PHARMACEUTICAL AND TOXICOLOGICAL CHEMISTRY I
Academic year and teacher
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- Versione italiana
- Academic year
- 2022/2023
- Teacher
- ROMEO ROMAGNOLI
- Credits
- 9
- Didactic period
- Primo Semestre
- SSD
- CHIM/08
Training objectives
- The main objective of the course is to provide students with basics to learn about the various classes of drugs today in therapy and the related preparation by the modern synthetic methodologies. The classification is based as therapeutic groups as well as chemical class of substances.
The objective of the first part of the course is the knowledge of the nature of the interactions of drugs and their biological counterparts, the Research and Development (R&D) process, the significance of biosisoterism and the importance of prodrugs. The objective of the special part is knowledge the different classes of anti-infective drugs, anti-cancer drugs, prostanoic acid derivatives, main diuretic substances, molecules reducing blood sugar levels, steroid hormones, anti-inflammatory steroid-like structures.
Students must acquire a versatile scientific mindset that enables them to address the problems associated with the
research, development, use and control of drugs and health products, making use of all information sources
available, to solve them effectively and in an original way. They will also be able to develop and / or apply ideas or procedures
innovative in the field of pharmaceutical research and design. CTF students will be able to apply the baggage of
regulatory knowledge required in the professional fields of patenting new drugs and business management
pharmaceutical and hospital pharmacies, public and / or private. Prerequisites
- Organic e biological chemistry background.
Course programme
- General Introduction.
Chemistry and drugs. The discovery of drugs, Research and Development (R&D) process . Stereochemistry and biological activity. Metabolism of drugs .Bioisosterism. Classical and nonclassical bioisosters. Examples of bioisosteric analogs.Prodrugs. General aspects. Examples of prodrugs.
Second Part.
Antibacterial antibiotics. General aspects and classification. ß-Lactam antibiotics: penicillins, carbapenems, cephalosporins, monobactams. Macrolide antibiotics, polyenes and antifungal antibiotics. Polypeptides. Aminoglycoside antibiotics. Tetratracyclins. Phosphonates.Antibacterial Chemotherapeutics. Sulfonamides and quinolones as antibacterial agents. Nitrofurans and nitroimidazoles. Dihydrofolate reductase inhibitors.Antiprotozoal agents. Chincona alkaloids and analogs. Sulfamides and sulfones. Antibiotics as amebicides. Antitumor drugs. DNA-interacting drugs. DNA alkylators. Antimetabolites. DNA-intercalators. Platinium complexes. Antimitotic agents. Antiviral Agents. Pyrimidine and purine nucleosides and nucleotides and structural analogs. Drugs active on DNA viruses. Drugs anti-AIDS. Steroids hormones. Estrogens, progestins, androgens, glucocorticoids and mineralcorticoids. Diabetes Therapy. Insulin, sulfonylureas, biguanides.Diuretic agents Carbonic-anhydrase inhibitors Thiazides and hydrothiazides. Carbonic diuretics. Potassium-sparing diuretics.
Eicosanoids: prostaglandins, thromboxanes and leucotrienes. Didactic methods
- Lectures on all the topics of the course.
During the lessons students are asked to repeat the topics covered, trying to highlight the parts that are more difficult to be understood. In addition, students can partecipate to meetings , outside of the canonical lectures, to review the parts that still require further study. Learning assessment procedures
- The goal of the final examination test is to verify the level of achievement of the objectives of the course.
The student will be submitted to a written test followed by an oral test. In the written test, the student must answer to five questions related to questions on the synthetic procedure for the preparation of several drugs as well as to five questions on mechanism of action and structures of different classes of compounds. The answers are open and has to be synthetic but exhaustive.
Both in oral and in writing examination student must demonstrate knowledge of the mechanisms of interaction of drugs and enzymes which are targets of the drugs. Students must demonstrate knowledge of the basic concepts of pharmacokinetics, bioavailability and the nature of pro drugs.
Regarding the special part, student must know the structure, the mechanism of action and therapeutic use of the most important drugs treated. Reference texts
- "Principi di chimica farmaceutica" (Foye's).
