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RADIOCHEMISTRY AND RADIOPHARMACOLOGY (RCF 802)

MMed & B Rad (HONS) NUCLEAR MEDICINE

Study Guide:

RADIOCHEMISTRY & RADIOPHARMACOLOGY ( RCF 700/802)

 

Dr W K A Louw  PhD.

                                                                                   

1.         Basic chemical concepts

 

1.1       Elements and compounds

1.2          The Atom

1.3       Electronic structure of the atom

1.4       Chemical bonds

            1.4.1    Ionic bonds

1.4.2    Covalent bonds

1.4.2    Coordinate covalent bonds

1.4.3    Complex formation and chelates

1.5       Empirical and molecular formulas
 

1.6       Organic compounds

            1.6.1    Chemical bonding in organic compounds

1.6.2    Depiction of organic compounds

1.6.3    Types of organic compounds and nomenclature

1.6.4    Functional groups
 

1.7       Chemical reactions and chemical equations

1.7.1    Metathesis reactions

1.7.2    Oxidation-reduction reactions
 

1.8       Solutions and colloids

1.9       Acids and bases

1.9.1    Definitions

1.9.2    Acid and base reactions

1.9.3    Strong versus weak acids and bases

1.9.4    The pH concept

1.9.5    Buffer solutions

 

2.         Radiochemistry

2.1       Production of radionuclides

2.1.1    Cyclotron-produced radionuclides    

            2.1.1.1 Gallium-67

                        2.1.1.2 Iodine-123

                        2.1.1.3 Indium-111

                        2.1.1.4 Thallium-201

                        2.1.1.5 Short-lived radionuclides

2.1.2    Reactor-produced radionuclides

                        2.1.2.1 Fission or (n,f) reaction

                        2.1.2.2 Iodine-131

                        2.1.2.3 Molybdenum-99

                        2.1.2.4 Neutron capture or (n,γ) reaction

2.1.3    Target and its processing

2.1.4    Radionuclide generators

                        2.1.4.1 Principles of a generator

                        2.1.4.2 Important radionuclide generators
 

2.2       Radiopharmaceuticals and methods of radiolabeling

2.2.1      Definition of a radiopharmaceutical

2.2.2      Ideal radiopharmaceutical

2.2.3    Methods of radiolabeling

2.2.4    Important factors in labeling

2.2.5    Specific methods of labeling

2.2.5.1 Radioiodination

2.2.5.2 Labeling with ^99mTc

2.2.5.3  Kits for ^99mTc-labeling

 

3.         Characteristics of specific radiopharmaceuticals

3.1           ^99mTc- radiopharmaceuticals

3.1.1      ^99mTc-pertechnetate

3.1.2    ^99mTc- human serum albumin

3.1.3    ^99mTc- macroaggregated albumin

3.1.4    ^99mTc- phosphonates and phosphates

3.1.5    ^99mTc-pentetate (DTPA)

3.1.6    ^99mTc-labeled red blood cells

3.1.7    ^99mTc-iminodiacetic acid derivatives

3.1.8    ^99mTc-hexamethylpropylene amine oxime (HMPAO), (Ceretec)

3.1.9    ^99mTc-sestamibi (Cardiolite)

3.1.10  ^99mTc-teboroxime (Cardiatec)

3.1.11  ^99mTc-tetrofosmin (Myoview)

3.1.12   ^99mTc-mercaptoacetylglycylglycylglycine (MAG3)

3.1.13  ^99mTc-ethyl cysteinate dimer (ECD), (Neurolite)

3.1.15  ^99mTc-dimercaptosuccinic acid (DMSA)

3.1.16  ^99mTc-labeled tin colloid

 

3.2       Radioiodinated radiopharmaceuticals

3.2.1    ¹³¹I-sodium iodide

3.2.2    ¹²³I-sodium iodide

3.2.3    ¹²³I- or ¹³¹I-metaiodobenzylguanidine (MIBG)

3.2.4      ¹²³I-d,1-N-isopropyl-p-iodoamphetamine hydrochloride (IMP)

 

3.3       Miscellaneous Radiopharmaceuticals

3.3.1    ¹³³Xe gas

3.3.2    ²⁰¹thallous chloride

3.3.3    ¹⁸F-fluorodeoxyglucose (FDG)

3.3.4      ⁶⁷Ga-citrate

3.3.5      ¹¹¹In-DTPA-octreotide (Octreoscan)

3.3.6    Radiolabeled leucocytes and platelates

3.3.7    Radiolabeled monoclonal antibodies

3.3.8    Radiolabeled peptides

3.3.9      Other radiopharmaceuticals of clinical importance

 

3.4       Therapeutic radiopharmaceuticals

3.4.1    Radiobiological rationale

3.4.2    ¹³¹I-sodium iodide

3.4.3    ¹³¹I-MIBG

3.4.4    ³²P-sodium phosphate

3.4.5    ⁸⁹Sr-strontium chloride (Metastron)

3.4.6    ¹⁸⁶Re-hydroxyethylidene diphosphonate (HEDP)

3.4.7      ¹⁵³Sm-ethylenediaminetetramethylene phosphonic acid (Quadramet)

 

4.         Quality control of radiopharmaceuticals

4.1      Physiochemical tests

4.1.1   Physical characteristics

4.1.2      pH and ionic strength

4.1.3      Radionuclidic purity

4.1.4      Radiochemical purity

4.1.5      Chemical purity

4.1.6      Radioassay

4.2      Biological tests

4.2.1   Sterility

4.2.2   Apyrogenicity

4.2.3   Toxicity