Pharmaceutical Chemistry I

Code:

MI072220

Acronym:

QFARM1

Keywords
Classification	Keyword
OFICIAL	Physical Sciences

Instance: 2013/2014 - 2S

Active?	Yes
Responsible unit:	Organic and Pharmaceutical Chemistry Laboratory
Course/CS Responsible:	MSc in Pharmaceutical Sciences

Cycles of Study/Courses

Acronym	No. of Students	Study Plan	Curricular Years	Credits UCN	Credits ECTS	Contact hours	Total Time
MICF	218	Official Curriculum	2	-	7	78	175,5

Teaching language

Portuguese

Objectives

- It is intended that students become capable of, for the various types of drugs, interpreting and foreseeing their structure-activity relationships, metabolism, as well as the mechanisms of action at a molecular level. - The therapeutical applications shall be related to "Acto Farmacêutico". - In the laboratorial classes it is intended that the student acquire knowledge on methodologies used on the analysis of drugs, having in line a programmatic coordination with the theory lectured

Learning outcomes and competences

 

At the end of the CU, students must have a broad and integrated understanding of the entire chemical and pharmaceutical drugs discovery, planning, and development. The CU also aims to promote and develop critical thinking, teamwork and autonomy. At the end of the CU, students should be able to easily communicate their ideas, collaborate and work in team and to be able to solve problems using the scientific and investigational method.

 

Working method

Presencial

Pre-requirements (prior knowledge) and co-requirements (common knowledge)

 

- It is assumed students have the basic knowledge provided by the subjects: Organic Chemistry I, Organic Chemistry II, Pharmaceutical Chemistry I, Biochemistry, Pharmacology and Instrumental Analysis Methods.

Program

Theoretical component - Medicinal Chemistry: definition and glossary (IUPAC). Factors affecting the mode of action of drugs: physical-chemical factors and stereochemical factors (chirality, eutomer/distomer, eudismic ratio). Methods for search and discovery of new drugs: definition of pharmacophore, establishment and optimisation of “lead structures”, molecular modification (classical and special processes), isosteric substitution. Definition of pro-drugs, soft and hard drugs. Establishment of structure-activity relationship (SAR, QSAR). Molecular recognition and application of artificial molecular recognition in Pharmaceutical Chemistry. Computational Chemistry in the structure determination and molecular properties, conformational analysis, pharmacophore identification and de novo design. Structures, syntheses, mechanisms of action, structure-activity relationships and metabolism of the following families of drugs: GENERAL ANESTHETICS Historical development. Inhalation anesthetics Intravenous anesthetics. LOCAL ANESTHETICS Mechanism of action of drugs in ionic channels. Amide and ester derivatives. HYPNOTICS, SEDATIVES AND ANXIOLYTICS Historical development. Neuronal systems involved in anxiety regulation and state of alert. GABAergic and serotoninergic systems. Barbiturates. Amides, imides, alcohols and carbamates, chloral and derivatives. Benzodiazepins ANTIPSYCHOTICS Historical development. Role of dopamine as a CNS transmitter, pharmacological intervention in dopaminergic ways. Phenotiazines. Tioxanthenes. Butyrophenones. Diphenylbutylamines ANTIDEPRESSANTS Neuronal systems involved in humour regulation, involved messengers, possibilities of pharmacological intervention. Historical development MAO-A inhibitors. Tricyclic and tetracyclic agents. Selective serotonin reuptake inhibitors. Others NARCOTIC ANALGETICS Nociceptive and antinociceptive systems, messengers involved in transmission, pharmacological intervention possibilities. Exogenous analgetics: opioid agonists. Morphine, morphinan, benzomorphan, oripavine and phenylpiperidine derivatives . Other opioids. Opioid antagonists. Endogenous narcotic analgesics: opioid peptides and derivatives . Specific chemical drug delivery systems for CNS. HISTAMINERGIC AGENTS Histamine and other autacoids: chemical structure and functions. Histaminic receptors. H1 antagonists: First generation (ethanolamine, alkylamine, ethylenodiamine, piperazine and phenothiazine derivatives). New generation antihistaminic agents. Antihistaminic potency and stereochemistry relationships. Classical and actual pharmacophore for antihistaminic H1 H2 antagonists: structural evolution and pharmacophore; applications as antisecretors in peptic ulcer. H3 antagonists: “state of art” and perspectives for therapeutic application. ANALGESICS- ANTIPYRETICS AND non-steroid ANTI-INFLAMMATORY AGENTS Pain, fever, inflammation: mechanism and transmitters involved. Arachidonic acid cascade (leukotrienes, prostaglandins, thromboxanes). Arachidonic acid methabolism via cycloxygenase (COX). COX 1 e COX 2 structure and functions. Classes of anti-inflammatory agents (AINEs): Salicilic acid and derivatives. “New” applications for acethylsalicilic acid. Fenamates Arylacetic acid. Profens: Chirality-activity and -toxicity relationships. Oxicams: supramolecular chemistry; formation of inclusion complexes. Main secondary effects and strategies for avowing them. Recent strategies in research for new AINEs. p-Aminophenol derivatives. PARKINSON AND ALZHEIMER - Traditional and recent therapeutics approaches. 

