OBIETTIVI FORMATIVI

The aim of this course is to provide the students with knowledge about fundamental concepts of the main pharmacological classes, the basic concepts of pharmacokinetics and pharmacodynamics, correlated to the study and the development of new drugs, and the methodologies of pharmacological experimentation. The course will be focused to study cellular molecular mechanisms of the action of drugs, deepening their receptorial mechanisms and signal transduction. Moreover, the course will underline the progresses, obtained using new technologies, molecular biology and biotechnology, towards the investigation of innovative pharmaceuticals molecules and the finding of new therapeutic targets.

OBIETTIVI FORMATIVI (DETTAGLIO) E RISULTATI DI APPRENDIMENTO

Al termine del corso lo studente dovrà conoscere:

I principali principi che regolano la farmacocinetica ed i parametri che ne consentono la valutazione

I principali principi della farmacodinamica e le caratteristiche dell'interazione farmaco-bersaglio molecolare

Il funzionamento dei principali sistemi di trasduzione del segnale e la loro modulazione farmacologica

Le caratteristiche delle principali classi farmacologiche 

MODALITA' DIDATTICHE

L'insegnamento di farmacologia si compone di 5 CFU suddivisi in 32 ore di lezioni frontali e 16 di laboratorio. In base al regolamento didattico la frequenza è obbligatoria. Le attività di laboratorio verranno svolte dividendo gli studenti in piccoli  guppi per favorire la partecipazione individuale dei singoli studenti.

L'attività di laboratorio sarà tenuta da docenti collaboratori alla didattica. Le attività di laboratorio saranno precedute da un'introduzione teorica su quello che si andrà svolgere e verteranno sull'usodi tecniche di base ed innovative nell'ambito della ricerca farmacologica. 

PROGRAMMA/CONTENUTO

1) GENERAL PHARMACOLOGY 

 Introduction to pharmacology and its sub-branches, definition of drug and toxic agent, active component and excipient. Cell diversity as main target of the action of the drugs. Drug development and drug repositioning. Pharmacognosy

2) PHARMACOKINETICS

1) Different routes of drug administration, absorption of drugs and the conditions that may modulate it, bioavailability and bioequivalence. Drug distribution and redistribution

2) Drug metabolism: phase 1 e phase 2 enzymes. Drug excretion and its modulation, individual factors that may modify the responses to the drugs

3) MECHANISM OF ACTION OF THE DRUGS

1) DRUG-RECEPTOR INTERACTION 

Qualitative and quantitative characteristics – gradual and quantal responses, the concept of receptor affinity, Bmax, intrinsic activity, efficacy, and potency - techniques to measure receptor density, saturation curves, Scatchard analysis to determine Bmax and Kd, concentration-effect curves, up e down-regulation – agonism e antagonism – structure-activity relationship – biased agonism therapeutic index)

2) DRUG EFFECTS 

Receptor- and non-receptor-mediated mechanisms. Different receptor classes. ADRs,

Pharmacoallergy, idiosyncrasy, tolerance, dependence, pharmacogenetics, pharmacogenomics.

4) DRUG MOLECULAR TARGETS

1. G protein-coupled receptors, mechanisms of activation and signal transduction pathways; pharmacological modulation
2. Ion channels and ionotropic receptors; pharmacological modulation
3. Growth factor receptors endowed with intrinsic tyrosine kinase activity, signal transduction pathways; pharmacological modulation
4. Intracellular receptors, signal transduction pathways; pharmacological modulation
5. Ionic pumps and transporters; pharmacological modulation
6. Pharmacological modulation of the enzyme activity
7. Molecular targets of the neurotransmission and their pharmacological modulation: the noradrenergic/adrenergic neurotransmission
8. Molecular targets of the neurotransmission and their pharmacological modulation: the cholinergic neurotransmission
9. Pharmacological control of cell proliferation
10. Pharmacological control of inflammation: NSAIDs and glucocorticoids

TESTI/BIBLIOGRAFIA

Si raccomanda l'uso del testo:

Farmacologia generale e molecolare, di Francesco Clementi e Guido Fumagalli.  Edra Edizioni, 2018

In aggiunta tutto il materiale utilizzato durante le lezioni frontali sara fornito agli studenti tramite Aulaweb, in anticipo rispetto alla lezione.