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Pharmacology > Antibiotics-Drugs, MOAs, adverse effects, key features. > Flashcards

Antibiotics-Drugs, MOAs, adverse effects, key features. Flashcards

1
Q

B-lactam compounds

A

Penicillins, cephalosporins, monobactams, carbapenems.

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2
Q

B-Lactam common traits

A

Are bactericidal, all contain a lactam ring, susceptible to B-lactamase

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3
Q

Penicillin compounds MOA

A

Bind to and inhibit PBP enzymes. PBPs play important role in synthesis and maintenance of bacterial cell wall peptidoglycan

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4
Q

Penicllin compounds key adverse effects

A

Hypersensitivity Rxn: Rash, hives, itching, respiration diffulcty, anaphylaxis (w/ anaphylaxis, expect cross reactivity)

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5
Q

Narrow spectrum B-lactam drugs, key features, and sensitive organisms

A

Penicillin G and V. B-lactamase sensitive.

Sensitive organisms: streptococci, pneumococci, meningococci, Treponema pallidum

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6
Q

Very Narrow Spectrum B-lactam drugs/key features/sensitive organisms

A

Methicillin, nafcillin, oxacillin. B-lactamase RESISTANT

Sensitive organisms: Staphylococci (not MRSA)

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7
Q

Broad spectrum B-lactam drugs/key features`

A

Ampicillin, amoxicillin. B-lactamase sensitive

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8
Q

Extended spectrum B-lactams

A

Piperacillin, Ticarcillin, Azlocillin. B-lactamase sensitive.
Sensitive organisms: Gran-negative rods, antipseudomonal

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9
Q

B-lactamase inhibitors MOA

A

Inhibit bacterial B-lactamase-often given with a B-lactam antibiotic

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10
Q

B-lactamase key adverse effects

A

Similar to penicillin agent that it is administered with

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11
Q

Cephalosporins MOA

A

Similar to penicillins, bind to and inhibit Penicillin binding proteins (PBPs). Generally more resistant to B-lactamase

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12
Q

Cephalosporins key adverse effects

A

Hypersensitivity

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13
Q

Cephalosporin-Sensitivity vs. Generation

A

As you go from 1st to 4th generation cephalosporin, the drugs go from more specific to less specific (1st gen=very specific, 4th generation=broad spectrum)

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14
Q

1st Generation cephalosporin selectivity

A

Gram + cocci

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15
Q

1st Generation cephalosporin-Agents

A

Cefazolin, Cephalexin

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16
Q

1st generation cephalosporins- key features

A

Used for surgical prophylaxis, does NOT enter CNS

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17
Q

2nd Generation Cephalosporin Agents

A

Cefotetan, Cefaclor, Fefuroxime

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18
Q

2nd gen cephalosporin key features

A

do NOT enter CNS, EXCEPT for cefuroxime

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19
Q

3rd Generation Cephalosporin agents

A

Ceftriaxone, Cefotaxime, Cefdinir, Cefixime

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20
Q

3rd Gen Cephalosporin key features

A

Most enter CNS, Used in treating meningitis and sepsis

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21
Q

4th Gen cephalosporin agents

A

Cefepime

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22
Q

4th gen cephalosporin key features

A

B-lactamase resistant, enter CNS, broadest spectrum

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23
Q

Monobactam (aztreonam) MOA, clinical use

A

Bind to and inhibit PBPs. Can penetrate the cerebrospinal fluid.
Used to treat serious infections=>pneumonia, meningitis, and sepsis.
B-lactamase resistant

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24
Q

Monobactam (aztreonam) adverse effects

A

Hypersensitivity=>skin rashes and itching, not as concerned w/ anaphylactic rxns.

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25
Q

Carbapenems MOA

A

Bind to and inhibit PBPs. B-lactamase resistant, but susceptible to a similar enzyme (carbamenemase).

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26
Q

Carbapenems adverse effects

A

GI: Nausea, vomiting, and diarrhea

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27
Q

Vancomycin MOA/ TX

A

Prevents elongation of peptidoglycan cell wall structure by binding to the D-ala-D-ala pentapeptide and acting as a steric inhibitor.
Used to treat MRSA, enterococci, and C. dif.

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28
Q

Vancomycin adverse effects

A

Skin: flushing (red neck or “red man syndrome”).

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29
Q

Vancomycin Tissue penetration

A

Good tissue penetration except for CNS

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30
Q

Bacitracin MOA

A

Blocks incorporation of amino acids and nucleic acids into the cell wall

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31
Q

Bacitracin-adverse effects

A

Hypersensitivity rxns-rare

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32
Q

Where is bacitracin commonly found?

