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PharmU6 > Antibiotics > Flashcards

Antibiotics Flashcards

1
Q

What is the mechanism of action of the B-Lactam abx?

A

Bind to penicillin-binding proteins–PBPs

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2
Q

What is a significant cause of resistance in gram-negative organisms?

A

B-lactamase

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3
Q

Name the natural penicillins

A

Penicillin G and V

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4
Q

What are the penicillinase-resistant penicillins or anti staphylococcal penicillins?

A

Oxacillin
Nafcillin
Dicloxacillin

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5
Q

What are the aminopenicillins?

A

Ampicillin

Amoxicillin

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6
Q

What are the anti-pseudomonad penicillins?

A

Ticarcillin

Piperacillin

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7
Q

What is the drug of choice for T. palladium (syphilis) infection?

A

Penicillin

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8
Q

What are the strep infections treated with penicillin?

A

S. pneumoniae
B-hemolytic streptococci
Viridian group strep

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9
Q

What Gram negative organism is treated with penicillin?

A

N. meningitidis

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10
Q

What abx are used for the tx of MSSA?

A

Anti-staphylococcal penicillins–Oxacillin, Nafcillin, Dicloxacillin

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11
Q

Why are Oxacillin, Nafcillin, Dicloxacillin great Abx to use against MSSA?

A

Bulky side chain streakily shields the B-lactam ring–Prevents degradation from penicillinase

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12
Q

Why do the anti-staphylococcal penicillins Oxacillin, Nafcillin, Dicloxacillin lack activity against gram negative bacteria ?

A

Bulky side chain precepts entry into gram-negative cell

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13
Q

What are the side effects of Oxacillin?

A

Hepatotoxicity and neutropenia

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14
Q

What are the side effects of Nafcillin?

A

Hepatotoxicity and neutropenia + thrombophlebitis

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15
Q

What is the major advantage to using Ampicillin and Amoxicillin?

A

Amino group increases hydrophilicity–improving penetration into gram-negative cell membrane

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16
Q

Ampicillin and amoxicillin are the drugs of choice for what?

A

Enterococcus

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17
Q

Amoxicillin clinical uses are?

A

Otitis media
Upper and lower-respiratory tract infections
Lyme disease

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18
Q

IV ampicillin is used for?

A

Listeria

DOC for Enterococcal infection

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19
Q

Which amino penicillin is better absorbed PO?

A

Amoxicillin

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20
Q

What is the primary use of Piperacillin and Ticarcillin?

A

Used in combination with a B-lactamase inhibitor to expand spectrum to include B-lactamase-producing organims

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21
Q

Name the extended spectrum penicillins/B-lactamase inhibitor combinations

A

Piperacillin/tazobactam–zosyn

Amoxicillin/clavulanate–Augmentin

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22
Q

What ate the two extended spectrum penicillins/B-lactamase inhibitor combinations that are active against Pseudomonas aeruginosa?

A

Pip/taz and tic/clav

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23
Q

Name the first generation cephalosporins…

A

Cefazolin
Cephalexin
Cephadroxil

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24
Q

What is the mechanism of action of the cephalosporins–Gen 1-4?

A

Form a complex with a PBP, prevent extracellular transpeptidase activity

These are broader spectrum than penicillins

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25
Q

What cephalosporin is DOC for surgical prophylaxis?

A

Cefazolin

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26
Q

What is the spectrum for the 1st gen cephalosporins?

A

MSSA and streptococci

Some enteric Gram negative rods
-Proteus mirabilis
-E. coli
-Klebsiella pneumonia
PEcK
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27
Q

Name the 2nd generation cephalosporins…

A

Cefuroxime
Cefoxitin
Cefotetan

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28
Q

What are the 2nd generation cephalosporins used for?

A

Gram-positive–staph and strep–> less active than 1st gens

Gram-negative–H. flu and N. gonorrheae

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29
Q

Name the 3rd generation cephalosporins…

A

Ceftazadime
Cefpodoxime
Ceftriaxone

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30
Q

What are the uses for the 3rd generation cephalosporins?

A

Extended activity against enterobacteriaceae

Strep

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31
Q

What is Ceftazidime active against?

A

Third gen–Pseudomonas

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32
Q

What are the 3rd generations cephalosporins associated with–in terms of dz?

A

C. difficile diarrhea

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33
Q

Why shouldn’t Ceftriaxone be used in neonates?

