing Factor (Wr), to
be used along with Gy.
Wr modifies the numerical value of the dose equivalents and is defined
by the radiation and biological effect produced. Its value could not be
measured by any instrument.
Further, a new unit known as ‘Sievert (Sv)’ came into existence. It is obtained by
multiplying Wr with Gy units, which is given as follows

7. Exposure Rate Constant


It is the dose of absorbed radiation at an exposure rate of roentgen per hour
from a 1 curie radioactive source, placed at distance of 1m. It may also be
described as
1/10th the dose of exposure rate of radiation from a 1 curie source which is at 1
foot distance.
8. Relative Biological Effectiveness (RBE)
It is the unit which determines the relative effects of different types of radiation
emitted such as α, β and γ rays on the biological system.
PRODUCTION OF RADIOISOTOPES
Radioisotopes can be produced by the following methods.
1. Reactor Irradiation
In this method, a moderator contains a reactor with a fissionable material or fuel.
The fissionable material used in this method is uranium which produces a
neutron flux, where the slow neutrons are accelerated to form fast neutrons by
thermal and other processes.
This nuclear reaction is known as “Neutron activation or bombardment”, which
ultimately results in the formation of radioisotopes that can be applied for
medicine.A maximum flux of 1014 neutrons cm–2s–1is produced using
moderator containing heavy water as reactor and uranium as fuel (Harwell
reactor DIDO).
Example

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

DETECTION AND MEASUREMENT OF RADIOACTIVITY


Radioactivity (emission of α, β or γ-rays) emitted by radionuclides is
detected and measured using various techniques and instruments.
Two important characteristics of radionuclides that are to be considered
during detection of radioactivity are,
1. Mass of nuclide
2. Emitted particle and type of energy associated with it.
The instruments used to detect and measure various types of radiations are
given below.
Mass Spectrometer
It detects and measures the masses of heavy particles like α-rays or neutrons
easily, but it is difficult to measure the masses of light particles such as electrons
or positrons (β-rays). Hence,
β-rays are detected by measuring the energy of emission.
Although gamma rays are not particulate in nature, they are detected from the
mark of exposure left, whenever they hit the photographic plates.
Limitation
Mass spectrometer is practically not very useful due to inconvenience in
laboratories.
Gas Ionisation Devices.The selection of instrument to measure radioactivity
depends on two factors, the extent of energy emitted and penetration
ability of radiation.
The various types of gas ionisation devices are discussed below.
1. Pulse Ionisation Chambers
Ionisation chambers are filled with a gas and consists of two electrodes, which
are maintained at different electrical potentials of about 50-100 V for each
centimeter distance between them and a measuring device.
The measuring device indicates the electric current produced due to emission of
electrons, following ionisation of the gas in the chamber by the radiation.
Advantage
These chambers are available in different sizes and shapes.
2. Proportional Counters
Proportional counters are used to detect both αand β-rays. They are
modified ionisation chambers whose construction resembles that of G-M counter.
These chambers
produce large number of free electrons, each primary electron is liberated
on application of ionisation potential.
This stream of free electrons produce an amplified current pulse through electric
circuit.
This voltage range which produces ionisation of gas is called proportional region
and the measuring devices are called proportional counters.α-particles are
detected and measured at low voltage difference, whereas at high voltages, both
α and β particles are detected. β-particles can be measured by this device.
3. Geiger-Muller Counters (G-M Counters)
G-M counters are the most commonly used detectors of radiation (α, βand -
rays). G-M counter is a cylindrical chamber containing the ionising gas and a
quenching vapour. The quenching agents commonly used are chlorine and
bromine (inorganic), ethyl alcohol and ethyl formate
(organic). Their role is to prevent the motion of electric pulses from
positive ions to the cathode and to absorb photons emitted by the excited
atoms or molecules returning
to ground state.The ionising gas is filled at a pressure less than atmospheric
pressure to avoid high operating voltages.
Design and Construction
G-M counter generally consists of a cylindrical chamber of 1-2 cm diameter,
which acts as a cathode. The anode is a coaxial thin wire in the centre. The inner
space
of the chamber is filled with an ionising gas mixture and a small quantity of
quenching vapour.
G-M counters vary in design and construction depending on the purpose for
which they are used.
1.Counting Solid Radioactive Sources
(a) End Window Type G-M Counter: It is the most commonly used type of
G-M counter. Its construction is similar to the general structure, but it
contains a window which is made up of an aluminium alloy, mica or a thin
glass bubble as shown in the figure given below
b) Thin Glass-walled G-M Counter: It is used to detect and measure beta-
particles (medium and high energy) and gamma rays. It is composed of a thin
glass-walled
tube of about 1 cm diameter. The thickness of the glass wall is generally
about 20-40 mg/cm2 but varies with the length of the counter. Inner wall of the
glass
tube is coated with graphite that serves as cathode as shown in the figure

