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Anti-bacterial Drugs
cell wall inhibitors (penicillin,cephalosporins,carbapenem,monobactams); protein synthesis inhibitors (aminoglycoside,tetracycline,clindamycin,chloramphenicol,macolides); DNA interference(quinolones)
55
Pharmacology
Graduate
09/15/2009
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Cards

Term
Beta-Lactams (class)
 Definition

-Mechanism: inhibition of cell-wall synthesis

-Target: almost always gram+ (and occasional gram -)

-Include:

  • penicillins
  • cephalosporins
  • carbapenems (imipenem)
  • monobactams (aztreonam)
Term
Penicillin
 Definition
  • Class-Beta-Lactams
  • Mechanism-inhibition of cell wall synthesis; bind to PBP's in cell wall leading to inhibition of transpeptidase responsible for peptidoglycan cross-linking in cell-wall
  • Target organism-Gram +; not good for Gram - b/c beta-lactamases "snip" B-lactam ring
  • Cidal/Static-Cidal
  • Special-Penicillin G must be given IV/IM b/c degraded by GI tract; 15% have allergy to it due to formation of a hapten (penicillin metabolite that triggers allergic reaction)
Term
Methicillin
 Definition
  • Class-Beta-lactams
  • Sub-class-penicillin
  • Mechanism-Inhibition of cell-wall synthesis
  • Target-Gram+, in particular Staphylococcus (produces penicillinase so we needed an upgrade from penicillin V)
  • Cidal/Static-Cidal
  • Special-MRSA-bacteria synthesizes form of PBP that doesn't have as much affinity for beta-lactam and therefore does not destroy the bacteria
Term
Amoxicillin
 Definition
  • Class-Beta-lactams
  • Sub-class-penicillin
  • Mechanism-Inhibition of cell-wall synthesis
  • Target-Gram+, with gram - coverage of Haemophilis influenzae
  • Cidal/Static-Cidal
  • Special-Ampicillin also falls under this category*
    		•
    Term
    Penicillin V
    		 Definition
  • Class-Beta-lactams
  • Sub-class-penicillins
  • Mechanism-Inhibition of cell-wall synthesis
  • Target-Gram+, in particular Streptococcus
  • Cidal/Static-Cidal
  • Special-upgrade from Penicillin G, b/c not degraded by GI tract and can be taken orally
    		•
    Term
    Piperacillin
    		 Definition
  • Class-Beta-lactams
  • Sub-class-penicillin
  • Mechanism-Inhibition of cell-wall synthesis
  • Target-Gram+, as well as coverage of Pseudomonas aeriginosa (which normally is not covered by penicillins)
  • Cidal/Static-Cidal
  • Special-none
    		•
    Term

    Zosyn

    (piperacillin-tazobactam)

    		 Definition
  • Class-Beta-lactams
  • Sub-class-Extended spectrum penicillin + Beta-lactamase inhibitor
  • Mechanism-Inhibition of cell-wall synthesis for gram + & beta-lactamase inhibitors neutralize many of the lactamases that otherwise inactivate the extended spectrum penicillins (so we have gram (-) coverage too!)
  • Target-Gram+ (Staph/Strep), Gram (-) H.influenzae, Pseudomonas and Bacteroides
  • Cidal/Static-Cidal
  • Special-same activity as Augmentin; mainly given IV
    		•
    Term

    Augmentin

    (amoxicillin-clauvulanate acid)

