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PHARMACOLOGY > Antibacterial Drugs > Flashcards

Antibacterial Drugs Flashcards

1
Q

Mechanism: Aminoglycosides

Gentamicin

Neomycin

Amikacin

Tobramycin

Streptomycin

A

Bactericidal (unlike other protein synthesis inhibitors)

Irreversible inhibition of initiation complex through binding of 30S ribosomal subunit

Also blocks translocation

Can cause misreading of mRNA

Requires O2 for uptake; ineffective against anaerobes

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2
Q

Resistance: Cephalosporins

A

Structural change in penicillin-binding proteins (transpeptidases)

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3
Q

Name the monobactam(s)

A

Aztreonam

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4
Q

Adverse effects: Cephalosporins

A
  1. Hypersensitivity reactions
  2. Autoimmune hemolytic anemia
  3. Disulfiram-like reaction
  4. Vitamin K deficiency
  5. Increased nephrotoxicity of aminoglycosides
  6. Low rate of cross-reactivity even in penicillin-allergic patients
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5
Q

Class: Streptomycin

A

Aminoglycoside

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6
Q

Do not take tetracyclines with ___, ___, or ___ because divalent cations inhibit the drugs absorption in the gut

A

Milk (calcium)

Antacids (calcium or magnesium)

Iron-containing preparations

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7
Q

Imipenem is a board-spectrum beta-lactamase resistant carbapenem that is always administered with ___ (inhibitor of renal dehydropeptidase I) to decrease inactivate of drug in renal tubules.

A

Cilastatin

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8
Q

Resistance: Macrolides

Azithromycin

Clarithromycin

Erythromycin

A

Methylation of 23S rRNA-binding site prevent binding of the drug

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9
Q

Clinical use: 3rd generation cephalosporins

Ceftriaxone

Cefotaxime

Cefpodoxime

Ceftazidime

A

Serious gram (-) infections resistant to other beta-lactams

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10
Q

Organisms typically not covered by 1st - 4th generation cephalosporins

A

Listeria

Atypicals (Chlamydia, Mycoplasma)

MRSA

Enterococci

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11
Q

Mechanism: Antipseudomonal penicillins

Piperacillin

Ticarcillin

A

Same as penicillin

Extended spectrum

Susceptible to penicillinase

Use with beta-lactamase inhibitors

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12
Q

Adverse effects: Aminoglycosides

Gentamicin

Neomycin

Amikacin

Tobramycin

Streptomycin

A
  1. Nephrotoxicity (especially with cephalosporins)
  2. Ototoxicity (especially with loop diuretics)
  3. Teratogen (cause ototoxocity)
  4. Neuromuscular blockade
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13
Q

Name the antipseudomonal penicillins

A
  1. Piperacillin
  2. Ticarcillin
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14
Q

Resistance: Aminoglycosides

Gentamicin

Neomycin

Amikacin

Tobramycin

Streptomycin

A

Bacterial transferase enzymes inactivate the drug by:

  • Acetylation
  • Phosphorylation
  • Adenylation
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15
Q

Class: Gentamicin

A

Aminoglycoside

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16
Q

Adverse effects: Penicillin G, V

A
  1. Hypersentivity reactions
  2. Direct Coombs + hemolytic anemia
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17
Q

Mechanism: Sulfonamides

Sulfamethoxazole (SMX)

Sulfisoxazole

Sulfadiazine

A

Inhibit dihydropteroate synthase → inhibiting folate synthesis

Bacteriostatic (cidal when combined with trimethoprim)

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18
Q

Name the carbapendems

A

Older:

  • Imipenem
  • Meropenem

Newer:

  • Ertapenem (limited Pseudomonas coverage)
  • Doripenem
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19
Q

Mechanism: Fluoroquinolones

Enoxacin

Ciprofloxacin

Norfloxacin

Levofloxacin

Ofloxacin

Moxifloxacin

Gemifloaxacin

A

Inhibits prokaryotic topoisomerase II (DNA gyrase) and topoisomerase IV

Bactericidal

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20
Q

Class: Amikacin

A

Aminoglycoside

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21
Q

Adverse effects: Penicillinase-sensitive penicillins (aminopenicillins)

