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Biodistribution of Radiopharmaceuticals

Biodistribution of Radiopharmaceuticals. Jim Corley, RPh, MS, BCNP Medical College of Georgia. Biodistribution of Radiopharmaceuticals. Properties of a Radioactive Element That Determine Tissue Localization and Excretion. Determinants of Localization of Radioactive Drugs

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Biodistribution of Radiopharmaceuticals

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  1. Biodistribution of Radiopharmaceuticals Jim Corley, RPh, MS, BCNP Medical College of Georgia

  2. Biodistribution of Radiopharmaceuticals • Properties of a Radioactive Element That Determine Tissue Localization and Excretion. • Determinants of Localization of Radioactive Drugs • Determinants of Renal Excretion

  3. Properties of a Radioactive Element That Determine Tissue Localization and Excretion

  4. Chief Determinants of Biological Localization • Oxidation state at physiologic pH • Solubility of the stable state • Tendency toward incorporation into organic compounds • Tendency to be chelated or to form protein complexes in circulation or in a particular tissue

  5. _ _ + + I- 2.15 Å TcO4- 1.99 Å ClO4- 1.74 Å K+ 1.33 Å Tl+ 1.40 Å Oxidation State, Ionic Size and Charge _

  6. Group I: THE ALKALI METALS

  7. Element Na K Rb Cs Subgroup I Cu Ag Au Principle Location Muscle Muscle Muscle Muscle Liver Protein Liver Group I: THE ALKALI METALS • Principle Excretion • Urine • Urine • Urine • Urine • Urine • Feces • Urine

  8. Group II: Alkaline Earths

  9. Element Be Mg Ca Sr Ba Ra Subgroup II Zn Cd Hg Principle Location Bone Bone Bone Bone Bone Liver Liver Kidney Group II: THE ALKALINE EARTHS • Principle Excretion • Urine • - • Feces • Urine & Feces • Urine & Feces • Urine & Feces • - • Feces • Feces Pediatric Nuclear Medicine 1974

  10. Group III: Lanthanides & Actinides

  11. Element B Al Ga In Tl Subgroup III Sc Y La Principle Location No radioisotopes available No radioisotopes available Bone, muscle Bone, liver Muscle Bone, liver Bone Liver Group III: THE LANTHANIDES & ACTINIDES • Principle Excretion • - • - • Feces • Feces • Feces • Feces • Urine • Urine & feces

  12. Rare Earths

  13. Element Ce Pr Nd Pm Sm Eu Gd Tb Dy Ho Er Tm Yb Lu Principle Location Liver, bone Liver, bone Liver, bone Liver, bone Liver, bone Liver, bone Bone, liver Bone Bone Bone Bone Bone Bone Bone RARE EARTHS • Principle Excretion • Feces & Urine • Feces & Urine • Feces & Urine • Feces & Urine • Feces & Urine • Feces & Urine • Urine • Urine • Urine • Urine • Urine • Urine • Urine • Urine

  14. Group IV

  15. Element C Si Ge Sn Pb Subgroup IV Ti Zr Hf Principle Location - - Bone, liver Bone Bone - Bone Liver, bone Group IV • Principle Excretion • - • - • Urine • Urine • Urine & Feces • - • Feces • Feces & Urine Pediatric Nuclear Medicine 1974

  16. Group V

  17. Element N P As Sb Bi Subgroup V V Nb Ta Principle Location - Muscle, bone Blood Blood Bi Liver, kidney, bone Liver, kidney, bone Liver, kidney, bone Group V • Principle Excretion • - • Urine • Urine • Urine • Urine • Urine & Feces • Urine & Feces • Urine Pediatric Nuclear Medicine 1974

  18. Group VI

  19. Element O S Se Te Po Subgroup VI Cr Mo W Principle Location - - Blood Blood Blood, liver, kidney Bone, blood Liver Bone Group VI Principle Excretion - - Urine Urine - Urine Urine Urine Pediatric Nuclear Medicine 1974

  20. Group VII: Halogens

  21. Element F Cl Br I At Subgroup VII Mn Tc Re Principle Location Bone - Liver, GI tract Thyroid GI tract Liver GI tract GI tract Group VII: THE HALOGENS Principle Excretion Urine - Urine Urine Urine Feces Urine Urine Pediatric Nuclear Medicine 1974

