Antibiotics 1 Flashcards

0
Q

Aerobic bacteria resistant to …

A

Metronidazole

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1
Q

Anaerobes resistant to…

A

Aminoglycerides

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2
Q

Gram - bacteria not penetrated by…

A
Standard penicillins (lipophillic) 
Vancomycin (high mw)
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3
Q

Clostridium difficile caused by..

A

Clindamycin
Cephalosporins
Fluoroquinolones

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4
Q

Treat Clostridium difficile with..

A

Metronidazole or vancomycin

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5
Q

Antibiotics that should have reduced dose in patients with decreased kidney function

A
Aminoglycosides
Vancomycin 
Cephalosporins
Sulfonamides/trimethoprim 
Extended spectrum penicillins
Carbapenems 
Ethambutol
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6
Q

Antibiotics whose does should be reduced in patients with decreased liver function

A
Clindamycin
Macrolides
Chloramphenicol
Tetracycline
Metronidazole
Isoniazid
Rifampin
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7
Q

Most antibiotics are what FDA pregnancy category

A

B or C

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8
Q

What two antibiotics are pregnancy category D?

A

Aminoglycosides and tetracyclines

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9
Q

Most common allergies against antibiotics

A

Beta lactate, sulfonamides, trimethoprim,erythromycin

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10
Q

Beta lactam antibiotics work by..

A
  • Bactericidal
  • Disrupts cross-linking of cell wall by irreversible inhibition of transpeptidases and other penicillin binding proteins (covalent binding)
  • most effective when bacteria is actively dividing
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11
Q

Resistance to beta lactamase

A
  • inability of lipophillic penicillins to penetrate G- membrane
  • acquired mutation of penicillin-binding proteins
  • beta lactamases-cleavage of beta lactam ring
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12
Q

Penicillin G

A

Unstable in stomach - parenteral

Gram + bugs mostly and anaerobes

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13
Q

Penicillin V

A

Oral penicillin

Gram + bacteria and anaerobes

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14
Q

Nafcillin

A

Penicillinase resistant
Anti staph
Used for PEN G resistant staph that is MSSA
No gram -

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15
Q

MRSA

A

Methicillin resistant staph aureus

Altered penicillin binding proteins

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16
Q

Amoxicillin

A
  • Aminopenicillins
  • Activity against G- due to increased penetration
  • suseptible to beta lactamases -given orally with beta lactamase inhibitor (clavulanic acid)
  • upper respiratory infections
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17
Q

Ticarcillin, piperacillin

A

Includes organisms susceptible to aminopeninicillins plus pseudomonas aeruginosa

  • given IV for serious, hospital-acquired G- infections
  • used by beta lactamases inhibitor (clavulanic acid)
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18
Q

Clavulanic acids

A
  • Beta lactamase inhibitor
  • Combined with aminopeninicillins or antipseudomonal extended spectrum (ticarcillin, piperacillin)
  • no bactericidal activity of their own,
  • works with beta lactamases, not against altered penicillin binding proteins
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19
Q

Cephalosporins

A
Beta lactam abx
Given parenterally 
Not effective against MRSA
Grouped into 5 generation 
1)increasing G- bacteria and aerobes
2)increasing resistance to beta lactamases
3) increasing penicillin into CNS
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20
Q

Cefazolin

A

1st generation cephalosporin
Gram +, MSSA and strep
Can be given if mild penicillin allergy
Used before surgery to prevent infections

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21
Q

Cefoxitin

A

Second generation cephalosporins
More activity against G-, higher affinity against PBP
Not used often

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22
Q

Ceftriaxone

A

3rd generation cephalosporin
Good CNS penetration and Gram - coverage
Most widely used
-meningitis, (s. Pneumo, n. Meningitidis, h.flu) and gonnorhea

