Unit 6-Antibiotics Flashcards
1
Q
Penicillin G (IV); penicillin V (PO) Drug class
A
Penicillins (Cell wall synthesis inhibitor)
2
Q
Penicillin G (IV); penicillin V (PO) Mechanism
A
Form a complex with a PBP, prevent extracellular transpeptidase activity
3
Q
Penicillin G (IV); penicillin V (PO) Uses
A
Streptococcal species, resistance in some species (S. pneumoniae, S. anginosus group, viridians group); mouth anaerobes; syphilis; poor Staph
Not effective against β-lactamase-producing bacteria.
4
Q
Penicillin G (IV); penicillin V (PO) Side effects
A
Hypersensitivity reactions
Seizures at high doses in patients w/ renal dysfunction.
5
Q
oxacillin (IV); nafcillin (IV); dicloxacillin (PO)
Drug class
A
Penicillinase-resistant penicillin
6
Q
oxacillin (IV); nafcillin (IV); dicloxacillin (PO)
Mechanism
A
Bulky side chain shields β-lactam ring from penicillinase
7
Q
oxacillin (IV); nafcillin (IV); dicloxacillin (PO)
Uses
A
Methicillin-sensitive S. aureus (MSSA)
8
Q
oxacillin (IV); nafcillin (IV); dicloxacillin (PO)
Side effects
A
Hypersensitivity reactions
Hepatotoxicity & neutropenia w/ oxacillin; neutropenia & thrombophlebitis w/ nafcillin
9
Q
Ampicillin (IV, PO); amoxicillin (PO)
Drug class
A
Aminopenicillin
10
Q
Ampicillin (IV, PO); amoxicillin (PO)
Mechanism
A
Semi-synthetic penicillins with special side group allows improved penetration into Gram - membrane
11
Q
Ampicillin (IV, PO); amoxicillin (PO)
Uses
A
Streptococcus (DoC for Enterococcus); mouth anaerobes; E. coli, Proteus mirabilis, Listeria
“Amoxicillin better absorbed than ampicillin PO. Gram-negative activity improved compared to PCN. Still not effective against penicillinase-producing Staph”
12
Q
Ampicillin (IV, PO); amoxicillin (PO)
Side effects
A
Hypersensitivity reactions
Delayed hypersensitivity reaction common if given during viral infection
13
Q
Piperacillin (IV); Ticarcillin
Drug class
A
Extended spectrum penicillin
14
Q
Piperacillin (IV); Ticarcillin
Mechanism
A
More manipulations to extend aminopenicillin spectrum
15
Q
Piperacillin (IV); Ticarcillin
Uses
A
Activity of aminopenicillins plus Proteus; Klebsiella, Serratia, Enterobacter, Pseudomonas
Rarely used without tazobactam
16
Q
Piperacillin (IV); Ticarcillin
Side effects
A
Hypersensitivity reactions
17
Q
Zosyn IV (piperacillin + tazobactam); Augmentin PO (amoxicillin + clavulanate) Drug class
A
Combination therapy penicillins
18
Q
Zosyn IV (piperacillin + tazobactam); Augmentin PO (amoxicillin + clavulanate) Mechanism
A
Suicide inhibitors that allow penicillins to do their job
19
Q
Zosyn IV (piperacillin + tazobactam); Augmentin PO (amoxicillin + clavulanate) Uses
A
Retention of spectrum of parent drug with increased activity against β-lactamase producing organisms
(S. aureus, gut anaerobes, all Haemophilus, E. coli)
Augmentin not effective against Pseudomonas
20
Q
Zosyn IV (piperacillin + tazobactam); Augmentin PO (amoxicillin + clavulanate) Side effects
A
Hypersensitivity reactions;
Augmentin: diarrhea
Immune-mediated thrombocytopenia
21
Q
