Name of Ag.Head Of Deparment:Dr. Rosa O. Johnson-Ajinwo

COURSE DESCRIPTION FOR PHARMACEUTICAL & MEDICINAL CHEMISTRY

YEAR TWO  FIRST SEMESTER

PCH 221.1:    Pharmaceutical Chemistry I (Physical and Inorganic Pharmaceutical Chemistry)    3 Units (45 hours)

Introduction and relevance to pharmacy;

Inorganic Chemistry: Atomic and molecular structure; Periodic table and electronic configuration of elements; Consideration of properties (including storage, Limit test, assay, uses) of inorganic compounds and elements of pharmaceutical importance; coordinate compounds and the importance of metal ions in biological and pharmaceutical systems.

Physical Chemistry:  Principles of thermodynamics, solutions (including solubility and distribution of pharmaceutical solutions); chemical/reaction kinetics, phase equilibrium study of multi component systems and applications in partition and absorption chromatography. Electrochemistry: chemical and ionic equilibra; (including dissociation constants of acids and bases; preparation and mechanism of buffering actions, Henderson-Hasselbalch equation, e.t.c); pharmaceutical electrolytes.

• Radioisotopes, types and sources of radioactive decay; detection and measurement radioactivity; Diagnostic radionuclides; Applications, uses and disposal of pharmaceutically important radioisotopes.

PHA 233.1:  Biochemistry for Pharmacy Students I (Theory & Practicals)       Units: 3   (45 hours)

Acids, bases and buffers

Chemistry of amino acids, proteins and their derivatives; Functions, methods of isolation and identification; Primary, secondary, tertiary and quaternary structures of proteins; Determination and biochemical importance of the structures.

Chemistry and structures of carbohydrates; their nomenclature.

Vitamins and minerals.

YEAR TWO              SECOND SEMESTER

PCH 222.2:                Practical Pharmaceutical Chemistry I  1 Unit (45 hours)

At least 10 practicals to illustrate and complement the theoretical principles involved in PCH 221.1 and 223.2

PCH 223.2:    Pharmaceutical Chemistry II (Pharmaceutical Organic Chemistry) 2 Units (30 hours)

Introduction and relevance to pharmacy

Fundamental concepts in organic chemistry: Bonding, Structure and reactivity of organic compounds; Hybridization, resonance, Inductive, mesomeric, delocalization, aromaticity and electronic effects, types of organic reactions.

Survey of Classes of organic compounds: Concept of functional group and nomenclature of organic compounds with examples of pharmaceutical important compounds in each class.

Stereochemistry and shapes of organic compounds: Isomerism- structural and stereochemical; optical activity and measurement; Geometry of alkenes and aromatics; Naming & Resolution of stereoisomers; medical examples of Cis/Trans and E/Z Isomers; Biological/pharmaceutical applications of Isomers; Enantiopure medications, etc.

PHA 236.2:    Biochemistry for Pharmacy Students II                 3 Units (45 hours)

Amino acid, carbohydrate and lipid metabolisms.

Nucleosides, nucleotides and nucleic acids; Classification of viruses based on the manner of gene expression (TMV, T₄ phage, Tumour viruses, e.t.c.)

Enzymes: Structures and functions; Simple kinetics of enzyme-catalyzed reactions; Specific enzymes and their functions; Clinical applications of enzymes.

Water and mineral metabolism; Acid-base control; Disturbance of acid-base control; Renal function and composition of urine.

Laboratory practicals to illustrate some of the topics covered above.

YEAR THREE         FIRST SEMESTER

PCH 321.1:    Pharmaceutical Chemistry III (Advanced Pharmaceutical Organic Chemistry) 2 Units (30 hours)

Aromatic compounds: (Chemistry, properties and pharmaceutical importance) Benzene, anthrancene, phenanthrene, naphthalene and their derivatives; alcohols, phenols, arylhalides, e.tc; Use of active methylene groups in synthesis.

Named organic synthetic reactions and reaction mechanisms of pharmaceutical importance.

Organometallic compounds: Grignard reagents; preparation, reactions and pharmaceutical uses.

Heterocyclic Chemistry: Nomenclature, properties, reactions of the following class of compounds: furans, thiophenes, pyroles, pyridine Isoquinolines, quinolines, etc. Heterocyclic rings with more than one heteroatom.

PCH 322.1: Practical Pharmaceutical Chemistry II          1 Unit

Laboratory classes in application of selected synthetic methods to the synthesis of pharmaceutical

agents, selected clinical assay procedures. This will include qualitative analysis of organic

compound preparation of their derivatives and photochemical methods used in drug synthesis

PCH 323.1:    Pharmaceutical Analysis I (Basic & Electroanalytical Methods) 2 Units (30 hours)

Basic Methods of Analysis: Aqueous and non-aqueous, acid base, redox and complexometric titrations; gravimetric analysis, etc.

