Antimicrobials: PCNs/BLI Flashcards by jennifer cortese

Penicillins are what type of antibiotics?

cell wall active

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Penicillins are what type of antibiotics?

cell wall active, beta lactam.

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Penicillin MoA

Disrupts bacterial cell wall formation by inhibiting certain enzymes which create cross-linking, resulting in cell lysis and cell death.

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Dose adjustments for PCNs (2)

dose adjust for CrCl < 50 ml/min

- may need hepatic adjustment

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what do dose adjustments for PCN look like?

More often extending the interval between doses rather than decreasing the dose.

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spectrum of activity for PCNs

mostly gram positive

some have gram negative activity

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5 classes of penicillins

natural
aminos
pennicillinase resistant (aka anti staph)
ureidos (aka anti pseudomonal)
beta lactamase inhibitors

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adverse events: PCNs (4)

hypersensitivity
neutropenia
interstitial nephritis
CNS toxicity (seizures)

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caution of PCN use in the longterm

neutropenia

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interstitial nephritis in PCN use

Symptoms and action

inc BUN
inc creatinine
inc in eiosiniphils
potential fever

will have to stop the drug.

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absorption of PCNs is hindered by

susceptible to first pass effect

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peak concentration of PCNs

1-2 hours

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half life of PCNs

short

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distribution of PCN

widely distributed to tissues/fluids

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metabolism of PCNs

none to minimal hepatic metabolism

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elimination of PCN (2)

kidneys

some biliary

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natural PCNs are indicated for what organisms? (4)

streptococcal
enterococcus
t. pallidum

-some anaerobes like peptococcous / peptostreptococcus

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natural penicillin drugs (4)

PCN G
PCN V
procaine PCN
benzathine PCN

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distribution sites of PCNs (6)

lungs
ascites
synovium
pericardium
ascitic fluid
soft tissues

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drug of choice for Treponema pallidum (ie: syphilis)

natural PCN

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natural PCN dose adjustment

for CrCl <50

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Natural PCN is the drug of choice for (2)

syphilis

Strep

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aminopenicillins MoA/activity

Same as natural PCN + extended gram negative spectrum.

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Aminopenicillins do not do well with treating

Staph

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Aminopenicillins are more active against ______ than other PCNs.

Enterococcus

drug examples of aminopenicillin (2)

amoxicillin | ampicillin

important point about aminopenicillins

they are not very beta lactamase stable and frequently are targeted by beta lactamase released by bacteria,

distribution of aminopenicillins (4)

renal tissue septic joints ascites CSF (if inflamed meninges)

aminopenicillin is the drug of choice for?

for sensitive enterococcal infections.

when circumstance may aminopenicillin be warranted?

UTIs while pregnant.

penicillinase resistant PCNs (anti staph PCNs) are clinically effective for

staphylococcus aureus *** streptococcal peptrostreptococcal

Penicillinase resistant PCN (anti staph) drug examples (3)

oxacillin nafcillin dicloxacillin

Penicillinase resistant PCNS (anti staph) gram activity

gram positive only. no gram neg activity.

Penicillinase resistant PCNs (anti staph) distribution

``` bone joint cardiac tissue (endocarditis) ```

Penicillinase resistant PCNs (anti staph) are the drug of choice for

MSSA | methicillin sensitive S aureus infections

Why are Penicillinase resistant PCNs (anti staph) the drug of choice against MSSA?

Their structure prevents the B-lactamase made by S. aureus from attacking the B-lactam nucleus.

Penicillinase resistant PCNs (anti staph) dosing and half life

very short half life | give q4 hrs

Penicillinase resistant PCNs (anti staph) dosage adjustment

for severe hepatic impairment

drawback of nafcillin, a Penicillinase resistant PCNs (anti staph)

large sodium content when given IV

elimination of Penicillinase resistant PCNs (anti staph)

hepatic, not renal

Penicillinase resistant PCNs (anti staph) in the renal patient

safe b/c this drug is eliminated by the liver

Ureidopenicillins (Anti Pseudomonal PCNs) product

piperacillin

Ureidopenicillins (Anti Pseudomonal PCNs) known as Piperacillin is indicated in

gram negatives: pseudomonas bacteroides

Ureidopenicillins (Anti Pseudomonal PCNs) known as Piperacillin may also be used for

some enterococcal

Ureidopenicillins (Anti Pseudomonal PCNs) known as Piperacillin works against aerobes or anaerobes?

Mainly aerobes | slight coverage of anaerobes

Ureidopenicillins (Anti Pseudomonal PCNs) known as Piperacillin and staphylococcus

no efficacy

beta lactamase stability of Ureidopenicillins (Anti Pseudomonal PCNs) known as Piperacillin

piperacillin not very beta lactamase stable.

piperacillin is always given with what and why?

a BLI (beta lactamase inhibitor)

Ureidopenicillins (Anti Pseudomonal PCNs) known as Piperacillin distribution

pleural ascities wounds

dose adjustment for Ureidopenicillins (Anti Pseudomonal PCNs) known as Piperacillin

dose adjust for CrCl <50mL/min

Beta-Lactam/Beta Lactamase Inhibitors active against

H influenza M Catarrhalis N gonorrhoeae B fragilis

Beta-Lactam/Beta Lactamase Inhibitors gram activity

gram negative (including anaerobes) and gram positive

Beta-Lactam/Beta Lactamase Inhibitors are very useful in what two scenarios

"mixed" infections | or broad empiric coverage as a single agent

Beta-Lactam/Beta Lactamase Inhibitors - how do they work?

Act as a decoy against the beta lactamase being produced by organism. BLIs block the attack on the B lactam nucleus by absorbing the attack themselves, thus allowing binding to transpeptidase enzymes and disruption of cell wall formation. They have no antimicrobial activity.

Beta-Lactam/Beta Lactamase Inhibitors examples

- Ampicillin/Sulbactam - Amoxicillin/Clavulnic Acid - Pipercillin/Tazobactam

Beta-Lactam/Beta Lactamase Inhibitors distribution

high

Beta-Lactam/Beta Lactamase Inhibitors dose adjustment

CrCl < 50 mL/min

Piperacillin/Tazobactam is the only combo indicated for

psuedomonas

Amoxicillin/Clavulanic Acid (Augmentin) main side effect

diarrhea

General monitoring for PCNs

C&S CBC c diff LFTs RFTs

Pregnancy and lactation considerations for PCNs (3)

Category B Crosses Placenta Excreted in milk

What population is most susceptible to the side effects of PCNs?

newborns and geriatric

Which natural PCN requires hepatic dose adjustment?

PCN G

In general, PCNs are great against

staph strep & some PCNs have broader activity

likely to see interstitial nephritis in what combo?

PCN with vanco