PHARMACEUTICAL CHEMISTRY and TOXICOLOGY II

Academic Year 2024/2025 - Teacher: LOREDANA SALERNO

Expected Learning Outcomes

The education goal of the course is to provide students with the tools to study the fundamental concepts that characterize Medicinal and Toxicological Chemistry. Selected classes of drugs that interact with neurotransmitter receptors, with intracellular receptors, with enzymes and with ionic channels will be examined, investigating their mechanisms of action and chemical-pharmaceutical properties.

The intended training objective is to provide the student with the skills necessary to understand the problems related to the design, the mechanism of action at the molecular level, the drug-receptor interactions, the toxicity, and the structure-activity relationships of the classes of drugs taken in exam

Course Structure

The course will be carried out mainly by means of frontal lessons. During class lectures, all the subjects are presented in details. Students are asked to actively discuss about them and about a number of case studies.

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.

Information for students with disabilities and/or DSA.

To ensure equal opportunities and in compliance with current laws, interested students may request a personal interview in order to plan any compensatory and/or dispensatory measures, based on the educational objectives and specific needs. You can also contact the CInAP (Centre for Active and Participated Integration - Services for Disabilities and/or DSA) contact teacher of our Department, prof.Santina Chiechio

Required Prerequisites

A correct understanding of the topics developed in the Course requires preliminary knowledge of General Chemistry, ORGANIC CHEMISTRY, Biological Chemistry, Anatomy, Physiology, Pathology, Pharmacology and Pharmaceutics I

Attendance of Lessons

The course includes lectures for 63 hours (9 CFU) and classroom exercises for 12 hours (1 CFU). Classroom attendance, as per the teaching regulations, is mandatory for at least 70% of the course lessons assessed in all their forms of completion. If the teaching is taught in mixed mode or remotely, the necessary changes may be introduced with respect to what was previously declared, in order to respect the planned program and reported in the syllabus.

Detailed Course Content

Drugs acting on the cholinergic system

Drugs acting on the adrenergic system

Drugs acting on histaminergic receptors. Antiallergic and antigastrolesive drugs

Non-steroidal anti-inflammatory drugs (NSAID)

Drugs for Parkinson's therapy

Anxiolytic drugs

Antipsychotic drugs

Antidepressant drugs

Opioid analgesics

Antihypertensive drugs

Other

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. A. GASCO, F. GUALTIERI, C. MELCHIORRE, Chimica Farmaceutica, CEA, Milano, 2015

4. D.A. WILLIAMS, T.L. LEMKE, Foye's Principi di Chimica Farmaceutica, VI Edizione italiana, Piccin, Padova, 2014.

5. Slides presented during classes

Course Planning

 SubjectsText References
1Agenti attivi sul sistema colinergico1,2,3
2Agenti attivi sul sistema adrenergico1,2,3
3Agenti attivi sui recettori istaminergici. Farmaci antiallergici e antigastrolesivi1,2,3
4Farmaci antinfiammatori non steroidei1 e 2
5Farmaci per la terapia del Parkinson1 e 2
6Farmaci ansiolitici1 e 2
7Farmaci antipsicotici1 e 2
8Farmaci antidepressivi1 e 2
9Analgesici oppioidi1 e 2
10Farmaci antipertensivi1,2,3

Learning Assessment

Learning Assessment Procedures

The learning assessment consists of a written test including multiple choice questions and open-ended questions. The former will be given a fixed grade, the latter a variable grade based on the level of depth. The wrong answer will be given a negative grade. The test is designed to assess the level of knowledge of the basic concepts of Pharmaceutical Chemistry, of the fundamental aspects concerning the design, synthesis, mechanisms of action at the molecular level and the structure-activity relationships (SAR) of the drug classes illustrated during the course. During the course, some classroom exercises will be proposed set up with the same modality as the exam. It is not permitted to consult texts or use PCs, smartphones. The learning assessment may also be carried out electronically, if conditions require it. Information for students with disabilities and/or DSA: To ensure equal opportunities and in compliance with current laws, interested students may request a personal interview in order to plan any compensatory and/or dispensatory measures, based on the educational objectives and specific needs. You can also contact the CInAP (Centre for Active and Participated Integration - Services for Disabilities and/or DSA) contact teacher of our Department.

Examples of frequently asked questions and / or exercises

Multiple choice question examples.

Example 1 Activation of M2 and M4 cholinergic receptors causes:

activation of adenylate cyclase 

inhibition of adenylate cyclase 

opening of an ion channel of a channel receptor

none of these

 Example 2 One of the following statements about H2 antihistamines is false

They are highly hydrophilic substances 

They are substances with a low partition coefficient 

They are substances with a high dipole moment 

They are always ionized on the basic group of the side chain

Open-ended question examples. 

Example 1 Describe the SARs of adrenergic agonists. Example 2 Write the structural formula of Naloxone. Example 3 Describe the synthesis of Diazepam