Practical works.

Mandatory literature

British Pharmacopeia, British Pharmacopeia Commision, The Stationary Office, London, 2001
M.M. Pinto, H.M. Cidade; Obtenção de complexos de inclusão; Inclusion complex of Diazepam with Cyclodextrins in Solid Phase, Pratical Studies for Medicinal Chemistry, Exercise 1.8, Ed., CYTED, 2006
C.M. Corrêa; Latenciação do Sulfatiazol" Práticas de Química Farmaceutica y Medicinal, M.A.F.Prado e E.J.Barreiro,Ed., CYTED, 92-94, 2002
Barreiro Eliezer J.; Química medicinal: as bases moleculares da ação dos fármacos. ISBN: 85-7307-782-4
United States Pharmacopeial Convention, Inc.; The United States pharmacopeia. ISBN: 1-889788-10-4
Carmén Avendano; Introduccion a la quimica farmacêutica, McGaw Hill-Interamerica de Espana, 2001
Martindale The Complete Drug Reference, 33Th Ed., Pharmaceutical Press, London, 2002
Silverman Richard B.; The^organic chemistry of drug design and drug action. ISBN: 0-12-643732-7
R.J.S. Hickman, J. Neill; Influence of pH on drug absorption from the gastrointestinal tract, J. Chem. Ed.,74 (7), 855-856, 1997
M.A.F. Prado; Determinação de constantes hidrofóbicas de substituintes de sulfonamidas por meio de cromatografia em camada delgada em fase reversa”, Prácticas de Química Farmacêutica y Medicinal do Sulfatiazol, Ed,. CYTED, 8-11, 2002
Nogrady Thomas; Medicinal chemistry: a biochemical approach. ISBN: 0-19-505369-9
Comissão da Farmacopeia Portuguesa; Farmacopeia portuguesa VIII. ISBN: 972-8425-67-8
Patrick Graham L.; An^introduction to medicinal chemistry. ISBN: 0 19 850533 7
Pinto Madalena M. M. 340; Manual de trabalhos laboratoriais de química orgânica e farmacêutica. ISBN: 978-972-757-750-7

Teaching methods and learning activities

- Theoretical classes (3 hours/week): Presentations in “Power Point”; it is intended to transmit knowledge in an attractive and deductive manner. - Some classes will be destined to the clarification of some matters and for solving some practical exercises in a way that stimulates the mind and taste for the subjects approached in both theoretical and laboratorial classes. - The laboratorial tasks (3 hours/week) are performed in groups of 2 or 3 students, according to a chronogram. The logic of execution and its objectives are previously explained in the theoretical and laboratorial demonstration classes. - The lecturer responsible is available for students consultation on the times announced at the beginning of the semester or at a time previously arranged and agreed.

keywords

Physical sciences > Chemistry > Computational chemistry
Physical sciences > Chemistry > Organic chemistry
Natural sciences > Biological sciences > Biodiversity
Physical sciences > Chemistry > Combinatorial chemistry
Physical sciences > Chemistry > Applied chemistry > Pharmaceutical chemistry
Health sciences
Health sciences > Pharmacological sciences
Physical sciences > Chemistry > Biochemistry > Metabolism

Evaluation Type

Distributed evaluation with final exam

Assessment Components

designation	Weight (%)
Exame	70,00
Participação presencial	0,00
Trabalho laboratorial	30,00
Total:	100,00

Amount of time allocated to each course unit

designation	Time (hours)
Frequência das aulas	0,00
Trabalho laboratorial	70,00
Total:	70,00

Eligibility for exams

a) During pratical classes the students will be evaluated by an oral presentation of a work. The performance of this is compulsory. b)Attendance to theoretical classes is not compulsory. c)Students that do not achieve 9,5 in pratical work distributed evaluation must performe a pratical exam previously to the final exam in date according to the lective calendar. d)The written final exam will include all matters discussed in theoretical classes. e)For students evaluated before 2009/2010 the written final exam will include all matters discussed in theoretical classes in this year f) Students need to have at least 8.6 in the final written exam.

Calculation formula of final grade

The final grade is attributed by the following manner: - 50% from the final written exam - 30% from the laboratorial component - 20% from the oral presentation of a work Students with final grades equal or superior to 10 will be approved and with final grades inferior to 10 will be reproved.

Examinations or Special Assignments

During practical classes the students will be evaluated by one oral presentation which encompass themes related to the subjects teached. The performance of this is compulsory.

Internship work/project

not applicable

Special assessment (TE, DA, ...)

- Students that by law do not need to attend the practical classes, and do not have frequency in these classes must perform a practical exam previously to the final written exam in date according to the lective calendar. The evaluation of students in the special conditions contemplated by Law follows that specified in the current “Evaluation Norms” of FFUP. - It is assumed students have the basic knowledge provided by the subjects: Organic Chemistry I, Organic Chemistry II, Pharmaceutical Chemistry I, Biochemistry, Pharmacology and Instrumental Analysis Methods.

Classification improvement

-For classification improvement the student has to perform the laboratorial exam and the written exam.