MEDICINAL AND TOXICOLOGICAL CHEMISTRY 1

Alphabetic division AC-DL-MQ-RZ

Course Sheet

Course code:

00201

Academic Year of enrolment:

2022

Year of supply:

2024/2025

Divisions:

Cognomi A-G

Type of Course:

Characterising

Degree:

Course of Single Cycle Degree 5 years in PHARMACY

Disciplinary Sector:

Pharmaceutical Chemistry

Is part of:

MEDICINAL AND TOXICOLOGICAL CHEMISTRY 1

Location:

CHIETI

Credits:

Programme Year:

Professor and Collaborators:

AMMAZZALORSO Alessandra

Cycle:

Second semester

Obligatory attendance:

Yes

Minimum hours of attendance:

Hours of classroom activity:

100

Individual study hours:

200

Prerequisites:

The Biochemistry exam is preparatory to this course. Students must have a basic knowledge of general and inorganic chemistry (ionization and solubility equilibria), organic chemistry (funtional groups and their reactivity, nomenclature of organic compounds), biochemistry (basic knowledge of proteins and aminoacids).

Objectives

The main goal of this course is the knowledge of chemical aspects of drugs and of their mechanisms of action. Medicinal chemistry deals with mechanism of action of drugs, chemical-toxycological profiles, chemico-physical properties and structure-activity relationships of the major classes of drugs. Main educational goals include the knowledge of the different phases of drug research and development and of pharmacokinetic and pharmacodynamic properties of drugs. The main objective of the systematic part is the chemical knowledge of different pharmaceutical compounds.

Contents

Medicinal Chemistry deals with mechanism of action of drugs, chemical-toxicological profiles, chemico-physical properties and structure-activity relationships of the major classes of drugs.

Extended Syllabus

GENERAL SECTION
Basic principles of pharmaceutical research. Steps in the development of a drug.
Drug-receptor interactions: forces involved, drug-receptor theories, topographical and stereochemical considerations.
Chemico-physical properties and biological activity: solubility, acidity, logP.
Absorption, distribution, and excretion of drugs: routes of administration, factors affecting absorption. Pharmacokinetic and pharmacodynamic considerations.
Drug geometry and biological activity: conformational and configurational stereoisomers.
Drug metabolism: oxidative reactions, reductions, hydrolysis, enzymatic induction, phase I and phase II reactions. Prodrugs and soft drugs.
Drug classification and nomenclature. ATC classification.

SYSTEMATIC SECTION
Drugs acting on autonomic nervous system:
Adrenergic system. Biosynthesis and catabolism of adrenergic neurotransmitters. Adrenergic agonists and antagonists: structure-activity relationships.
Cholinergic system. Biosynthesis and catabolism of acetylcholine. Direct and indirect cholinergic drugs. Acetylcholinesterase inhibitors. Cholinergic antagonists.

Drugs acting on central nervous system
Neurotransmitters in CNS: GABA and glutamic acid.
General anaesthetics: stages of anaesthesia, pre-medication. Anaesthetics for inhalation and intravenous administration. Mechanism of action and toxicity.
Anxiolytics and hypnotics: characteristic phases of the sleep, mechanism of action, barbiturates, analogues of the barbiturates, benzodiazepines, melatoninergic drugs.
Antiepileptic drugs: main types of epilepsy, mechanism of action, barbiturates, hydantoin derivatives, succinimides, benzodiazepines, other compounds.
Opioid analgesics: endogenous peptides, morphine and its derivatives, analgesic receptors. Phenylpiperidines and diphenylpropylamines. Morphine antagonists. Antitussive and antidiarrheal opioids.
Neuroleptics: mechanism of action, phenothiazines, tioxantenes, butyrophenones, atypical drugs.
Local anaesthetics: mechanism of action, cocaine, ester and amide derivatives.
Analeptics, methylxanthines, nootropic drugs. Psychodysleptics.
Antidepressants: mechanism of action, NA and/or 5HT uptake inhibitors, MAO inhibitors, atypical antidepressants.
Anorexiant drugs: amphetamine and its derivatives.

Antihypertensive drugs: adrenergic drugs, peripheral vasorelaxant compounds. Organic nitrates in the treatment of Angina pectoris.
Histaminergic system: biosynthesis and metabolism of histamine. H1 and H2 antihistaminergic drugs: structure-activity relationships.
Serotoninergic system: biosynthesis and metabolism of serotonine. Serotoninergic drugs: triptans and 5-HT3 antagonists.
Dopaminergic system: biosynthesis and metabolism of dopamine.

Drugs used in Parkinson Disease: dopaminergic and anticholinergic therapy. Enzymatic inhibitors: dopa decarboxylase inhibitors, MAO inhibitors, COMT inhibitors.
Drugs used in Alzheimer Disease: aetiology of AD and therapeutic approaches. Acetylcholinesterase inhibitors and NMDA antagonists.
ADHD: aetiology and therapeutic approach.
Drugs for Multiple Sclerosis and Amyotrophic Lateral Sclerosis.

Recommended Bibliography

Chimica Farmaceutica
Alberto Gasco, Fulvio Gualtieri, Carlo Melchiorre
Casa Editrice Ambrosiana

Foye’s Principi di Chimica Farmaceutica
VI Edizione italiana. Piccin, Padova

G. L. Patrick: Chimica Farmaceutica
III Edizione, EdiSES, Napoli

Teaching Methods

The course consists of about 77 hours of frontal lessons and exercises in the classroom, where exercises for the preparation to the written examination will be proposed.

Evaluation methods

Verification of learning:

The learning verification will be made through a written and oral examination. The written exam consists of multiple-choice tests, where chemical formulas and biosynthetic schemes will be required to the students. The oral examination will be focused on all topics covered by the programme. In both examinations, students have to demonstrate a good knowledge of mechanisms of interations of drugs and basic principles of pharmacokinetic and pharmacodynamic. Moreover, students must be able to describe the chemical structure, the mechanism of action and the therapeutic profile of most important classes of drugs.

Contacts/More Information

Università degli Studi
"G. d'Annunzio"

Chieti - Pescara

Aree