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Radiopharmaceuticals
Mrs. Dipali Kulkarni
Assistant Professor,
Yash Institute of Pharmacy,
Aurangabad.
Measurement of radioactivity,
study of radio isotopes –
Sodium iodide 131,
Storage conditions,
precautions &
Pharmaceutical application of radioactive substance .
Radiopharmaceuticals are used in various branches
like,
1) Diagnostic applications (Radioactive tracers)
2) Radiotherapy (Radioisotopes in Therapy)
3) Sterilization(Pharmaceuticals and surgical instruments)
4) Research. (Biological and medicinal studies by use of
radioactive isotopes as tracers)
5) Analytical Applications.
Applications of radiopharmaceuticals in pharmacy:
1. Phosphorus 32: Used for diagnosis of cancer.
2. Chromium51: Used for diagnosis of red cell survival &
volume.
it is also Used to estimate GI blood losses through stool or
urine.
3. Co 57, 58 used measurement of absorption of vit. B12
Diagnosis of Pernicious anemia.
4.Iodine131:Determination of Thyroid function
.
Diagnostic applications
 Radioactive tracers find use in medicine for diagnostic
purposes.
1. Labelled cyanocobalamine finds use for measuring the
glomerular filtration rate.
2. Ferric citrate injection finds use for the diagnosis of
haematological disorders.
3. Colloidal gold injection is used diagnostically to study blood
circulation in liver.
4. Sodium iodide injection finds use in diagnosis of proper
functioning of thyroid gland.
5. Sodium iodohippurate injection finds use in the study of
renal function.
6. Sodium rose Bengal injection finds use as diagnostic agent
to test liver function.
 The therapeutically used radioisotopes have been found to
depend mainly on their ability to ionize atoms.
 The energy measurement involved in radiation and resulting in
ionization may be expressed in millions of electron volts called
MeV.
 The strength of alpha, beta and gamma rays in expressed in MeV.
 All radiations bring about ionization of atoms in their paths.
 The radiation of short wavelength (gamma rays) is having high
penetrating power than long wavelength (beta rays).
 The greater the MeV of the rays, the more destructive it
becomes to the surrounding tissues.
 RADIOPHARMACEUTICALS CAN DESTROY MALFUNCTIONING
CELLS.
 This method of therapy is called radiotherapy. It can be used for
both benign and malignant cancers.
Radiotherapy
Some radioisotope are have ability to destroy
the disease without destroying healthy tissues.
a)Iodine 131: Used in the treatment of
hyperthyroidism
b) Used in the treatment of thyroid cancer.
C)Cobalt 60: Used in treatment of cancer involving cervix,
vagina, uterus, bladder, mouth, tongue and lips.
d)Phosphorus 32: Used in treatment of various types of
cancer in polycythaemia (erythrocytosis) & Leukemia.
Radiotherapy
Examples:
 Gold (198 Au) treatment of abdominal and pleural effusions associated with
malignant tumours. It is given in the form of colloidal gold suspension.
 Gold (198 Au) treatment of carcinoma of uterus and urinary bladder.
 Cobalt labelled cyanocobalamine (vitamin B12) is used in diagnosis of
pernicious anaemia.
 Sodium iodide preparation finds use in treatment of thyroid disorders.
 Calcium is used to study bone structure and in carcinoma of bone.
 Strontium 90 is used in diagnosis of superficial carcinomas.
 Radioisotopes may be used internally or externally.
 If the radioisotope are used externally or used as implants in sealed capsule in a
tissue, the dose could be terminated by removal or sources.
 If they are given internally, as unsealed sources, the dose cannot be stopped by
the removal of the source.
 The total dose in therapeutic applications may be calculated on the basis of
effective half life of the isotope, concentration of the isotope and the type and
energy of the radiation emitted.
Used for sterilization of Pharmaceuticals in their final
packed containers, thermolabile drugs
Hormones, Vitamins, Antibiotics, Surgical dressings,
Disposable syringes.
No heat or chemical gets involved.
Examples: Cobalt 60: Used for the sterilization of
disposable syringes, catheters and surgical dressings
and surgical instruments in hospitals.
Sterilization
Used in biochemical reactions,
may be used for detection of mechanism of
reactions.
