FAR 458 : Nuclear Pharmacy

Use Of Radioisotopes In
Medicine

Mohd Ikhwan Hashim RPh

Nuclear Pharmacy Unit, AMDI, USM
 Presentation Outline

• Radioisotopes In Diagnostic
• Radioisotopes In Therapeutic
• Radioisotopes Use In Medicine
DIAGNOSTIC
Application Of Nuclear Medicine
In Diagnostic
• Using radiation ; information regarding the
functioning of a specific organ in the human
body or to treat a disease.
• Radioactive isotopes in medicine are used to
form images of the thyroid, bones, heart, liver
and many other organs.
• Radioactive isotopes used in medicine have also
helped in treating diseased organs and
tumors.
 Diagnostic
Radiopharmaceuticals
Diagnostic techniques in nuclear
• Diagnostic techniques in nuclear medicine
use radioactive medicine
tracers which emit gamma
rays from within the body.
• These tracers are generally short-lived
isotopes linked to chemical compounds which
permit specific physiological processes to be
scrutinized.
• These radiotracers can be given by injection,
inhalation or orally.
• Tc-99m-HDP for bone scan imaging
 Indication Of Diagnostic
Radiopharmaceuticals
• examine blood flow to the brain,
• functioning of the liver, lungs, heart or
kidneys,
• to assess bone growth,
• the effects of surgery
• assess changes since treatment.
A radioisotope used for diagnosis must emit
gamma rays of sufficient energy to escape
from the body and it must have a half-life
short enough for it to decay away soon after
imaging is completed.
 Diagnostic
BLOOD RADIOLABELLING
•
Biochemical Analysis
It is very easy to detect the presence or absence of
some radioactive materials even when they exist in
very low concentrations.
• Radioisotopes can therefore be used to label
molecules of biological samples in vitro (out of the
body).
• Pathologists have devised hundreds of tests to
determine the constituents of blood, serum, urine,
hormones, antigens and many drugs by means
of associated radioisotopes.
• These procedures are known as radioimmuno-
assays and, although the biochemistry is complex,
kits manufactured for laboratory use are very easy
to use and give accurate results.
 Diagnostic ;
Positron Emission Tomography
• Positron Emission Tomography (PET)- a more
precise and sophisticated technique using
isotopes produced in a cyclotron.
• A positron-emitting radionuclide is introduced,
usually by injection, and accumulates in the
target tissue.
• As it decays it emits a positron, which promptly
combines with a nearby electron resulting in the
simultaneous emission of two identifiable
gamma rays in opposite directions
• These are detected by a PET camera and give
very precise indication of their origin
Electron–positron annihilation
 Diagnostic ;
Positron Emission Tomography

• New procedures combine PET with

Computed X-ray tomography (CT) scans to
give co-registration of the two images
(PETCT), enabling 30% better diagnosis than
with traditional gamma camera alone. It is a
very powerful and significant tool which
provides unique information on a wide variety
of diseases from dementia to cardiovascular
disease and cancer (oncology).
 Properties of a diagnostic radiopharmaceutical

1. Pure gamma emitter

•radioisotope should be a pure gamma ray emitter, decaying
by either electron capture or isomeric transition
•alphas and betas are not image-able – non-penetrating
radiation, high LET, radiation dose
 Properties of a diagnostic radiopharmaceutical

2. 100 < gamma energy < 250 keV

•ideal imaging energy range is 100-250 keV
•Image quality is suboptimal above or below it
•Use of these higher energies compromises image quality
since greater collimation is required, decreasing both
sensitivity and resolution
•Commonly used radioisotopes considered ideal from an
energy standpoint include Tc-99m, In-111, and I-123
 Properties of a diagnostic radiopharmaceutical

3. Effective half-life = 1.5 X test duration

•Minimize radiation dose and maximize dose for optimal
image quality
•The relationship between effective half-life [t(eff)],
biological half-life [t(biol)] and physical half-life
[t(phys)]
1 / t(eff) = 1 / t(biol) + 1 / t(phys )
 Properties of a diagnostic radiopharmaceutical

4. High target:nontarget ratio

•If this ratio is not high enough (5:1 minimum for planar
imaging, about 2:1 for SPECT imaging), a non-diagnostic
scan can result, making it difficult or impossible to
distinguish pathology from background
•very low target:nontarget ratio may be a non-diagnostic
scan, resulting in an unnecessary radiation dose, a delay
in the diagnosis and the necessity of repeating the
procedure
 Properties of a diagnostic radiopharmaceutical

