SCIENZE DEL FARMACO E DELLA SALUTEApplied Pharmaceutical SciencesAcademic Year 2022/2023
1008630 - CHIMICA FARMACEUTICA - ANALISI CHIMICO-TOSSICOLOGICA DELLE PIANTE OFFCINALI E DEI PRODOTTI NUTRACEUTICI
Module 1008631 - CHIMICA FARMACEUTICA
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
Versione in italiano