Cefazolin (IV); cephalexin (oral)
Drug class
A
1st generation cephalosporin (Cell wall synthesis inhibitor)
22
Q
Cefazolin (IV); cephalexin (oral)
Mechanism
A
Form a complex with a PBP, prevent extracellular transpeptidase activity; broader spectrum than penicillins
23
Q
Cefazolin (IV); cephalexin (oral)
Uses
A
S. aureus; strep (NO Enterococcus); E. coli, Proteus, Klebsiella; mouth anaerobes
Cefazolin-DOC for surgical prophylaxis
24
Q
Cefazolin (IV); cephalexin (oral)
Side effects
A
Hypersensitivity reactions
25
Cefuroxime
| Drug class
2nd generation cephalosporin
26
Cefuroxime
| Mechanism
As 1st generation cephalosporins
27
Cefuroxime
| Uses
Less. S. aureus coverage; 1st generation plus Haemophilus (including penicillinase strains); above and below diaphragm anaerobes
28
Cefuroxime
| Side effects
Hypersensitivity reactions
29
Cefoxitin; cefotetan
| Drug class
2nd generation cephalosporin
30
Cefoxitin; cefotetan
| Mechanism
As 1st generation cephalosporins
31
Cefoxitin; cefotetan
| Uses
More active against E. coli & Klebsiella than 1st generation; B. fragilis
32
Cefoxitin; cefotetan
| Side effects
Hypersensitivity reactions
33
Ceftazadime (IV); cefpodoxime (PO); ceftriaxone (IV)
| Drug class
3rd generation cephalosporin
34
Ceftazadime (IV); cefpodoxime (PO); ceftriaxone (IV)
| Mechanism
As 1st generation cephalosporins
35
Ceftazadime (IV); cefpodoxime (PO); ceftriaxone (IV)
| Uses
Ceftazidime: poor gram-positive activity
Ceftriaxone less active against MSSA than 1st generation cephs, but active against Strep;
enhanced activity against gram-negatives
Ceftazdime: Pseudomonas
36
Ceftazadime (IV); cefpodoxime (PO); ceftriaxone (IV)
| Side effects
Higher association with C. difficile diarrhea than other classes
Ceftriaxone-biliary sludging, precipitation with calcium containing solutions in neonates
37
Cefepime (IV)
| Drug class
4th generation cephalosporin
38
Cefepime (IV)
| Mechanism
As 1st generation cephalosporins
crosses BBB
39
Cefepime (IV)
| Uses
3rd generation, plus Staphylococcus coverage
40
Cefepime (IV)
| Side effects
Mostly allergenic
41
Ceftaroline (IV)
| Drug class
5th generation cephalosporin
42
Ceftaroline (IV)
| Mechanism
Possesses a side chain that acts as a "Trojan horse" allowing access to PBP2a
43
Ceftaroline (IV)
| Uses
Gram positive-MRSA, MSSA, Streptococci, E. faecalis not faecium Gram negative activity similar to ceftriaxone
Only cephalosporin with activity against MRSA!
44
Ceftaroline (IV)
| Side effects
Mostly allergenic
45
Ceftazidime/Avibactam (IV)
| Drug class
Extended-spectrum cephalosporin/b-lactamase inhibitor combinatioon
46
Ceftazidime/Avibactam (IV)
| Mechanism
As 1st generation cephalosporins. B-lactamase inhibitor increases gram(-) spectrum.
47
Ceftazidime/Avibactam (IV)
| Uses
Increased Psuedomonas, CRE, ESBL activity
48
Ceftazidime/Avibactam (IV)
| Side effects
Higher association with C. difficile diarrhea than other classes
Mostly allergenic
49
Ceftolozane/Tazobactam (IV)
| Uses
Increased activity against Psuedomonas, ESBLs. Not active against CREs.
