CHIMICA FARMACEUTICA II

Pietro CAMPIGLIA CHIMICA FARMACEUTICA II

0760100023
DIPARTIMENTO DI FARMACIA
CORSO DI LAUREA MAGISTRALE A CICLO UNICO DI 5 ANNI
PHARMACY
2015/2016

OBBLIGATORIO
YEAR OF COURSE 4
YEAR OF DIDACTIC SYSTEM 2010
SECONDO SEMESTRE
CFUHOURSACTIVITY
1080LESSONS
Objectives
THE COURSE AIMS TO PROVIDE STUDENTS BASIC KNOWLEDGE ABOUT GENERAL STRATEGIES OF DESIGN, SYNTHESIS, THE STUDY OF THE MECHANISMS AND CHEMICAL-TOXICOLOGICAL ASPECTS AND THE RELATIONSHIPS BETWEEN CHEMICAL STRUCTURE AND BIOLOGICAL ACTIVITY OF DRUGS. FOR THIS PURPOSE, THE CHEMICAL-PHYSICAL PROPERTIES AND STEREO-ELECTRONIC PROPERTIES OF THE DRUGS WILL BE ANALYZED IN A CRITICAL AND PLACED IN RELATION TO THE THERAPEUTIC USE OF THE DRUG. ALSO, IT WILL BE DISCUSSED POTENTIAL STRUCTURAL CHANGES, DICTATED BY METABOLIC PROCESSES THAT ALLOW TO MODULATE THE PROFILE OF A DRUG TO ITS THERAPEUTIC USE. IT IS EXPECTED THAT THE STUDENT ACQUIRES KNOWLEDGE OF THE BASIC CONCEPTS RELATED TO THE STUDY OF THE CHEMICAL AND MOLECULAR DRUGS AND IS ABLE TO DISCUSS THE MECHANISMS OF ACTION AND STRUCTURE-ACTIVITY RELATIONSHIPS BASED ON THE CHEMICAL PROPERTIES OF THE MOLECULES INVOLVED. IT IS ALSO EXPECTED THAT THE STUDENTS ACQUIRE THE NECESSARY ELEMENTS TO DESIGN DRUGS ON A RATIONAL BASIS.
Prerequisites
STUDENTS HAVE TO KNOW ORGANIC AND INORGANIC CHEMISTRY, BIOLOGY, BIOCHEMISTRY, ELEMENTS OF ANATOMY AND PHYSIOLOGY.
Contents
PART I: PRINCIPLES OF DRUG DISCOVERY
DRUGDISCOVERY FROM NATURAL PRODUCTSDRUG DESIGN AND RELATIONSHIP OF FUNCTIONAL GROUPS TO PHARMACOLOGIC
ACTIVITY .MOLECULARMODELING .RECEPTORS AND DRUG ACTION
PART II: DRUG RECEPTORS AFFECTING NEUROTRANSMISSION AND ENZYMES AS CATALYTIC RECEPTORS
DRUGSAFFECTINGCHOLINERGICNEUROTRANSMISSION. ADRENERGIC RECEPTORS AND DRUGS AFFECTING ADRENERGIC
NEUROTRANSMISSION .SEROTONIN RECEPTORS AND DRUGS AFFECTING SEROTONERGIC NEUROTRANSMISSION .
AMINO ACID NEUROTRANSMITTERS IN THE CENTRAL NERVOUS SYSTEM . INHIBITORS OF NERVE CONDUCTION:
LOCAL ANESTHETICS .PHOSPHODIESTERASEINHIBITORS
PART III: PHARMACODYNAMIC AGENTS
SECTION 1: DRUGS AFFECTING CENTRAL NERVOUS SYSTEM
GENERAL ANESTHETICS. SEDATIVE-HYPNOTICS. ANTISEIZURE AGENTS . ANTIDEPRESSANTS. PSYCHOTHERAPEUTIC DRUGS:
ANTIPSYCHOTIC AND ANXIOLYTIC AGENTS .HALLUCINOGENS, STIMULANTS AND RELATED DRUGS OF ABUSE OPIOIDANALGESICS.
DRUGS USED TO TREAT NEUROMUSCULAR DISORDERS: ANTIPARKINSONIAN AND SPASMOLYTIC AGENTS
SECTION 2: DRUGS AFFECTING THE CARDIOVASCULAR SYSTEM
CARDIAC AGENTS: CARDIAC GLYCOSIDES, ANTIANGINAL, AND ANTIARRHYTHMIC DRUGS . DIURETICS. ANGIOTENSIN
CONVERTING ENZYME INHIBITORS, ANTAGONISTS AND CALCIUM BLOCKERS .CENTRAL AND PERIPHERAL SYMPATHOLYTICS
AND VASODILATORS .ANTIHYPERLIPOPROTEINEMICS AND INHIBITORS OF CHOLESTEROL BIOSYNTHESIS

Teaching Methods
LECTURES
Verification of learning
WRITTEN EXAMINATION INTRODUCTION TO THE ORAL INTERVIEW
Texts
D.A. WILLIAMS, T.L. LEMKE, FOYE’S PRINCIPI DI CHIMICA FARMACEUTICA, PICCIN.
• G.L. PATRICK, INTRODUZIONE ALLA CHIMICA FARMACEUTICA, EDISES, II EDIZIONE
• WILSON&GISVOLD CHIMICA FARMACEUTICA .ED.CEA
• T. NOGRADY, D. WEAVER, MEDICINAL CHEMISTRY – A MOLECULAR AND BIOCHEMICAL APPROACH, 3RD ED., OXFORD UNIVERSITY PRESS.
• MONOGRAFIE DELLA COLLANA "CHIMICA DEI RECETTORI", EDITORE C. MELCHIORRE, CLUEB (BOLOGNA).
• C. WERMUTH, LE APPLICAZIONI DELLA CHIMICA FARMACEUTICA, EDISES.
• P. KROGSGAARD-LARSEN, T. LILJEFORS, U. MADSEN ED., TEXTBOOK OF DRUG DESIGN AND DISCOVERY, TAYLOR & FRANCIS.
• GOODMAN & GILMAN'S THE PHARMACOLOGICAL BASIS OF THERAPEUTICS, TWELFTH EDITION, MCGRAW-HILL
MEDICAL PUBLISHING DIVISION (2011).
• WILSON AND GISVOLD'S TEXTBOOK OF ORGANIC MEDICINAL AND PHARMACEUTICAL CHEMISTRY-LIPPINCOTT WILLIAMS & WILKINS
• KLEEMANN, ENGEL, KUTSCHER, REICHERT, PHARMACEUTICAL SUBSTANCES, 5TH ED., THIEME VERLAG.
• BURGER’S MEDICINAL CHEMISTRY, DRUG DISCOVERY AND DEVELOPMENT. 7TH EDITION. WILEY. JOURNAL OF MEDICINAL CHEMISTRY, ACS.
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