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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
Q

telavancin mechanism of action

A

binds to cell wall precursors like vancomycin. depolarizes cell membrane. `

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26
Q

telavancin spectrum

A

vancomycin’s spectrum PLUS VISA, VRSA, some VRE isolates

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27
Q

telavancin clinical uses

A

SSTI, hospital acquired pneumonia. infrequently used.

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28
Q

telavancin side effects

A

nephrotox, more so than vancomycin. GI: n/v, metallic taste. potentially teratogenic.

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29
Q

dalbavancin mechanism of action

A

inhibition of cell wall precursors

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30
Q

dalbavancin spectrum

A

gram positive: MRSA, MSSA, strep, coag negative staph. NO GRAM NEGATIVE ACTIVITY. Anaerobes: c. perf, c. diff, prop. acnes, peptostrepto

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31
Q

oritavancin mechanism of action

A

inhibition of cell wall precursors, binds to pentaglycl bridging segment in peptidoglycan and inhibits transpeptidation. interaction and disruption of the cell membrane

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32
Q

oritavancin spectrum

A

similar to dalbavancin, but active against VRE.

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33
Q

dalbavancin and oritavancin clinical uses

A

SSTI, can be given in infusion centers (good for outpatient setting). very expensive though!!!

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34
Q

aminoglycoside agents

A

gentamicin, tobramycin, amikacin, streptomycin

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35
Q

aminoglycoside mechanism of action

A

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
Q

aminoglycoside mechanism of resistance

A

enzymatic modification, reduced uptake or decreased cell permeability, altered ribosome binding sites.

37
Q

aminoglycoside spectrum

A

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
Q

aminoglycoside clinical uses

A

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
Q

aminoglycosides side effects

A

nephrotoxicity. ototoxicity. neuromusular damage (rare)

40
Q

aminoglycoside pharmacokinetics

A

distributed extensively into urine. distribution into tissues

41
Q

aminoglycoside pharmacodynamics

A

concentration dependent. High peak is important!!! biphasic killing. higher the peak, the faster the killing.

42
Q

tetracycline agents

A

doxycycline, minocycline, tetracycline

43
Q

tetracycline mechanisms of action

A

passive diffusion through porins in gram-negative organisms. binds to 30S ribosomal subunit preventing protein synthesis

44
Q

tetracycline mechanisms of resistance

A

efflux pump. ribosomal protection (through dissociation of tet from ribosomal binding sites)

45
Q

tetracycline spectrum

A

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
Q

tetracycline clinical uses

A

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
Q

tetracycline side effects

A

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
Q

glycylcycline agent

A

tigecycline

49
Q

glycylcycline chemistry/mechanism of action

A

9-glycl substitution enables tigecycline to overcome two major types of resistance: efflux pumps and ribosomal protection

50
Q

tigecycline spectrum

A

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
Q

tigecycline clinical uses

A

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
Q

tigecycline side effects

A

GI: significant N/V and diarrhea.

Transaminitis. increased mortality.

53
Q

macrolide agents

A

azithromycin, clarithromycin, erythromycin.

54
Q

macrolide mechanism of action

A

reversible binding to 50S subunit of ribosome.

55
Q

macrolide mechanisms of resistance

A

decreased permeability in enterobacteriaceae. Alteration in the 50S receptor site. Alteration in the 23S ribosomal RNA of the 50S ribosomal subunit. Enzymatic inactivation

56
Q

macrolide spectrum

A

gram pos: s. pneumoniae, signif resistance in beta hemolytic strep. Gram neg: h. influenzae and m. catarrhalis.
Atypicals: legionella, chlamydia, mycoplasma
Anaerobes: actinomyces

57
Q

macrolides clinical uses

A

uncomplicated upper and lower respiratory tract infections. Mycobacterial infection. H. pylori in combo with other agents.

58
Q

macrolides side effects

A

GI: abdominal cramps, N/V, diarrhea. Thrombophlebitis with erythromycin. Cardiac: QT prolongation -> torsades de pointes

59
Q

what is the safest macrolide to use?

