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BR-Antimicrobials

5/21/06

QuestionAnswer
Drugs that block cell wall synthesis by inhibiting peptidoglycan x-linking PCN, Ampicillin, Ticarcillin, Piperacillin, Imipenem, Aztreonam, Cephalosporins
Drugs that block peptidoglycan synthesis Bacitracin, Vancomycin, Cycloserine
Drugs that block protein synthesis at 50S ribosomal subunit Chloramphenicol, Erythromycin/Macrolides, Lincomycin, Clindamycin, Streptogramins (Quinupristin, Dalfopristin), Linezolid
Drugs that block protein synthesis at 30S ribosomal subunit Aminoglycosides, Tetracyclines
Drugs that block nucleotide synthesis Sulfonamides, Trimethoprim (TMP)
Drugs that block DNA topoisomerases Quinolones
Drugs that block mRNA synthesis Rifampin
Bactericidal antibiotics Penicillin, Cephalosporins, Vancomycin, Aminoglycosides, Fluoroquinolones, Metronidazole
Drugs that disrupt bacterial/fungal cell wall membranes Polymyxins
Drugs that disrupt fungal cell wall membranes Amphotericin B, Nystatin, Fluconazole/azoles
PCN (G = IV, V = oral); hypersensitivity rxn and hemolytic anemia Bactericidal for G+ cocci (1st line for Pneumococcal Pneumonia); G+ rods, G- cocci, Spirochetes (syphilis, lyme dz)
Methicillin, Nafcillin, Dicloxacillin (hypersensitivity rxn; meth = interstitial nephritis) Narrow spectrum Abx; Penicillinase Resistant d/t bulkier R group; use for Staph aureus
Ampicillin, AmOxicillin (better oral availability); (hypersensitivity, amp rash, pseudomembranous colitis) Wider spectrum HELPS kill enterococci (Haemophilus, E. coli, Listeria, Proteus, Salmonella, enterococcus); sensitive to penicillinase, but can combine with Clavulanic Acid (inhibitor);
Carbenicillin, Piperacillin, Ticarcillin (hypersensitivity) Extented spectrum (Pseudomonas, G- rods); use with Clavulanic acid
Cephalosporins b-lactam drugs inhibit cell wall synthesis but are less susceptible to penicillinases; bactericidal
1st generation cephalosporins (Cephalexin, Cefadroxil, Cefazolin): PEcK Proteus, E. coli, Klebsiella
2nd generation cephalosporins (Loracarbef, Cefprozil, Cefuroxime, Cefaclor): HEN PEcKS Haemophilus, Enterobacter, Neisseria, Proteus, E. coli, Klebsiella, Serratia
3rd generation cephalosporins (Ceftazidime, Ceftriaxone) great G- coverage; Tx meningitis, Pseudomonas, Gonorrhea
4th generation cephalosporins increased activity against Pseudomonas and G+ bugs
Cefoperazone 2nd generation cephalosporin; use in pts with decreased renal failure; HEN PEcKS
Ceftazidime 3rd generation cephalosporin; use for Pseudomonas (and other G-s)
Ceftriaxone 3rd generation cephalosporin; use for GONORRHEA (and other G-s)
Cephalosproin toxicity Disulfiram-like rxn w/ethanol (ex: Cefamandole d/t methylthiotetrazole grp); hypersensitivity rxns d/t x-reactivity w/PCNs in some pts; They increase nephrotoxicity of aminoglycosides
Aztreonam G- rods ONLY: Klebsiella, Pseudomonas, Serratia; Good for RENAL PTs who can't tolerate aminoglycosides; resistant to b-lactamase; no PCN x-allergenicity
Imipenem/Cilastatin (imipenem is renally longer LASTIN' with ciLASTIN) #1 for ENTEROBACTER; Broad spectrum (G+ cocci, G- rods, Anaerobes); can cause seizures
Vancomycin (nephrotoxic, ototoxic, thrombophlebitis, "red man syndrome" from fast infusion) Save for SERIOUS G+ MULTI-DRUG RESISTANT bugs: S. aureus and Clostridium difficile; changes AAs from D-ala to D-lac;
Protein Synthesis Inhibitors: "Buy AT 30, CELL at 50" 30s (Aminoglycosides - bactericidal, Tetracyclines); 50S (Chloramphenicol, Erythromycin, Lincomycin, cLindamycin); all except aminoglycosides are bacteriostatic
Gentamicin, Neomycin, Tobramycin, Streptomycin, Amikacin Aminoglycosides; Good for SEVERE G- Rod infxns; bactericidal - no initiation complex/misread mRNA; synergistic with b-lactams; requires O2 for uptake (no anaerobic coverage);
Neomycin used for bowel surgery
Toxicity of Aminoglycosides + Cephalosporins Nephrotoxicity
Toxicity of Aminoglycosides + Loop diuretics Ototoxicity
Tetracycline, Doxycycline, Demeclocycline (VACUUM your BedRoom Tonight) Vibrio, Acne, Chlamydia, Ureaplasma, Urealyticum, Mycoplasma pneumoniae, Borrelia, Rickettsia, Tularemia; Bacteriostatic; bind 30S/prevent tRNA attachment; don't take with Ca or Fe b/c divalent cations bind in gut
Doxycycline safe to use in renal patients
