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pharmacology > protein synthesis inhibitors > Flashcards

protein synthesis inhibitors Flashcards

1
Q

what are the protein synthesis inhibitors?

A

30s: tetracyclines, aminoglycosides
50s: Macrolides, Clindamycin, Streptogramins, Oxazolidinones

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2
Q

doxycycline excretion: renal?

A

not renal - hepatic and fecal

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3
Q

Tetracycline: MOA, Spectrum, bactericidal or static?

A 
Bacteriostatic
MOA: 30s subunit (protein) 
spectrum: BROAD (+ and -). 
-atypicals: ricksettsia (ticks, mites, fleas, lice), chlamydia, mycoplasmic pneumoniae 
-spirochete: lyme disease
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4
Q

tetracycline resistance

A

3 possible ways:

  • efflux pump (bacteria expels drug out of cell)
  • enzymatic inactivation
  • bacteria proteins that prevent binding of drug to ribosome
  • resistance to one tetracycline DOES NOT mean to resistance to all
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5
Q

Additions to spectrum of tetracyclines: doxycycline and minocycline

A

doxy: atypical: CAP, malaria, prophylaxis
mino: P. Acnes

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6
Q

PK of tetracyclines

A 
Oral administration
Absorption decreased by: 
Divalent cations ( Ca, Fe, Mg or Al)
Diary products
Antacids (don't take with these)
=reduced bioavailability when with foods

poor CNS penetration

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7
Q

super infection can occur with what type of antibiotic?

A

any broad spectrum (most often cause is candida or Cdiff)

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8
Q

serious adverse effects of tetracycline

A 
Skin: photosensitivity 
Staining of teeth
Bind to calcium deposited in newly formed bone or teeth in young children and fetal teeth during pregnancy
Teeth fluorescence/discoloration
Enamel dysplasia

Fetal bone deformities
Deposit in bone leading to deformity or growth inhibition

CONTRAINDICATED in pregnant women, infants, children < 8 years or younger
“TETRAcycline = TERATogenic”

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9
Q

Glycycline –> tigecycline

A

Tetracycline derivative (semisynthetic of minocycline)
(IV drug)
MOA: 30s subunit
Spectrum: BROAD (+ and -) including MRSA, VRE
anaerobes
atypical- legionella (CAP)

clinical uses: CAP, infections of deep tissue and intra-abdominal

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10
Q

aminoglycosides

A 
"GNATS" - all "mycin" except Amikacin
Gentamycin
Neomycin
Amikacin
Tobramycin
Streptomycin
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11
Q

post antibiotic effect is most common in what type of abx?

A

those that inhibit protein/DNA/RNA.

PAE- suppression of bacterial growth after brief drug exposure

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12
Q

PK of aminoglycosides: Absorption, distribution, elimination

A

abs: only IV (occassional IM) or topical (conjunctivitis)
- hospital drug
distribution: good, no CSF or eye (unless topical) but can use for meningitis with other drugs if inflamed and synergistic (beta lactams)
elimination: renal, MUST make dose adjustment w/ kidney failure. (monitor serum drug levels )

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13
Q

aminoglycosides are good to treat what?

A

gram neg serious infections: bacterial meningitis, sepsis, (endocarditis), osteomyelitis, etc)

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14
Q

aminoglycosides adverse effects

A

ototoxic, nephrotoxic, neuromuscular blockade

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15
Q

triple antibiotic ointment

A

neomycin (gram- and gram +, too nephrotoxic for oral or IV- hence ointment)
polymixin (gram -)
bacitracin (gram +)

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16
Q

“mean GNATS caNNOT kill anaerobes”

A

mean (aminoglycosides)
GNATS: gentamycin, neomycin, amikacin, tobramycin, streptomycin
NNOT: nephrotoxicity, neuromuscular blockade, ototoxic, teratogen (oto and nephro for fetus too)

17
Q

erythromycin is used mostly for what?

A

acne (only macrolide that is bacteriostatic instead of cidal

18
Q

fidaxomicin use for?

MOA, spectrum, adverse

A

Cdiff but VERY expensive
MOA: thought of as macrolide but binds to RNA polymerase and stops protein binding
Spectrum: NARROW- CDiff (gram +)
Adverse: bowel obstruction or GI hemorrhage

19
Q

macrolides

A

“FACE” fidaxomycin, azithromycin, clarithromycin, erythromycin
..or girls names - “FrIDA, AZI, CLARe, ERYn”

20
Q

macrolide MOA and spectrum

A

MOA: 50s subunit
spectrum: gram + cocci

21
Q

atypical pneumonias

A

chlamydia, mycoplasma, legionella(CAP)

22
Q

macrolides- drug resistance patterns

A

primarily why we dont use erythromicin anymore

  1. target modification- prevent abx to ribosome bind
  2. efflux
  3. drug inactivation
23
Q

z pack

A

axithromycin: - LONG half life- different Dosing - “Zpack” - pt only takes for 5 days but actually stays in system for 10 days - increases pt compliance
EASIER IS BETTER -

24
Q

macrolide excretion

A

bile and feces

25
Q

generally use macrolides for what clinical uses?

A

STIs and CAP

26
Q

adverse effects of MACROlides

A 
"MACRO" 
GI Motility (usual stomach upset) 
Arrhythmia
acute Cholestatic hepatitis 
Rash
Eosinophilia
  • erythro and clindo are worst for these, Azithromycin is best to use to limit adverse effects
  • first 2 most important
27
Q

Erythromycin and Clarithromycin have what significant danger?

A

drug interaction- inhibit CYP34A - increases serum levels of other drugs (esp. statins and warfarin)

28
Q

treatment of anerobes above and below diaphram

A

above: clindamycin
below: metronidazole

29
Q

abx most common cause of superinfection Cdiff

A

Clindamycin and fluoroquinolones

30
Q

Clindamycin: MOA, Bactericidal?, Spectrum

A

MOA: 50s subunit (tunnel)
bacterioSTATIC
spectrum: gram + cocci (strep and staphy) MRSA, MSSA
anerobes- above diaphragm

31
Q

adverse effects of clindamycin

A

superinfections Cdiff

32
Q

streptogramins: combo of what? MOA, bactericidal?, spectrum

A

daflopristin/quinupristin (synercid)
MOA: 50s subunit
bactericidal?: yes- conc dependent
spectrum: FOR LIFE THREATENING VRE

33
Q

what do you take for life threatening VRE?

A

streptogramin: dafl/quinu- pristin

34
Q

1st choice for MRSA

A

vancomycin

35
Q

1st choice for MSSA

A

PCN antistaph or Trimethoprim “Anti Staph: MiSSA, TriMe”

36
Q

oxazolidnones: drugs in group, MOA, bactericidal?, spectrum

A

tedizolid and linezolid (more common one)
MOA: 50s subunit
bactericidal?: no STATIC
spectrum: multi-drug resistant gram + (VRE, MRSA)
…also HAP and CAP

37
Q

Buy AT 30, CEL at 50

A

protein synthesis inhibitors

30: Aminoglycosides and Tetracyclines
50: Clindamycin, Erythromycin (macrolides), Linezolid (oxazolidnones)

38
Q

protein synthesis inhib: cidal or static?

A

static at low doses, cidal at high doses

pharmacology (24 decks)

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