LEARNING OUTCOMES

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.

AIMS AND LEARNING OUTCOMES

At the end of the course, the student will know:

The principles at the basis of pharmacokinetics, and the parameters used for their evaluation

The principles at the basis of pharmacodynamics and the molecular bases of the interactions between drugs and molecular targets

The bases of the functioning of the main intracellular transduction systems and their pharmacological modulation

The features of the main classes of drugs

TEACHING METHODS

Pharmacology course will comprise 5 CFU, organized as 32 hours of frontal teaching and 16 hours of laboratory practice. According to the didactic rules of the Medical-pharmaceutical Biotechnology Master course, the frequency is mandatory. Laboratory activities will be delivered by teacher collaborators to small student groups, following a schedule that will be communicated, to favor the individual participation to the activities.

All laboratory activities will be preceded by a theoretic introduction about the relevance of the techniques analyzed, and will be focused on the use basic and innovative approaches in pharmacology research

SYLLABUS/CONTENT

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

RECOMMENDED READING/BIBLIOGRAPHY

General and Molecular Pharmacology: Principles of Drug Action Edizione Inglese  a cura di Francesco Clementi, Guido Fumagalli, Christiano Chiamulera, Emilio Clementi, Riccardo Fesce, Wiley Ed.

Moreover, all the slides used during the frontal lessons will be made available via Aulaweb site, before the respective lesson.