Pharmacology I

Anatomophysiology I and II, Cellular and Molecular Biology, Biochemistry, Organic Chemistry, Pharmaceutical Chemistry

The content pertaining to modules 1-3 capitalize on fundamental knowledge in pharmacological sciences, which is applied to solving real cases, fostering analytical and critical thinking in Pharmacology. Module 4 advocates for the practical application of knowledge in more complex scenarios, developing pharmacological competencies in practical aspects, and enhancing oral and written communication skills. The selected teaching methodologies (TM) integrate innovative pedagogical strategies through active learning moments, centered on the student, with the goal of fostering the knowledge trilogy in its dimensions: knowing-knowing (knowledge), knowing-doing (skills), and knowing-being (competencies).

TM1 – Interactive expository teaching through suitable audiovisual means, with active individual learning moments focused on solving pharmacological problems for knowledge application: Mentimeter Platform (Wordcloud, Q&A, Multiple Choice, Ranking tools) [Modules 1-3]

TM2 – Interactive expository teaching through audiovisual means with active group learning moments focused on the analysis and discussion of scientific articles in the field for knowledge application: Jigsaw Activities [Modules 1-3]

TM3 – Interactive expository teaching through audiovisual means with active group learning moments focused on the analysis and discussion of scientific articles in the field for knowledge application: Think-Pair-Share Activities [Modules 1-3]

TM4 – Project-based teaching: The practice is action-oriented through the formulation, in groups, of the pharmacological gap, hypothesis design, and selection of appropriate pharmacological assays/biomedical methodologies to solve the problem. The teacher facilitates the learning process through synchronous guidance on the Jamboard Platform. In this process, the practice is action-oriented with the development of analytical and problem-solving skills in practical pharmacological cases using the Vienna LiverTox Workspace and NCI-ALMANAC algorithms available online [Module 4]

TM5 – Project-based teaching: The practice is action-oriented through the exploration, in groups, of pre-clinical pharmacological assays in a real-world context – Hands-on laboratory [Module 4]

TM6 – Project-based teaching: The practice is action-oriented with the conceptualization and development, in groups, of an explanatory Infographic for each pharmacological project through the Canva platform [Module 4]

TM7 – Project-based teaching: The practice is action-oriented with the group presentation of the developed project in a Pitch format, aiming to gain oral communication skills in pharmacological sciences [Module 4]

By the end of the course unit, students are expected to have developed skills to:

 C1 – Characterize fundamental concepts of pharmacokinetics and pharmacodynamics.

C2 – Understand the mechanisms of action of pharmacologically active molecules, proficient in modulating: i) the central nervous system, ii) inflammation and pain, and iii) the respiratory system.

C3 – Contextualize the origin of adverse effects and drug interactions of the molecules under consideration, applying systemic thinking algorithms and recognizing how complex physiological systems are modulated in different domains.

C4 – Apply the drug research and development process in its pre-clinical phase, selecting appropriate biomedical methodologies/protocols, with a view to pharmacotherapeutic innovation.

C5 – Analyze and criticize thoughtfully, demonstrating proficiency in oral and written communication strategies in pharmacological sciences.

Theoretical Matrix (T)

Module 1. Basic Principles of Pharmacology and Fundamentals of Pharmacokinetics and Pharmacodynamics (9h T)

1.1. Origin of drugs and nomenclature

1.2. Definition of therapeutic effect, side effect, and adverse effect

1.3. Effects of drugs on biological systems: levels of organizational complexity

1.4. Main pharmacological molecular targets: ionotropic, metabotropic, and kinase-coupled receptors; enzymes and transporters.

1.5. Macromolecular nature of drug receptors: kinetics of drug-receptor binding.

1.6. Relationship between receptor occupancy percentage and pharmacological effect. Dose-response curve (Emax, EC50, and ED50)

1.7. Definition of concepts: specificity, affinity, efficacy, potency, synergism, interaction, bioavailability, bioequivalence, desensitization, and tolerance

1.8. L.A.D.M.E. System

1.9. AUC Curve: incorporation, disposition, and pharmacokinetic parameters

1.10. Administration routes

Module 2. Pharmacology of the Central Nervous System (CNS) (27h T)

2.1. Introduction to neuropharmacology and psychopharmacology

2.1.1. Review of nervous action potential and neurotransmission

2.1.2. Classes of neurotransmitters and receptors: excitatory and inhibitory

2.1.3. Strategies for modulating nervous action potential

2.2. Pharmacokinetic and pharmacodynamic considerations of the following pharmacological groups:

2.2.1. CNS Stimulants

2.2.1.1. Stimulants of the cerebral cortex

2.2.1.2. Stimulants of the brainstem

2.2.1.3. Stimulants of the spinal cord

2.2.2. Sedative-Hypnotic Drugs

2.2.2.1. Anxiolytics, sedatives, and hypnotics: barbiturates, benzodiazepines, azapirones, BZD receptor agonists, and melatonin receptor agonists