2.Counting Liquid Radioactive Sources


(a) This type of G-M counter is similar to the general
structure, with an annular space of 10 cm
3 volume
which accommodates the radioactive liquid sample.
It contains a spiral wire cathode.
Example: 3% uranium salt solution producing 10,000 counts/min can be
detected using this type of G-M counter. It is shown in figure (a) given below.

(b) Another type of G-M counter for liquids which is composed of an


annular space of 5 cm
3 volume and
connected by a plug or socket as shown in the figure (b). It mainly consists of a
thin walled tube.
3.Counting Radioactivity Gases
This type of counter is used for counting gaseous radioactive sources. In
this, the radioactive gas and ionising gas are simultaneously introduced into the
chamber. A lead or copper cathode makes the counter more efficient for
detecting γ-rays
Figure: G-M Counter for Gases
Working of G-M Counters
G-M counters require a high voltage source, low gain amplifier and a sealing unit
for its working. It also contains a probe unit which serves as an electrical switch
for recording the number of pulses, while each pulse is directing the current to
scaler and then to counting unit.
G-M counter is placed on a lead shield, which holds a source in one or more
shelves and absorbers between the instrument and source. It helps in
reducing the counting rate in the absence of a source, known as
background counting rate. In case of end window type, the reduction in
background counting is facilitated by decreasing its active length, however it may
effect the counting rate.
Generally, G-M counter operates at high voltage i.e., 100 volts above the
threshold levels, as shown in the figure.

The graph/curve represents following voltages,


A ‘Starting Voltage’ : When the voltage of the counter is being adjusted by
raising, at a specific voltage the counter starts registering the pulses which is
called starting voltage.
B ‘Threshold Voltage’ :From the point of starting voltage, both the
counting rate and the size of the pulses are markedly increased with small
change in voltage, upto a specific voltage called threshold voltage (≥ 150-200
volts). After this
voltage, the counting rate remains constant.
C ‘Plateau Voltage’ : At higher voltages, sensitivity varies and spurious
discharge of pulses occur, giving rise to slope of the plateau.
D ‘Working Voltage’: It is generally l00 volts above the threshold voltage.
Scintillation CountersScintillation counters can measure α, β and γ-rays.
Unlike the gas ionisation devices, these can detect evenchargeless
radiations (
γ-rays) with great ease. These counters make use of phosphorescent or
florescent materials for the detection of radiation, which produce scintillations o
r flashes of visible light when the radiation (photons) falls on their
surfaces.
Earlier, these counters were slow, not sensitive and tedious to work with, as
the scintillations were manually counted. However, recent advances in the
construction of these instruments has made the counting easier and
popular.
This is because of the introduction of a new type of amplifier called
photomultiplier tube, a sensitive detector. It consists of a series of photoelectric
cells directly linked
to the electron multipliers and coupled with solid-state detectors or
fluorescent material, which makes it superior to other counting instruments.
Furthermore, a thallium activated sodium iodide was introduced, which has led
to the advancement in the application of scintillation technique to gamma
counting and energy determination.
Therefore, a scintillation counter makes use of a cell, photomultiplier tube
coupled with phosphorescent or fluorescent material to amplify and convert the
flash lights produced into electric pulses.
Detection of Gamma Radiation
Gamma rays passing through a small window of the instrument, enter the
phosphor crystal (i.e., sodium iodide activated by 1% thallium) and produce
scintillations. They
are detected by the photomultiplier tubes which convert them into electric
impulses and are recorded using a scaler.

