ORGANIC PHARMACEUTICAL CHEMISTRY III

Course Information
TitleΟΡΓΑΝΙΚΗ ΦΑΡΜ/ΚΗ ΧΗΜΕΙΑ ΙΙΙ / ORGANIC PHARMACEUTICAL CHEMISTRY III
Code70
FacultyHealth Sciences
SchoolPharmacy
Cycle / Level1st / Undergraduate
Teaching PeriodWinter
CommonNo
StatusActive
Course ID180000113

Programme of Study: Programme of Studies 2008-

Registered students: 359
OrientationAttendance TypeSemesterYearECTS
CoreCompulsory Course748

Class Information
Academic Year2018 – 2019
Class PeriodWinter
Faculty Instructors
Weekly Hours5
Class ID
600131541
Type of the Course
  • Scientific Area
Course Category
Specific Foundation / Core
Mode of Delivery
  • Face to face
Digital Course Content
Erasmus
The course is also offered to exchange programme students.
Language of Instruction
  • Greek (Instruction, Examination)
Prerequisites
General Prerequisites
Basic principles of Pharmacochemistry Synthetic Organic Chemistry
Learning Outcomes
This course is concerned with the discovery, design, synthesis and identification of biologically active compounds acting on the central nervous system (CNS), antiepileptics drugs: miscellaneous anticonvulsants, miscellaneous antiparkinson agents, NMDA receptor antagonists for the treatment of Alzheimer’s disease, antimigraine agents, agonists/antagonists of Αdenosine, Inhibitors of adenyl-cyclase- Inhibitors of PDEs, Μethylphenidate and analogues, Inhibitors of serineproteases, Statines, Αgonists/Αntagonists of CCK. Quantitative structure-activity relationships (SAR/QSAR). Finally, agents used illegally, such as opioids, cannabinoids and other drugs of addiction, with special pharmaco-sociologic interest, are studied. Aims are the critical knowledge and thorough examination of synthesis, structure, correlation of structure with drug action, fate of the drugs in the organism, sites of loss, therefore duration of drug action. Aim is also to familiarise the students with relations governing molecules acting on CNS and the central nervous system site of action, as well as the involved neurotransmitters. Scills: By the end of this course, the students should be able to: Know the synthesis of the important drug molecules used for pathologic conditions concerning CNS and cardiovascular system, the physical and chemical properties of these drugs, the biological properties that give the therapeutic potential to these groups of drugs, the structural changes (i.e. metabolism) and fate of these molecules in the organism, the duration of action, the possibility of biodetoxication or biotoxication. Reach conclusions on the relationships between action and structural and physicochemical characteristics and examples are studied of characteristic molecules used illegally as narcotic and addictive agents, from the pharmacochemical point of view.
General Competences
  • Apply knowledge in practice
  • Retrieve, analyse and synthesise data and information, with the use of necessary technologies
  • Adapt to new situations
  • Make decisions
  • Work autonomously
  • Work in teams
  • Work in an international context
  • Work in an interdisciplinary team
  • Generate new research ideas
  • Design and manage projects
  • Appreciate diversity and multiculturality
  • Respect natural environment
  • Demonstrate social, professional and ethical commitment and sensitivity to gender issues
  • Be critical and self-critical
  • Advance free, creative and causative thinking
Course Content (Syllabus)
1) Eleni A. Rekka Τhis course analyses synthetic pathways, extraction-isolation, physical, chemical, biological properties, purity and quality control, identification, quantitative determination, molecular mode of action, side effects, fate in the organism - drug metabolism, structure-activity relationships, therapeutic uses, adverse actions and doses of drugs acting on the Central Nervous System, i.e. hypnotics, anxiolytics, neuroleptics (drugs acting against mania and psychoses), antidepressants. Opioids and other centrally acting analgesic and antitussive agents. Opioid antagonists. Introduction to addiction. Agents used in detoxication and addiction therapy. Cannabinoids, psychotoxic and psychedelic drugs. 