Antibiotics Chart

Class/MOA Drug/MOA MOR Susceptibility Adverse Rxns Clinical Use/DOC Unique Features Cell Membrane Antibiotics MembraneActive Polymyxins (Colistin = Polymyxin E) Enzyme modifies lipid A - Low levels of resistance Gram (-), Growing and Non-Growing Cells Nephrotoxic, neurotoxic Salvage Gram (-) therapy In topical combo Bactericidal; Cell membrane binder Daptomycin (Cubicin) Gram (+); (MRSA, VRE, VRSA) Re-surfaced due to activity of MRSA Bactericidal; Binds/depolarized cell membrane Not effective vs Pneumonia Cell Wall Antibiotics: Mostly Gram (+) 𝛃-Lactams: Bactericidal (vs actively growing cells); Binds Penicillin Binding Proteins (PBP) and inhibits cell wall synthesis, Largest single class of cell-wall inhibitors Characteristic 4-member ring, Avoid use with bacteriostatic agents, Food absorbs and lowers bioavailability (F) Penicillins Penicillin G Suffix: -icillin Penicillin V Requires porins to pass outer membrane Penicillinase-Resistant Beta-lactamase degrades betalactams Methicillin, Nafcillin, Oxacillin Semi-Synthetic: Piperacillin, Ticarcillin Methicillin: mecA gene encodes PBP2A that confers resistance to all β-Lactams Penicillinase Sensitive Penicillins Aminopenicillins: Amoxicillin, AmpicillinResistant enterococcus due to betalactamase Gram (+) (S. pneumoniae, S pyogenes, Actinomyces) Gram (-): (N meningitidis, T pallidum) Hypersensitivity, direct Coombs + hemolytic anemia Narrow Spectrum Gram (+) Hypersensitivity, interstitial nephritis Broad spectrum ↑ Gram (-) Anaerobes, Pseudomonas Broad-spectrum: HHELPSS: H influenzae, H pylori, E. coli, Listeria monocytogenes, Proteus Steven-Johnson Syndrome (Rash) Administered IV/IM Administered Orally Staph aureus (except MRSA) Beta-lactamase resistant; acid sensitive Severe hospitalacquired Pseudomonas More resistant to betalactamases HELPSS kill enterococci Oral bioavailability : (Amoxicillin>Ampicillin) Sensitivity to beta- Cephalosporins Prefix: Ceph- or Cef- Ampicillin production mirabilis, Salmonella, Shigella, enterococci Gen I: (SS PEK) Cephalexin, Cefazolin Betalactamases, changes in PBPs, decreased membrane permeability Gram (+) Cocci: Strep, staph Gram (-): Klebsiella, Proteus, E. Coli Same Gram (+) ↑Gram (-): Add H. influenzae, Neisseria and Serratia Gen II: (Add HENS) Cefaclor Cefoxitin Cefuroxime (Fake Fox Fur) lactamases Hypersensitivities DOC: Surgical prophylaxis Penicillin crossreactivity (avoid if rxn is anaphylaxis) Disulfiram-like reactions: Hypoprothrombinem ia, Thrombocytopenia, Platelet dysfunction Some anaerobes Gen III: (Add ME) Ceftriaxone Cefotaxime Ceftazidime (Ax Taz) Gram (+): Strep viridans Serious Gram (-): Pseudomonas, Meningitidis Gen IV: Cefepime Broad spectrum: Gram (+) organisms Gram (-): Pseudomonas Gen V: Ceftaroline Broad Spectrum Gram (+): MRSA Some Gram (-): (NOT Pseudomonas) Binds PBP2A Monobactams Prototype: Aztreonam Carbapenems Prototype: Imipenem/ Cilastatin (prevents renal clearance, “cilastatin make it lastin”) Nephrotoxicity with aminoglycosides Autoimmune hemolytic anemia, Vitamin K deficiency Ceftriaxone DOC: Neisseria gonorrhoeae and meningitidis Ceftazidime:Pseudomo nas Increased activity against Pseudomonas Penetrates CSF; “Big Gun” antibiotic, penetrates CSF Formulated as prodrug Gram (-) aerobes: Pseudomonas Usually non-toxic Penicillin and aminoglycoside intolerant patients Works with penicillin allergy; synergistic with aminoglycosides Carbapentamase Broad spectrum Imipenem: Susceptible to human renal dehydropeptidase Cilastatin: Peptidase inhibitor GI distress, skin rash, lowered seizure threshold at high plasma levels Aerobic function: Aspiration pneumonia, intra-abdominal infections Resistant against broadspec. Penicillinases Gram (+) cocci (except MRSA, VRE) Gram (-) cocci: Enterobacter, Pseudomonas, Empiric sepsis, HApneumonia Penetrate CSF well, “big gun” antibiotics for serious infections Also: Meropenem 𝛃-Lactamase Inhibitors MOA: Suicide inhibitor that binds and inactivates