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MS2 Unit 6 Pharm > Antibiotics 2 > Flashcards

Antibiotics 2 Flashcards

1
Q

carbapenem agents

A

imipenem-cilastatin, meropenem, ertapenem, doripenem

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2
Q

carbapenem spectrum

A

broad spectrum against gram-positive, gram-negative, and anaerobic organisms. stable against most beta lactamases including ESBLs and AmpCs. hits pseudomonas except ertapenem

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3
Q

what bug developed high level resistance against carbapenems?

A

E. faecium.

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4
Q

carbapenem clinical uses

A

complicated UTIs, complicated intraabdominal infections, healthcare acquired pneumonia, bone and SSTI, bacterial meningitis. These are usually caused by gram negative things.

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5
Q

carbapenem side effects

A

generally well tolerated. lower association with c. diff colitis, coag abnormalities, nephrotox or hepatotox. CNS: low incidence of seizures, but higher than other antibiotics.

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6
Q

what drug do carbapenems interact with?

A

substantially decrease valproic acid concentrations

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7
Q

what is great about the ertapenem halflife?

A

very long, allows q24h dosing. good for outpatient settings. has poor activity against pseudomonas / acinetobacter though

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8
Q

what is the most active carbapenem against pseudomonas?

A

doripenem!

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9
Q

monobactam agents

A

aztreonam

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10
Q

aztreoname spectrum

A

gram negative: enterobacteriaceae and pseudomonas. NO ACTIVITY AGAINST GRAM POSITIVE OR ANAEROBIC BACTERIA!

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11
Q

azteronam

A

rarely used alone empirically. alternative to penicillin to provide gram-negative coverage in combo with another agent. best used as definitive therapy for gram-neg infections. give if someone has a severe penicillin allergy

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12
Q

glycopeptide agent

A

vancomycin

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13
Q

vancomycin mechanism of action

A

inhibits late stages of cell wall synth by binding to the D-Ala D-ala terminus of the nascent peptidoglycan pentapeptide. prevents elongation by inhibiting transglycosylase.

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14
Q

mechanisms of resistance to vancomycin

A

enterococcus (VRE) can do target modication. VISA can get a thickened cell wall. VRSA gets a plasmid-mediated transfer of the vanA gene cluster from VRE.

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15
Q

vancomycin spectrum

A

gram pos: staphylococci (MRSA, MSSA), streptococci, enterococci, bacillus, corynebacterium.

Anaerobes: peptostrepto, actinomyces, propionibacterium, clostridium.

NO GRAM NEGATIVE ACTIVITY

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16
Q

vancomycin clinical uses

A

SSTI especially when MRSA is suspected (purulent cellulitis). Bacteremia and endocarditis. Meningitis and ventriculitis. Pneumonia. Bone and joint infection. Neutropenic fever. Surgical prophylaxis. C. diff colitis (only the oral form)

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17
Q

vancomycin side effects

A

nephrotox at high concentrations, infusion reactions (redman syndrome), maculopapular rash, drug fever, phlebitis, neutropenia, thrombocytopenia

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18
Q

lipopeptide agent

A

daptomycin

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19
Q

daptomycin mechanism of action

A

insertion into the gram-positive cell membrane causing depolarization and ulimate cell death. Not a cell-wall active agent. resistance arises due to alteration of the cell membrane.

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20
Q

daptomycin spectrum

A

gram pos: s. aureus, strepto/entero cocci.

Anaerobe: has invitro activity against gram-pos anaerobes

NO GRAM NEGATIVE ACTIVITY

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21
Q

daptomycin clinical uses

A

SSTI, s. aureus bacteremia and endocarditis, osteoarticular infection, enterococcal infections. Not effective for pneumonia.

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22
Q

why is daptomycin not effective for pneumonia?

A

it is inactivated by the surfactant!

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23
Q

daptomycin side effects

A

CPK elevation and possible skeletal muscle damage. paresthesia, peripheral neuropathy. eosinophilic pneumonia-rare. causes myalgias.

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24
Q

lipoglycopeptide agents

A

telavancin, dalbavancin, oritavancin.

