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 |