Knowledge Objectives for Chemotherapy SectionFall Semester 2011Selective Toxicity Refer to your handout and know:Definitions (Chemotherapy, Selective Toxicity, Chemotherapeutic Index)General bases for selective toxicityThe table in the handout summarizes the important ones for the drugs we are presentingGeneral bases for drug resistance (again summarized in handout)How R-factor plasmids workHow environmental antibiotics encourage the development of multiresistant microorganismsSulfonamides and Quinolones Sulfonamides:Know the basic sulfonamide structure and how it relates to PABAKnow in a general way the folate synthesis pathway, and where it is affected by sulfonamidesand trimethoprimKnow why they are selectively toxic to microorganismsKnow important factors of disposition, i.e. : rapid absorption, high degree of plasma proteinbinding, metabolism by acetylation, renal elimination.Know major toxicities and side effects (especially hematological and dermatological)How do bacteria become resistant?Compare mechanism of action of trimethoprim to that of SA'sWhat combinations are used?Why is this an effective combination?Know the major differences between short acting vs. long acting SA’s (disposition, toxicity)Know names of 4 major short acting and 1 long acting sulfonamideWhen would non-absorbable SA's be used?Know major uses for bacterial and non-bacterial infectionsQuinolones (oxacin drugs)What is their common structural feature?How do they work?Why are they selectively toxic?What side effects are known?What is their general clinical usefulness?Antibiotics.1. Know the components of bacterial cell wall, basic processes of cell wall synthesis andmaintenance, and basic processes of bacterial protein synthesis.2. Know the mechanisms of antimicrobial activity for:penicillins, cephalosporins, bacitracin, vancomycin, aztreonam, imipenem, clavulanicacid, sulbactam, aminoglycosides, tetracyclines, chloramphenicol and the macrolides.3. Know the classification of penicillins and cephalosporins according to their chemicalstructure and their antimicrobial spectrum. Know lactamase resistant/sensitive drugs.4. Know the most common adverse effects of the antimicrobial drugs.5. Know the mechanisms of bacterial resistance for antimicrobial drugs.6. Know the most common applications of these antibiotics for the treatment ofdisease. Which drugs are broad spectrum, and which have specific or unique uses.Antitubercul osi s Drugs1 .Know the major symptoms of tuberculosis and leprosy.2. Know the mechanism of action of first and second line of anti-TB drugs.3. Know the antimycobacterial agents used in prophylaxis and treatment of TB.4. Know the most common adverse effects of the therapy.Antiprotozoal, Antihelminthic, and Antifungal Drugs 1 .Know the organisms responsible for malaria, onchocerciasis, amebiasis, andgiardiasis.2. Know the mechanisms of action of the antihelminthic and antiprotozoal drugs3. Know the life cycle of Plasmodium, and how this affects malaria treatment. Knowwhich drugs are useful for which life stages.4. Know the mechanisms of action of the major antimalarial drugs.5. Know the major adverse effects of antimalarial drugs.6. Understand how resistance to , and relapse from, antimalarial drugs occurs.7. Know the topical and systemic antifungal agents.8. Know the mechanisms of action of antifungal agents.9. Know the differences in absorption and adverse effects of imidazoles and triazoles.10. Know the adverse effects of systemic antifungal agents.Antineoplastic Drugs1. If given the name of an antineoplastic, know how to place it in a specific class. Forthe alkylating agents know the subclasses, e.g., nitrosoureas which can cross theblood brain barrier.2. Know the mechanisms of cytotoxicity of the different classes.3. Most antineoplastics inhibit bone marrow function. Remember the exceptions to thisrule, e.g., vincristine, asparginase, bleomycin.4. Regarding therapeutic uses:Know at least one application for each drug.5. Know how resistance can develop and know specifically mentioned druginteractions.Antiviral Drugs1. Know which antiviral agents are used to treat influenza, herpes or HIV. Within each class,the drugs are listed in order of their relative importance.2. Know which antiviral agents are not analogs of nucleosides.3. Know the rationale for using nucleoside analogs and their mechanisms as antiviralagents.4. Know the most common side
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