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RADIOPHARMACEUTICALS
RADIOPHARMACEUTICALS
• The Main Group of These compounds are the radiotracers used to diagnose
• The elements are known as radioactive because they are unstable and undergo
radionuclides.
Alpha Rays
• These rays or particles have least penetrating power, positive charge and can be
• These particles produce about 30,000 ion pairs per cm of path when they pass
• Because of low penetrating power of alpha particles, elements which emit alpha rays
do not find use in biological applications because they cannot penetrate tissue.
226 222
Ra
86 86 Rn +42He
• All alpha particles are having the same energy.
Beta Rays
• They have negligible mass, about 1/1836 that of the hydrogen ion.
Gamma Rays
• They have more penetrating power than alpha and beta rays.
• They are having the same character as that of very short electromagnetic waves
called X- rays.
• The penetrating power of gamma radiation has been found to depend on atomic
• They are produced during disintegration of radioactive substances along with beta
termed as isotopes. The isotopes have been differing in nuclear masses and thus in atomic
Radio isotopes have been those that undergo nuclear changes or rearrangements
that cause the emission of radioactive radiations. Just as atoms and molecules undergo
chemical reactionsso do nuclei with one another and with neutrons which are termed as
nuclear reactions.
When the radioactive isotopes undergo nuclear reactions, they produce alpha, beta,
and gammaparticles.
The nucleus obtained after the nuclear changes or rearrangement may be that of a
different element which may be stable. The original nuclide is called the parent and the
decay.
Stability of isotopes.
The naturally occurring nuclides are having favorable ratio of protons and neutrons
in most elements. Any deviation from the natural ratio, i.e., increase or decrease in the
number of neutrons alters the atomic number, and the stability of the nucleus.
Thus, the stable ratio for potassium is 1:1.115. If one more neutron is added to the
Similarly, any addition or removal of a neutron from the nucleus of iodine causes
instability.
Most isotopes of elements with Z no. 83 or less are stable and are described as
stable isotopes. However, some of the naturally occurring nuclides with Z no. less than 83
are unstable. All the nuclides with Z no. above 83 whether naturally occurring or
RADIONUCLIDES TYPES–
1)Natural Radionuclides - consists of 40 high atomic weight elements like U, 226Ra (could
238
be alpha, beta or gamma emitters) and moderate atomic weight elements like K &37Rb.
40
2)Artificial Radionuclides- also known as synthetic radionuclides, are not found in nature
&are very unstable hence decayaway in a short period of time. For example, 95Tc and 146Pm
CHARACTERISTICS OF RADIONUCLIDE-
2) Half life
the decay of the individual atom, i.e., atomic nuclei of the radioactive substance (which
means there is occurrence of spontaneous changes of particles and energy emitting into
other nuclear species) which has been found to be irregular where half of a given number
of radioactive nuclei decay and half of them remains un-decay. After a certain amount of
time, when the measurement of number of disintegrations per second is done along with
taking a certain amount of radionuclide, it is seen that, half of the total amount of original
atoms would have got disintegrated, whereas, the other half of the original active atoms
would be left behind. Hence, in this way, the number of disintegrations per second will
equivalently also now be the half of the original value. Irrespective of the quality is
present, the decay time of the radionuclide has been constant to its half and this time has
Half-life, t = 0.693 (Where, λ = is the disintegration constant in the unit of sec -¹,
Half-lives vary very considerably for various radionuclides. Let us consider some examples
In the case of medicines, the T½ of a nuclide will decide its utility. Inconvenience can be
caused for setting up satisfactory experiments if the T½ is too short. On the other handit
fissionable material in a moderator, which slows down the fast neutrons to thermal
energies. The fissionable material like uranium is taken in the form of rods which
are arranged in a lattice pattern. A heavy water moderated reactor using enriched
uranium for example: Harwell reactor DIDO is having a maximum neutron flux of
59 1 60
27 Co + 0 n 27Co + ɣ
Cyclotron Irradiation: In this, charged particles usually protons are accelerated to a high
velocity so as to overcome the repulsion from nucleus. The beam of the particles are
generally small and the cost is high, the number of samples that can be irradiated at a
time has been limited and the yield is also low. But on the other hand, many isotopes which
otherwise cannot be produced in a reactor could be produced in the cyclotron and also it
Measurement Of Radioactivity
In order to measure the radiation of alpha, beta, and gamma particles, many techniques
involving detection and counting of individual particles or photons have been available. The
gas ionisation devices include pulse Ionisation Chamber, Proportional Counter and Geiger-
Muller Counter. Scintillation methods are specially employed for counting gamma
radiations.
