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37 Cards in this Set

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Penicillins:
MOA/PD?
Resistance & Counteraction?
MOA/PD: B-Lactam & is bacteriocidal by inhibiting cell wall synthesis & work best on rapidly dividing organisms
(1) Bind to penicillin binding proteins which inhibit transpeptidase enzymes
(2) Also cause activation of cell wall autolytic enzymes

Resistance & Counteraction: Intracellular, Cell wall lacking, & Mycobacterium are inherently resistant
(1) Bacteria produce B-lactamases to break down penicillins, Decreased cell wall penetration, Altered PBPs
(2) Resistance has been counteracted somewhat with advent of B-lactamase inhibtors
Penicillins:
Usual excretion, exceptions, drugs that can reduce excretion?
Distribution?
Usual excretion: Most excreted unchanged by kidney w/ 20% being metabolized to penicollic acid
Exceptions: Nafcillin & to certain extent amplicillin are excreted through bile

Distribution: Good but low in CNS unless meninges are inflammed
What are the B-lactamase inhibitors?
Sulbactam
Clavulanic acid
Tazobactam
Penicillin classifications?
(1) Acid labile: Penicillin G
(2) Acid stable: Penicillin V
(3) Penicillinase resistant: Cloxaxillin, Oxacillin, Nafcillin, Dicloxacillin, Methicillin
(4) Broad spectrum: Ampicillin, Amoxicillin
(5) Anti-pseudomonas: Mezlocillin, Carbenicillin, Azlocillin, Ticarcillin, Piperacillin
Penicillins:
General spectrum?
General spectrum: Gram +ve microbes that may not elaborate penicillinase
Penicillins:
General AE?
Interstitial nephritis?
Rash if given to person w/ mono?
Platelet dysfunction?
General AE:
(1) Hypersensitivity w/ hemolytic anemia sometimes noted
(2) CATION TOXICITY in people w/ renal and CVS disease [b/c preparations of Na+, K+ salts]
(3) Jarisch-Herxheimer reaction in syphillis
(4) Superinfection, Intrathecal injection can cause arachnoiditis [convulsions in high dose]
(5) DIARRHEA relatively frequent

Interstitial nephritis: Methicillin
Rash in mono: Ampicillin
Platelet dysfunction: Carbenicillin & ticarcillin
Penicillin G:
Stability?
Types, Route, & Use?
Stability: Acid labile
Types, Route & Use:
(1) Benzyl --> IV, Soluble form
(2) Procaine --> Repository form [therapeutic concentrations maintained for 12-24hr]
(3) Benzathine --> Low but adequate concentrations in prophylaxis
Penicillin V:
Stability?
Route, & Use?
Stability: Acid stable

Route & Use: Oral, Mild infections & prophylaxis
Penicillins [Extended spectrum]:
Names & Route?
Spectrum?
Names & Route:
(1) Amoxicillin --> High oral bioavailibility
(2) Ampicillin --> IV, Rash in mono infection

In addition to Gram +ve add gram -ve
(1) E. coli
(2) Proteus
(3) Salmonella, Shigella,
(4) Listeria monocytogenese
Penicillins [penicillinase resistant]:
Names?
Cloxacillin
Oxacillin
Nafcillin [bile]
Dicloxacillin
Methacillin [nephrotoxic, parenteral only]
Penicillins [anti-pseudomonas]:
Names?
Mezlocillin
Carbenicillin [platelet dysfunction]
Azlocillin
Ticaracillin [platelet dysfunction]
Piperacillin
Imipenem & Meropenem:
Use?
MOA/PD?
Use:
(1) Aerobic, anaerobic, gram +ve & -ve infections
(2) NOT MRSA or C. difficile

MOA/PD: Beta-lactam w/ greater resistance to beta-lactamase [cell wall synth inhib]
Aztreonam:
MOA/PD?
AE?
MOA/PD: Monocyclic beta-lactam [cell wall synth inhib]

AE: Skin rash, Nausea, Vomit, Increased LFT
Bacitracin:
MOA/PD?
MOA/PD:
(1) Inhibit lipid phosphatases thus interfering w/ isoprenyl phosphatewhich is normally used in cell wall synth
(2) It is the ONLY STAGE 2 INHIBITOR of peptidogylcan synthesis [N-cetylmuramyl peptide transferred to CARRIER LIPID and then is modified to form growing peptidoglycan subunit]
Bacitracin:
Use?
Topical only [systemically nephrotoxic]:
(1) INFECTED CORNEAL ULCERS
(2) Skin: Furunculosis, Impetigo, Pyoderma, Carbuncle
(3) Abscesses
Vancomycin:
MOA/PD?
Resistance?
MOA/PD: Binds to growing D-alanyl-D-alanine cell wall precursor thus inhibiting the enzyme TRANSGLYCOLASE [inhib cell wall synth-STAGE 3]