    		 Definition
  • Class-Beta-lactams
  • Sub-class-Extended spectrum penicillin + beta-lactamase
  • Mechanism-Inhibition of cell-wall synthesis for gram + & beta-lactamase inhibitors neutralize many of the lactamases that otherwise inactivate the extended spectrum penicillins (so we have gram (-) coverage too!)
  • Target-Gram+ (Staph/Strep), Gram (-) H.influenzae, Pseudomonas and Bacteroides
  • Cidal/Static-Cidal
  • Special-Zocyn has same activity*; mainly given IV
    		•
    Term
    Cephalosporins
    		 Definition
  • Class-Beta-lactams
  • Mechanism-Inhibition of cell-wall synthesis with broader spectrum than penicillins
  • Target-Gram+ and gram (-)
  • Cidal/Static-Cidal
  • Special-longer half-life than penicillins; most commonly prescribed therapy for infectious dz; Two side groups allow for manipulation against B-lactamases; entrance through gram(-) porins; enhancement of PBP binding
    		•
    Term
    First generation cephalosporins
    		 Definition
  • Class-Beta-lactams
  • Sub-class-cephalosporins
  • Mechanism-Inhibition of cell-wall synthesis
  • Target-Gram+ and a few gram(-); see Keflex and Ancef cards*
  • Include- Cephalexin (Keflex) and Cefazolin (Ancef)
  • Cidal/Static-Cidal
  • Special-narrow spectrum; sensitive to beta lactamase so does not target many gram(-)
    		•
    Term
    Cephalexin (Biocef/Keflex?)
    		 Definition
  • Class-Beta-lactams
  • Sub-class-first generation cephalosporins
  • Mechanism-Inhibition of cell-wall synthesis
  • Target-Gram+ including Strep and Staph, Gram(-) mainly E.coli
  • Cidal/Static-Cidal
  • Special-none
    		•
    Term
    Cefazolin (Ancef)
    		 Definition
  • Class-Beta-lactams
  • Sub-class-first generation cephalosporins
  • Mechanism-Inhibition of cell-wall synthesis
  • Target-Gram+ including Strep and Staph, Gram(-) mainly E.coli
  • Cidal/Static-Cidal
  • Special-surgical prophylaxis
    		•
    Term
    Second-generation Cephalosporins
    		 Definition
  • Class-Beta-lactams
  • Sub-class-cephalosporins
  • Mechanism-Inhibition of cell-wall synthesis
  • Target-Gram+ and broader gram(-)
  • Cidal/Static-Cidal
  • Include- Cefaclor (Ceclor) and Cefuroxine*
  • Special-extended spectrum with broader coverage of gram(-)
    		•
    Term
    Cefaclor (Ceclor)
    		 Definition
  • Class-Beta-lactams
  • Sub-class-second-generation cephalosporins
  • Mechanism-Inhibition of cell-wall synthesis
  • Target-Gram+ and a few gram(-) with addition of H. influenzae
  • Cidal/Static-Cidal
  • Special-extended spectrum from first generation; also include the drug Cefuroxime
    		•
    Term
    Third-generation Cephalosporins
    		 Definition
  • Class-Beta-lactams
  • Sub-class-cephalosporins
  • Mechanism-Inhibition of cell-wall synthesis
  • Target-Gram+ and a few gram(-); see Ceftriaxone and Cefixime (Suprax)* for details
  • Include- Ceftriaxone and Cefixime (Suprax)*
  • Cidal/Static-Cidal
  • Special-more resistant to cephalosporinases; more able to penetrate CSF
    		•
    Term
    Ceftriaxone
    		 Definition
  • Class-Beta-lactams
  • Sub-class-third-generation cephalosporins
  • Mechanism-Inhibition of cell-wall synthesis
  • Target-Gram+, Gram(-) including N. gonorrhoeae (for gonorrhea)
