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Therapeutics III > Study > Flashcards

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1
Q

Macrolides

A

Erythromycin, clarithromycin, azithromycin

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2
Q

Macrolides MOA

A

Blocks peptide formation at the 50s ribosomal subunit to inhibit protein synthesis

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3
Q

Macrolides C vs S

A

Static

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4
Q

Macrolides PD

A

Time-dependent

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5
Q

Macrolides pathogens

A

Broad spectrum
Gram +, Neisseria, Treponema
DOF for atypicals (mycoplasma, legionella, chlamydia)

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6
Q

Macrolides main uses

A

Used in pregnancy and for penicillin allergies
STI (chlamydia, gonorrhea)
RTI (pharyngitis, otitis, CAP)
Gastroparesis

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7
Q

Do macrolides have MRSA or pseudomonas coverage?

A

No

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8
Q

Macrolides AE

A

GI

Increased QTc interval

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9
Q

Macrolides DDI

A

CYP3A4 inhibitor- increases levels of: warfarin, statins, theophylline, triazolam, carbamazepine, cyclosporine, sildenafil, etc.
Less interactions with azithromycin

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10
Q

Macrolides resistance

A

Low level resistance is associated with the mef gene (efflux pump)
High levels are associated with target-site modification, Domain 5 is methylated, coded by erm gene, and macrolides cant bind

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11
Q

Oxazolidinones

A

Linezolid, Tedizolid

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12
Q

Linezolid MOA

A

Inhibits early protein synthesis at 70s initiation complex

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13
Q

Linezolid S vs C

A

Static

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14
Q

Linezolid PD

A

Time-dependent

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15
Q

Linezolid pathogens

A

Narrow spectrum

Gram (+), MRSA, VRE

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16
Q

Linezolid main uses

A

Alternative to vanc in MRSA, VRE

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17
Q

Linezolid MRSA or pseudomonas coverage?

A

MRSA

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18
Q

Linezolid AE

A

GI, rashes, neuropathy

Warnings: serotonin syndrome, hematologic (weekly CBC)

