Antibiotics II Flashcards

1
Q

Tetracyclines

Protein Synthesis Inhibitors

A

DOXYCYCLINE
Tetracycline
Minocycline
Tigecycline

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2
Q

Aminoglycosides

Protein Synthesis Inhibitors

A

GENTAMYCIN
TOBRAMYCIN
Amikan
Streptomycin

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3
Q

Cloramphenicol

category?

A

(Protein Synthesis Inhibitors)

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4
Q

Antifolates

DNA Synthesis Inhibitors

A

SULFAMETHOXAZOLE (SMX)
TRIMETHOPRIM / SMX (Cotrimoxazole)
Dapsone

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5
Q

Fluoroquinolones

DNA Synthesis Inhibitors

A

CIPROFLOXACIN
LEVOFLOXACIN
MOXIFLOXACIN
Ofloxacin

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6
Q

(Urinary Tract Antisceptics)

A

Nitrofurantoin

Methenamine

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7
Q

How to initiate protein synthesis?

A

f-met tRNA = binds initiation factors and 30s + 50s

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8
Q

Protein synthesis inhibitors - 30s inhibitor

A

Buy AT 30, CCELL at 50.

Aminoglycosides [-cidal]
Tetracyclines [-static]

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9
Q

Protein synthesis inhibitors - 50s inhibitor

A

Buy AT 30, CCELL at 50.

Chloramphenicol, Clinda [-static]
Erythromycin [-static]
Lincomycin [-static]
Linezolid [variable]

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10
Q

Tetracyclines

[-static}
characteristics

A

*bacteria selective (no euk)
*binds reversibly to 30S
*blocks binding of amino-tRNA to A site
(can’t add aminos)
*gram +/-

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11
Q

Tetracyclines

resistance

A

*efflux (use DOXY, mino, tige)
*30S ribosome protection (use tige)
*Enzymatic inactivation (acetylation)
TIGECYCLINE -no cross resistance

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12
Q

Doxycycline PO/IV
Minocycline

(Tetracyclines)

A

low renal clearance

longer t1/2

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13
Q

Tigecycline IV

Tetracyclines

A
  • glycylcycline

* MDR organisms - MRSA, VRE, ESBL

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14
Q

Doxycycline

Tetracyclines
use

A

atypical pneumonia
NGU (chlamydia)
Rocky Mtn. Spotted Fever
Lyme Disease

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15
Q

Tetracyclines

[-static}
ADME

A
  • Ca, Mg, Fe, Al, food, divalent metals - down absorption
  • bones/teeth
  • Minocycline - CSF
  • non-renal elimination = Mino/doxy/Tige (SAFEST FOR kidney problems)
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16
Q

Tetracyclines

[-static}
Toxicities

A
  • gut microflora change
  • superinfection
  • Mino/doxy - vestibular dysfunction (up CNS penetration)
  • Outdated - renal tubular acidosis (fanconi syndrome)
  • grey teeth - no kids under 8 + pregger
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17
Q

Aminoglycosides

Mnemonic

A

Mean GNATS can NOT kill anaerobes

amino-, genta/neo/amikan/tobra/strepto
Nephro/oto-toxic, teratogen
need O2 - inner membrane transport

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18
Q

Aminoglycosides

MOA

A
  • binds 30s
  • slows proof-reading
  • more bacterial membrane permiability
  • OUT by kidney
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19
Q

Aminoglycosides

resistance

A
  • **Enzymatic inactivation
  • Impaired uptake
  • ribosomal protein mutation (strepto)
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20
Q

Aminoglycosides

efficacy

A

*-cidal
*irreversible
*works hours after cleared
*concentration-dependent killing
LOWER TOXICITY - 1x day (larger dose)

21
Q

Aminoglycoside

Specificity

A

*Aerobic Gram -ve enteric
(pseudomonas)
*Genta/Tobra - all Gram -, Pseudomonas (more tobra)

22
Q

Aminoglycosides

synergy

A

+ B-lactam/vanc
*thinner cell wall, more penetration
+ Pen/Vanc
*wall inhibitor (ALWAYS), more Rx in periplasmic space

23
Q

Aminoglycosides

ADME

A
  • doesn’t cross membrane, stays in plasma (use- sepsis!) + B lactam = up tissue levels
  • NO ORAL, use iv/im
  • Tobra - nebulized (Pseudomonas - cystic fibrosis)
24
Q

