PHARMACEUTICAL AND TOXICOLOGICAL CHEMISTRY II
Academic year and teacher
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- Versione italiana
- Academic year
- 2022/2023
- Teacher
- STEFANO MANFREDINI
- Credits
- 9
- Didactic period
- Secondo Semestre
- SSD
- CHIM/08
Training objectives
- Update February 2022. The course in Pharmaceutical Chemistry and Toxicology II is integrated with the previous course in Pharmaceutical Chemistry and Toxicology I for the treatment of the chemical-pharmaceutical aspects of the main classes of drugs.
The objective of the course in question is to give the student the knowledge of the chemical type: SAR, interactions, mechanisms of action of the main drugs used for the treatment of various diseases.
The main knowledge acquired will be:
-knowledge of the concepts of mechanisms of interaction with the specific targets that characterize the pharmaceutical chemistry of traditional drugs;
-chemical-pharmaceutical knowledge of the drugs treated during the course, the relationship between the chemical structure of the drug and its biological activity (SAR), the mode of chemical interaction of the drug with the biological substrate.
The main skills acquired will be:
-to describe and discuss in appropriate language the salient aspects and problems related to the drugs treated;
- identify the functional groups and structural properties of drugs that are important for their action, and predict the chemical and chemical-physical properties of drugs, inferable from their structure;
-to identify the consequences of the presence of functional groups on the biological properties of drugs. Prerequisites
- Basic knowledges in the areas of Inorganic chemistry, Organic chemistry, Anatomy, Physiology and Pathology.
Course programme
- The course consists of 72 hours of frontal classroom teaching.
It deals with the study and understanding of the structure and activity relationships of neurotransmitters and/or autacoids promoting certain physiological and pathophysiological activities; of biological substrates as targets for interaction of neurotransmitters and/or autacoids. Interaction of neurotransmitters and/or autacoids and/or drugs with biological substrates. Evaluation of endocellular biochemical parameters as a result of drug/biological substrate interaction.
MEDICINES TREATED DURING THE COURSE
Part I: The drug and the biological substrate of interaction
(a) Drugs and substrates: state of the art drug therapy
(b) Structure of proteins and their function
(c) Enzymes: structure and function
(d) Receptors: structure and function
(e) Receptors and signal translation
Part II) DRUGS ACTIVE ON NEUROTRASMISSION
1. Drugs active on cholinergic neurotransmission
2. Adrenergic drugs
3. Drugs active on serotonergic neurotransmission
4. Local anaesthetics
Part III) DRUG ACTIVE ON THE CENTRAL NERVOUS SYSTEM
5. Anaesthetics
6. Hypnotics
7. Anticonvulsants
8. Anxiolytics and antipsychotics
9. Hallucinogens, stimulants and drugs of abuse
10. Opioid analgesics
11. Antiparkinson and spasmolytics
Part IV) DRUGS ACTIVE ON THE CARDIOVASCOLAR SYSTEM
12. Cardiac drugs: cardiac glucosides, antianginal and anti-arrhythmic drugs
13. Central and peripheral sympathizers; vasodilators
14. Angiotensin converting enzyme and renin inhibitors, angiotensin antagonists and Ca++ channel blockers
15. Vasopressin and its modulation
16. Antitrombotics and trombolitics
17. Diuretics
Part V) DRUGS ACTIVE ON THE IMMUNITY SYSTEM
18. Antihistamines and negative histamine receptor-2 modulators
Every class of drug is treated:
(a) structure
(b) the relationship between structure and pharmacological activity
(c) evaluation of the pharmacophoric functions present in the structure of the medicinal product
(d) evaluation and importance of chirality
(e) importance of metabolites
(f) use of prodrugs Didactic methods
- Lectures with presentation of various biological systems, discussion of the structures of medicines with particular reference to the functional groups proposed and in relation to the interaction with biological substrates /SAR and QSAR). Presentation of "Clinical cases" in order to determine the best medication within a narrow range of possible treatment options. The didactics can use the intervention of external experts in the professional, industrial or clinical field in order to provide examples of applications and relevant to the world of the profession.
Learning assessment procedures
- The objective of the examination is to verify the level of achievement of the objectives indicated above. Verification will be oral and written. Students who attend the lessons assiduously (at least 75%) and who intend to complete the final oral assessment, for the overcoming of the remaining part of the program, by June 30 of the year of the course, can make use of written assessments (in April). The evaluation will be taken into account only if successfully passed, if in the partial test the evaluation is between 18-21 will be taken into account as 0.5 points to be added to the oral evaluation on the second part of the program. For scores between 22-25 will be taken into account as 1 point to be added to the oral evaluation on the second part of the program. For scores between 26-28 will be taken into account as 1.5 points to be added to the oral evaluation on the second part of the program. For scores between 29-31 will be taken into account as 2 points to be added to the oral evaluation on the second part of the program. The test in progress aims to align the effectiveness of the teaching method with learning and thus improve the understanding of the subject and the possibility of successfully passing the oral test after completion of the assessment with better scores.
The ongoing evaluation is carried out in written form through 10 open-ended questions. To pass the test one must acquire at least 18 points out of 31. The time allowed for the written test is 2 hours.
It is not allowed to consult texts or use PCs, smart phones.
The oral test aims to assess the knowledge of the subject and the ability to connect and compare in a transversal way different aspects covered during the course.
To pass the test one must acquire at least 18 points out of 31. In particular, the test uses questions on at least three different topics and the final grade does not corresponds to the average of the evaluations of the answers increased with the scores acquired in the ongoing evaluation.
The achievement of an organic and complete vision of the topics studied in depth in class, the demonstration of expressive mastery and competence in specific terminology, the possession of adequate synthesis and connection skills between the various areas of the subject, as well as between it and the other matter studied, will be evaluated with marks of excellence.
The mostly mnemonic knowledge of the subject, the ability to analyse less clearly, the correct exposure but with uncertainties in the use of reference terminology, will lead to discrete or acceptable evaluations.
The approximate competence of the subjects and the superficial understanding of the subject matter, the lack of propensity for analysis and the expression not always appropriate, will lead to sufficient or just above sufficiency evaluations.
Educational gaps, inappropriate language, lack of orientation among the materials offered in the course program, lead to the expectation that the examination will be a waste of time for both student and teacher.
The Distance Modes are contained in the Classroom page dedicated to the students of the Course. Reference texts
- Foye's. Principi di chimica farmaceutica VI Edizione, by Piccin Nuova Libreria SpA, Padova
Chimica farmaceutica. Alberto Gasco (Autore), Fulvio Gualtieri (Autore), Carlo Melchiorre (Autore) Casa Editrice Ambrosiana