2.2.3. Antiepileptic Drugs (AEDs)

2.2.3.1. Classic AEDs

2.2.3.2. Second-generation AEDs

2.2.4. General, local anesthetics, and skeletal muscle relaxants

2.2.4.1. Inhalation anesthetics

2.2.4.2. Intravenous anesthetics

2.2.4.3. Muscle relaxants: neuromuscular junction blockers and spasmolytics

2.2.5. Antipsychotic Drugs

2.2.5.1. First-generation antipsychotics (phenothiazines, butyrophenones, thioxanthenes)

2.2.5.2. Second-generation antipsychotics

2.2.6. Psychostimulant Antidepressant Drugs

2.2.6.1. Tricyclics

2.2.6.2. Non-tricyclics

2.2.6.3. MAO-A Inhibitors

2.2.6.4. Selective 5HT reuptake inhibitors

2.2.6.4. Non-selective 5HT and NA reuptake inhibitors

2.2.8. Central Non-opioid Analgesics

2.2.9. Opioid Analgesics: pure agonists, partial agonists, mixed agonist-antagonists, antagonists

2.2.10. Anti-inflammatory and antinociceptive drugs

2.2.10.1. Introduction to eicosanoids and leukotrienes synthesis pathways and nociceptive pathways

2.2.10.2. Non-steroidal anti-inflammatory drugs (NSAIDs): carboxylic acid derivatives, enolic acid derivatives, and others; coxibs

2.2.10.3. Steroidal anti-inflammatory drugs: glucocorticoids

2.2.10.4. Immunosuppressants: calcineurin inhibitors, mesalazine, anti-proliferatives/metabolics, dimethyl fumarate, glatiramer acetate, fingolimod

2.2.10.5. Biological therapy

2.2.10.6. Central action muscle relaxants: α2 agonists, BZDs, baclofen

2.2.10.7. Triptans

2.2.10.8. Classic and non-classic cannabinoids

2.3. Pharmacology of Neurodegenerative Diseases

2.3.1. Alzheimer’s Disease: acetylcholinesterase inhibitors, non-competitive antagonists of NMDA receptors, active and passive experimental immunotherapy

2.3.2. Parkinson’s Disease: Anticholinergics, dopaminomimetics, immunotherapy, and experimental anti-α-synuclein antibodies

Module 3. Pharmacology of the Respiratory System (9h T) Pharmacokinetic and pharmacodynamic considerations of the following pharmacological groups:

3.1. Bronchodilators:

3.1.1. β2 Sympathomimetics

3.1.2. Muscarinic cholinergic antagonists

3.1.3. Methylxanthines

3.2. Inflammation modulators: leukotriene LTD4 receptor antagonists, lipoxygenase inhibitors, phosphodiesterase inhibitors

3.3. Biological therapy: anti-IL5, anti-IL4R, anti-IgE

3.4. Antihistamines: 1st generation and 2nd generation

3.5. Central and peripheral action antitussives

3.6. Expectorants and mucolytics

Practical Matrix (P)

 Module 4. The preclinical research and development (R&D) process of drugs and health products in Pharmacology

4.1. Certification in experimental pharmacology

4.2. In silico phase: computer-aided drug design (CADD, 4h)

4.3. In vitro phase: cellular models (8h)

4.3.1. Cell lines

4.3.2. Primary cultures

4.3.3. Organoids and spheroids

4.4. In vivo phase: animal models of human disease (10h)

4.4.1. Genetic

4.4.2. Surgical

4.4.3. Toxicological

4.4.4. Diet-induced

4.4.5. Choice of species and influential factors

4.4.6. Single and repeated exposure protocols

4.4.5. In vitro/in vivo correlations: dose translation

4.4.6. Translational evaluation of preclinical protocols

4.4.7. Ethical and regulatory issues

4.5. Biomedical methodologies for efficacy and safety assessment (4h)

4.6. Protocols to meet regulatory efficacy and safety requirements relevant to EMA and FDA agencies (4h)

NAO

Principal bibliography
Terapêutica Medicamentosa e suas Bases Farmacológicas, 5a edição. Coordenado por S. Guimarães, D. Moura e P. Soares da Silva. Porto Editora, 2006.
Basic & Clinical Pharmacology, de Katzung, 10a edição, editado pela McGraw-Hill.
Goodman and Gilman’s. The Pharmacological Basis of Therapeutics, 10a edição. Editado por A. G. Gilman et al. Pergamon Press.
Guide to drug development: a comprehensive review and assessment, 1ª edição. Spilker, Bert 2009. Wolters Kluwer Health/Lippincott Williams & Wilkins. 1st edition.

Secondary Bibliography

Professor notes

Scientific articles