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19
Q

Lincosamide

A

Clindamycin

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20
Q

Lincosamide MOA

A

Binds to 50s, inhibiting protein synthesis

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21
Q

Lincosamide C vs S

A

Static

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22
Q

Lincosamide PD

A

Time-dependent

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23
Q

Lincosamide pathogens

A

Broad spectrum

Gram +, anaerobes, pneumocystis, toxoplasma

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24
Q

Lincosamide main uses

A 
Skin, soft tissue, bone infections
Used for its anti-toxin properties
IA anaerobes infections
Acne, rosacea
Toxoplasma, pneumocystis
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25
Lincosamide MRSA/pseudomonas?
No
26
Lincosamide resistance
Altered target, decreased binding, efflux
27
Streptogramin
Quinupristin-dalfopristin (Synercid)
28
Streptogramin MOA
Dalfopristin alters conformation of the 50s ribosome such that affinity for quinuprostin is increased.
29
Streptogramin s vs c
Synergistically cidal
30
Streptogramin PD
Concentration-dependent
31
Streptogramin spectrum
Gram +, MRSA, VRE
32
Streptogramin MRSA/pseudomonas coverage?
MRSA
33
Streptogramin AE
Local vein reactions | Arthralgia
34
Streptogramin DDI
Inhibits 3A4 metabolism
35
Streptogramin resistance
Increased binding to target, enzymatic inactivation, efflux
36
Lefamulin MOA
Inhibits protein synthesis through interactions with A and P sites of Domain 5 of 50s subunit
37
Lefamulin C vs S
both
38
Lefamulin PD
Time-dependent
39
Lefamulin pathogens
Strep, staph (MRSA), atypicals
40
Lefamulin main uses
CAP
41
Lefamulin MRSA/ pseudomonas?
MRSA
42
Lefamulin AE
Injection site reactions, insomnia, embryo-fetal toxicity, GI, increased LFTs, QTc prolongation
43
Lefamulin DDI
Inhibits 3A4 | Avoid quinidine, amiodarone, sotalol, procainamide
44
Lefamulin and food
Food decreases absorption
45
Aminoglycosides
Gentamicin, Tobramycin, streptomycin, amikacin
46
Aminoglycosides MOA
Irreversibly binds to the 30s ribosome
47
Aminoglycosides C vs S
Cidal
48
Aminoglycosides PD
Concentration dependent
49
Aminoglycosides pathogens
``` Primarily gram (-). pseudomonas Gram (+) if synergistic with cell wall agents ```
50
Aminoglycosides uses
``` Severe gram (-) infections (in combo) Gram (+) of synergistic with cell wall inhibitors (endocarditis) Tuberculosis (streptomycin) ```
51
Aminoglycosides MRSA/pseudomonas coverage?
Pseudomonas
52
Aminoglycosides AE
Nephrotoxicity, ototoxicity, neuromuscular blockade
53
Aminoglycosides resistance
Enzyme modification, altered 30s, efflux
54
Aminoglycosides PAE
LONG PAE, requires serum concentration monitoring
55
Tetracyclines
Tetracyclines, doxycyclines, tigecycline
56
Tetracyclines MOA
Binds to the 30s ribosome, blocking the formation of initiation complex
57
Tetracyclines C vs S
Static
58
Tetracyclines PD
Time-dependent
59
Tetracyclines pathogens
Broad spectrum Gram (+), (-), atypicals, anaerobes Tigecycline- MDR, VRE, MRSA
60
Tetracyclines uses
``` GI infections RTI STI Alternative for syphilis in penicillin allergy DOC for tickborne diseases (doxy) ```
61
Tetracyclines MRSA/ pseudomonas?
Tigecycline- MRSA
62
Tetracyclines AE
Tooth discoloration, enamel hyperplasia in childern, photosensitivity, GI, hepatotoxicity, AKI Minocycline- dizziness, vertigo, tinnutis
63
Tetracyclines DDI
Antacids and dairy products intefere with absorption May potentiate the effects of oral anticoagulants Decreased effficacy of BC
64
Tetracyclines BBW
Tigecycline- increased risk of death
65
Fluoroquinolones
Ciprofloxacin, levofloxacin, moxifloxacin
66
Fluoroquinolones MOA
Inhibits DNA gyrase blocking DNA replication and leading to cell death
67
Fluoroquinolones C vs S
Cidal
68
Fluoroquinolones PD
Concentration dependent
69
Fluoroquinolones Pathogens
``` Broad spectrum Cipro- best form gram (-) Others- Gram (+) All- atypicals, M. Tuberculosis Moxi, Gemi- anaerobes ```
70
Fluoroquinolones main uses
``` RTI (not cipro) UTIs/prostatitis (not moxi) GI Osteomyelitis Anthrax Tuberculosis ```
71
Fluoroquinolones MRSA/Pseudomonas?
Delafloxacin- MRSA | Ciprofloxacin, levofloxacin- pseudomonas
72
Fluoroquinolones AE
GI, CNS, rash, photosensitivity, hematuria, QTc prolongation, tendonitis, peripheral neuropathy, hypoglycemia, mental health Do not use in pregnancy or <18 yo
73
Fluoroquinolones DDI
antacids impair absorption
74
Fluoroquinolones resistance
Chromosomal mutation leading to altered target site, efflux mechanisms
75
Fluoroquinolones BBW
Reserve for no other options
76
Sulfonamides
Bactrim Sulfadiaxine + pyrumethamine Sulfadoxine + pyrimethamine
77
Sulfonamides MOA
Folate inhibitor, blocks purine production and nucleic acid synthesis
78
Sulfonamides C vs S
Synergistically cidal
79
Sulfonamides PD
Time-dependent
80
Sulfonamides pathogens
Broad spectrum Gram (+), Gram (-) Pneumocystis (PJP) Atypicals
81
Sulfonamides uses
Uncomplicated UTIs PJP (Pneumocystis) Prostatitis, skin infections, infectious diarrhea, toxoplasmosis, malaria
82
Sulfonamides MRSA/pseudomonas?
Community acquired MRSA
83
Sulfonamides AE
GI, rash, urticaria, photosensitivty, B.M suppression, hyperkalemia, AKI, hypersensitivity Do NOT use in newborns or 3rd trimester
