Ateneo - UPO

The course focuses on the description of the biological basis of infectious diseases, which underpins the use of the main classes of antimicrobial drugs; these will also be addressed from the perspective of chemical synthesis.
The types covered will be:
1. Antiprotozoals;
2. Antibacterials;
3. Antivirals;
4. Antifungals.

For the Pharmacology module:
Govoni S, Spampinato SM, Navarra P, et al. - Farmacologia, Casa Editrice Ambrosiana, Second Ed. (2023); F. Rossi, V. Cuomo, C. Riccardi – Farmacologia, Edizioni Minerva Medica, last ed; B.G. Katzung, S.B. Master, A.J. Trevor – Farmacologia Generale e Clinica, Piccin, last ed; Goodman & Gilman – Le Basi Farmacologiche della Terapia. Il manuale, Zanichelli, last ed; H.P. Rang, M.M. Dale, J.M. Ritter, Farmacologia, Casa Editrice Ambrosiana, last edition
For the Chemistry module:
G. Costantino, G. Sbardella, Chimica Farmaceutica, EdiSES
A. Gasco, F. Gualtieri, C. Melchiorre Chimica Farmaceutica Casa Editrice Ambrosiana;
W. Foye, Principi di Chimica Farmaceutica, Piccin;
E. Stevens, Medicinal Chemistry: The Modern Drug Discovery Process, Pearson.

The course aims to introduce students to the main drugs used in antimicrobial therapy.The specific objectives of the course as a whole, classified according to the Dublin Descriptors, are as follows:
1. Knowledge and understanding: To provide knowledge on the fundamental aspects of the pharmacokinetic, pharmacodynamic, and clinical profiles of the molecules used in the therapy of infectious diseases, and to provide the critical tools for understanding therapeutic choices.
2. Applying knowledge and understanding: For both the specifically covered drugs and analogous compounds, the student will be able to apply the acquired knowledge and understanding to recognize structures and discuss their chemical, physicochemical, and pharmacological properties. They will also be able to discuss their mechanism of action, structure-activity relationships, metabolic properties, and propose potential synthetic routes for their production.
3. Making judgements: Management of the acquired knowledge for the purpose of making judgements regarding therapeutic choices, structure-activity relationships, metabolism and related toxicity, production, and drug-drug interactions. Furthermore, students will be provided with the necessary tools to apply these skills to the critical evaluation of texts and articles in medicinal chemistry and pharmacology.
4. Communication skills: Ability to communicate and illustrate, in an original manner, a topic covered during lectures, and to respond appropriately to questions, criticisms, and suggestions.
5. Learning skills: Ability to learn and to manage, in a dynamic and as autonomous as possible manner, one's own body of knowledge on the chemistry and pharmacology of antimicrobials.

None. It is strongly suggested that the student has already positively performed the following courses: BIologi, Biochemistry, Physiology, Pathology, General Pharmacology, Microbiology, Anatomy

The course is given with the support of slides, which are given to the students at the beginning of the lessons.
General and specific topics will be introduced, basic concepts will be provided for the understanding of each issue, and discussions with the students will be held. It will be explained how to acquire the competences needed to predict the chemical and physico-chemical properties of drugs starting from their structures, to identify the structural elements necessary for their mechanism of action and to recognize alert groups that can lead to toxicological problems. At the end of each module practical exercises will be solved in order to prepare the students to the exam. It will stimulate the active participation of the student through the recall of concepts already addressed in other courses, which relate to various aspects of the drug and the disease.

Within the same exam session, students may retake the examination only if at least three weeks have elapsed since their previous unsuccessful attempt.
Students with physical disabilities, Learning Disabilities or Special Education Needs can request specific services and tools via the Staff Sviluppo e Coordinamento Carriere e Servizi alle Studentesse e agli Studenti, consulting the University webpage: https://www.uniupo.it/en/services/services-students-physical-or-learning-disabilities Students with disabilities, learning disabilities or special education needs, once they have contacted the University Staff, can refer to the tutor in charge of the course to define the examination modalities, concerning academic aspects.

