Pharm antimicrobials 2 Flashcards

(57 cards)

1
Q

vancomycin class

A

glycopeptide - cell wall synthesis inhibitor

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2
Q

vancomycin mechanism

A

binds rapidly and irreversibly to the D-alanyl-D-alanine group on the peptide side-chain of the membrane-bound precurosr; glycan chain extension, transpeptidation inhibited

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3
Q

vancomycin spectrum - why?

A

gram + only - molecule is HUUUUGGGGGEEEEE!!! can’t get into gram -

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4
Q

vancomycin clinical uses

A

serious, multidrug-resistant organisms including MRSA, s epidermidis, enterococcus, clostridium difficile

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5
Q

vancomycin adverse effects

A

well tolerated in general but NOT trouble free (Nephrotoxicity, Ototoxicity, Thrombophlebitis and red man syndrome)
Red man driving a van down the intestine getting c diff

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6
Q

vancomycin administration

A

IV only - not absorbed orally

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7
Q

what is the advantage of vancomycin not being absorbed orally?

A

c difficile is in gut - it doesn’t need to be absorbed to treat this

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8
Q

daptomycin class

A

cell wall TOXIN - lipopetide

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9
Q

daptomycin mechanism

A

penetrates gram + cell wall forming a channel for subsequent leakage of intracellular ions
-insertion into the gram + cell membrane causing depolarization and ultimate cell death

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10
Q

daptomycin spectrum

A

gram + cocci only - used for VRE and VRSA (vancomycin resistant organisms)

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11
Q

what is daptomycin not used for? why?

A

pneumonia because it avidly binds to and is inactivated by surfactant

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12
Q

daptomycin side effects

A

myopathy and rabdomyolysis,

also eosinophilic pneumonia

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13
Q

what are the lipoglycopeptides (analogs of vancomycin)

A

-vancins

dalbavancin, telavancin, oritavancin

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14
Q

-vancins mechanism

A

binds to same target as vancomycin (D-alanyl-D-alanine group on peptide side-chain of the membrane-bound precursor)–> cell wall precursor and inhibits transglycosylation

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15
Q

-vancins spectrum

A

similar to vancomycin (gram + only) but active against VRE and more anaerobe coverage

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16
Q

-vancins side effects

A

metallic taste, nausea, HA, nephrotoxicity, teratogenic (don’t take if preggers)
also very very expensive

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17
Q

what is the half life of the -vancins? what is the longer half life due to?

A

telavancin - 7.5 hr
dalbavancin and oritavancin long (100+ hrs)
-due to lipophilic side chain that prolongs half life

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18
Q

are protein synthesis inhibitors bacteriocidal or bacteriostatic?

A

bacteriostatic EXCEPT aminoglycosides

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19
Q

30 S ribosomal subunit protein synthesis inhibitors

A

ATG = DNA = small

aminoglycosides, tetracyclines, glycylcyclines

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20
Q

50S ribosomal subunti protein synthesis inhibitors

A

COM = bigger and better!

clindamycin, oxazolidinones, macrolides

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21
Q

what are the aminoglycosides?

A

gentamicin, tobramycin, amikacin, streptomycin

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22
Q

aminoglycoside mechanism

A

bactericidal: irreversible inhibition of initiation complex through binding of the 30S subunti - can cause misreading of mRNA - also inhibits initiation

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23
Q

aminoglycoside spectrum

A

extremely effective against G- rods (esp enterics)

covers pseudomonas aeruginosa!!

24
Q

what are aminoglycosides ineffective against? why?

A

anaerobes!! have O2 dependent uptake mechanism!!!

