Pharmaceutical Chemistry - CHEMICAL-TOXICOLOGICAL ANALYSIS OF OFFICINAL PLANTS AND NUTRACEUTICAL PRODUCTS
Module Pharmaceutical Chemistry

Academic Year 2023/2024 - Teacher: Loredana SALERNO

Expected Learning Outcomes

Knowledge and understanding
The course aims to provide students with the tools to study the fundamental concepts that characterize Pharmaceutical Chemistry

Applying knowledge and understanding
The student acquires knowledge of the strategies used for the discovery and design of new active ingredients, of the steps necessary for the development of these drugs and for their development as medicaments. In addition, he will have knowledge of the moments of the action of the drugs, from administration to elimination and of the conditioning properties of the drug-two-phase interaction. The student will have knowledge of selected classes of drugs and will understand how they interact with neurotransmitter receptors, with intracellular receptors, with enzymes and with ion channels, deepening their mechanisms of action, chemical-pharmaceutical and toxicological properties, and structure-activity relationships

EXPECTED LEARNING RESULTS
The student will know and understand the issues related to the design, the mechanism of action at the molecular level, drug-receptor interactions, toxicity, metabolism and structure-activity relationships of the classes of drugs examined, in particular those of origin natural

Course Structure

The course will be held mainly through lectures. During the lessons the student will be asked to actively participate in the discussion on the topics presented and in particular in case studies. Classroom exercises on exam methods will be proposed during the course.

Should teaching be carried out in mixed mode or remotely, it may be necessary to introduce changes with respect to previous statements, in line with the programme planned and outlined in the syllabus.

Learning assessment may also be carried out on line, should the conditions require it.

Detailed Course Content

GENERAL PART
Definition and objectives of Pharmaceutical Chemistry, history and evolution. Discovery of drugs from natural products. Definition of drug. Different ways to classify drugs. ATC classification of drugs. Nomenclature of drugs. Stages of drug action: pharmaceutical, pharmacokinetics, pharmacodynamics. Pharmacokinetics: absorption, metabolism (phase I and phase II), distribution and elimination of a drug. Pharmacodynamics: Drug targets. Molecular drug-target interaction: description of the different chemical bonds involved in the interaction. Receptors: G protein coupled receptors, receptors with intrinsic enzymatic activity, ion channels ligand-gated and voltage-gated. Enzymes and enzymatic inhibition, competitive and non-competitive inhibitors. Nucleic acids. Lipids. Carbohydrates. Discovery, design and development of drugs. Optimization of interaction with the target. Optimization of target access. Prodrugs and Softdrugs. The introduction of drugs on the market.
SYSTEMATIC PART
Examples of drugs derived from natural substances (the following examples will be integrated in class).
OPIOID ANALGESICS. Introduction. Morphine: structure and properties, structure-activity relationships. Opioid receptors, development of morphine analogues, agonists, antagonists.
ANTICANCER. General information on neoplastic diseases and therapeutic approaches, classification of anticancer drugs. Plant-based anticancer drugs

Textbook Information

1. G.L. PATRICK, Chimica Farmaceutica, III Edizione italiana, EdiSES, Napoli, 2015

2. T.L. LEMKE et al., Foye's L'essenziale, Principi di Chimica Farmaceutica, I Edizione italiana, Piccin,

Padova, 2017.

3. R.B. Silverman, M.W. Holladay., Manuale di chimica farmaceutica, progettazione, meccanismo d'azione e metabolismo dei farmaci. Edra

3. Slides of the lessons