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25
telavancin mechanism of action
binds to cell wall precursors like vancomycin. depolarizes cell membrane. `
26
telavancin spectrum
vancomycin's spectrum PLUS VISA, VRSA, some VRE isolates
27
telavancin clinical uses
SSTI, hospital acquired pneumonia. infrequently used.
28
telavancin side effects
nephrotox, more so than vancomycin. GI: n/v, metallic taste. potentially teratogenic.
29
dalbavancin mechanism of action
inhibition of cell wall precursors
30
dalbavancin spectrum
gram positive: MRSA, MSSA, strep, coag negative staph. NO GRAM NEGATIVE ACTIVITY. Anaerobes: c. perf, c. diff, prop. acnes, peptostrepto
31
oritavancin mechanism of action
inhibition of cell wall precursors, binds to pentaglycl bridging segment in peptidoglycan and inhibits transpeptidation. interaction and disruption of the cell membrane
32
oritavancin spectrum
similar to dalbavancin, but active against VRE.
33
dalbavancin and oritavancin clinical uses
SSTI, can be given in infusion centers (good for outpatient setting). very expensive though!!!
34
aminoglycoside agents
gentamicin, tobramycin, amikacin, streptomycin
35
aminoglycoside mechanism of action
oxygen-dependent, active transport across the bacterial cell membrane. binds to the 30S subunit of ribosomes and interferes with an initiation complex, inhibiting protein synth.
36
aminoglycoside mechanism of resistance
enzymatic modification, reduced uptake or decreased cell permeability, altered ribosome binding sites.
37
aminoglycoside spectrum
gram neg: enterobacteriaceae and Pseudomonas gram pos: synergy with cell wall active agent against enterococcus (cant give as monotherapy) Amikacin: some types of mycobacteria and nocardia Anaerobes: NONE!!!!!
38
aminoglycoside clinical uses
infections caused by gram-negative bacilli. UTI. hospital acquired pneumonia when combined with a beta lactam. Enterococcal infection combined with cell wall active agent. Cystic fibrosis. Orthopedic surgery (used in antibiotic cement)
39
aminoglycosides side effects
nephrotoxicity. ototoxicity. neuromusular damage (rare)
40
aminoglycoside pharmacokinetics
distributed extensively into urine. distribution into tissues
41
aminoglycoside pharmacodynamics
concentration dependent. High peak is important!!! biphasic killing. higher the peak, the faster the killing.
42
tetracycline agents
doxycycline, minocycline, tetracycline
43
tetracycline mechanisms of action
passive diffusion through porins in gram-negative organisms. binds to 30S ribosomal subunit preventing protein synthesis
44
tetracycline mechanisms of resistance
efflux pump. ribosomal protection (through dissociation of tet from ribosomal binding sites)
45
tetracycline spectrum
atypical: chlamydia and mycoplasma pneumoniae spirochetes: borrelia, leptospira, treponema pallidum Rickettsiae. Gram pos: s. pneumoniae, CA-MRSA gram neg: h. influenzae, neiserria rapidly growing mycobacteria
46
tetracycline clinical uses
tick borne illness Drug of Choice! lyme disease, ehrlichiosis, anaplasmosis. CAP. SSTI caused by CA-MRSA. conbo therapy for h. pylori. prophylaxis for exposure to anthrax, tularemia, plague, Q fever, brucellosis
47
tetracycline side effects
GI: n/v, diarrhea. Photosensitivity and hyperpigmentation! MAINLY IN THE HANDS teeth and bone: tooth discoloration in kids. inhibition of bone growth in infants Nephrotox and neurotox
48
glycylcycline agent
tigecycline
49
glycylcycline chemistry/mechanism of action
9-glycl substitution enables tigecycline to overcome two major types of resistance: efflux pumps and ribosomal protection
50
tigecycline spectrum
organisms covered by tetracycline plus some tetracycline-resistant organisms. Broad spectrum: gram negative, gram positives, anaerobes. activity against stenotrophomonas. Doesn't hit pseudomonas, proteus, providencia, morganella
51
tigecycline clinical uses
FDA approved for complicated skin and soft tissue infections, intra-abdominal infection, CAP. also used for carbapenem resistant enterobacteriaceae. Not advised for treating bacteremia due to low serum concentrations
52
tigecycline side effects
GI: significant N/V and diarrhea. | Transaminitis. increased mortality.
53
macrolide agents
azithromycin, clarithromycin, erythromycin.
54
macrolide mechanism of action
reversible binding to 50S subunit of ribosome.
55
macrolide mechanisms of resistance
decreased permeability in enterobacteriaceae. Alteration in the 50S receptor site. Alteration in the 23S ribosomal RNA of the 50S ribosomal subunit. Enzymatic inactivation
56
macrolide spectrum