  • Cidal/Static-Cidal
  • Special-none
    		•
    Term
    Cefixime (Suprax)
    		 Definition
  • Class-Beta-lactams
  • Sub-class-third-generation cephalosporins
  • Mechanism-Inhibition of cell-wall synthesis
  • Target-Gram+, some Gram(-)
  • Cidal/Static-Cidal
  • Special-used to txt Strep respiratory infections
    		•
    Term
    Fourth-generation Cephalosporins
    		 Definition
  • Class-Beta-lactams
  • Sub-class-cephalosporins
  • Mechanism-Inhibition of cell-wall synthesis
  • Target-Gram+, with additional gram(-) coverage; coverage of Pseudomonas
  • Includes: Cefepime and Ceftazidime
  • Cidal/Static-Cidal
  • Special-none
    		•
    Term
    Carbapenems
    		 Definition
  • Class-Beta-lactams
  • Mechanism-Inhibition of cell-wall synthesis
  • Target-Gram+, Gram(-)
  • Include: meropenem; imipenem + cilastatin (primaxin)
  • Cidal/Static-Cidal
  • Special-Also utilize beta-lactam ring but with different side chains, so more resistant to B-lactamases; these drugs can utilize special porins in gram(-) bacteria to gain access to PBPs; Great for broad coverage esp. patients with penicillin/Zocyn allergy*
    		•
    Term
    Imipenem + Cilastatin (Primaxin)
    		 Definition
  • Class-Beta-lactams
  • Sub-class-Carbapenem
  • Mechanism-Inhibition of cell-wall synthesis
  • Target-Gram+, Gram(-)
  • Cidal/Static-Cidal
  • Special-very resistant to B-lactamases; concern with sexure and hypersensitivity at high risk; imipenem is ALWAYS co-administered with Cilastain to avoid degradation by renal dehydropeptidase; used for broad spectrum coverage esp. when patient has penicillin allergy and cannot use Zocyn
    		•
    Term
    Meropenem
    		 Definition
  • Class-Beta-lactams
  • Sub-class-Carbapenem
  • Mechanism-Inhibition of cell-wall synthesis
  • Target-Gram+, Gram(-)
  • Cidal/Static-Cidal
  • Special-very resistant to B-lactamase so good gram(-) coverage; does not need Cilastatin b/c it is stable and can be processed by kidney (unlike imipenem)
    		•
    Term
    Monobactams (Aztreonam)
    		 Definition
  • Class-Beta-lactams
  • Mechanism-Inhibition of cell-wall synthesis
  • Target-Gram(-), especially aerobic including pseudomonas
  • Includes: Only drug available in this class is Aztreonam
  • Cidal/Static-Cidal
  • Special-Ineffective against gram+; high affinity for PBP form in gram(-) bacteria
    		•
    Term
    Vancomycin
    		 Definition
  • Class-Polypeptide (glycopeptide)
  • Mechanism-Inhibits cell wall synthesis (by inhibiting the polymerization of cell wall)
  • Target-Gram+ ONLY; noted for use against MRSA; only for serious infections
  • Cidal/Static-Cidal
  • Special-works by binding to terminal alanine-alanine chains and prevents polymerization (step before penicillins); used to txt bacterial endocarditis*; poor oral absorption; concern w/VRE resistance
  • Allergy/Toxicity- poor interaction with anesthesia resulting in shock (hypotension/cardiac arrest)*; rapid IV infusion triggers histamine release in "red man syndrome"
    		•
    Term
    Bacitracin
    		 Definition
  • Class-Polypeptide (mixture)
  • Mechanism-Inhibits cell wall synthesis
  • Target-Gram+
  • Cidal/Static-Cidal