Amoxicillin

Ampicillin

A
  1. Hypersensitivity reactions
  2. Rash
  3. Pseudomembranous colitis
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22
Q

Mechanism: Chloramphenicol

A

Blocks peptidyltransferase at 50S subunit

Bacteriostatic

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23
Q

Mechanism: Tetracyclines

Tetracycline

Doxycycline

Minocycline

A

Bacteriostatic

Bind 30S and prevent attachment of aminoacyl-tRNA

Limited CNS penetration

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24
Q

Mechanism: Cephalosporins

A

Beta-lactam antibiotics that inhibit cell wall synthesis but are less susceptible to penicillinases

Bactericidal

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25
Q

Adverse effects: Monobactam

Aztreonam

A

Usually non-toxic

  1. Occasional GI upset
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26
Q

Adverse effects: Macrolides

Azithromycin

Clarithromycin

Erythromycin

A
  1. GI motility issues
  2. Arrhythmia (prolonged QT interval)
  3. Acute cholestatic hepatitis
  4. Rash
  5. Eosinophilia
  6. P-450 inhibitor (except azithromycin)
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27
Q

Adverse effects: Linezolid

A
  1. Bone marrow suppression
    • Especially thrombocytopenia
  2. Peripheral neuropathy
  3. Serotonin syndrome (when mixed with other serotonergic agents)
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28
Q

Resistance: Penicillin G, V

A

Penicillinase in bacteria (a type of beta-lactamase) cleaves beta-lactam ring

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29
Q

Clinical use: 5th generation cephalosporins

Ceftaroline

A

Broad gram (+) and gram (-) organism coverage

Unlike 1st - 4th generation, covers:

  • Listeria
  • MRSA
  • Enterococcus faecalis

Does NOT cover pseudomonas (vs 4th generation)

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30
Q

Adverse effects: Metronidazole

A
  1. Disulfiram-like reaction (severe flushing, tachycardia, hypotension) with alcohol
  2. Headache
  3. Metallic taste
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31
Q

Resistance: Sulfonamides

Sulfamethoxazole (SMX)

Sulfisoxazole

Sulfadiazine

A

Altered enzyme (bacterial dihydropteroate synthase)

Decreased uptake

Increased PABA synthesis

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32
Q

In general:

___ treats anaerobic infections above the diaphragm

___ treats anaerobic infections below the diagphram

A

Clindamycin (above)

Metronidazole (below)

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33
Q

Adverse effects: Carbapenems

Imipenem

Meropenem

Ertapenem

Doripenem

A
  1. GI distress
  2. Skin rash
  3. CNS toxicity (seizures)
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34
Q

Mechanism: Tigecycline

A

Glycylcycline - tetracycline derivative

Binds 30S → inhibiting protein synthesis

Bacteriostatic

35
Q

Clinical use: 4th generation cephalosporins

Cefepime

A

Gram (-) organisms

Increased activity against:

  • Pseudomonas
  • Gram (+) organisms
36
Q

50S inhibitors

A

Chloramphenicol (static)

Clindamycin (static)

Macrolides (static)

Linezolid (variable

37
Q

Adverse effects: Daptomycin

A
  1. Myopathy
  2. Rhabdomyolysis
38
Q

Adverse effects: Sulfonamides

Sulfamethoxazole (SMX)

Sulfisoxazole

Sulfadiazine

A
  1. Hypersensitivity reactions
  2. Hemolysis if G6PD deficient
  3. Nephrotoxicity (tubulointerstitial nephritis)
  4. Photosensitivity
  5. Stevens-Johnson syndrome
  6. Kernicterus in infants
  7. Displace other drugs from albumin (e.g., warfarin)
  8. P-450 inhibitor
39
Q

Mechanism: Penicillinase-resistant penicillins

Dicloxacillin

Nafcillin

Oxacillin

Methacillin (D/C)

A

Same as penicillin

Narrow spectrum

Penicillinase-resistant because bulky R-group blocks access of beta-lactamase to beta-lactam ring

40
Q

Use of ___ is limited owing to its toxicities, but is still often used in developing countries due to low cost.