5. Minimal radiation dose to patient and Nuclear Medicine

personnel
•compliance with ALARA guidelines
•the smallest dose possible should be injected,
consistent with good image quality
•dose should be scaled down based on the patient's
body mass in paediatrics
 Properties of a diagnostic radiopharmaceutical

6. Patient Safety
• No toxicity and wide margins of safety

7. Chemical Reactivity
•Ability to bind to a variety of
compounds under physiological
conditions
 Properties of a diagnostic radiopharmaceutical

8. Inexpensive, readily available

radiopharmaceutical
•stable both pre and post-reconstitution
Properties of a diagnostic radiopharmaceutical

9. Simple preparation and quality control if manufactured

in house
 Principal radionuclides used in diagnostic
radiopharmaceuticals

Technetium- 99mTc 6.01 h isomeric transition 141

99m
Iodine-123 123I 13.27 h electron capture 159
Indium-111 111In 67.31 h electron capture 171, 245
Gallium-67 67Ga 78.27 h electron capture 91, 93, 185,
209, 300
Thallium-201 201Tl 72.91 h electron capture 69-71 (X-rays),
80 (X-rays)
Krypton-81m 81mKr 13.1 s isomeric transition 190
Carbon-11 11C 20.38 min positron emission 511
(annihilation)
Nitrogen-13 13N 9.96 min positron emission 511
(annihilation)
Oxygen-15 15O 122.24 s positron emission 511
(annihilation)
Fluorine-18 18F 109.77 min positron emission 511
(annihilation)
Therapeutic
 Properties of a therapeutic radiopharmaceutical
1. Pure beta minus emitter
•Due to their high LET, beta particle emitters are quite
capable of destroying tissue
•far more controllable than alpha emitting radionuclides
from the standpoint of distribution in tissue
•beta emitters are easier to detect if spilled
 Properties of a therapeutic radiopharmaceutical

2. Medium/high energy (>1 meV).

•no exact minimum energy required, beta emitters with
Emax >1 MeV are preferred
•LET of these high energy particles is sufficient to
cause adequate but regulated tissue damage
•Some therapeutic isotopes, e.g., I-131, are imageable
and add to the information obtained during therapeutic
treatment
 Properties of a therapeutic radiopharmaceutical

3. Effective half-life
•moderately long, e.g., hours or days
•good examples of therapeutic radiopharmaceuticals
with an ideal teff include I-131 sodium iodide for
treatment of hyperthyroidism (teff is 6 days)
•Ho-166 FHMA for intraarticular radiation synovectomy
(teff is 1.2 days)
 Properties of a therapeutic radiopharmaceutical

4. High target:nontarget ratio.

•Target:non-target ratio is critical in therapeutic
procedures
•A low target:non-target ratio may result in inadequate
treatment of the primary disease and delivery of a
potentially lethal radiation dose to bone marrow or
other radiosensitive tissues
•It is especially important therefore to assure the
radiochemical purity of these drugs
 Properties of a therapeutic radiopharmaceutical
5. Minimal radiation dose to patient and Nuclear Medicine
personnel
•The usual rules of the TDS concept apply: one should
minimize TIME, maximize DISTANCE, and use the
appropriate amount of SHIELDING
•specific rules governing the release of patients from the
hospital after administration of a therapeutic
radiopharmaceutical to minimize risks to family and public
•Eg I-131 - The release criteria are set by the NRC and
state that the patient may be released when his radiation
burden becomes <30 mCi or when a reading taken 1 meter
from the patient's chest is <5 mR/hr, whichever level is
reached first
 Properties of a therapeutic radiopharmaceutical

6. Patient Safety
•No toxicity
•safe and provide wide margins of safety

7. Inexpensive, readily available

radiopharmaceutical.
•Inexpensive and readily available therapeutic
radiopharmaceuticals
•Many valuable procedures are being performed
infrequently or not at all because of the general
unavailability of the isotope or its great expense
 Properties of a therapeutic radiopharmaceutical

8. Simple preparation and quality control if manufactured

in house
•simple and require relatively little manipulation
•no complicated equipment or time consuming steps
•quality control be performed on every batch of drug
prepared
 Therapeutic
Radiopharmaceuticals

• For some medical conditions, it is useful to

destroy or weaken malfunctioning cells using
radiation.
• The radioisotope that generates the radiation
can be localized in the required organ in the
same way it is used for diagnosis - through a
radioactive element following its usual
biological path, or through the element being
attached to a suitable biological compound. In
most cases, it is beta radiation which causes
the destruction of the damaged cells. This is
radionuclide therapy (RNT) or radiotherapy.
 Therapeutic ;
RADIOTHERAPY