  • Special-ototoxicity and nephrotoxicity with parenteral use so only used topically ("triple antibiotic ointment")
    		•
    Term
    Polymixin B
    		 Definition
  • Class-Polymixin B (a class of it's own?)
  • Mechanism-Inhibits cell membrane
  • Target-Gram(-)
  • Cidal/Static-Cidal
  • Special-aka Neosporin; long hydrophobic tail to interact with outer membrane of gram(-); used topically
    		•
    Term
    Aminoglycosides
    		 Definition
  • Class-Aminoglycosides
  • Mechanism-interfere with binding of tRNA to 30s ribosomal subunit, blocking protein synthesis
  • Target-Broad spectrum; excellent against gram(-) H.influenza*, enterobacteriaceae*, pseudomonas*
  • Include-Gentamycin; Tobramycin; Streptomycin*; Amikacin*
  • Cidal/Static-Cidal
  • Special-prolongs effects of neuromuscular blocking agents*; Nephrotoxicity and ototoxicity well-recognized s/e of aminoglycosides
    		•
    Term
    Gentamycin
    		 Definition
  • Class-Aminoglycosides
  • Mechanism-Interference with 30s ribosomal subunit
  • Target-broad spectrum (aerobic gram(-); aerobic gram(+))
  • Cidal/Static-Cidal
  • Special-often combined with ampicillin (amp + gent combo) for synergistic activity; nephro/ototoxic
    		•
    Term
    Tobramycin
    		 Definition
  • Class-Aminoglycosides
  • Mechanism-Interference with 30s ribosomal subunit
  • Target-broad spectrum; particularly for hospital acquired infections like Pseudomonas
  • Cidal/Static-Cidal
  • Special-often combined with ampicillin (amp + gent combo) for synergistic activity; nephro/ototoxic
    		•
    Term
    Streptomycin
    		 Definition
  • Class-Aminoglycosides
  • Mechanism-Interference with 30s ribosomal subunit
  • Target-broad spectrum; used to treat TB
  • Cidal/Static-Cidal
  • Special-none
    		•
    Term
    Amikacin
    		 Definition
  • Class-Aminoglycosides
  • Mechanism-Interference with 30s ribosomal subunit
  • Target-broadest spectrum of all aminoglycosides
  • Cidal/Static-Cidal
  • Special-none.
    		•
    Term
    Tetracyclines
    		 Definition
  • Class-Tetracyclines
  • Mechanism-Interference with 30s ribosomal subunit (similar to aminoglycosides)
  • Target-broad spectrum, however more active against gram+
  • Include: Minocycline*; Doxycycline
  • Cidal/Static-Static
  • Special-calcium chelators so s/e on bones and teeth so contraindicated in young children and pregnancy (except for Rocky Mountain spotted fever)
    		•
    Term
    Doxycycline
    		 Definition
  • Class-Tetracyclines
  • Mechanism-Interference with 30s ribosomal subunit
  • Target-Broad spectrum, in particular chlamydia, mycoplasma, tick-borne disease
  • Cidal/Static-Static
  • Special-take on empty stomach so enzymes don't inactivate it; milk and dairy impair absorption; photosensitivity*; teeth discoloration*; avoid in pts with renal dz (acidosis)*; potentiates D-tubocurarine
    		•
    Term
    Macrolides
    		 Definition
  • Class-Macrolides
  • Mechanism-block peptide elongation at 50s ribosomal subunit
  • Target-broad coverage
  • Include- Erythromycin; Clarithromycin*; Clindamycin*; azithromycin
  • Cidal/Static-Static
  • Special-end in "romycin or thromycin"
    		•
    Term
    Erythromycin
    		 Definition

