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PREPARED BY
Mr. Shivkant Patel
Assistant Professor
Department of Pharmacy,
Sumandeep Vidyapeeth Deemed to be University, Vadodara
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
1
APPLICATIONS OF
RADIOPHARMACEUTICALS
B.PHARMACY 1ST SEMESTER
PHARMACEUTICAL INORGANIC
CHEMISTRY
NUCLEAR PHARMACY
 WHERE DO WE START?
 X Rays discovered in 1895
 Artificial radioactivity discovered in 1934
 First clinical use of radioactivity 1937
 Radioactive iodine used succesfully to treat
cancer 1946
 Widespread use of nuclear medicine 1950
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
2
RADIOPHARMACEUTICALS
Pharmaceuticals are the substances used to
diagnose, treat and prevent diseases.
Radiopharmaceuticals are the radioactive
pharmaceuticals used in nuclear medicine.
These drugs are made up of two
components-
A radioactive isotope and a carrier molecule.
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
3
APPLICATIONS
Radioisotopes are used in medicine in four
different ways
∆Diagnostic
∆Therapeutic
∆Research
∆Sterilization
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
4
DIAGNOSTIC RADIOPHARMACEUTICALS
 DEFINITION:
 Examples:
 Biliary tract blockage—Technetium Tc
 Bone diseases—Sodium Fluoride F 18,
Technetium Tc
 Heart disease—Ammonia N 13,
 Kidney diseases—Iodohippurate Sodium I 123,
 Red blood cell diseases—Sodium Chromate Cr
51
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
5
BRAIN SCAN
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
6
KIDNEY- SODIUM IODOHIPPURATE
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
7
BONE SCAN
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APPLICATIONS OF
RADIOPHARMACEUTICALS
8
THYROID GLAND SCAN
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
9
MRI SCAN
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
10
EXAMPLES:
Brain tumors diagnosis:using I 131
Diagnosis of helicobacter pylori: C14
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
11
RADIO IMMUNO ASSAY
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
12
THERAPEUTIC RADIOPHARMACEUTICALS
 DEFINITION: molecules used to deliver their
ionic radiations in therapeutic doses to the
diseased sites.
 AIM : Destroy diseased tissues without
destroying healthy tissues.
 Divisions of therapy:
∆External
∆Internal
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
13
EXTERNAL THERAPY
 α- radiations : poorly penetrating
 β-radiations : weakly penetrating . Used for
surface treatment of disorders. ex:eyes
 γ- radiations : highly penetrating . Used for deep
seated tumors.
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
14
INTERNAL THERAPY
Administration:
Example:
Chromic phosphate P 32 suspension:
Chromic phosphate suspended in 30%
dextrose solution is given in the form of
injection for the treatment of malignant
carcinoma of ovary.
I 131 is used to destroy thyroid cells in case of
thyrotoxicosis.
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
15
RESEARCH
 Used as tracers for studying biochemical
processes.
 Examples:C14, H 3, radio isotopes of
Na,Mg,Ca,Cu etc.
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
16
STERILISATION:
 Used to sterilise pharmaceuticals in their final
packed containers and surgical instruments
in hospitals.Thermolabile substances like
vitamins, hormones, antibiotics etc can be
safely sterilised.
 Example:Co 60, Cesium 137
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
17
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
18
RADIOPHARMACEUTICAL PREPARATIONS
Fludeoxyglucose (18F) injection:
Description: Fludeoxyglucose (18F) injection
(18F-FDG) is a colourless or slightly yellow
and sterile solution.
Radionuclide production: 18F is a
radioisotope of fluorine and may be
prepared by proton
irradiation of 18O deuteron irradiation of 20Ne or
alpha irradiation of 16O and processed in a
manner that 18F obtained is carrier free.
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
19
GRAPHIC FORMULA
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
20
Category: Diagnostic radiopharmaceutical
for liver diseases.
Chemical name. 2-[18F] fluoro-2-deoxy-D-
glucopyranose (2-[18F] fluoro-2- deoxy –
Dglucose
The radioactive half life of 18F is 109.8 minutes
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
21
SODIUM IODIDE (131 I ) CAPSULES
 Description. White or coloured gelatine
capsule contained in a sealed secondary
container
The radioactive half-life of
131I is 8.06 days.
