Università degli Studi di Perugia

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Unit MEDICINAL CHEMISTRY II

Course
Pharmacy
Study-unit Code
65004411
Location
PERUGIA
Curriculum
In all curricula
Teacher
Violetta Cecchetti
Teachers
  • Violetta Cecchetti - Didattica Ufficiale
  • Oriana Tabarrini - Didattica Ufficiale (Codocenza)
  • Giuseppe Manfroni - Didattica Integrativa
Hours
  • 70 ore - Didattica Ufficiale - Violetta Cecchetti
  • 7 ore - Didattica Ufficiale (Codocenza) - Oriana Tabarrini
  • 2 ore - Didattica Integrativa - Giuseppe Manfroni
CFU
11
Course Regulation
Coorte 2015
Offered
2018/19
Learning activities
Caratterizzante
Area
Discipline chimiche, farmaceutiche e tecnologiche
Sector
CHIM/08
Type of study-unit
Obbligatorio (Required)
Type of learning activities
Attività formativa monodisciplinare
Language of instruction
Italian
Contents
General introduction, historical development, classification, mechanism of action, structure-activity relationship, nomenclature and synthetic aspects of the following therapeutic classes: chemotherapeutic agents, steroidal and nonsteroidal anti-inflammatory agents, cardiovascular drugs.
Reference texts
Lecture notes;

Lemke, T.L.; Williams, D.A. Foye's Principi di Chimica Farmaceutica. VI Ed. Italiana. Piccin (Italia);

Gasco A.; Gualtieri, F.; Melchiorre C. Chimica Farmaceutica. I Ed. 2015. Casa Editrice Ambrosiana (Milano);

Graham L. Patrick. Chimica Farmaceutica Edizione Integrata a cura di G. Costantino. 2015. EdiSES (Napoli)
Educational objectives
The main goal of this class is the rational understanding, through the knowledge of the chemical structure and of the physicochemical properties, of the features which characterize a drug, such as administration, absorption, distrbution, metabolism, excretion, mechanism of action, drug-target interaction, structure-activity relationship, etc.
Prerequisites
In order to understand the topics covered by the teaching and achieve the learning objectives it is necessary to have acquired the knowledge of the chemical and biological basic courses. In addition, it is useful to have taken the exam of "Pharmacokinetics and Pharmacology and Pharmacognosy" and it is indispensable to have successfully passed the exam of "Organic Chemistry"
Teaching methods
Lectures supported by PowerPoint presentations
Other information
There are 8 hours of teaching support, organized into classroom activities each one of 2-3 hours, that will take place during and in part at the end of the course to prepare for the final exam. The support teaching activities are: revision and evaluation tests of the principal aspects of the main classes of drugs covered in the course.
Learning verification modality
The exam consists of an oral test of about 30-40 min. The oral test is designed to assess the level of knowledge attained by the student on the theoretical contents covered in the program, his/her logical reasoning, the ability to communicate appropriately organizing ideas and concepts logically and coherently.
The evaluation is a minimum of 18 and a maximum of 30 with the possibility of honours.
Extended program
Pharmaceutical industry. Historical development of drugs. Drug nomenclature. ATC classification. WHO and list of essential drugs.
CHEMOTHERAPEUTIC AGENTS
Strategy in chemotherapy, host-parasite relationships. Drug resistance.
History, chemical aspects/general properties, mechanism of action, structure-activity relationships (SAR), spectrum of action, therapeutic use, adverse reactions and general synthetic methods of the following classes of chemotherapeutic agents.
ANTIBACTERIALS
- Inhibitors of metabolic processes: Sulfonamides. Trimetoprim. Nitrofurans and nonbenzenoid nitro derivatives.
- Inhibitors of bacterial cell wall biosyntheis: ß-lactam antibiotics. (penicillins, cephalosporins, oxacefems, carbapenems, monobactams and ß-lactamase inhibitors). Cycloserine. Bacitracin. Vancomycin and teicoplanin.
- Antibacterials interfering with functionality of cytoplasmic membrane: polymyxins and tyrothricin.
- Inhibitors of protein biosyntheis: Tetracyclines. Aminoglycosides. Macrolides. Chloramphenicol.
- Antibacterials interfering with functionality of nucleic acids: Quinolones. Oxazolidinones.
ANTIMYCOBACTERIALS
- Antituberculosis first-line and secon-line agents.
- Antileprosy agents: hints.
ANTIPROTOZOAL DRUGS
- Antimalrials (antimalarial drugs): Quinine and its synthetic derivatives. 4-Aminoquinolines. 8-Aminoquinolines. Acridines. Dihidrofolate reductase inhibitors. Artemisinin and its derivatives. Combination drug therapy.
- Other antiprotozoals against trypanosomiasis, leishmaniasis and tricomoniasis
ANTIFUNGAL DRUGS - Allylamines. Morfpholines. Flucytosine. Azoles. Griseofulvin. Polyenes, Echinocandins.
ANTICANCER DRUGS
- Alkylating agents: Nitogen mustards. Aziridines. Mitomycin C. Methanesulfonates. Procarbazine and dacarbazine. Nitrosoureas. Pt-complexes.
- Antimetabolites: Aminoacid antagonists. Folic acid antagonists. Purine and pyrimidine antagonists.
- Antimtotics: Vinca alkaloids. Taxanes.
- Antibiotics: Anthracyclines. Dactinomycin. Bleomycins. (Mitomycin C)
- Miscellaneus: Etoposide and teniposide. Champtothecins. Hydroxyurea. Asparaginase. Imantinib.
Angiogenesis and cancer.
ANTIVIRAL DRUGS - Amantadine. Interferon and interferon inductors. Purine and pyrimidine antagonists. Anti-HIV agents: Co-receptor inhibitors. Fusion inhibitors. Nucleoside and non-nucleoside RT inhibitors. Integrase inhibitors. Protease inhibitors. Combination drug therapy.

