Antibiotics (from Forystek table) – Flashcards
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Penicillins (drugs) |
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Penicillin G Penicillin V |
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Penicillins (MOA) |
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Competitive inhibition of transpeptidase enzyme (penicillin binding proteins) a inhibits cell wall synthesis |
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Penicillins (pharm profile) |
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Procaine and benzathine pen G are IM, IV Penicillin V is oral |
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Penicillins (uses) |
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Strep, Staph, Clostridia N. meningitides Syphilis |
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Penicillins (side effects) |
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Serum sickness: Ag/Ab complex causing hemolytic anemia |
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Aminopenicillins (drugs) |
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Ampicillin Amoxicillin |
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Aminopenicillins (MOA) |
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Competitive inhibition of transpeptidase enzyme (penicillin binding proteins) ? inhibits cell wall synthesis |
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Aminopenicillins (pharm profile) |
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Amoxicillin- PO |
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Aminopenicillins (uses) |
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Broader GM- coverage HELPS kill entercoccus (Haemophilus, E. coli, Listeria, Proteus, Salmonella and Enterococcus) |
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Aminopenicillins (side effects) |
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Maculopapular rash in patients with mono, CLL, or taking Allopurinol Pseudomembranous colitis |
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Penicillinase-R penicillins (drugs) |
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Nafcillin Oxacillin (IV/PO) Methicillin |
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Penicillinase-R penicillins (MOA) |
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Competitive inhibition of transpeptidase enzyme (penicillin binding proteins) ? inhibits cell wall synthesis |
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Penicillinase-R penicillins (pharm profile) |
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IV |
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Penicillinase-R penicillins (uses) |
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S. aureus (except MRSA) Nafcillin- severe (IV 4 hrs) Dicloxacillin- mild |
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Penicillinase-R penicillins (side effects) |
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Interstitial nephritis (methicillin), not used Increases liver enzymes |
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Carboxy/Ureidopenicillins (drugs) |
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Ticarcillin Carbenicillin Piperacillin |
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Carboxy/Ureidopenicillins (MOA) |
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Competitive inhibition of transpeptidase enzyme (penicillin binding proteins) ? inhibits cell wall synthesis |
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Carboxy/Ureidopenicillins (uses) |
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Extended GM- rod coverage, Pseudomonas and anaerobes (B. fragilis) |
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Carboxy/Ureidopenicillins (side effects) |
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TCP Takes care of pseudomonas and B. fragilis Lower dose in kidney failure |
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?-Lactamase inhibitors (drugs) |
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Clavulanic acid Tazobactam |
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?-Lactamase inhibitors (combinations) |
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Clavulanic acid + amoxicillin= augmentin Clavulanic acid + ticarcillin = timentin Tazobactam + piperacillin = Zosyn Ampicillin + sulbactam = Unasyn |
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?-Lactamase inhibitors (uses) |
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Coverage against ?-lactamase producing species (aureus, influenza, fragilis) |
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Cephalosporins - 1st generation (drugs) |
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Cefazolin Cephalexin |
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Cephalosporins - 1st generation (MOA) |
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Same as penicillins (?-lactam drugs inhibit cell wall synthesis) Less susceptible to penicillinases |
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Cephalosporins - 1st generation (uses) |
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GM+ cocci prophylaxis surgery PECK- proteus, ecoli, and klebsiella |
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Cephalosporins - 1st generation (mnemonic) |
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Fazoli’s symbol is phelex (phallic) |
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Cephalosporins - 2nd generation (drugs) |
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Cefaclor Cefoxitin Cefuroxime |
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Cephalosporins - 2nd generation (MOA) |
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Same as penicillins (?-lactam drugs inhibit cell wall synthesis) Less susceptible to penicillinases |
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Cephalosporins - 2nd generation (uses) |
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GM+ cocci Anaerobes (cefoxitin/cefotetan) HEN PECK Haemophilus, enterobacter, neisseria, proteus, ecoli, klebsiella) |