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
22
production: Complies with 131I production and
general conditions in radiopharmaceutical
preparation. Iodine-131 may be obtained by neutron
irradiation of tellurium or by extraction from uranium
fission products.
Radiopharmaceutical formulation: The content of 131I
is not less than 90.0% and not more than 110.0% of
the stated content on the label at the reference date
and hour. The method of manufacture is such that the
specific activity used is not less than 185MBq of iodine-
131 per mg of iodine for diagnostic capsules and
185MBq of iodine-131 per microgram of iodine for
therapeutic capsules.
Category: Diagnostic and therapeutic
radiopharmaceutical
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
23
TC 99 GENERATOR
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
24
SODIUM PHOSPHATE (32P ) INJECTION
Description: A clear, colourless sterile solution
containing radioactive disodium and
monosodium (32P) orthophosphate made
isotonic to blood with sodium chloride.
Radionuclide production: 32P is radioactive
isotope of phosphorous and may be
produced by neutron irradiation of sulfur. The
radioactive half-life of 32P is 14.3 days
Category: Therapeutic radiopharmaceutical.
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
25
PHAMACOPOEIAL PRERERATIONS:
 Fludeoxyglucose (18F) injection.
 Gallium Citrate (67Ga) injection
 Sodium Phosphate (32P) injection
 Strontium Chloride (89Sr) injection
 Technetium (99mTc) labelled Red Blood
Cells injection
 Technetium (99mTc) Sulphur Colloid injection
5/2/2022
APPLICATIONS OF
RADIOPHARMACEUTICALS
26
THANKS

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Applications of Radiopharmaceuticals

  • 1. PREPARED BY Mr. Shivkant Patel Assistant Professor Department of Pharmacy, Sumandeep Vidyapeeth Deemed to be University, Vadodara 5/2/2022 APPLICATIONS OF RADIOPHARMACEUTICALS 1 APPLICATIONS OF RADIOPHARMACEUTICALS B.PHARMACY 1ST SEMESTER PHARMACEUTICAL INORGANIC CHEMISTRY
  • 2. NUCLEAR PHARMACY  WHERE DO WE START?  X Rays discovered in 1895  Artificial radioactivity discovered in 1934  First clinical use of radioactivity 1937  Radioactive iodine used succesfully to treat cancer 1946  Widespread use of nuclear medicine 1950 5/2/2022 APPLICATIONS OF RADIOPHARMACEUTICALS 2
  • 3. RADIOPHARMACEUTICALS Pharmaceuticals are the substances used to diagnose, treat and prevent diseases. Radiopharmaceuticals are the radioactive pharmaceuticals used in nuclear medicine. These drugs are made up of two components- A radioactive isotope and a carrier molecule. 5/2/2022 APPLICATIONS OF RADIOPHARMACEUTICALS 3
  • 4. APPLICATIONS Radioisotopes are used in medicine in four different ways ∆Diagnostic ∆Therapeutic ∆Research ∆Sterilization 5/2/2022 APPLICATIONS OF RADIOPHARMACEUTICALS 4
  • 5. DIAGNOSTIC RADIOPHARMACEUTICALS  DEFINITION:  Examples:  Biliary tract blockage—Technetium Tc  Bone diseases—Sodium Fluoride F 18, Technetium Tc  Heart disease—Ammonia N 13,  Kidney diseases—Iodohippurate Sodium I 123,  Red blood cell diseases—Sodium Chromate Cr 51 5/2/2022 APPLICATIONS OF RADIOPHARMACEUTICALS 5
  • 9. THYROID GLAND SCAN 5/2/2022 APPLICATIONS OF RADIOPHARMACEUTICALS 9
  • 11. EXAMPLES: Brain tumors diagnosis:using I 131 Diagnosis of helicobacter pylori: C14 5/2/2022 APPLICATIONS OF RADIOPHARMACEUTICALS 11
  • 12. RADIO IMMUNO ASSAY 5/2/2022 APPLICATIONS OF RADIOPHARMACEUTICALS 12
  • 13. THERAPEUTIC RADIOPHARMACEUTICALS  DEFINITION: molecules used to deliver their ionic radiations in therapeutic doses to the diseased sites.  AIM : Destroy diseased tissues without destroying healthy tissues.  Divisions of therapy: ∆External ∆Internal 5/2/2022 APPLICATIONS OF RADIOPHARMACEUTICALS 13