A

Biliary sludging and kernicterus–interaction with Ca++ containing solutions causing precipitation

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34
Q

What drug should be used in neonates instead of ceftriaxone?

A

Cefotaxime

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35
Q

Name the 4th generation cephalosporins?

A

Cefepime

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36
Q

What are the clinical uses of the 4th generation cephalosporins–cefepime?

A

Gram-negative–enterobacteriaceae and pseudomonas

Gram-positive–MSSA and S. pneumoniae

Geared toward nosocomial infections–pseudomonas

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37
Q

Why are the 4th gen cephalosporins used to tx meningitis?

A

Can cross BBB

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38
Q

Name the 5th generation cephalosporins?

A

Ceftaroline

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39
Q

What is unique about the 5th gen cephalosporins–Ceftaroline?

A

Possesses a side chain that mimics a portion of the cell wall structure and acts as a “Trojan horse” allowing access to the PBP2a

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40
Q

What are the uses of the 5th gen cephalosporins–Ceftaroline?

A

Gram-positive–S. aueus–MSSA and MRSA, E. faecalis, S. Pneumoniae

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41
Q

What is the major use of Ceftazidime/Avibactam?

A

Complicated UTI and intraabdominal infection

Increases Gram negative spectrum

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42
Q

Name the Carbapenems…

A

Imipenem-cilastatin
Meropenem
Ertapenem
Doripenem

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43
Q

What are the uses of the carbapenems?

A

Broad spectrum–Excludes MRSA

Used for highly-resistant organisms

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44
Q

What is the major rare side effect seen with carbapenems?

A

Seizures

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45
Q

What drug interaction is seen with carbapenems?

A

Decrease valproic acid concentrations

46
Q

What is Ertapenem used for?

A

Has a long t 1/2 making it ideal for outpatient polymicrobial infections

47
Q

Which carbapenem has the most activity against pseudomonas?

A

Doripenem

48
Q

Name the Monobactam…

A

Aztreonam

49
Q

What are the primary uses of aztreonam–monobactam?

A

Gram-negative–Enterobacteriaceae and Pseudomonas

Rarely used alone–alternative to penicillin to provide gram-negative in combination with another agent

50
Q

What is the mechanism of action of Vancomycin?

A

Inhibits late stages of cell wall synthesis

  • Binds to D-Ala-D-Ala terminus of the nascent peptidoglycan pentapeptide
  • Inhibits transglycosylase preventing elongation of peptidoglycan and cross-linking
51
Q

What are the uses of Vancomycin?

A

Gram-positive

  • Staph–MRSA
  • Strep
  • Enterococci
  • Bacillus spp and Corynebacterium spp

Anaerobes

  • Peptostreptococcus
  • Actinomyces
  • Propionibacterium
  • Clostridium–C. diff oral form

DOES NOT work for Gram negative

52
Q

What can occur with vancomycin infusion?

A

Redman syndrome–Secondary to histamine release

53
Q

What is the mechanism of action for Daptomycin a lipopeptide?

A

Insertion into the gram-positive cell membrane causing depolarization and ultimate cell death
–Penetrates bacterial cell wall–forming a channel for subsequent leakage of intracellular ions

54
Q

What is the mechanism of resistance for daptomycin?

A

Alteration of cell membrane–increased fluidity, increased net surface charge, reduced daptomycin surface binding

55
Q

What are the uses for daptomycin?

A

Gram-positive–Staph, strep, enterococci–VRE

NO GRAM-Negative activity

56
Q

Why isn’t daptomycin used for pneumonia?

A

Not effective fro pneumonia due to inactivation by pulmonary surfactant

57
Q

What are the side effects of daptomycin?

A

Myalgia and rarely rhabdomyolysis

Eosinophilic pneumonia

58
Q

Name the lipoglycopeptides…

A

Telavancin
Dalbavancin
Oritavancin

59
Q

What are the lipoglycopeptides telavancin, dalbavancin, and oritavancin?

A

Binds to same target as vancomycin and inhibits transglycosylation

They have similar coverage with compared to vanco BUT are active against VRE and have more anaerobe coverage

60
Q

What are the side effects of the lipoglycopeptides telavancin, dalbavancin, and oritavancin?

