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ABBEY MSII U6 > Pharm antimicrobials 2 > Flashcards

Pharm antimicrobials 2 Flashcards

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
Q

clinical use of aminoglycosides - what is it given with? why?

A

synergistic with cell-wall active agents for enterococcus infections (esp penicillins because they facilitate entry), cystic fibrosis (pseudomonas common infection)

26
Q

aminoglycosides side effects

A

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
Q

which aminoglycoside is toxic and is typically only used topically for skin infections?

A

neomycin

28
Q

which aminoglycoside has the broadest spectrum?

A

amikacin

29
Q

what are the tetracyclines?

A

-cycline

doxycycline, minocycline, tetracycline

30
Q

tetracycline mechanism

A

inhibits 30S ribsome - blocks access of tRNA anticodon to its codon

31
Q

tetracycline spectrum

A

gram + (s. pneumoniae, MRSA), very effective againast intracellular pathogens (mycoplasma, chlamydia, legionella, rickettsia) and mycobacteria

32
Q

what does tetracycline treat?

A

“the diseases soldiers get”

chlamydia, yickettsia, borrelia, m pneumonia, acne, tick borne illness

33
Q

how is doxycycline eliminated?

A

fecally - can be used in patients with renal failure

34
Q

tetracycline drug interaction

A

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
Q

tetracyclines side effects

A 
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
Q

mechanism of resistance to tetracyclines

A

efflux pump!

37
Q

tigecycline class

A

glycylcycline

38
Q

what is different about tigecycline (glycylcyclines)

A

9-glycl substitution enables it to overcomes two major types of resistance = efflux pumps and ribosomal protection

39
Q

tigecycline spectrum

A

broad spectrum (covers tetracycline plus resistant organism) includes MRSA, VRE, enterobacteriaceae!!, anaerobes

40
Q

what does tigecycline NOT have activity against?

A

pseudomonas

41
Q

tigecycline side effects

A

GI - significant nausea, vomiting, and diarrhea - transaminitis, increased mortality –> used in situations when alternative agents are not suitable

42
Q

what are the macrolides?

A

-THROMYCINs

azithromycin, clarithromycin, erythromycin

43
Q

macrolides mechanism of action

A

inhibit protein synthesis by blocking translocation (macroSLIDES) bind to 50S subunit - bacteriostatic

44
Q

macrolides spectrum

A

atypical pneumonias (mycoplasma, chlamydia, legionalla), gram + cocci (strep in patients allergic to penicillin), B pertussis

45
Q

macrolides side effects

A

well tolerated usually - MACRO: GI Motility issues, Arrhythmia with prolonged QT, Colestatic hepatitis, Rash, eOsinophilia

46
Q

macrolides drug interaction

A

increases serum concentration of theophylline, oral anticoagulants

47
Q

which macrolide has the least GI distress?

A

erythromycin

48
Q

clindamycin mechanism

A

binds to 50S subunit “A site” –> blocks peptide transfer (translocation) - bacteriostatic

49
Q

clindamycin spectrum

A

treats anaerobic infections ABOVE the diaphragm (bacteroides spp, clostridium perfringens)
also effective against invasive group A strep

50
Q

which drug is used ABOVE the diaphragm for anaerobic infections? BELOW?

A 
above = clindamycin
below = metronidazole
51
Q

clindamycin side effects

A

pseudomembranous colitis (C difficile overgrowth) because everything else was killed off, fever, diarrhea

52
Q

what are the oxazolidinones?

A

-ZOLID

linezolid, tedizolid

53
Q

oxazolidinones mechanism

A

inhibit protein synthesis by binding to 50S subunit and preventing formation of initiation complex

54
Q

oxazolidinones spectrum

A

gram + including MRSA and VRE

NO gram - and poor anaerobe

55
Q

oxazolidinones side effects

A

severe side effects if used for 2+ weeks - HEMATOLOGIC toxicity (bone marrow suppression with thrombocytopenia), peripheral neuropathy, SEROTONIN SYNDROME

56
Q

what drug interaction does oxazolidinones have?

A

Serotonin syndrome if used with MAOis and SSRIs

57
Q

how must tetracycline be taken?

A

with water and standing upright - cause pill esophagitis

ABBEY MSII U6 (18 decks)

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