  • Class-Macrolides
  • Mechanism-block peptide elongation at 50s ribosomal subunit

  • Target-broad coverage, drug of choice for Legionella, Campylobacter, Mycoplasma, Bordetella*

  • Cidal/Static-Static
  • Special-GI upset so take with food; hospital aquired Staph usually resistant*

    		•
    Term
    Clarithromycin
    		 Definition

     

  • Class-Macrolides
  • Mechanism-block peptide elongation at 50s ribosomal subunit

    •  

  • Target-broad coverage

    •  

  • Cidal/Static-Static
  • Special-less GI upset
    		•
    Term
    Clindamycin
    		 Definition

     

  • Class-Lincosamide
  • Mechanism-block peptide elongation at 50s ribosomal subunit

    •  

  • Target-broad coverage

    •  

  • Cidal/Static-Static
  • Special-similar to Erythromycin but better for anaerobic bacteria (ie-gut, deep seated wound); can upset flora in GI system leading to pseudomembranous colitis = superinfection (C.diff)
    		•
    Term
    Chloramphenicol
    		 Definition

     

  • Class-Chloramphenicol
  • Mechanism-block peptide elongation at 50s ribosomal subunit
  • Target-broad spectrum coverage; effective against most anaerobic and aerobic, including Salmonella

    •  

  • Cidal/Static-Static
  • Special-toxicity potential with aplastic anemia, therefore rarely used; used to txt meningococcal meningitis due to ability to cross BBB if severe penicillin allergy
    		•
    Term
    Tigecycline
    		 Definition

     

  • Class-Glycylcycline (related to tetracycline)
  • Mechanism-inhibit at 30s ribosomal subunit
  • Target-broad spectrum coverage; covers aerobic gram+ and gram-, anaerobic (weaker tahn meropenem and zosyn) and atypical bacteria
  • Cidal/Static-Static
  • Special-use when patients allergic to penicillin; this is a type of tetracycline with different coverage
    		•
    Term
    Linezolid
    		 Definition

     

  • Class-Linezolid (oxazolidinone)
  • Mechanism-block 50s ribosomal subunit in order to prevent formation of functioning 70s complex

    •  

  • Target-Mainly gram+ (staph and strep); good for VRE and MRSA

    •  

  • Cidal/Static-Static
  • Special-aka Zyvox orally
    		•
    Term
    Quinupristin-dalfopristin (Synercid)
    		 Definition

     

  • Class-N/A
  • Mechanism-interfers with peptide-chain elongation in a synergistic manner

    •  

  • Target-useful for VRE or MRSA

    •  

  • Cidal/Static-unknown
  • Special-many side effects
    		•
    Term
    Daptomycin
    		 Definition

     

  • Class-N/A
  • Mechanism-fatty acid chain intermingles with cell membrane to disrupt it

    •  

  • Target-gram+ pathogens like MRSA, VRE

    •  

  • Cidal/Static-unknown
  • Special-cannot fit through gram(-) porins to affect them
    		•
    Term
    Quinolones
    		 Definition
    • Class-quinolones
    • Mechanism-inhibit bacterial DNA gyrase (to uncoil DNA) and topoisomerase IV 
    • Target-broad coverage, mainly gram(-)
    • Include: Nalidixic acid*; norfloxacin*; ciprofloxacin; levofloxacin
    • Cidal/Static-N/A
    • Special-low toxicity; oral use; associated w. QT prolongation, may predispose to ventricular arrythmias
    Term
    Nalidixic Acid
    		 Definition

     

  • Class-Quinolones
  • Mechanism-inhibit bacterial DNA gyrase 
  • Target-generally gram(-)  
  • Cidal/Static-
  • Special-Norfloxacin ALSO for UTI*
    		•
    Term
    Ciprofloxacin
    		 Definition

     

  • Class-Quinolones
  • Mechanism-inhibit bacterial DNA gyrase 
  • Target-wide spectrum of coverage; Pseudomonas and Anthrax

    •  

  • Cidal/Static-
  • Special-systemic use; penetrates CSF; good absorption
    		•
    Term
    Levofloxin
    		 Definition

     

  • Class-Quinolones
  • Mechanism-inhibit bacterial DNA gyrase

    •  

  • Target-enhanced against gram+; better coverage for severe S. pneumoniae including penicillin resistant strains and Pseudomonas

    •  

  • Cidal/Static-
  • Special-also include Moxifloxacin with this card
    		•
    Term
    Metronidizole (Flagyl)
    		 Definition

     

