LEARNING OUTCOMES

The aims of the course are to give to the students the fundamental knowledge on the chemical and physico-chemical characteristics, the strucure-activity-relationship (SAR), the molecular mechanisms of actions and the toxicology of some classes of drugs. In detail, the students will be able to discuss the mechanisms of actions and the SAR of the drugs on the basis of their chemical strucures. The students will be able to describe the synthesis of some drugs.

AIMS AND LEARNING OUTCOMES

The course aims to provide the student with the knowledge of drugs currently in use in hormonal pathologies, CNS,cardivascular, gastrointestinal, respiratory diseases, together with the mechanism of action of the drugs and their toxic effects. Syntheses, structure-activity relationships (SAR), optimization studies and action mechanisms of these therapeutic classes are reported. Furthermore, the course aims to provide students with the basic knowledge useful for design and synthesis of biologically active molecules.

Another fundamental objective of this course is the demonstration of the practical application in the field of pharmaceutical chemistry of all the knowledge acquired by the student during other courses, in particular those relating to general and organic chemistry and biochemistry.

At the end of the course the student will be able to recognize the main drugs of the categories listed in the program, describe their synthesis, structure-activity relationships, know the mechanisms of action and toxic effects.

PREREQUISITES

Knowledge of general inorganic chemistry, organic chemistry and biochemistry.

TEACHING METHODS

Theoretical frontal lessons with the use of slides. 

The slides available as teaching material on Aulaweb and are the basis for detailed explanations by the teacher on the various topics of the course, in particular regarding syntheses and mechanism of action of the discussed drugs.

SYLLABUS/CONTENT

The first part of the course is related to the hormones on the whole (bio-synthesis, physiological role, therapeutic use, synthetic drugs related to them). In particular will be discussed: Calcium homeostasis regulators (parathyroid hormone, bisphosphonates, calcitonine); thyroid hormones (T3, T4), antithyroid drugs; insulin, glucagon, oral hypoglycemic drugs; steroid hormones: mineral- and glucocorticoids, estrogens, antiestrogens, progestins, antiprogestins, contraceptives, androgens, anti-androgens, anabolic steroids.

The second part of the course describes the following therapeutic class: cholinergic, adrenergic and  serotoninergic system drugs; local and systemic anesthetics; hypnotic/sedative drugs; ansiolitics, antipsycotics, anticonvulsants, muscle relaxants, antiparkinson drugs, opioids and derivatives, antidepressants, psychotomimetics and other central stimulant drugs; cardiovascular drugs; antihypertensive drugs,  diuretics; antiaggregants, anticoagulants, fibrinolitics; non steroidal antiinflammatory drugs; antihistaminics. As a part of the discussion of the different therapeutic classes are examined: the physico-chemical properties, design strategies, the structure of biological targets and the mechanisms of interaction, the structure-activity relationships. The synthetic methods are reported for:

Protirelin, levothyroxine, sulphonylureas, bisguanides, Carbacol, Betanecol, Fisostigmine, Neostigmine, Piridostigmiea, Ecotiophato, Atropin, Scopolamine, Benztropine, Triesifenidile, Succinilcholine, Pancuronium, Vencuronium, Atracurium, Salbutamol, Lidocaine, Chlordiazepoxide, Diazepam, Bromazepam, Lorazepam, Alprazolam, Triazolam, Aloperidol, Luminal, Valproic ocid, Meprobamate, Levodopa, Heroin, Hydromorphon, Hydrocodeinon, Oxymorphon, Oxycodon, Ethorphine, Buprenorphine, Levorfanol, Butorfanol, Meperidine, Fentanil Methadon, Propoxyphen, Tramadol, Loperamide, Desipramine, Nortriptiline, Imipramine, Amitriptiline, Fluoxetine, Trazodone, Selegiline, Milrinon, Amiodarone, Captopril, Enalapril, Verapamil, 1,4-dihydropiridine, Hydrochlorotiazide, Furosemide, Etacrinic acid, Triamterene, Indomethacine, Diclofenac, Ibuprofen, meclofenamic acid, Piroxicam, Fenbenzamine, Difenidramine, Ciproeptadine, Cetirizine, Cimetidine

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RECOMMENDED READING/BIBLIOGRAPHY

The book suggested is  “Chimica Farmaceutica” Autori Gasco, Gualtieri, Melchiorre, Editore CEA.

Some topics are developed by the teacher on the basis of  specific literature.

Moreover the teacher updates the program, by adding the new drugs, which are launched on the market.