  • 14. EXTERNAL THERAPY  α- radiations : poorly penetrating  β-radiations : weakly penetrating . Used for surface treatment of disorders. ex:eyes  γ- radiations : highly penetrating . Used for deep seated tumors. 5/2/2022 APPLICATIONS OF RADIOPHARMACEUTICALS 14
  • 15. INTERNAL THERAPY Administration: Example: Chromic phosphate P 32 suspension: Chromic phosphate suspended in 30% dextrose solution is given in the form of injection for the treatment of malignant carcinoma of ovary. I 131 is used to destroy thyroid cells in case of thyrotoxicosis. 5/2/2022 APPLICATIONS OF RADIOPHARMACEUTICALS 15
  • 16. RESEARCH  Used as tracers for studying biochemical processes.  Examples:C14, H 3, radio isotopes of Na,Mg,Ca,Cu etc. 5/2/2022 APPLICATIONS OF RADIOPHARMACEUTICALS 16
  • 17. STERILISATION:  Used to sterilise pharmaceuticals in their final packed containers and surgical instruments in hospitals.Thermolabile substances like vitamins, hormones, antibiotics etc can be safely sterilised.  Example:Co 60, Cesium 137 5/2/2022 APPLICATIONS OF RADIOPHARMACEUTICALS 17
  • 19. RADIOPHARMACEUTICAL PREPARATIONS Fludeoxyglucose (18F) injection: Description: Fludeoxyglucose (18F) injection (18F-FDG) is a colourless or slightly yellow and sterile solution. Radionuclide production: 18F is a radioisotope of fluorine and may be prepared by proton irradiation of 18O deuteron irradiation of 20Ne or alpha irradiation of 16O and processed in a manner that 18F obtained is carrier free. 5/2/2022 APPLICATIONS OF RADIOPHARMACEUTICALS 19
  • 21. Category: Diagnostic radiopharmaceutical for liver diseases. Chemical name. 2-[18F] fluoro-2-deoxy-D- glucopyranose (2-[18F] fluoro-2- deoxy – Dglucose The radioactive half life of 18F is 109.8 minutes 5/2/2022 APPLICATIONS OF RADIOPHARMACEUTICALS 21
  • 22. SODIUM IODIDE (131 I ) CAPSULES  Description. White or coloured gelatine capsule contained in a sealed secondary container The radioactive half-life of 131I is 8.06 days. 5/2/2022 APPLICATIONS OF RADIOPHARMACEUTICALS 22
  • 23. production: Complies with 131I production and general conditions in radiopharmaceutical preparation. Iodine-131 may be obtained by neutron irradiation of tellurium or by extraction from uranium fission products. Radiopharmaceutical formulation: The content of 131I is not less than 90.0% and not more than 110.0% of the stated content on the label at the reference date and hour. The method of manufacture is such that the specific activity used is not less than 185MBq of iodine- 131 per mg of iodine for diagnostic capsules and 185MBq of iodine-131 per microgram of iodine for therapeutic capsules. Category: Diagnostic and therapeutic radiopharmaceutical 5/2/2022 APPLICATIONS OF RADIOPHARMACEUTICALS 23
  • 24. TC 99 GENERATOR 5/2/2022 APPLICATIONS OF RADIOPHARMACEUTICALS 24
  • 25. SODIUM PHOSPHATE (32P ) INJECTION Description: A clear, colourless sterile solution containing radioactive disodium and monosodium (32P) orthophosphate made isotonic to blood with sodium chloride. Radionuclide production: 32P is radioactive isotope of phosphorous and may be produced by neutron irradiation of sulfur. The radioactive half-life of 32P is 14.3 days Category: Therapeutic radiopharmaceutical. 5/2/2022 APPLICATIONS OF RADIOPHARMACEUTICALS 25
  • 26. PHAMACOPOEIAL PRERERATIONS:  Fludeoxyglucose (18F) injection.  Gallium Citrate (67Ga) injection  Sodium Phosphate (32P) injection  Strontium Chloride (89Sr) injection  Technetium (99mTc) labelled Red Blood Cells injection  Technetium (99mTc) Sulphur Colloid injection 5/2/2022 APPLICATIONS OF RADIOPHARMACEUTICALS 26