Resistance: Relatively uncommon
(1) Cytoplasmic protein that reduces access of drug
(2) VR enterococci use D-alanyl-D-lactate which has 1000X less affinity for vanco than D-alanyl-D-alanine
Vancomycin: Use?
RESERVED ONLY FOR:
(1) MRSA
(2) Orally for metronidazole resistant pseudomembranous colitis
Vancomycin: AE?
(1) RED-MAN or RED-NECK SYNDROME (flushing)
(2) THROMBOPHLEBITIS
(3) OTOTOXIC & NEPHROTOXIC
(4) Pain, Chills, Rash, Fever, Hypotension, Rarely neutropenia
Aztreonam: Use?
Limited to gonococci, pseudomonas, & H. Infleuenzae
Imipenem & Meropenem:
Metabolism [different]?
AE [different]?
Metabolism: Imipenem inactivated by renal dehydropeptidase [therefor given w/ cilastin which inhibits it]

AE: Seizures [imipenem more likely]
Cilastin: Use?
Adminstered w/ imipenem to prevent hydrolysis by renal dehydropeptidase
Cephalosporins:
MOA/PD?
Similar to penicillin: Cidal
(1) Cell wall synth inhib
(2) Resistance also similar to penicillins
Cephalosporins:
Ineffective against?
MRSA
C. difficile
Listeria monocytogenese
Cephalosporins:
Elimination & Exceptions?
All unchanged through kidneys except:
(1) Cefamandole [2nd generation, disulfuram/hypoprothrombinemia]
(2) Cefoperazone [3rd generation, disulfuram/hypoprothrombinemia]
(3) Ceftrioxone [3rd generation, CSF]
Cephalosporins:
Oral route only?
Oral route only: All with an 'x' in the name and DON'T have a 't' in the name + cefaclor
(1) Cefadroxil [1st generation]
(2) Cephalexin [1st generation]
(3) Cefaclor [2nd generation, Oral, CSF, Serum sickness]
(4) Cefixime [3rd generation]
Cephalosporins:
Oral & IV?
(1) Cephradine [1st generation]
(2) Cefuroxime [2nd generation]
Cephalosporins [1st gen]: Coverage/Use?
Gram +ve:
Staph [au, ep], Strep [pn, py], Anaerobic streptococci
Gram -ve [M PEcK]:
Moroxela catarrhalis, Proteus mirailis, E. coli, Klebsiella pneumoniae
Cephalosporins [2nd gen]: Coverage/Use?
Gram +ve --> Reduced compared to 1st
Strep [pn, py], Anaerobic streptococci
Gram -ve [HENPEcK] --> Enhanced compared to 1st
H. Influenzae, Enterobacter aerogenes, Neisseria gonorrhoeae, Proteus mirailis, E. coli, Klebsiella pneumoniae
Cephalosporins [3rd gen]: Coverage/Use?
Gram +ve --> Weak compared to 1st
Gram -ve [HENPEcK] --> Enhanced compared to 2nd
H. Influenzae, Enterobacter aerogenes, Neisseria gonorrhoeae, Proteus mirailis, E. coli, Klebsiella pneumoniae

Use: Gram -ve bacilli resistant to 2nd generation cephalosporines
Cephalosporins [4th gen]: Coverage/Use?
Coverage: Same as that for 1st and 3rd generations +pseudomonas aeruginosa

Use: Reserved for gram -ve bacilli resistant to 3rd generation cephalosporins
Cephalosporins: B. Fragilis?
(1) Cefoxitin [2nd generation]
(2) Ceftizoxime [3rd generation]
Cephalosporins: Pseudomonas aeruginosa?
(1) Ceftazidime [3rd generation]
(2) Cefepine [4th generation]
Cephalosporins: Disulfuram-like reaction & hypoprothrombinemia & bleeding?
(1) Cefamandole [2nd generation,
billiary]
(2) Cefotetan [2nd generation] --> Notes say no hypoprothrombinemia but lippincott says yes
(3) Moxolactam [3rd generation]
(4) Cefoperazone [3rd generation, billiary]
Cephalosporins: CSF Distribution?
(1) Cefaclor [2nd generation, Oral, CSF, Serum sickness]
(2) Cefuroxime [2nd generation, CSF]
Cephalosporins: Renal toxicity at high doses?
Cephalothin [1st generation]
Cephalosporins:
AE?
Renal toxicity at high doses?

Disulfuram-like reaction & hypoprothrombinemia & bleeding by inhib vit. K depend factors?
AE:
(1) 10% CROSS sensitivity w/ penicillin
(2) Rarely hemolytic anemia

Renal toxicity at high doses: Cephalothin [1st generation]

Disulfuram-like reaction & hypoprothrombinemia:
(1) Cefamandole [2nd generation,
billiary]
(2) Cefotetan [2nd generation] --> Notes say no hypoprothrombinemia but lippincott says yes
(3) Moxolactam [3rd generation]
(4) Cefoperazone [3rd generation, billiary]
Penicillins: DI?
(1) ANTAGONSIM w/ tetracyclines in treatment of pneumococcal meningitis
(2) Non pseudomonal penicillin w/ an anti-pseudomonal may induce b-lactamases that would otherwise not be activated