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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
Adverse effects: Monobactam Aztreonam
Usually non-toxic 1. Occasional GI upset
26
Adverse effects: **Macrolides** Azithromycin Clarithromycin Erythromycin
1. GI motility issues 2. Arrhythmia (prolonged QT interval) 3. Acute cholestatic hepatitis 4. Rash 5. Eosinophilia 6. P-450 inhibitor **(except azithromycin)**
27
Adverse effects: Linezolid
1. Bone marrow suppression * Especially **thrombocytopenia** 2. **Peripheral neuropathy** 3. **Serotonin syndrome** (when mixed with other serotonergic agents)
28
Resistance: Penicillin G, V
**Penicillinase** in bacteria (a type of beta-lactamase) cleaves beta-lactam ring
29
Clinical use: 5th generation cephalosporins Ceftaroline
Broad gram (+) and gram (-) organism coverage **Unlike 1st - 4th generation, covers:** * Listeria * MRSA * Enterococcus faecalis Does **NOT** cover pseudomonas (vs 4th generation)
30
Adverse effects: Metronidazole
1. Disulfiram-like reaction (severe flushing, tachycardia, hypotension) with alcohol 2. Headache 3. Metallic taste
31
Resistance: **Sulfonamides** Sulfamethoxazole (SMX) Sulfisoxazole Sulfadiazine
Altered enzyme (bacterial dihydropteroate synthase) Decreased uptake Increased PABA synthesis
32
In general: \_\_\_ treats anaerobic infections **above** the diaphragm \_\_\_ treats anaerobic infections **below** the diagphram
**Clindamycin** (above) **Metronidazole** (below)
33
Adverse effects: Carbapenems Imipenem Meropenem Ertapenem Doripenem
1. GI distress 2. Skin rash 3. CNS toxicity (seizures)
34
Mechanism: Tigecycline
Glycylcycline - tetracycline derivative Binds **30S** → inhibiting protein synthesis Bacterio**static**
35
Clinical use: 4th generation cephalosporins Cefepime
**Gram (-) organisms** **Increased activity against:** * Pseudomonas * Gram (+) organisms
36
50S inhibitors
Chloramphenicol (static) Clindamycin (static) Macrolides (static) Linezolid (variable
37
Adverse effects: Daptomycin
1. Myopathy 2. Rhabdomyolysis
38
Adverse effects: **Sulfonamides** Sulfamethoxazole (SMX) Sulfisoxazole Sulfadiazine
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
Mechanism: Penicillinase-resistant penicillins Dicloxacillin Nafcillin Oxacillin Methacillin (D/C)
Same as penicillin Narrow spectrum Penicillinase-resistant because **bulky R-group** blocks access of beta-lactamase to beta-lactam ring
40
Use of ___ is limited owing to its toxicities, but is still often used in developing countries due to low cost.
Chloramphenicol
41
Name the penicillinase-resistant penicillins
1. Dicloxacillin 2. Nafcillin 3. Oxacillin 4. Methicillin (D/C)
42
Mechanism: Daptomycin
**Lipopeptide** that disrupts cell membranes of gram-positive cocci by creating **transmembrane channels**
43
Resistance: Penicillinase-sensitive penicillins (aminopenicillins) Amoxicillin Ampicillin
**Penicillinase** in bacteria (a type of beta-lactamase) cleaves beta-lactam ring
44
Adverse effects: Dapsone
Hemolysis if G6PD deficient
45
Resistance: Linezolid
Point mutation of ribosomal RNA
46
Mechanism: Trimethoprim
Inhibits bacterial dihydrofolate reductase Bacterio**static**
47
\_\_\_ is a **carbapenem** that is stable to renal **dehydropeptidase I** (no need for cilastatin) and has less risk for seizures
Meropenem
48
Adverse effects: Chloramphenicol
1. **Anemia** (dose dependent) 2. **Aplastic anemia** (dose **in**dependent) 3. **Gray baby syndrome** (premature infants because they lack liver UDP-glycuronyltransferase, which metabolizes the drug)
49
Adverse effects: **Tetracyclines** Tetracycline Doxycycline Minocycline
1. GI distress 2. Discoloration of teeth 3. Inhibition of bone growth (children) 4. Photosensitivity 5. **Contraindicated in pregnancy**
50
Clinical use: 1st generation cephalosporins Cefazolin Cephalexin