A

Chloramphenicol

41
Q

Name the penicillinase-resistant penicillins

A
  1. Dicloxacillin
  2. Nafcillin
  3. Oxacillin
  4. Methicillin (D/C)
42
Q

Mechanism: Daptomycin

A

Lipopeptide that disrupts cell membranes of gram-positive cocci by creating transmembrane channels

43
Q

Resistance: Penicillinase-sensitive penicillins (aminopenicillins)

Amoxicillin

Ampicillin

A

Penicillinase in bacteria (a type of beta-lactamase) cleaves beta-lactam ring

44
Q

Adverse effects: Dapsone

A

Hemolysis if G6PD deficient

45
Q

Resistance: Linezolid

A

Point mutation of ribosomal RNA

46
Q

Mechanism: Trimethoprim

A

Inhibits bacterial dihydrofolate reductase

Bacteriostatic

47
Q

___ is a carbapenem that is stable to renal dehydropeptidase I (no need for cilastatin) and has less risk for seizures

48
Q

Adverse effects: Chloramphenicol

A
  1. Anemia (dose dependent)
  2. Aplastic anemia (dose independent)
  3. Gray baby syndrome (premature infants because they lack liver UDP-glycuronyltransferase, which metabolizes the drug)
49
Q

Adverse effects: Tetracyclines

Tetracycline

Doxycycline

Minocycline

A
  1. GI distress
  2. Discoloration of teeth
  3. Inhibition of bone growth (children)
  4. Photosensitivity
  5. Contraindicated in pregnancy
50
Q

Clinical use: 1st generation cephalosporins

Cefazolin

Cephalexin

A
  1. Gram (+) cocci
  2. Proteus mirabilis
  3. E. coli
  4. Klebsiella pneumoniae
  5. Cefazolin used prior to surgery to prevent S. aureus wound infections
51
Q

Name the penicillinase-sensitive penicillins (aminopenicillins)

A
  1. Amoxicillin
  2. Ampicillin
52
Q

Fluoroquinolones must NOT be taken with ___

53
Q

Mechanism: Carbapenems

A

Inhibit peptidoglycan (cell wall) synthesis

54
Q

30S inhibitors

A

Aminoglycosides (cidal)

Tetracyclines (static)

Tigecycline (tetracycline derivative)

55
Q

Class: Neomycin

A

Aminoglycoside

56
Q

Fluoroquinolones are contraindicated in ___, ___, and ___ due to possible damage to cartilage

A

Pregnancy women

Nursing mothers

Children <18 year old

57
Q

Adverse effects: Tigecycline

58
Q

Name the tetracyclines

A

Tetracycline

Doxycycline

Minocycline

59
Q

Mechanism: Penicillinase-sensitive penicillins (aminopenicillins)

Amoxicillin

Ampicillin

A

Same as penicillin

Wider spectrum

Penicillinase sensitive

Can combine with clavulanic acid to protect against destruction by beta-lactamase

60
Q

Mechanism: Macrolides

Azithromycin

Clarithromycin

Erythromycin

A

Inhibit protein synthesis by blocking translocation

Bind to 23S rRNA of the 50S subunit

61
Q

Mechanism: Monobactam

Aztreonam

A

Inhibits cell wall synthesis

Prevent PTG cross-linking by binding to penicillin-binding protein 3

Less susceptible to beta-lactamases

Synergistic with aminoglycosides

No cross-allergenicity with penicillins

62
Q

___ is used prior to surgery to prevent S. aureus wound infections

A

Cefazolin (1st gen cephalosporin)

