AIMS AND CONTENT

LEARNING OUTCOMES

Learning outcomes will be a basic knowledge of: i) drug pharmacokinetic: absorption and distribution of drug; drug metabolism and excretion); ii) general pharmacodynamics: main targets and mechanisms of drug action; dose-response curves for agonists and antagonists; biochemical and physiological drug effects and their molecular mechanisms; iii) main factors of variability in the individual response and side-effects, drug safety and mechanisms of drug-drug interferences. The mechanisms of action, pharmacokinetic aspects and side effects of some drug classes will be described.

AIMS AND LEARNING OUTCOMES

Aims. The course aims to provide basic knowledge of drug mechanisms of action underlying clinical applications (pharmacodynamics) and a general understanding of pharmacokinetic properties and drug safety evaluation, so that students acquire knowledge of General Pharmacology and understand response variability. The Professor also aims to develop basic functional literacy and basic personal and social skills.

 Learning outcomes. As learning outcomes, students must demonstrate knowledge of the meaning of drug, pharmacological target, and drug-related effects; they must recall the mechanisms of drug action, routes of administration, and the elements of pharmacokinetics and variability in drug response. Students must also be able to draw and obtain information from dose–response curves (for agonists, partial agonists, and antagonists) and kinetic curves, and apply the general concepts of pharmacodynamics and pharmacokinetics to molecules belonging to specific drug classes.

TEACHING METHODS

Teaching will consist of lectures with in-depth exploration of the syllabus. Through icebreaker activities, specific topics will be introduced and may also be addressed through peer education and peer evaluation to promote active learning and the ability to communicate effectively in oral form using appropriate terminology. These activities may be carried out in pairs, in groups, or individually, and may require a final presentation to the class on the topic addressed, followed by feedback from the Professor, classmates, and class discussion.

To enable students to use data from toxicological and pharmacological tests to evaluate drug safety, classroom exercises will be conducted using data available in the literature. To improve the ability to analyse and describe dose–response relationships and the differing behaviour of agonists, partial agonists, and antagonists, exercises will be proposed several times during the course, considering targets and pharmacologically active molecules already discussed in previous lectures. Attendance is recommended to support achievement of the learning outcomes.

SYLLABUS/CONTENT

INTRODUCTION

Definition of active substances (drug, medicinal product or pharmaceutical formulation, equivalent drugs). Disciplines that study drugs: general pharmacology, cellular and molecular pharmacology, pharmacognosy, clinical pharmacology, pharmacoeconomics, pharmacogenetics, pharmacogenomics, pharmacovigilance, chemotherapy, toxicology. Discovery and development of new drugs. Generics, biotechnological drugs, and orphan drugs

PHARMACODYNAMICS

Interaction between drug and living organism: definitions of biological target (receptor and non-receptor mechanisms), affinity, competition, agonist, antagonist, allosteric agonists or antagonists, partial agonist, inverse agonist.

Pharmacological targets:

A) Receptors and modulation of their responses. Classes of receptors and their signal transduction systems: intracellular/intranuclear receptors; membrane receptors (ligand-gated ion channels, G protein-coupled receptors); receptor transport and cellular trafficking; modulation of receptor responses (desensitization and sensitization); modulation of drug-induced receptor responses. Ligand-gated ion channels: classification; molecular organization and ion channel structure; binding sites for endogenous agonists and pharmacological modulation. Examples. G protein-coupled receptors: molecular organization of receptors and G proteins; effector systems (e.g., adenylate cyclase, phospholipase C) and second messenger cascades. Examples.

B) Voltage-dependent ion channels: molecules with pharmacological action on sodium and calcium channels.

C) Membrane and vesicular transporters: examples include amphetamines and cocaine.

D) Enzymes: acetylcholinesterase, COX.

QUANTITATIVE PHARMACOLOGY

Qualitative and quantitative aspects of drug–receptor interaction; characteristics of drug–receptor binding, concept of affinity; dose–effect relationship; intrinsic activity: agonists, partial agonists; competitive and non-competitive antagonists.