betalactamase Glycopeptide Antibiotics MOA: Bactericidal: Binds D-Ala, DAla part of cell wall Meropenem: Not dehydropeptidase sensitive Anaerobes: Bacteroides fragilis Anti-Pseudomonal Antibiotics Clavulanic Acid Sulbactam Tazobactam 1. Aminoglycoside 2.extended-spectrum antibiotic 3. Beta-lactamase inhibitor (CAST) Vancomycin Other: Teicoplanin and LipoglycoPeptides (Suffix: -vancin) Gram (-) Cell Wall Gram (+) only: MRSA, S epidermidis, sensitive Enterococcus, C. difficile Substitute terminal Dalanine with Dlactate (VRE, VRSA) Generally tolerated DOC: MRSA and C. well but NOT trouble Diff (oral), enteric endocarditis free: Nephrotoxicity Ototoxicity Thrombophlebitis Nosocomial Infections: (pneumonia and staph epidermidis) “Red Man Syndrome”: Diffuse flushing caused by fast IV infusion (Tx with antihistamine Reduced susceptibility due to high Dala termini (VISA>GISA) Bacitracin Administered IV, not absorbed in GI tract Beta-lactamase not effective against CNS and bone penetration 90% secretion by glomerular scr'n Most active against Gram (+) Restricted to topical use; not used for blood stream infection Inhibits translation of peptidoglycan precursors Fosfomycin Used in combination with beta-lactam antibiotics to extend activity UTIs: Single-dose Tx Inhiibits formation of cytoplasmic subunits Antimycobacterials Inhibition of translocation and steps in mycolic acid synthesis Cycloserine Anti-TB (not first choice) Inhibits translocation and cross-linking Isoniazid Preferred over cycloserine Inhibits specific steps in mycolic acid synthesis ● 30S Ribosomal Antibiotics Inhibit peptide formation; all bacteriostatic except for aminoglycosides Tetracyclines Suffix: -cycline MOA: Bacteriostatic; Reversible binding of 30s Aminoglycosides Suffix: -micin, mycin Tetracycline, Doxycycline, Minocycline Active Efflux -Tygacil is bulkier and resistant to efflux Tigecycline (Tygacil) Gentamycin (-mycin, -micin) Bactericidal, Irreversible binding of 30s Transferases: resistance to one is not resistant to all Broad Spectrum Many Gram (+) and Gram (-) Rickettsiae, Chlamydiae, Mycoplasma pneumoniae, Helicobacter pylori, Helicobacter pylori propionibacterium, Treponema pallidum Gram (-) Aerobic Bacilli TCNs and teeth turn yellowish (08yrs) GI: (Most Common): Irritation, diarrhea, superinfection (C. diff) Photosensitivity DOC: Tick-borne bacteria (Rocky mountain spotted fever, Lyme disease) Chlamydia Mycoplasma pneumoniae Doxycycline metabolized by liver Tetracycline eliminated in bile/urine Bind 30s more efficiently Also: Stomach ulcer, bacterial acne, syphilis Cochlear and Vestibular toxicity Combo with Betalactam for VRE Some Gram (+) t1/2: 2-3hr t1/2 (renal and ear): 30700 hour range Nephrotoxicity Broad spectrum Spectinomycin Bacteriostatic; Reversible binding to 30s 50s Ribosomal Antibiotics ● Inhibit peptide formation; all bacteriostatic except for streptogramins Chloramphenicol Bacteriostatic: Binds to 50S MLS Antibiotics Lincosamides: Aplastic anemia Antibiotic modification by CAT (chloramphenico l acetyltransferas es) Modification of the 50s subunit Gray baby syndrome Gram (+) cocci (Strep, staph, not MRSA) GI and Skin reactions Mostly topical use (in eye drops) due to toxicity Used more in 3rd world country Bacteriostatic: Reversibly binds 50s Clindamycin Suffix for Macrolide: mycin Erythromycin, azithromycin (Z pack), clarithromycin Macrolides: Anaerobes Erm Erythromycin resistant methylase Gram (-) Good for: Hemophilus Effective: Enterobacter GI: Motilin receptor Legionella agonist pneumophila and Bordetella pertussis Cholestatic Jaundice Azithromycin+Gentam icin: 100% effective for Prolonged QTc gonorrhoeae interval Useful in treating patients with penicillin allergies T1/2-69 hr; usually a 5 day tx Azithromycin has excellent distribution Potassium Channel Block: Arrhythmogenic Synercid is the first injectable streptogramin to gain FDA approval Streptogramins: Quinupristin + Dalfopristin Bactericidal: A + B act synergistically