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PHARM ORAL 2021 > Antimicrobials > Flashcards

Antimicrobials Flashcards

1
Q

ampicillin: class + use

A
  • class
    • broad spectrum, beta lactam ABX
    • 2nd generation penicillin
  • use
    • GI/GU
    • dental
    • endocarditis prophylaxis
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2
Q

ampicillin: MOA

A
  • Bactericidal
  • Binds to penicillin binding protein (PBP)
  • activates autolysins → enzymatic destruction of cell wall
  • inhibit enzyme (transpeptidases) needed for cell wall synthesis and integrity
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3
Q

ampicillin: PK

A
  • E1/2t: 2 hrs (can be up to 20 hrs in RF)
  • PB: 20%
  • Elimination: excreted 90% unchanged in the urine
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4
Q

ampicillin: SE

A
  • highest incidence of rash among penicillins (7-10 days after therapy) - mostly due to impurities in the commmercial preparation of the drug and not true allergic reaction to drug
  • anaphylaxis
  • diarrhea, GI upset
  • drug induced SLE
  • interstitial nephritis
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5
Q

ampicillin: cautions/contraindications

A
  • hypersensitivity to PCN; consider cross reactivity w/ cephalosporins
  • may potentiates warfarin
  • ↓ dose in RF
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6
Q

ampicillin: dose

A
  • 2 grams IV 30 min preop: administer over 10-15 minutes (rapid infusion can cause seizures)
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7
Q

cefazolin (ancef): class + use

A
  • class
    • Broad-spectrum, ß lactam ABX
    • 1st generation cephalosporin
  • use
    • SSI prophylaxis in CV, ortho, biliary, pelvic, intraabdominal (favorable therapeutic index)
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8
Q

cefazolin: MOA

A
  • bactericidal
  • binds to penicillin binding protein (PBP)
  • activates autolysins → enzymatic destruction of cell wall
  • inhibits enzyme (transpeptidases) needed for cell wall synthesis and integrity
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9
Q

cefazolin: PK

A
  • E ½ life: 2 hrs
  • PB: 80% (high)
  • Excretion: 80-100% unchanged in urine
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10
Q

cefazolin: SE

A
  • ***favorable therapeutic index*** (low toxicity, highly effective)
  • Hypersensitivity
  • anaphylaxis (1% - 2% cross reactivity with PCN allergy)
  • Superinfection (C. diff)
  • Thrombophlebitis @ IV site (uncommon)
  • Hemolytic anemia (very rare)
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11
Q

cefazolin: cautions/drug interactions

A
  • CAUTIONS
    • hypersensitivity
      • cross reactivity with penicillin (1-2%) and other cephalosporins
    • renal failure → dose adjust
    • crosses placenta
  • drug interactions
    • ETOH use (if going home with prescription) → disulfiram like reaction
    • Probenecid (gout drug) → prolong DOA
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12
Q

cefazolin: dose

A
  • 1-2 grams IV 30 min preop, ↓ dose in RF
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13
Q

gentamycin: class + use

A
  • class
    • broad-spectrum aminoglycoside ABX
  • use
    • pleural, ascitic, synovial infections
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14
Q

gentamycin: MOA

A
  • bactericidal
  • works on 30s ribosomal subunit
  • blocks the initiation of protein synthesis/premature termination of protein synthesis/abnormal protein formation in bacterial cells
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15
Q

gentamycin: PK

A
  • E1/2t: 2 – 3 hrs (20-40 fold ↑ in RF)
  • Very positively charged
  • PB: < 30% (poor)
  • Elimination: almost 100% renal excretion unchanged
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16
Q

gentamycin: SE

A
  • limited by their toxicity
  • ototoxicity (especially w/ diuretics → furosemide, mannitol)
    • drug tends to concentrate around ear
  • nephrotoxicity (especially w/ ampho B, cyclosporine, etacrynic acid, vancomycin, NSAIDS)
    • drug tends to concentrate around kidney
  • skeletal muscle weakness: inhibit the pre junctional release of Ach and ↓ post synaptic sensitivity to the neurotransmitter (impacts patients with NM pathology i.e., MG) → profound blockade with NDNMB
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17
Q

gentamycin: cautions/contraindications/drug interactions

A
  • CAUTIONS
    • hypersensitivity
    • ↓ dose in RF
    • vestibulocochlear impairment
    • caution in pts w/ muscle weakness & MG
    • ↑ nephrotoxic potential of other drugs such as loop diuretics, NSAID’s & other abx
    • Crosses the placenta → could cause harm to fetus (ototoxicity, nephrotoxicity)
  • DRUG INTERACTION
    • ​IV admin associated with potentiation of NDNMB (usually reversible with calcium and neostigmine)
18
Q

gentamycin: dose

A
  • 60-120 mg IV
  • toxic levels @ >9 mcg/ml – monitor levels
19
Q

clindamycin: class + use

A
  • class
    • Linomycin antibiotic
  • use
    • commonly used in female GU surgeries
    • SSI prophylaxis with true anaphylactic PCN allergy
20
Q

clindamycin: MOA

A
  • usually bacteriostatic
  • blocks protein synthesis by binding to 50S ribosomal subunit
21
Q

clindamycin: PK

A
  • Peak: 60 min
  • E ½ t: 2.5 hours
  • Metabolism: primarily hepatic
  • Elimination: 10% excreted unchanged in urine
22
Q

clindamycin: SE

A
  • Diarrhea (related or unrelated to pseudomembranous colitis due to C diff infection)
  • Skin rash/hypersensitivity
  • Prolonged pre and post junctional effects at NMJ in the* *absence of NDMR → not antagonized with anticholinesterases or calcium
  • Blood dyscrasias (eosinophilia, leukopenia, thrombocytopenia)
23
Q

