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Chapter 18

RADIOPHARMACEUTICALS

Asst. Prof. MA. LOURDES LICSI – MOJARES, R. Ph.
                     Faculty
              CEU School of Pharmacy
RADIOPHARMACEUTICALS
   Used for diagnostic
    or therapeutic
    procedures

   Frequently prepared
    as parenteral
    dosage form
RADIOPHARMACEUTICALS:
composition

   DRUG COMPONENT

   RADIAOCTIVE
    COMPONENT
     Mostly “radionuclides” that emit
    gamma radiation.
DRUG                                 PRIMARY USES
111
   In capromab pendetide             Monoclonal antibody f or imaging prostate cancer
(ProstaScint)

  I, sodium iodide and 131I,
123
                                     Thyroid imaging and uptake
sodium iodide
99m
      T pertechnetate
       c                             Imaging of thyroid, salivary glands, ectopic
                                     gastric mucosa, parathyroid glands,
                                     dacryocystography, cystography
99m
      T red blood cells (Ultratag)
       c                             Imaging of GI bleeding, cardiac chambers,
                                     cardiac f irst- pass
99m
      T sulfur colloid
       c                             Imaging of reticuloendothelial system, bone
                                     marrow, gastric emptying, GI bleeding,
                                     lymphoscintigraphy, arthrograms
133
     Xe                              Pulmonary ventilation imaging
 Y microspheres (T
90
                  heraSphere)        Therapy f or biopsy- proven, unresectable
                                     hepatocellular carcinoma
166
     Ho-DOT P and 186Re-H DP
           M             E           Bone cancer therapy
Positron Emission Tomograpy
  (PET) Radiopharmaceuticals
   - Used for imaging procedures
PET Pharmaceuticals include :
1. Carbon-11
  As a tracer, used to study myocardial
   metabolism
  11
      C glucose is use for cerebral glucose
   metabolism
2. Nitrogen-13
  Used as tracer for cerebral and
   myocardial blood flow
PET Radiopharmaceuticals
3.  Oxygen-15
Four 15 O are available for clinical use:
     15
         OO (oxygen gas) - used in the study of oxygen
    metabolism
   C 15 O (carbon monoxide) – administered via
    inhalation; serves as tracer for RBC volume
   CO 15 O (carbon dioxide)
   H 2 15 O (water) – commonly used as tracer of cerebral
    and myocardial perfusion
   Flourine-18
   For cerebral glucose metabolism, myocardial
    glucose metabolism and tumor glucose metabolism
   Gallium-68
   Binds with transferrin forming 68 Ga-transferrin
   68
       Ga-transferrin is employed in pulmonary studies
    of vascular permeability
Drug antidote for
  radiation exposure
PRUSSIAN BLUE

      Ferric
  hexacyanoferrate

 Radiogardase capsule

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Ch. 18 radiopharmaceuticals

  • 1. Chapter 18 RADIOPHARMACEUTICALS Asst. Prof. MA. LOURDES LICSI – MOJARES, R. Ph. Faculty CEU School of Pharmacy
  • 2. RADIOPHARMACEUTICALS  Used for diagnostic or therapeutic procedures  Frequently prepared as parenteral dosage form
  • 3. RADIOPHARMACEUTICALS: composition  DRUG COMPONENT  RADIAOCTIVE COMPONENT Mostly “radionuclides” that emit gamma radiation.
  • 4. DRUG PRIMARY USES 111 In capromab pendetide Monoclonal antibody f or imaging prostate cancer (ProstaScint) I, sodium iodide and 131I, 123 Thyroid imaging and uptake sodium iodide 99m T pertechnetate c Imaging of thyroid, salivary glands, ectopic gastric mucosa, parathyroid glands, dacryocystography, cystography 99m T red blood cells (Ultratag) c Imaging of GI bleeding, cardiac chambers, cardiac f irst- pass 99m T sulfur colloid c Imaging of reticuloendothelial system, bone marrow, gastric emptying, GI bleeding, lymphoscintigraphy, arthrograms 133 Xe Pulmonary ventilation imaging Y microspheres (T 90 heraSphere) Therapy f or biopsy- proven, unresectable hepatocellular carcinoma 166 Ho-DOT P and 186Re-H DP M E Bone cancer therapy
  • 5. Positron Emission Tomograpy (PET) Radiopharmaceuticals - Used for imaging procedures PET Pharmaceuticals include : 1. Carbon-11  As a tracer, used to study myocardial metabolism  11 C glucose is use for cerebral glucose metabolism 2. Nitrogen-13  Used as tracer for cerebral and myocardial blood flow
  • 6. PET Radiopharmaceuticals 3. Oxygen-15 Four 15 O are available for clinical use:  15 OO (oxygen gas) - used in the study of oxygen metabolism  C 15 O (carbon monoxide) – administered via inhalation; serves as tracer for RBC volume  CO 15 O (carbon dioxide)  H 2 15 O (water) – commonly used as tracer of cerebral and myocardial perfusion  Flourine-18  For cerebral glucose metabolism, myocardial glucose metabolism and tumor glucose metabolism  Gallium-68  Binds with transferrin forming 68 Ga-transferrin  68 Ga-transferrin is employed in pulmonary studies of vascular permeability
  • 7. Drug antidote for radiation exposure PRUSSIAN BLUE Ferric hexacyanoferrate Radiogardase capsule