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23
Q

Cefepime

A

4th generation cephalosporin

Highly resistant to beta lactamases

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24
Carbapenems
Most powerful and broad spectrum beta lactams Highly resistant to inactivation by most beta lactamases Used for multi drug resistant infections, anaerobic and aerobic
25
Impenem/cilastatin
Carbapenems -beta lactams Given parenterally Cilastatin prevents renal inactivation of imipenem
26
Azetreonam
``` Monobactams Single beta lactam ring, not fused with 2nd ring -used w/ penicillin allergies Only effective against gram - aerobes Highly resistant against beta lactamase ```
27
Vancomycin
Glycopeptide Prevents polymerization of cell wall precursors Reserved for serious infections Only effective against gram + Given IV for systemic and dermal, oral for GI tract infections
28
Drugs for VRSA and VRE
Linezolid Daptomycin Quinupristin/dalfopristin
29
Vancomycin resistance
Alters D-Ala-D-Ala to D-Ala-D-lactate | Decreased binding affinity
30
Vancomycin adverse rxns
Ototoxic, nephrotoxic | Rapid infusion- red man syndrome
31
Fosfomycin
Cell wall inhibitor | Gram - UTIs
32
Bacitracin
Cell wall inhibitor Inhibits bactoprenol (lipid that transfers murein monomers across inner cell membrane) bacitracin inhibits phosphorylation -active against Gram + Found in neosporin w/ neomycin/polymyxin B
33
Aminoglycosides
Gentamicin, amikacin, streptomycin, neomycin Highly polar cations - attracted to aerobic Gram (-) drugs Concentration dependent Binds to 30S - misreading of mRNA = nonsense codons
34
Aminoglycoside adverse rxns
``` Ototoxicity-irreversible Elevated trough levels impede egress out of inner ear cells Tinnitus is warning sign Prolonged exposure worse Nephrotoxicity -reversible ```
35
Tetracyclines
Tetracycline, doxycycline, tigecycline Bind to 30S subunit Orally effective, except tigecycline
36
2 classes that bind to 30s subunit
Aminoglycosides | Tetracyclines
37
Use of tetracyclines
Aerobic and anaerobic G+ and G- organisms | Rickettsial infections, chlamydia, Lyme disease, mycoplasma pneumoniae
38
Tetracyclines adverse rxns
``` Deposition in bones and teeth GI irritation Renal toxicity Superinfection -CDAD and candida Photosensitivity Hepatotoxic in pregnant women ```
39
Macrolides
Erythromycin, azithromycin, | Bind to 50S subunit, inhibit translocation
40
Doxycycline
Tetracycline | Inhibit protein synthesis
41
Erythromycin
Macrolides | Inhibit protein synthesis
42
Azithromycin
Macrolides | Inhibit protein synthesis
43
Macrolide resistance mechanisms
Plasma mediated methylation of 50S subunit that decreases binding affinity Efflux transporters
44
Macrolide uses
Substitute for pen-sensitive patients Atypical pneumoniae Pertussis, diphtheria, chlamydia
45
Macrolide adverse rxns
Increased GI motility | Prolonged QT interval
46
Clindamycin
Inhibits protein synthesis -binds 50S subunit Don't use with macrolides Used for most anaerobic bacteria and G+aerobes Group A strep and gas gangrene
47
Clindamycin adverse rxns
C. Diff associated diarrhea
48
Chloramphenicol
Inhibits protein synthesis - 50S subunit Broad spectrum, not used much in US Only used form life-threatening bacterial meningitis
49
Chloramphenicol adverse rxns
Gray baby syndrome-drug accumulates in nursing babies due to insufficient liver metabolism and renal function Bone marrow suppression Aplastic anemia
50
Linezolid
Binds to site on 23S rRNA of the 50s subunit MDR against gram + pathogens -VRE and MRSA Reversible myelosupression Interacts with MAOI and SSRI
51
Quinupristin-Dalfopristin
Bactericidal when combined Inhibit protein synthesis Inhibits peptidyl transferase center of 23S rRNA/same site as macrolides Gram + organisms Serious infections caused by VRE
52
Fluoroquinolones
Nucleic acid synthesis inhibitor | Ciprofloxacin
53
Ciprofloxacin
Fluoroquinolone - inhibits Nucleic acid synthesis | Inhibits topoisomerase II enzymes (DNA gyrase or topoisomerase IV)
54
Inhibit cell wall synthesis - inhibit transpeptidation
Penicillins Cephalosporin Carbapenems
55
Inhibit cell wall synthesis-inhibition of murein precursor synthesis
Fosfomycin Glycopeptides Bacitracin
56
Inhibit cell wall synthesis- inhibit mycolic acid synthesis
Isoniazid Ethambutol Pyrazinamide
57
Inhibit protein synthesis - binds to 30S subunit
Aminoglycosides | Tetracyclines
58
Inhibit protein synthesis- binds to 50S subunit
Macrolides Chloramphenicol Streptogramins Oxazolidinones
59
Inhibition of Nucleic acid synthesis - interferes with folic acid metabolism
Sulfonanamides | Trimethoprim
60
Inhibition of Nucleic acid synthesis- inhibition of DNA gyrase
Fluoroquinolones
61
Inhibition of Nucleic acid synthesis - inhibition of RNA polymerase
Rifampin
62
Disruption of plasma membrane structure/function - dissolve plasma membran
Polymyxins
63
Disruption of plasma membrane structure/function -membrane depolarization
Cyclic lipopeptides
64
Cirpofloxacin uses