50
Imipenem - cilastatin; Meropenem; Ertapenem; Doripenem (all IV)
Drug class
Carbapenam (Cell wall synthesis inhibitor)
51
Imipenem - cilastatin; Meropenem; Ertapenem; Doripenem (all IV)
Mechanism
Similar to pencillins
52
Imipenem - cilastatin; Meropenem; Ertapenem; Doripenem (all IV)
Uses
```
Broad spectrum (excludes MRSA)
Ertapenem: not effective against Pseudomonas, Acinetobacter
Used for highly-resistant organisms
```
53
Imipenem - cilastatin; Meropenem; Ertapenem; Doripenem (all IV)
Side effects
Imipenem: higher risk of seizures than other β-lactams (cumulative dose-dependent) if dose not adjusted for renal failure
Significant interaction with valproic-acid (VPA) (reported predominantly with meropenem)-significant reduction in VPA concentration leading to seizures
Low cross-reactivity with PCN (~1%)
54
Aztreonam (IV)
| Drug class
Monobactam (Cell wall synthesis inhibitor)
55
Aztreonam (IV)
| Mechanism
Similar to pencillins
56
Aztreonam (IV)
| Uses
Gram- aerobic bacilli including Pseudomonas, no G+, no anaerobes
57
Aztreonam (IV)
| Side effects
Not usually used as monotherapy; no cross-allergenicity with penicillins
58
Vancomycin (IV, PO)
| Drug class
Cell wall synthesis inhibitor (Glycopeptide)
59
Vancomycin (IV, PO)
| Mechanism
Binds rapidly and irreversibly to the D-alanyl-D-alanine group on the peptide side-chain of the membrane-bound precursor; glycan chain extension, transpeptidation inhibited
60
Vancomycin (IV, PO)
| Uses
G+s only (MRSA, Enterococcus, coagulase-negative Staph, Strep)
PO: C. difficile
IV not effective for C. difficile. Slowly bactericidal against Staph.
Bacteriostatic against Enterococcus. Inferior to β-lactams for MSSA infection
61
Vancomycin (IV, PO)
| Side effects
IgE hypersensitivity reactions (histamine mediated); "red man syndrome"); dose-dependent nephrotoxicity; immune-mediated thrombocytopenia
Dose-dependent ototoxicity and nephrotoxicity; immune-mediated thrombocytopenia
62
Dalbavancin; Telavancin; Oritavancin
| Drug class
Lipoglycopeptides (anaolgs of vancomycin)
63
Dalbavancin; Telavancin; Oritavancin
| Mechanism
Binds to same target as vancomycin and inhibits transglycosylation
64
Dalbavancin; Telavancin; Oritavancin
| Uses
Similar to vancomycin but active against VRE & more anaerobe coverage
65
Dalbavancin; Telavancin; Oritavancin
| Side effects
Metallic taste, nausea, HA, nephrotoxicity, teratogenic
Pregnancy test needed for women of childbearing potential.
66
Daptomycin (IV)
| Drug class
Cell wall toxin (cyclic lipopeptide)
67
Daptomycin (IV)
| Mechanism
Penetrates bacterial cell wall, forming a channel for subsequent leakage of intracellular ions
68
Daptomycin (IV)
| Uses
G+ cocci only; use for VRE, VRSA
69
Daptomycin (IV)
| Side effects
Myalgia and rarely rhabdomyolysis
Eosinophilic pneumonia
Resistance has occurred during therapy. Higher doses (8-10 mg/kg/d) recommended for severe infections
70
Colistin (IV, INH)
| Drug class
Cell wall toxin (polymixin)
71
Colistin (IV, INH)
| Mechanism
Penetrates bacterial cell wall, forming a channel for subsequent leakage of intracellular ions
72
Colistin (IV, INH)
| Uses
G- only; usually reserved for Pseudomonas species resistant to all other antibacterials
73
Colistin (IV, INH)
| Side effects
Nephrotoxicity, neurotoxicity
74
Ciprofloxacin (IV, PO)
| Drug class
1st generation fluoroquinolone / Nucleic acid synthesis inhibitor
75
Ciprofloxacin (IV, PO)
| Mechanism
Inhibits DNA gyrase at low concentrations
76
Ciprofloxacin (IV, PO)
| Uses
Enterobactericeae, including Pseudomonas;
| Atypicals
77
Ciprofloxacin (IV, PO)
| Side effects
GI, AMS
QT prolongation, tendon rupture
Divalent cations chelate ORAL quinolones decreasing bioavailability
78
Levofloxacin (IV, PO); Moxifloxacin (IV, PO)
| Drug class
2nd generation fluoroquinolone / Nucleic acid synthesis inhibitor
79
Levofloxacin (IV, PO); Moxifloxacin (IV, PO)
| Mechanism
Inhibits DNA gyrase at low concentrations; inhibits topoisomerase IV at high concentrations
80
Levofloxacin (IV, PO); Moxifloxacin (IV, PO)
| Uses
```
Adds pneumococcus (Strep pneumoniae) to spectrum of 1st generation fluoroquinolones.