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Cephalosporins - 2nd generation (mnemonic) |
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It’s a FACt that FOX has FUR |
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Cephalosporins - 3rd generation (drugs) |
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Ceftriaxone Cefixime Ceftaxidime |
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Cephalosporins - 3rd generation (MOA) |
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Same as penicillins (?-lactam drugs inhibit cell wall synthesis) Less susceptible to penicillinases |
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Cephalosporins - 3rd generation (uses) |
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Multidrug resistant GM- infections Bacterial meningitis Gonorrhea (ceftriaxone/cefixime) Pseudomonas (ceftaxidime) |
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Cephalosporins - 3rd generation (mnemonic) |
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TRI and FIX TAZ |
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Cephalosporins - 3rd generation (pharm profile) |
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Penetrates BBB well (especially ceftriaxone) Ceftriaxone- IM Cefixime- PO |
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Cephalosporins - 4th generation (drugs) |
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Cefepime Cefpiramide |
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Cephalosporins - 4th generation (MOA) |
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Same as penicillins (?-lactam drugs inhibit cell wall synthesis) Less susceptible to penicillinases |
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Cephalosporins - 4th generation (uses) |
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Regains some GM+ coverage Pseudomonas |
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Cephalosporins - 4th generation (mnemonic) |
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E pime on my piramide |
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Monobactam (drugs) |
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Azetreonam |
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Monobactam (MOA) |
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Binds to PBP in GM- only (No GM+ or anaerobe) |
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Monobactam (uses) |
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Serious nosocomial GM- (klebsiella, Pseudomonas, serratia) |
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Monobactam (side effects) |
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Does not cross react with penicillin allergy |
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Carbapenems (drugs) |
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Imipenem/Cilastatin Meropenem Doripenim |
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Carbapenems (MOA) |
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?-lactam |
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Carbapenems (pharm profile) |
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Imipenem inactivated in kidney by dihydro-peptidase (must give with cilastatin) |
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Carbapenems (uses) |
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VERY broad spectrum (GM+ cocci, GM- rods, Pseudomonas, anaerobes) Drug choice of choice Enterobacter- most reliable activity against ES?L |
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Carbapenems (side effects) |
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Seizures (decrease threshold) Carbapenamases: KPC + metallo-?-lactamases, hydrolyse carbapenams, must report |
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Sulfonamides (drugs) |
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TMP-SMX |
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Sulfonamides (MOA) |
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TMP inhibits DHF reductase (DHF? THF) SMX is PABA analogue that inhibits dihydropteroate synthase Overall, they decrease folate and DNA, RNA, and proteins |
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Sulfonamides (pharm profile) |
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Affects protein binding displaces rifampin, warfarin, MTX and phenytoin May decrease heme s/e by giving leukovorin (folonic acid) ? is in CNS |
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Sulfonamides (uses) |
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TMP-Smx Tree (respiratory) M (mouth, GI tract) ? Gm- diarrhea P (Pee)? prostatitis, UTI, urethritis SMX (syndrome) AIDS ? P. jirovecii, prohpylaxis or others such as toxoplasmosis, nocardia, rheumathic fever, and kansaii |
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Sulfonamides (side effects) |
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Hematopoietic in AIDS patients (megaloblastic anemia, leucopenia) Erythema nodosum Hypersensitivity to sulfa Not in pregnancy or breast feeding because kernicterus (SMX) Hemolysis in G6PD deficiency |
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Floroquinolones (drugs) |
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Ciprofloxacin Moxifloxacin Gemifloxacin Levofloxacin Sparfloxacin |
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Floroquinolones (MOA) |
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Inhibit bacterial DNA gyrase (topo II) Gm- or Topo 4 (Gm+) Inhibits DNA synthesis BacteriCIDAL |
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Floroquinolones (pharm profile) |
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Binds to antacids, sulfurate |
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Floroquinolones (uses) |
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Gm- rods of GI/GU Community acquired pneumo (levo, spar GM+ atypical) Pseudomonas: cipro GM+ levo moni gemi |
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Floroquinolones (side effects) |
