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Pharmacology > Unit 6-Antibiotics > Flashcards

Unit 6-Antibiotics Flashcards

1
Q 
Penicillin G (IV); penicillin V (PO)
Drug class
A

Penicillins (Cell wall synthesis inhibitor)

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2
Q 
Penicillin G (IV); penicillin V (PO)
Mechanism
A

Form a complex with a PBP, prevent extracellular transpeptidase activity

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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.

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4
Q 
Penicillin G (IV); penicillin V (PO)
Side effects
A

Hypersensitivity reactions

Seizures at high doses in patients w/ renal dysfunction.

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5
Q

oxacillin (IV); nafcillin (IV); dicloxacillin (PO)

Drug class

A

Penicillinase-resistant penicillin

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6
Q

oxacillin (IV); nafcillin (IV); dicloxacillin (PO)

Mechanism

A

Bulky side chain shields β-lactam ring from penicillinase

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7
Q

oxacillin (IV); nafcillin (IV); dicloxacillin (PO)

Uses

A

Methicillin-sensitive S. aureus (MSSA)

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8
Q

oxacillin (IV); nafcillin (IV); dicloxacillin (PO)

Side effects

A

Hypersensitivity reactions

Hepatotoxicity & neutropenia w/ oxacillin; neutropenia & thrombophlebitis w/ nafcillin

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9
Q

Ampicillin (IV, PO); amoxicillin (PO)

Drug class

A

Aminopenicillin

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10
Q

Ampicillin (IV, PO); amoxicillin (PO)

Mechanism

A

Semi-synthetic penicillins with special side group allows improved penetration into Gram - membrane

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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”

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12
Q

Ampicillin (IV, PO); amoxicillin (PO)

Side effects

A

Hypersensitivity reactions

Delayed hypersensitivity reaction common if given during viral infection

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13
Q

Piperacillin (IV); Ticarcillin

Drug class

A

Extended spectrum penicillin

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14
Q

Piperacillin (IV); Ticarcillin

Mechanism

A

More manipulations to extend aminopenicillin spectrum

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15
Q

Piperacillin (IV); Ticarcillin

Uses

A

Activity of aminopenicillins plus Proteus; Klebsiella, Serratia, Enterobacter, Pseudomonas

Rarely used without tazobactam

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16
Q

Piperacillin (IV); Ticarcillin

Side effects

A

Hypersensitivity reactions

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17
Q 
Zosyn IV (piperacillin + tazobactam); Augmentin PO (amoxicillin + clavulanate)
Drug class
A

Combination therapy penicillins

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18
Q 
Zosyn IV (piperacillin + tazobactam); Augmentin PO (amoxicillin + clavulanate)
Mechanism
A

Suicide inhibitors that allow penicillins to do their job

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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

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20
Q 
Zosyn IV (piperacillin + tazobactam); Augmentin PO (amoxicillin + clavulanate)
Side effects
A

Hypersensitivity reactions;
Augmentin: diarrhea

Immune-mediated thrombocytopenia

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21
Q

Cefazolin (IV); cephalexin (oral)

Drug class

A

1st generation cephalosporin (Cell wall synthesis inhibitor)

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22
Q

Cefazolin (IV); cephalexin (oral)

Mechanism

A

Form a complex with a PBP, prevent extracellular transpeptidase activity; broader spectrum than penicillins

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23
Q

Cefazolin (IV); cephalexin (oral)

Uses

A

S. aureus; strep (NO Enterococcus); E. coli, Proteus, Klebsiella; mouth anaerobes

Cefazolin-DOC for surgical prophylaxis

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24
Q

Cefazolin (IV); cephalexin (oral)

Side effects

A

Hypersensitivity reactions

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25
Q

Cefuroxime

Drug class

A

2nd generation cephalosporin

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26
Q

Cefuroxime

Mechanism

A

As 1st generation cephalosporins

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27
Q

Cefuroxime

Uses

A

Less. S. aureus coverage; 1st generation plus Haemophilus (including penicillinase strains); above and below diaphragm anaerobes

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28
Q

Cefuroxime

Side effects

A

Hypersensitivity reactions

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29
Q

Cefoxitin; cefotetan

Drug class

A

2nd generation cephalosporin

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30
Q

Cefoxitin; cefotetan

Mechanism

A

As 1st generation cephalosporins

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31
Q

Cefoxitin; cefotetan

Uses

A

More active against E. coli & Klebsiella than 1st generation; B. fragilis

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32
Q

Cefoxitin; cefotetan

Side effects

A

Hypersensitivity reactions

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33
Q

Ceftazadime (IV); cefpodoxime (PO); ceftriaxone (IV)

