Ateneo - UPO

• Drugs acting on the eicosanoids system
• Drugs acting on the steroid hormones system: glucocorticoids
• Diuretic drugs
• Lipid lowering drugs
• Drugs acting on the istaminergic system. H1and H2-Antihistaminics and other ulcer medications
• Drugs acting on the CNS: anesthetics, anti-anxiety drugs, sedative-hypnotics, anticonvulsivant drugs, opioid analgesics, neuroleptics, antidepressants, antiParkinson and antiAlzheimer drugs
• Drugs acting on the adrenergic system. Nasal decongestants.
• Antitussive drugs and bronchodilators
• Antihypertensive drugs
• Drugs for thyroid disorders.

1) Foye-Lemke-Williams: Principi di Chimica Farmaceutica; Casa Editrice Piccin.
2) Gasco, F. Gualtieri, F. C. Melchiorre: Chimica Farmaceutica; Casa Editrice Ambrosiana.
3) G. Costantino, G. Sbardella, Chimica Farmaceutica, EdiSES

By the end of the course, the student should gain a good understanding of the aspects dealing with the mode of action of drugs. During the course the principal drug families will be addressed: their structure-activity relationships, therapeutical indications, and their related metabolic and chemical-toxicological aspects should be known by the students.

Preparatory exam: Pharmaceutical Chemistry 1
The course is based on the assumption that students have knowledge in organic chemistry and biochemistry.

During the lessons all the different drugs classes will be addressed, from a medchem perspective, including the structures, the SAR and the relative mechanism of action; moreover, the main aspects of the metabolic fate of the drugs were treated highlighting in particular the formation of reactive and toxic species.

Students with physical disabilities, Learning Disabilities or Special Education Needs can request specific services and tools via the Staff Sviluppo e Coordinamento Carriere e Servizi alle Studentesse e agli Studenti, consulting the University webpage: https://www.uniupo.it/en/services/services-students-physical-or-learning-disabilities

Students with disabilities, learning disabilities or special education needs, once they have contacted the University Staff, can refer to the tutor in charge of the course to define the examination modalities, concerning academic aspects.

The assessment consists of a written test and an oral examination. The written test in consists of 25 questions (1 point each) and lasts 1 hour. In the questions, the identification of the structural formula, the mechanism of action and the therapeutic indication of drugs are generally required. Where applicable, the metabolic pathways of the drugs and SAR, may also be asked. The oral part can be done only if the score of the written test is equal/higher than 15. The oral part is a presentation supported by slides and following discussion on a drug chosen by the student among (or also beyond) the drugs addressed during the course. The oral part is worth 0-7 points that are added to the score of the written part. The oral part is sufficient only when the score is at least 3.

Arachidonic acid cascade: prostaglandins, thromboxanes and leukotrienes. Non steroidal antinflammatory drugs: mode of action, SAR, pharmacological profile, (COX 1 and COX 2 selectivity) and main aspects of their metabolism. Anti-inflammatory corticosteroids. Calcium antagonists. Diuretics: classification of drugs, structures and mechanism of action. Lipid lowering drugs: blood lipoproteins and cholesterol biosynthesis. Statins: mechanism of action, SAR. Fibrates. Antihistaminics: histamine; H1 antagonists. H2 antagonists: proton pump inhibitors, structures and activation mechanism. Other anti-ulcer drugs. Drugs acting on the CNS. General anesthetics: gaseous, volatiles and intravenous (modes of action). Sedative-hypnotics: structures and mechanism of action and SAR: barbiturates, chloral hydrate; benzodiazepines. Antihepileptic drugs. Opioid analgesics: peptidergic transmission. Morphine: mode of action, therapeutic use, SAR; partial agonists and antagonists. Neuroleptics: dopamine and its receptors; phenothiazines, thioxanthenes, butyrophenones. Antidepressants: MAO irreversible and reversible inhibitors: mechanism of inhibition. Serotonin cycle. Reuptake inhibitors (serotonin and other neurostransmitter): tricyclic antidepressants endowed with 6,6,6 and 6,7,6 cycle (structure, mode of action). Anti Parkinson drugs: levodopa and DOPA-decarboxylase inhibitors, COMT inhibitors, MAO inhibitors; dopamine receptor agonists. AntiAlzheimer drugs. Epinephrine and norepinephrine biosynthesis and metabolism. -agonists and antagonists. Non selective -agonists and 2- selective agonist. - non selective antagonists and selective 1-antagonists. Antitussive, antiasthma and bronchodilator drugs: structures and mechanism of action. ACE inhibitors and antihypertensive drugs. Local anesthetics: structures and mechanism of action. Drug for thyroid disorders.

At the end of the course the student will know the structures, the mechanism of action and the structure-activity relationship of the classes of drugs included in the program. In addition, the student will also know the aspects related to the metabolism of drugs, with particular regard to the cases in which it is associated with the adverse effects.