The method selected for the measurement of radioactivity depends upon the extent of
Ionisation Chamber - The ionization chamber is the simplest of all gas-filled radiation
detectors and is widely used for the detection and measurement of certain types of
detector device used to measure particles of ionization radiation. The key feature is
its ability to measure the energy of incident radiation, by producing a detector output
pulse that is proportional to the radiation energy absorbed by the detector due to an
ionizing event hence the detector’s name. It is widely used where energy levels of
incident radiation must be known, such as in the discrimination between alpha and beta
III. Geiger counter – A Geiger counter still the most popular radiation detector They
do not the use of a high-gain amplifier and they can detect alpha, beta and gamma
radiation. It used for detecting and measuring ionizing radiation. It I widely used in
applications Such as radiation dosimetry, radiological protector, experimental physics
and the nuclear industry.
material as the detecting medium. These detectors produce pulse of electric current by
means of pairs of charge carriers, electrons and holes, generated when the detectors
Geiger-Muller Counters.
These are still the most popular radiation detectors. They do not need the use of a high-
gain amplifier and they can detect alpha, beta, and gamma-radiation
A G-M counter is having the ionising gas and is also having a quenching vapour whose
functions have been to prevent the spurious pulses that may get produced due to the
positive ions reaching the cathode and to absorb the photons emitted by excited atoms
and molecules returning to the ground state. Both chlorine and bromine are generally
employed as quenching agents. Ethyl alcohol are used as organic-quenching agents. The
filling gas pressure has been much below the atmospheric pressure for avoiding the use of
It consists of a hollow metal case enclosed in a thin glass tube. This hollow metal
A fine tungsten wire is stretched along the axis of the tube and is insulated by
The tube is evacuated and then partially filled with a mixture of 90% argon at 10
through a resistance R and the negative terminal is connected to the metal tube.
The direct current voltage is kept slightly less than that which will cause a
At one end of the tube a thin window of mica is arranged to allow the entry of
Principle of Geiger-Muller counter
The basic principle of the Geiger Muller counter can be understood as follows. When an
ionizing particle passes through the gas in an ionizing chamber, it produces a few ions. If
the applied potential difference is strong enough, these ions will produce a secondary ion
avalanche whose total effect will be proportional to the energy associated with the
If the applied potential difference is very high, the secondary ionization phenomenon
becomes so dominant that the primary ionizing event loses its importance. In other words,
the size of the final pulse produced depends only on the triggering off of ionization by an
A high energy particle entering through the mica window will cause one or more of the
argon atoms to ionize. The electrons and ions of argon thus produced cause other argon
atoms to ionize in a cascade effect. The result of this one event is sudden, massive
electrical discharge that causes a current pulse. The current through R produces a voltage
pulse of the order of 10μV. An electron pulse amplifier accepts the small pulse voltage and
each incoming particle produces a pulse, the number of incoming particles can be counted.
The chamber is filled with an inert gas (helium, neon, or argon) at low pressure. Ahigh
voltage is applied to this chamber. The metallic chamber will conduct electricity. When
radiation enters the chamber through the window, the photons in the radiation will ionize
the inert gas inside the chamber. This will make the gas conductive. The electrons
produced due to ionization are accelerated due to the potential that we applied and these
electrons cause even more ionization. The ionized electrons travel towards the anode. The
anode is connected to a counter. The counter counts the electrons reaching the anode.
Radiopharmaceutical
A care should be taken to protect the person from harmful radiation of radioactive during
storage and handling of radioactive material. In order, to have protection from hazard of
radiation, radioactive material must be stored in a separate area where not frequently
visited by people and usually provide sufficient shielding in a thick glass. Similarly, in order
to protect from gamma radiation, lead shielding has to be used and must be regularly
checked its storage area for radioactivity. Or when radioactive liquid to be handled it
must be carried in trays, so that, spillage will get absorb in absorbent tissue paper. And
The following precautions have to be taken during handling and storage of Radioactive
substance÷
Direct contact should be avoided. It should be handled with forceps
or suitable instruments.
