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Anti-Infectives Exam 2 > Lecture 5 - Macrolides, Tetracycline, & Tigecycline > Flashcards

Lecture 5 - Macrolides, Tetracycline, & Tigecycline Flashcards

1
Q

Drugs that are considered Macrolides

A

Erythromycin
Clarithromycin
Azithromycin

Fidaxomicin

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2
Q

Erythromycin MOA

A

Protein synthesis inhib, bacteriostatic

Inhibits RNA-depended protein synthesis at the step of chain elongation

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3
Q

Which part of ribosome does Erythromycin bind?

A

Binds to 23S ribosomal RNA component of 50S subunit of bacterial ribosome at the peptide exit tunnel

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4
Q

Erythromycin Gram + activity

A

Limited staph coverage due to resistance

some activity against strep, but growing resistance for S.pnemoniae

No activity against enterococci

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5
Q

Erythromycin Gram - activity

A
  1. campylobacter jejuni
  2. Coxiella burnetti (Q fever)
  3. Bordetella pertussis (whooping cough)
  4. Moraxella catarrhalis
  • No activity agent Enterobacteriaceae or non-fermenters
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6
Q

Erythromycin Anaerobic activity

A

(-): moderate, including Prevotella

(+): better activity, including Actinomyces, P/C acnes, Lactobacilli, Clostridium spp, and Peptostreptococci

Bacteroides Fragilis & Clostridiodes difficile are resistant

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7
Q

Erythromycin Atypical Bacteria uses

A

Usually used as an add on

active against most Atypical except Mycoplasma genitalium***

Myco. Tuberculosis is resistant

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8
Q

Erythromycin GI issue

A
  1. In low pH enivocnoment (stomach), erythromycin is degraded to an inactive intermediate that is associated with GI adverse effects associated with its use

Has DDI due to ABCB1

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9
Q

Erythromycin metabolism & excretion

A
  1. All macrolide are lipophilic and widely distributed in blood and tissues
  2. Conc in tissues is 50X those found in plasma

3, substrate of SLCO1B1 and SLCO1B3 for uptake into hepatocytes

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10
Q

Erythromycin DI

A

Inhibits CYP3A4
Inhibits P-gp & ABCB1

QTc prolongation

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11
Q

Erythromycin ADR

A
  • *** Ototoxicity in large doses
  • **QT prolongation (whole macrolide class)

GI, allergic reactions

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12
Q

Clinical uses of Erythromycin

A

Most frequently used for its motility effects = due to its GI effects

other macrolides are better with less SE/DI

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13
Q

Clarithromycin vs Erythromycin

A

It has similar coverage but better tolerance and SE

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14
Q

Clarithromycin Gram + Activity

A

2-4 fold more active than Erythromycin against most strep, including S.penumoniae (growing resistance) , S.pyogenes, MSSA(but not drug of choice).

Most staph resistent to macrolides

No activity against Enterococci

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15
Q

Clarithromycin Gram - activity

A
  1. campylobacter jejuni
  2. Coxiella burnetti (Q fever)
  3. Bordetella pertussis (whooping cough)
  4. Moraxella catarrhalis (slightly more than Erythromycin)
  • No activity agent Enterobacteriaceae or non-fermenters
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16
Q

Clarithromycin Anaerobic bacteria

A

Not as active against Actinomyces

(+):P/C acnes, Lactobacilli, Clostridium spp, and Peptostreptococci

Bacteroides Fragilis & Clostridiodes difficile are resistant

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17
Q

Clarithryomycin Atypical Bacteria activity

A

Active against most Atypical except Mycobacterium Genitalium

useful against CAP

1 of main drugs against Mycobacterium

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18
Q

Drugs that work against M.abscessus

A

Azithromycin and Clarithromycin

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19
Q

Clarithromycin PK properties

A

More acid-stable than erythromycin and is not degraded as extensively in the stomach

Also affects ABCB1 = DI

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20
Q

Clarithromycin Metabolism & Excretion

A
  1. Lipophilic and widely distributed in blood tissues

2. thought to undergo metabolism by CYP3A4 in liver & inhibits CYP3A4, leading to similar DI as erythromycin

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21
Q

Clarithromycin ADR

A

Rare: Mania, Ototoxicity = large dose, QT prolongation

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22
Q

Clarithromycin DI

A

Inhibits CYP3A4
Inhibits P-gp, ABCB1, OATP1B1/B3

QTc prolongation

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23
Q

Clarithromycin Clinical uses

A

combo with amoxicillin or metronidazole and a PPI for H.pylori (1st line)