Drug class

A

3rd generation cephalosporin

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34
Q

Ceftazadime (IV); cefpodoxime (PO); ceftriaxone (IV)

Mechanism

A

As 1st generation cephalosporins

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35
Q

Ceftazadime (IV); cefpodoxime (PO); ceftriaxone (IV)

Uses

A

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

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36
Q

Ceftazadime (IV); cefpodoxime (PO); ceftriaxone (IV)

Side effects

A

Higher association with C. difficile diarrhea than other classes
Ceftriaxone-biliary sludging, precipitation with calcium containing solutions in neonates

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37
Q

Cefepime (IV)

Drug class

A

4th generation cephalosporin

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38
Q

Cefepime (IV)

Mechanism

A

As 1st generation cephalosporins

crosses BBB

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39
Q

Cefepime (IV)

Uses

A

3rd generation, plus Staphylococcus coverage

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40
Q

Cefepime (IV)

Side effects

A

Mostly allergenic

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41
Q

Ceftaroline (IV)

Drug class

A

5th generation cephalosporin

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42
Q

Ceftaroline (IV)

Mechanism

A

Possesses a side chain that acts as a “Trojan horse” allowing access to PBP2a

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43
Q

Ceftaroline (IV)

Uses

A

Gram positive-MRSA, MSSA, Streptococci, E. faecalis not faecium Gram negative activity similar to ceftriaxone

Only cephalosporin with activity against MRSA!

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44
Q

Ceftaroline (IV)

Side effects

A

Mostly allergenic

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45
Q

Ceftazidime/Avibactam (IV)

Drug class

A

Extended-spectrum cephalosporin/b-lactamase inhibitor combinatioon

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46
Q

Ceftazidime/Avibactam (IV)

Mechanism

A

As 1st generation cephalosporins. B-lactamase inhibitor increases gram(-) spectrum.

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47
Q

Ceftazidime/Avibactam (IV)

Uses

A

Increased Psuedomonas, CRE, ESBL activity

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48
Q

Ceftazidime/Avibactam (IV)

Side effects

A

Higher association with C. difficile diarrhea than other classes

Mostly allergenic

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49
Q

Ceftolozane/Tazobactam (IV)

Uses

A

Increased activity against Psuedomonas, ESBLs. Not active against CREs.

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50
Q

Imipenem - cilastatin; Meropenem; Ertapenem; Doripenem (all IV)
Drug class

A

Carbapenam (Cell wall synthesis inhibitor)

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51
Q

Imipenem - cilastatin; Meropenem; Ertapenem; Doripenem (all IV)
Mechanism

A

Similar to pencillins

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52
Q

Imipenem - cilastatin; Meropenem; Ertapenem; Doripenem (all IV)
Uses

A 
Broad spectrum (excludes MRSA)
Ertapenem: not effective against Pseudomonas, Acinetobacter 
Used for highly-resistant organisms
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53
Q

Imipenem - cilastatin; Meropenem; Ertapenem; Doripenem (all IV)
Side effects

A

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%)

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54
Q

Aztreonam (IV)

Drug class

A

Monobactam (Cell wall synthesis inhibitor)

55
Q

Aztreonam (IV)

Mechanism

A

Similar to pencillins

56
Q

Aztreonam (IV)

Uses

A

Gram- aerobic bacilli including Pseudomonas, no G+, no anaerobes

57
Q

Aztreonam (IV)

Side effects

A

Not usually used as monotherapy; no cross-allergenicity with penicillins

58
Q

Vancomycin (IV, PO)

Drug class

A

Cell wall synthesis inhibitor (Glycopeptide)

59
Q

Vancomycin (IV, PO)

Mechanism

A

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
Q

Vancomycin (IV, PO)

Uses

A

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
Q

Vancomycin (IV, PO)

Side effects

A

IgE hypersensitivity reactions (histamine mediated); “red man syndrome”); dose-dependent nephrotoxicity; immune-mediated thrombocytopenia

Dose-dependent ototoxicity and nephrotoxicity; immune-mediated thrombocytopenia

62
Q

Dalbavancin; Telavancin; Oritavancin

Drug class

A

Lipoglycopeptides (anaolgs of vancomycin)

63
Q

Dalbavancin; Telavancin; Oritavancin

Mechanism

A

Binds to same target as vancomycin and inhibits transglycosylation

64
Q

Dalbavancin; Telavancin; Oritavancin

Uses

A

Similar to vancomycin but active against VRE & more anaerobe coverage

65
Q

Dalbavancin; Telavancin; Oritavancin

Side effects

A

Metallic taste, nausea, HA, nephrotoxicity, teratogenic

Pregnancy test needed for women of childbearing potential.

