核医药物生理学.docVIP

核醫藥物生理學 Radiopharmaceuticals Pharmaceutical Radionuclide Diagnosis or treatment Difference with Conventional Pharmaceuticals in No pharmacologic effect No dose-response relationship The Same with Conventional Pharmaceuticals in Sterile Pyrogen free An Ideal Radiopharmaceutical should have Easy availability Short effective half-life Particle emission Decay by electron capture or isomeric transition High target-to-nontarget activity ratio The Mechanism of Radiopharmaceuticals Passive diffusion: DTPA Ion exchange: MDP Capillary blockage: MAA Phagocytosis: S-colloid Active transport: Tl-201 Cell sequestration: Damaged RBC Metabolism: FDG Receptor: IBZM Compartmental localization: RBC Ag-Ab complex formation: CEA Chemotaxis: WBC 99mTc-labeled RBC Diffusion into RBC Sn2+ + 99mTc7+→Sn4+ + 99mTc5+ 99mTc5+: 80% bind in β-chain of the globin part of Hgb and 20% bind in heme stannous citrate, stannous gluceptate and stannous pyrophosphate 99mTc-HMPAO 99mTcO4- eluted within 2 h 99mTcO4- has been eluted in the same generator Add phosphate buffer to PH = 6 Add methylene blue as scavenger (to remove free radicals and excess Sn2+) Stabilization may prolong from 30 min to 4 h after preparation Acidic vs. Alkaline Condition for DMSA An Ideal Therapeutic Radiopharmaceutical Strong β energy Short physical half-life Relatively long biological half-life ( emission for the mapping of post-therapy distribution Therapeutic Radiopharmaceuticals for Pain Relieve 89Sr 186Re-HEDP 153Sm-EDTMP 117mTin(4+) DTPA Lymphoscintigraphy Sentinel node Satellite node  Radiopharmaceuticals for Brain Imaging SPECT Blood-brain-barrier: 99mTcO4-, 99m Tc-DTPA, 201Tl, 67Ga Perfusion agent: 123I-IMP, 99m Tc-HMPAO, 99m Tc-ECD Receptor agent: 123I-IBZM (2) PET Perfusion agent: [15O]H2O, [13N]NH3 Metabolic agent: [18F]FDG, [11C]methylmethionine Neurotransmitter agent: [18F]fluorodopa Receptor agent: [11C]raclopride Considerations of Radiopharmaceuticals in Brain Tumor Increased vascularity Abnormal cap