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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
Carbapenems MOA
Bind to and inhibit PBPs. B-lactamase resistant, but susceptible to a similar enzyme (carbamenemase).
26
Carbapenems adverse effects
GI: Nausea, vomiting, and diarrhea
27
Vancomycin MOA/ TX
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.
28
Vancomycin adverse effects
Skin: flushing (red neck or "red man syndrome").
29
Vancomycin Tissue penetration
Good tissue penetration except for CNS
30
Bacitracin MOA
Blocks incorporation of amino acids and nucleic acids into the cell wall
31
Bacitracin-adverse effects
Hypersensitivity rxns-rare
32
Where is bacitracin commonly found?
In topical and ophthalmic ointments, often combined w/ other antimicrobial agents
33
Fosfomycin MOA
Blocks an early step in cell wall synthesis=>prevents synthesis of UDP-N-aceylmuramic acid
34
Fosfomycin is commonly used in what?
Uncomplicated UTIs in females=>broad spectrum
35
Classes that are bacterial protein synthesis inhibitors
aminoglycosides, macrolides, tetracycline and "others"
36
Aminoglycosides MOA
Binds to 30s and blocks formation of initiation complex (step 1). Used in combo w/ B-lactams to treat serious gram (-) infections.
37
Aminoglycosides adverse effects
Nephrotoxicity=>renal tubular necrosis | Ototoxicity=> dizziness, ringing, fullness
38
Macrolides MOA
Binds to 50s and impairs the translocation of "P" site (step 4)
39
Macrolides adverse effects
GI: stomach cramps, nausea, vomiting, diarrhea (motilin receptor agonist)
40
Tetracycline MOA
Binds to 30s subunit of ribosome and prevents binding of a new aminoacyl-tRNA to "A) site (step 1)
41
Tetracycline adverse effects
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
Clindamycin MOA
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
Clindamycin adverse effects
GI: Nausea, vomiting, diarrhea, C.difficile infection
44
Chloramphenicol MOA
Binds to 50s subunit and prevents tarspeptidation or peptidyl bond formation (step 2)
45
Chloramphenicol adverse effects
Blood: Suppression of RBC production | Gray Baby Syndrome: Infants lack glucuronic acid conjugation=> gray color, shock, vomiting, vascular collapse
46
Linezolid MOA
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
Linezolid clinical indications
Effective against resistant bacteria=> penicillin, methicillin, and vancomycin resistance
48
Linezolid adverse effects
Blood: Myelosuppression=> anemia, leukopenia, pancytopenia, thrombocytopenia
49
Sulfonamide MOA
Compete with PABA for dihydropteroate synthase and block dihydrofolic acid synthesis and thus DNA synthases
50
Sulfonamide adverse effects
Skin: Hypersensitivity, photosensitivity, Steven-Johnson syndrome (serious/fatal skin and mucous membrane eruption)
51
Sulfonamide common clinical use
Urinary Tract Infections
52
Trimethoprim MOA
Inhibitor of bacterial dihydrofolate reductase (DHFR) resulting in impaired DNA synthesis
53
Trimehtoprim adverse effects
Blood: Bone marrow suppression, megaloblastic anemia, leukopenia, granulocytopenia
54
Trimethoprim common clinical use
Urinary Tract Infections
55
TMP-SMX
Synergistic activity of trimethoprim and sulfamethoxazole, commonly used to treat UTIs and prostatis
56
Fluoroquinolone MOA
Disrupt the winding of DNA and the seperation of DNA strands during transcription and replication. Inhibit topoisomerase II and topoisomerase IV
57
Fluoroquinolone adverse effects
GI: Nausea, vomiting, diarrhea Drug-Nutrient interaction: Binds divalent cations (Ca2+), prevents absorption Cardio: QT prolongation
58
Group 1 fluoroquinolones
Norfloxacin-least active
59
Group 2 fluoroquinolones
Ciprofloxacin, levofloxacin, ofloxacin-works well against gram (-) and some activity against gram (+)
60
Group 3 fluoroquinolones
Gatifloxacin, Gemifloxacin, Moxifloxacin-Best activity against gram-positive
61
Metronidazole MOA
Prodrug-inactive until taken-up by organism and undergoes chemical reduction. Metabolites bind to DNA and disrupt function and cause damage
62
Metronidazole adverese effects
GI: nausea, vomiting, diarrhea Metabolism: Disulfiram effect=> avoid alcohol
63
Metronidazole clinical indications
- Only use for anaerobic bacteria - Also effective against protozoa - Mild to moderate C. dif infections
64
Daptomycin (lapopetide) MOA
Binds to membrane and causes depolarization of the membrane=>bactericidal. Insertion into membrane is calcium dependent
65
Daptomycin adverse effects
Musculoskeletal system: Myopathyk, rhabdomyolysis
66
Daptomycin clinical indications
Useful against gram positive organisms, and resistant organisms (MRSA)
67
Polymyxin B MOA
Binds to phospholipids in cell membrane and disrupts structure (punches holes) specifically LPS
68
Polymyxin B adverse effects
Rare
69
Polymyxin B clinical indications
Topical agent for skin infections, usually in comvination with bacitracin. Primarily effective against Gram (-) bacteria.
