MEDICINAL AND TOXICOLOGICAL CHEMISTRY 1

Alphabetic division AC-DL-MQ-RZ

Course Sheet

Course code:

00201

Academic Year of enrolment:

2020

Year of supply:

2022/2023

Divisions:

Cognomi H-Z

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:

DE FILIPPIS Barbara

Cycle:

Second semester

Obligatory attendance:

Yes

Minimum hours of attendance:

Hours of classroom activity:

Individual study hours:

211

Prerequisites:

The study requires a good knowledge of Organic Chemistry and the fundamental concepts of Physiology and Biochemistry.
In order to understand and be able to apply most of the topics described in the course, it is necessary to have successfully passed the exam in Organic Chemistry and Biochemistry. The topics covered in the course require a good knowledge of protein structures, of the main types of inter and intramolecular interactions, the main chemical-physical parameters that characterize a drug. A good knowledge of these issues is an important prerequisite for the student who wants to take the course profitably.
Preliminary examinations: Organic chemistry and biochemistry

Objectives

The main purpose of the course is to offer an understanding of the chemistry of biologically active molecules and the way in which they perform their biological action. Pharmaceutical chemistry explores the mechanisms of action at the molecular level, the chemical-toxicological aspects, the chemical-physical properties and the structure-activity relationships of the main classes of drugs active at SNC and peripheral level.
Understanding of the structure-activity relationship and analysis of some parameters (hydrophilic / lipophilic ratio, chirality, metabolism, pharmacophoric units) essential for the pharmacodynamics, pharmacokinetics and bioavailability of a drug.

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 medicinal chemistry and pharmaceutical research. Main stages of development of a drug.
Classification of drugs based on activity: drugs structurally specific and non-specific.
Receptor theory: ligand binding sites; receptor-ligand interactions; type of ligand-receptor interactions; kinetic aspects of ligand-receptor interactions; affinity, efficacy, agonisn, competitive and non-competitive antagonism, dose-response curves.
Chemical and physical properties and biological activity: receptors as recognition entities, affecting factors, solubility, ripartition coefficient, ionization and activity; absorption, distribution, elimination of drugs.
Structural features and biological activities of drugs: critical distances, intermolecular distances, intramolecular distances, space structural of molecole: geometric, optical, conformational isomerism; electronic distribution, vinylogy, mesomery. Homology, isostery and bioisostery.
Drug metabolism: I and II type metabolic reactions. Prodrugs.
Drug nomenclature: Nomenclature and numeration of heterocyclic compounds; ATC classification.

SYSTEMIC SECTION
Brief introduction of Central Nervous System: nervous fibers, electrical transmission of nerve impulse, synaptic impulses, neurotrasmitters.
Classification of drugs affecting the Autonomic Nervous System
Drugs of Adrenergic neurotrasmission: biosynthesis and catabolism of catecholamines; sympathetic drugs with direct and indirect action, agonists and antagonists on  and - adrenergic receptors: structural and activity relationship.
Drugs affecting Cholinergic neurotrasmission: biosynthesis and catabolism of acetylcholine; muscarinic and nicotinic receptors. Cholinergic drugs with direct or indirect actions; anticholinesterase drugs; reversible and irreversible inhibitors; natural and synthetic anticholinergics. Ganglion and neuromuscular blocking agents.
Classification of Drugs Central Nervous System.
The main neurotransmitters in the CNS: GABA and glutamic acid.
Depressants
S.N.C.: General anesthetics: stages of anesthesia, volatile anesthetics and intravenous, mechanism of action and toxicity.
Sedative-hypnotics: fundamentals of the physiology of sleep, hypnotic ideal, general structures of hypnotics. Barbiturates: physical-chemical properties and structure-activity relationships, hypnotic benzodiazepines, non-benzodiazepine hypnotics, agonists of melatonin receptor.
Anticonvulsant: main forms of epilepsy, general formula and structure-activity relationships of anticonvulsants. Drugs acting on the GABAergic system.
Opioid analgesics: morphine analgesic and structure of basic receptors painkillers, endorphins. Major classes of opioid analgesics. Morphine-antagonists. Antitussive and antidiarrheal.
Minor tranquilizers: anxiolytics: benzodiazepines, SAR, GABAA receptor. Non-benzodiazepine anxiolytics.
Major tranquilizers: tricyclic neuroleptics, butyrophenones and diphenylbutylpiperidine; atypical neuroleptics.
Local anesthetics: cocaine, the general formula of local anesthetics, electronic distribution and anesthetic activity; main classes of amide and ester compounds.
CNS stimulants: Analeptics; xanthines; nootropic. Psychodysleptics: phenylethylamine derivatives, indole, cannabinoids.
Antidepressants: tricyclic compounds, monoamine reuptake inhibitors and non-selective; MAO inhibitors. Second-generation antidepressants: SSRIs, SNRIs, SARI, NaSSA, DNRI.
Anorectic drugs: amphetamine and derivatives.
Antihypertensive drugs: drugs acting on the adrenergic system; ganglion, peripheral vasodilators. Antianginal: organic nitrates.
Drugs of the histaminergic system: biosynthesis and metabolism of histamine, the chemical properties and biological role of histamine, receptor subtypes. Anti-H1 of the first generation and second generation. Anti-H2.
Drugs acting on the serotonergic system: biosynthesis and metabolism of serotonin, serotonin receptors and their ligands. Anti-migraine triptans. 5-HT3 receptor antagonists.
Parkinson's disease: etiology, theory neurotoxic, biosynthesis and metabolism of dopamine, dopaminergic therapy, enzyme inhibitors, anticholinergic therapy.
Alzheimer's disease: etiology, treatment approaches. Acetylcholinesterase inhibitors and glutamate antagonists.
ADHD: etiology, treatment approaches.
SLA and Multiple Sclerosis: etiology and treatment approaches

Recommended Bibliography

- Foye: Principi di Chimica Farmaceutica; V Edizione ital. a cura di Dall’Acqua e Caffieri. Piccin, Padova
-G. L. Patrick: Introduzione alla Chimica Farmaceutica; II edizione, EdiSES, Napoli
- Gasco, Gualtieri, Melchiorre; Chimica Farmaceutica, II edizione, CEA

Teaching Methods

Frontal lessons with the aid of multimedia supports. During the course, the teacher checks the students' ability to know about the topics proposed through self-assessment tests to be carried out independently or in a group comparison. This has no impact on the final evaluation of the student but aims to monitor and accompany the student to a methodical and continuous study throughout the course.

Evaluation methods

Verification of learning:

The final evaluation consists of a written exam and an oral exam. The written test consists of a multiple-choice test and requires the writing of molecules and biosynthetic schemes. The student must answer 10 questions in a maximum time of one hour. For each complete answer, a score of 3 is associated. The type of questions (open answer or multiple answer) is intended to cover the entire program carried out and to verify the level of learning achieved, the ability to correctly apply the acquired knowledge, the ability to process independent judgment solutions and the ability to communicate in a written way. The exam is completed with an oral exam aimed at confirming the student's level of learning and the ability to argue written answers. The oral exam focuses on topics related to the entire program. The student must demonstrate his knowledge of the chemical structures and chemical properties of drugs, the drug target and the pathology for which the drugs are used.

Contacts/More Information

Università degli Studi
"G. d'Annunzio"

Chieti - Pescara

Aree