A

In topical and ophthalmic ointments, often combined w/ other antimicrobial agents

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33
Q

Fosfomycin MOA

A

Blocks an early step in cell wall synthesis=>prevents synthesis of UDP-N-aceylmuramic acid

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34
Q

Fosfomycin is commonly used in what?

A

Uncomplicated UTIs in females=>broad spectrum

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35
Q

Classes that are bacterial protein synthesis inhibitors

A

aminoglycosides, macrolides, tetracycline and “others”

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36
Q

Aminoglycosides MOA

A

Binds to 30s and blocks formation of initiation complex (step 1).
Used in combo w/ B-lactams to treat serious gram (-) infections.

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37
Q

Aminoglycosides adverse effects

A

Nephrotoxicity=>renal tubular necrosis

Ototoxicity=> dizziness, ringing, fullness

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38
Q

Macrolides MOA

A

Binds to 50s and impairs the translocation of “P” site (step 4)

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39
Q

Macrolides adverse effects

A

GI: stomach cramps, nausea, vomiting, diarrhea (motilin receptor agonist)

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40
Q

Tetracycline MOA

A

Binds to 30s subunit of ribosome and prevents binding of a new aminoacyl-tRNA to “A) site (step 1)

41
Q

Tetracycline adverse effects

A

Nutrient interaction: Bind calcium which results in growth of calcified tissue, particularly during growth (bone, teeth)=>do not use in children, or in pregnant females.
Ecological effects: Disrupt normal flora
Skin: Photosensitivity

42
Q

Clindamycin MOA

A

Binds to 50s subunit of ribosdome and prevents formation of initiation complexes (step 1) and translocation to “P” site similar to macrolides (step 4)

43
Q

Clindamycin adverse effects

A

GI: Nausea, vomiting, diarrhea, C.difficile infection

44
Q

Chloramphenicol MOA

A

Binds to 50s subunit and prevents tarspeptidation or peptidyl bond formation (step 2)

45
Q

Chloramphenicol adverse effects

A

Blood: Suppression of RBC production

Gray Baby Syndrome: Infants lack glucuronic acid conjugation=> gray color, shock, vomiting, vascular collapse

46
Q

Linezolid MOA

A

Inhibits protein synthesis by binding to P site of 50 S ribosome and inhibits the formation of the ribosomal-fMet tRNA complex (step 1) (blocks first charged tRNA from coming in)

47
Q

Linezolid clinical indications

A

Effective against resistant bacteria=> penicillin, methicillin, and vancomycin resistance

48
Q

Linezolid adverse effects

A

Blood: Myelosuppression=> anemia, leukopenia, pancytopenia, thrombocytopenia

49
Q

Sulfonamide MOA

A

Compete with PABA for dihydropteroate synthase and block dihydrofolic acid synthesis and thus DNA synthases

50
Q

Sulfonamide adverse effects

A

Skin: Hypersensitivity, photosensitivity, Steven-Johnson syndrome (serious/fatal skin and mucous membrane eruption)

51
Q

Sulfonamide common clinical use

A

Urinary Tract Infections

52
Q

Trimethoprim MOA

A

Inhibitor of bacterial dihydrofolate reductase (DHFR) resulting in impaired DNA synthesis

53
Q

Trimehtoprim adverse effects

A

Blood: Bone marrow suppression, megaloblastic anemia, leukopenia, granulocytopenia

54
Q

Trimethoprim common clinical use

A

Urinary Tract Infections

55
Q

TMP-SMX

A

Synergistic activity of trimethoprim and sulfamethoxazole, commonly used to treat UTIs and prostatis

56
Q

Fluoroquinolone MOA

A

Disrupt the winding of DNA and the seperation of DNA strands during transcription and replication. Inhibit topoisomerase II and topoisomerase IV

57
Q

Fluoroquinolone adverse effects

A

GI: Nausea, vomiting, diarrhea
Drug-Nutrient interaction: Binds divalent cations (Ca2+), prevents absorption
Cardio: QT prolongation

58
Q

Group 1 fluoroquinolones

A

Norfloxacin-least active

59
Q

Group 2 fluoroquinolones

A

Ciprofloxacin, levofloxacin, ofloxacin-works well against gram (-) and some activity against gram (+)

60
Q

Group 3 fluoroquinolones

A

Gatifloxacin, Gemifloxacin, Moxifloxacin-Best activity against gram-positive

61
Q

Metronidazole MOA

A

Prodrug-inactive until taken-up by organism and undergoes chemical reduction. Metabolites bind to DNA and disrupt function and cause damage

62
Q

Metronidazole adverese effects

A

GI: nausea, vomiting, diarrhea
Metabolism: Disulfiram effect=> avoid alcohol

63
Q

Metronidazole clinical indications

A
  • Only use for anaerobic bacteria
  • Also effective against protozoa
  • Mild to moderate C. dif infections
64
Q