clindamycin: cautions/contraindications

A
  • Severe liver disease – DOSE DECREASE
  • Concurrent administration with NDMR can produce long lasting, profound neuromuscular blockade
    • not antagonized with anticholinesterases or calcium
24
Q

clindamycin: dose

A

600 mg IV preop

25
Q

vancomycin: class + use

A
  • class
    • broad-spectrum, glycopeptide antibiotic
    • Gram + only
    • narrow spectrum
  • use
    • activity against MRSA
    • severe C diff infection
    • good choice in severe PCN allergy patients
    • severe staph infections
    • streptococcal, enterococcal endocarditis
    • cardiac/orthopedic procedures using prosthetic devices
    • CSF and shunt related infections
26
Q

vancomycin: MOA

A
  • bactericidal – “slowly” cidal
  • inhibits bacterial wall synthesis = cell lysis & death
  • binds and inactivates cell wall precursors = “don’t have the building blocks”
27
Q

vancomycin: PK

A
  • Peak: 60 min
  • E ½ time: 6 hours (up to 9 days with RF patients)
  • PB: 50%
  • Very poor absorption upon oral admin (PO only for intestinal infection)
  • Slow CSF penetration unless there is meningeal inflammation
  • Elimination: 90% unchanged in urine
28
Q

vancomycin: SE

A
  • **narrow therapeutic index**
  • Thrombophlebitis
  • Ototoxicity @ conc > 30 mcg/ml AND nephrotoxicity (increased risk if giving with aminoglycosides)
  • Hypersensitivity (maculopapular skin rash)
  • Severe hypotension and “Red man syndrome” (flushing due to histamine release) if given IV in less than 30 minutes
  • diarrhea, GI upset
  • thrombocytopenia (rare)
29
Q

vancomycin: cautions/drug interactions

A
  • Cautions
    • hypersensitivity
    • hearing loss
    • renal failure (dose adjust)
  • Drug Interactions
    • Other nephrotoxic drugs: Toradol, NSAIDS, Ampho B, contrast dye, cyclosplorine
    • Synergistic action with aminoglycosides (vanc increases access of aminoglycosides to actual site of action → aminoglycosides then inhibit 30s ribosomal subunit) → HOWEVER, can also cause additive toxicity
30
Q

vancomycin: dose

A
  • 1 gram in 250 ml SLOWLY over 60 min
  • 10 – 15 mg/kg SLOWLY over 60 minutes
31
Q

metronidazole (flagyl): class + use

A
  • class
    • synthetic antibiotic
  • use
    • **recommended for pre-op prophylaxis for colorectal surgery**
    • endocarditis
    • pseudomembranous colitis (C diff)
    • abdominal and pelvic sepsis
    • CNS infections
    • anaerobic gram-negative bacilli & clostridium
32
Q

metronidazole: MOA

A
  • bactericidal
  • broken down & activated by anaerobic organisms & form cytotoxic compounds that bind to bacteria & damage it
33
Q

metronidazole: PK

A
  • E ½ t: 8 hours
  • PB: <20%
  • Absorption: well absorbed orally and widely distributed in tissue including CNS
  • Metabolism: 30-60% in liver
  • Elimination: 70% excreted in the urine & 6-15% fecal elimination
34
Q

metronidazole: SE

A
  • Dry mouth
  • Metallic taste
  • Nausea
  • seizures
  • Rare: neuropathy and pancreatitis
35
Q

metronidazole: cautions/contraindications

A
  • Avoid alcohol – disulfuram like reactions
  • Seizure history
36
Q

metronidazole: dose

A

500 mg IV over 10-20 min

37
Q

ciprofloxacin: class + use

A
  • CLASS
    • broad-spectrum, fluoroquinolone antibiotic
  • USE
    • complicated GI/GU
    • variety of systemic infections including resp. tract, TB, anthrax
38
Q

ciprofloxacin: MOA

A
  • bactericidal
  • inhibits DNA gyrase and topoisomerase, which are critical bacterial enzymes used in DNA replication & cell division (stops growth and proliferation)
39
Q

ciprofloxacin: PK

A
  • PB: 30%
  • Vd: 2.5 L/kg
  • E ½ time: 3 – 8 hours
  • Absorption: GI absorption rapid and penetration to body fluids and tissues is excellent
  • Metabolism: CYP450 metabolism in the liver
  • Elimination:
    • 30% excreted in the feces
    • 50% excreted unchanged in the urine (dose adjust RF)
40
Q

ciprofloxacin: SE

A
  • Class warning for QT prolongation
  • Rashes
  • Phototoxicity (severe sunburn)
  • Nausea
  • CNS disturbances
  • C diff superinfection, opportunistic candida
  • Tendinitis and Achilles tendon rupture due to extracellular cartilage matrix weakening
    • Highest risk: >65, corticosteroid use, s/p transplant
    • Avoid IV form <18 years old → rare, but can cause disability because they’re still growing
41
Q

ciprofloxacin: cautions/contraindications/drug interactions

A
  • cautions
    • decrease dose in renal dysfunction
    • caution with MG → muscle weakness
  • contraindications
    • b/c of tendinitis and achilles tendon rupture:
      • avoid IV form < 18 yo
      • age > 65
      • corticosteroid use
      • s/p transplant
  • Drug Interactions
    • ​CYP450 interactions (↑ levels of theophylline, warfarin and tinidazole)
42
Q

ciprofloxacin: dose

A

200-400 mg IV over 60 min

PHARM ORAL 2021 (9 decks)

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