Università degli Studi di Urbino Carlo Bo / Portale Web di Ateneo


MEDICINAL CHEMISTRY II
CHIMICA FARMACEUTICA E TOSSICOLOGICA II

A.Y. Credits
2019/2020 12
Lecturer Email Office hours for students
Andrea Duranti every working friday from h 15 to h16. Additionally every working day following appointment made via E-mail: giorgio.tarzia@uniurb.it
Teaching in foreign languages
Course with optional materials in a foreign language English
This course is entirely taught in Italian. Study materials can be provided in the foreign language and the final exam can be taken in the foreign language.

Assigned to the Degree Course

Pharmacy (LM-13)
Curriculum: PERCORSO COMUNE
Giorno Orario Aula
Giorno Orario Aula

Learning Objectives

Learning outcome: the students should become able to appreciate the basic elements of the mode of action, chemical properties and metabolic transformation of the classes of drugs, or individual drugs, listed below. and be able to critically evaluate the information available in the scientific literature.

Program

1. Drugs affecting the Cardiovascular system
1.1 Cardiac glycosides
1.2 Antianginal and antiarrhytmic drugs
1.3 Diuretics
1.4 Angiotensin enzyme inhibitors and Angiotensin II receptor AT1 antagonists
1.5 Calcium channel blockers
1.6 Central and peripheral sympatholytics and vasodilators
1.7 Centrally acting sympatholytic drugs ( methyldopa, clonidine, guanabenz, guanfacine)
1.8 Beta-Adrenergic blocking drugs
1.9 Alpha-Adrenergic blocking drugs
1.10 Mixed alpha/beta-adrenergic blocking drugs
1.11 Vasodilators
1.11.1 Arterial vasodilators (hydralazine, minoxidil, diazoxide)
1.11.2 Arterial and venous vasodilators (sodium nitroprusside)
1.12 Antihyperlipoproteinemics and inhibitors of cholesterol biosynthesis
1.13 Antithrombotics, thrombolytics and Coagulants
2. Drugs affecting the hormonal system
2.1 Insulin and oral hypoglycemic drugs
2.2 Estrogens, Progestins and Androgens
2.3 Thyroid hormones and thyroid drugs
3. Antiulcer drugs.
3.1 H2 receptor Antagonists
3.2 H+/K+-ATPase proton pump inhibitors
4. Chemotherapeutic Agents
4.1 Antibiotics and antimicrobials.
4.1.1 Sulfonamides
4.1.2 Trimethoprim
4.1.3 Quinolones
4.1.4 Phosphomycin
4.2 Inhibitors of bacterial cell wall biosynthesis
4.2.1 Penicillins and beta-lactamases irreversible inhibitors
4.2.2 Cephalosporins
4.2.3 Carbapenems
4.2.4 Monobactams
4.2.5 Vancomycin and Teichoplanin
4.2.6 Bacitracin
4.3 Inhibitors of protein biosynthesis
4.3.1 Aminoglycosides.
4.3.2 Macrolides
4.3.3 Teyracyclines
4.3.4 Chloramphenicol
4.3.5 Linezolid
4.4 Antiparasitic Agents
4.4.1 Nitroimidazoles and Nitrofurans
4.4.2 Pentamidine
4.4.3 Atovaquone
4.4.4 Antimalarial drugs
4.4.4.1 Quinine, 4- and 8- substituted quinolines
4.4.4.2 Pyrimethamine and Pyrimethamine-Sulphadoxine combination
4.4.4.3 Artemisinins
4.6 Antifungal drugs
4.6.1 Polyenes
4.6.2 Imidazoles and Triazoles
4.6.3 Allylamines
4.6.4 Morpholines
4.6.5 Echinocandine
4.6.6 Flucitosine, Griseofulvin, Haloprogin
4.7 Antimycobacterial agents
4.7.1 Anti-Tuberculosis
4.7.1.1 Capreomycin
4.7.1.2 Cycloserine
4.7.1.3 Ethanbutol
4.7.1.4 Isoniazide
4.7.1.5 Kanamycin
4.7.1.6 p-Aminosalicylic acid
4.7.1.7 Pyrazinamide
4.7.1.8 Rifampin
4.7.1.9 Rifapentine
4.7.1.10 anti-mycobacterium avium intracellulare (Azithromycin, Clarithromycin)
4.7.1.11 anti-Leprosy (Dapsone, Clofazimine, Thalidomide)
4.8 Antiviral agents and Protease inhibitors
4.8.1 Antiviral agents interfering with cellular penetration and early replication (Amantadine, Rimantadine, Zanamivir, Oseltamivir)
4.8.2 Agents interfering with viral nucleic acid replication (acyclovir, valacyclovir,Cidofovir, Cytarabine, Famciclovir, Fomivirsen, Foscarnet, Ganciclovir, Idoxuridin, Ribavirin, Trifluorothymidine, Vidarabine)
4.8.3 Antiretroviral agents and Protease Inhibitors (Zidovudine, Didanosine, Zalcitabine, Stavudine, Lamivudine, Abacavir, Nevirapine, Delavirdine, Efavirenz, Sequinavir, Ritonavir, Indinavir, Nelfinavir, Amprenavir, Lopinavir, Ritonavir)