For the Pharmacology module, an oral examination will be held.
Oral examination is performed by asking to the student some questions related to topics indicated in the course programme and given during the specific classes. To obtain positive results, the student must show a sufficient level of knowledge and of associative capabilities related to the different arguments; he/she must show that he understood and knows the critical concepts of the various topics. Greater levels of knowledge together with a demontrated capability of application of this background to the practice leads to an evalutation superior to that required for the minimal score. To obtain a high level of evaluation the student has to be able to utilize his/her knowledge to debate deeply some of the critical aspects of the different topics.
For the Chemistry module, the exam consists of a written test.The questions will aim to assess both the knowledge of the course content and the ability to apply this content to antimicrobial drugs. This will include recognizing the structure of a drug, identifying functional groups, acidic, basic, or stereogenic centers within that structure, metabolic reactions, synthetic routes for preparation, etc.Through these assessments, it will be verified that the student has achieved the objectives of knowledge and understanding of the content, the ability to present it clearly and correctly, and the capacity to apply the acquired knowledge and skills to specific problems regarding the chemical-pharmaceutical aspects of the drug classes covered."Ed ecco la versione in italiano leggermente revisionata nello stile per allinearsi perfettamente alla fluidità di quella inglese (e correggendo il refuso obbiettivi in obiettivi):"Per il modulo di Chimica, l'esame consiste in una prova scritta.Le domande mireranno ad accertare sia la preparazione in merito ai contenuti del corso, sia la capacità di applicare tali contenuti ai farmaci antimicrobici, prevedendo il riconoscimento della struttura di un farmaco, l'identificazione in tale struttura di gruppi funzionali, centri acidi, basici o stereogenici, le reazioni metaboliche, le vie di sintesi per la preparazione, etc.Attraverso tali verifiche, verrà accertato che lo studente abbia raggiunto gli obiettivi di conoscenza e comprensione dei contenuti, la capacità di esporli in modo chiaro e corretto, e la capacità di applicare le conoscenze e competenze acquisite a problemi specifici riguardanti gli aspetti chimico-farmaceutici delle classi di farmaci trattate.

General principles of antimicrobial therapy regarding drug selection based on pharmacokinetic/pharmacodynamic (PK/PD) profiles, host-dependent factors, and the biological characteristics of the pathogen. Bactericidal versus bacteriostatic agents; concentration-dependent versus time-dependent therapeutic efficacy. Mechanisms of drug resistance and associated clinical challenges.Antibacterial AgentsCell Wall Synthesis Inhibitors:Beta-lactams: Penicillins, Cephalosporins (1st to 5th generation), Monobactams (Aztreonam), and Carbapenems (Imipenem, Meropenem).Glycopeptides & Lipoglycopeptides: Vancomycin, Teicoplanina, Dalbavancin.Fosfomycin.Cyclic Lipopeptides: Daptomycin (specifically targeting resistant Gram-positive pathogens).BacitracinProtein Synthesis Inhibitors (Ribosomal Targets):Aminoglycosides (30S subunit inhibitors): Gentamicin, Amikacin, Tobramycin.Tetracyclines & Glycylcyclines (30S subunit inhibitors): Doxycycline, Minocycline, Tigecycline.Macrolides & Ketolides (50S subunit inhibitors): Azithromycin, Clarithromycin, Telithromycin.Lincosamides: Clindamycin.Oxazolidinones: Linezolid, Tedizolid (critical for Methicillin-Resistant Staphylococcus aureus - MRSA).Nucleic Acid Synthesis Inhibitors:Fluoroquinolones (DNA gyrase & Topoisomerase IV inhibitors): Ciprofloxacin, Levofloxacina, Moxifloxacin.Rifamycins (RNA polymerase inhibitors): Rifampicin (cornerstone of anti-tuberculosis therapy).Nitroimidazoles: Metronidazole (targeting anaerobic bacteria and protozoa).Antimetabolites (Antifolates):Sulfonamides & Dihydrofolate Reductase Inhibitors: Co-trimoxazole (Sulfamethoxazole/Trimethoprim).Cell Membrane Disruptors:Polymyxins: Colistin (Polymyxin E) and Polymyxin B (utilized as last-line therapy for pan-drug-resistant Gram-negative bacteria).Antifungal AgentsAzoles: Topical Imidazoles (Ketoconazole, Clotrimazole) and Systemic Triazoles (Fluconazole, Voriconazole, Posaconazole, Isavuconazole).Polyenes: Amphotericin B (including liposomal formulations) and Nystatin.Echinocandins (Glucan synthesis inhibitors): Caspofungin, Micafungin, Anidulafungin.Allylamines: Terbinafine.Antimetabolites: Flucytosine.Antiviral AgentsAnti-Herpesvirus Agents: Acyclovir, Valacyclovir, Ganciclovir, Foscarnet.Anti-Influenza Agents: Neuraminidase inhibitors (Oseltamivir, Zanamivir) and Endonuclease inhibitors (Baloxavir marboxil).Antiretroviral Therapy (ART for HIV):NRTIs & NNRTIs (Nucleoside/Non-Nucleoside Reverse Transcriptase Inhibitors).Protease Inhibitors (PIs) and Integrase Strand Transfer Inhibitors (INSTIs).Direct-Acting Antivirals (DAAs) for HCV: NS3/4A, NS5A, and NS5B inhibitors (e.g., Sofosbuvir, Glecaprevir/Pibrentasvir).Anti-SARS-CoV-2 Agents: Nirmatrelvir/Ritonavir, Remdesivir.Antiparasitic AgentsAntimalarials: Chloroquine, Artemisinina derivatives, Atovaquone/Proguanil.Antihelminthics: Albendazole, Mebendazole, Ivermectin, Praziquantel.

Ideally, at the end of the course, the student is able to recognize the structure of the main antimicrobial drugs and to discuss their medicinal chemistry properties. Moreover She/he has to know the pharmaco-therapeutical approach to the different pathologies, and be able to give advice to patients and to develop control capabilities. Finally, he/she should have enough skills to follow the continuous evolution of pharmacology and pharmacotherapy.