PHARMACEUTICAL AND TOXICOLOGICAL CHEMISTRY I
Learning outcomes of the course unit
This course provides an introduction to Medicinal Chemistry and is integrated with the Medicinal Chemistry courses delivered in the following years.
The course aims at providing the students with the knowledge and the understanding of the basic chemical and toxicological aspects of drugs, to apply them to the study and the analysis of the different classes of drugs. Moreover, the knowledge and the methodology of study acquired allow the student to describe and discuss, with proper language, the most relevant aspects and problems related to the topics treated during the course.
Besides the knowledge about the general aspects of drug action, the student will learn about the most important drugs for the therapeutic classes treated, such as their name, mechanism of action, therapeutic application, metabolic fate and toxicity.
Basic groundings of Organic Chemistry and Physiology
Course contents summary
The first lessons treat general topics on drugs, such as names of drugs, structural, chemical and physicochemical properties of drugs which influence their action. The most important mechanisms of actions are also discussed, as well as an introduction to structure-activity relationships is made. This general part of the course also treats drug absorption, distribution, metabolism and excretion, with particular emphasis on metabolic reactions. Prodrug strategies will also be discussed, with examples of activation mechanisms.
The second part of the course describes the most relevant classes of antibacterial, antiprotozoal, antifungal, anthelmintic, antiviral and anticancer classes of drugs. For each class the chemical formula of the most important drugs are described, as well as the most relevant information about their mechanism of action, structure activity relationships, chemical and physicochemical properties, metabolic reactions and toxicity.
Names and classification of drugs
Origin of drugs
Moments of drug action: the pharmaceutical, pharmacodynamic and pharmacokinetic phases.
Drug targets: membranes, receptors, enzymes, nucleic acids.
Mechanisms of action of drugs
Structure and action of drugs
Chemical and physicochemical properties influencing drug action
Isosteres and bioisosteres
Antibacterial agents: sulfa-drugs, beta-lactams, quinolones, aminoglycosides, tetracyclines, macrolides, oxazolidinones; other antibacterial drugs.
Antiprotozoal drugs: nitro-heterocyclic drugs, antimalarial drugs; other antiprotozoal agents.
Antifungal drugs: azoles, allylamines, polyenic drugs, other antifungal agents.
Insecticides: pyrethrum and derivatives
Antiviral drugs: anti-herpetic, anti-HIV, anti-flu, drugs for hepatitis B and C; other antiviral agents.
Anticancer drugs: alkylating agents, intercalating agents, antimetabolites, antimitotics, DNA-polymerase and topoisomerase inhibitors, tyrosin kinase inhibitors; other anticancer agents.
Thomas L. Lemke, David A. Williams, Victoria F. Roche, S. William Zito: Foye’s Principi di Chimica Farmaceutica, sesta edizione italiana; Piccin, Padova, 2013.
John M. Beale, Jr., John H. Block: Wilson & Gisvold Chimica Farmaceutica; Casa Editrice Ambrosiana, Milano, 2014.
Alberto Gasco, Fulvio Gualtieri, Carlo Melchiorre: Chimica Farmaceutica; Casa Editrice Ambrosiana, Milano, 2015.
G. L. Patrick: Introduzione alla chimica farmaceutica, seconda edizione; Edises Napoli, 2010.
Teacher-led lessons with slides.
Assessment methods and criteria
The oral examination will be preceded by a written questionnaire (usually 5 questions) about the most important aspects of the topics treated during the course. If the answers to the questionnaire will be evaluated as sufficient (usually 3 correct answers), the student will sustain the oral part of the examination. In the oral examination, the answers to questions related to all the topics treated during the course will be used to assess the knowledge and the comprehension of the contents of the course achieved by the student. The ability of the student to apply the acquired knowledge will be also evaluated through connections among topics.