Levofloxacin: Pseudomonas
Moxifloxacin: No Pseudomonas, but has anaerobic activity
```
Moxifloxacin urine concentrations low-not ideal for UTI
Levofloxacin and ciprofloxacin are the only PO agents effective against Pseudomonas
81
Levofloxacin (IV, PO); Moxifloxacin (IV, PO)
| Side effects
As with cipro; QT prolongation: moxi>levo>cipro
82
Metronidazole (IV, PO)
| Drug class
Nucleic acid synthesis inhibitors (Nitroimidazole)
83
Metronidazole (IV, PO)
| Mechanism
Reduced (only under anaerobic conditions, which generate lots of acid) to an active free radical, which damages bacterial and certain protozoal DNA
84
Metronidazole (IV, PO)
| Uses
Anaerobes excluding Actinomycetes and Peptostreptococcus (DoC for C. difficile); some protozoa; H. pylori
85
Metronidazole (IV, PO)
| Side effects
metallic taste,disulfiram-like reaction (because it blocks aldehyde dehydrogenase)
CNS toxicity-seizure, neuropathy with long-term/high dose therapy
86
Rifampin (IV, PO)
| Drug class
Nucleic acid synthesis inhibitor
87
Rifampin (IV, PO)
| Mechanism
Inhibits DNA-dependent RNA polymerase to halt RNA transcription)
88
Rifampin (IV, PO)
| Uses
Mycobacterium tuberculosis; Staph aureus
89
Rifampin (IV, PO)
| Side effects
Centrilobular hepatitis; serious flu-like hyper-sensitivity syndrome characterized by fever, myalgias, interstitial nephritis, thrombocytopenia, hemolytic anemia (occurs if drug given in intermittent dosing regimens)
NEVER use as monotherapy due to risk of resistance
Potent inducer of CYP 450 system-results in lower concentration of substrates
90
Isoniazid (INH)
| Drug class
Antitubercular
91
Isoniazid (INH)
| Mechanism
Inhibition of mycolic acid synthesis
92
Isoniazid (INH)
| Uses
Mycobacterium
93
Isoniazid (INH)
| Side effects
Hepatitis; neurotoxicity:memory loss, psychosis (pyridoxine can alleviate); hypersensitivity reactions
Phenytoin toxicity potentiated by INH.
94
Pyrazinamide
| Drug class
Antitubercular
95
Pyrazinamide
| Mechanism
Unknown
96
Pyrazinamide
| Uses
Mycobacterium
97
Pyrazinamide
| Side effects
N&V; hepatotoxicity; hypersensitivity reactions
98
Ethambutol
| Drug class
Antitubercular
99
Ethambutol
| Mechanism
Inhibits arabinosyl transferase enzymes involved in cell wall synthesis
100
Ethambutol
| Uses
Mycobacterium
101
Ethambutol
| Side effects
Neuropathy; optic neuritis
102
Gentamicin; tobramycin
| Drug class
Aminoglycoside / Protein synthesis inhibitor
103
Gentamicin; tobramycin
| Mechanism
Inhibits 30S ribosome: forms a tight complex with ribosomal protein, causing codon-anticodon misreading and production of inactive proteins (bactericidal); also, inhibits initiation
104
Gentamicin; tobramycin
| Uses
Extremely effective against G- rods; ineffective against anaerobes due to an oxygen-dependent uptake mechanism,
Rapid lethal effect; synergistically useful with cell-wall active agents for Enterococcus infections
105
Gentamicin; tobramycin
| Side effects
Dose-dependent oto/nephrotoxicity (not observed if used less than 48 hours)
106
Doxycycline; Minocycline (both IV, PO)
| Drug class
Tetracycline / Protein synthesis inhibitor
107
Doxycycline; Minocycline (both IV, PO)
| Mechanism
Inhibits 30S ribosome: blocks access of tRNA anticodon to its codon
108
Doxycycline; Minocycline (both IV, PO)
| Uses
utility for Gram+ (S. pneumoniae, MRSA); very effective against intracellular pathogens (mycoplasma, chlamydia, legionella, rickettsia)
109
Doxycycline; Minocycline (both IV, PO)
| Side effects
GI; skin photosensitivity
Pill esophagitis if not taken with water
ORAL forms are chelated with divalent cations (Calcium, Mg, iron, etc.)
