Pharmacology I

Base Knowledge

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

Teaching Methodologies

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)

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

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

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

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

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

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

Learning Results

Upon completion of the course unit, students are expected to be capable of:

C1 – Interpreting the mechanisms of action of pharmacologically active molecules, competent to modulate: i)

the central nervous system, ii) inflammation and pain, iii) the respiratory system, and iv) the cardiovascular

and renal systems

C2 – Contextualizing the origin of adverse effects and drug interactions of the aforementioned molecules,

applying systemic thinking algorithms and recognizing how complex physiological systems are modulated in

different domains

C3 – Understanding and applying the methodologies associated with the pre-clinical research process in

Pharmacology

C4 – Applying the drug research and development process in its pre-clinical phase, selecting appropriate

biomedical methodologies/protocols with a view to pharmacotherapeutic innovation

C5 – Reasoning analytically and critically, with proficiency in oral and written communication strategies in

pharmacological sciences

Program

Theoretical Matrix (T)

Module 1. Pharmacology of the Central Nervous System (CNS) (24h)

1.1. Introduction to neuropharmacology and psychopharmacology

1.1.1. Review of nerve action potentials and neurotransmission

1.1.2. Classes of neurotransmitters and receptors: excitatory and inhibitory

1.1.3. Strategies to modulate nerve action potentials

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

1.2.1. CNS stimulants

1.2.1.1. Cerebral cortex stimulants

1.2.1.2. Brainstem stimulants

1.2.1.3. Spinal cord stimulants

1.2.2. Sedative-hypnotic drugs

1.2.2.1. Anxiolytics, sedatives, and hypnotics: barbiturates, benzodiazepines, azapirones, agonists of BZD and

melatonin receptors

1.2.3. Antiepileptic drugs (AEDs)

1.2.3.1. Classical AEDs

1.2.3.2. Second-generation AEDs

1.2.4. General and local anesthetics and skeletal muscle relaxants

1.2.4.1. Inhalational anesthetics

1.2.4.2. Intravenous anesthetics

1.2.4.3. Muscle relaxants: neuromuscular junction blockers and spasmolytics

1.2.5. Antipsychotic drugs

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

1.2.5.2. Second-generation antipsychotics

1.2.6. Psychoanaleptic antidepressants

1.2.6.1. Tricyclics

1.2.6.2. Non-tricyclics

1.2.6.3. MAO-A inhibitors

1.2.6.4. Selective serotonin reuptake inhibitors (SSRIs)

1.2.6.5. Non-selective serotonin and norepinephrine reuptake inhibitors

1.2.8. Non-opioid central analgesics

1.2.9. Opioid analgesics: pure agonists, partial agonists, mixed agonist-antagonists, antagonists

1.2.10. Anti-inflammatory and antinociceptive drugs

1.2.10.1. Introduction to eicosanoid and leukotriene synthesis pathways and nociceptive pathways

1.2.10.2. Non-steroidal anti-inflammatory drugs (NSAIDs): derivatives of carboxylic acids, enolic acids, and

others; coxibs

1.2.10.3. Steroidal anti-inflammatory drugs: glucocorticoids

1.2.10.4. Immunosuppressants: calcineurin inhibitors, mesalazine, antiproliferative/metabolic agents,

dimethyl fumarate, glatiramer acetate, fingolimod

1.2.10.5. Biological therapy

1.2.10.6. Centrally acting muscle relaxants: α2 agonists, BDZs, baclofen

1.2.10.7. Triptans

1.2.10.8. Classical and non-classical cannabinoids

1.3. Pharmacology of neurodegenerative diseases

1.3.1. Alzheimer’s disease: acetylcholinesterase inhibitors, non-competitive NMDA receptor antagonists,

experimental active and passive immunotherapy

1.3.2. Parkinson’s disease: anticholinergics, dopaminomimetics, experimental immunotherapy, and anti-α-

synuclein antibodies

Module 2. Pharmacology of the Respiratory System (9h)

Pharmacokinetic and pharmacodynamic considerations of the following pharmacological groups:

2.1. Bronchodilators:

2.1.1. β2 sympathomimetics

2.1.2. Muscarinic cholinergic antagonists

2.1.3. Methylxanthines

2.2. Inflammation modulators: leukotriene LTD4 receptor antagonists, lipoxygenase inhibitors,

phosphodiesterase inhibitors

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

2.4. Antihistamines: first and second generation

2.5. Centrally and peripherally acting antitussives

2.6. Expectorants and mucolytics

Module 3. Pharmacology of the Cardiovascular and Renal Systems (12h)

3.1. Review of electrocardiophysiology

Pharmacokinetic and pharmacodynamic considerations of the following pharmacological groups:

3.2. Vaughan Williams classification of antiarrhythmic drugs

3.3. Class IA, IB, IC, II, III, and IV antiarrhythmics

3.4. β-receptor blockers: selective and non-selective

3.5. Modulators of the renin-angiotensin-aldosterone system: ACE inhibitors, AT antagonists

3.6. Nitrovasodilators

3.7. Diuretics: carbonic anhydrase inhibitors, loop diuretics, thiazide diuretics, potassium-sparing diuretics,

osmotic diuretics

Practical Matrix (P)

Module 1. The Preclinical Research and Development (R&D) Process of Medicines and Health Products in

Pharmacology (15h)

1.1. Certification in experimental pharmacology

1.2. In silico phase: computer-aided drug design (CADD)

1.3. In vitro phase: cellular models

1.3.1. Cell lines

1.3.2. Primary cultures

1.3.3. Organoids and spheroids

1.4. In vivo phase: animal models of human disease

1.4.1. Genetic models

1.4.2. Surgical models

1.4.3. Toxicological models

1.4.4. Diet-induced models

1.4.5. Species selection and influencing factors

1.4.6. Single and repeated exposure protocols

1.4.7. In vitro/in vivo correlations: dose translation

1.4.8. Translational evaluation of preclinical protocols

1.4.9. Ethical and regulatory issues

1.5. Biomedical methodologies for assessing efficacy and safety

1.6. Protocols for meeting regulatory requirements on efficacy and safety relevant to EMA and FDA agencies

Module 2. Models for Assessing Extent of Absorption and Current EMA Guidelines (15h)

2.1. Transporter toolkit and international guidelines for identifying substrates, inhibitors, and inducers of

transporters

2.1.1. Membrane models: ATPase assay and membrane vesicle assay

2.1.2. Cellular models: cell lines overexpressing a transporter (Caco-2) or transfected with transporter genes

(MDCK-MDR1, MDCK-BCRP)

2.1.2.1. Accumulation assays (bidirectional assays and sandwich-cultured hepatocytes)

2.1.2.2. Uptake assays

2.1.3. In vivo models

2.2. Practical models for studying intestinal absorption

2.2.1. In vitro models (isolated organ)

2.2.2. Ex vivo models (open perfusion)

2.2.3. In vivo models (fluorescent probes, scintigraphic methods)

2.3. Simulated prediction of CYP substrates and inhibitors

Curricular Unit Teachers

Liliana Pereira Santos

Internship(s)

NAO

Bibliography

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