  22. Group VIII: Platinum Metals

  23. Element Fe Ru Os Co Rh Ir Ni Pd Pt Principle Location Blood, liver Muscle General Liver Muscle Liver - Liver, kidney Liver,muscle,kidney Group VIII: THE PLATINUM METALS Principle Excretion Feces Urine Urine Urine Urine Urine - Urine Urine & Feces Pediatric Nuclear Medicine 1974

  24. Useful Positron Isotopes C-11 N-13 O-15 F-18 Ga-68 Rb-81

  25. Biodistribution of Radiopharmaceuticals • Properties of a Radioactive Element That Determine Tissue Localization and Excretion • Determinants of Localization of Radioactive Drugs • Determinants of Renal Excretion

  26. Biodistribution of Radiopharmaceuticals Determinants of Localization of Radioactive Drugs A. Organ characteristics B. Drug characteristics

  27. Biodistribution of Radiopharmaceuticals Determinants of Localization of Radioactive Drugs A. Organ characteristics  Relative Blood Flow to the organ  Types of capillaries in the organ  Capillary "density" or number per unit volume of tissue  Specific drug-receptor sites

  28. Biodistribution of Radiopharmaceuticals Determinants of Localization of Radioactive Drugs B. Drug characteristics  Molecular size and shape  Degree and strength of binding to plasma proteins  Lipid solubility  Specific drug receptor and transport mechanisms

  29. Chemical Structures Influencing Lipid Solubility

  30. Mechanisms of Localization • Active Transport • Phagocytosis • Cell Sequestration • Capillary Blockade • Simple or Exchange Diffusion • Compartmental Localization • Metabolic Substitution Pediatric Nuclear Medicine 1974

  31. Mechanisms of Localization Active Transport Thyroid scanning with iodide or pertechnetate Renal scanning with Iodohippurate Liver scanning with HIDA Pancreatic scanning with Selenomethionine Pediatric Nuclear Medicine 1974

  32. Active Transport - Thyroid scanning with iodide or pertechnetate • 43 year old female • Exophthalmus • Agitated • elevated free T4 • undetectable TSH • Tc-99m pertechnetate scan • RAIU 66% • Treatment 7.3mCi NaI-131

  33. Active Transport - Liver scanning with HIDA

  34. Mechanisms of Localization Phagocytosis Liver scanning with colloids Spleen scanning with colloids or heat damaged red blood cells Bone marrow scanning with micro-colloids Pediatric Nuclear Medicine 1974

  35. Phagocytosis - Colloids

  36. Phagocytosis - Liver scanning with colloids

  37. Mechanisms of Localization Cell Sequestration Spleen counting with heat or disease damaged red blood cells (Cr-51 or Tc-99m) Capillary Blockade Lung scanning with Tc-99m labeled human serum albumin (MAA) Pediatric Nuclear Medicine 1974

  38. Spleen scanning with colloids or heat damaged red blood cells

  39. Mechanisms of Localization Simple or Exchange Diffusion Bone scanning with F-18 or Tc-99m phosphonates Brain scanning with Tc-99m pertechnetate or DTPA

  40. Bone Agents Structure Pyrophosphate MDP HDP

  41. Types of Bone Scans Whole Body Limited Three-phase

  42. Brain scanning with Tc-99m pertechnetate or DTPA Normal

  43. Brain scanning with Tc-99m pertechnetate or DTPA Brain Death

  44. Mechanisms of Localization Compartmental Localization Blood pool scanning of heart and vascular system with Tc-99m RBC or HSA Cerebrospinal fluid space with In-111 DTPA

  45. Cerebrospinal fluid space with In-111 DTPA CSF Leak Posterior Nasal Pharynx

  46. Cerebrospinal fluid space with In-111 DTPA

  47. Mechanisms of Localization Metabolic Substitution F-18 Fluorodeoxyglucose (FDG) Imaging for Cancer, Brain, Heart • Molecular Formula C6H1118FO4 • Molecular Weight 166.15 daltons • Half life 110 min • D-glucose C6H12O6 • M.W.= 180.16 dal

  48. F-18 FDG Imaging for Cancer - Lymphoma

  49. F-18 FDG Imaging for Heart - Ischemia Ischemia or Infarct Lateral Wall

  50. F-18 FDG Imaging for Heart - Ischemia Reversible Ischemia Lateral Wall

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