Note: High voltage applied to the photomultiplier tubes is associated with


amplifying system, but not detector.
Types of Scintillators
1. Inorganic Scintillators:
Alkali halides are the widely used compounds due to their high insulation
capacity and presence of large gap between valence band and the conduction
band.
These compounds are activated to reach excited states, which emit visible
light on decaying.
E.gs: NaI(Tl), CsI(Tl), CsI(Na), LiI(Eu), BaF2, Bismuth germanate.
NaI (Tl) is available in various shapes and sizes with high detection efficiency,
hence used for gamma counting.
2. Organic Scintillators
The most widely used organic scintillators are anthracene (high efficiency)
and stilbene (low efficiency). Liquid scintillators are used in large volume
detectors mainly for counting α and β rays with high efficiency.
Use
They are used for detecting and measuring 31H(tritium), 14C (Carbon-14).
Limitation
They have poor energy resolution.
Autoradiography
This technique is used in case of physiological studies of plants and
animals for detection and measurement of gamma rays. The radioactive
substance is administered to an animal and the localised tissue is removed after
sufficient time which is embedded in paraffin. Then it is cut into thin sections by
microtome and placed in a dark room with photographic emulsion. After
sufficient time of exposure, the radioactive substance emit particles which darken
the photographic emulsion, therefore fixing it.
Solid State Detectors
These are the most advanced detectors of radioactivity.
Types of Solid State Detectors
1. Semi-conductor Devices
These devices are composed of semi-conductors with a very small band gap of
about 2 to 3 eV and thus produce huge quantities of electron pairs per
incident radiation quantum. These conductors have high energy resolution.
They are of two types, n-type (electron rich) and p-type (electron deficient). A
semi-conductor device is a diode of both n and p-type semiconductors.
An intrinsic region, with no charge carriers, is produced when a reverse bias is
applied across the diode resulting in transport of electrons towards n-type and
holes towards p-type.
The incident radiation gets absorbed forming e–-h+ pairs whose motion is
influenced by applied electric field and the electrons get collected across a
resistance resulting in voltage pulse proportional to energy of incident radiation.

Table: Applications of Semiconductor Detectors


Photographic Emulsion (Autoradiography)
Photographic emulsions of silver halide grains are placed in a gelatin matrix and
supported with a film of glass or cellulose acetate. Silver halide grains of the
photographic film gets sensitized by the ionising radiations and remain intact,
until they are developed. These photographic emulsions are commonly used in
detecting and determining γ-radiation in physiological studies of plants and
animals.
E.gs: Radiographic films and nuclear emulsions.
3. Cerenkov Detectors
These detectors depend on the light emitting fast charged particles when passed
through an optically transparent medium (refractive index >1).
Advantages
1. They possess high resolution compared to the conventional counting
instruments.
2. They have a compact structure.
3. The interpretation of output signal is easy.
Disadvantages
1. They are expensive.
2. They require low temperatures for their working and maintenance.

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.