25
clinical use of aminoglycosides - what is it given with? why?
synergistic with cell-wall active agents for enterococcus infections (esp penicillins because they facilitate entry), cystic fibrosis (pseudomonas common infection)
26
aminoglycosides side effects
the MEAN GUY! (bacteriocidal) - punch to the ear (ototoxicity) - punch to the kidney (nephortoxicity) - punch a pregnant woman (teratogen) - knock them out (neuromuscular blockade)
27
which aminoglycoside is toxic and is typically only used topically for skin infections?
neomycin
28
which aminoglycoside has the broadest spectrum?
amikacin
29
what are the tetracyclines?
-cycline | doxycycline, minocycline, tetracycline
30
tetracycline mechanism
inhibits 30S ribsome - blocks access of tRNA anticodon to its codon
31
tetracycline spectrum
gram + (s. pneumoniae, MRSA), very effective againast intracellular pathogens (mycoplasma, chlamydia, legionella, rickettsia) and mycobacteria
32
what does tetracycline treat?
"the diseases soldiers get" | chlamydia, yickettsia, borrelia, m pneumonia, acne, tick borne illness
33
how is doxycycline eliminated?
fecally - can be used in patients with renal failure
34
tetracycline drug interaction
ORAL forms are chelated with divalent cations - don't take with milk (Ca), antacids (Ca, Mg), iron supplements because they can inhibit drug absorption in gut
35
tetracyclines side effects
``` think of soldier in night vision goggles GI distress (need to take with water and standing up);, discoloration of teeth and inhibition of bone growth in children, photosensitivity and hyperpigmentation ```
36
mechanism of resistance to tetracyclines
efflux pump!
37
tigecycline class
glycylcycline
38
what is different about tigecycline (glycylcyclines)
9-glycl substitution enables it to overcomes two major types of resistance = efflux pumps and ribosomal protection
39
tigecycline spectrum
broad spectrum (covers tetracycline plus resistant organism) includes MRSA, VRE, enterobacteriaceae!!, anaerobes
40
what does tigecycline NOT have activity against?
pseudomonas
41
tigecycline side effects
GI - significant nausea, vomiting, and diarrhea - transaminitis, increased mortality --> used in situations when alternative agents are not suitable
42
what are the macrolides?
-THROMYCINs | azithromycin, clarithromycin, erythromycin
43
macrolides mechanism of action
inhibit protein synthesis by blocking translocation (macroSLIDES) bind to 50S subunit - bacteriostatic
44
macrolides spectrum
atypical pneumonias (mycoplasma, chlamydia, legionalla), gram + cocci (strep in patients allergic to penicillin), B pertussis
45
macrolides side effects
well tolerated usually - MACRO: GI Motility issues, Arrhythmia with prolonged QT, Colestatic hepatitis, Rash, eOsinophilia
46
macrolides drug interaction
increases serum concentration of theophylline, oral anticoagulants
47
which macrolide has the least GI distress?
erythromycin
48
clindamycin mechanism
binds to 50S subunit "A site" --> blocks peptide transfer (translocation) - bacteriostatic
49
clindamycin spectrum
treats anaerobic infections ABOVE the diaphragm (bacteroides spp, clostridium perfringens) also effective against invasive group A strep
50
which drug is used ABOVE the diaphragm for anaerobic infections? BELOW?
``` above = clindamycin below = metronidazole ```
51
clindamycin side effects
pseudomembranous colitis (C difficile overgrowth) because everything else was killed off, fever, diarrhea
52
what are the oxazolidinones?
-ZOLID | linezolid, tedizolid
53
oxazolidinones mechanism
inhibit protein synthesis by binding to 50S subunit and preventing formation of initiation complex
54
oxazolidinones spectrum
gram + including MRSA and VRE | NO gram - and poor anaerobe
55
oxazolidinones side effects
severe side effects if used for 2+ weeks - HEMATOLOGIC toxicity (bone marrow suppression with thrombocytopenia), peripheral neuropathy, SEROTONIN SYNDROME
56
what drug interaction does oxazolidinones have?
Serotonin syndrome if used with MAOis and SSRIs
57
how must tetracycline be taken?
with water and standing upright - cause pill esophagitis