Aims

To introduce the principles of toxicology and drug and toxin metabolism; to equip students with a knowledge and understanding of the mechanism of toxicity of a range of chemicals encountered in the environment and workplace.

To introduce the basic concepts of the aetiology of cancer and pathogenic disease; to impart an understanding of the host-pathogen relationship, and the concepts of selective toxicity and resistance; to equip students with an understanding of the basic principles of chemotherapy of cancer and infectious disease; to provide an understanding of the molecular mechanisms underpinning the action of anticancer and anti-infective drugs.

Outline Of Syllabus

Pharmacokinetics and Drug Metabolism
Principles of pharmacokinetics
Processes and mechanisms of drug metabolism
Selected case studies in drug metabolism

Toxicology
Principles of Toxicology and toxicokinetics
Critical toxicological issues for drug discovery
Allergens and reactive metabolites
Ion channels – hERG and acetyl choline signalling
Carcinogenesis and Oxidative Stress

Basic Principles of Enzymology
Overview of the role of amino acid side-chains, metal ions and coenzymes in catalysis
Characteristics of enzymes: stability, substrate specificity, stereospecificity,
catalytic groups, factors affecting catalysis, enzyme kinetics
Overview of selected enzyme mechanisms
Model systems for enzymes (probing proximity effects, solvation, strain), acid-base
and nucleophilic catalysis

Cancer Chemotherapy
Introduction to cancer
Cytotoxic chemotherapeutic agents: DNA reactive drugs, antimetabolites, topoisomerase
inhibitors, mitotic poisons
DNA Repair Enzymes
Antiendocrine drugs
Current approaches to cancer chemotherapy
New therapies: Targeting receptor tyrosine kinase signalling and kinase inhibitors case
studies

Chemotherapy of Infectious Diseases
Introduction and historical overview
Principles of antimicrobial chemotherapy
Antibacterial agents: β-lactam antibiotics, glycopeptides, quinolones,
oxazolidinones, macrolides
Antifungal agents: polyene macrolides, azoles, allylamines
Antiprotozoal agents (antimalarials: quinine and synthetic analogues, artemisinin; metronidazole)
Antiviral chemotherapy: drugs against Covid-19, neuraminidase inhibitors (influenza), chain terminators (e.g. acyclovir), drugs for HIV (reverse transcriptase and protease inhibitors)


Laboratory
Synthesis of a variety of antibacterial and antifungal drugs with further
investigation of their physicochemical properties

Teaching Rationale And Relationship

Students acquire an understanding of the subject through attendance and participation in online lectures. An understanding of the topics is reinforced by problem solving, and critical background reading of the scientific literature.

In practical classes competencies in practical procedures, observation, record-keeping and report writing, will be taught and learnt.

Assessment Rationale And Relationship

The alternate online assessment will assess the student's knowledge and understanding of the basic principles of the subject as well as the information literacy in the context of chemical toxicology and written presentation skills.

The laboratory component practical involves the assessment of a diverse selection of skills learnt in about 4 experiments per student, spread over the major areas of medicinal chemistry.

Students are required to obtain at least 35% in the laboratory component in order for the examination mark to be included in the final module mark. Students who score <35% in the laboratory will obtain a module mark based solely on the laboratory practical.

Study Abroad students may request to take their assessment before the semester 1 exam period, in which case the format of the paper may differ from that shown in the MOF. Study Abroad students should contact the school to discuss this.