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PHARMACEUTICAL AND TOXICOLOGICAL CHEMISTRY II (PCT)

CODE 67558
ACADEMIC YEAR 2022/2023
CREDITS
  • 9 cfu during the 4th year of 8451 CHIMICA E TECNOLOGIA FARMACEUTICHE (LM-13) - GENOVA
  • SCIENTIFIC DISCIPLINARY SECTOR CHIM/08
    LANGUAGE Italian
    TEACHING LOCATION
  • GENOVA
  • SEMESTER 2° Semester
    PREREQUISITES
    Prerequisites
    You can take the exam for this unit if you passed the following exam(s):
    • Pharmaceutical chemistry and technology 8451 (coorte 2019/2020)
    • GENERAL AND INORGANIC CHEMISTRY (PCT)(MD) 55401
    • ORGANIC CHEMISTRY I (PCT)(MD) 60822
    • ORGANIC CHEMISTRY II (PCT)(MD) 60828
    • MEDICINAL AND TOXICOLOGICAL CHEMISTRY I 80446
    Prerequisites (for future units)
    This unit is a prerequisite for:
    • Pharmaceutical chemistry and technology 8451 (coorte 2019/2020)
    • DRUG SYNTHESIS (WITH PRACTICE) 80453
    TEACHING MATERIALS AULAWEB

    OVERVIEW

     

    The course of Chimica Farmaceutica e Tossicologica II is held for students of the fourth year of the degree in CTF (Medicinal Chemistry and Technology)

    The course is  9 CFU (72 hours of lessons), whithout any laboratory exercises.

    The attendance of the course is registered for the evaluation of the course done by the students, that are classified in those who attended the course and those who didn't attended.

    To have the attendance of the course the student must follow  50% of the lessons.

     

     

    AIMS AND CONTENT

    LEARNING OUTCOMES

    The aims of the course are to give to the students the fundamental knowledge on the chemical and physico-chemical characteristics, the strucure-activity-relationship (SAR), the molecular mechanisms of actions and the toxicology of some classes of drugs. In detail, the students will be able to discuss the mechanisms of actions and the SAR of the drugs on the basis of their chemical strucures. The students will be able to describe the synthesis of some drugs.

     

    AIMS AND LEARNING OUTCOMES

    The course aims to provide the student with the knowledge of drugs currently in use in hormonal pathologies, CNS,cardivascular, gastrointestinal, respiratory diseases, together with the mechanism of action of the drugs and their toxic effects. Syntheses, structure-activity relationships (SAR), optimization studies and action mechanisms of these therapeutic classes are reported. Furthermore, the course aims to provide students with the basic knowledge useful for design and synthesis of biologically active molecules.

    Another fundamental objective of this course is the demonstration of the practical application in the field of pharmaceutical chemistry of all the knowledge acquired by the student during other courses, in particular those relating to general and organic chemistry and biochemistry.

    At the end of the course the student will be able to recognize the main drugs of the categories listed in the program, describe their synthesis, structure-activity relationships, know the mechanisms of action and toxic effects.

    PREREQUISITES

    Knowledge of general inorganic chemistry, organic chemistry and biochemistry.

    TEACHING METHODS

    Theoretical frontal lessons with the use of slides. 

    The slides available as teaching material on Aulaweb and are the basis for detailed explanations by the teacher on the various topics of the course, in particular regarding syntheses and mechanism of action of the discussed drugs.

    SYLLABUS/CONTENT

     

    The first part of the course is related to the hormones on the whole (bio-synthesis, physiological role, therapeutic use, synthetic drugs related to them). In particular will be discussed: Calcium homeostasis regulators (parathyroid hormone, bisphosphonates, calcitonine); thyroid hormones (T3, T4), antithyroid drugs; insulin, glucagon, oral hypoglycemic drugs; steroid hormones: mineral- and glucocorticoids, estrogens, antiestrogens, progestins, antiprogestins, contraceptives, androgens, anti-androgens, anabolic steroids.

    The second part of the course describes the following therapeutic class: cholinergic, adrenergic and  serotoninergic system drugs; local and systemic anesthetics; hypnotic/sedative drugs; ansiolitics, antipsycotics, anticonvulsants, muscle relaxants, antiparkinson drugs, opioids and derivatives, antidepressants, psychotomimetics and other central stimulant drugs; cardiovascular drugs; antihypertensive drugs,  diuretics; antiaggregants, anticoagulants, fibrinolitics; non steroidal antiinflammatory drugs; antihistaminics. As a part of the discussion of the different therapeutic classes are examined: the physico-chemical properties, design strategies, the structure of biological targets and the mechanisms of interaction, the structure-activity relationships. The synthetic methods are reported for:

    Protirelin, levothyroxine, sulphonylureas, bisguanides, Carbacol, Betanecol, Fisostigmine, Neostigmine, Piridostigmiea, Ecotiophato, Atropin, Scopolamine, Benztropine, Triesifenidile, Succinilcholine, Pancuronium, Vencuronium, Atracurium, Salbutamol, Lidocaine, Chlordiazepoxide, Diazepam, Bromazepam, Lorazepam, Alprazolam, Triazolam, Aloperidol, Luminal, Valproic ocid, Meprobamate, Levodopa, Heroin, Hydromorphon, Hydrocodeinon, Oxymorphon, Oxycodon, Ethorphine, Buprenorphine, Levorfanol, Butorfanol, Meperidine, Fentanil Methadon, Propoxyphen, Tramadol, Loperamide, Desipramine, Nortriptiline, Imipramine, Amitriptiline, Fluoxetine, Trazodone, Selegiline, Milrinon, Amiodarone, Captopril, Enalapril, Verapamil, 1,4-dihydropiridine, Hydrochlorotiazide, Furosemide, Etacrinic acid, Triamterene, Indomethacine, Diclofenac, Ibuprofen, meclofenamic acid, Piroxicam, Fenbenzamine, Difenidramine, Ciproeptadine, Cetirizine, Cimetidine

    RECOMMENDED READING/BIBLIOGRAPHY

    The book suggested is  “Chimica Farmaceutica” Autori Gasco, Gualtieri, Melchiorre, Editore CEA.

    Some topics are developed by the teacher on the basis of  specific literature.

    Moreover the teacher updates the program, by adding the new drugs, which are launched on the market.

     

     

    TEACHERS AND EXAM BOARD

    Exam Board

    SILVIA SCHENONE (President)

    PAOLA FOSSA

    ANNA CARBONE (Substitute)

    GIANCARLO GROSSI (Substitute)

    FRANCESCA MUSUMECI (Substitute)

    ANDREA SPALLAROSSA (Substitute)

    LESSONS

    LESSONS START

    The course usually starts in the last week of September

    Class schedule

    All class schedules are posted on the EasyAcademy portal.

    EXAMS

    EXAM DESCRIPTION

    The exam is oral and in the presence of two professors, one is who held the course. The exam lasts depending on the preparation of the student, usually 30-60 min.

    At the request  of the students who follow the lessons, a written exam on the first part of the program can be held during the period of the course.

    ASSESSMENT METHODS

    During the exam, the professor evaluates if the student has achieved: 1) the knowledge of the treated topics, 2) the ability of applying the achieved knowledge on real problems, 3) the ability of using an appropriate scientific language and of linking different topics treated during this course.

    Exam schedule

    Date Time Location Type Notes

    FURTHER INFORMATION

    During the course the professor is available for the students, to give explanations on the treated topics.