Ex: Iodine 131,
Sodium 24,
Phosphorus 32.
5)Analytical: Plays major role when dealing with
dilute solutions.
Research
Calcium (Ca-44 and Ca-45) radioactive calcium used to study bone structure
and in treatment of carcinoma of bone.
Strontium -90 Used in the radiotherapy of superficial carcinomas.
Cyanocobalamine (Co-57) Used in the diagnosis of pernicious anaemia.
Calcium -47 It is having half life of 4.7 days. It is used in
calcium absorption studies.
Cyanocobalamine
(Co-60 Solution
USP)
Used to study absorption and deposition of
vitamin B12 in normal individuals.
Gold (Au-198) solution Finds use in estimation of reticuloendothelial
activity.
Iron (Fe-59) Finds use in research studies about utilization
and absorption of Iron salts.
Labeling ,handling and storage of
radiopharmaceuticals
Name of Radioisotope.
Ex.I131
Strength in Microcurie or Milicurie per mililitre
at given time and date RADIOACTIVE..Indicates
Warning.
Name And Percentage of any bactericide added.
if not the statement must be there that the
product (INJECTION) does not contain any
bactericide.
Expiry date and name of manufacturer.
Radioactive Materials
Must Never Be Touch
With Hand But
Smoking ,Eating & drinking
Activities Should Not Be
Carried Out In The
Laboratory
Protective Clothing Or
Shielding Must Be Used
While Handling The
Radioactive Material
Handled By Means Of
Forceps Or Suitable
Instruments.
Radioactive Materials
Should Be Kept In
Suitable Labeled
Containers Shielded
By Lead Bricks And
Preferably In
Remote Area.
Storage
Used as a diagnostic aid for studying the functioning of the
thyroid gland.
Used in scanning the thyroid for determining the size, position
and possible tumour location.
Used in the treatment of severe cardiac disease (Sodium
iodide I-131), which reduces work load on heart.
Radioactive iodine in thyroid carcinoma (cancer): The
isotope is used most frequently after the surgical removal
of cancer to treat any residual tumour tissues.
Uses of Sodium iodide I-131
 Iron 59 is a beta and gamma emitting isotope.
 Used in diagnosis to study the iron metabolism and to study
the red blood cell formation.
 The preparation is administered orally for studying the
absorption of iron from GIT.
 Administered I.V to study incorporation of iron in
formation of red blood cells.
 Used to study the formation and destruction of spleen, liver
etc. from outside the body.
Iron59
Def: These are chemical compounds which have
ability to absorb X rays and block the passage
it through tissues.
➢Used for describing the body structures of the
particular part in the form of image.
➢X rays are capable of passing through most
soft tissues, but bones, cartilages and teeth's
are capable of blocking the passage of X rays.
Xrays are electromagnetic radiations and
interact with electrostatic field of electrons of
an atom.
Radiopaque (Contrast Media):
Radiopaques are administered like Barium sulphate
and Iodine for diagnosis of diseases in soft tissues
which shows image of that organ.
They do Not have Pharmacodynamic effect in the
body.
Chem. Form.: BaSO4 Mol. Wt.: 233.39
Synonyms: Barii sulfas, Barium meal.
Properties:
➢It is fine, heavy, white, odourless, tasteless, bulky powder,
free from gritty particles.
➢Practically insoluble in water & organic solvents.
➢Very slightly soluble in acids, alkalies & many salt
solutions.
➢Soluble in conc. Sulphuric acid with the
formation of bisulphate salt.
BaSO4+ H2SO4 Ba(HSO4)2
Barium sulphate
➢Used as a radiopaque CONTRAST MEDIA for the X Ray
examination of various organs.
➢It is administered in the form of suspension. It is insoluble
salt is not absorbed.
➢Roentgenographic or Fluoroscopic.
➢in the diagnosis of structural and motility of Interior part
of the alimentary canal, from the mouth to the
duodenum .
Precautions:
▪ Barium sulphate may be used
cautiously in elderly patients.
▪ Once absorbed in blood can produced
Cardiac arrest.
Storage: Store in well closed containers.
Dosage forms:
• Suspension:
• Single dose powder.
•Single disposable, prefilled cups as enema kit.
Dose: 1) 60-450 gm (Oral). 2)150-750gm (Rectal).
