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Antimicrobials Flashcards

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1
Q

Sub-classes of Beta-lactam antibiotics

A

Penicillins
Cephalosporins
Monobactams
Carbapenems

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2
Q

Beta-lactamase inhibitors

A

Clavulanic acid
Sulbactam
Tazobactam
NXL104

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3
Q

Penicillin mechanism of action

A

binds to penicillin binding proteins in bacterial cell wall - blacks transpeptidase crosslinking

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4
Q

Penicillin activity spectrum

A

Gram positives and syphillis

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5
Q

Penicillin toxicity

A

hypersensitivity rxns, hemolytic anemia

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6
Q

Penicillinase resistant penicillins

A

methicillin
nafcillin
dicloxacillin

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7
Q

Penicillinase resistant penicillin treats which orgs?

A

S. aureus

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8
Q

Penicillinase resistant penicillin toxicity

A

hypersensitivity,

methicillin: interstitial nephritis

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9
Q

Aminopenicillins

A

Ampicillin

Amoxacillin

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10
Q

Aminopenicillins mechanism of action

A

binds penicillin binding proteins (block transpeptidase activity), wider spectrum

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11
Q

Aminopenicillin use

A 
select gram positive and negative bacteria, including:
H. influenzae
Listeria
Proteus
Salmonella
Enterococci
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12
Q

Aminopenicillin toxicity

A

hypersensitivity
ampicillin rash
pseudomembranous colitis

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13
Q

Antipseudomonal drugs

A

Ticarcillin
Piperacillin
Cerbenicillin

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14
Q

Antipseudomonal mechanism of action

A

binds penicillin binding proteins (block transpeptidase activity), wider spectrum

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15
Q

Antipseudomonal use

A

Pseudomonas and gram neg rods

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16
Q

Antipseudomonal toxicitiy

A

hypersensitivity rxn

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17
Q

Bacteriostatic antibiotics

A 
Erythromycin
Clindamycin
Sulfamethoxazole
Trimethoprim
Tetracycline
Chloramphenicol
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18
Q

Bactericidal antibiotics

A 
Vancomycin
Fluoroquinolones
Penicllin
Amnioglycosides
Cephalosporins
Metronidazole
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19
Q

1st generation cephalosporins

narrow spectrum

A

Cefazolin
Cephalexin

Cefadroxil
Cephaloridine
Cephalothin
Cephapirin
Cephradine
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20
Q

1st generation cephalosporin coverage

A

Gram positive cocci
Proteus
E. coli
Klebsiella

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21
Q

Cephalosporin mechanism of action

A

beta lactams
inhibit cell wall synthesis
less susceptible to penicillinases

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22
Q

2nd generation cephalosporins

expanded spectrum

A

Cefoxitin
Cefaclor
Cefuroxime

Cefamandole
Cefmetazole
Cefonicid
Cefotetan
Cefprozil
Loracarbef
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23
Q

2nd generation cephalosporin coverage

A 
same as 1st gen. PLUS:
H. influenzae
Enterobacter
Neisseria
Serratia
(inc. gram neg coverage)
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24
Q

