-
Penicillins
- Bind PBPs, Bactericida;, GM+.
- Inhibited by Beta lactamases; Efflux of drug; Porin size (Gm-)
- PenG=IV, IM; PenV=PO; 1st generation; effective vs growing bacteria
-
Methicillin (IV), Dicloxacillin, Naficillin, Oxacillin (PO)
- Gm+ Same inhibition as Penicillins
- Resistances due to penicillinase of Staph (mec A encodes PBP2); CA has PV toxin
-
Ampicillin
Amoxicillin
- Bind PBPs, Bactericidal, Gm+; growing E. coli, ProteusSame inhibition as penicillins
- PO; 2nd generation, Broad-spectrum
-
Carbenicillin, Ticarcillin, Piperacillin
- Bind PBPs, Bactericidal, Gm+ & Gm-, including PseudomonasSame inhibition as PenicillinsPO, 3rd generation, Extended Spectrum
-
-
Cefazolin, Cephalothin, Cefalexin
- Bind PBPs
- Bactericidal
- E.coli, Klebs, Proteus, Gm+ cocci
- Inhibition - Pen
- 1st gen cephs, Narrow spectrum
-
Cefoxitin, Cefaclor
- Bind PBPs
- Bactericidal
- 1st gen microbes + H. flu, Enterobacteriaceae, Bacteriodes
- Inhibition - Pen
- 2nd gen, Expanded spectrum
-
Ceftazidine, Cefixime, Cefotaxime, Ceftriaxone
- Bind PBPs
- Bactericidal
- Broad Spectrum +, Psuedo. Aerug.
- Inhibition - Pen
- 3rd gen, Broad spectrum, including Meningtis in kids
-
Cefepime
- Bind PBPs
- bactericidal
- Broad spectrum + Pseudo. Aerug.
- 4th gen; Ext spectrum
-
Carbapenems
- Bind PBPs
- Bactericidal
- Broad spectrum
- Resistant to Beta-Lactamases
- Broad Spectrum
-
Monobactams
(Aztreonam)
- Bind PBPs
- Bactericidal
- Aerobic Gm; Enterobacteriaceae
- resistant to Beta-lactamases
- IV use; Narrow spect vs Gm- Rods; Given to those allergic to penicillin
-
Clavulanis acid
Tazo- & Sulbactams #
- Beta-lactamase inhibitors
- Depends on penicillin
- Variable targets
- Plasmid and Chrom. Encoded
- Dependent on Penicillin
-
Vancomycin
- Affects (D-ala)2 chain in growing cells
- MRSA; C. diff; No effect vs E. faecium or faecalis Inh - Doesnt cross OM of Gm-; Modify D-ala to D-ala-D-ser or D-lactate
- Given IV; Rx vs antibiotic assoc. colitis (AAC); Drug of last resort except for MRSA, AAC
-
Isoniazid
- Affects mycolic acid synthesis
- Bactericidal
- Mycobacteria (growing cells)
- Dec drug uptake; res in TB
- PO; 1st line TB Rx; Hepatotoxic
-
Aminoglycosides
(Streptomycin, Gentamycin, Kanamycin, Tobramycin, Neomycin, Spectinomycin)
- Irreversible bind 30S ribosomes
- bactericidal
- Gm- (include Pseudomonas; ineffective vs. anaerobes, streptococci, enterococci)
- Mutation in 30S binding site; Dec. drug uptake; Enzymatic modification of drug
- Nephro- & ototoxic; Streptomycin 1st line vs. TB
-
Tetracyclines
- Reversible bind 30S ribo. subunits
- Bacteriostatic
- Selective Gm- and +; Chlamydia, Rickettsia, Mycoplasma
- Dec. drug uptake;
Active efflux; Protection of 30S ribo - Stain teeth in young kids <8 y/o; NVD; Photosens.
-
Macrolides
(Erythromycin, Azithromycin, Clarithromycin, Telithromycin)
- Reversible bind 50S ribo subunit
- Bacteriostatic
- MAC complex; Mycoplasma; Pneumococcus; Chlamydia ineffective vs. EnterobacteriaceaeMethylation of 23S rRNA; dec drug uptake; Intrinsic res. of OM for Enterics
- NV Crosses placenta; Hepatotoxic
-
Rifamycin B
(Rifampin, Rifabutin)
- Binds RNA polymerase
- Bactericidal vs. TB; Static vs. Staph & Strep
- TB; Neisseria meningitides, prophylaxis, M. avium
- Turns urine orange; 1st line vs TB
-
Lincosamides
(Clindamycin)
- Bind 50S ribo subunits
- Bacteriostatic
- Strep, Staph, Gm - rods; anaerobes except C. difficile Inh - Plasmid - encoded res.
