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Pharmacology > ID: protein synthesis inhibitors > Flashcards

ID: protein synthesis inhibitors Flashcards

1
Q

Jarish-Herxheimer rxn

A

is a transient clinical phenomenon that occurs in patients infected by spirochetes who undergo antibiotic treatment. The reaction occurs within 24 hours of antibiotic treatment of spirochete infections, including syphilis, leptospirosis, Lyme disease, and relapsing fever.

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2
Q

which is Quinupristin/Dalfopristin effective against:

  • E. Faecalis
  • E. Faecium
A

E. Faecium

**VRE

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3
Q

Aminoglycosides (5)

-list them

A

Amikacin

Gentamycin

Neomycin

Streptomycin

Tobramycin

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4
Q

resistance to tetracyclines?

A

develops by decreasing accumulation of the drug rather than altering chemical structure
**use of efflux pumps–>decreasing influx

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5
Q

Clindamycin

  • MOA
  • spectrum
  • cidal or static?
  • resistance?
  • indication
  • kinetics (abs, penetration, met, drug-drug, pregnancy/BF?)
  • adv rxn
A

MOA: binds to the 50S subunit–inhib protein synthesis–can potentiate phagocytosis of bacteria by opsonization
*similar to macrolides

  • Bacteriostatic
  • Bacteriocidal against some staph (toxin prod staph and MRSA), strep, anaerobes

Spectrum: NOT effective for most gram(-)s

  • *has post-antibiotic effect
  • *used for Gram+ infections–MRSA, streotococcus, anaerobes

-resistance is similar to Erythromycin

Kincetics:

  • abs: good after PO
  • Penetrates well into bone, poorly into CNS
  • metabolized by CYP3A4
  • Rifampin reduces levels of clinda

OK with pregnancy and BF

SE:

  • PO use is limited due to diarrhea
  • –diarrhea is possible up to 20%: Possible C. Diff/pseudomembranous colitis
  • skin rash
  • caution with neuromuscular blocking agents
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6
Q

which macrolides are ok to use in pregnancy

-which not ok?

A

Erythromycin
Azithromycin

Clarithromycin– cat C

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7
Q

Fidamoxin
-drug class

  • moa
  • Spectrum
  • Abs
A

considered macrolide

MOA: termintes protein synthesis and causes cel death

narrow spectrum: gram+ aerobes and anaerobes

NOT well abs…..so IND is C. Diff

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8
Q

list the abx that MOA target 50S subunit

A 
Macrolides 
Clindamycin 
Linezolid 
Chloramphenicol 
Streptogramins
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9
Q

Doxycyline
DOC for?
abs?
advantages compared to the other tetracyclines

A
  1. Chlamydia spp
  2. Mycoplasma pneumoniae
  3. Lyme Dz ****
  4. rocky mt spotted fever
  5. vibrio cholerae

Abs:
*ok with or w/o food

advantages

  1. twice daily dosing
  2. IV, Po and ok to take with food
  3. less likely to cause photosensitivity
  4. onlny tretracycline to be used in kids <8 because it does not bind to Ca as well
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10
Q

Streptomycin indications

A
  1. M. TB–active
  2. Plague
  3. Tularemia
  4. Brucellosis
  5. endocarditis
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11
Q

do aminoglycosides cross placenta?

A

YES

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12
Q

Clarithromycin

-which pathogens

A 
Legionella 
Moraxella 
H. Pylori 
Ureaplasma 
Mycoplasma pneumoniae **** FIRST LINE
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13
Q

erythromycin

-abs

A

poor abs after PO bc it is destroyed by stomach acid

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14
Q

MOA for macrolides

A

Bind irreversible to the 50S unit

  • -inhib protein synthesis
  • bacteriostatic BUT high doses=bactericidal

*can have some anti-inflammatory effects…. prevention of CF exacerbations

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15
Q

bacteria need ___ to survive

A

protein

*they synthesize it

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16
Q 
Lincosamide 
drug(s) in this class? -routes
A

Clindamycin
PO
IV
topical

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17
Q

tetracyclines are avoided in ____ trimester and contraindicated in ___trimester

A

avoid in 1st

contraindicated 2nd/3rd

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18
Q

SE macrolides (4)

A
  1. GI distress/motility
  2. Cholestatic jaundice
  3. Ototoxicity
  4. Prolonged QTc
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19
Q

Chloramphenicol

  • when do we use
  • moa
  • spectrum
  • route
  • abs
  • penetration
  • dose adjustments
  • pregnancy/BF?
  • adv rxn
A

ABX of LAST resort for LIFE THREATENING infections

*CHLOROX… CHLORamphenicol

MOA:
*binds irreversibly to 50s

  • broad spectrum
  • spirochetes
  • chlamydia
  • rickettsia
  • anaerobes

IV— wide distribution

  • yes CNS pen
  • liver dysfunction– needs dose adjustment
  • contra: BF

YES IN PREGNANCY !