A 
Metallic taste
Nausea
HA
Nephrotoxicity
Teratogenic--Telavancin
61
Q

What drug is reserved for pseudomonas species resistant to all other antibacterials?

A

Colistin–penetrates bacterial cell wall, forcing a channel for subsequent leakage of intracellular ions

62
Q

All protein synthesis inhibitors are bacteriostatic EXCEPT?

A

Aminoglycosides

63
Q

What abx target the 30s ribosomal subunit?

A

Aminoglycosides–gentamicin, tobramycin, amikacin
Tetracyclines–doxycycline, minocycline
Glycylcyclines–tigecycline

64
Q

What abx target the 50s ribosomal subunit?

A

Macrolides–azithromycin, clarithromycin
Clinamycin
Oxazolidinones–linezolid, tedizolid

65
Q

Name the aminoglycosides…

A

Gentamicin
Tobramycin
Amikacin
Streptomycin

66
Q

What is the mechanism of aminoglycosides?

A

Bind to the 30s subunit of bacterial ribosomes and interfere with an initiation complex btw mRNA and the 30s subunit–inhibits protein synthesis

Bacteriacidal

67
Q

Why are aminoglycosides ineffective against anaerobes?

A

They have an oxygen dependent uptake mechanism

68
Q

What are the uses of the aminoglycosides?

A

Gram-negative
-Enterobacteriaceae and Pseudomonas

Gram-positive
-Synergy with cell wall active agent against enterococcus–CANNOT give as mono therapy

69
Q

What are the side effects of the aminoglycosides?

A

Nephrotoxicity
Ototoxicity
Neuromuscular blockage

70
Q

Name the tetracyclines

A

Doxycycline
Minocycline
Tetracycline

71
Q

What is the mechanism of action of the tetracyclines?

A

Passive diffusion through porins in gram-negative organism

-Bind 30s ribosomal subunit preventing protein synthesis

72
Q

What are the uses of the tetracyclines?

A 
Atypical organisms
-C. pneumoniae
-M. pneumoniae
Spirochetes
-Borrelia burgodorferi
-Leptospira
-T. pallidum
Rickettsiae
Gram-positive
-S. pneumoniae
-CA-MRSA
Gram-negative
-H. influenzae
-Neiserria spp
73
Q

Tetracyclines are the DOC for what?

A

Tick-borne illnesses

  • Lyme
  • Ehrlichiosis
  • Anaplasmosis
74
Q

What are the drug interactions that occur with tetracyclines?

A

Di, Tri-valent cations–oral forms only

  • Reduced tetracycline absorption
  • Avoid coadminstration with antacids, sucralfate, multivitamins, iron, etc
75
Q

What allows tigecycline to overcome two major resistances and what are these?

A

9-glycl substitution

Efflux pumps and Ribosomal protection

76
Q

What are the uses for tigecycline?

A

Broad-spectrum–includes MRSA, VRE and acinetobacter

77
Q

Tigecycline is one of the only drugs effective against what?

A

Carbapenem-resistant enterobacteriaceae–CRE

78
Q

What are the macrolides?

A

Azithromycin
Clarithromycin
Erythromycin

79
Q

What is the mechanism of action of the macrolides–Azithromycin, Clarithromycin, Erythromycin?

A

Reversible binding to 50s subunit–blocks translocation by inference with tRNA release following peptide bond formation

80
Q

What are the macrolides effective for?

A

Intracelular pathogens

  • Mycoplasma
  • Chlamydia
  • Legionella

H. influenzae
S. pneumoniae–high level of resistance

81
Q

What are the side effects seen with marcolides?

A

Thrombophlebitis

QT-prolongation–Torsades

82
Q

What is the mechanism of action of Clindamycin?

A

Binding to 50s ribosomal subunit preventing protein synthesis –at A site–blocking peptide bond formation

83
Q

What is clindamycin used for in combination therapy?

A

Plasmodium falciparum with quinine

Toxic-shock syndrome with penicillin

84
Q

What are the side effects of clindamycin?

A

Diarrhea and pseudomembranous colitis –C. diff

85
Q

What is the mechanism of action of linezolid and tedizolid–oxaxolidinones?

A

Binds to 23 S ribosomal RNA of the 50S subunit inhibiting protein synthesis

86
Q

What are the uses for linezolid and tedizolid?

