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Pharmacology Review: Antimicrobials
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1
Pharmacology Review - Antimicrobials
1st gen cephalosporin: G+ cocci, PEcK (Proteus
mirabilis, E. coli, Klebsiella pneumoniae)
1.
2nd gen cephalosporin: G+ cocci, HEN PEcKS
(Haemophilus influenze, Enterobacter aerogenes,
Neisseria species, Proteus mirabilis, E. coli, Klebsiella
pneumoniae, Serratia marcescens
2.
30S protein synthesis inhibitors: Aminoglycosides and
tetracyclines
3.
3rd Generation cephalosporin: serious G- infections
resistant to other Beta lactams; meningitis (most
penetrate BBB)
4.
4th gen cephalosporin: increased activity against
pseudomonas G+ organisms
5.
50S protein synthesis inhibitors: CELL /
Chloramphenicol, Erythromycin, Lincomycin,
cLindamycin // all are bacteriostatic
6.
Aminoglycosides: (streptomycin, gentamicin, tobramycin,
amikacin) / bactericidal
7.
Aminoglygosides: Mechanism of Action: Block protein
synthesis at 30s ribosomal subunit
8.
Amphotericin B: Mechanism of Action: disrupt fungal cell
membranes
9.
Ampicillin: Mechanism of Action: Blocks cell wall
synthesis by inhibition of petidoglycan cross-linking
10.
Ampicillin, Amoxicillin: Same mechanism of action as
penicillin. Wider spectrum; penicillinase sensitive
11.
Ampicillin, amoxicillin (clinical use): ampicillin /
amoxicillin HELPS kill enterococci (Haemophilus
influenzae, Escherichia coli, Listeria monocytogenes,
Proteus mirabilis, Salmonella, enterococci)
12.
Ampicillin, amoxicillin (toxicity): Hypersensitivity
reactions; ampicillin rash; pseudomembranous colitis
13.
Aztreonam: A monobactam resistant to Beta lactamases.
Inhibits cell wall synthesis - synergistic w/
aminoglycosides / no cross-alergenicity w/ penicillins
14.
Aztreonam: Mechanism of Action: Blocks cell wall
synthesis by inhibition of peptidoglycan cross-linking
15.
Aztreonam (clinical use): G- rods (klebsiella species,
Pseudomonas species, Serratia species) // no activity
against anaerobes. // used for penicillin-allergic
patients and those w/ renal insufficiency who can't
tolerate aminoglycosides / usually nontoxic - can cause
GI upset
16.
Bacitracin: Mechanism of Action: Block peptidoglycan
synthesis
17.
Carbenicillin, Piperacillin, ticarcillin: Same mechanism
of action as penicillin; extended spectrum -
pseudomonas species and G- rods; susceptible to
penicillinase; use w/ clavulanic acid; can cause
hypersensitivity reaction
18.
Cephalosporin toxicity: hypersensitivity, increased
nephrotoxicity of aminoglycosides, disulfiram-like
reactions w/ ethanol
19.
Cephalosporins: Mechanism of Action: Blocks cell wall
synthesis by inhibition of peptidoglycan cross-linking
20.
Cephalosporins (mechanism of action): beta lactam
drugs that inhibit cell wall synthesis but are less
susceptible to penicillinases; bactericidal
21.
Chloramphenicol: Mechanism of Action: Block Protein
synthesis at 50s ribosomal subunit
22.
Clindamycin: Mechanism of Action: Block Protein
synthesis at 50s ribosomal subunit
23.
DOC for enterobacter: imipenem / cilastatin24.
2
Erythromycin/Macrolides: Mechanism of Action: Block
Protein synthesis at 50s ribosomal subunit
25.
fluconazole (azoles): Mechanism of Action: disrupt fungal
cell membranes
26.
Gonorrhea: Ceftriaxone (3rd Gen ceph)27.
Imipenem: Mechanism of Action: Blocks cell wall
synthesis by inhibition of peptidoglycan cross-linking
28.
Imipenem / cilastatin: Broad-spectrum, beta
lactamase-resistant / always given w/ cilastatin (inhibits
renal dihydropeptidase 1 --> decrease imipenem
inactivation in renal tubules)
29.
Imipenem / Cilastatin (clinical use): G+ cocci, G- rods,
and anaerobes
30.
Imipenem / cilastatin (toxicity: GI distress, skin rash, and
CNS toxicity (seizures) at high plasma levels
31.
Lincomycin: Mechanism of Action: Block Protein
synthesis at 50s ribosomal subunit
32.
methicilin, nafcillin, dicloxacillin (toxicity):
hypersensitivity reactions
33.
Methicillin (toxicity): interstitial nephritis34.
Methicillin, nafcillin, dicloxacillin: same mechanism of
action as penicillin. Narrow spectrum; Penicillinase
resistant due to bulkier R group
35.
Methicillin, nafcillin, dicloxacillin: clinical use --> treat
staph aureus
36.
Nystatin: Mechanism of Action: disrupt fungal cell
membranes
37.
Penicillin: 2 forms G (IV form) // Penicillin V (oral)38.
Penicillin: Mechanism of Action: Blocks cell wall synthesis
by inhibition of peptidoglycan cross-linking
39.
Penicillin (clinical use): bactericidal for G+ cocci, G+
rods, G- cooci, and spirochetes. Not penicillinase
resistant
40.
Penicillin (mechanism of action): 1. Binds
penicillin-binding proteins 2. Blocks transpeptidase
cross-linking of cell wall 3. Activates autolytic enzymes
41.
Penicillin (toxicity: hypersensitivity reactions, hemolytic
anemia
42.
Pentamidine: Mechanism of Action: unknown mechanism
of action
43.
Piperacillin: Mechanism of Action: Blocks cell wall
synthesis by inhibition of peptidoglycan cross-linking
44.
Polymyxins: Mechanism of Action: Disrupt
bacterial/fungal cell membranes
45.
Pseudomonas: ceftazidime (3rd gen ceph)46.
Quinolones: Mechanism of Action: Block DNA
topoisomerases
47.
remember: amOxicillin has greater Oral bioavailability
than ampicillin
48.
Rifampin: Mechanism of Action: Block mRNA synthesis49.
Streptogramins (quinupristin,dalfopristin): Mechanism
of Action: Block Protein synthesis at 50s ribosomal
subunit
50.
Tetracyclines: bacteriostatic51.
Tetracyclines: Mechanism of Action: Block protein
synthesis at 30s ribosomal subunit
52.
Ticarcillin: Mechanism of Action: Blocks cell wall
synthesis by inhibition of peptidoglycan cross-linking
53.
Vancomycin: Mechanism of Action: Block peptidoglycan
synthesis
54.
Vancomycin (clinical use): used for serious, G+
multidrug-resistant organisms. including staph aureus
and Clostridium difficile (pseudomembranous colitits)
55.
Vancomycin (mechanism of action): inhibits cell wall
mucopeptide formation by binding D-ala D-ala portion
of cell wall precursors / Bactericidal / resistance occurs
w/ amino acid change of D-ala D-ala to D-ala D-lac
56.
Vancomycin tocicity: NOT - Nephrotoxicity, Ototoxicity,
and Thrombophlebitis, diffuse flushing -->"red man
syndrome" (can prevent w/ pretreatment w/
antihistamines and slow infusion rate)
57.
3
What can you combine w/ ampicillin or amoxicillin to
enhance spectrum: clavulanic acid (penicillinase
inhibitor)
58.