PHARM: Antibiotics Flashcards

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1
Q

What is the MOA of daptomycin?

CIDAL or STATIC?

A

Rapidly disrupts bacterial cell membranes (results in depolarization and loss of membrane potential and K+ efflux)–BACTERICIDAL

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2
Q

What are the mechanisms of resistance to daptomycin?

A

none are identified

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3
Q

What is the ROA of daptomycin?

A

IV indusion once a day after hemodialysis

NOT IM–direct muscle toxicity

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4
Q

What type of metabolism does daptomycin undergo?

A

primary (bound to serum albumin)

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5
Q

How is daptomycin eliminated?

A

Renal elimination (dose adjust for renal toxicity)

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6
Q

What are the adverse effects of daptomycin?

A

Muscle pain and weakness

monitor for development due to serum creatinine phosphokinase elevations

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7
Q

What drugs does daptomycin have DDIs with?

A

statins (if co-administered)

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8
Q

What are the therapeutic uses of daptomycin?

A
  • Aerobic G(+) Bacteria
  • Multidrug-resistant strains of staph, strep, and enterococcus
  • Complicated skin and soft tissue infections
  • MSSA and MRSA bacteremia
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9
Q

What type of infection is daptomycin unable to treat?

A

pneumonia (inactivated by surfactant)

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10
Q

What is the MOA of linezolid?

STATIC or CIDAL?

A

Binds to the 23S RNA on 50S ribosomal subunit to inhibit protein synthesis

STATIC with staph and enterococci

CIDAL with strep

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11
Q

What are the mechanisms of resistance to linezolid?

A

-Point mutation in 23S RNA

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12
Q

What are the indications for linezolid?

A
  • MRSA
  • Resistnat staph epi
  • Enterococcus faecium and faecalis
  • Serious VRE infections**
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13
Q

What is the ROA of linezolid?

A

Oral and Parenteral

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14
Q

How does food intake alter linezolid metabolism?

A

delays absorption but not peak drug levels

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15
Q

How is linezolid metabolized?

A

Non-enzymatic oxication

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16
Q

How is linezolid eliminated?

A

Non-renal and renal mechanisms (no dose adjustment needed in patients with renal deficiency or mild/moderate liver failure)

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17
Q

What are the AEs of linezolid?

A
  • Diarrhea
  • Headache
  • Nausea/vomiting
  • Myeosuppression (if therapy > 2 weeks)- with optic and peripheral neuropathy
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18
Q

What chemical is contained within the oral suspension of linezolid?

A

aspartame

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19
Q

Describe the basis for DDIs with linezolid?

A

Linezolid is a non-selective inhibitor of monoamine oxidase (caution with co-administration of drugs metabolized by MAO like PE, SSRIs, etc.)

HTN can occur from decreased breakdown of tyramine

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20
Q

List 2 streptogramins.

A

Dalfopristin

Quinupristin

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21
Q

How are streptogramins administred?

A

IV administration in a 70:30 combination of the two types

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22
Q

What is the MOA Of streptogramins?

A

protein synthesis inhibition (bind to ribosome peptidyltransferase domain to inhibit tRNA synthetase and block AA addition to peptide chain)

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23
Q

Are streptogramins bacteriostatic or bacteriocidal?

A

Synergistic bactericidal combination (but static when given alone)

24
Q

What are mechanisms of resistance to streptogramins?

A
  • Changes in 23S ribosomal target site

- Constitutive expression of “erm” gene encoding MLSb phenotype

25
Q

How are streptogramins metabolized?

A

Hepatic metabolism via conjugation via CYP3A4

26
Q

How are streptogramins excreted?

A

Biliary excretion

27
Q

What are the adverse effects of streptogramins?

A
  • Thrombophlebitis/pain at infusion site
  • Increase in conjugated bilirubin (and liver enzymes)
  • Joint or muscle pain (most often in people with CLD)
  • CYP450 inhibitor
28
Q

What are the indications for streptogramins?

A
  • G(+) bacteria except for E. faecalis
  • VRE infections
  • SSSI from MRSA or strep pyogenes
  • Bone infections due to VRE and MRSA
29
Q

What is the MOA of Glycylcycline/Tigecycline?