Polarimetry and Refractometry: Principles and applications in pharmacy.

Electroanalytical Methods:  polarography (principles and applications in pharmacy); Amperometric titrations, conductimetric and potentiometric titrations (with emphasis on their applications in pharmacy).

YEAR THREE SECOND SEMESTER

PCH 324.2: Medicinal Chemistry I (Introduction to Medicinal Chemistry) 2 Units (30 hours)

Natural Products:  Introduction to natural products of pharmaceutical/Medicinal importance e.g. Glycosides, Amino Acids, steroids, Vitamins, purines, xanthines, terpenes, e.t.c

Photochemistry: General principles, characteristics and fate of excited species with emphasis on their synthetic applications and relevance to drug product stability, photostability testing of drugs and selected photochemical processes of biological interest e.g. vision, bioluminescence, vit. D, photosynthesis, e.t.c

Physicochemical principles of Drug action and Receptor Site Theories: Physicochemical factors which affect drug action (e.g. Pka, Ionization, dissociation, etc) and drug-receptor theories.

YEAR FOUR                        FIRST SEMESTER

PCH 421.1:    Pharmaceutical Analysis II (Instrumental Methods of Analysis) 2 Units (30 hours)

Principles of Chromatography:  (TLC, GC, HPLC) Applications in pharmaceutical analysis.

Molecular spectroscopy:  Instrumentation, Principles and analytical applications (IR, UV-Vis).

NMR and Mass Spectroscopy:  Instrumentation, Principles and analytical applications.

Atomic Absorption Spectroscopy: (Atomic absorption and emission, flame photometry) Principles and applications.

Fluorescence Spectroscopy:  Instrumentation, Principles and analytical applications.

PCH 422.1:    Practical Pharmaceutical Analysis  1 Unit 45 hours)

Laboratory practicals to illustrate the analytical methods used in drug analysis. It will involve chromatographic and spectroscopic characterization of pharmaceuticals.

YEAR FOUR                        SECOND SEMESTER

PCH 423.2:    Medicinal Chemistry II (Chemistry of the Pharmacodynamic Agents) 3 Units (45 hours)

Specific examples from each of the following classes of drugs will be studied with special emphasis on: Development from natural products (where appropriate), nomenclature, physical and chemical properties, Structure-Activity Relationships, Synthesis (where necessary), assay, Metabolism (where applicable), uses and chemical stability:

Drugs acting on the CNS: General anesthetics, Sedative- hypnotics, anticonvulsants, tranquilizers, Antidepressants.

Drugs acting on the cardiovascular systems: Antihypertensives and Diuretics

Analgesics: Narcotics and Antipyretics including NSAIDs.

Drugs acting on the ANS:  The sympathomimetic amines, antihistamines (including the development of antagonists at H₁ and H₂ receptors).

Vitamins and steroids (including the steroid hormones).

PCH 424.2:    Practical Medicinal Chemistry         1 Unit (45 hours)

Synthesis of simple pharmaceutical compounds representing different types of reactions. This will involve the use of selected synthetic methods in medicinal chemistry as well as selected assay procedures.

YEAR FIVE  FIRST SEMESTER

PCH 521.1:    Medicinal Chemistry III (Chemotherapeutic Agents & Drug Design) 2 Units (30 hours)

The following classes of drugs (with common examples) will be studied with respect to: Nomenclature, physicochemical properties, stereochemistry, synthesis (where necessary), Structure Activity Relationship, metabolism and uses:-

Sulphonamides and Antibiotics; Antiprotozoals (Antimalarials, Antihelmintics, Trypanocides, Schistosomicides & Amoebicides); Anticancer and Antiviral Agents (with emphasis on drugs used for HIV/AIDS treatment).

Drug design:  Principles of drug development and design; Approaches to drug design, historical background: The concept of isosterism as a tool in drug design, SAR in drug design; antimetabolite and pro-drug approach to design new drugs.

YEAR FIVE 2ND SEMESTER

PCH 523.2:    Drug Metabolism and Analysis        2 Units (30 hours)

Introduction (Drug bioavailability; Drug absorption, distribution, metabolism and elimination).

Drug metabolic reactions: phases, sites and enzymes involved; first-pass metabolism.

Toxicity of drug metabolites.

Factors influencing drug metabolism: stereochemistry, physiological factors, etc.

Applications of chemical, physicochemical and biopharmaceutical analytical methods in identification and quantification of drugs & drug metabolites.

PHA 502.2:    Project            6 Units

Each student is expected to carry out an individual research project of choice supervised by an academic staff.

Such project will be assigned at the beginning of the final year (500 levels).

The research result is presented, bound for grading after a project seminar presented by each student.