Radiopharmaceuticals

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Radiopharmaceuticals

  • 1. Radiopharmaceuticals Mrs. Dipali Kulkarni Assistant Professor, Yash Institute of Pharmacy, Aurangabad.
  • 2. Measurement of radioactivity, study of radio isotopes – Sodium iodide 131, Storage conditions, precautions & Pharmaceutical application of radioactive substance .
  • 3. Radiopharmaceuticals are used in various branches like, 1) Diagnostic applications (Radioactive tracers) 2) Radiotherapy (Radioisotopes in Therapy) 3) Sterilization(Pharmaceuticals and surgical instruments) 4) Research. (Biological and medicinal studies by use of radioactive isotopes as tracers) 5) Analytical Applications. Applications of radiopharmaceuticals in pharmacy:
  • 4. 1. Phosphorus 32: Used for diagnosis of cancer. 2. Chromium51: Used for diagnosis of red cell survival & volume. it is also Used to estimate GI blood losses through stool or urine. 3. Co 57, 58 used measurement of absorption of vit. B12 Diagnosis of Pernicious anemia. 4.Iodine131:Determination of Thyroid function . Diagnostic applications
  • 5.  Radioactive tracers find use in medicine for diagnostic purposes. 1. Labelled cyanocobalamine finds use for measuring the glomerular filtration rate. 2. Ferric citrate injection finds use for the diagnosis of haematological disorders. 3. Colloidal gold injection is used diagnostically to study blood circulation in liver. 4. Sodium iodide injection finds use in diagnosis of proper functioning of thyroid gland. 5. Sodium iodohippurate injection finds use in the study of renal function. 6. Sodium rose Bengal injection finds use as diagnostic agent to test liver function.
  • 6.  The therapeutically used radioisotopes have been found to depend mainly on their ability to ionize atoms.  The energy measurement involved in radiation and resulting in ionization may be expressed in millions of electron volts called MeV.  The strength of alpha, beta and gamma rays in expressed in MeV.  All radiations bring about ionization of atoms in their paths.  The radiation of short wavelength (gamma rays) is having high penetrating power than long wavelength (beta rays).  The greater the MeV of the rays, the more destructive it becomes to the surrounding tissues.  RADIOPHARMACEUTICALS CAN DESTROY MALFUNCTIONING CELLS.  This method of therapy is called radiotherapy. It can be used for both benign and malignant cancers. Radiotherapy
  • 7. Some radioisotope are have ability to destroy the disease without destroying healthy tissues. a)Iodine 131: Used in the treatment of hyperthyroidism b) Used in the treatment of thyroid cancer. C)Cobalt 60: Used in treatment of cancer involving cervix, vagina, uterus, bladder, mouth, tongue and lips. d)Phosphorus 32: Used in treatment of various types of cancer in polycythaemia (erythrocytosis) & Leukemia. Radiotherapy
  • 8. Examples:  Gold (198 Au) treatment of abdominal and pleural effusions associated with malignant tumours. It is given in the form of colloidal gold suspension.  Gold (198 Au) treatment of carcinoma of uterus and urinary bladder.  Cobalt labelled cyanocobalamine (vitamin B12) is used in diagnosis of pernicious anaemia.  Sodium iodide preparation finds use in treatment of thyroid disorders.  Calcium is used to study bone structure and in carcinoma of bone.  Strontium 90 is used in diagnosis of superficial carcinomas.  Radioisotopes may be used internally or externally.  If the radioisotope are used externally or used as implants in sealed capsule in a tissue, the dose could be terminated by removal or sources.  If they are given internally, as unsealed sources, the dose cannot be stopped by the removal of the source.  The total dose in therapeutic applications may be calculated on the basis of effective half life of the isotope, concentration of the isotope and the type and energy of the radiation emitted.
  • 9. Used for sterilization of Pharmaceuticals in their final packed containers, thermolabile drugs Hormones, Vitamins, Antibiotics, Surgical dressings, Disposable syringes. No heat or chemical gets involved. Examples: Cobalt 60: Used for the sterilization of disposable syringes, catheters and surgical dressings and surgical instruments in hospitals. Sterilization
  • 10. Used in biochemical reactions, may be used for detection of mechanism of reactions. Ex: Iodine 131, Sodium 24, Phosphorus 32. 5)Analytical: Plays major role when dealing with dilute solutions. Research
  • 11.