Smoking, drinking and eating should be avoided in
must be used.
It should be stored in suitable labelled container and shield by lead brick in remote
area.
APPLICATION OF RADIOISOTOPES
The radioisotopes have numerous applicationsin medicine,agriculture,industry and pure
1. Diagnosis diseased-states
Radioisotopes and their formulations find varied application in the diagnosis therapy and
healthcare. The radiations given out by some and very effecting in curing diseases.
The isotope is for detection only and should have minimal effect on body tissue.
Radioisotopes are also havingan important role in the field of agriculture. Radioisotope
were used for producing high yielding crop seeds to increase the agricultural yield.
Radiation from certain radioisotope were also used for killing injects which damage food
Fertilizers labelled with radioactive isotope such as phosphorus-32 and Nitrogen-15 have
been used to study the uptake, retention and utilization of fertilizers. Excessive use of
fertilizers effect biodiversity and damages the environment. The radiation helps to
Science and industry uses radioisotopesin a variety of way to improve productivity and in
some cases to gain information that cannot be obtained in any other way.
Sealed radioactive sources are used in industrial radiography gauging application and
mineral analysis.
Short lived radioactive material is used in float racing and mixing measurements. Various
radioactive decay series are used to measure the edges of materials incorporating them.
Gamma sterilization is used for medical supplies some bulk commodities and increasing
The use of radioisotopes in industry in shows good quality products and bring down the
process control.Radio traces are also used in the oil and gas industry to help determine the
subsurface.
Application of radioisotope in biological sciences:
Radioisotopes are frequently used for tracing metabolic pathways. Mixing Radiolabeled
substrates and sample of the experimental material and collecting samples at various
Times extract and separate the products by chromatography. Radioactivity detector can
Cesium-137 and Cobalt-60 are both used to shrink the size of tumors within the bodies
of Cancer patients.
Radio isotopes are used to diagnose and treat other disorders such as Chromium-51, which
Radioisotope is used for labelling of cells all entities for identification for tracing specific
molecule in an organism. Radioactive carbon-14 decay could be used to the age of organic
materials.
Thyroid Glands
The thyroid, or thyroid gland, is an endocrine gland in vertebrates. In humans it is in
the neck and consists of two connected lobes. The thyroid is located at the front of the
neck, below the Adam's apple. Microscopically, the functional unit of the thyroid gland is
rate and protein synthesis, and in children, growth and development. Calcitonin plays a role
hypothalamus.
occurs when your thyroid gland produces too much of the hormone thyroxine.
Hyperthyroidism can accelerate your body's metabolism, causing unintentional weight loss
and a rapid or irregular heartbeat. Several treatments are available for hyperthyroidism.
Hypothyroidism - Hypothyroidism (underactive thyroid) is a condition
in which your thyroid gland doesn't produce enough of certain crucial hormones
wide ranging
Goiter -A goitre, or goiter, is a swelling in the neck resulting from an enlarged
thyroid gland. A goitre can be associated with a thyroid that is not functioning properly.
Worldwide, over 90% of goitre cases are caused by iodine deficiency. The term is from
the Latin gutturia, meaning throat.
Radio pharmaceuticals: -
Radio pharmaceuticals are the radioactive substances or radioactive Drugs for diagnostic
or therapeutic interventions.
Composition: -
A radioactive isotope that can be injected safely into the body, and a carrier molecule
Radio isotope: -
A version of chemical element that has an unstable nucleus and emits radiation during its
Work: -
The radiotracer, injected into a vein, emits gamma radiation as it decays. A gamma camera
Uses: -
specific disease site, such as cancerous tumors, with high specificity in the
metastasis.
Advantages: -
Nuclear medicine procedures have no side effects and are complete ly safe.
Disadvantages: -
Nuclear medicine tests are not recommended for pregnant women because unborn babies
Filling in patient’s teeth, dental braces and permanent bridges may cause some distortion
Radionuclide Identification
The spectrum of iodine-131 has been complex but the most abundanttype of
photon is having an energy of 0.364 McV.
The gamma-ray scintillation spectrum of the sodium iodide 1-131solution is
same as specimen of 1-131 of known purity, which exhibits major
photoelectric peak having an energy of 0.365 MeV.
Radiochemical Purity
The test for radiochemical purity has been performed in such a way that all
the radioactivity of the solution has been due to iodide ion and not due to
iodate ion.
