miscellaneous abx Flashcards

1
Q

Vancomycin (Vancocin) administration/metabolism

A

IV (poor oral absorption)

  • widely distributed and does penetrate the CSF when the meninges are inflamed
  • 90% of vancomycin is eliminated by renal excretion, adjust dose with renal failure
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2
Q

Vancomycin (Vancocin) MOA

A

inhibits bacterial cell wall synthesis by binding to the D- alanyl-D-alanine portion of the peptidoglycan pentapeptide, bactericidal

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3
Q

how does resistance to Vancomycin develop?

A

bacterial enzymes that can induce alterations in the cell wall precursors so that vancomycin can’t bind as well
i.e. Vancomycin resistant enterococci replace D-alanyl-D- alanine with D-alanyl-D lactate or D-alanyl-D-serine

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4
Q

vanco spectrum

A

MRSA, MSSA, S. epidermidis, Streptococci, Corynebacterium diptheria, Clostridium spp. (the only anaerobe effective against)

NOT against G-s

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5
Q

vanco uses

A

serious staph infections
G+ infections in pts allergic to PCNs/cephs (tx w. aminoglycoside for synergism)
C. diff colitis (oral vanco)
staph meningitis in a PCN-allergic pt, if caused by S. pneumo include with a 3rd gen ceph

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6
Q

vanco SEs

A

-Ototoxicity and Nephrotoxicity: (rare)m ore common when given in combo with another ototoxic abx (i.e. amino glycoside)
-“Red man” or “Red Neck” syndrome – If vancomycin is infused too rapidly
is can cause flushing of the face, neck and torso due to histamine release.
minor: Injection site irritation, and chills and fever

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7
Q

Clindamycin (Cleocin)

A
  • oral and parental, distributed widely EXCEPT does not penetrate well into the CNS even with inflammation of the meninges
  • does have good abscess penetration
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8
Q

clindamycin MOA: similar to ??

A

imilar to erythromycin and chloramphenicol – binds to 50 S ribosomal subunit and inhibits bacterial protein synthesis; bacteriostatic

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9
Q

resistance to clindamycin develops how?

A
  • Mutations in the 50 S bacterial ribosomal subunit which prevents Clindamycin binding
  • Modification of the binding site by the enzyme methylase that prevent clindamycin binding
  • Enzymatic inactivation of clindamycin
  • Bac resistant to clindamycin are usually resistant to
    erythromycin. (similar mech)
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10
Q

clindamycin spectrum

A

most Staph aureus strains (has activity against some community acquired MRSA), Strept. Pneumoniae, but enterococci are resistant.

  • NOT useful against G- AEROBES
  • is active against G- and G+ anaerobes (B. fragilis and C. perfringens)
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11
Q

clindamycin uses

A
  • anaerobic infections (abscesses)- NOT brain abscesses
  • used in combo w. amino glycoside/ceph to tx deep wounds
  • *ppx against endocarditis in valvular heart dis. pts who are having dental procedures
  • alternative to PCN/ceph in allergic pts
  • PCP and toxoplasma gondii (+pyrimethamine) in AIDS pt
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12
Q

clindamycin SEs

A

C. diff-induced Pseudomembranous colitis (tx w. oral Vancomycin, Metronidazole, and Cholestyramine (not orally w. vanco: antagonistic effect)

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13
Q

Nitrofurantoin (Furadantin, Macrobid, Macrodantin)

A
  • Rapidly absorbed after oral admin, metabolized/excreted by glomerular filtration and tubular secretion (40% of free drug is found in the urine), often so quickly drug effects not seen!
  • don’t use in renal failure
  • reduced forms can damage DNA, both bactericidal and static
  • admin w. acidifying agent (more active @ pH
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14
Q

nitrofurantoin spectrum?

resistance development??

A
  • G+ and G- bac
  • NOT effective against Pseudomonas and many Proteus strains (resistant)
  • Bac resistance takes a long time to develop and there is no cross resistance with other abx
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15
Q

nitrofurantoin uses

A

-tx UTIS and for ppx for recurrent UTIs (used of UTIs caused by E. coli resistant to TMP-SMX and FQs)

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16
Q

nitrofurantoin SEs

A
  • GI: anorexia, N/V
  • hemolytic anemia (rare, seen in pts w. G6PD deficiency)
  • neurological, pulmonary fibrosis, chronic active hepatitis, allergic reactions
  • contraindicated in renal failure, caution w. preggos
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17
Q

Polymyxin B sulfate (generic) MOA

what does resistance involve?

A

interacts with cell membrane phospholipids, and disrupts cell membrane perm., and causing leakage of intracellular components, bactericidal
-Resistance may involve inability of the polymyxins to pass through the cell wall.