1. Thyroid function test is based on the quantity of radioactive iodine


taken up by the thyroid gland in 24 hours. Initially, the radioactive iodine is
administered either by oral or intravenous (i.v) route and the activity
is measured at regular intervals upto 24 hours.
(a) A normal patient (euthyroid) is expected to absorb around 1-45% of the
dose administered.
(b) When the uptake exceeds 50%, then hyperthyroidism is inferred.
(c) When the uptake does not exceed even 10%, then hypothyroidism is
inferred.However, it is necessary to carry out additional tests such as
plasma clearance and urinary excretion of the isotope to confirm the findings of
the uptake procedure.
2. Thyroid scanning procedures also utilize I-131 for determining the size,
shape, location of thyroid gland as well as the regions which have high and
low ability of concentrating iodide. Another use of such procedures
is the confirmation of thyroid tumours which have lower concentrations of the
isotope. The dose of I-131 required in these procedures is about thrice of that
used for thyroid uptake studies.
However iodine-125 is more preferred for scanning procedures as it
possesses relatively lower energy and hence lower level of exposure of
radiations to the patients.
3. Another therapeutic use of sodium iodide-I131 is in destroying the
thyroid tissue or altering the hormone secreting ability of the tissue cells.
However, for the radioactive iodine to be effective in these cases, it should
attain sufficient concentrations in iodine storage areas of the gland, as this is
necessary to alter the functioning of the thyroid cells or any neighbouring tumour
cells.
Some of the various diseased states in which this isotope is being used is
hyperthyroidism, thyroid carcinoma and cardiac disorders.
(a) Usage of sodium iodide-I131 in the treatment of hyperthyroidism
is based on the fact that this isotope would prevent the thyroid
cells from synthesizing the thyroid hormones. However, to achieve
such a goal, it is very important to use the isotope in the correct
dosage. This is because usage of low dosages would require
retreatment while usage of higher doses would completely destroy the
dividing ability of the nucleus thereby leading to hypothyroidism.
Studies conducted on I-125 for the treatment of hyperthyroidism has
shown it to be more beneficial than I-131 isotope because of lower
energy and shorter path-length radiation.
(b) Sodium iodide I-131 is used in patients who have undergone surgery for
the removal of cancerous thyroid gland. Here it helps in treating
any residual tumour mass. Hence usage of I-131 in thyroid
carcinoma offers no direct cure but is only palliative (only relieves
pain without curing the actual condition).
(c) It has been proposed that sodium iodide-I131 can also be beneficial in
the treatment of severe cardiac disorders such as angina pectoris and congestive
cardiac failure as it would induce a hypothyroid state and hence would decrease
the work load on the heart. Its usage can be helpful only when the conventional
therapy has not been successful.
Packing and Labelling
Sodium iodide-I131 solution is generally packed in single dose or multiple
dose containers. However, due care should be taken to avoid the absorption
of radionuclides on the container walls as well as that of laboratory vessels. This
can be achieved by rinsing all the vessels (which would contain sodium
iodide-I131) with a solution made up of 0.25% NaI and 0.8% sodium bisulfite
followed by rinsing with water until the rinsing is rendered neutral. Expiry date of
sodium iodide I-131 solution is 1 month from the date of standardization.
Marketed Products
Several marketed products of diagnostic preparations containing sodium
iodide-I131 available are Isotope®, Radiocaps®-131 (which are capsules) and
Tracervial® - 1311.
Similarly, therapeutic preparations of sodium iodide-I131 are available
under the brand names Onodide® I-131 (oral solution), The iodide® 131
(capsules), Iodotope Therapeutic® (capsules and solution) etc.
Doses
1. For diagnostic purpose, the usual dose of sodium iodide-I131(capsules or
solution) lies in between 5-50 mc. Doses of 300 μc are required for scanning
metastatic thyroid cancer.
2. Therapeutic doses of sodium iodide-I131 vary according to the condition.
Thyroid cancer requires a dose of about 100 - 200 mc while doses in
hyperthyroidism are based on the weight of the thyroid gland, with general range
being 80 - 120 mc/g of tissue.
6. STORAGE AND HANDLING OF RADIOPHARMACEUTICALS
Storage and handling of radiopharmaceuticals is extremely important in
avoiding the exposure to radioactive emissions and thus preventing hazardous
effects caused due to those radiations.
Radioactive materials must be stored in containers shielded with thick
glass or perspex and lead for gamma radiations. These containers should be
placed in areas which are rarely visited by people and should be regularly
checked for radioactivity. The areas where the radioactive materials are being
used should be checked for contamination. Any used radioactive material must
be disposed only after
complete discharge of its activity.
Precautions to be taken while working with detectors, tracer
experiments, radio-assays, manufacturing, handling or storage of
radiopharmaceutical are mentioned as follows,
1. Radioactive materials must be handled only by using forceps or suitable
instruments and must never be touched directly with hand.
2. While handling radioactive liquids, an absorbent tissue paper should be
placed in trays, to avoid spillage while carrying.
3. Any glass apparatus to be used should be made inactive and pipettes
operated by mouth should not be used for handling radioactive liquids.
4. Activities such as smoking, eating and drinking must be avoided in and
around the working areas of radioactive substances.
5. Proper protection of personnel working in the radioactive labs must be
ensured by the use of lead shielded clothing.
7. APPLICATIONS OF RADIOPHARMACEUTICALS
Radionuclides are widely used clinically or medicinally for,
1. Diagnostic purposes
2. Therapeutic purposes
3. Research
4. Sterilisation.
Selection of radioactive isotope plays an important role in the clinical
application. It depends on the following,
(a) Type of radiation produced/emitted
(b) Energy of radiation
(c) Properties of the radiation.
When a radionuclide is used as a tracer, its chemical identity and form of
isotope has to be identical with the element to be examined.
1. Radioisotopes in Diagnosis
Some pathophysiological conditions of the body are accurately diagnosed
by employing certain radioisotopes. They are used to study their fate in
the body or estimation of the amount in an organ by radio immuno assays