It is carried out by preparing a chromatogram and showing that the
radioactive part of the paper chromatogram has been coinciding with the
position of the iodide ion and that the site of the iodate ion has been
inactive.
solution has to be diluted with water until its activity has been equivalent to
about 20,000 counts per minute.
It is mixed with an equal volume of a solution having 0.1% w/v of KI, 0.2%
w/v of KIOg and 1 per cent w/v of NaHCO3. Two drops of the above mixture
are put on a strip of chromatographic paper and allowed to dry
On the same paper separate drops of a l% w/v solution of K1 and a 2% w/v
solution of KIOg, are placed and allowed to dry. The chromatogram is
developed by ascending chromatography by employing a mixture of 3 volumes
of methyl alcohol and I volume of water.
the positions of inactive potassium iodide and potassium iodate spots could
be determined by the application of two filter papers one impregnated with
acetic acid and potassium iodate solution to detect the iodide, and the other
impregnated with acetic acid and potassium iodide solution to detect the
iodate. lodine will get liberated at the site of the spot and would be seen.
It is possible to detect the radioactivity distribution by autoradiography or
by scanning with a collimated Geiger-Muller counter
Potassium salts, iodide and iodate, have been acting as carriers for the
iodide ions and for any iodate ion present in the Sodium Iodide I-i3l solution.
Assay
It is possible to determine the activity by a suitable counting equipment by
comparison with &standardize 1:131 solution or by measurement of an instrument
Iodine-13i has been emitting both beta particles and gamma rays in its decay
process.
Other requirements
labelling and expiration date have been almost similar to those for other radioactive
solution
expiration date for Sodium Iodide Solution has been not later than one month after
the date of standardization.
Uses
the most common isotope and chemical form in use and a diagnostic aid for studying
the functioning of the thyroid gland
involves the measurement of the uptake of radioactive iodine in a 24 hour period.
The euthyroid (normal) patient will be taking up from 1% to 45% of the
administered dose in 24 hours.
If the uptake has been found to be less than 10% the patient has been hypothyroid,
and an uptake of over 50% has been an indication of hyperthyroidism. Other
measurements may be carried out for confirming the results of uptake procedures,
i.e., plasma clearance and urinary excretion of the isotope.
Scanning procedures can be carried out with iodine- 125 which is having the
advantage of lower radiation exposure to the patient due to the lower energy.
Sodium Iodide 1-131 is also used therapeutically for destroying thyroid tissue or at
least to alter the function of the tissue cells.
The disease states in which this isotope is being used are hypothyroidism
(thyrotoxicosis) thyroid carcinoma, and severe cardiac disease.
The tissue effect has been primarily due to the beta radiation which is of relatively
short range. Therefore, the isotope must get concentrated in the iodine storage
areas (colloid) of the gland so as to have any effect on cells synthesizing thyroid
hormone (thyoxine) or on any adjacent tumor cells.
The using of sodium iodide I-131 in the treatment of hyperthyroidism is carried out
with the intention of impairing the hormone synthesizing capability of the apex of
the thyroid cells.
Radioactive iodine in thyroid carcinoma has been at best only palliative, offering no
direct cure. The isotope has to be used most frequently after surgical removal of a
cancerous thyroid as a means of treating any residual tumor tissue.
It is possible to ease severe cardiac diseases through the use of sodium iodide I-
131, which is used to induce a hypothyroid state as a means of reducing the work
load on the heart.
Sodium Rose Bengal I-131 injection,C20H2Cl4I4Na2O5.Rose Bengal Is dye which was used
for many years as a colorimetric diagnostic aid in liver function detemination.
When injected intravenously,the dye is rapidly and selectively taken up by polygonal
cells of the normally functioning liver after 30 min.
After this time the dye is excreted into the intestine.
Sodium rose Bengal labelled with I-131 is useful as a radioactive tracer in:
1.The determination of liver function.
2.Provided information about the hepatic blood follow in the liver.
3.Used as indication of possible obstruction.
4.This preparation remain in the liver long enough to provide radio active photo scan
of the liver by determining: The Size , location, and the presences of abscesses,
cysts, Tumor.
Since the metabolism of the dye and its uptake by thyroid are possibilities, the
patient should be given(Lugol solution) at least 24 hrs before taking the preparation
, in order to make saturation of the thyroid by iodine from lugols solution.