• External irradiation (sometimes

called teletherapy) can be carried
out using a gamma beam from a
radioactive cobalt-60 source, though
in developed countries the much
more versatile linear accelerators
are now being utilized as a high-
energy x-ray source (gamma and x-
rays are much the same)
 Radiotherapy ; Brachytherapy

• Rapidly
Radionuclide therapy
dividing cells are (RNT)
particularly sensitive to
damage by radiation. For this reason, some
cancerous growths can be controlled or
eliminated by irradiating the area containing the
growth.
• Internal radionuclide therapy is by
administering or planting a small radiation
source, usually a gamma or beta emitter, in the
target area. Short-range radiotherapy is known
as brachytherapy, and this is becoming the main
means of treatment.
• Irridium-192 for treatment of cervical cancer
 SOME Isotopes used in Medicine

• Many radioisotopes are made in nuclear reactors,

some in cyclotrons. Generally neutron-rich ones
and those resulting from nuclear fission need to be
made in reactors, neutron-depleted ones are made
in cyclotrons. There are about 40 activation product
radioisotopes and five fission product ones made in
reactors.
• Reactor Radioisotopes (half-life indicated)
• Bismuth-213 (46 min): Used for targeted alpha
therapy (TAT), especially cancers, as it has a high
energy (8.4 MeV).
• Chromium-51 (28 d): Used to label red blood cells
and quantify gastro-intestinal protein loss.
 Isotopes used in Medicine

• Cobalt-60 (5.27 yr): Formerly used for external

beam radiotherapy, now used more for sterilizing
• Erbium-169 (9.4 d): Use for relieving arthritis pain
in synovial joints.
• Holmium-166 (26 h): Being developed for
diagnosis and treatment of liver tumours.
• Iodine-125 (60 d): Used in cancer brachytherapy
(prostate and brain), also diagnostically to
evaluate the filtration rate of kidneys and to
diagnose deep vein thrombosis in the leg. It is
also widely used in radioimmuno-assays to show
the presence of hormones in tiny quantities.
 Isotopes used in Medicine

• Iodine-131 (8 d)*: Widely used in treating

thyroid cancer and in imaging the thyroid; also
in diagnosis of abnormal liver function, renal
(kidney) blood flow and urinary tract
obstruction. A strong gamma emitter, but used
for beta therapy.
• Iron-59 (46 d): Used in studies of iron
metabolism in the spleen.
• Potassium-42 (12 h): Used for the
determination of exchangeable potassium in
coronary blood flow.
 Isotopes used in Medicine

• Rhenium-186 (3.8 d): Used for pain relief in bone

cancer. Beta emitter with weak gamma for
imaging.
• Rhenium-188 (17 h): Used to beta irradiate
coronary arteries from an angioplasty balloon.
• Samarium-153 (47 h): Sm-153 is very effective in
relieving the pain of secondary cancers lodged in
the bone, sold as Quadramet. Also very effective
for prostate and breast cancer. Beta emitter.
• Technetium-99m (6 h): Used in to image the
skeleton and heart muscle in particular, but also for
brain, thyroid, lungs (perfusion and ventilation
 Isotopes used in Medicine

• Xenon-133 (5 d)*: Used for pulmonary (lung)

ventilation studies.
• Carbon-11, Nitrogen-13, Oxygen-15,
Fluorine-18: These are positron emitters used
in PET for studying brain physiology and
pathology, in particular for localising epileptic
focus, and in dementia, psychiatry and
neuropharmacology studies. They also have
a significant role in cardiology. F-18 in FDG
(fluorodeoxyglucose) has become very
important in detection of cancers and the
monitoring of progress in their treatment,
using PET.
 Isotopes used in Medicine

• Copper-64 (13 h): Used to study genetic

diseases affecting copper metabolism, such
as Wilson's and Menke's diseases, and for
PET imaging of tumours, and therapy.
• Indium-111 (2.8 d): Used for specialist
diagnostic studies, eg brain studies, infection
and colon transit studies.
• Iodine-123 (13 h): Increasingly used for
diagnosis of thyroid function, it is a gamma
emitter without the beta radiation of I-131.
 Isotopes used in Medicine

• Palladium-103 (17 d): Used to make

brachytherapy permanent implant seeds for
early stage prostate cancer.
• Phosphorus-32 (14 d): Used in the treatment
of polycythemia vera (excess red blood cells).
Beta emitter.
• Potassium-42 (12 h): Used for the
determination of exchangeable potassium in
coronary blood flow.
 mohdikhwan@usm.my
ikhwan_5120@yahoo.com
https://www.facebook.com/mohdikhwan.hashim
Presented by
Mohd Ikhwan bin Hashim RPh