Bridging Courses

Medicinal Chemistry I

Learning Achievements (Dublin Descriptors)

The course is meant to make the students understand  the fundamental relationship between chemical structure of a drug and its interaction with biological targets. The course deals with the medicinal chemistry techniques that lead to the discovery, optimization and proof of the mode of action of the treated drugs as well as their metabolites and when possible their anticipation. The students are expected to understand that the chemical structure of a drug and its rational modification are among the basic factors to rationalize the mode of action and and to improve the profile of most small molecular weight  drug. The course is meant to enable students  to integrate into a general method of evaluation the notions studied on the particular classes of drugs dealt with during the course and be able to independently and critically transfer these notions with a simple but technically correct language

Teaching Material

The teaching material prepared by the lecturer in addition to recommended textbooks (such as for instance slides, lecture notes, exercises, bibliography) and communications from the lecturer specific to the course can be found inside the Moodle platform › blended.uniurb.it

Supporting Activities

Highlight classroom sessions on single classes of drugs.


Didactics, Attendance, Course Books and Assessment

Didactics

frontal lessons in the italian language

Attendance

Attendance is recommended but is but not mandatory. Students should have a sufficient knowledge of organic chemistry to  understand the chemical and metabolic behaviour of the drugs treated during the course.

Knowledge of english sufficient to read and understand a brief scientific text related to the drugs that are being treated in the program and proposed by the teacher to better understand some particular aspects of a given drug or class of drugs.

Course books

Required:

Foye's Principles of Medicinal Chemistry, T.L.Lemke, D.A.Williams editors, sixth edition., Lippincot, Williams and Wilkins 2008.

Essentials of Foyes Princuples of Medicinal Chemistry Wolters Kluwers Health Inc. 2017

Optional

J.M. Beale, Jr., J.M.Block, Wilson & Gisvold's Textbook of Organic and Pharmaceuticall Chemistry 12th edition, Lippincot, Williams & Wilkins 2011.

G. L. Patrick An Introduction to Medicinal Chemistry 5th edition, Oxford University Press 2013.

A. Gasco, F. Gualtieri, C. Melchiorre editors, Chimica Farmaceutica, Casa Editrice Ambrosiana 2015.

Assessment

The final exam consists of a preliminary written test followed by an oral interrogation and failure in any one of the two proofs implies repetition of both. The written test consists of ten open questions, relevant to drugs covered during the semester, and it must be completed within two hours:The single answer are evaluated assigning a score variable from 0 to 3 points depending on the quality of the answers. A score of  at least 18/30 is necessary to be admitted to the oral examination. The interrogation on topics different from or in part coincident with those of the written test lasts 30-45 minutes. The scheme allows a uniform and thorough evaluation of the students knowledge and understanding of the topics treated during the semester.

Additional Information for Non-Attending Students

Attendance

Same as for the attending students.

Course books

Same as for the attending students.

Assessment

Same as for the attending students.

« back Last update: 04/11/19

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