- NVD; Skin rashes
-
Pleuromutilins
(Tiamulin, retapamulin)
Altabax
Interact with 50S ribo subunit at peptidyl trans. center at A&P binding sites (a)
- Staph aureus, Strep. pyo, Pneumococcus, H flu, Moraxella, anaerobes (P acnes) (b)
- Mutations in rplC (Staph aureus)
- Site irritation
-
Cloramphenicol (Cm or Cam)
- Revers. binds 50S ribo; prevents peptide bond formation
- Bacteriostatic ex for H. flu, Meingococcus (cidal)
- Salmonella typhiCm acetyl-transferase; Alter OM porins
- Aplastic anemia; Toxic for neonates; Drug of last resort except for typhoid fever
-
Oxazolidinones
(Linezolid)
- bind 50S at 23S rRNA to inhibit pr synthesis
- Bacteriostatic ex. for strep (cidal)
- Staph, Strep, Enterococci, esp. VRE
- Mutation of 23S rRNA binding site
- Thrombocytopenia, neutropenia
-
Streptogramins (Synercid): Quinupristin & Dalfopristin
- Two drugs bind different sites on 50S ribo
- bactericidal ex. for E. faeciumGm+, including S.aureusEfflux mech. (Esp. E. faecalis)
- IV; Arthralgia
-
Sulfonamides
- PABA antagonist
- Bacteriostatic
- Broad Spect
- Plasmid encoded enzyme; PseudomonasAllergic rxn; Jaundice
-
Trimethoprim
- Dihydrofolate reductase inhibitor
- Bacteriostatic
- Broad Spectrum
- Plasmid-encoded enzyme; Pseudomonas Megaloblastic anemia, leukopenia, granulocytopenia
-
Dapsone
- Dihydrofolate
- Leprosy
- Rash, Hemolysis
-
Flouroquinolones
(Ciprofloxacin, Levofloxacin, Ofloxacin,Gemifloxacin, Naldixic acid)
- Inhibit alpha subunit of DNA Gyrase (topo II & IV)
- Bactericidal
- Wide range
- Altered alpha subunit, DNA gyrase; qnrA, qnrB on plasmid ^ decrease drug uptake feq of 10E-8
- NVD, arrhythmias, arthropathy in patients <10 y/o
-
Ethambutol
- Inhibits arabinogalactan synthesis
- Mycobacteria
- Inh - Decrease drug uptake; altered target sites
- 1st line vs TB
-
Pyrazinamide
- Inhibits arabinogalactan sythesis
- Mycobactera
- Inh - Decrease drug uptake; altered target sites
- 1st line vs TB
-
Pyrazinamide
- Mycobacteria
- pncA mutations
- 1st line vs TB
-
Polymixin B, Polymixin E (colistin)
- Interact w/ LPS, phospholipids in OM
- Bactericidal
- Gm - including Pseudomonas; but not Proteus and Neisseria
- Inh - Gm+ lack outer membrane
- Topical use; nephrotoxic
-
Bacitracin
- inhibits lipid carrier of peptidoglycan
- Gm+
- Inh - Gm-: intrinsic res; membrane impermeable
- Topical use; Nephrotoxic
-
Metronidazole
- Reduction of nitro group disrupts DNA
- Anaerobes, protozoans
- Inh - Decrease uptake; elimination of reduced nitro group
- No effect vs aerobes or facult. NV with EtOH; GI irritant; Not used with CNS disease -
-
Augmentin
Combination of penicillin + Beta-lactamase inhibitor
-
Gemifloxacin or Factive
- Used to treat pneumonia
- acute sinusitis
-
1st Line TB drugs
INH, rifampin, ethambutol, pyrazinamide (rifabutin no FDA approved)
-
2nd line TB drugs
- Cycloerine, ethionomide, p-aminosalicylate, streptomycin, capreomycin
- (levofloxacin, gatifloxacin, amikacin/kanamycin no FDA-approved)
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