3rd generation cephalosporins

borad spectrum

A 
Ceftriaxone
Ceftazidime
Cefotaxime
Cefdinir
Cefditoren
Cefpodoxime

Cefixime
Cefoperazone
Ceftibuten
Ceftizoxime

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25
3rd generation cephalosporin coverage
serious gram neg. infections Ceftriaxone: Neisseria Ceftazidime: Pseudomonas
26
4th generation cephalosporins
Cefepime Cefteroline Cefpirome* Ceftobiprole* *not licensed for use in the US
27
cephalosporin toxicity
``` Hypersensitivity Vitamin K deficiency Cross-hypersensitivity w/ penicillins Nephrotoxicity of aminoglycosides rxn with alcohol ```
28
Monobactam
Aztreonam
29
Aztreonam mechanism
beta lactamase resistant monbactam | binds PBPs
30
Aztreonam use
Gram neg rods only
31
Aztreonam toxicity
occasional GI upset
32
Imipenem/Cilastatin mechanism
Beta lactamase resistant cerbapenem | Cilastatin is a renal dihydropeptidase 1 (to decrease renal inactivation)
33
Imipenem coverage
Broad spectrum Gram positive cocci Gram neg rods Anerobes
34
Imipenem toxicity
GI distress skin rash CNS toxicity (seizures) at high levels
35
Vancomycin mechanism of action
Binds to terminal D-Ala D-Ala of peptide side chain of peptidoglycan to inhibit cell wall synthesis
36
Vancomycin coverage
``` Gram positives only reserved for resistant infections - S. aureus - Enterococci - C. diff ```
37
Vancomycin toxicity
(well tolerated in general) Nephrotoxicity Ototoxicity Red man syndrome (hypersensitivity)
38
Mechanism of resistance to vancomycin
Bacteria changes terminal D-Ala D-Ala to D-Ala D-Lactate
39
30s ribosomal inhibitors
Tetracyclins | Aminoglycosides
40
50s ribosomal inhibitors
``` Clindamycin Chloramphenicol Erythromycin Linezolid Lincomycin ```
41
Aminoglycosides
``` Gentamicin Neomycin Amikacin Tobramycin Streptomycin ```
42
Mechanism of action of aminoglycosides
Bing to 30s ribosomal subunit to prevent protein synthesis | Requires O2 for uptakes
43
Aminoglycoside use
No anaerobe coverage Severe gram neg. rod infections Synergistic with Beta-lactams Neomycin for bowel suregery
44
Aminoglycoside toxicity
Nephrotoxicity (esp. w/ cephalosporins) Ototoxicity (esp. w/ loop diuretics (for hypertension)) Teratogen
45
Mechanisms of aminoglycoside resistnace
Inactivating enzymes - phosphorylation, adenylation, acetylation Methylation of 16s ribosomal RNA - high resistance to all aminoglycs Efflux pumps
46
Tetracyclin mechanism of action
Binds to 30s ribosomal RNA to block tRNA and inhibit protein synthesis
47
Tetracyclins (drugs)
Tetracyclin Doxycyclin Tigecyclin (similar struct)
48
Tetracyclin coverage
Most GPs and GNs, esp: - Brucella - B. bergdorferi - Chlamydia (intracel. accumulation) - H. pylori - Rikettsia
49
Tetracyclin toxicicty
GI ditress Teeth discoloration Inhibited bone growth in children Photosensitivity
50
Tetracyclin administration considerations
Absorption inhibited by milk/antacids/iron preps | Can be used in pts w/ kidney failure (b/c poor urine conc)
51
Mechanisms of resistance to tetracyclins
Ribosomal protection proteins Efflux pumps Reduced uptake
52
Macrolide drugs
Erythromycin Azithromycin Clarithromycin
53
Macrolide mechanism of action
Binds to 50s subunit of ribosome to inhibit translocation and protein synthesis
54
Macrolide uses
Atypical pneumonias from mycoplasma, chlamydia, legionella URIs STDs Gram pos cocci (in pts allergice to penicillin) Neisseria
55
Macrolide toxicity
``` (Generally very safe!) Prolonged QT GI discomfort Hypersensitivity Transient hearing loss Acute cholestatic hepatitis ```
56
Mechanism of resistance to macrolides
Methylation of the 50s ribosomal subunit (23s binding site) by the erm gene (for erythromycin) Efflux pump encoded by the mef gene (low level resistance)
57
Chloramphenicol mechanism of action
Binds to 50s ribosomal subunit, blicks tRNA
58
Chloramphenicol use/coverage
``` Broad Crosses BBB well - Meningitis (esp low income countries): - H. flu - Neisseria - S. pneumo ```
59
Chloramphenicol toxocity
Dose-related bone marrow suppression (resolves) | Rare but irreversible aplastic anemia (why not available in US)
60
Clindamycin mechanism of action
Binds to 50s ribosomal subunit, inhibits RNA dependent protein synthesis (bacteriostatic)
61
Clindamycin coverage
Excellent for anerobes esp aspiration pneumonia and lung abcesses Reduces toxin production (S. pyogenes and S. aureus)
62
Clindamycin toxicity
Pseudomembeanous colitis Fever Diarrhea
63
Sulfonamide mechanism of action
Competitively inhibits PABA incorporation into folic acid (used in purine synthesis)
64
Sulfonamide coverage
Broad spectrum Gram pos and Gram negs | Also opportunistic infection prophylaxis (in HIV pts)
65
Sulfonamide toxicity
``` Hypersensitivity, Serum sickness GI intolerance Hemolysis in pts w/ G6PD Nephrotoxicity Photosensitivity ```
66
Mechanism of resistance to sulfonamide
Decreased permeability Decreased target enzyme affinity Increased PBPA synthesis
67
Trimethoprim mechanism of action
Inhibits dihydrofolate reductase, potentiating sulfonamide activity
68
Trimethoprim coverage/use
used in combo with sulfamethoxazole for recurrent UTIs, Shigella, Salmonella, pneumocystis
69
Trimethoprim toxicity
Bone marrow suppression (leucopenia, agranulocytosis, thrombocytopenia)
70
Fluoroquinolone mechanism of action
Inhibits bacterial DNA gyrase (exhibits post-antibiotic effect, inc w/ longer exposure or higher dosage)
71
Sulfonamide drugs
Sulfamethoxazole Sulfisoxazole Sulfadiazine
72
1st generation fluoroquinolones
Naladixic acid
73
2nd generation fluoroquinolones
Norfloxacin Ciprofloxacin Ofloxacin
74
3rd generation fluoroquinolones
Levofloxacin | Moxifloxacin
75
4th generation fluoroquinolones
Trovafloxacin (withdrawn)
76
1st generation fluoroquinolone coverage
(Naladixic acid) Good for gram negs. (not pseudomonas) Indicated for uncomplicated UTIs
77
2nd generation fluoroquinolone coverage
``` Gram negs (inc Pseudomonas), some gram pos (not pneumo) Indicated for UTIS, STDs, skin/soft tissue infections ```
78
3rd generation fluoroquinolone coverage
Like 2nd generation, but expanded gram pos coverage (inc pneumo) Indicated for COPD, comm. acq. pneumonia, sinusitis (not for GC b/c of high resistance)
79
Fluoroquinolone toxicity
GI upset

Antimicrobials (3 decks)

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