Mycobacterial infections
Bartonella spp.
Pertussis

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24
Q

Azithromycin Gram + activity

A

Less active against S.pneumoniae & S.pyogenes than erythromycin

no activity against Enterococci

some activity against strep, but growing resistance

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25
Q

Azithromycin Gram - activity

A

Most common macrolide used

more active, especially in H.influenzae & M. catarrhalis

  1. campylobacter jejuni
  2. Coxiella burnetti (Q fever)
  3. Bordetella pertussis (whooping cough)
  4. Moraxella catarrhalis
  5. N.gonorrhoeae

Questionable activity in Enterobacteriaceae
No activity in non-fermenters

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26
Q

Azithromycin Anaerobic bacteria

A

Not as active against Actinomyces

(+):P/C acnes, Lactobacilli, Clostridium spp, and Peptostreptococci

Bacteroides Fragilis & Clostridiodes difficile are resistant

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27
Q

Drugs for Mycobacteria

A

Azithromycin & Clarithromycin have activity against M. avian complex, but Clarithromycin is 4X more active

Azith usually used for prophylaxis

Both have activity against M.abscessus

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28
Q

Azithromycin Atypical Bacteria Activity

A

greater activity than Erythromycin against Ureaplasma urealyticum & Chlamydia Trachomatis

more active against Legionella pneumophilia and M. pneumoniae

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29
Q

Azithromycin PK properties

A

more acid-stable than Erythromycin, resulting in longer serum 1/2 life and increased conc in tissue

absorption limited in intestine by P-gp transporters

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30
Q

Azithromycin Metabolism & excretion

A

lipophilic and widely distributed in blood and tissues

doesn’t interact with SLCO1B1/B3 and doesn’t inhibit CYP3A4 activity

Most excreted unchanged in bile = hepatic

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31
Q

Azithromycin ADE

A

GI > 10%

Rare: Elevated LFTs, ototoxicity = high dose, QTc prolongation

32
Q

Azithromycin Clinical uses

A

CAP (L.pneumophila, C.pneumoniae, M. pneumoniae

Infectious Diarrhea : Campylobacter jejune
STI: Chalmydia trachomatis

Mycobacterial infections

Pertussis
Bartonella spp.

33
Q

Fidaxomicin MOA

A

Baactericidal

Bacterial RNA polymerase inhibition at transcription initiation

34
Q

Fidaxomicin Spectrum of activity

A

Only clinically used for C.difficile

35
Q

Fidaxomicin Metabolism & Excretion

A

excreted almost entirely through the feces

oral form minimally absorbed via GI

36
Q

Does Fidaxomicin have DI

A

nah

37
Q

Fidaxomicin ADR

A

GI = nausea, abdominal pain, vomiting, GI hemorrhage

some hypersensitivity - rare

38
Q

Fidaxomicin clinical uses

A

used for C.difficile

Vancomycin is used 1st, and then consider this drug

39
Q

Tetracyclines

A 
Tetracycline
Doxycycline
minocycline
Omadacycline
Eravacycine

Tigecycline

40
Q

Tetracycline MOA

A

Protein synthesis inhibitor

Bacteriostatic

41
Q

Where are the Tetracycline binding sites

A

Binding sites on the 30S subunit of the 70S ribosome (primary = Tet1) and secondary (Tet2)

42
Q

1st gene Tetracycline

A

Tetracycline

43
Q

Tetracycline Gram + activity

A

Worst activity out of all Tetracyclines

some against MSSA

Limited against Streptococci, including Group A/B

Limited activity against Enterococci

44
Q

Tetracycline Gram - activity

A

Vibrio Cholerae = cholera

1st line H.pylori (w/ bismuth, PPI, Metronidazole)

45
Q

Tetracycline Anaerobic bacteria activity

A

has some against Gram +/-

B.Fragilis has resistance
None against C.diff

46
Q

Tetracycline Activity Atypical Bacteria

A

good activity against most that cause urogenital infections and those that cause CAP

reduced activity against M.genitalium

47
Q

Tetracycline Metabolism & Excretion

A

eliminated primarily in the kidneys, about 30-60% of oral dose is excreted in urine and 20-60% in feces

