Antimicrobial Drugs Session Objectives 2010
Antibiotics I - Overview (Dery)
By the end of the session you should be able to:
- Discuss the process of choosing the correct antibiotic.
- Discuss the process of identifying the infecting organism.
- Describe the time dependent and concentration dependent pharmacokinetic/pharmacy of antibiotics.
- Describe how to determine the antimicrobial susceptibility of infecting organisms.
- Describe the host factors necessary to understand so that the correct antibiotic is chosen.
- Describe the indications for antimicrobial combinations, including antimicrobial synergism and antagonism.
- Discuss therapeutic drug monitoring.
Antibiotics II - Beta Lactams (Schieffelin)
- Explain the mechanism of action of β-lactam antibiotics.
- Describe the metabolism and pharmacokinetic properties of penicillins and other beta-lactams.
- Discuss primary therapeutic indications for penicillin G and the repository penicillins.
- Describe the indications for broad-spectrum penicillins, including penicillinase-resistant penicillins, aminopenicillins and anti-pseudomonal penicillins.
- List the combinations of inhibitors of β-lactamase with penicillins, their clinical usage & explain the reason why they are combined.
- Describe the antimicrobial spectrum and pharmacokinetic properties of the four generations of cephalosporins.
- Explain the major side effects of penicillins and other beta-lactams including superinfection and hypersensitivity.
- Describe the antimicrobial activity of monobactams and carbapenems.
- List the major side effects of carbapenems and monobactams.
- Penicillins: penicillin G, penicillin V, methicillin, oxacillin, nafcillin, dicloxacillin, ampicillin, amoxicillin, ticarcillin, piperacillin
- Cephalosporins: cephalexin, cefazolin, cefuroxime, cefoxitin, cefotetan, cefaclor, cefotaxime, ceftriaxone, ceftazidime, cefixime, cefepime
- Monobactams: aztreonam
- Carbapenems: doripenem, ertapenem, meropenem, imipenem (& imipenem + cilastatin)
- Beta-Lactamase Inhibitors: clavulanic acid, sulbactam, tazobactam
Antibiotics III - Macrolides, Tetracyclines & Fluoroquinolones (Oberhelmen)
- Describe the mechanism of action of each class
- Explain the pharmacokinetic properties and compare erythromycin with clarithromycin, and azithromycin
- Describe the primary therapeutic indications for each class of antibiotics
- Describe the major drug interactions of macrolides due to inhibition of cytochrome P450 enzymes
- Discuss the major toxicities and side effects of each class of antibiotics
- Explain the drug interaction of tetracyclines & antacids, and tetracyclines and penicillins
- List the advantages of newer fluoroquinolones over older fluoroquinolones
- Describe the adverse effects of fluoroquinolones, including contraindications in children & pregnant women.
- Macrolides: erythromycin, clarithromycin, azithromycin;
- Tetracyclines: tetracycline, doxycycline, minocycline
- Fluoroquinolones: ciprofloxacin, levofloxacin, moxifloxacin
Antibiotics IV - Aminoglycosides, Nitrofurantoin & Polymyxins (Van Dyke)
- Discuss the mechanism of action of the aminoglycosides
- Explain the mechanism of acquired microbial drug resistance to aminoglycosides
- Describe the range of organisms which the aminoglycosides are active against
- Describe the pharmacokinetic properties of the aminoglycosides; explain the importance of peak and trough levels.
- Discuss the dose adjustment for aminoglycosides in patients with compromised renal function
- Explain the rational basis for combination therapy with an aminoglycoside and a cell wall synthesis inhibitor
- Discuss the main toxicities of aminoglycosides
- Discuss the mechanism of action of nitrofurantoin
- Describe the range of organisms which nitrofurantoin is active against
- Describe why its use is limited to urinary tract infections
- Discuss the main toxicities from nitrofurantoin
- Discuss the mechanism of action of polymyxins.
- Describe the range of organisms which polymyxins are active against.
- Describe the toxicities from polymyxins and how this influences their use
- Aminoglycosides: amikacin, gentamicin, kanamycin, neomycin, netilmicin, streptomycin, tobramycin
- Urinary Antiseptic: nitrofurantoin
- Polymyxins: colistin, colistimethate, polymyxin B
Antibiotics V - Clindamycin, Metronidazole, Rifamycins & Sulfonamides (Mushatt)
- Discuss the mechanisms of action of clindamycin, metronidazole and the rifamycins
- Discuss the mechanism of action of sulfonamides and explain the synergistic inhibition due to sequential blockade with trimethoprim
- Describe their pharmacokinetic/pharmacodynamic properties
- Describe the range of organisms which these agents are active against
- Discuss their therapeutic indications
- Describe the major toxicities of these antibiotics
- Understand the mechanism of drug interactions with rifampin
- Explain the rational basis for combination therapy between rifampin and other antibiotics.
- Rifamycins: rifampin, rifabutin
- Sulfonamides: trimethoprim-sulfamethoxazole, sulfadiazine
Antibiotics VI - Vancomycin, Daptomycin, Linezolid & Quinupristin/Dalfopristin (Barbeau)
- Discuss the differences in the mechanisms of action for each class of agents: glycopeptides (e.g. vancomycin, telavancin, teicoplanin), daptomycin, linezolid, and streptogramins (e.g., quinupristin/dalfopristin).
- Describe the pharmacokinetic properties of each class of agents: glycopeptides (e.g., vancomycin, telavancin, teicoplanin), daptomycin, linezolid, and streptogramins (e.g., quinupristin/dalfopristin).
- Describe the antimicrobial spectrum of each class of agents: glycopeptides (e.g., vancomycin, telavancin, teicoplanin), daptomycin, linezolid, and streptogramins (e.g., quinupristin/dalfopristin).
- Describe the main therapeutic indications and toxicities/side effects of each class of agents: glycopeptides (e.g., vancomycin, telavancin, teicoplanin), daptomycin, linezolid, and streptogramins (e.g., quinupristin/dalfopristin).
- Glycopeptides: vancomycin, telavancin, teicoplanin
- Membrane Active Agents: daptomycin
- Oxazolidinones: linezolid
- Streptogramins: quinupristin/dalfopristin (combination)
Antifungal Drugs (Mondal)
- List the antifungal drugs useful in treatment of fungal infections.
- Explain the mechanism of action of each of these drugs.
- Compare the pharmacokinetic properties of various antifungals.
- Describe the major therapeutic indications of each of these drugs.
- List the adverse effects associated with the antifungal drugs.
- Know the liposomal preparations of Amphotericin B.
- Be aware of the antifungal drug interactions, e.g. with warfarin.
Amphotericin-B, Nystatin, Ketoconazole, Fluconazole, Itraconazole, Terbinafine, Griseofulvin, Flucytosine, Caspofungin
PBL on Antimicrobial Drugs (Faculty)
- Generate hypotheses in relation to patient’s illness.
- Predict the infecting organisms and list the antibiotics that can be used to treat an infection.
- Be able to select alternative antibiotics for patients with a history of antibiotic allergy