gram pos: s. pneumoniae, signif resistance in beta hemolytic strep. Gram neg: h. influenzae and m. catarrhalis. Atypicals: legionella, chlamydia, mycoplasma Anaerobes: actinomyces
57
macrolides clinical uses
uncomplicated upper and lower respiratory tract infections. Mycobacterial infection. H. pylori in combo with other agents.
58
macrolides side effects
GI: abdominal cramps, N/V, diarrhea. Thrombophlebitis with erythromycin. Cardiac: QT prolongation -> torsades de pointes
59
what is the safest macrolide to use?
azithromycin! only has one interaction. much safer than the other macrolides
60
clindamycin mechanism of action
binding to 50S ribosomal subunit preventing protein synth.
61
clindamycin mechanisms of resistance
alteration in 23S ribosomal RNA of 50S ribosomal subunit. Alteration in 50S ribosomal proteins of the receptor site. Enzymatic inactivation
62
clindamycin spectrum
gram pos: streptococci including group B strep. Staph aureus. NO GRAM NEGATIVE ACTIVITY Anaerobes: B. fragilis, clostridium, peptostreptococcus, fusobacterium, prevotella. Toxoplasmosis, plasmodium falciparum
63
clindamycin clinical uses
tends to be an alternative treatment, mainly for surgical prophylaxis and SSTIs caused by staph aureus. Combo with penicillin for toxic shock. combo with quinine for falciparum malaria
64
clindamycin side effects
diarrhea, pseudomembranous colitis
65
oxazolidinone agents
linezolid, tedizolid.
66
oxazolidinone mechanism of action
binds to 23 S ribosomal RNA of the 50S subunit inhibiting protein synthesis
67
linezolid and tedizolid spectrum
activity against gram-positives: staphylococci, enterococci, streptococci. NO GRAM NEGATIVE ACTIVITY. poor activity against anaerobes.
68
linezolid and tedizolid clinical uses
tedi is approved for SSTI. linezolid is used for enterococcal infection, nosocomial pneumonia caused by s. aureus, CAP caused by s aureus, SSTI. not recommended for s. aureus bacteremia
69
linezolid and tedizolid side effects
hematologic toxicity, reversible myelosuppression, mitochondrial toxicity, serotonin syndrome
70
fluoroquinoline agents and mechanism of action
end in -floxacin. Inhibit DNA gyrase and inhibit topoisomerase IV
71
fluoroquinolone spectrum
gram pos: s. aureus, s. pneumoniae, enterococcus (poor). gram neg: enterobacteriaceae, h flu, p aeruginosa, atypicals. mycobacterium moxifloxicin has moderate activity against anaerobes
72
fluoroquinolone clinical uses
resistance in enterobacteriaceae problematic. UTI. GI and abdominal infections: traveler's diarrhea. STDs: gonoccoal urethritis, chlamydial infection. Respiratory tract infections. Bone and joint infection. cutaneous anthrax. adjunctive therapy in MDR TB
73
fluoroquinolone side effects
GI: mild CNS: headache, dizziness, confusion Tendinitis and tendon rupture rare. QT prolongation
74
metronidazole mechanisms of action
interacts with DNA to cause a loss of helical DNA structure and strand breakage resulting in inhibition of protein synthesis
75
metronidazole antimicrobial spectrum
anaerobes: b. fragilis, clostridial species. | Protozoa
76
metronidazole clinical uses
C. diff diarrhea. intra-abdominal infections. surgical prophylaxis in colon surgery. trichomoniasis.
77
rifamycin agents
rifampin, rifabutin, rifaximin
78
rifamycin mechanism of action
bind to DNA dependent RNA polymerase inhibiting RNA synthesis
79
rifamycin spectrum
gram pos: staphylococci, streptococci, c. diff, listeria gram neg: h flu, n meningitidis, h. pylori mycobacterium
80
clinical uses for rifamycins
rifampin: m. tuberculosis infection. adjunct in endocarditis. prophylaxis for n. meningitidis rifabutin: alternative to rifampin for MAC or tuberculosis rifaximin: hepactic encephalopathy, recurrent C. diff, traveler's diarrhea
81
isoniazid mechanism
inhibition of synthetic pathways of mycolic acid
82
pyrazinamide and ethambutol mechanisms of action
pyrazinamide: unknown ethambutol: inhibits arabinosyl transferase enzymes involved in biosynth of cell walls
83
bacterial anti-metabolite agents
trimethoprim-sulfamethoxazole (bactrim)
84
trimeth-sulfameth mechanism of action
sulfa: interferes with bacterial folic acid synth trimeth: inhibits dihydrofolic acid reduction to tetrahydrofolate
85
trimeth-sulfameth spectrum
gram pos: CA-MRSA, MSSA. not ideal for beta hemolytic strep. listeria Gram neg: enterobacteriaceae. toxoplasmosis, nocardia, pneumocystis. NO ANAEROBES
86
trimeth-sulfameth clinical uses
prophylaxis and treatment of pneumocystitis jiroveccii pneumonia. toxoplasmosis encephalitis. UTI. listeria meningitis. CA-MRSA

MS2 Unit 6 Pharm (9 decks)

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