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Anti-Infectives Exam 2 > Lecture 4 - Linezolid, Tedizolid, Clindamycin & Lefamulin > Flashcards

Lecture 4 - Linezolid, Tedizolid, Clindamycin & Lefamulin Flashcards

1
Q

Oxazolidinones

A

Linezolid

Tedizolid

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2
Q

Miscellaneous Gram + antibiotics

A

Clindamycin

Lefamulin

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3
Q

Gram + antibiotics

A

Glycopeptides & Lipoglycopeptides
Oxazolidinones
Miscellaneous

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4
Q

Linezolid MOA

A
  1. Protein synthesis inhibitor (Binds to V-domain of 23S RNA component of the 50S ribosomal subunit)
  2. Its bacteriostatic
  3. Manipulation of A/B are necessary for antibacterial activity
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5
Q

Linezolid Spectrum of Activity Gram +

A

Broad Gram + activity

Active against Enterococcus species, inc E.faecalis + VRE (considered Txm of choice depending on source)

Active against MSSA/MRSA (good if no DI + can tolerate)

Active against all Streptococcal species

** Used in Polymicrobial inf (intra-abdominal or SSTI) when also need to cover Enterococci or MRSA

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6
Q

Linezolid Spectrum of Activity Gram + Bacillus

A

Active against Listeria Monocytogenes (Txm of choice is Ampicilin+Gentamicin tho)

Active against Nocardia species (Txm of choice is Bactrim tho)

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7
Q

Linezolid Spectrum of Activity Anaerobes

A

Broad active against Gram + anaerobes

Active against: Actinomyces, Propionbacterium, peptostreptococci

Some activity: Prevotella, Fusobacterium

Limited activity: B. fragilis (Gram - anaerobes in GI)

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8
Q

Linezolid has no activity in….

A

Gram - and Atypical

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9
Q

Linezolid Activity in Other organisms

A

Has activity against Mycobacteria, including M.tuberculosis….txm option for drug resistant TB**

Also active against non-TB Mycobacteria (inc Mycobacterium abscenssus - MDR and MAC, Mycobacterium avid complex)

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10
Q

Linezoid M & E

A

Bioavailability is ~ 100%, so PO and IV dose is same

High conc into epithelial lining fluid (>100%), bone and joint tissues

Doesn’t req renal adjustment due to majority elim non-renal

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11
Q

** Linezolid Drug Interactions **

A
  1. Reversible, non-selective monoamine oxidase inhibitor
  2. Associated w/ development of Serotonin Syndrome in pts receiving concurrent serotonergic agents

Small inc in BP in pt using Tyramine

** don’t use with Serotonin drugs **

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12
Q

Tedizolid MOA

A

Protein Synthesis inhibitor

And to V-domain of 23S RNA component of 50S ribosomal unit

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13
Q

Tedizlod Gram + Spectrum of activity

A

shown to be 2-8 X more potent than Linezoid

active against Enterococcus species, inc E.faecalis + VRE

Active against MSSA + MRSA
Active against all Streptococcal species

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14
Q

Tedizolid Gram + bacillus activity

A

Has shown to have MIC90 values several-old lower than those of linezolid for a number of species

exception: Nocardia nova complex & Nocardia brasiliensis

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15
Q

Tedizolid Spectrum of activity Anaerobes

A

broad activity against Gram + anaerobes

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16
Q

Where does Tedizolid not have activity?

A

Gram - and Atypical

17
Q

Tedizolid Spectrum of activity in Mycobacteria

A

appears to be more potent for strains tested, but clinical significance of in vitro findings is unclear

18
Q

Tedizolid M & E

A

12hrs 1/2life = QD dosing

Pro drug, given Oral or IV

No renal dose adjustment required

19
Q

Tedizolid DI

A
  1. weak, reversible monoamine oxidase inhbition
  2. wasn’t tested for use with serotonergic agents but no negatives shown in animal investigation and other preliminary tests

OK to use in pts on Serotonin drugs

20
Q

Oxazolidinones ADR

A

GI - Diarrhea
Hepatic - inc LFT
Hematologic toxicity = inc w/ linezolid
Neuropathy = inc w/ linezolid

21
Q

Clindamycin MOA

A

Lincosamide antibiotic

Protein synthesis inhib, reversibel binde to 50S ribo subunit

Suppression of exotoxins (a toxins, TSST-1, PVL, enterotoxins)

22
Q

Clindamycin Spectrum of Activity

A

No enterococcal coverage

Active against MSSA/MRSA but not good choice, but ager doing D-test can possibly use

Limited in Streptococcal species due to resistant

** used in combo with Penicillin for Group A Streptococcal toxic shock syndrome **

23
Q

Combo of Penicillin and Clindamycin is used in….

A

Group A streptococcal toxic shock syndrome

24
Q

What does Clindamycin not cover

A

Gram - and Atypical

25
Q

Clindamycin Spectrum of Activity anaerobes

A

Clindamycin considered treatment of choice for Gram + anaerobes

** use limited due to resistance and high risk of C.difficile infections

Gram - anaerobic (B. fragilis = GI) limited due to resistance

26
Q

Clindamycin other uses

A

Activity against Toxoplasmosis

activity against Pneumocystis used as combo with Primaquine

Activity against malaria (Plasmodium falciparum) and is alternative for malaria in pregnancy

27
Q

Clindamycin M & E

A

Absorption ~90%, delayed by ingestion of food.

most drug metabolized to products with variable antibacterial activity

normal 1/2life is 2.4hrs, dosing q6/8hrs

28
Q

Clindamycin DI

A

CYP3A4 Inducers decrease serum conc

CYP3A4 Inhibitors inc serum conc

29
Q

Clindamycin ADR

A

GI = 20% diarrhea, C.dif infection**
Dermatologic
Hepatic

30
Q

Lefamulin MOA

A

Pleuromutilin antibiotic

protein synthesis inhibitor, tight-fit binding to A/P sites of 50S ribosomal subunit

31
Q

Lefamulin Gram + Spectrum of activity

A

Active against MSSA, MRSA, Staphylococci

Strep, including susceptible and resistant S.pneumoniae

active against B/A hemolytic strep

Some against E.faecium, not against E.faecalis tho

32
Q

Lefamulin Gram - Spectrum of Activity

A

No activity against Enterobacterales

No activity against non-fermenting Gram -

** good activity against Gram - organisms associated with community acquired pneumonia (H. influenzae, M.catarrhalis)

33
Q

Lefamulin Anaerobes Spectrum of activity

A

Activity against common anaerobes

acts coverage against C.difficile and B.fragilis

34
Q

Lefamulin Activity against Atypical?

A

C.pneumoniae
M.pneumoniae
L.pneumophilia

35
Q

Lefamulin M & E

A

Absorption dec by food, take 1hr before or 2hr after meal

dose reduced in pics with Child-Pugh Class C

36
Q

Lefamulin DI

A

can cause inc in QT interval

** CI in Pimozide ***

37
Q

Lefamulin ADR

A 
GI = diarrhea, n,v
Prolonged QTc
CNS
Hermatologic & oncologic
Local injection site

Anti-Infectives Exam 2 (8 decks)

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