PHARMACOKINETICS

A) Drug absorption and routes of administration: enteral routes (oral, sublingual, rectal); systemic parenteral routes (intravascular, intramuscular, cutaneous); other routes (inhalational, topical-regional applications, intracavitary, dermal or transcutaneous). Modes of membrane passage and parameters (partition coefficient, drug solubility, extent and permeability of absorptive surface, vascularization).

B) Drug distribution and elimination: apparent volume of distribution; drug–plasma protein binding, free and bound fractions; factors influencing distribution.

C) Drug metabolism. Phase I enzymatic reactions: oxidation and cytochrome P450; reductions; hydrolysis. Phase II enzymatic reactions: glucuronidation, sulfation, methylation, acetylation, conjugation with amino acids and glutathione.

D) Renal excretion; hepatic excretion and enterohepatic circulation. Half-life, clearance.

VARIABILITY IN DRUG RESPONSE

Allergy, tolerance, sensitization, dependence, metabolic induction and inhibition, age, and gender.

ELEMENTS OF SPECIAL PHARMACOLOGY

General anaesthetics; anti-inflammatory drugs; anti-ulcer drugs.

SPECIAL PHARMACOLOGY

General anaesthetics; anti-inflammatory drugs; anti-ulcer drugs.

ELEMENTS OF TOXICOLOGY

Toxicological tests, acute and chronic toxicity. Drug safety.

RECOMMENDED READING/BIBLIOGRAPHY

• Golan DE et al – Principi di farmacologia – Casa Editrice Ambrosiana
• Goodman & Gilmans – Le basi farmacologiche della terapia – McGraw-Hill
• Govoni et al –  Farmacologia –  CEA (seconda edizione 2023)
• Rang HP et al –   Farmacologia –  Elsevier-Masson S.r.l. (sesta edizione - 2008)

• Lecture notes
• Copies of the iconography used in lectures, downloadable from AulaWeb

TEACHERS AND EXAM BOARD

Exam Board

MARINA POZZOLINI (President)

EMANUELE BOSI

CHIARA CERVETTO (President Substitute)

LESSONS

LESSONS START

Please consult the detailed timetable on the UNIGE portal and at https://easyacademy.unige.it/portalestudenti/

Please also refer to the specific AulaWeb page of the course for any updates.

Class schedule

PHARMACOLOGY

EXAMS

EXAM DESCRIPTION

Assessment of students’ achievement of the stated objectives will take place through an oral examination lasting approximately 30 minutes. The maximum mark achievable for the Pharmacology module is 30/30 (with honours - lode). The mark contributes to the final grade of the integrated course according to the specific CFUs (credits) of the module.

An optional written test is planned during the course

ASSESSMENT METHODS

The appointed committee is able to verify with high accuracy the achievement of the learning objectives of the module by asking varied questions concerning the programme actually covered during lectures.

Regarding assessment of pharmacokinetics learning outcomes, students must demonstrate knowledge of the kinetic properties (time–action) of drugs, also considering routes of administration and the different phases: absorption, distribution, metabolism, and excretion. Regarding assessment of mechanistic aspects, students must demonstrate knowledge of molecular targets and the effects resulting from their interaction with the xenobiotic.

For the final evaluation, the committee will assess: level of knowledge of the topics addressed by the questions; presentation skills; capacity for reasoning and making connections with other topics in the course syllabus. If the learning objectives are not achieved, the student will be invited to further review their knowledge and, if necessary, seek additional explanations by contacting the course professor.

FURTHER INFORMATION

Attendance is recommended.

Students with a physical disability or learning disability certificate filed with the University can find information on support services on the UNIGE disability and DSA page. They may also contact Professor Cristina Carbone (cristina.carbone@unige.it), DISTAV contact person for disability support.

Students are invited to contact the professor for further information.