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PHARMACEUTICAL AND TOXICOLOGICAL CHEMISTRY II

Academic year and teacher
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Versione italiana
Academic year
2022/2023
Teacher
REMO GUERRINI
Credits
9
Didactic period
Primo Semestre
SSD
CHIM/08

Training objectives

Training objectives
Knowledge about the different drug classes and their synthetic approaches limited to some selected molecules. Knowledge about drug –target interactions with particular emphasis to G-protein coupled receptors, enzymes, transport proteins and ionic channels. Understanding of the structure-activity relationship and analyses of some parameters (i.e. hydrophilic/lipophilic balance, chirality, metabolism, pharmacophore units) essential for the pharmacodynamics, pharmacokinetics and bioavailability of drugs. These information are necessary to develop skills useful for discovery and production of novel drugs.

Prerequisites

Prerequisites

Advanced Organic Chemistry (obligatory); Pharmaceutical and Toxicological Chemistry I (suggested); Biochemistry (suggested); Physiology (suggested); Pathology (suggested); Pharmacology (suggested).

Course programme

Course Syllabus
Drugs for the Cholinergic system: agonists and antagonists for the muscarinic and nicotinic receptors. Reversible and irreversible acetylcholinesterase inhibitors. Neuromuscular blockers. Adrenergic drugs: agonists and antagonists for the alpha and beta receptors. Nasal decongestants, bronchodilators, antihypertensive drugs, alpha1 blockers to treat benign prostatic hypertrophy. Serotoninergic drugs: antimigraine; antiemetics; prokinetic agents. Antidepressant drugs: MAO and COMT inhybitors; Thymoleptics; Catecholamine Reuptake Inhibitors. Drugs for the GABA and Glutamate receptors: barbiturates; benzodiazepines; anticonvulsant. Drugs for the dopaminergic system: antiparkinson and antipsychotics. Antiistamine drugs: Antiallergic, Antiasthmatic, Antiulcer. H+/K+ ATPase inhibitors. Vascular resistance and Vasodilators: renin-angiotensin system; nitric oxide; phosphodiesterase inhibitors; endothelin receptor antagonists; calcium channel blockers. Antiarrhythmic agents. Non steroidal anti inflammatory drugs. Prostaglandin analogues and leukotriene receptor antagonists. Narcotic analgesics and anti cough.

Didactic methods

Didactic methods
Frontal teaching will be performed using the blackboard together with the support of multimedial systems to describe in details drug-target interactions. The students will be involved in a feed-back discussion during the teaching lecture, to stimulate their attention and participation and to underline the most difficult arguments that must be analyzed and understood.

Learning assessment procedures

Learning assessment procedures
The learning validation is based on two stages: firstly the continuous monitoring during the teaching course. The teacher verifies the knowledge capability of the students regarding the proposed topics. This happens through easy questions in a friendly feed-back manner that has no impact on the student final evaluation. Secondly the student’s oral evaluation on at least three drug classes or three drugs. The student must demonstrate his/her knowledge about chemical structures and chemical properties of drugs, the pharmacological target and the pathology for which the drugs are employed. The student must know the synthetic path of a limited number of compounds and must be able to relate the pharmacological activity (potency, efficacy, selectivity and toxicity) with the chemical structure of the drugs.

Reference texts

Reference texts
Graham L. Patrick, Chimica Farmaceutica (edizione integrata a cura di Gabriele Costantino) III Edizione, EdiSES.
FOYE’S: Principi di Chimica Farmaceutica, Piccin Editore, Padova. Chimica Farmaceutica (A. Gasco, F. Gualtieri, C. Melchiorre) Casa Editrice Ambrosiana.