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Radio Pharmaceutical

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12 views21 pages

Radio Pharmaceutical

Uploaded by

Rifaaa
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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RADIOPHARMACEUTICA

LS
CONTENT
S  RADIOPHARMACEUTICAL
 COMPONENTS OF RADIOPHARMACEUTICAL
 IDEAL RADIOPHARMACEUTICAL
 DESIGN OF NEW RADIOPHARMACEUTICAL
 FACTORS INFLUENCING THE DESIGN OF NEW
RADIOPHARMACEUTICAL
 RADIOPHARMACEUTICALS USED IN HOSPITALS FOR
DIAGNOSIS
RADIOPHARMACEUTIC
AL
 A RADIOPHARMACEUTICAL is a radioactive compound
used for the diagnosis and therapeutic treatment of
human disease.

 In nuclear medicine nearly 95% of the


radiopharmaceuticals are used for diagnostic purposes,
while the rest 5% are used for therapeutic treatment.

 Radiopharmaceuticals usually have minimal


pharmacologic effect, because in most cases they are
used in tracer quantities. Though in therapeutic field
they can cause tissue damage by radiation.
 A radiopharmaceutical may be a radioactive element
such as 133Xe, or a labeled compound such as 131I-
iodinated proteins and 99mTc labeled compounds.

 Radiopharmaceutical are also known by other terms


such as radiotracer and tracer
 Many different organs can be imaged depending on
the type of radioactive medication used. The
radioactive medication is most commonly injected
into the blood stream through a vein, but might be
given in different ways, including:
ADMINISTRATIO  swallowed;
N  injected directly into the tissue beneath the skin;
 injected into a shunt;
 injected into a joint; or
 inhaled (breathed in).
Components of
radiopharmaceu  A radiopharmaceutical has two components:
tical 1. a radionuclide
2. a pharmaceutical
 In designing a radiopharmaceutical, a pharmaceutical
is first chosen on the basis of its preferential
localization in a given organ or its participation in the
physiologic function of the organ.
 After that, a suitable radionuclide is tagged onto the
chosen pharmaceutical .
 After administration of the radiopharmaceutical,
radiations emitted from it are detected by a radiation
detector.
Ideal
radiopharmaceut Easy availability
ical  The radiopharmaceutical should be easily produced,
inexpensive, and readily available in any nuclear
medicine facility.
Short effective half life
 half-life is the time needed for half of the
radiopharmaceutical to disappear from the biologic
system .
 Radiopharmaceuticals should have a relatively short
effective half-life ,which should not be longer than the
time necessary to complete the study
Particle emission
 Radionuclides decaying by α or β particle emission
should not be used as the label in diagnostic
radiopharmaceuticals as these particles cause more
radiation damage.
 Although many beta emitting radionuclides are used
such as 131 I. But alpha particles should not be used
for clinical studies.
High target to non target activity ratio
 The radiopharmaceutical should be localized
preferentially in the organ under study since the
activity from non target areas can obscure the
structural details of the picture of the target organ.
 Therefore, the target-to-non target activity ratio
should be high.
Design of new
radiopharmaceu
tical General
considerations
 A radiopharmaceutical should be designed to
evaluate the function and/or structure of an organ of
interest.
 The method of preparation should be simple, easy,
and reproducible, and should not alter the desired
property of the labeled compound.
 Optimum conditions of temperature, pH, ionic
strength, and molar ratios should be established and
maintained for maximum efficacy of the
radiopharmaceutical.
 Once a radiopharmaceutical is developed its clinical
efficacy must be evaluated by testing it first in
animals and then in humans
Factors influencing
 The following factors need to be considered before,
the design of new during, and after the preparation of a new
radiopharmaceutical radiopharmaceutical.

Stoichiometry
 In preparing a new radiopharmaceutical, one needs
to know the amount of each component to be added.

Charge of the
molecule
 The charge on a radiopharmaceutical determines its
solubility in various solvents. The greater the charge,
the higher the solubility.
Size of the molecule
 The molecular size of a radiopharmaceutical is an
important determinant in its absorption in the biologic
system. Larger molecules (mol. wt. > ~60,000)are not
filtered by the glomeruli in the kidney.

Protein binding
 Almost all drugs, radioactive or not, bind to plasma
proteins to variable degrees. Protein binding is greatly
influenced by a number of factors, such as the charge on
the radiopharmaceutical molecule, the pH, the nature of
protein, and the concentration of anions in plasma.
 Protein binding affects the tissue distribution and plasma
clearance of a radiopharmaceutical and its uptake by the
organ of interest.
Solubility
 For injection, the radiopharmaceutical should be in
aqueous solution at a pH compatible with blood pH
(7.4).
 Lipid solubility of a radiopharmaceutical is a
determining factor in its localization in an organ. The
higher the lipid solubility of a radiopharmaceutical,
the greater the diffusion through the cell membrane
and hence greater its localization in the organ.
Stability
 It must be stable both in vitro and in vivo.

Bio distribution
 It includes tissue distribution, plasma clearance,
urinary excretion, and fecal excretion after
administration of the radiopharmaceutical.
THANK
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