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

These radionuclides are administered either internally or externally,


(a) External Use of Radioisotopes
They are externally administered or implanted in tissues as sealed capsules.
Their action can be terminated by removing the dose or sources from the body.
(b) Internal Use of Radioisotopes
They are administered internally as unsealed sources into the systemic
circulation. Once the dose is given, the action of these nuclides cannot be
terminated as it is difficult to remove the source from the body.
They can be administered internally by,
(i) IM (Intramuscular Injection): For radiation of deep tissues
(ii) IV (Intravenous Injection): Into the systemic
circulation, if the
nuclide has selective affinity to a specific tissue.
Calculation of total dose of nuclide for therapeutic application is based on,
(a) Concentration of the nuclide
(b) Half-life (t½) of the nuclide
(c) Type and energy of the radiation emitted (as radiations with greater
energy (MeV) are harmful to surrounding tissues).
Among the radiations emitted by the radioisotopes, γ-rays are of shorter
wavelength and higher penetrating power than β and α-rays. Thus, short
exposures of γ-rays is sufficient to destroy cancer or tumour cells in the
patients and is called as radiation therapy. This is usually combined with
chemotherapy and repeated
at regular intervals of time.
Examples
(a) Radiolabelled Cobalt
(i) Cobalt gun (60Co) is employed in the therapy of cancers of abdomen
and lower parts of the body.
(ii) Other isotopes of cobalt used in therapy are 57Co, 58Co.
(b) Radiolabelled Gold (198Au)
It is usually administered as colloidal gold suspension. It is employed in
the therapy of cancers of uterus and urinary bladder. It is also used in the
treatment of abdominal and pleural effusions produced in case of malignant
tumours in lungs and abdomen.

(c) Radiolabelled Phosphorous (32P)


It is given internally to produce β-radiations for the treatment of
neoplastic tumours. It is also used as sodium phosphate (32P) to
treat polycythemia vera caused due to leukaemia by decreasing the
rate of erythropoiesis.
(d) Radiolabelled Iodine
(i) 131I finds use in radiation therapy of thyroid disorders.
(ii) 125I is administered internally to treat deep seated chest
tumours by emission of low energy gamma radiations.
Certain chemicals, that naturally concentrate in organs or tissues of the body,
are labelled with radioisotopes to enhance the selective accumulation of the
nuclides.
For example, some antibodies labelled with technetium-99m (99mTc) that
bind to specific antigen are used to find its effect on a specific site of the body.
3. Research
Biological and medicinal research uses various radioisotopes as tracers for
their study. Such extensive studies have resulted in detailed knowledge of many
biochemical processes. Carbon-14 (C14)and Tritium (H31) are the commonly used
radioisotope tracers.
ExampleStable isotopes of carbon, calcium, hydrogen, chromium and
iron are usually applied in research. Other isotopes of sodium, magnesium,
calcium, copper and cerium have also been employed as radioisotope
tracers.
4. Sterilization
Surgical instruments in hospitals and most of the pharmaceuticals in their
final packed containers are sterilized using constant radiations emitted from
some strong radiation sources. Since, this type of sterilization involves no
chemicals or heat, many pharmaceuticals and various thermolabile substances
such as vitamins, hormone and antibiotics are safely sterilized. For instance,
Cobalt-60 or Cesium-137 is used as radiation source to sterilize pharmaceuticals
and mainly surgical instruments.However, some pharmaceuticals get ionized due
to radiations and are destroyed. Hence, care should be taken in employing this
method of sterilization.

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

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