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
Name the penicillinase-sensitive penicillins (aminopenicillins)
1. Amoxicillin 2. Ampicillin
52
Fluoroquinolones must **NOT** be taken with \_\_\_
Antacids
53
Mechanism: Carbapenems
Inhibit peptidoglycan (cell wall) synthesis
54
30S inhibitors
Aminoglycosides (cidal) Tetracyclines (static) Tigecycline (tetracycline derivative)
55
Class: Neomycin
Aminoglycoside
56
**Fluoroquinolones** are contraindicated in \_\_\_, \_\_\_, and ___ due to possible **damage to cartilage**
Pregnancy women Nursing mothers Children \<18 year old
57
Adverse effects: Tigecycline
1. N/V
58
Name the tetracyclines
Tetracycline Doxycycline Minocycline
59
Mechanism: Penicillinase-sensitive penicillins (aminopenicillins) Amoxicillin Ampicillin
Same as penicillin **Wider spectrum** Penicillinase sensitive Can combine with **clavulanic acid** to protect against destruction by **beta-lactamase**
60
Mechanism: **Macrolides** Azithromycin Clarithromycin Erythromycin
Inhibit protein synthesis by blocking **translocation** Bind to **23S rRNA** of the **50S** subunit
61
Mechanism: Monobactam Aztreonam
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
\_\_\_ is used prior to surgery to prevent S. aureus wound infections
Cefazolin (1st gen cephalosporin)
63
Adverse effects: **Fluoroquinolones** Enoxacin Ciprofloxacin Norfloxacin Levofloxacin Ofloxacin Moxifloxacin Gemifloxacin
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
Mechanism: Penicillin G, V
**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
Adverse effects: Vancomycin
1. Nephrotoxicity 2. Ototoxicity 3. Thrombophlebitis 4. Diffuse flushing (red man syndrome) * Largely preventable by pretreatment with **antihistamines** and **slow infusion rate**
66
Mechanism: Metronidazole
Forms toxic free radical metabolites in the bacterial cell that damage DNA Bacteri**cidal** and antiprotozoal
67
Resistance: Chloramphenicol
Plasmid-encoded **acetyltransferase** inactivates the drug
68
Adverse effects: Penicillinase-resistant penicillins Dicloxacillin Nafcillin Oxacillin Methicillin (D/C)
1. Hypersensitivity reactions 2. Interstitial nephritis
69
Mechanism: Linezolid
Inhibits protein synthesis by binding to **50S** subunit and preventing formation of the **initiation complex**
70
Mechanism: Vancomycin
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
Resistance: Vancomycin
Occurs in bacteria (Enterococcus) via amino acid modification of D-ala-D-ala → D-ala-D-**lac**
72
Adverse effects: Clindamycin
1. Pseudomembranous colitis (C. difficile) 2. Fever 3. Diarrhea
73
Adverse effects: Trimethoprim
1. Megaloblastic anemia 2. Leukopenia 3. Granylocytopenia Adverse effects may be alleviated with supplemental **folinic acid**
74
Name the beta-lactamase inhibitors
1. Clavulanic acid 2. Avibactam 3. Sulbactam 4. Tazobactam
75
Adverse effects: Antipseudonomal penicillins Peperacillin Ticarcillin
1. Hypersensitivity reactions
76
Most protein synthesis inhibitors are ___ with the exception of \_\_\_
Bacteriostatic Exception: Aminoglycosides
77
Resistance: **Tetracyclines** Tetracycline Doxycycline Minocycline
**Decrease uptake** and **increase efflux** out of bacterial cells by **plasmic-encoded transport pumps**
78
Daptomycin is NOT used for \_\_\_
**Pneumonia** - daptomycin avidly binds to and is inactivated by **surfactant**
79
Mechanism: Clindamycin
Blocks peptide **transfer (translocation)** at **50S** subunit Bacteriostatic
80
Class: Tobramycin
Aminoglycoside
81
\_\_\_ is an aminoglycoside used for bowel surgery
Neomycin
82
Clinical use: 2nd generation cephalosporins Cefaclor Cefoxitin Cefuroxime
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
Mechanism: Dapsone
Similar to sulfonamides (inhibits dihydropteroate synthase) , but structurally distinct

PHARMACOLOGY (33 decks)

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