A

azithromycin! only has one interaction. much safer than the other macrolides

60
Q

clindamycin mechanism of action

A

binding to 50S ribosomal subunit preventing protein synth.

61
Q

clindamycin mechanisms of resistance

A

alteration in 23S ribosomal RNA of 50S ribosomal subunit. Alteration in 50S ribosomal proteins of the receptor site. Enzymatic inactivation

62
Q

clindamycin spectrum

A

gram pos: streptococci including group B strep. Staph aureus.
NO GRAM NEGATIVE ACTIVITY
Anaerobes: B. fragilis, clostridium, peptostreptococcus, fusobacterium, prevotella.
Toxoplasmosis, plasmodium falciparum

63
Q

clindamycin clinical uses

A

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
Q

clindamycin side effects

A

diarrhea, pseudomembranous colitis

65
Q

oxazolidinone agents

A

linezolid, tedizolid.

66
Q

oxazolidinone mechanism of action

A

binds to 23 S ribosomal RNA of the 50S subunit inhibiting protein synthesis

67
Q

linezolid and tedizolid spectrum

A

activity against gram-positives: staphylococci, enterococci, streptococci. NO GRAM NEGATIVE ACTIVITY. poor activity against anaerobes.

68
Q

linezolid and tedizolid clinical uses

A

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
Q

linezolid and tedizolid side effects

A

hematologic toxicity, reversible myelosuppression, mitochondrial toxicity, serotonin syndrome

70
Q

fluoroquinoline agents and mechanism of action

A

end in -floxacin. Inhibit DNA gyrase and inhibit topoisomerase IV

71
Q

fluoroquinolone spectrum

A

gram pos: s. aureus, s. pneumoniae, enterococcus (poor).
gram neg: enterobacteriaceae, h flu, p aeruginosa, atypicals.
mycobacterium
moxifloxicin has moderate activity against anaerobes

72
Q

fluoroquinolone clinical uses

A

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
Q

fluoroquinolone side effects

A

GI: mild
CNS: headache, dizziness, confusion
Tendinitis and tendon rupture rare.
QT prolongation

74
Q

metronidazole mechanisms of action

A

interacts with DNA to cause a loss of helical DNA structure and strand breakage resulting in inhibition of protein synthesis

75
Q

metronidazole antimicrobial spectrum

A

anaerobes: b. fragilis, clostridial species.

Protozoa

76
Q

metronidazole clinical uses

A

C. diff diarrhea. intra-abdominal infections. surgical prophylaxis in colon surgery. trichomoniasis.

77
Q

rifamycin agents

A

rifampin, rifabutin, rifaximin

78
Q

rifamycin mechanism of action

A

bind to DNA dependent RNA polymerase inhibiting RNA synthesis

79
Q

rifamycin spectrum

A

gram pos: staphylococci, streptococci, c. diff, listeria
gram neg: h flu, n meningitidis, h. pylori
mycobacterium

80
Q

clinical uses for rifamycins

A

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
Q

isoniazid mechanism

A

inhibition of synthetic pathways of mycolic acid

82
Q

pyrazinamide and ethambutol mechanisms of action

A

pyrazinamide: unknown
ethambutol: inhibits arabinosyl transferase enzymes involved in biosynth of cell walls

83
Q

bacterial anti-metabolite agents

A

trimethoprim-sulfamethoxazole (bactrim)

84
Q

trimeth-sulfameth mechanism of action

A

sulfa: interferes with bacterial folic acid synth
trimeth: inhibits dihydrofolic acid reduction to tetrahydrofolate

85
Q

trimeth-sulfameth spectrum

A

gram pos: CA-MRSA, MSSA. not ideal for beta hemolytic strep. listeria
Gram neg: enterobacteriaceae. toxoplasmosis, nocardia, pneumocystis. NO ANAEROBES

86
Q

trimeth-sulfameth clinical uses

A

prophylaxis and treatment of pneumocystitis jiroveccii pneumonia. toxoplasmosis encephalitis. UTI. listeria meningitis. CA-MRSA

MS2 Unit 6 Pharm (9 decks)

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