STATIC or CIDAL

A

Inhibition of protein translation by binding to 30S subunit

Bacteriostatic

30
Q

What are mechanisms of resistance to Glycylcycline/Tigecycline?

A

Trick question- it overcomes many of the resistance to tetracyclines by having high affinity binding at additional ribosomal sites and NOT being expelled by efflux pumps

31
Q

What is the ROA of Glycylcycline/Tigecycline?

A

IV infusion (slow)

32
Q

How is Glycylcycline/Tigecycline distributed?

A

extensively beyond plasma nad into tissues

33
Q

How is Glycylcycline/Tigecycline metabolized?

A

Very little metabolism (long half life)

Need to dose adjust for impaired liver function

34
Q

How is Glycylcycline/Tigecycline excreted?

A

Biliary/fecal AND renal

35
Q

What are the adverse effects of Tigecycline?

A
  • Diarrhea, N/V
  • Injection site RXN
  • Possible hepatic and pancreatic toxicity
  • Affects teeth and bones
  • Sunlight sensitivity
36
Q

What are the therapeutic uses of Tigecycline?

A
  • Broad spectrum- G(+), G(-), anaerobes, MRSA
  • NO activity against Pseudomonas or proteus
  • NOT for under 18 y/o
37
Q

Other than Tb, what is rifampin used for?

A
  • MRSA and Staph. Epi
  • Prophylactically for people exposed to meningitis caused by meningococci or H. Flu
  • Eradication of staphlococcus in nasal carriers
  • Anti-leprosy
38
Q

What is rifampin commonly given with when it is not being used to treat Tb?

A

Beta-lactam or vancomycin

39
Q

What is the MOA of clindamycin?

A

INhibition of protein synthesis (binds to 50s subunit of ribosome)

40
Q

Should clindamycin be given with erythromycin?

A

NO- binding sites are very clost and render one another ineffective

41
Q

What are the mechanisms of resistance to clindamycin?

A
  • Slowly occurring

- Decreased affinity of drug for ribosome (methylation of “erm”-encoded genes)

42
Q

What are the therapeutic uses of clindamycin?

A
  • Effective for G(+) and G(-) anaerobes
  • MRSA, G.A.S.
  • Bacteroides fragilis (outside CNS)
43
Q

How is clindamycin absorbed?

A
  • Rapid and almost complete oral absorption
  • Rate inhibited by food
  • Acid stable
44
Q

Can clindamycin penetrate the CSF or placenta?

A

CANNOT penetrate CSF or intracellular

CAN penetrate bone, abscesses, placenta, breast milk

45
Q

How is clindamycin metabolized?

A

Liver metabolized (dose adjust for liver failure)

46
Q

How is clindamycin excreted?

A

Bile and urine

47
Q

What are the AEs of clindamycin?

A
  • Pseudomembranous colitis from C. diff (treat with metronidazole or vancomycin)
  • GI problems
  • Hypersensitivity rashes
48
Q

What is the MOA of mupirocin?

STATIC or CIDAL

A

Binds reversible to staphylococcal isoleucyl tRNA synthetase to inhibit protein and RNA synthesis

Depends on concentration

49
Q

How is mupirocin administered?

A

topically (ointment with polyethylene glycol)

50
Q

What are the indications for mupirocin?

A
  • Impetigo (staph, strep, MRSA)

- Eliminate MRSA carriage by patients/health care workers

51
Q

Does mupirocin get absorbed systemically?

A

NO- quickly inactivated upon absorption

52
Q

What is the MOA of bacitracin?

A

inhibits movement of peptidoglycan building blocks of cell wall from inside to outside the cell membrane by inhibiting dephosphorylation of the isoprenyl pyrophosphate carrier protein

53
Q

What are the therapeutic indications fro bacitracin?

A

G(+) cocci and bacilli

54
Q

What is the ROA of bacitracin?

A

Topically (in ointment with neomycin and polymyxin B)

55
Q

What are the AEs of bacitracin?

A

Severe nephrotoxicity with parenteral use