A

Gram-positives

  • Staph–MRSA and MSSA
  • Enterococci–VRE
  • Strep
87
Q

What drugs are recommended fro 1st line therapy of S. aureus bacteremia?

A

Vancomycin and daptomycin

88
Q

What are the side effects of linezolid and tedizolid?

A

Bone marrow suppression–thrombocytopenia after 2 wks

Lactic acidosis
Optic neuritis
Peripheral neuropathy

Irreversibly inhibits MOA which poses a risk for serotonin syndrome with serotonergic drugs

89
Q

What are the Nucleic acid synthesis inhibitors?

A

Fluoroquinolones–Ciprofloxacin, Levofloxacin, Moxifloxacin
Metronidazole
Rifamycins–Rifampin, Rifabutin, Rifaximin

90
Q

Name the Fluoroquinolones…

A

Ciprofloxacin
Levofloxacin
Moxifloxacin

91
Q

What is the mechanism of action of the fluoroquinolones?

A

Inhibit DNA gyrase
Inhibit topoisomerase IV–Quinolones trap or stabilize the enzyme DNR complexes after strand breakage and before resealing of DNA

92
Q

What is Ciprofloxacin used for?

A

Enterobactericeae
Pseudomonas–PO
Atypicals

93
Q

What is Levofloxacin used for?

A

Pseudomonas-PO

94
Q

What is Moxifloxacin used for?

A

Anaerobes

95
Q

What are the major side effects of the fluoroquinolone?

A

Tendinitis–tendon rupture

QT prlongation–Moxifloxacin

96
Q

What are the drug interactions for the fluoroquinolones?

A

Di-, tri-valent cations

Ciprofloxacin–inhibits CYP 1A2

  • Increase theophylline levels–can lead to seizure
  • Increases tizanidine concentrations resulting in hypotension
97
Q

What is the mechanism of action of metronidazole?

A

Interacts with DNA to cause a loss of helical DNA structure and strand breakage resulting in inhibition of protein synthesis
–Reduced only under anaerobic conditions to an active free radical which damages bacterial and certain protozoal DNA

98
Q

What are the uses of metronidazole?

A

Anaerobes

  • B. fragilis
  • Clostridial species–including difficile

Protozoa

  • Trichomonas
  • Giardia
  • Entamoeba histolytica
99
Q

Name the Rifamycins…

A

Rifampin
Rifabutin
Rifaximin

100
Q

What is the mechanism of action of the Rifamycins?

A

Bind to DNA-dependent RNA polymerase inhibiting RNA synthesis

101
Q

What are the uses for Rifampin?

A

Mycobacterium tuberculosis

Staph aureus

102
Q

What are the side effects of Rifampin?

A

Flu-like symptoms–> fever, myalgia, interstitial nephritis
Thrombocytopenia, hemolysis
Transaminitis

103
Q

What is Rifampin an inducer of?

A

CYP 450 system–lower concentration of substrates

104
Q

What is the mechanism of action of Isoniazid?

A

Inhibition of synthetic pathways of mycolic acid

105
Q

What are the side effects of isoniazid?

A

Hepatitis

Neurotoxicity –peripheral neuropathy–pyridoxine can alleviate

106
Q

What is the mechanism of action of Ethambutol?

A

Inhibits arabinosyl transferase enzymes involved in biosynthesis of cell wall

107
Q

What are the 4 drugs used for TB tx?

A

Rifampin
Isoniazid
Pyrazinamide
Ethambutol

108
Q

What is the mechanism of action of Sulfamethoxazole?

A

Interferes with bacterial folic acid synthesis and growth via inhibition of dihydrofolic acid formation from paraaminobenzoic acid (PABA)

109
Q

What is the mechanism of action of Trimethoprim?

A

Inhibits dihydrofolic acid reduction to tetrahydrofolate resulting in sequential inhibition of enzymes of the folic acid pathway

110
Q

What are the uses for Sulfamethoxazole/Trimethoprim?

A

Uncomplicated UTIs
Pneumocystis
Pneumonia
Toxoplasmosis infections in immunocompromised pts

111
Q

Trimethoprim-Sulfamethoxazole is prophylaxis and tx for?

A

Pneumocystis jiroveccii pneumonia

112
Q

What is the major drug interaction that occurs with trimethoprim-sulfamethoxazole?

A

Warfarin–inhibition of CYP 2C9 leading to increase in INR

PharmU6 (7 decks)

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