2) Ioannis Nicolaou Pharmacochemical approach (as design, synthesis, physicochemical properties, target cell interactions, structure-activity relationships, pharmacochemical interpretation of toxicity, metabolism) of the below classes of drugs: miscellaneous anticonvulsants, miscellaneous antiparkinson agents, NMDA receptor antagonists for the treatment of Alzheimer’s disease, antimigraine agents. 3) Dimitra Hadjipavlou-Litina Stimulants-Αnaleptics -Agonists/antagonists of Αdenosine, Inhibitors of adenyl-cyclase- Inhibitors of PDEs, Μethylphenidate and analogues, Inhibitors of serineproteases, Statines, Αgonists/Αntagonists of CCK. Quantitative structure activity relationships (SAR/QSAR). Examples of Quantitative structure activity relationships determination and chemical identifications.
Keywords
pharmacochemistry, structure, activity
Educational Material Types
  • Notes
  • Slide presentations
  • Book
Use of Information and Communication Technologies
Use of ICT
  • Use of ICT in Course Teaching
  • Use of ICT in Communication with Students
Description
1) Eleni A. Rekka, professor Relevant announcements are presented in the corresponding place of the website of the School of Pharmacy. 2) Ioannis Nicolaou, Lecturer Lectures, notes, statements etc are presented in the corresponding place of the website of the School of Pharmacy 3) Dimitra Hadjipavlou-Litina, professor Lectures, notes, statements etc are presented in the corresponding place of the website of the School of Pharmacy
Course Organization
ActivitiesWorkloadECTSIndividualTeamworkErasmus
Lectures144
Laboratory Work96
Total240
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 4 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. To compute the final grade: the grade given by each tutor is taken (E. Rekka = 4.5/ D. Hadjipavlou-Litina = 3.5 /I. Nicolaou = 2.5) and the final grade is calculated by addition of the course exam grade (80%) and the lab exam grade (20%).
Student Assessment methods
  • Written Exam with Short Answer Questions (Summative)
  • Labortatory Assignment (Summative)
Bibliography
Course Bibliography (Eudoxus)
Ειδική Οργανική Φαρμακευτική Χημεία, Π.Κουρουνάκης
Additional bibliography for study
1) Ελένη Ρέκκα • A. Korolkovas, “Essentials of Medicinal Chemistry”, Wiley International Publications, John Wiley & Sons, 2003. • J.M. Beale, J. Block, “Wilson and Gisvold's Textbook of Organic Medicinal and Pharmaceutical Chemistry”, Lippincott Williams & Wilkins; 12th ed., 2010 2) Ιωάννης Νικολάου • Journal of Medicinal Chemistry (ACS Publications) • Bioorganic & Medicinal Chemistry Letters - Elsevier • Bioorganic & Medicinal Chemistry (ISSN 0968-0896) • The Journal of Biological Chemistry • Chemical Research in Toxicology (ACS Publications) • Drug Metabolism and Disposition 3) Δήμητρα Χατζηπαύλου-Λίτινα • Medicinal Chemistry Principles and Practice, Ed. F.D.King. 1994, The Royal Society of Chemistry, ISBN 0-85186-494-5 • Contemporary Drug Synthesis Li J.J, Johnson D., Sliskovic D., Roth B. Wiley-Interscience,2004, ISBN 0-471-21480-9 • New Trends in Synthetic Medicinal Chemistry, Ed. F. Gualtieri, Wiley –VCH, Vol. 7, 2000 • Annual Reports in Medicinal Chemistry, Academic Press • Journal of Medicinal Chemistry (ACS Publications) • Bioorganic & Medicinal Chemistry Letters - Elsevier • Bioorganic & Medicinal Chemistry (ISSN 0968-0896) • “Practical Pharmaceutical Chemistry part I, II) The Athlone Press 1975 • “Principles of Medicinal Chemistry” W.O. Foye, ed. Lea & Febiger, 1995 • “Remington’s Pharmaceutical Sciences”, Osol A. ed. Mack Publishing Co., 1980 • « Goodman & Gilman’s The Pharmacological Basis of Therapeutics » Goodman a., Hardman J., Limbird L., eds MacMillan Publishing Co 2001 • “Strategies for Organic Drug Synthesis and Design” Lednicer, D., ed. Wiley J. & Sons 2000 • ”Essentials of Pharmacology” Theocharidis T. Little, Brown & Company 2nd edition, 1999 • Drug Actions, Basic Principles and Therapeutic Aspects, Mutschler/Devendorf • Archiv.Pharm 317, 183-185, 1984 • Arch Pharm 325, 483-90, 1992. • Arch Pharm 328, 689-698, 1995 • Intensive Care Med. 18, 449-454, 1992 • Greenblatt et al. (1999) FEBS Letters 463, p321 • Dvir et al. (2003) JACS 125, p363 • Bar-On et al. (2002) Biochemistry 41, p3555. • Kryeger et al.,(1997) Structure 7,297 • Raves et al. (1997) Nature Structural Biology 4, p57 • Εθνικό Συνταγολόγιο 2007, Εθνικός Οργανισμός Φαρμάκων
Last Update
22-11-2016