ADV RXN:
1. blood dyscrasias and risk of irreversible bone marrow suppression** BBW for the bone marrow suppresion****

  1. gray baby syndrome in neonates
  2. many drug-drug interactions due to inhibition of liver metabolizers (warfarin, phenytoin)
20
Q

which macrolides do you take without food

A

Erythromycin

Azithromycin

21
Q

list the abx that MOA target 30S subunit

A

tetracyclines
aminoglycosides–erythromycin
gentamycin, tobramycin
streptomycin

22
Q

name the new tetracyclines and routes

A

Eravacycline–IV–intraabdominal infections

Omadcycline–PO, IV—CAP, MSSA, MRSA

Sarecycline–PO—mod to sev acne in 9YO+

23
Q

Tetracyclines

  • list them and routes
  • moa
  • spectrum
  • not tx for?
  • abs–what can decrease it
  • which drug chelates the most
  • doisng? which drug in particular
  • drug-drug interactions
  • contra
A

tetracycline–PO
Minocycline–IV/PO
Doxycycline–IV/PO

MOA:

  • enter bacteria by both passive diffusion or active transport and [ ] intracellularlly in organisms
  • reversibly bind to 30S subunit of bacterial ribosome—inhib protein synthesis
  • bacteriostatic

Spectrum:

  • broad spectrum VERY
  • Aerobic gram+
  • Aerobic gram-
  • atypical pathogens: protoza, spirochetes, mycobacteria,

not tx for N. gonorrhoeae due to resistance

Absoprtion:

  • adequate
  • decreased by: dairy products, iron, aluminum, ca, magnesium

tetracycline chelates the most

doxycycline requires adjustment for severe hepatic dysfunciton

AVOID w. PCN

contra: kids under 8, pregnant (yes crosses placenta)
* doxycycline in special cases when benefits outweight the risk– can be used in preg and kids– bc it is not teratogeneic and does not cause dental staining

24
Q

aminoglycosides are generally combined with which other ABX?
-why?

A

beta-lactams

*synergy against serious gram+ infections

25
Q

Erythromycin

  • specturm
  • simialr to?
A

similar to PCN G—- alternative if PCN allergy**

spectrum:
* gram+ —– strep, corynebacterium

26
Q

are aminoglycosides generally used as monotherapy?

A

no

NEVER monotherapy for Gram+

27
Q

Linezolid and Tedizolid

  • drug class?
  • routes
  • cidal or static
  • spectrum
  • indications
  • abs
  • distribution
  • dosing adjustents?
  • adv rxn
A

Oxazolidinones

  • Linezolid (PO, IV)
  • Tedizolid (IV, PO)
  • bacteriostatic
  • Linezolid bactericidal to streptococci

spectrum:
* Mainly used for resistant gram+ infections–MRSA, VRE
* other: corynebacterium, Bacillus, Listeria, MSSA, coag. neg S aurea

INDS: not first line bc they are bacteriostatic
*gram+ infeections that are resistant
**MRSA
***VRE
Tedizolid: limited to use in skin infections for PTs 12+ YO\
*Linezolid is alternative to daptomycin

ABS: 100% after PO
distribution: yes penetrates CNS, bone, alveoli, is bound to serum proteins

No renal or hepatic dose adjustments*

adv rxn:
1. MC: GI upset, HA, rash
2. myelosuppression
3. Peripheral or otic neuropathy (can be irreversible)
4. Serotonin syndrome if given with SSRIs, SNRIs, MAOIs Bupropion
5. Lactic Acidosis with prolonged used*
WHY WE WANT TO AVOID LONG TERM USE*****

28
Q

Aminoglycosides
-drugs?
-routes
MOA

spectrum (not effective for?)

  • synergistic with?
  • indications
A

-mycin
except for Amikacin

IV ONLY*** because PO abs is poor
-except for neomycin=topical only bc IV is too nephrotoxic

MOA:

  • enter bacteria through porin channel
  • bind irreversible to 30S unit
  • inhibit protein synthesis
  • bactericidal
  • use is limited due to toxicity

Spectrum:
*mostly gram(-) aerobic bacilli
EX: pseudomonas
**BUT these drugs are INFERIOR to beta-lactams

NOT effective for:
-anaerobics

Synergistic with: PCNs for Gram+ infections: enterococci and streptococci

INDS:

  • MC use=empiric tx for serious infections (combo with other agents)
  • *septicemia
  • *Hosp aquired resp infections
  • *complicated UTIs
  • *Osteomyelitis
29
Q

protein give baceteria?

