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Teaching Plan of International Edcation School of KMU Teaching Department: Basic Medical Class time: 2016.12.3 subject Pharmacology grade 2014 major Clinical Name of Ning Huang professional Lec Lecture or Lecture Class 2 teacher title ture experiment hour 29 Aminoglycoside, Tetracyclines, Chlorampherico topic( chapter) teaching material ( book Textbook of pharmacology, Zhou Honghao, Kexue chubanshe, 2006.3, title , chief editor , 1st publishing house , publishing time,edition) Teaching aims & requirements: Teaching aims: To Grasp antimicrobial spectrum, indications, pharmacokinetics and clinical uses of Aminoglycoside, Tetracyclines, Chlorampherico . Requirements: Aminoglycoside, Tetracyclines, Chlorampherico characteristics of the pharmacological effects. Key teaching points & difficult points: Key teaching points: to master the mechanism of action of contraceptives, usage and adverse reactions. Difficulty: the mechanism of action of Aminoglycoside, Tetracyclines, Chlorampherico . Teaching methods: 1) Lecture. Various teaching methods are furnished in pharmacology lectures. Multimedia courseware in aid of blackboard is the common way of teaching. Animations are also used to illustrate the mechanism of drugs, making the abstracts lively and easy to understand. 2) “Case based learning” (CBL) mode. Using a case-based approach engages students in discussion of specific scenarios that resemble or typically are real-world examples. This method is learner-centered with intense interaction between participants as they build their knowledge and work together as a group to examine the case. The instructor's role is that of a facilitator while the students collaboratively analyze and address problems and resolve questions that have no single right answer. With case-based teaching, students develop skills in analytical thinking and reflective judgment by reading and discussing complex, real-life scenarios. Design of PPT and blackboard-writing:Mechanism of action of Chlorampherico 1 Contents Section 1 Aminoglycoside supplementary means and time allotment 30min Mechanism of action Aminoglycosides are irreversible inhibitors of protein synthesis. Once an aminoglycoside has entered the cell, it binds to specific 30s subunit ribosomal proteins. Normal protein synthesis include three steps: step 1 Initiation, step 2 Extension and step 3 Termination. Aminoglycosides inhibite protein synthesis in at least three ways: (1) They interfere with the “initiation complex” of peptide formation. (2) They induce misreading of mRNA, which causes incorporation of incorrect amino acids into the peptide, resulting in a non-functional or toxic protein. (3) They cause a breakup of polysomes into nonfuntional monosomes. Mechanism of resistance Pharmacokinetics Application in clinic Adverse effects 2 Contents supplementary means and time allotment Section 2 Tetracyclines 20min Mechanism of action Tetracyclines enter microorganisms in part by passive diffusion and in part by an energy-dependent process of active transport. Susceptible cells concentrate the drug intracellularly. Once inside the cell, tetracyclines bind reversibly to the 30s subunit of the bacterial ribosome, interfering with the attachment of t-RNA to the mRNA ribosome. This prevents addition of amino acids to the growing peptide. 10min Mechanism of resistance Three mechanisms of resistance to tetracyclines have been described. First, decreased intracellular accumulation due to either impaired influx or increased efflux by an active transport protein pump. Second, ribosome protection due to production of proteins that interfere with tetracyclines binding to the ribosome. Third, enzymatic inactivation of tetracyclines. The most important of these is production of an efflux pump. The pump protein is encoded on a plasmid and may be transmitted by transduction or by conjugation. Because these plasmids commonly encode resistance genes for other drugs, for example, aminoglycosides, sulfonamides and chloramphenicol, tetracyclines resistance is a marker for resistance to multiple drugs. Pharmacokinetics Application in clinic Adverse effects Note: The contents of the teaching plan mainly includes the specific teaching content, time arrangement, the use of teaching aids, important professional vocabulary, complement of teaching content, etc. 3 Contents Section 3 supplementary means and time allotment Chlorampherico Antibacterial spectrum 30min Chloramphenicol is a broad-spectrum bacteriostatic antibiotic. It is active against both aerobic and anaerobic gram-positive and gram-negative organisms. Haemophilus influenzae, Neisseria meningitidis and some strains of Bacteroides are highly susceptible, and for them chloramphenicol may be bactericidal. The effect to G+ is not as good as penicilin and tetracycline. It also can repress Rickett’s organism,chlamydia and mycoplasma.Mechanism of action Chloramphenicol is a potent inhibitor of microbial protein synthesis. It acts primarily by binding reversibly to the 50s subunit of the bacterial ribosome, and interferes with peptidyl transferase in the step of protein synthesis. It is a bacteriostatic antibiotic. Resistance Almost all microorganisms could develop resistance to chloramphenicol. Clinically significant resistance is due to production of chloramphenicol acetyltransferase, a plasmid-encoded enzyme that inactivates the drug Clinical application Due to its severe adverse effects, chloramphenicol is seldom used in clinic. 30min It is used only when the benefits of therapy outweigh the risks of the potential toxicity and there are no other antimicrobial agents to select. It may be considered for treatment of serious typhoid fever, bacterial meningitis, anaerobic infections, rickettsial diseases, and brucellosis Adverse effects Interaction with other drugs Chloramphenicol inhibits hepatic microsomal enzymes that metabolize several drugs. Half-life is prolonged and the serum concentration of phenytoin, tolbutamide, chlorpropamide and warfarin is increased. 4 Contents supplementary means and time allotment Resistance Almost all microorganisms could develop resistance to chloramphenicol. Clinically significant resistance is due to production of chloramphenicol acetyltransferase, a plasmid-encoded enzyme that inactivates the drug Clinical application Due to its severe adverse effects, chloramphenicol is seldom used in clinic. It is used only when the benefits of therapy outweigh the risks of the potential toxicity and there are no other antimicrobial agents to select. It may be considered for treatment of serious typhoid fever, bacterial meningitis, anaerobic infections, rickettsial diseases, and brucellosis Adverse effects Interaction with other drugs Chloramphenicol inhibits hepatic microsomal enzymes that metabolize several drugs. Half-life is prolonged and the serum concentration of phenytoin, tolbutamide, chlorpropamide and warfarin is increased. 5 1.Tetracyclines and chloramphenicol are broad-spectrum antibiotics and they are active against both aerobic and anaerobic G+ and G-, rickettsia, mycoplasma and chlamydia. The tetracyclines are a large group of drugs with a common basic Summary structure and activity. Tetracyclines include natural tetracyclines, such as tetracycline, tetramycin, chlortetracycline, demeclocycline and semisynthetic, such as metacycline, doxycycline, minocycline. Tetracyclines are stable in acid solution and easily distroyed in alkaline solution. 2. Aminoglycoside, Tetracyclines, Chlorampherico,: action, use, mechanism of action, adverse reactions. Aminoglycoside, Tetracyclines, Chlorampherico,: action, use, mechanism of action, adverse reactions. Assignments Sulfonamides, Quinolones , Polypeptide antibiotics Preview Implementation and analysis Comments of Department Head of Department: Date: 6