84
Sulfonamides DDI
CYP2C9 inhibitor- increases effects of sulfonyureas, warfarin, anticoagulants, cyclosporine, methotrexate
85
Nitrofurantoin MOA
Inhibits several enzyme systems, including acetyl coA, inhibiting metabolism
86
Nitrofurantoin C vs S
Cidal
87
Nitrofurantoin PD
Time-dependent
88
Nitrofurantoin pathogens
Primarily gram (-) E. coli Also covers E. faecalis, MSSA
89
Nitrofurantoin uses
UTI (cystitis only)
90
Nitrofurantoin MRSA/Pseudomonas?
no
91
Nitrofurantoin AE
N/V/D, rash, pulmonary toxicity, increased LFTs, peripheral neuropathy, anemia
92
Nitrofurantoin DDI
Antacids (Mg) decrease abs. Probenecid decreases renal excretion Ethanol increases CNS depression
93
Nitrofurantoin CrCl cutoff
<40ml/min
94
Penicillins
Natural- pen vk, pen g Anti-staphylococcal- nafcillin, oxacillin, dicloxacillin Amino- amoxicillin, ampicillin Ureido-piperacillin
95
Beta lactam MOA
Cleaves the beta lactam bond of PBP inhibiting the 3rd step of cell wall synthesis
96
Penicillin pathogens
Natural- Gram +, strep, syphilis Anti-staphylococcal- narrow spectrum, Gram +, MSSA Amino- Gram +, some Gram - Ureido- Gram +, Gram -, pseudomonas
97
Penicillin uses
Pen G- syphilis, meningitis Pen VK- strep throat Anti-staphylococcal- serious MSSA infections Amino- IA, pelvic, skin, pulmonary, bite wounds, STIs Ureido- pneumonia, bacteremia, IA, diabetic foot, neutropenia
98
Penicillin MRSA/pseudomonas?
Ureido- pseudomonas
99
Beta lactam AE
GI/rash/allergy
100
Beta lactam resistance
Beta lactamases break a bond in the beta lactam nucleus, disabling it. Beta lactamase inhibitors extend spectrum
101
Cephalosporins
``` 1st- cefazolin, cephalexin 2nd- cefoxitin, cefuroxime 3rd- ceftriaxone, ceftazidime, cefdinir 4th- Cefepime, ceftolozane 5th- Ceftaroline ```
102
Beta lactam S vs C
Cidal
103
Beta lactam PD
Time dependent
104
Cephalosporin pathogens
Spectrum increases from 1st to 4th generation due to enhanced beta lactamase activity. All cover Gram + 3/4th- penetrate CNS for meningitis and pseudomonas 5th- MRSA
105
Cephalosporin uses
1st- surgical prophylaxis, UTI, RTI 2nd- mixed infections, Cefuroxime- meningitis 3rd- Broader- meningitis, gonorrhea, serious hospital infections 4th- serious hospital infections, very broad 5th- MRSA
106
Cephalosporin MRSA/pseudomonas?
5th- MRSA | 3rd and 4th- pseudomonas
107
Glycopeptides
Vancomycin
108
Glycopeptides MOA
Complexes to D-Ala-D-Ala precursor of cell wall pentapeptide interfering with elongation of the peptidoglycan backbone
109
Glycopeptides C vs S
Cidal
110
Glycopeptides PD
Time-dependent killing
111
Glycopeptides pathogens
Gram + ONLY, MRSA | Oral-C.diff
112
Glycopeptides uses
MRSA
113
Glycopeptides AE
Nephrotoxicity, ototoxicity, phlebitis, Red Man Syndrome
114
Vanc trough
Little to no PAE | Trough concentration: 10-20ug/mL
115
Daptomycin MOA
Binds to gram + via Ca dependent interaction with membrane disruption and loss of K
116
Daptomycin C vs S
Cidal
117
Daptomycin PD
concentration-dependent
118
Daptomycin pathogens
Gram +, MRSA
119
Daptomycin uses
Alternative to vanc for MRSA (non-pneumonia)
120
Daptomycin AE
myopathy (monitor CPK levels)
121
Polymyxins MOA
Binds with anionic LPS molecules by displacing Ca and Mg from the outer membrane of gram negative bacteria, leading to permeability changes, leakage, and cell death
122
Polymyxins S vc C
Cidal
123
Polymyxins PD
Concentration-dependent
124
Polymyxins pathogens
Gram -
125
Polymyxins uses
Last resort for MDR
126
Polymyxins MRSA/ pseudomonas?
no
127
Polymyxins AE
nephrotoxicity, neurotoxicity
128
Atypical microorganisms
Legionella, chlamydia, mycoplasma
129
Treatment of atpicals
Fluoroquinolones Macrolides Tetracyclines
130
Anaerobic coverage
``` Metronidazole B-lactam/B-lactamase inihbitors Cefoxitin, Cefotetan Carbapenems Clindamycin Moxifloxacin Tigecycline Chloramphenicol ```
131
Pseudomonas coverage
``` Pip/Tazo Cefepime Ceftazidime Ceftolozane Carbapenems Ciprofloxacin, Levofloxacin Aminoglycosides Aztreonam Polymyxin B, Colistin ```
132
Gram negative coverage
``` PCNs (Ureido>Amino) 2nd, 3rd, 4th gen cephalosporins Carbapenems Aztreonam Aminoglycosides Fluoroquinolones TMP/SMZ Tigecycline Polymyxin B, Colistin ```
133
MDR Gram (-) pathogens
``` Serratia Pseudomonas Acinetobacter Citrobacter Enterobacter ``` -Requires broad spectrum coverage with cefepime, pip/tazo, or carbapenems
134
ESBL producers
``` Klebsiella E. coli Enterobacter Proteus Serratia ``` Requires carbapenems
135
Agents with CA-MRSA coverage
TMP/SMZ Doxycycline Clindamycin
136
Agents with skin MRSA coverage
Dalbavacin, oritavancin, delafloxacin
137
Agents with MRSA coverage
Vanc, Dapto, linezolid, ceftaroline, telavancin, tigecycline, synercid
138
MSSA treatment and alternatives
1st line- nafcillin, oxacillin | Alt- cefazolin
139
MRSA treatment and alternatives
Treatment- Vanc | Alt- linezolid, dapto, ceftaroline, tigecycline, dalbavancin, oritavancin
140
MRSE treatment and alt
Treatment- Vanc | Alt- linezolid, dapto
141
S. pneumonia treatment and alt
T- cefazolin, ceftriaxone | Alt- penicillin, erythromycin
142
E. faecalis treatment and alt
T- ampicillin | alt- Vanc
143
VRE treatment and alt
T- Linezolid | Alt- dapto, tigecycline

Therapeutics III (7 decks)

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