Diploma in Pharmacy / Бакалавр (Diploma) в Области Фармацевтического Дела

Course Details

Course Information Package

Course Unit TitleDESIGN,DISCOVERY & DEVELOPMENT OF DRUGS
Course Unit CodePHA410
Course Unit Details
Number of ECTS credits allocated6
Learning Outcomes of the course unitBy the end of the course, the students should be able to:
  1. Explain the basics of the historical perspectives of drug discovery; the difference in discovering drugs in antiquity, serentipity, the try-and-error- method, the iatrochemistry era, that of synthetic dyes, massive pharmacological testing and antibiotics.
  2. Identify the meaning and use of lead compound, pharmacophore, lead optimisation, drug receptor-fitting and docking, molecular graphics, receptor mapping.
  3. Identify the exact meaning, applications, profitable use of lead compound, pharmacophore, lead optimisation.
  4. Identify the meaning and use of important bases of rational drug design.
  5. Distinguish, applying theoretical calculations, pKa, lipophilicity (log P) and topological polar surface area (TPSA) of bioactive molecules.
  6. Distinguish the docking of molecules to the active site of receptors and the meaning of receptor targeting and QSAR.
  7. Distinguish the contribution of clinical phases I, II, III and pharmacovigilance.
  8. Analyse advantages of the massive pharmacological screening and the approach of rational drug design and have a fair idea on the prospects for the future in the field of drug discovery and development.
Mode of DeliveryFace-to-face
PrerequisitesPHA301,PHA401Co-requisitesNONE
Recommended optional program componentsNONE
Course Contents·  Organisation of a pharmaceutical industry: Chemical section, production of the active principle compounds. Formulation section, solid, liquid, injectable forms. Analytical control section. Sterile area.
·  Scaling-up process, from laboratory to pilot plant quantities. Massive production. Problems and solutions of industrial-mass production. Prevention and assessment of trans contamination. Washing and cleaning machines. Sterilization, sterile area, disinfection, control and assessment.
·  Setting of the whole plant. Personnel, education, skills, consciousness, health, health safeguard. Care and protection of the pharmaceutical plant environment. Good manufacturing practice. In vitro and in vivo evaluation of the product quality. Development of novel pharmacotechnological forms and delivery systems. Research section, design of novel molecules, of improved or novel technological products - drug releasing forms. Innovations in analytical methods. Administration and Product promotion sections and follow-up.
·  The patent office for the new molecules and the innovative delivery systems will be presented.
·  Laboratory Work: Prediction, applying theoretical calculations, of pKa, lipophilicity (log P) and topological polar surface area (TPSA) of bioactive molecules; Find the pharmacophore of local anaesthetics. Show that one of them acquires local anaesthetic action. Discuss the optimisation performed starting from cocaine to common local anaesthetic; Find the pharmacophore of morphine-like analgesics. Demonstrate that one of them has the analgesic activity. Discuss the performed pharmacophore optimisation and indicate the lead compound; Docking of molecules to the active site of receptors; Demonstrate the antimicrobial activity of methylene blue, a synthetic dye; Suggest structural modifications on a centrally acting analgesic in order to restrict its activity to the intestine. Show lack of CNS action; Find a compound that would act as an antidote to paracetamol hepatotoxicity, based on the mechanism of the hepatotoxic action of paracetamol overdose; Synthesis of a compound for protection against paracetamol hepatotoxicity, based on rational drug design.
Recommended and/or required reading:
Textbooks
  • «Οργανική Φαρμακευτική Χημεία, Θέματα Φαρμακοχημείας-Σχεδιασμού φαρμάκων», Ε.Α. Ρεκκα, Π.Ν. Κουρουνάκης, Εκδ. Φ. Χατζηπάντου, Θεσσαλονίκη 2010.
References
  • “Textbook of Drug Design and Discovery”, T. Liljefors, P. Krogsgaard-Larsen, U. Madsen, CRC Press; 3rd edition, 2002.
Planned learning activities and teaching methodsThe taught part of course is delivered to the students by means of lectures, conducted with the help of computer presentations. Lecture notes and presentations are available through the web for students to use in combination with the textbooks.
Lectures are supplemented with laboratory work.
Assessment methods and criteria
Tests20%
Laboratory work20%
Final Exam60%
Language of instructionGreek
Work placement(s)NO

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