Toxicity of Tetracycline, doxycycline, demeclocycline discoloration of teeth and inhibition of bone growth in kids; photosensitivity; GI distress
Erythromycin, Azithromycin, Clarithromycin (GI discomfort is bad; acute cholestatic hepatitis, eosinophilia, rash) URIs, Pneumonias, STDs, Strep infxns in PCN-allergies; Mycoplasma, Legionella, Chlamydia, Neisseria; Macrolides; block protein translocation (23S rRNA of 50S subunit); Bacteriostatic
Chloramphenicol (anemia, aplastic anemia, gray baby d/t lack of liver UDP-glucuronyl transferase) Meningitis (H. influenza, N. menigitidis, S. pneumoniae); Bacteriostatic; inhibits 50S peptidyltransferase; Toxicity = use conservatively
Clindamycin (causes C. difficile overgrowth) blocks 50S peptide bond; bacteriostatic; Tx ANAEROBIC infxns above diaphragm (Bacteriodes fragilis, Clostridium perfringens
Sulfamthoxazole (SMX), Sulfisoxazole, Triple Sulfas, Sulfadiazine G+, G-, Nocardia, Chlamydia coverage; UTI; bacteriostatic; sulfonamides; PABA-antimetabolites inhibit dihydropteroate synth; hemolysis in G6PD deficiency; nephrotoxic, kernicterus infant, diplaces warfarin from albumin
Trimethoprim Treat recurrent UTIs, Shigella, Salmonella, Pneumocystis carinii; bacteriostatic; inhibits bacterial dihydrofolate reductase; use in combo w/SMX to block folate synth; may cause marrow suppression
Ciprofloxacin, Norfloxacin, Ofloxacin, Sparfloxacin, Moxifloxacin, Gatifloxacin, Enoxacin, Nalidixic acid Treat G- rods in UTI, GI infxns; PSEUDOMONAS, Neisseria, some G+s; Bactericidal; inhibit DNA gyrase (topoisomerase II); Fluoroquinolones; contra in pregnancy; may cause Tendonitis/rupture
Metronidazole: GETon the metro! Antiprotozoal: Giardia, Entamoeba, Trichomonas, Gardernela vaginalis, ANAEROBES (Bacterioides, Clostridium); Use as part of triple therapy for H.pylori (w/bismuth, amoxicillin or tetracycline); Disulfiram-like rxn w/alcohol, HA
Polymyxin B, Polymyxin E Use for resistant G- infections; alter osmotic properties in bacterial membrane; cationic basic ptns that act as detergents; can be neurotoxic, nephrotoxic
Anti-TB drugs RESPIre: rifampin, ethambutol, streptomycin, pyrazinamide, isoniazid (INH); all are hepatotoxic; (2nd line = Cycloserine)
Isoniazid Can solely prophylax against TB; decreases mycolic acid synthesis; "INH" = injures neurons and hepatocytes; also causes hemolysis in G6PD deficiency; B6/pyridoxine can prevent neurotoxicity
Rifampin Treats TB; delays dapsone resistance in leprosy; Meningococcal prophylaxis for Hib; "4 Rs" = RNA polymerase inhibitor, revs up P450; Red/orange body fluids, Rapid resistance if used alone
Penicillin/cephalosporin resistance mechanism b-lactamase cleavage of b-lactam ring
Aminoglycoside resistance mechanism modification via acetylation, adenylation, or phosphorylation
Vancomycin resistance mechanism terminal D-ala of cell wall replaced with D-lac; decreases affinity
Chloramphenicol resistance mechanism modification via acetylation
Macrolide resistance mechanism methylation of rRNA near erythromycin's ribosomal binding site
Tetracycline resistance mechanism decreased or increased transport out of cell
Sulfonamide resistance mechanism altered enzyme (bacterial dihydropteroate synthase); dec uptake or inc PABA synthesis
Nonsurgical antimicrobial prophylaxis for Meningococcal infection Rifampin (drug of choice), minocycline
Nonsurgical antimicrobial prophylaxis for Gonorrhea Ceftriaxone
Nonsurgical antimicrobial prophylaxis for Syphilis Benzathine PCN-G (IV)
Nonsurgical antimicrobial prophylaxis for h/o recurrent UTIs TMP-SMX
Nonsurgical antimicrobial prophylaxis for Pneumocystic carinii pneumonia TMP-SMX (drug of choice), aerosolized pentamidine
Amphotericin B Treat systemic mycoses: Cryptococcus, Blastomycoses, Coccidioides, Aspergillus, Histoplasma, Candida, Mucor; binds ergosterol, "tears" pores in membrane; fever/chills, hypotension, nephrotoxic, Arrhythmias
Nystatin "swish and swallow" for oral candidiasis; binds ergosterol disrupting fungal membranes
Fluconazole, Ketoconazole, Clotrimazole, Miconazole, Itraconazole, Voriconazole Treat Systemic mycoses and hypercortisolism: inhibit ergosterol synthesi
Fluconazole Treat cryptococcal meningitis in AIDS and all candidiasis infxns (except yeast)
Ketoconazle Treat Blastomyces, Coccidioides, Histoplasma, Candida albicans, hy
Created by: bscaryp
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