  • 12. Calcium (Ca-44 and Ca-45) radioactive calcium used to study bone structure and in treatment of carcinoma of bone. Strontium -90 Used in the radiotherapy of superficial carcinomas. Cyanocobalamine (Co-57) Used in the diagnosis of pernicious anaemia. Calcium -47 It is having half life of 4.7 days. It is used in calcium absorption studies. Cyanocobalamine (Co-60 Solution USP) Used to study absorption and deposition of vitamin B12 in normal individuals. Gold (Au-198) solution Finds use in estimation of reticuloendothelial activity. Iron (Fe-59) Finds use in research studies about utilization and absorption of Iron salts.
  • 13. Labeling ,handling and storage of radiopharmaceuticals Name of Radioisotope. Ex.I131 Strength in Microcurie or Milicurie per mililitre at given time and date RADIOACTIVE..Indicates Warning. Name And Percentage of any bactericide added. if not the statement must be there that the product (INJECTION) does not contain any bactericide. Expiry date and name of manufacturer.
  • 14. Radioactive Materials Must Never Be Touch With Hand But Smoking ,Eating & drinking Activities Should Not Be Carried Out In The Laboratory Protective Clothing Or Shielding Must Be Used While Handling The Radioactive Material Handled By Means Of Forceps Or Suitable Instruments.
  • 15. Radioactive Materials Should Be Kept In Suitable Labeled Containers Shielded By Lead Bricks And Preferably In Remote Area. Storage
  • 16.
  • 17. Used as a diagnostic aid for studying the functioning of the thyroid gland. Used in scanning the thyroid for determining the size, position and possible tumour location. Used in the treatment of severe cardiac disease (Sodium iodide I-131), which reduces work load on heart. Radioactive iodine in thyroid carcinoma (cancer): The isotope is used most frequently after the surgical removal of cancer to treat any residual tumour tissues. Uses of Sodium iodide I-131
  • 18.  Iron 59 is a beta and gamma emitting isotope.  Used in diagnosis to study the iron metabolism and to study the red blood cell formation.  The preparation is administered orally for studying the absorption of iron from GIT.  Administered I.V to study incorporation of iron in formation of red blood cells.  Used to study the formation and destruction of spleen, liver etc. from outside the body. Iron59
  • 19. Def: These are chemical compounds which have ability to absorb X rays and block the passage it through tissues. ➢Used for describing the body structures of the particular part in the form of image. ➢X rays are capable of passing through most soft tissues, but bones, cartilages and teeth's are capable of blocking the passage of X rays. Xrays are electromagnetic radiations and interact with electrostatic field of electrons of an atom. Radiopaque (Contrast Media):
  • 20. Radiopaques are administered like Barium sulphate and Iodine for diagnosis of diseases in soft tissues which shows image of that organ. They do Not have Pharmacodynamic effect in the body.
  • 21. Chem. Form.: BaSO4 Mol. Wt.: 233.39 Synonyms: Barii sulfas, Barium meal. Properties: ➢It is fine, heavy, white, odourless, tasteless, bulky powder, free from gritty particles. ➢Practically insoluble in water & organic solvents. ➢Very slightly soluble in acids, alkalies & many salt solutions. ➢Soluble in conc. Sulphuric acid with the formation of bisulphate salt. BaSO4+ H2SO4 Ba(HSO4)2 Barium sulphate
  • 22. ➢Used as a radiopaque CONTRAST MEDIA for the X Ray examination of various organs. ➢It is administered in the form of suspension. It is insoluble salt is not absorbed. ➢Roentgenographic or Fluoroscopic. ➢in the diagnosis of structural and motility of Interior part of the alimentary canal, from the mouth to the duodenum .
  • 23. Precautions: ▪ Barium sulphate may be used cautiously in elderly patients. ▪ Once absorbed in blood can produced Cardiac arrest. Storage: Store in well closed containers. Dosage forms: • Suspension: • Single dose powder. •Single disposable, prefilled cups as enema kit. Dose: 1) 60-450 gm (Oral). 2)150-750gm (Rectal).