18
Q

polymyxin B spectrum

A

only susceptible G- bac (e.g. Enterobacter aerogenes, E. coli, Klebsiella pneumonia, H. influenzae, Acinetobacter baumannii, Pseudomonas aeuriginosa)

19
Q

polymyxin B uses

A

topical treatment of Infections of the eye, skin, mucous membranes, ear, wounds, burns (G-s)

  • used IV as alternative for drug-resistant resp. tract infections (HAP, HCAP, VAP) caused by DR-G-
  • septicemia, UTIs (IV, IM)
  • meningitis (typ. in combo)
  • irrigate the bladder to prevent bacteriuria/bacteremia assoc. w. indwelling catheters (used w. neomycin)
20
Q

polymyxin B SEs (both dose-dependent) (why polymyxins are reserved as alternate tx)

A
  • Neurotoxicity*: (facial flushing; dizziness that may progress to ataxia; mental confusion; nystagmus; muscle weakness; drowsiness; giddiness; peripheral paresthesia, visual disturbances, slurred speech, coma and seizures)
  • Nephrotoxicity*: (albuminuria, proteinuria, cylindruria, azotemia, inc. in serum creatinine (dec. in creatinine clearance), acute tubular necrosis, oliguria, hematuria, leukocyturia, and excessive excretion of e-lytes)
21
Q

Metronidazole (Flagyl)

A
  • oral, IV, rectal, topical (vag)
  • widely distributed, including the CNS and brain abscesses
  • crosses the placenta and appears in breast milk
  • metabolized in the liver and exreted by the kidneys
22
Q

metronidazole MOA

A

reduction of the drug to compounds that bind to intracellular macromolecules, bactericidal

23
Q

metronidazole spectrum

A
  • active against clindamycin-resistant B. fragilis (drug of choice in adults*)
  • bactericidal activity against Anaerobes (including bacteriodes fragilis)
  • NOT v. effective against Not very effective against G+ and G- AEROBES
24
Q

metronidazole uses

A
  • Anaerobic infections (soft tissue infection, intra-abdominal infections, pelvic infections, brain abscesses).
  • C. diff Pseudomembranous colitis
  • PUD caused by H. pylori (Triple therapy)
25
Q

metronidazole SEs

A
  • Carcinogenic potential, don’t use in pregnancy or in women during breast
  • Disulfiram-like interaction with alcohol.
26
Q

Bacitracin

A
  • opthalmic and dermatologic ointments

- not used much parenterally because of nephrotoxicity

27
Q

Bacitracin MOA

A
  • inhibits cell wall formation, interferes with the lipid that carries peptidoglycan subunits to the site of cell wall formation.
  • No cross resistance with other antimicrobials.
28
Q

Bacitracin spectrum

A

-similar spec. to PCN: G+ cocci and bacilli
-G-s such as Neisseria, H. influenzae; and the spirochete Treponema palladium
-

29
Q

Bacitracin uses

A

-topically for open wounds to eradicate mixed microorgs
-eye infections (e.g. conjunctivitis)
(may be used in combo, i.e.: bacitracin + polymyxin + neomycin)

30
Q

bacitracin SEs

A

Serious nephrotoxicity from parenteral use; renal failure due to tubular and glomerular necrosis.
-Hypersensitivity reactions from topical use are rare.

31
Q

Quinupristin/Dalfopristin (Synercid) used for ??

spectrum:

A

IV tx of bacteremia and other life threatening infections caused by vancomycin-resistant Enterococcus faecium, and complicated skin infections caused by S. aureus and Strep pyogenes (when resistant to other abx, or contraindicated due to allergy)
-Enterococcus faecium, MRSA/MSSA, S. epidermidis, PCN-susc. and resistant S. pneumo

32
Q

Quinupristin/Dalfopristin (Synercid) MOA

A

(similar to the macrolide)

  • inhibits bac protein synthesis by binding to the 50 S ribosomal subunit.
  • The two drugs bind to different sites on the 50 S ribosome and prevent the extrusion of new proteins which results in bacterial cell death.
33
Q

Quinupristin/Dalfopristin (Synercid) resistance occurs via ??

A

Modification of the quinupristin binding site on the 50S ribosomal subunit, enzymatic destruction of dalfopristin or efflux

34
Q

Quinupristin/Dalfopristin SEs

A
  • Erythema, pain, itching and burning at the site of infusion
  • Arthralgias/myalgias
  • inhibit CYP3A4
35
Q

Linezolid (Zyvox)

MOA?

A

Oral admin, Parenteral

Bacterial protein synthesis inhibitor by binding to the 50S bacterial ribosomal
subunit and prevents formation of the 70S translational initiation complex; Bactericidal for Streptococci with bacteriostatic activity against many other bac

36
Q

Linezolid Resistance in ?? and ?? is caused by ??

A

enterococci and staphylococci

point mutations in the 23S rRNA of the 50S subunit.

37
Q

Linezolid spectrum/uses

A

-Vanco-resistant Enterococcus facacium
-Nosocomial pneumonia or CAP due to S. aureus
or PCN-susc. Strep pneumo
-Skin/skin structure infections: MRSA and Strep Pyogenes

38
Q

Linezolid SEs

A

reversible inhibitor of monoamine oxidase (co-
admin with tyramine rich foods can result in HTN)
-N/V/D
-Thrombocytopenia
-oral formulation contains phenylalanine, avoid in PKUs
-C. diff-assoc. colitis

39
Q

Daptomycin (Cubicin)

A
  • poor oral absorption, admin IV
  • avoid IM due to musc. tox
  • 80% excreted in the urine, adjust dose if creatinine clearance is below 30 mL/min
40
Q

Daptomycin (Cubicin) MOA

A

concentration-dependent killing effect by binding to and depolarizing bacterial cell membranes which leads to loss of membrane potential, postassium efflux, and cell death.
-no known resistance mechs

41
Q

Daptomycin spectrum/uses

A
  • Bactericidal for aerobic, facultative and anaerobic G+ bac

- Complicated skin/skin structure infections caused by MRSA/MSSA, hemolytic streptococci, and vanco-susc. E. faecalis

42
Q

Daptomycin SEs

A

Skeletal muscle damage/Myopathy

Peripheral neuoropathy