Unit 6-Antibiotics Flashcards Preview

Pharmacology > Unit 6-Antibiotics > Flashcards

Flashcards in Unit 6-Antibiotics Deck (133):
1

Penicillin G (IV); penicillin V (PO)
Drug class

Penicillins (Cell wall synthesis inhibitor)

2

Penicillin G (IV); penicillin V (PO)
Mechanism

Form a complex with a PBP, prevent extracellular transpeptidase activity

3

Penicillin G (IV); penicillin V (PO)
Uses

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

Penicillin G (IV); penicillin V (PO)
Side effects

Hypersensitivity reactions
Seizures at high doses in patients w/ renal dysfunction.

5

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

Penicillinase-resistant penicillin

6

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

Bulky side chain shields β-lactam ring from penicillinase

7

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

Methicillin-sensitive S. aureus (MSSA)

8

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

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

9

Ampicillin (IV, PO); amoxicillin (PO)
Drug class

Aminopenicillin

10

Ampicillin (IV, PO); amoxicillin (PO)
Mechanism

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

11

Ampicillin (IV, PO); amoxicillin (PO)
Uses

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

Ampicillin (IV, PO); amoxicillin (PO)
Side effects

Hypersensitivity reactions
Delayed hypersensitivity reaction common if given during viral infection

13

Piperacillin (IV); Ticarcillin
Drug class

Extended spectrum penicillin

14

Piperacillin (IV); Ticarcillin
Mechanism

More manipulations to extend aminopenicillin spectrum

15

Piperacillin (IV); Ticarcillin
Uses

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

Rarely used without tazobactam

16

Piperacillin (IV); Ticarcillin
Side effects

Hypersensitivity reactions

17

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

Combination therapy penicillins

18

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

Suicide inhibitors that allow penicillins to do their job

19

Zosyn IV (piperacillin + tazobactam); Augmentin PO (amoxicillin + clavulanate)
Uses

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

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

Hypersensitivity reactions;
Augmentin: diarrhea

Immune-mediated thrombocytopenia

21

Cefazolin (IV); cephalexin (oral)
Drug class

1st generation cephalosporin (Cell wall synthesis inhibitor)

22

Cefazolin (IV); cephalexin (oral)
Mechanism

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

23

Cefazolin (IV); cephalexin (oral)
Uses

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

Cefazolin-DOC for surgical prophylaxis

24

Cefazolin (IV); cephalexin (oral)
Side effects

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