66
Q

Daptomycin (IV)

Drug class

A

Cell wall toxin (cyclic lipopeptide)

67
Q

Daptomycin (IV)

Mechanism

A

Penetrates bacterial cell wall, forming a channel for subsequent leakage of intracellular ions

68
Q

Daptomycin (IV)

Uses

A

G+ cocci only; use for VRE, VRSA

69
Q

Daptomycin (IV)

Side effects

A

Myalgia and rarely rhabdomyolysis

Eosinophilic pneumonia

Resistance has occurred during therapy. Higher doses (8-10 mg/kg/d) recommended for severe infections

70
Q

Colistin (IV, INH)

Drug class

A

Cell wall toxin (polymixin)

71
Q

Colistin (IV, INH)

Mechanism

A

Penetrates bacterial cell wall, forming a channel for subsequent leakage of intracellular ions

72
Q

Colistin (IV, INH)

Uses

A

G- only; usually reserved for Pseudomonas species resistant to all other antibacterials

73
Q

Colistin (IV, INH)

Side effects

A

Nephrotoxicity, neurotoxicity

74
Q

Ciprofloxacin (IV, PO)

Drug class

A

1st generation fluoroquinolone / Nucleic acid synthesis inhibitor

75
Q

Ciprofloxacin (IV, PO)

Mechanism

A

Inhibits DNA gyrase at low concentrations

76
Q

Ciprofloxacin (IV, PO)

Uses

A

Enterobactericeae, including Pseudomonas;

Atypicals

77
Q

Ciprofloxacin (IV, PO)

Side effects

A

GI, AMS
QT prolongation, tendon rupture
Divalent cations chelate ORAL quinolones decreasing bioavailability

78
Q

Levofloxacin (IV, PO); Moxifloxacin (IV, PO)

Drug class

A

2nd generation fluoroquinolone / Nucleic acid synthesis inhibitor

79
Q

Levofloxacin (IV, PO); Moxifloxacin (IV, PO)

Mechanism

A

Inhibits DNA gyrase at low concentrations; inhibits topoisomerase IV at high concentrations

80
Q

Levofloxacin (IV, PO); Moxifloxacin (IV, PO)

Uses

A 
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
Q

Levofloxacin (IV, PO); Moxifloxacin (IV, PO)

Side effects

A

As with cipro; QT prolongation: moxi>levo>cipro

82
Q

Metronidazole (IV, PO)

Drug class

A

Nucleic acid synthesis inhibitors (Nitroimidazole)

83
Q

Metronidazole (IV, PO)

Mechanism

A

Reduced (only under anaerobic conditions, which generate lots of acid) to an active free radical, which damages bacterial and certain protozoal DNA

84
Q

Metronidazole (IV, PO)

Uses

A

Anaerobes excluding Actinomycetes and Peptostreptococcus (DoC for C. difficile); some protozoa; H. pylori

85
Q

Metronidazole (IV, PO)

Side effects

A

metallic taste,disulfiram-like reaction (because it blocks aldehyde dehydrogenase)

CNS toxicity-seizure, neuropathy with long-term/high dose therapy

86
Q

Rifampin (IV, PO)

Drug class

A

Nucleic acid synthesis inhibitor

87
Q

Rifampin (IV, PO)

Mechanism

A

Inhibits DNA-dependent RNA polymerase to halt RNA transcription)

88
Q

Rifampin (IV, PO)

Uses

A

Mycobacterium tuberculosis; Staph aureus

89
Q

Rifampin (IV, PO)

Side effects

A

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
Q

Isoniazid (INH)

Drug class

A

Antitubercular

91
Q

Isoniazid (INH)

Mechanism

A

Inhibition of mycolic acid synthesis

92
Q

Isoniazid (INH)

Uses

A

Mycobacterium

93
Q

Isoniazid (INH)

Side effects

A

Hepatitis; neurotoxicity:memory loss, psychosis (pyridoxine can alleviate); hypersensitivity reactions

Phenytoin toxicity potentiated by INH.

