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

Lecture 5 - Macrolides, Tetracycline, & Tigecycline Flashcards

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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
Azithromycin Gram - activity
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
26
Azithromycin Anaerobic bacteria
Not as active against Actinomyces (+):P/C acnes, Lactobacilli, Clostridium spp, and Peptostreptococci Bacteroides Fragilis & Clostridiodes difficile are resistant
27
Drugs for Mycobacteria
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
28
Azithromycin Atypical Bacteria Activity
greater activity than Erythromycin against Ureaplasma urealyticum & Chlamydia Trachomatis more active against Legionella pneumophilia and M. pneumoniae
29
Azithromycin PK properties
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
30
Azithromycin Metabolism & excretion
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
31
Azithromycin ADE
GI > 10% Rare: Elevated LFTs, ototoxicity = high dose, QTc prolongation
32
Azithromycin Clinical uses
CAP (L.pneumophila, C.pneumoniae, M. pneumoniae Infectious Diarrhea : Campylobacter jejune STI: Chalmydia trachomatis Mycobacterial infections Pertussis Bartonella spp.
33
Fidaxomicin MOA
Baactericidal Bacterial RNA polymerase inhibition at transcription initiation
34
Fidaxomicin Spectrum of activity
Only clinically used for C.difficile
35
Fidaxomicin Metabolism & Excretion
excreted almost entirely through the feces oral form minimally absorbed via GI
36
Does Fidaxomicin have DI
nah
37
Fidaxomicin ADR
GI = nausea, abdominal pain, vomiting, GI hemorrhage some hypersensitivity - rare
38
Fidaxomicin clinical uses
used for C.difficile Vancomycin is used 1st, and then consider this drug
39
Tetracyclines
``` Tetracycline Doxycycline minocycline Omadacycline Eravacycine ``` *Tigecycline*
40
Tetracycline MOA
Protein synthesis inhibitor Bacteriostatic
41
Where are the Tetracycline binding sites
Binding sites on the 30S subunit of the 70S ribosome (primary = Tet1) and secondary (Tet2)
42
1st gene Tetracycline
Tetracycline
43
Tetracycline Gram + activity
Worst activity out of all Tetracyclines some against MSSA Limited against Streptococci, including Group A/B Limited activity against Enterococci
44
Tetracycline Gram - activity
Vibrio Cholerae = cholera 1st line H.pylori (w/ bismuth, PPI, Metronidazole)
45
Tetracycline Anaerobic bacteria activity
has some against Gram +/- B.Fragilis has resistance None against C.diff
46
Tetracycline Activity Atypical Bacteria
good activity against most that cause urogenital infections and those that cause CAP reduced activity against M.genitalium
47
Tetracycline Metabolism & Excretion
eliminated primarily in the kidneys, about 30-60% of oral dose is excreted in urine and 20-60% in feces
48
Tetracycline adverse effects
GI = most common Teeth & bone deposits = reasons why avoided in meds Photosensitivity and Hyperpigmentation
49
Tetracycline DI
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
Tetracycline Clinical uses
1st line for H.pylori w/ metronidazole, bismuth, PPI Treatment of cholera (Vibrio cholerae)
51
2nd Gen Tetracyclines
Doxycycline | Minocycline
52
Doxy & Mino Gram + activity
** improved activity against Staph, including MSSA/MRSA Less active against Streptococci, including Group A/B Limited activity against Enterococci
53
Doxy & Mono Gram - activity
Limited enterobacteriaceae coverage mino has broader activity against MDR Gram - organisms (stenotrophomonas and acinetobacter)
54
Doxy is preferred agent for what infections
Borrelia burgdorgeri = Lyme disease Yersinia pestis = Black Plague Ehrlichia spp, Anaplasma spp. = tick borne disease R.ricketsii = Rocky Mountain spotted fever
55
Doxy & Mino Anaerobic bacteria activity
Similar activity against Gram +/- anaerobes C.diff = no activity B.fragilis has resistance
56
Doxy & Mino Atypical Bacteria Activity
good activity against most that cause urogenital infections and those that cause CAP reduced activity against M.genitalium
57
Doxy & Mino Metabolism & Excretion
Less than 30% of doxy is renally excreted Mino extensively metabolized in liver, only 4-19% eliminated by kidneys
58
Mino specific rare Adverse effects
Neurotoxicity | Hypersensitivity reactions
59
Mino/Doxy common adverse effects
GI Teeth & bone deposits Photosensitivity & Hyperpigmentation
60
Doxy & Mino DI
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
Drugs that can decrease conc of doxy
Carbamazepine Phenytoin fosphenytoin
62
Doxy & Mino clinical uses
Doxy: CAP, Travelers poop, Urogenital infections, tick borne disease, bioterrorism Mino: Acne, MDR Stenotrophomonas & Acinetobacter
63
3rd gen Tetracyclines
``` Tigecycline = IV Omadacycline = Oral Eravacycline = IV ```
64
3rd gen Tetracyclines Gram + activity
improved against all Gram + Great S.aureus, MSSA,MRSA coverage improved Streptococcal coverage improved activity against Enterococci, including VRE
65
3rd gen Tetracyclines Gram - activity
sig improved coverage of Enterobacteriaceae improved activity against MDR Acineto-, Stenotrop-
66
3rd gene Tetracyclines Anaerobic bacteria activity
less B.fragilis resistance some activity against C.diff no activity against actinomyces
67
3rd gene Tetracyclines Atypical bacteria
activity against Mycobacteria Atypical bacteria similar for CAPs, reduced against C.trach, U.ureal, M.genit
68
Eravacycline M&E
1/2 life is 20hrs | ~34% urine ~46% poop
69
Tigecycline M&E
1/2life ~27-67hrs | excreted 59% poop, 33% urine
70
Omadacycline M&E
1/2life ~16hrs food decreases rate/extent of absorption excretion mostly through poop
71
Tigecycline GI sideeffects
Diarrhea vomiting heartburn
72
Omadacycline GI sideeffects
Nausea | Heartburn
73
Omadcycline DI
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
Eravacycline DI
substrate: CYP3A4 minor
75
Tigecycline DI
none
76
Omadacycine uses
oral options for infections caused by MDR Gram - M.abscessus infections
77
Eravacycline & Tigecycine Clinical uses
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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