Widely used to tx common urogenital, respiratory, GI infections caused by Gram (-) microbes (e. Coli, k. Pneumoniae, enterobacter, salmonella, shigella...) Prophylaxis for anthrax
65
Ciprofloxacin adverse effects
Achilles' tendon rupture - avoid in children under 18 Confusion, somnolence, and visual disturbances in elderly Some prolong QT interval (Careful with IA and III antiarrhymic drugs)
66
Metronidazole
Inhibits Nucleic acid synthesis Prodrug, converted by PFOR or nitroreductase (enzymes found in bacteria) Only works in anaerobes Drug of choice for CDAD Metallic taste, dark red-brown urine Disulfiram rxn with ethanol
67
Metronidazole use and adverse rxns
Drug of choice for CDAD Headache, GI disturbances, metallic taste, dark red-brown urine Disulfiram like rxn with ethanol Inhibits metabolism of warfarin
68
Sulfamethoxazole (SMX)
Folic acid inhibitor (Nucleic acid inhibitor) Inhibits dihydropteroate acid Structural analog of PABA
69
Sulfamethoxazole resistance due to
Synthesis of sufficient PABA to overcome competitive inhibition Mutation of dihydropteroate synthase active site Decreased drug uptake
70
Sulfamethoxazole therapeutic uses and adverse rxns
Broad spectrum -gram + and - UTIs in combo with trimethoprim Kernicterus
71
Trimethoprim (TMP)
Folic acid inhibitor Competitive inhibitor of dihydrofolate reductase (DHFR) Nucleic acid inhibitor
72
Trimethoprim use and adverse rxns
Enteric gram - and + bacilli Suppresses bone marrow in folic acid deficient patients (pregnant, alcoholics, malnourished) Fetal malformations
73
Co-trimoxazole
TMP/SMX | Bactericidal combo that inhibits folate synthesis
74
Co-trimoxazole (TMP/SMX) use and adverse rxns
UTIs pneumocystis jirovicii pneumonia -infection in immunocompromised Otitis media
75
Daptomycin
Plasma membrane disrupter In presence of calcium, inserts lipophilic tail into plasma membrane and forms an ion channel that permits efflux of k = membrane depolarization
76
Daptomycin uses
Only gram + bacteria - MRSA and VRSA (complicated skin and endocarditis) Inactivated by sur
77
Daptomycin adverse rxn
Myopathy
78
Colistin
Polymyxin- plasma membrane disrupter Binds to negatively-charged LPS in out membrane of G- bacteria Disrupts membrane
79
Polymyxin B
Polymyxin- plasma membrane disrupter Binds to negatively-charged LPS in out membrane of G- bacteria Disrupts membrane
80
Colistin sulfate
Topical and oral (GI) use
81
Colistimethate
Polymyxin for parenteral use, prodrug of Colistin
82
Colistimethate uses
Treatment of last resort for MDR G- bacterial infections
83
Colistimethate, polymyxin B use
Topical for infections of skin, mucous membranes, eye and ear
84
Isoniazid
Inhibits synthesis of mycolic acid Prodrug activated by mycobacterial catalase/peroxidase (katG) to free radicals Free radicals bind to NAD+ and NADP+ to in inhibit enzymes involved in mycolic acid synthesis
85
Isoniazid metabolism
Inactivated in liver by acetylation | N-Acetul-INH is excreted by the kidneys
86
Isoniazid adverse rxns
1. Peripheral neuropathy From drug-induced deficiency in pyridoxine (reversed by taking vitamin B6) 2. Hepatotoxicity
87
Rifampin
Inhibits DNA dependent RNA polymerase Used in combination with isoniazid for TB Leprosy Broad spectrum for n. Meningitidis, h. Flu, s. Aureus, legionella
88
Rifampin adverse rxns
Hepatotoxicity Discoloration of body fluids (red-orange) Strong induction of CYP isoforms -increasing elimination of numerous other drugs (esp HIV drugs)
89
Ethambutol
Disrupts assembly of mycobacterial cell wall Inhibits arabinosyl transferase III Used in combo for tx of TB
90
Ethambutol adverse effect
Optic neuritis
91
Pyrazinamide
Prodrug converted to pyrazinoic acid by mycobacterial pyrazinamidase Used as part of combo tx for TB as a sterilizing agent
92
Latent TB tx
Monotherapy for 6mo with INH or Rifampin
93
Active TB tx
First 2 mo ( induction phase) INH, rifampin, pyrazinamide Streptomycin or ethambutol if resistant to INH Next 4 mo (continuation phase) Intermittent therapy with INH + rifampin
94
Pen G and V are _____ spectrum and work against _____ and ______
Narrow spectrum, gram +, anaerobes
95
Penicillinase resistant penicillin that works against MSSA
Nafcillin
96
MRSA is due to
Altered PBPs
97
Amoxicillin is ____ spectrum and works against ______. Used mainly for _____ infections
Broad, gram -, URI (h. Flu, strep pneumo, m. Cat)
98
Ticarcillin and piperacillin work against gram - bacteria as well as _____. Often given IV for _______ infections
Psuedomonas, serious hospital acquired gram -
99
____ and ____ are often used with beta-lactamase inhibitors (clavulanic acid)
Amoxicillin, ticarcillin/piperacillin
100
T/F respository preps (benzathine) fatal if given IV?
True
101
Penicillin allergy is from
Non-enzymatic breakdown of penicilloyl
102
1st gen cephalosporin
Cefazolin
103
2nd gen cephalosporin
Cefoxitin
104
3rd gen cephalosporin
Ceftriaxone
105
4th gen cephalosporin is _____. Used for _____
Cefepime, resistant infections
106
Aztreonam is used for ____
Aerobic gram - bacteria