63
Q

Adverse effects: Fluoroquinolones

Enoxacin

Ciprofloxacin

Norfloxacin

Levofloxacin

Ofloxacin

Moxifloxacin

Gemifloxacin

A
  1. GI upset
  2. Superinfections
  3. Skin rashes
  4. Headache
  5. Dizziness
  6. Leg cramps, myalgias (less common)
  7. P-450 inhibitor
  8. Prolonged QT interval
  9. Tendonitis or tendon rupture
    • In patients >60 years old
    • In patients taking prednisone
64
Q

Mechanism: Penicillin G, V

A

D-Ala-D-Ala structural analog

Bind penicillin-binding proteins (transpeptidases) → block transpeptidase cross-linking of peptidoglycan in cell wall

Activates autolytic enzymes

Penicillinase sensitive

65
Q

Adverse effects: Vancomycin

A
  1. Nephrotoxicity
  2. Ototoxicity
  3. Thrombophlebitis
  4. Diffuse flushing (red man syndrome)
    • Largely preventable by pretreatment with antihistamines and slow infusion rate
66
Q

Mechanism: Metronidazole

A

Forms toxic free radical metabolites in the bacterial cell that damage DNA

Bactericidal and antiprotozoal

67
Q

Resistance: Chloramphenicol

A

Plasmid-encoded acetyltransferase inactivates the drug

68
Q

Adverse effects: Penicillinase-resistant penicillins

Dicloxacillin

Nafcillin

Oxacillin

Methicillin (D/C)

A
  1. Hypersensitivity reactions
  2. Interstitial nephritis
69
Q

Mechanism: Linezolid

A

Inhibits protein synthesis by binding to 50S subunit and preventing formation of the initiation complex

70
Q

Mechanism: Vancomycin

A

Inhibits cell wall PTG formation by binding
D-ala-D-ala portion of cell wall precursors

Bactericidal against most bacteria (bacteriostatic against C. difficile)

Not susceptible for beta-lactamase

71
Q

Resistance: Vancomycin

A

Occurs in bacteria (Enterococcus) via amino acid modification of D-ala-D-ala → D-ala-D-lac

72
Q

Adverse effects: Clindamycin

A
  1. Pseudomembranous colitis (C. difficile)
  2. Fever
  3. Diarrhea
73
Q

Adverse effects: Trimethoprim

A
  1. Megaloblastic anemia
  2. Leukopenia
  3. Granylocytopenia

Adverse effects may be alleviated with supplemental folinic acid

74
Q

Name the beta-lactamase inhibitors

A
  1. Clavulanic acid
  2. Avibactam
  3. Sulbactam
  4. Tazobactam
75
Q

Adverse effects: Antipseudonomal penicillins

Peperacillin

Ticarcillin

A
  1. Hypersensitivity reactions
76
Q

Most protein synthesis inhibitors are ___ with the exception of ___

A

Bacteriostatic

Exception: Aminoglycosides

77
Q

Resistance: Tetracyclines

Tetracycline

Doxycycline

Minocycline

A

Decrease uptake and increase efflux out of bacterial cells by plasmic-encoded transport pumps

78
Q

Daptomycin is NOT used for ___

A

Pneumonia - daptomycin avidly binds to and is inactivated by surfactant

79
Q

Mechanism: Clindamycin

A

Blocks peptide transfer (translocation) at 50S subunit

Bacteriostatic

80
Q

Class: Tobramycin

A

Aminoglycoside

81
Q

___ is an aminoglycoside used for bowel surgery

82
Q

Clinical use: 2nd generation cephalosporins

Cefaclor

Cefoxitin

Cefuroxime

A
  1. Gram (+) cocci
  2. Proteus mirabilis
  3. E. coli
  4. Klebsiella pneumoniae
  5. H. influenzae
  6. Enterobacter aerogenes
  7. Neisseria spp.
  8. Serratia marcescens
83
Q

Mechanism: Dapsone

A

Similar to sulfonamides (inhibits dihydropteroate synthase) , but structurally distinct

PHARMACOLOGY (33 decks)

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