ORGANIC-RADIOPHARMACEUTICAL CHEMISTRY

Course Information
TitleΟΡΓΑΝΙΚΗ-ΡΑΔΙΟΦΑΡΜΑΚΕΥΤΙΚΗ ΧΗΜΕΙΑ / ORGANIC-RADIOPHARMACEUTICAL CHEMISTRY
CodeΝΠ38
FacultyHealth Sciences
SchoolPharmacy
Cycle / Level1st / Undergraduate
Teaching PeriodSpring
CommonNo
StatusActive
Course ID180000279

Programme of Study: Programme of Studies 2008-

Registered students: 290
OrientationAttendance TypeSemesterYearECTS
CoreCompulsory Course844

Class Information
Academic Year2018 – 2019
Class PeriodSpring
Faculty Instructors
Weekly Hours4
Class ID
600137844
Type of the Course
  • Scientific Area
Course Category
Specific Foundation / Core
Mode of Delivery
  • Face to face
Language of Instruction
  • Greek (Instruction, Examination)
Learning Outcomes
This course is an introduction to the applications of modern pharmacochemical aspects in drug design and in the successful confrontation of pathologic conditions (incurable, insufficiently cured diseases, toxicity of chemicals), using contemporary pharmacochemical methods. Relations of chemical structure, physicochemical properties and activity are studied. Another aim is the acquisition of satisfactory knowledge of the medicinal chemistry of free radicals, role of oxygen in life, free radical reactions in biological systems, reactive oxygen species and mechanisms of radical attack to lipids, proteins and DNA. Knowledge of physiological defensive mechanisms against free radicals, as well as explanation of oxidative stress are among the aims of this course. Comprehension of the blood-brain barrier, construction, function and physiologic role, in relation to drug action, is another aim. Furthermore, the course aims at providing basic knowledge on the properties and medical applications of ionizing radiation, as well as the nuclear properties requirements of radionuclides used in radiopharmacy. In a deeper scope, this course covers the pharmaceutical radiochemistry of commonly used radionuclides in radiopharmacy. The design and mechanism of action of common radiopharmaceuticals at the target site is discussed. Finally, the course covers methods of evaluation of the radiochemical purity of radiopharmaceuticals.
General Competences
  • Apply knowledge in practice
  • Retrieve, analyse and synthesise data and information, with the use of necessary technologies
  • Make decisions
  • Work in teams
  • Advance free, creative and causative thinking
Course Content (Syllabus)
This course presents some modern aspects in the broad field of bioactive molecules (drugs, poisons) and the molecular approach to pathologic conditions, aiming to a rational confrontation of them through drug design. The effect of the chemical characteristic groups on activity and toxicity of drug molecules is studied and an approximation in physicochemical properties/chemical structure/activity relationships is performed. Further topics are: Pharmacochemistry of free radicals. Role of oxygen in aerobic life, free radical reactions in biological systems. Reactive oxygen species. Mechanisms of radical attack on lipids, proteins, DNA. Defence of the body against radical offence, the involved mechanisms. Structure, function of blood brain barrier and drug permeability. Radioactivity: Radioactive decay, α, β-, β+, particle emissions, electron capture, γ ray emission, isomeric transition, internal conversion, Auger electrons. Law of radioactivity, Half-life, Successive decay equations, transient and secular equilibrium. Interaction of radiation with matter: ionization, bremsstrahlung, annihilation, photoelectric effect, Compton scattering, pair production. Radiolysis of water, effect of radiation on macromolecules, DNA strand breaks, oxygen effect. Radionuclide generator: Principles of a generator. 99Mo/99mTc generator. Yield of 99mTc. Radionuclide, radiochemical and chemical purity of 99Μο/99mTc generator eluate. Labeled compounds: Radionuclide, radiochemical and chemical purity of labeled compounds. Methods of radiochemical yield calculation (radiochromatography). Radiopharmaceuticals: general principles, diagnostic and therapeutic radiopharmaceuticals. Properties of 99mTc. Chemistry of 99mTc. Labeling with 99mTc (Labeling with reduced 99mTc, Formation of 99mTc-complexes by ligands exchange, reducing agents). Techentium(V), oxo core, isomerism. Methods of radioiodination of proteins (iodine chloride, iodogen, chloramin-T, enzymatic methods) Radiopharmaceuticals of 99mTc and other radionuclides (preparation, clinical applications, pharmacokinetic data). Sodium pertechnetate, technetium-sulfur colloid, technetium-human albumin macroaggregates, technetium-DTPA, technetiumglucoheptate, technetium-succimer, trivalent and pentavalent, technetiummethylendiphosphonate, technetium-iminodiacetic acid derivatives, technetiumhexamethylene amine oxime, technetium- ethyl cysteinate dimmer, technetiummercaptoacetyltriglycine, technetium-hexacis(2-methoxy-isobutyl-isonitrile). [188Re]- rhenium-(hydroxiethylidine diphosphonate). [111In]-Indium-tris (oxine). [123/131Ι]- Sodium Iodide, [123/131Ι]-metaiodobenzyl-guanidine. [18F]-2-fluorodeoxyglucose. Thallium-201. Labeling monoclonal antibodies-advantages and disadvantages. Direct labeling of mAbs with radio-iodine and technetium. Red blood cell labeling with technetium and indium.
Use of Information and Communication Technologies
Use of ICT
  • Use of ICT in Course Teaching
  • Use of ICT in Communication with Students
Course Organization
ActivitiesWorkloadECTSIndividualTeamworkErasmus
Lectures60
Laboratory Work60
Total120
Student Assessment
Description
Examination of the course can be done either by successful participation in two written mid-term exams (grade ≥5 in each mid-term exam) of by a final written examination at the end of the semester. Student eligibility to participate in the mid-term exams is gained by regular attendance of the lectures throughout the semester. Τhe evaluation process is based on questions that the students are asked to answer based on their knowledge obtained from the lectures as well as on the critical thinking and ability to combine, evaluate and handle the acquired knowledge and information. The duration of the examination is 3 hours. The examination at the end of the semester is performed at dates, time and place arranged by the department. During the laboratory work, students hand over a report of their results and are evaluated. At the end of the laboratory work, there is a written examination on this. Successful termination of the laboratory course permits their participation to the final examination. At the examination of the course, each instructor gives out separate exam forms. To compute the final grade, the grade given by each tutor is weighted proportionately to the number of hours he/she has taught. Final grade is calculated by addition of the course exam grade (90%) and the lab exam grade (10%).
Student Assessment methods
  • Written Exam with Short Answer Questions (Summative)
  • Εργαστηριακές εξετάσεις (Summative)
Bibliography
Course Bibliography (Eudoxus)
1) Ε. Χιωτέλλης, «Ραδιοφαρμακευτική Χημεία», Εκδ. Πήγασος, 2000 2) Ε.Α. Ρέκκα, Π.Ν. Κουρουνάκης, «Οργανική Φαρμακευτική Χημεία: Θέματα Φαρμακοχημείας-Σχεδιασμού Φαρμάκων», Εκδ. Φ. Χατζηπάντου, 2010 (ISBN 978-960-98594-3-1)
Additional bibliography for study
1) R. Rodrigo, “Oxidative Stress and Antioxidants: Their Role in Human Disease”, 2009, Nova Science Pub Inc. 2) Gopal B. Saha, “Fundamentals of Nuclear Pharmacy”, Springer, 5th Ed.2003.
Last Update
22-11-2016