BY

Mrs. K.SHAILAJA., M. PHARM.,

LECTURER
DEPT OF PHARMACY PRACTICE,
SRM COLLEGE OF PHARMACY
INTRODUCTION
DEFINITION:
Radiopharmaceuticals are the radioactive substances or
radioactive drugs used for diagnostic or therapeutic inventions.
PRINCILPLE:
y Unstable or radioactive isotopes have a property to decompose
or decay by emission of nuclear particles and some of them are
used in diagnostic or therapeutic interventions.
y The three main types of radiation decay are α particles , β
particles , γ photons.
™ α particles have the largest mass and charge of the 3 typesof
radiation consisting of two protons and two neutrons thus being
identical with the He nucleur.
™ β particles are electrons . They are not as destructive as α
particles but can be used therapeutically.
™ γ rays are electromagnetic vibrations comparable with light but
of much shorter λ .because of their short wavelength and high
energy, they are very penetrating.
™ Thus , the clinical utility of a radiopharmaceuticals is
determined mainly by a physical properties of
radionucleide.(eg. Radiation, energy, half life)
™ For therapeutic use, however radionucleides should emit
particulate radiation(i.e.β particles),which deposits the
radiation within the target organ.
™Radioiodine is a prime example and used for the 
hyperthyroidism and eradication of metastatic disease of 
thyroid gland.

™Since Iodine 131 emits both β and γ radiation, it can be used 

diagnostically(γ rays) and therapeutically(β rays).

™Fraction of nuclei disintegrating with time is always 
constant on progressively fewer atoms are left.
DIAGNOSTIC IMAGING
Therapeutic isotopes are utilised for their destructive effects on
tissue.It is necessary that they have sufficient energy to
penetrate throughout the tissue being treated, but
radioactivity spreading to surrounding tissue is undesirable,
however and difficult to control.
¾ Radiopharmaceuticals are used to diagnose the 
presence of disease or evaluate the progression of 
disease following a specific therapy intervention. 
Radiopharmaceuticals can also be used to evaluate 
drug induced toxicity and to a lesser extent have been 
used to treat diseased tissue with radiation.

¾ Imaging procedures are classified either as dynamic 
and static. Dynamic study provides useful info through 
the rate of accumulation and removal of 
radiopharmaceutical from a specific organ.A static 
study provides perfusion and morphological status of 
organs assessing adequacy of blood flow, organ size, 
shape, position, chances of space occupying  lessions
etc.
 USES OF RADIOPHARMACEUTICALS
Diagnostic uses
y serves as traces
y when introduce into the body,emit radiation that is subsequently 
detected and measured e.g. to analyse thyroid function‐radioactive 
iodine(orally)the thyroid is then scanned to determine radioiodine 
concentration and location.Greter than normal update by the 
thyroid indicates hyperthyroidism.
Therapeutic uses
y Radioisotopes are used as internal or external radiation sources to 
treat disorders such as hyperthyroidism and cancer.
y Internal radiation source
y Radioisotopes administered orally or intravenously or implanted 
in the target tissue or organ will roduce radiation that destroyes
disease results and prevents new tissue growth.
y External radiation source
y Radiotion used for therapy in cancer patients.
Use of radiopharmaceuticals in
different organ systems
Pulmonary systems
used in lung perfusion scans,to detect acute pulmonary embolism
and ventillation scans which help differentiate pulmonary
embolism from chronic obsructive pulmonary disease
examples 1)macro-aggregated albumin
2)Xenon 133 gas
Skeletal systems
nuclear bone scans are particularly valuable for detecting
cancer metastasis.
The radionuclei is absorbed onto hydroxy appetite bone matrix
via chemisorption. E.g.methylene diphosphamate stanus
chloride.
Hepatobilliary system
Various radiopharmaceuticals used are as follows:
y Sulphur cloride
y Iodine 131 sobium rose pengal
y Disofenin
Renal system
y glucoheptonic acid
y DMSA( 2,3 dimer- capto succinic acid)
y DTPA(diethylene triamine pentacetic acid)
Cardiovascular system
y pyrophosphate
y Thallous chloride 201
miscellaneous agents
y Sodium iodide 123
y Gallium citrate 67
 Criteria for a optimal
radiopharmaceutical
y Should have a relatively short half life
y Should emit γ paricles
y The energy should range from 30-300 kilo electron volts.
y Metabolic stability-1st order kinetics –to localize the target
site differ vein metabolised
y Organ specificity
y Excretion
y Availability
y Technitium 99m is currently the most widely accepted
radioisotope for imaging studies.
 Half life of radiopharmaceuticals
y Physical half-life refers to the time needed for a
radioactive substance to lose 50% of its activity through
decay.
y Biological half-life refers to the time needed for the body
to eliminate 50% of the radioactive substance.
y The combined effect of physical and biological half-life
determines the effective half-life required for the
radioactivity of an administered radioisotope to decrease
by 50%.