94
Q

Pyrazinamide

Drug class

A

Antitubercular

95
Q

Pyrazinamide

Mechanism

A

Unknown

96
Q

Pyrazinamide

Uses

A

Mycobacterium

97
Q

Pyrazinamide

Side effects

A

N&V; hepatotoxicity; hypersensitivity reactions

98
Q

Ethambutol

Drug class

A

Antitubercular

99
Q

Ethambutol

Mechanism

A

Inhibits arabinosyl transferase enzymes involved in cell wall synthesis

100
Q

Ethambutol

Uses

A

Mycobacterium

101
Q

Ethambutol

Side effects

A

Neuropathy; optic neuritis

102
Q

Gentamicin; tobramycin

Drug class

A

Aminoglycoside / Protein synthesis inhibitor

103
Q

Gentamicin; tobramycin

Mechanism

A

Inhibits 30S ribosome: forms a tight complex with ribosomal protein, causing codon-anticodon misreading and production of inactive proteins (bactericidal); also, inhibits initiation

104
Q

Gentamicin; tobramycin

Uses

A

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
Q

Gentamicin; tobramycin

Side effects

A

Dose-dependent oto/nephrotoxicity (not observed if used less than 48 hours)

106
Q

Doxycycline; Minocycline (both IV, PO)

Drug class

A

Tetracycline / Protein synthesis inhibitor

107
Q

Doxycycline; Minocycline (both IV, PO)

Mechanism

A

Inhibits 30S ribosome: blocks access of tRNA anticodon to its codon

108
Q

Doxycycline; Minocycline (both IV, PO)

Uses

A

utility for Gram+ (S. pneumoniae, MRSA); very effective against intracellular pathogens (mycoplasma, chlamydia, legionella, rickettsia)

109
Q

Doxycycline; Minocycline (both IV, PO)

Side effects

A

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
Q

Tigecycline (IV)

Drug class

A

Glycylcyline

111
Q

Tigecycline (IV)

Mechanism

A

Inhibits 30S ribosome: glycyl group prevents efflux out of cell

112
Q

Tigecycline (IV)

Uses

A

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
Q

Tigecycline (IV)

Side effects

A

Much higher tissue concentrations than serum. Not effective in bacteremia
Higher all-cause mortality than other drugs

114
Q

Clindamycin (IV, PO)

Drug class

A

Protein synthesis inhibitors

115
Q

Clindamycin (IV, PO)

Mechanism

A

Binds to 50S subunit at “A site,” blocking peptide bond formation

116
Q

Clindamycin (IV, PO)

Uses

A

CA-MRSA/MSSA, Strep (resistance in Group B strep and S. aureus increasing
Mouth anaerobes
NO gram negative

117
Q

Clindamycin (IV, PO)

Side effects

A

Antibiotic-associated diarrhea; C. difficile colitis

118
Q

Azithromycin (Z-Pak PO, IV))

Drug class

A

Macrolide /Protein synthesis inhibitors

119
Q

Azithromycin (Z-Pak PO, IV))

Mechanism

A

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
Q

Azithromycin (Z-Pak PO, IV))

Uses

A

Effective for intracellular pathogens (mycoplasma, chlamydia, legionella). H. influenzae; ; S. pneumoniae (high level of resistance)

121
Q

Azithromycin (Z-Pak PO, IV))

Side effects

A

GI distress with oral administration, less so than with erythromycin
Potential for polymorphic ventricular tachycardia (TdP)

122
Q

Linezolid & Tedizolid (both IV, PO)

Drug class

A

Protein synthesis inhibitor

123
Q

Linezolid & Tedizolid (both IV, PO)

Mechanism

A

Binds to 50S ribosome and inhibits peptidyl transferase

124
Q

Linezolid & Tedizolid (both IV, PO)

Uses

A

Gram+ organisms; MRSA, MSSA, Enterococcus including VRE

125
Q

Linezolid & Tedizolid (both IV, PO)

Side effects

A

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
Q

Trimethoprim

Drug class

A

Antimetabolite (DHFR Inhibitor)

127
Q

Trimethoprim

Mechanism

A

Prevent folic acid from being reduced (active); DHF –> THF

128
Q

Trimethoprim

Uses

A

Uncomplicated UTIs; Pneumocystis pneumonia & Toxoplasmosis infections in immunocompromised patients

129
Q

Trimethoprim

Side effects

A

Hyperkalemia in patients with severe renal insufficiency

At very high concentrations will inhibit mammalian DHFR; usually given as combo with sulfamethoxazole (Bactrim)

130
Q

Sulfamethoxazole

Drug class

A

Antimetabolite (Dihydropterate synthase inhibitor)

131
Q

Sulfamethoxazole

Mechanism

A

Prevent pteridine + PABA –> dihydropteric acid

132
Q

Sulfamethoxazole

Uses

A

Uncomplicated UTIs; Pneumocystis pneumonia & Toxoplasmosis infections in immunocompromised patients
Usually given as combo with trimethoprim (Bactrim)

133
Q

Sulfamethoxazole

Side effects

A

Allergies

Pharmacology (26 decks)

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