CARDIOVASCULAR DRUGS
History, chemical aspects/general properties, mechanism of action, structure-activity relationships (SAR), therapeutic use, adverse reactions and general synthetic methods of the following classes of drugs.
CARDIOTONIC AGENTS - Cardiac glycosides. Non-glycoside drugs.
ANTIARRHYTHMIC DRUGS - Na-channel blockers. ß-Adrenoceptor blocking agents. K-channel blockers. Ca-channel blockers.
ANTIANGINAL DRUGS - Organic nitrates. (ß-Adrenoceptor blockers. Ca-channel blockers).
ANTIHYPERTENSIVES
- Antiadrenergic agents: Clonidine, a-methyldopa, guanetidine. a-Adrenoceptor blocking agents. ß-Adrenoceptor blocking agents.
- Ca-channel blockers: Arylalkylamines. Benzothiazepines. Dihydropyridines.
- K-channel openers.
- Drugs acting on renin-angiotensin system: Renin inhibitors. Angiotensin-converting enzyme inhibitors. AT1-antagonists.

DIURETICS - Osmotic diuretics. Carbonic anhydrase inhibitors. Thiazides and analogs. High-ceiling diuretics (aminobenzoic acid derivatives and fenoxyacetic acid derivatives). Potassium-sparing diuretics.

ANTITHROMBOTICS – Oral anticoagulants (cumarin derivatives), heparin and its forms, direct thrombin inhibitors, inhibitors of Xa. Antiplatelet drugs.

ANTIHYPERLIPOPROTEINEMICS and INHIBITORS OF CHOLESTEROL BIOSYNTHESIS – Inibitori HMG CoA reductase inhibitors, fibrates, bile acid sequestrants, ezetimibe, nicotic acid.


ANTI-INFLAMMATORY DRUGS
History, chemical aspects/general properties, mechanism of action, structure-activity relationships (SAR), therapeutic use, adverse reactions and general synthetic methods of the following classes of drugs.
Steroidal anti-inflammatory drugs - Natural and semisynthetic glucocorticoides.
Nonsteroidal anti-inflammatory drugs (NSAID) - Salicylates. Aniline derivatives. Fenamic acids. Arylalkanoic acids. Oxicams. COX-2 inhibitors.
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