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Tendonitis with tendon rupture CNS effects, photosensitivity Not in pregnancy or children because of cartilage damage. Resistance is due to an altered target, or binding/inactivating enzyme |
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Metronidazole (drugs) |
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Metronidazole |
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Metronidazole (MOA) |
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Metabolized INSIDE anaerobic bacteria and damages DNA BacteriCIDAL |
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Metronidazole (pharm profile) |
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Does not enter blood very well, so it enters the GI tracts and kills C. diff enters CNS as well |
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Metronidazole (uses) |
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GET GAP at the Metro Giadia Entamoeba Trichomonas Gardernella vaginalis Anaerobes Pylori |
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Metronidazole (side effects) |
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Disulfiram (antibuse) like side effects with alcohol NOT in pregnancy |
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Polymixins (drugs) |
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Polymixin B Polymixin E colistin |
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Polymixins (MOA) |
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Cationic basic proteins (detergent) that disrupts osmotic properties of the membrane. Polymixins “mix up” membranes |
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Polymixins (pharm profile) |
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Bacteriocidal regardless of growth phase |
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Polymixins (uses) |
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Resistant GM- infections |
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Polymixins (side effects) |
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Neurotoxicity Acute tubular necrosis Bottom of the barrel choice |
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Aminoglycosides (drugs) |
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Gentamycin Goes to ECF- which is larger in shock, give more to ICU patients Neomycin Amikacin Tobramycin Streptomycin |
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Aminoglycosides (MOA) |
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bactericidal Synergistic with ?-lactam antibiotics b (must diffuse though cell wall) Inhibits 30S |
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Aminoglycosides (pharm profile) |
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Requires O2 for uptake (NOT effective vs. anaerobes) Punch holes in cytoplasm |
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Aminoglycosides (uses) |
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Severe GM- rod infection Resistance by aminoglycoside inactivating Neomycin for bowel surgery aminoglycoside + penicillin for enterococcal endocarditis (vanco for pen. Resistance) |
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Aminoglycosides (side effects) |
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GNATS can NOT kill anaerobes drug accumulates in proximal tubules Nephotoxic (increases w/cephalo’s) Ototoxic (increases w/loop diuretics) Teratogenic |
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Tetracyclines (drugs) |
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Tetracyline Doxycycline Demeclocycline Minocycline |
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Tetracyclines (MOA) |
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bacteriostatic Inhibit 30S R. Efflux pumps+ ribosome protection proteins |
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Tetracyclines (pharm profile) |
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Absorption inhibited by divalent cations (no milk, antacids, or iron containing compounds) |
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Tetracyclines (uses) |
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VACuUM The BR (bedroom) Vibrio, Acne, Chlamydia, Ureaplasma, Mycoplas,a. Tularemia, H. pylori, Borrelia, Rickettsea Nocardia- minocycline Bemeclocycline in SIADH |
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Tetracyclines (side effects) |
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Teeth/bone discoloration (chelates Ca2+) Not in pregnancy Not in renal dz (only doxy) Photosensitivity Superinfection (yeasty) |
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Macrolides (drugs) |
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Erythromycin (g+) Azithromycin (g-, long .5) Clarithromycin (g+) |
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Macrolides (MOA) |
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Inhibit protein synthesis by binding to the 50S subunit (or 23 srRNA) Bacteriostatic |
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Macrolides (pharm profile) |
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Ery and clari inhibit CYP450 (higher levels of warfarin/theophilline) w/cisapride get torsades de pointes? tachycardia and DEATH |
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Macrolides (uses) |
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Community acquired pneumonia: S. pneumo and atypical (legionella, Chlamydia and mycoplasma) GM+ cocci alternative with pen allergy STDS Chlamydia/GC + H.pylori |
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Macrolides (side effects) |
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GI irritation (common and dose related) Not in pregnancy (cholestatic hepatitis in the mother) |
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Lincosamides (drugs) |
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Clindamycin |
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Lincosamides (MOA) |
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Inhibit protein synthesis by binding to the 50S subunit (or 23 srRNA) Bacteriostatic |
