Radiopharmaceuticals františek Melichar


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  RADIOPHARMACEUTICALS


Radiopharmaceuticals Scope of Presentation

  • Basic information

  • Diagnostic radiopharmaceuticals

    • SPECT,
    • PET
  • Therapeutic radiopharmaceuticals

    • palliative radiopharmaceuitcals
    • Immunotherapeutic radiopharmaceuticals
    • radiation synovectomy


Radiopharmaceuticals

  • A radiopharmaceutical is

  • a radioactive compound used for the diagnosis and therapeutic treatment

  • of human diseases



Radiofarmaceuticals

  • Has two components :

  • radionuclide

  • pharmaceutical

  • proteins, Mab, inorganic, organic compounds



Radiopharmaceuticals designing

  • First chosen is on basis of its preferential localization in given organ

  • or

  • its participation in the physiologic function of the organ



Radiopharmaceuticals

  • Difference

  • between

  • radiochemicals and radiopharmaceuticals



Ideal radiopharmaceutical

  • Easy availability

  • Shorf effective Half-Life

  • Particle Emission

  • Decay by Electron Capture or Isomeric Transition

  • High Target-to Nontarget Activity Ratio



Radiopharmaceuticals

  • Radioactive element - 133Xe

  • Labeled compounds - 131I iodinated proteins

  • 99mTc labeled compounds

  • [18F]FDG



Radiopharmaceuticals

  • Radiopharmaceuticals usually have no pharmacologic effect, because in most cases they are used in trace quantities

  • Differ from conventional drugs

  • but they should be sterile and pyrogen free



Easy availability (1)

  • Nuclear reactor (n,p), (n,)

  • A ZX (n,) A+1 ZX

  • 98Mo (n,) 99Mo 99mTc

  • Particle accelerators

  • 68Zn (p,2n) 67Ga

  • 203Tl (p,3n) 201Pb +or EC 201Tl



Easy availability (2)

  • Starting material and product have diferent chemical identities

  • Enriched target

  • Secondary source

  • Generator of radionuclides

  • 99Mo/99mTc, 113Sn/113mIn, 81Rb/81mKr,82Sr/82Rb, 90Sr/90Y,68Ge/68Ga



Short Effective Half-Life

  • Physical half-life TP , t1/2

  • p=0,693/Tp - decay constant

  • Biologic half-life Tb

  • b=0,693/Tb

  • Effective half-life Te

  • e= p+ b

  • 1/Te=1/Tp +1/Tb



Particle Emission

  • Diagnostic purpose -undesirable

  • Therapeutic purpose - ,

  • Radiation damage of abnormal cells



High Target-to Nontarget Activity Ratio

  • To provide maximum efficacy in

  • the diagnosis (therapy)

  • and minimum radiation dose to the patient



Factors Influencing the Design of New Radiopharmaceuticals (1)

  • Compatibility-incorporation radionuclide into the molecule 111In-DTPA

  • Stechiometry- concentration 99mTc approx. 10-9 mol/l

  • Charge of the Molecule

  • Size of Molecule



Factors Influencing the Design of New Radiopharmaceuticals (2)

  • Protein Binding

  • Solubility

  • Stability

  • Biodistribution



Type of radiopharmaceutical for diagnostic and therapy

  • Type of radiopharmaceutical for diagnostic and therapy

  • Parenteral pharmaceuticals (solutions or colloid suspenses),

  • peroral pharmaceuticals

  • inhalation pharmaceuticals

  • topic pharmaceuticals



Radionuclide suitable for application in nuclear medicine



Diagnostic radiopharmaceuticals for SPET

  • 99mTc dominant radionuclide in the NM

  • Radiofarmaceuticals precurzor

  • source is radionuclide generator

  • 99Mo (-,T1/2=66,2 h) / 99mTc (IT,T1/2=6,02 h)

  • Other radionuclides for labeling radiopharmaceuticals

  • 201 Tl (EC, T1/2= 72 h) , 67 Ga (EC, T1/2 =77,9 h),

  • 111 In (EC, T1/2 =2,8 d), 123 I (EC, T1/2 = 13,2 h),

  • 125 I (EC, T1/2 =60,1 d),

  • 81Rb (EC, +, T1/2 = 4,57h, /81mKr(IT, T1/2 = 13 s)



Radionuclide generator 99Mo (-,T1/2=66,2 h) / 99mTc (IT,T1/2=6,02 hod)





Sorption generator



Diagnostic radiopharmaceuticals for PET

  • Emission + , anihililation gama kvant 511 keV



Positron (+) radiation - annihilation



Application of Positron Emission Tomography



18F - Physical properties

  • 8O



Cyclotron production of 18F



Cyclotron U-120M



Target equipment



The metabolic „fate“ of glucose (GLU) and FDG



Oncology



Process of 2-[18 F]FDG syntesis



18F-FDG synthesis assembly



Radiochemical purity - HPLC method



[18F]NaF, injection – syntetisation modul



[18F]NaF injekce- picture of rabbit









3´-FLT and biosynteze DNA



Therapeutic radionuclide

  • Radionuclide for teletherapy 60Co , 137Cs

  • Radionuklidy for brachytherapy 192 Ir, 145 Sm ,103Pd , 125I

  • Palliative aplication [89Sr]SrCl2, ,,[153Sm]SmEDTMP (etylendiaminN,N,Nˇ,Nˇ,-

  • tetrakismethylenfosfonová kyselina)

  • [186 Re] ReHEDP (hydroxyethylendifosfonová kyselina)

  • Radiation synovectomy compounds 166Ho, 186Re, 90Y

  • Therapeutic radiofarmaka Compounds 131I, 32 P, 188Re, 90Y, 166Ho , radiolanthanoides Immunotherapeutics- requested no added carry (carry free radionuclide 90Y, 188Re



Therapeutic and maximum range of  radionuclides in tissue



Chelation compounds



166Ho - Basic Information

  • 166Ho Physical Properties Overview

    •  - Radiation
      • Maximum Energy: 1.85 MeV 1.77 MeV
    • Gamma Radiation
      • Energy: 81 keV 1379 keV
    • Half life time: 26.8 hours
    • Daughter isotope: Eu-166 (stable)


166Ho-Macroaggregates Rheumatoid Arthritis Treatment

  • The Principle of Therapy

  • Inflamed synovial membrane destruction

  • The Method of Treatment

  • Radiation synovectomy

    • Suspension of 166Ho-Macroaggregates particles injection into the diseased joint
    • Particles are trapped by the inflamed synovial membrane
    • Destruction of the membrane through radiation


CHITOSAN CHARACTERISATION AND MEDICAL APPLICATIONS [1-3]    organic matrix in skeletons of crabs,    biodegradable, biocompatible, non-toxic pharmaceutical carriers,    hemostatics and blood anticoagulants,    aggregation of leukemia cells,    enzyme immobilization,    hypocholesterolemic activity -inhibition of micille formation, adsorption of cholesterol, fatty acids and monoglycerides,    metal ion chelation (amino groups of chitosan),    gel-forming in neutral conditions, soluble and viscous in acidic conditions.



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