48
Q

Tetracycline adverse effects

A

GI = most common

Teeth & bone deposits = reasons why avoided in meds

Photosensitivity and Hyperpigmentation

49
Q

Tetracycline DI

A

Food: Reduces absorption by 50%, dec iron absorb, calc dec tetracycline con

CYP3A4 inducers = reduce conc of it
CYP3A4 inhibitors = inc conc of it

Interacts with Vit K

50
Q

Tetracycline Clinical uses

A

1st line for H.pylori w/ metronidazole, bismuth, PPI

Treatment of cholera (Vibrio cholerae)

51
Q

2nd Gen Tetracyclines

A

Doxycycline

Minocycline

52
Q

Doxy & Mino Gram + activity

A

** improved activity against Staph, including MSSA/MRSA

Less active against Streptococci, including Group A/B

Limited activity against Enterococci

53
Q

Doxy & Mono Gram - activity

A

Limited enterobacteriaceae coverage

mino has broader activity against MDR Gram - organisms (stenotrophomonas and acinetobacter)

54
Q

Doxy is preferred agent for what infections

A

Borrelia burgdorgeri = Lyme disease
Yersinia pestis = Black Plague
Ehrlichia spp, Anaplasma spp. = tick borne disease
R.ricketsii = Rocky Mountain spotted fever

55
Q

Doxy & Mino Anaerobic bacteria activity

A

Similar activity against Gram +/- anaerobes

C.diff = no activity
B.fragilis has resistance

56
Q

Doxy & Mino Atypical Bacteria Activity

A

good activity against most that cause urogenital infections and those that cause CAP

reduced activity against M.genitalium

57
Q

Doxy & Mino Metabolism & Excretion

A

Less than 30% of doxy is renally excreted

Mino extensively metabolized in liver, only 4-19% eliminated by kidneys

58
Q

Mino specific rare Adverse effects

A

Neurotoxicity

Hypersensitivity reactions

59
Q

Mino/Doxy common adverse effects

A

GI
Teeth & bone deposits
Photosensitivity & Hyperpigmentation

60
Q

Doxy & Mino DI

A

Food: absorption reduced ~20% when w/ food or milk
Tetracycline dec absorption of iron
Ca dec conc of tetracyclines

Drug:
PPIs decrease bioavailability of doxy

other:
Vitamin K

61
Q

Drugs that can decrease conc of doxy

A

Carbamazepine
Phenytoin
fosphenytoin

62
Q

Doxy & Mino clinical uses

A

Doxy:
CAP, Travelers poop, Urogenital infections, tick borne disease, bioterrorism

Mino:
Acne, MDR Stenotrophomonas & Acinetobacter

63
Q

3rd gen Tetracyclines

A 
Tigecycline = IV
Omadacycline = Oral
Eravacycline = IV
64
Q

3rd gen Tetracyclines Gram + activity

A

improved against all Gram +

Great S.aureus, MSSA,MRSA coverage

improved Streptococcal coverage

improved activity against Enterococci, including VRE

65
Q

3rd gen Tetracyclines Gram - activity

A

sig improved coverage of Enterobacteriaceae

improved activity against MDR Acineto-, Stenotrop-

66
Q

3rd gene Tetracyclines Anaerobic bacteria activity

A

less B.fragilis resistance
some activity against C.diff
no activity against actinomyces

67
Q

3rd gene Tetracyclines Atypical bacteria

A

activity against Mycobacteria

Atypical bacteria similar for CAPs, reduced against C.trach, U.ureal, M.genit

68
Q

Eravacycline M&E

A

1/2 life is 20hrs

~34% urine ~46% poop

69
Q

Tigecycline M&E

A

1/2life ~27-67hrs

excreted 59% poop, 33% urine

70
Q

Omadacycline M&E

A

1/2life ~16hrs
food decreases rate/extent of absorption
excretion mostly through poop

71
Q

Tigecycline GI sideeffects

A

Diarrhea
vomiting
heartburn

72
Q

Omadacycline GI sideeffects

A

Nausea

Heartburn

73
Q

Omadcycline DI

A

Substate: P-gp, ABCB1
Food: serum lvls may dec if taken w/ high fat meal or dairy, separate by 4hrs and avoid food/drink for 2hrs after

74
Q

Eravacycline DI

A

substrate: CYP3A4 minor

75
Q

Tigecycline DI

A

none

76
Q

Omadacycine uses

A

oral options for infections caused by MDR Gram -

M.abscessus infections

77
Q

Eravacycline & Tigecycine Clinical uses

A

MDR Stenotroph/Acinetobac

if need gram +/- coverage (intra-abdominal infections)

Add on therapy in severe C.diff

Anti-Infectives Exam 2 (8 decks)

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