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PC2 > Tetracyclines > Flashcards

Tetracyclines Flashcards

1
Q

Tetracyclines are bactericidal/bacteriostatic

A

bacteriostatic

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2
Q

Tigecycline is bactericidal/bacteriostatic

A

bacteriostatic

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3
Q

Tetracycline was developed from

A

oxytetracycline and chlrotetracycline

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4
Q

Doxycycline and minocycline are ____ derivatives of oxytetracycline

A

semisynthetic

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5
Q

____ and ____ are derived from minocycline

A

tigecycline; omadacycline

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6
Q

Tigecycline is a

A

glycylcycline

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7
Q

Tetracyclines include

A

tetracycline, doxycycline, minocycline, eravacycline, omadacycline, tigecycline

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8
Q

Structure of tetracyclines

A

4 benzene rings with hydronaphthacene nucleus

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9
Q

Doxycycline spectrum coverage

A

dark purple: s. pneumoniae, MSSA, MRSA

light purple: streptococcus, viridans

dark red: Neisseria, h. influenzae, klebsiella, mycoplasma, chlamydia, legionella

light red: b. pertussis, E. coli, enterobacter , citrobacter, serratia, acinetobacter

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10
Q

Minocycline spectrum coverage

A

dark purple: s. pneumoniae, MSSA, MRSA

light purple: streptococcus, viridans

dark red: Neisseria, h. influenzae, E. coli, klebsiella, serratia, acinetobacter, fusobacteria,clostridium, mycoplasma, chlamydia, legionella

light red: b. pertussis, enterobacter, citrobacter

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11
Q

Tigecycline spectrum coverage

A

dark purple: all gram + (strep, staph, enterococci)

dark red: Neisseria, h. influenzae, E. coli, klebsiella, enterobacter, citrobacter, serratia, acinetobacter, bacteroides, prevotella, fusobacteria, clostridium, mycoplasma, chlamydia, legionella

light red: b. pertussis

other: CRE, CRAB, ESBL, and VRE

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12
Q

Eravacycline spectrum coverage

A

dark purple: all gram + (strep, staph, enterococci)

dark red: Neisseria, h. influenzae, E. coli, klebsiella, enterobacter, citrobacter, serratia, acinetobacter, bacteroides, prevotella, fusobacteria, clostridium, mycoplasma, chlamydia, legionella

light red: b. pertussis, p. mirabilis, morganella

other: CRE, CRAB, ESBL, VRE

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13
Q

Omadacycline spectrum coverage

A

Same as tigecycline
dark purple: all gram + (strep, staph, enterococci)

dark red: Neisseria, h. influenzae, E. coli, klebsiella, enterobacter, citrobacter, serratia, acinetobacter, bacteroides, prevotella, fusobacteria, clostridium, mycoplasma, chlamydia, legionella

light red: b. pertussis

other: CRE, CRAB, ESBL, and VRE

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14
Q

All tetracycline don’t cover

A

p.aeruginosa

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15
Q

All tetracyclines also cover

A

spirochetes and rickettsiae, mycobacteria and nocardia, parasites, bacillus anthracis, vibrio cholerae

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16
Q

Tetracyclines MOA

A

Entry:
gram +: through the inner cytoplasmic membrane via an active transport system that depends on pH differential

gram-: become charged and enter through porin channels (OmpF and OmpC)

inhibits bacterial protein synthesis

binds reversibly to 30s ribosomal unit; inhibits the enzyme binding of aminoacyl-tRNA to the ribosomal acceptor site which prevents peptide elongation and protein synthesis

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17
Q

Tetracycline no longer has ___ formulation due to ____

A

IV; hepatotoxicity

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18
Q

Tetracycline should be ____ in renal impairment

A

AVOIDED

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19
Q

Tetracycline can cause ____ impairment

A

hepatic

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20
Q

Doxycycline comes in ____ formulations

A

IV and PO

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21
Q

Doxycycline is ___ in renal impairment

A

SAFE

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22
Q

Doxycycline has increased ___ excretion which allows it to have decreased serum accumulation and therefore safe for renal impairment

A

fecal

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23
Q

Doxycycline ____ cause(s) hepatitis

A

does not

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24
Q

Minocycline is available in

A

IV and PO formulations

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25
Q

Minocycline has ___ in hepatic impairment

A

no effect

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26
Q

Minimal amount of minocycine is excreted ___

A

renally

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27
Q

Tetracycline PO availability

A

77-88%

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28
Q

Tetracycline 1/2 life

A

7 hours

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29
Q

Doxycycline PO availability

A

100%

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30
Q

Doxycycline 1/2 life

A

12-16 hours

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31
Q

Minocycline PO availability

A

90%

32
Q

Minocycline 1/2 life

A

16 hours

33
Q

Tigecycline 1/2 life

A

37-67 hours

34
Q

Eravacycline 1/2 life

A

20 hours

35
Q

Omadacycline PO availability

A

35%

36
Q

Omadacycline 1/2 life

A

16 hours

37
Q

Protein binding for tetracycline

A

eravacycline> tigecycline> doxycycline> minocycline> tetracycline> omadacycline

38
Q

Renal elimination for tetracycline

A

tetracycline> doxycycline> eravacycline> tigecycline> minocycline> omadacycline

39
Q

Fecal elimination for tetracycline

A

doxycycline> omadacycline> tigecycline> eravacycline> tetracycline> minocycline

40
Q

Tissue distribution for tetracycline

A

wide distribution except CSF, doxycycline is still used in some CNS infections

41
Q

Tetracyclines indications

A 
respiratory
GI
genitourunary
spirochetal 
malaria treatment and chemiprophylaxis
other: acne, bioterrorism
42
Q