It is prepared by refluxing rose Bengal acid with,radioiodide produced by the action
of an oxidizing agent on sodium radioiodide for about 15-20 hours.
The radioiodinated rose Bengal so produce is precipitated with acid,then washed
with water,and converted into its sodium salt by treatment with sodium hydroxide.
The product may be sterilized by autoclave or filtration formulated with propylene
glycol, and preserved at refrigerated temperatures.
Uses.
Certain compounds get excreted exclusively through the kidneys if one of the two
kidneys has been functioning properly, each would excrete nearly the same amount
of the above substances when present in blood in excess of the renal threshold.
The sodium iodohippurate 1-131 injection when administered intravenously is
excreted quickly and exclusively by the kidneys. I-131 has been emitting beta-
particles of 0.608 MeV energy and gamma-rays of 0.364 MeV energy.
Detection.
For external detection of the isotope, it becomes essential that the radionuclide
emits gamma-rays. As I-131 emits gamma-rays also, sodium iodohippurate 1-131 gets
administered intravenously and its relative concentration in each kidney may be
measured by using two identical crystal scintillation detectors, which have been
positioned one over each kidney.
IODINE-131
Most frequently employed of the two isotopes
Emits both b&c radiation for producing a rather complex emission spectrum
bombardment of tellurium-130, resulting the isotope along with c & b emission: Te (h, c) I.
Important emissions from iodine-131 for medical purposes have been the
0.608 MeV beta & the 0.364 MeV c (from metastable xenon-131) & half-
life
IODINE-125
Has been emitting significantly lower energy radiation than iodine-131.
In neutron reactor, isotope gets formed from the conversion of xenon , with
124
emitting c & K-capture X-radiation: Xe (n, g) K125 53I.
54
The iodine-125 then decays having a half-life of 60 days first emitting 0.027
isotope.
Both iodine-125 and iodine-131 can be produced in the reactor for producing
essentially carrier-free isotopes; i.e., they are free of, or have only trace
indicated for use in the determination of total blood and plasma volume and other
buffer with I –131 released from a NaI – NaIO3 mixture by adding HCl . The reaction
occurs almost instantaneously at a pH of 9.3. The 3 atoms of I – 131 get incorporated per
molecule of albumin. The protein may be purified by passing the reaction mixture over an
anionic exchange resin, when unreacted iodine gets removed. The Iodinated albumin may be
refrigerated temperature.
INDICATION :
It is indicated for use in determination of total blood and plasma volumes, cardiac
output, cardiac and pulmonary blood volumes and circulation times, and in protein
turnover studies, heart and great vessels delineation, localisation of the placenta
It also include the determination of body fluid volumes and the imaging of certain
tissue.
FERRIC CITRATE Fe-59
Fe-59 is an isotope of iron. It has a half life of 44.5 days and it is a beta and a
Monitoring badges should be worn by any person while handling open sources of Fe-
plasma iron clearance, plasma iron turnover rate and the utilization of iron in new
red blood cells. The preparation is administered orally for studying the absorption
determining plasma iron clearance and turnover, and the incorporation of iron into
erythrocytes.
Ferric citrate Fe-59 is usually put in a sterile solution having about 30µc per ml.
The solutions are preserved in benzyl alcohol and they are having an antioxidant
formation and destruction like spleen, sacrum and liver from outside the body. It
also under the trade name of Ferrutope. The usual oral and intravenous dose have
Sodium Phosphate P - 32
Sodium Acid Phosphate NaH2P³²O4 and Sodium Basic Phosphate Na2HP³²O4 are the two
forms in which the radioactive isotope of P - 32 is present. The emission of the Beta
Particles takes place. Radioactive isotope of P - 32 has a half-life of 14.3 days. It is used
in various kinds of treatments like;
³² ¹⁴ • ³ d ³²
P ––––––––––> S + 1.71 MeV β−
¹⁵ ¹⁶
● Oral.
● Intravenous.
The solution and the glass container may gradually darken while standing due to the
radiation even though the solution is originally clear as well as colorless. The pH of the
solution lies between 5.0 and 6.0 which indicates that the chemical form of the
preparation for the solution has been proved to be the mixture of Disodium Hydrogen
Phosphate (Na2HPO4) as well as Sodium Dihydrogen Phosphate (NaH2PO4).