Drugs active on receptor-channels, on G-protein receptors, on tyrosine kinase-associated receptors, ion channels, enzymes, and carriers. Active drugs on intracellular receptors and regulation of gene expression. Principles of gene therapy. Stem cells and principles of regenerative medicine. Pain therapy. Epigenetic drugs. Proteins as drugs. Monoclonal antibodies.
Knowledges on cellular and molecular mechanisms of drug action; Knowledges on drug seen not only as a therapeutic tool, but also as a mean of investigation to study several biological phenomena and, ultimately, to design new and more modern drugs. Cellular and molecular bases for the evaluation of the adverse and toxic effects of drugs and the new frontiers of regenerative medicine.
Skills: understanding of the mechanisms of action of drugs that emerge by the knowledge of molecular biology.
Skills acquired at the end of the course: Fundamental elements for the study of cellular and molecular mechanisms of action of drugs
Prerequisites
None
Teaching Methods
Frontal lessons supported by slides, available to students to the UNIFI e-learning platform.
Further information
.
Type of Assessment
Oral exam.
Course program
Nature and structure of the molecules present in the body by which drugs interact and molecular events underlying the cellular effects of drugs.
G protein coupled receptors: Molecular organization, function and effector systems. Adrenergic receptors (alpha and beta), muscarinic, angiotensin II, incretin, opioid receptors: molecular structure, function and drugs.
Ion channels target of drug action: Molecular organization, classification and pharmacology. Antiarrhythmic and antiepileptic drugs.
Ion pumps and target transporters of drug action: digitalis glycosides, sulfonylureas, glyphozines (SGLT2 inhibitors), anti-ulcer drugs.
Enzymes target of drug action: inhibitors of cyclooxygenases (non-steroidal anti-inflammatory drugs), phospholipase A2 (corticosteroids), hydroxymethylglutaryl-CoA reductase (or HMG-CoA reductase), propotein of the convertase subtilisin / Kexin type 9 (PCSK9 ), ACE, renin, dipeptidyl dipeptidase IV.
Channel receptors: molecular organization and modulation of the activity of channel receptors. Cholinergic nicotinic receptor: molecular structure and drugs active on this receptor.
GABAA receptor: structure and agonist and antagonist drugs on this receptor. Benzodiazepines and barbiturates. Glutamate and serotonin channel receptors: Molecular structure, function and active drugs on these receptors.
Gender differences in response to cardiovascular drugs
Cellular regenerative therapies in cardiovascular and musculoskeletal diseases.
Physiology and pathways of pain and general principles of therapy.
Monoclonal antibodies and antibody derivatives: structure of antibodies, activity and recycling, synthesis, selection of hybridomas, chimeric, humanized and human antibodies, protein variants, antibody fragments, conjugated to proteins, conjugated to drugs, indirect loading Ab, pharmacokinetics / pharmacodynamics , adverse reactions.
Epigenetic drugs: epigenetic enzymes, epigenetic drugs approved in therapy, epigenetic drugs in clinical and preclinical development.
Proteins as drugs: protein engineering, engineered insulin, scaffold protein, fusion proteins, targeted delivery, fusion protein, classification of fusion proteins, pharmacokinetics / pharmacodynamics, peptidomimetics.
Preclinical and clinical pharmacology