LEARNING OUTCOMES

Learning outcomes will be: a) basic knowledge about: i) drug pharmacokinetic: absorption and distribution of drug in the body; drug metabolism; excretion); ii) general pharmacodynamics: targets and mechanism of drug action; dose-response curve; agonists and antagonists; biochemical and physiological drug effects and their molecular mechanism; iii) individual variations and side-effects.

LEARNING OUTCOMES (FURTHER INFO)

The course provides basic knowledge on a) drug pharmacokinetic properties:  rate of absorption; distribution of drugs in the body; drug metabolism and excretion; b) basic pharmacodynamic concepts: targets and mechanisms of drug action; dose-response curve; biochemical and physiological drug effects and their molecular mechanism; c) individual variation in drug response and side-effects.

TEACHING METHODS

Frontal Lessons

Slides (aulaweb)

SYLLABUS/CONTENT

Essential lexicon in Pharmacology: active substances (drugs; medicinal preparations; medicinal herbes; placebo), drug classes.

Pharmacological Disciplines: general and cellular pharmacology; pharmacognosy; clinical pharmacology; pharmacoeconomics; pharmacogenetics and pharmacogenomics; pharmacovigilance; chemotherapy; toxicology.

Drug discovery and development. Generic and orphan drugs.

Mechanisms of drug action and relation between drug concentration and effect: target and action of drug not mediated by receptors, affinity and potency, receptor occupancy and copetition, agonist and atagonist, allosteric modulator, partial agonist, inverse agonist

Receptors and modulation of their response. Receptor classification, pathway and signaling transduction: intracellular/nuclear receptors; membrane receptors (ionotropic and G-protein coupled receptors); receptor trafficking;   receptor responses (desensitization and sensitization); drug modulation of receptor responses.

Ionotropic receptors. Tissue and subcellular distribution; molecular organization; classification (glutamatergic ionotropic receptors and GABAA); localization of binding site; channel structure; modulation of ionotropic receptor; drug and their mechanisms of action.

G-protein coupled receptors. Molecular organization and mechanism of action; signal transduction pathways involving the G protein–coupled receptors (the cAMP signal pathway and the phosphatidylinositol signal pathway).

Basic Pharmacodynamics: quantification of drug-receptor interactions and elicted responses; Affinity, Potency and Efficacy; Drug-receptor binding site equilibrium.

Basic Pharmacokinetics: Absorption and routes of drug administration: rate of absorption; partition-coefficient; drug dissolution; extension, permeability and vascolarization of absorption surface; enteral routes (oral, sublingual, rectal); parenteral systemic routes (intravascular, intramuscular; cutaneous); other routes (inhalation, transdermal, transmucosal, intracavity). Absorption kinetics. Drug delivery.

Drug distribution and elimination: the apparent distribution volume; drug binding to plasma proteins; free and bound drug concentration; relevant parameters in drug distribution. Elimination and the concept of half-life; renal excretion and clearence; epatic excretion and enterohepatic cycle.

Drug metabolism: enzymatic systems and phase I and II modifications (cytochome P450; oxidation, reduction, hydrolysis; methylation; sulphation; acetylation; glucoronidation; conjugation with amino acids or glutathione).

Individual variation in the drug response. Tollerance. Side-effects. Idiosyncratic and allergic reactions.  Drug dependency.

General Anesthetics; Agents for control of gastric Acidity and treatment of peptic ulcers. Biotechnological drugs.

Principles of Toxicology. Cellular toxicity pathways. Free radicals. teratogenesis and foetal toxicity. Glutamatergic Excitotoxicity and Hypoxia in the central nervous system.

RECOMMENDED READING/BIBLIOGRAPHY

Golan DE e altri - Principi di Farmacologia – Casa Editrice Ambrosiana

Rang HP, Dale MM, RitterJM, Flower RJ - Farmacologia - Ed. Elsevier Masson

Howland RD, Mycek MJ – Le basi della farmacologia – Ed Zanichelli

Notes of Lesson