against bacteria Oxazolidines Linezolid (Zyvox) and Tedizolid Bacteriostatic: Binds 50s subunit Gram (-): Efflux pumps Gram (+): rRNA point mutation - Gram (+) cocci; - MRSA - VRE - Strep pyogenes - Pen-Resistant Strep pneumoniae GI: Diarrhea Not DOC; last resort Hematological Anemia, myelosuppression, thrombocytopenia, leukopenia, pancytopenia Nucleic Acid Antibiotics Quinolones/ Fluoroquinolones Target DNA gyrase Suffix: = Oxacin 1st Gen: Nalidixic acid 2nd Gen: Ciprofloxacin, Lomefloxacin, Ofloxacin 3rd Gen: Levofloxacin, Moxifloxacin Resistance widespread, little clinical correlation; mostly DNA gyrase genes Potent vs Gram (-) aerobes Renal: Norfloxacin, Ofloxacin, Lomefloxacin, Ciprofloxacin Broad spectrum vs Mycobacterium Active vs Gram (+) Intracellular organisms GI (most common): Nausea, vomiting, abdominal discomfort Hypo/hyperglyc Photosensitivity Connective tissue: Especially in children Prolonged QTc interval Intracellular pathogens High bioavailability; Good for IV to PO switch Enterobacter: Prostatitis Chelators of divalent cations (Ca or Mg may decrease absorption; milk, antacids) Moxi: CA-Pneumonia Bile: Nalidixic acid, moxifloxacin Rifamycins: Rifampicin Binds beta subunit of DNA-dependent RNA polymerase; impairs transcription Single-step mutation in Beta subunit of RNA polymerase Gram (+) and Mycobacterium Harmless orange colored body fluids Cornerstone drug for TB Used to prevent colonization with Staph aureus later on in the course Many drug interaction!: Induces Cyt P450 Metronidazole: Bactericidal Anaerobic infections Rarely (if ever) used alone Clostridium difficile Antimetabolic Antibiotics Sulfonamides: Prophylaxis for immunocompromised patients Bacteriostatic; Competitive inhibitor of DHPS (dihydropteroate synthetase) Trimethoprim Bacteriostatic; Competitive inhibitor of DHFR (Dihydrofolate reductase) Mnemonics We’re ECSTaTiC about bacteriostatics ● Erythromycin, Clindamycin, Sulfamethoxazole, Trimethoprim, Tetracyclines, Chloramphenicol Very Finely Proficient At Cell Murder - Bactericidal Sulfonamides/trimethoprim are used as a Combination drug as a bactericidal “Bactrim” ● Vancomycin, Fluoroquinolones, Penicillins, Aminoglycosides, Cephalosporins, Metronidazole 1st Gen Cephalosporins: SS PEK ● Gram + ○ Streptococci, Staphylococci ● Gram ○ Proteus, E. Coli, Klebsiella pneumoniae 2nd Generation Cephalosporins: HENPEKS ● Gram + ○ Reduced coverage ● Gram ○ H. Influenzae, Enterobacteriaceae, Neisseria (gonorrhoeae, meningitidis), P. mirabilis, E. coli, K. pneumoniae, Serratis ● Anaerobes 3rd Generation Cephalosporins: HENPEK ME ● Gram + ○ Reduced coverage ● Gram ○ H. Influenzae, Enterobacteriaceae Neisseria (gonorrhoeae, meningitidis), P. mirabilis, E. coli, K. Pneumoniae, M. catarrhalis, Better activity with Enterobaceter FlouriqinoLONES: Hurt attachment to BONES Ribosome-Binding Antibiotics ● Buys AT 30: Tetracyclines and aminoglycosides ● CELLS at 50: Chloramphenicol, Erythromycin (Macrolides), Lincosamides (Clindamycin), Linezolid (Oxazolidinones/Zyvox), Streptogramins Drugs of Choice Beta-Lactams First line of defense for Gram + infections Nafcillin (Reduced Suscetpiblity) Susceptible strains of Staph. Aureus (not MRSA) Aminopenicillins Uncomplicated gram + UTIs, unless beta-lactam sensitivity Fosfomycin Single-dose UTI Ceftriaxone/3rd Gen Cephalosporin Neisseria gonorrhoeae, meningitidis Fluoroquinolone Prostatitis (Enterobacter), Community-Acquired Pneumonia Vancomycin 1st Line of Defense: MRSA (IV) and C. Diff (Orally) Linezolid Second Line of Defense: MRSA, VRE, Strep pyogenes, Penresistant strep pneumoniae Metronidazole Second Line of Defense: C. Diff Rifamycin TB - Not used alone (Vanc) Cycloserine Second Line of Defense: TB Aminoglycosides + Beta-Lactams VRE Doxycycline (Tetracyclines) Rickettsiae (Rocky mountain spotted fever), Chlamydiae Tetracyclines Borrelia (lyme disease), Mycoplasma pneumoniae (or macrolide) Macrolides Legionella pneumophila, bordetella pertussis