Tetracyclines adverse effects

A

GI: nausea, vomiting, diarrhea, heartburn, epigastric pain

pill esophagitis with doxycycline (patients should drink 8 oz of water and stand upright for 30 min)

reduced risk of c. diff

photosensitivity and hyperpigmentation: blue/black discolorations where scars or inflammation, muddy/brown discoloration on sun-exposed area; USE SUNSCREEN AND PROTECTIVE CLOTHING WHEN EXPOSED TO SUN

blue/black discoloration of gums secondary to bone pigmentation that is visible through non-pigmented oral mucosa occurs with long term use of minocycline and is permanent

nephotoxicity if impaired renal function

neurotoxicity with minocycline causing vertigo, dizziness, tinnitus, lack of concentration (reversible), vestibular effects higher in women

psuedotumor cerebri

43
Q

Tetracyclines are generally ___ in pregnancy

A

avoided

44
Q

Tetracyclines can cross the placenta, found in fetal tissues, and can have ____ effects on the developing fetus

A

toxic

45
Q

___ has been noted in animals treated early in pregnancy

A

embryotoxicity

46
Q

Tetracycline should be taken with/without food

A

without; can reduce absorption by 50%

47
Q

Doxycycline and minocycline should/should no be taken with food

A

food doesn’t not have effect that is clinically significant

48
Q

divalent and trivalent cations: Al, Ca, Mg, Fe, Zn interaction with tetracyclines

A

significant reduction of all tetracycline absorption

should not be administered concurrently

give tetracycline 1-2 hours before or 2 hours after divalent/trivalent cations

49
Q

Interaction of doxycycline with carbamazepine, phenytoin, barbiturates

A

decreased 1/2 life by 44-52%; increases hepatic metabolism, monitor for decreased therapeutic effect. avoid using at the same Time.

50
Q

oral anticoagulants with tetracyclines

A

increased risk of bleeding; tetracyclines impair utilization of prothrombin and decrease vit K production by intestinal bacteria

51
Q

Tigecycline decreases warfarin ___

A

clearance

52
Q

Oral contraceptives with tetracyclines

A

reduced levels when administered with tetracyclines; women should use additional form of birth control

reduction in bacterial hydrolysis of conjugated estrogen in intestine

53
Q

Tetracycline should be taken____. Doxycycline and minocycline should be taken ____.

A

on an empty stomach; with/without food

54
Q

Directions for taking tetracyclines (mostly doxycycline)

A

take with full 8 oz of water and stand up for at leaSt 30 min to reduce risk of esophageal irritation and ulceration

55
Q

Wear___ to prevent sunburn

A

sunscreen

56
Q

tigecycline is a ___ derivative of minocycline

A

semisynthetic

57
Q

the 9-glycyl substitution results in ___ which enables tigecycline to overcome 2 major types of resistance:

A

steric hindrance; tetracycline-specific efflux pumps and ribosomal protection

58
Q

Tigecycline spectrum coverage

A

no coverage against p. aeruginosa

reduced activity against proteus mirabilis, Providencia, morganella (over expressed multi drug efflux pumps)

59
Q

Tigecycline adverse effects

A

GI: nausea and vomiting dose related

transient elevations in transaminases and alkaline phosphatase levels

60
Q

Tigecycline does/does not need renal adjustment

A

does not

61
Q

Tigecycline has ___ protein binding

A

increased

62
Q

Can tigecycline be used in bacteremia?

A

no

63
Q

Tigecycline primary route of elimination

A

liver via biliary excretion

64
Q

Tigecycline indications

A

CA pneumonia
complicated intra-ab infections
complicated skin and skin structure infections
should only be used when other treatment is not available

65
Q

Tigecycline mechanism of resistance

A 
tet genes mediate resistance (plasmids and transposons)
efflux pumps (gram+ and gram -)
ribosomal protection proteins
enzymatic degradation
decreased drug permeability
target mutations
66
Q

Omadacycline was approved in

A

2018

67
Q

Omadacycline indication

A

Community acquired bacterial pneumonia or acute bacterial skin and skin structure infections

68
Q

Omadacycline is available in

A

PO and IV

69
Q

Omadacycline adverse effects

A

trasaminitis, hypertension, insomnia, GI upset

70
Q

Eravacycline approved in

A

2018

71
Q

Eravacycline indications

A

intra-ab infections

72
Q

Eravacycline need adjustment for severe ____ impairment

A

hepatic

73
Q

If eravacycline is used with a strong CYP 3A inducer:

A

need to increase the dose to 1/5mg/kg q12h

74
Q

Eravacycline adverse efffects

A

infusion related reactions, nausea, vomiting, diarrhea, hypotension, wound dehiscence

75
Q

Eravacycline is not indicated for treatment of complicated urinary tract infections because it

A

did not show statistical non-inferiority to ertapenem for treatment of complicated UTI

PC2 (18 decks)

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