Daptomycin (lapopetide) MOA

A

Binds to membrane and causes depolarization of the membrane=>bactericidal. Insertion into membrane is calcium dependent

65
Q

Daptomycin adverse effects

A

Musculoskeletal system: Myopathyk, rhabdomyolysis

66
Q

Daptomycin clinical indications

A

Useful against gram positive organisms, and resistant organisms (MRSA)

67
Q

Polymyxin B MOA

A

Binds to phospholipids in cell membrane and disrupts structure (punches holes) specifically LPS

68
Q

Polymyxin B adverse effects

69
Q

Polymyxin B clinical indications

A

Topical agent for skin infections, usually in comvination with bacitracin.
Primarily effective against Gram (-) bacteria.

70
Q

Penicillin and Cephalosporim Resistance Mechanisms

A
  • Expression of B-lactamase
  • Alteration of PBP binding to drug
  • Alteration in porin function
71
Q

Aminoglycoside resistance mechanism

A

Expression of enzymes that alter chemical structure of the drug

72
Q

Macrolide resistance mechanism

A
  • Transport of drug out of cell (drug efflux)

- Alteration of drug binding to 50S ribosomal subunit

73
Q

Tetracyclines resistance mechanism

A

Transport of drug out of cell (drug efflux)

74
Q

Sulfonamide resistance mechanism

A
  • Less sensitive drug target
  • Increased synthesis of PABA
  • Scavenge or use other sources of folic acid
75
Q

Fluoroquinolones resistance mechanism

A
  • Less sensitive drug target

- Transport out of cell (drug efflux)

76
Q

Chloramphenicol resistance mechanism

A

Expression of inactivating enzymes

77
Q

Uncomplicated Skin and soft tissue infection pharmacological considerations

A

Ampicillin, or cephalexin (1st generation cephalosporin)

If allergy: Vancomycin or clindamycin

78
Q

Complicated skin/soft tissue infection pharmacological considerations

A

Penicillin + lactamase inhibitor

79
Q

MRSA infection

A

Vancomycin, linezolid, or daptomycin

80
Q

Osteomyelitis pharmacoligical considerations

A

Vancomycin

Cephalosporins=> ceftriaxone or cefepime

81
Q

Surgery pharmacological consideration

A

Penicillin + lactamase inhibitor

82
Q

Septic arthritis pharmacological consideration

A

Empiric: Ceftriaxone
MRSA: Vancomycin, linezolid, daptomycin

83
Q

Prosthetic Joint pharmacological consideration

A

Rifampin (not covered in this section, but need to know)

84
Q

Acute sinusitis pharmacological considerations

A

Penicillin +lactamase inhibitors => amoxicillin + clavulanate

85
Q

Pharyngitis pharmacologic considerations

A

Penicillin or amoxicillin

Allergy: 1st generation chephalosporin

86
Q

Community acquried bacterial pneumonia pharmacological considerations

A

Ambulatory: Macrolides=> erythromycin, azithromycin, clarithromycin
Hospitalization: B-lactam + macrolide
MRSA: Vancomycin, linelozid

87
Q

Hospital acquired, healthcare associated pneumonia pharmacological considerations

A

Empiric: Ceftriaxone
MRSA: vancomycin, linezolid

88
Q

Uncomplicated UTI pharmacological considerations

A

Cystitis: TMP-SMX
Pyelonephritis: TMP-SMX, fluoroquinolone

89
Q

Complicated UTI pharm considerations

A

Fluorquionolone and TMP-SMX

90
Q

Prostatitis pharm considerations

A

Fluoroquinolone and TMP-SMX

91
Q

Intra-abdominal infection pharm considerations

A

Ticarcillin + clavulanate

92
Q

C. difficile infection pharm consideratiosn

A

Metronidazole (moderate)

Vancomycin (severe)

93
Q

Community acquired bacterial meningitis pharm considerations

A

Ceftriaxone or cefotaxime + vancomycin

94
Q

Neonatal meningitis

A

Ampicillin + cephalosporin plus/minus gentamicin

95
Q

Sepsis syndrome pharm considerations

A

3rd or 4th generation cephalosporin (cefepime) plus vancomycin

96
Q

Endocarditis pharm considerations

A

Ceftriaxone plus vancomycin

97
Q

Fever and neutropenia pharm considerations

A

Ciprofloxacin plus amoxicillin/clavulanate

98
Q

Multi-drug resistance pharm considerations

A

Enterococci: Linezolid, daptomycin, tigecycline
Gram (-) bacteria: Carbapenem (imipenem or meropenem)
If bacteria has carbapenemases=> Polymyxin B or Tigecycline

Pharmacology (11 decks)

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