A
  • structural integrity
  • ability to make energy
  • critical for bacteria to multiply
30
Q

Pharmkinetics of Tigecycline

  • abs
  • penetrates what well? and what not so well?
  • any dose adjustments
  • durg-drug interations
A
  • penetrates tissue well
  • but not plasma….. not good for bacteremia****
  • dose adjustment for hepatic dz BUT not renal
  • may decr warfarin clerance
31
Q

Quinupristin/Dalfopristin

  • drug class
  • route
  • MOA
  • cidal or static
  • Indications
  • penetration?
  • CYP ____ ____
  • adv rxn
A

Streptogramin

Quinupristin/Dalfopristin– IV
*combo of two streptogramins in ratio of 30:70

MOA:
-binds to 50s subunit— synergistic inhib of protein synthesis

Bactericidal

Inds: only gram+
*saved for severe infections
**Vancomycin-resistant enterococcus faecium
NOT FAECALIS

does not penetrate CNS
CYP 450 inhibitor

adv rxns:

  • Venous irritation–>use central line*
  • Hyperbilirubinemia
  • Arthralgia/myalgia at high doses
32
Q

why do we want to avoid long term use with Linezolid or Tedizolid?

A

lactic acidosis developement with LT use

33
Q

Macrolides/Ketolides

-list them and routes

A

Azithromycin (PO, IV)
Clarithromycin (PO)
Erythromycin (PO)

34
Q

which macrolide(s) are newer and more acid stables

A

Clarithromycin

Azithromycin

35
Q

which macrolide(s) are better abs

A

Clarithromycin

Azithromycin

36
Q

indication for Amikacin

A

useful when gentamycin or tobramycin resistance strains

37
Q

adv rxns with tetracyclines (9)

A
  • can accumulate in bones and teeth of growing kids
  • if allergic to one tetracycline– allg to all**
  • Photoxocitiy– sunburn BAD
  • GI discomfort
  • esophageal erosion (avoid b4 bed)
  • hepatoxocitiy– rare but fatal
  • nephrotoxicity can worsen it
  • vertigo with minocycline
  • Jarish-Herxheimer rxn for spirochete tx
38
Q

pharmkinetics for aminoglycosides

  • abs after PO
  • penetration
  • __ dependent
  • synergistic?
  • why do we monitor the levels closely
A

poor abs after PO

penetration:
- tissues=variable
- poor pen in CNS, lungs, eye, prostate, bile

[ ] dep. with post-abx effect

synergistic with beta-lactams

have to monitor levels closey to avoid toxicity

39
Q

Tigecycline

  • drug class?
  • route
  • derivative of?
  • why created
  • MOA
  • spectrum
  • indications
  • SE
A 
Glycycline class  
IV ONLY
  • derivative of minocycline
  • dev as a result of tetracycline resistance

MOA: same as tetracyclines

Broad spectrum

  • most gram+
  • many multi-drug resistant aerobic gram (-)s

INDS:

  • nosocomial soft tissue infections
  • *****MRSA
  • *****VRE
  • Anerobes
  • CAP
  • intra-abdominal infections

SE

  • Similar to other tetracyclines EXCEPT:
  • BBW for increased mortality……. so use this drug only when alternative treatments are not available
  • coagulopathy
  • Safety not established for PT <18YO
40
Q

Tetracycline and minocycline DOC for?

what happens to absoprtion when taken with or w/o food

A

acene

Abs for tetracycline is 50% decreased if taken with food

41
Q

which tetracycline is the only approved drug for use in peds

A

doxycycline

42
Q

Inds for tobramycin

A

pseudomonas

aerosolized for CF

43
Q

instructions to tell PT when they are on tetracycline tx (5)

A
  1. Take tetracycline on empty stomach– the others are ok to take with food
  2. Avoid just before bed to preveent esophageal erosion
  3. wear sunscreen
  4. beware of risk with pregnancy
  5. avoid dairy products, mag, aluminu, iron, ca
44
Q

Indication for gentamycin

A

endocarditis

45
Q

resistance to aminoglycosides?

A
  • less resistance comapred to other classes of ABX

- more specific for each aminoglycoside

46
Q

Azithromycin

-best against?

A

respiratory pathogens **

  • H. flu
  • Moraxella
  • Mycoplasma pneumoniae (FIRST LINE)
  • Neisseria
  • mycobacterium avium

STIs
*chlamydia

47
Q

contraindictions for aminoglyosides

A

PT with myasthenia gravis

Pharmacology (28 decks)

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