  • Class-antibacterial/antiprotozoal/drug for amebiasis (diarrhea)
  • Mechanism-addition of N-groups allowing easy diffusion into bacteria/organisms for DNA disruption
  • Target-intestinal and extraintestinal organisms such as: anaerobic bacteria ("ABC's" like C.diff); used for H.pylori to txt acid reflux; protozoans living in low oxygen environments (Entamoeba histolytica, Giardia lamblia, Trichomonas vaginalis)
  • Cidal/Static-Cidal
  • Special-avoid alcohol ingestion; may cause metallic taste and avoid alcohol ingestion; may cause metallic taste and furring of the tongue; Similar drug is Tinidazole; may get nausea due to increased penetration (CNS based, not gut irritation)
    		•
    Term
    Antituberculosis
    		 Definition

     

  • Class-Antituberculosis drugs
  • Mechanism-combination therapy to delay development of resistance
  • Long-term txt over months
  • Must combat unusual cell wall (waxy mycolic acid), a slow rate of growth, and must penetrate caseating granulomas
  • Include: Isoniazid; rifampin; ethambutol; pyrazinamide

    •  
    Term
    Isoniazid
    		 Definition
  • Class-Antituberculosis
  • Mechanism-inhibits synthesis of mycolic acids

  • Target-TB 
  • Cidal/Static-Cidal
  • Special-prodrug activated by mycobacterial catalase/peroxidase; often used as single agent in +PPD; taken in combo to txt active TB to avoid resistance; neural and hepatic toxicity
    		•
    Term
    Rifampin
    		 Definition
  • Class-Antituberculosis
  • Mechanism-inhibits initiation of mRNA synthesis by inhibiting DNA-dependent RNA polymerase

    •  

  • Target-TB

    •  

  • Cidal/Static-Cidal
  • Special-must be combined to avoid rifampin resistance; turns secretions orange
    		•
    Term
    Ethambutol
    		 Definition
  • Class-Antituberculosis
  • Mechanism-inhibits arabinosyl transferase needed to synthesis of arabinoglycan of mycobacterium cell wall
  • Target-TB 
  • Cidal/Static-Cidal
  • Special-optic neuritis concern
    		•
    Term
    Pyrazinamide
    		 Definition
  • Class-Antituberculosis
  • Mechanism-modified nictinamide, mechanism not clear 
  • Target-TB 
  • Cidal/Static-Cidal
  • Special-hepatic toxicity
    		•
    Term
    Sulfonamides (Sulfamethoxazole)
    		 Definition
  • Class-Antimetabolite
  • Mechanism-looks like PABA and competes with PABA for enzyme that couples PABA to dihydropteridine in synthesis of folic acid (so prevents synthesis)
  • Target-UTI, ear infections, prostatitis 
  • Cidal/Static-Cidal
  • Special-selective toxicity based on inability of bacteria to take up preformed folate; interactions can displace other drugs (anesthetics) from plamsa making more of the active form available (this can put patient into a coma); usually used in combo with Trimethoprim
    		•
    Term
    Trimethoprim (in combination, form is Bactrim or Septra)
    		 Definition
  • Class-Folate antagonist
  • Mechanism-interferes with folic acid metabolism at another point in pathway; inhibits folic acid (dihydrofolate) reductase 
  • Target-uncomplicated UTI, AIDS prophylaxis for Pneumocystitis 
  • Cidal/Static-Cidal
  • Special-use in combo with sulfamethoxazole (Bactrim/Septra)
    		•
    Term
    Minocycline
    		 Definition
  • Class-Tetracyclines
  • Mechanism-Interference with 30s ribosomal subunit
  • Target-Broad spectrum, in particular chlamydia, mycoplasma, tick-borne disease
  • Cidal/Static-Static
  • Special-take on empty stomach so enzymes don't inactivate it; milk and dairy impair absorption; photosensitivity; teeth discoloration; avoid in pts with renal dz (acidosis)*; potentiates D-tubocurarine
    		•
    Term
    Norfloxacin
    		 Definition

     

  • Class-Quinolones
  • Mechanism-inhibit bacterial DNA gyrase 
  • Target-generally gram(-)  
  • Cidal/Static-
  • Special-Similar to Nalidixic acid
    		•
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