Discolors teeth of younger children-avoid use in pregnancy as well
110
Tigecycline (IV)
| Drug class
Glycylcyline
111
Tigecycline (IV)
| Mechanism
Inhibits 30S ribosome: glycyl group prevents efflux out of cell
112
Tigecycline (IV)
| Uses
Broad spectrum including MRSA, VRE, Enterobacteriaceae, and anaerobes.
DOES NOT have activity against Pseudomonas. Often one of few drugs effective against carbapenem-resistant Enterobacteriaceae
113
Tigecycline (IV)
| Side effects
Much higher tissue concentrations than serum. Not effective in bacteremia
Higher all-cause mortality than other drugs
114
Clindamycin (IV, PO)
| Drug class
Protein synthesis inhibitors
115
Clindamycin (IV, PO)
| Mechanism
Binds to 50S subunit at “A site,” blocking peptide bond formation
116
Clindamycin (IV, PO)
| Uses
CA-MRSA/MSSA, Strep (resistance in Group B strep and S. aureus increasing
Mouth anaerobes
NO gram negative
117
Clindamycin (IV, PO)
| Side effects
Antibiotic-associated diarrhea; C. difficile colitis
118
Azithromycin (Z-Pak PO, IV))
| Drug class
Macrolide /Protein synthesis inhibitors
119
Azithromycin (Z-Pak PO, IV))
| Mechanism
Binds to 50S subunit & blocks translocation by interference with tRNA release following peptide bond formation (inhibiting the peptide exit tunnel)
Very long half life (68 hours), very high tissue distribution
120
Azithromycin (Z-Pak PO, IV))
| Uses
Effective for intracellular pathogens (mycoplasma, chlamydia, legionella). H. influenzae; ; S. pneumoniae (high level of resistance)
121
Azithromycin (Z-Pak PO, IV))
| Side effects
GI distress with oral administration, less so than with erythromycin
Potential for polymorphic ventricular tachycardia (TdP)
122
Linezolid & Tedizolid (both IV, PO)
| Drug class
Protein synthesis inhibitor
123
Linezolid & Tedizolid (both IV, PO)
| Mechanism
Binds to 50S ribosome and inhibits peptidyl transferase
124
Linezolid & Tedizolid (both IV, PO)
| Uses
Gram+ organisms; MRSA, MSSA, Enterococcus including VRE
125
Linezolid & Tedizolid (both IV, PO)
| Side effects
Bone marrow suppression; most often thrombocytopenia after 2 weeks
Lactic acidosis, optic neuritis, peripheral neuropathy (with long-term use)
Irreversibly inhibits MOA which poses a risk for serotonin syndrome with serotonergic drugs
No reports yet for tedizolid, but just released onto market
126
Trimethoprim
| Drug class
Antimetabolite (DHFR Inhibitor)
127
Trimethoprim
| Mechanism
Prevent folic acid from being reduced (active); DHF --> THF
128
Trimethoprim
| Uses
Uncomplicated UTIs; Pneumocystis pneumonia & Toxoplasmosis infections in immunocompromised patients
129
Trimethoprim
| Side effects
Hyperkalemia in patients with severe renal insufficiency
| At very high concentrations will inhibit mammalian DHFR; usually given as combo with sulfamethoxazole (Bactrim)
130
Sulfamethoxazole
| Drug class
Antimetabolite (Dihydropterate synthase inhibitor)
131
Sulfamethoxazole
| Mechanism
Prevent pteridine + PABA --> dihydropteric acid
132
Sulfamethoxazole
| Uses
Uncomplicated UTIs; Pneumocystis pneumonia & Toxoplasmosis infections in immunocompromised patients
Usually given as combo with trimethoprim (Bactrim)
133
Sulfamethoxazole
| Side effects
Allergies