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Lincosamides (pharm profile) |
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long presence in stool, altered gut flors |
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Lincosamides (uses) |
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Anaerobic infections above diaphragm, not CNS |
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Lincosamides (side effects) |
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Pseudomembranous colitis due to C. diff |
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Chloramphenicol (drugs) |
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Chloramphenicol |
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Chloramphenicol (MOA) |
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Inhibit protein synthesis by binding to the 50S subunit (or 23 srRNA) Bacteriostatic |
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Chloramphenicol (pharm profile) |
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Conjungated in liver UDP glucuronyl transferase (absent in premature) |
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Chloramphenicol (uses) |
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Very broad, usually meningitis or rickettsial, not really used |
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Chloramphenicol (side effects) |
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Anemia (reversible) Aplastic anemia GREY BABY SYNDROME |
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Glycopeptides (drugs) |
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Vancomycin |
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Glycopeptides (MOA) |
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Inhibits cell wall mucopeptide formation by binding D-ala D-ala portion of cell wall precursors Bactericidal except for enterococcus |
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Glycopeptides (pharm profile) |
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IV PO for C. diff |
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Glycopeptides (uses) |
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Serious GM+ multidrug resistant organisms (MRSA, enterococcus, refractory C. diff) There are VRE and SRE strains (VAN genes) Use in synergy w/aminoglycosides, rifampin) |
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Glycopeptides (side effects) |
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RED MAN NOT Red Man syndrome with rapid infusion, this is due to increased histamine release NOT Nephrotoxicity Ototoxicity Thrombophlebitis |
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Streptogramins (drugs) |
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Quinupristin/dalphopristin |
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Streptogramins (MOA) |
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Inhibits proteins synthesis, both bind to different sites on the 50S subunit |
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Streptogramins (pharm profile) |
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Inhibits CYP 450 |
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Streptogramins (uses) |
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VRE, but only e. faecium, does not work for e. facalis |
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Streptogramins (side effects) |
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peripheral IV pain and phlebitis, arthralgias, myalgias |
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Cyclic lipopeptides (drugs) |
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Daptomycin |
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Cyclic lipopeptides (MOA) |
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Calcium dependent binding on plasma membrane with depolarization (K+) release and death |
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Cyclic lipopeptides (uses) |
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Complicated skin/soft tissue and intra-abdomin MSSA, MRSA, VISA, VRSA, VRE, Pen-R pneumo |
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Cyclic lipopeptides (side effects) |
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Rhabdomyolysis: increased CPK, muscle discomfort |
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Glycylcylines (drugs) |
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Tigecycline |
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Glycylcylines (MOA) |
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Inhibit protein synthesis (binds to the 30S subunit) |
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Glycylcylines (uses) |
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Complicated skin/soft tissue and intra-abdomin MSSA, MRSA, VISA, VRSA, VRE, Pen-R pneumo |
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Glycylcylines (side effects) |
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GI Complications Increase in liver transaminases (AST/ALT) |
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Oxazolidinones (drugs) |
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Linezolid |
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Oxazolidinones (MOA) |
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Inhibits protein synthesis (binds to the 50S subunit) near the 30S subunit, prevents 70S formation (unique) |
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Oxazolidinones (pharm profile) |
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no cross resistance, 100% bioavailability PO |
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Oxazolidinones (uses) |
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VRE and some MRSA/VRSA also RAPID growing mycobacteria Chelonae, fortuitum |
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Oxazolidinones (side effects) |
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Bone marrow toxicity No cross reaction with other protein synthesis antibiotics Tongue discoloration |