70
Penicillin and Cephalosporim Resistance Mechanisms
- Expression of B-lactamase - Alteration of PBP binding to drug - Alteration in porin function
71
Aminoglycoside resistance mechanism
Expression of enzymes that alter chemical structure of the drug
72
Macrolide resistance mechanism
- Transport of drug out of cell (drug efflux) | - Alteration of drug binding to 50S ribosomal subunit
73
Tetracyclines resistance mechanism
Transport of drug out of cell (drug efflux)
74
Sulfonamide resistance mechanism
- Less sensitive drug target - Increased synthesis of PABA - Scavenge or use other sources of folic acid
75
Fluoroquinolones resistance mechanism
- Less sensitive drug target | - Transport out of cell (drug efflux)
76
Chloramphenicol resistance mechanism
Expression of inactivating enzymes
77
Uncomplicated Skin and soft tissue infection pharmacological considerations
Ampicillin, or cephalexin (1st generation cephalosporin) | If allergy: Vancomycin or clindamycin
78
Complicated skin/soft tissue infection pharmacological considerations
Penicillin + lactamase inhibitor
79
MRSA infection
Vancomycin, linezolid, or daptomycin
80
Osteomyelitis pharmacoligical considerations
Vancomycin | Cephalosporins=> ceftriaxone or cefepime
81
Surgery pharmacological consideration
Penicillin + lactamase inhibitor
82
Septic arthritis pharmacological consideration
Empiric: Ceftriaxone MRSA: Vancomycin, linezolid, daptomycin
83
Prosthetic Joint pharmacological consideration
Rifampin (not covered in this section, but need to know)
84
Acute sinusitis pharmacological considerations
Penicillin +lactamase inhibitors => amoxicillin + clavulanate
85
Pharyngitis pharmacologic considerations
Penicillin or amoxicillin | Allergy: 1st generation chephalosporin
86
Community acquried bacterial pneumonia pharmacological considerations
Ambulatory: Macrolides=> erythromycin, azithromycin, clarithromycin Hospitalization: B-lactam + macrolide MRSA: Vancomycin, linelozid
87
Hospital acquired, healthcare associated pneumonia pharmacological considerations
Empiric: Ceftriaxone MRSA: vancomycin, linezolid
88
Uncomplicated UTI pharmacological considerations
Cystitis: TMP-SMX Pyelonephritis: TMP-SMX, fluoroquinolone
89
Complicated UTI pharm considerations
Fluorquionolone and TMP-SMX
90
Prostatitis pharm considerations
Fluoroquinolone and TMP-SMX
91
Intra-abdominal infection pharm considerations
Ticarcillin + clavulanate
92
C. difficile infection pharm consideratiosn
Metronidazole (moderate) | Vancomycin (severe)
93
Community acquired bacterial meningitis pharm considerations
Ceftriaxone or cefotaxime + vancomycin
94
Neonatal meningitis
Ampicillin + cephalosporin plus/minus gentamicin
95
Sepsis syndrome pharm considerations
3rd or 4th generation cephalosporin (cefepime) plus vancomycin
96
Endocarditis pharm considerations
Ceftriaxone plus vancomycin
97
Fever and neutropenia pharm considerations
Ciprofloxacin plus amoxicillin/clavulanate
98
Multi-drug resistance pharm considerations
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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