Aminoglycosides:

Toxicities

A

*oto/nephro-toxic
(renal impairment - monitor plasma after 3 doses)
*irreversible
*Vestibular damage

25
Q

Chloramphenicol

MOA

A
  • Binds 50s
  • stops peptidyltransferase
  • can affect eukaryotic ribosomes (stop aerobic metabolism)
26
Q

Chloramphenicol

ADME

A
  • Liver metab
  • Cyp 2C/3A inhibition
  • caution-infants/alcoholics (bad liver)
27
Q

Chloramphenicol

Toxicities

A
Hematological Effects:
• Bone marrow suppression
• Aplastic anemia
DON'T USE
• “Gray Baby Syndrome”
• Potential for Drug Interactions:
28
Q

Antifolates (TMP/SMX) block

A

folate synthesis of Nucleic Acids

29
Q

SMX targets

Antifolates

A

PABA , block folate production (bacteria only–mammals have dietary folate)
*dihydropteroate synthase

30
Q

TMP targets

Antifolates

A

Folate (bacteria + humans)

  • Dihydrofolate Reductase
  • bacteria selective - HUGE dose needed for human
31
Q

Sulfonamides SMX

Antifolates
resistance

A
  • Impaired uptake, increased efflux
  • dihydropteroate synthase mutation
  • up PABA synthesis
32
Q

Sulfonamides SMX

Antifolates
characteristics

A
  • water insolubule
  • -static alone, -cidal w/ TMP
  • for select Gram +/-
33
Q

Cotrimoxazole (SMX/TMP PO)

Antifolates
use

A

UTI/prostatitis

Otitis/Sinusitis

34
Q

Dapson

Antifolates
Use

A

leprosy

35
Q

Sulfonamides SMX

Antifolates
ADME

A
  • CNS and CSF (fetus)
  • Hepatic metabolism
  • urine excretion (watch renal failure!)
  • acidic urine - crystalluria (so hydrate patient)
36
Q

Sulfonamides SMX

Antifolates
Adverse Effects

A

• Hypersensitivity
• Hematopoietic Toxicity
• urine Crystallization (give with fluids)
• bilirubin displacement (bind albumin)
NO w/ newborns, pregger - yellow baby, kernicterus

37
Q

Fluoroquinolones

MOA

A
  • stop DNA gyrase

* stop Topoisomerase IV (gram +)

38
Q

Fluoroquinolones

resistance

A
  • DNA gyrase/topoisomerase IV mutation
  • more efflux
  • less influx
39
Q

Fluoroquinolones

use against

A
  • Gram +/-

* concentration-dependent killing

40
Q

Ciprofloxacin

Fluoroquinolones
use against

A

Gram (-) rod

  • Complicated UTI (no longer 1st line)
  • Traveler’s diarrhea
  • anthrax
41
Q

Levafloxacin +Moxifloxacin

Fluoroquinolones
use against

A

Gram (-) rod + cocci

  • **S. PNEUMONIA
  • S. aureus (MSSA)
  • Legionella, chlamydia
  • **TB
  • some anaerobes
42
Q

Fluoroquinolones

ADME

A
  • ANTACIDS (Ca, Fe, Mg, Al) - LESS absorption
  • most URINE
  • Moxifloxacin - HEPATIC
43
Q

Fluoroquinolones

toxicities

A
  • GI toxicity (nausea, vomiting), dizziness, headache, rash
  • Cartilage
  • Tendonitis/rupture
  • acute psychosis
  • NO w/ NSAIDS - CNS effects (gaba-a)
  • QT prolongation (levo/moxi)
  • NO children, pregnant
44
Q

Acute uncomplicated Pyelonephritis

Rx 1st line

A

Cipro

TMP/SMX

45
Q

Urinary Tract Antiseptics

characteristics

A

*poorly absorbed

46
Q

Nitrofurantoin

Urinary Tract Antiseptics

A
  • UTI
  • bacterio-selective
  • MOA - free radical damage
  • NO preg/baby/renal dx
  • brown pee
47
Q

Methenamine
(1859)

(Urinary Tract Antiseptics)

A
  • less UTI activity than Nitro
  • need low pH - acidify urine
  • MOA - make formaldehyde, cross-link to proteins
  • resistance rare
48
Q

Acute Uncomplicated Cystitis

Rx 1st line

A

TMP/SMX

Nitrofurantoin