Antimicrobials Pharm

8/13/2019 Antimicrobials Pharm

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"Drug of Last Choice"(brain abscesses,

typhoid fever, rocky mountain)

Cholarmphenico

1st generation

cephalosporins

clinical uses (name

the drugs)

Sugical prophylaxis

Soft tissue infections

Cefazolin (p)Cephalexin (o)

Cefadroxil (o)

2nd generation

cephalosporins

clinical uses (name

the drugs)

intra-abdominal infections

Cefoxitin (p)

Cefotetan (p)Cefuroxime (o)

Cefprozil (o)

All lactams have

sulfur in their

structure, what is th

purpose of this?

increase lipid

solubility andhypersensitivit

Aminoglycosid

toxicity

nephrotoxicity ototoxicity

not for pregnantneuromuscular blocka

Aminoglycosides

Chloramphenicol

Macrolides

Tetracyclines

StreptograminsLinezolid

Clindamycin

Tigecycline

Inhibit bacteria

protein synthesi(translation)

Aminoglycoside

are bacteriostatic?

False...Bacteriocidal...uniq

to this group

Cause misreading of mRN

template

Aminoglycosides demonstrate

concentration dependent killing?

Does it demonstrate post-antibiotic eff

True - high levels of antibiot

facilitate entry through cel

wall and membrane

Ampicillin

Amoxicillin

TicarcillinPiperacillin

Extended Range Penicilli

Think (more gram - use

amoxicillin = oral mode

ampicilin = parenteral/or

As one moves down the

generations of

cephalosporins what is th

general trend in terms o

spectrum of activity?

Tend to be mor

effective againsGram - bacteria

Augmentin

amoxicillin +

clavulonic acid

Bacteroides infectio

would be suitable t

be treated with Aztreonam

False....NO

Anaerobes

Bacteroides, clostridium

and actinomyces are alrelevant organisms to b

treated with

aminoglycosides

False...dont treatanaerobes

Killing mechanism is Odependent uptake

Besides Clavulonic

acid what are othe

Beta-Lactamaseinhibitors?

Sulbactam

Tazobactam

Amoxicillin-Clavulanic Acid - Augment

Ticarcillin/Clavulanic Acid - Timentin Ampicillin/Sulbactam - Unasyn P

Piperacillin/Tazobactam - Zosy P

Blurred vision

GI disturbancesProlonged QT interval

Exacerbation of

Myasthenia gravis

Telithromycin

Toxicity symptoms

Cefatrixone

treats what the best?

3rd generation -> H Influenzae

and Gram -, Lym

Cefazolin (p)

Cephalexin (o)Cefadroxil (o)

First generation

Cephalosporin

Cefepime (p)

4th generation

cephalosporin

Cefepime is

used to tx what

4th generationcepha-->

pseudomonas

Cefotaxime (p)

Ceftriaxone (p)

Ceftazidime (p)Cefdinir (o)

3rd generation

cephalosporin

Cefotetan tx

what the best?

2nd generation

--> Bacteriode

Cefoxitin (p)

Cefotetan (p)

Cefuroxime (o)Cefprozil (o)

Secondgeneration

cephalsporins

Ceftazidime

used to tx what

3rd generation

--> pseudom

Cephalosporin

Toxicity

Allergic/Hypersensitivity

Cross allergy/sensitivity bw penicillins and cephalospo

uncommon

Disulfiram-like reaction (cefoperazone) (ingestion with

alcohol produced headache, nausea, vomiting, abdomi

Bleeding diathesis

Phlebitis

Biliary obstruction

CephalosporinDO NOT tx

listeriaatypicals

MRSA enterococci

Cephalosporinexcreted into

biliary tract

Ceforperazone(3rd generation

Ceftriaxone (3rd

Chloramphenicolmechanism of

action

binds 50s subunit

inhibits peptidyl

transferase bacteriostatic

Chloramphenicolmechanism or

resistance

plasmid mediated producti

of antibiotic inactivatingenzyme (acetyl transferase

Reduced permeability of bacterial organism to drug

Clavulonic Aci

beta-lactamase inhibit

often used with

penicillins to enhanceaction

Clindamycin isprimary

absorbed?

Clindomycinused against

what spectrum

Gram + and

Anaerobes

NOTENTEROCOCCI

Clinical uses o

aminoglycoside

less potent when used alone often

less potent when used alone...often

combination

synergistic with cell wall active dru

gram - nosocomial

empirically for neonatal infections1st and 2nd line against

mycobacterial infections

Clinical Uses o

penicillin

t h iti

strep pharyngitis

rheumatic fever

prophylaxissyphilis

Clinical uses o

Tetracyclines

prostatitisgingavitis

Concentrates inphagocytic cells

and other tissue

Azithromycin

Concentrates inrespiratory

secretions

Macrolides

Daptomycin isused in all age

groups?

False..notapproved for

children

Daptomycinmechanism of actio

and clinical uses

new lipopeptide antibiotic...IV only

p p p y

Cidal --> disrupts multiple aspects of bacteriplasma membrane function --> inhibits cell w

Resistance mechanism not yet defined

Skin and soft tissue infections, sepsis,

endocarditis (resistant gram + infections)

Difference in

excretion bw

tetracycline anddoxycycline

tetra = urine

doxy = feces

Do penicillin crosseinto CNS, prostate

and eye

Minimally

DOC for borellia

bergdorfi?

Ceftriaxone -->

3rd generation

DOC for

legionella

think atypical

Think Macrolide

KAPLAN FACT

DOC for nosocomilife threatening

diseases

Imipenem/Meropene

DOC fo o al

DOC for oral

treatment of

animal bites

Augmentin

(ampicillin +

clavulonic)

DOC for Rocky

Mountain

Spotted Fever

tetracycline

DOC fortularemia, TB an

Bubonic blague

DOC of Atypica

Mycobacteria

Clarithromycin

(macrolide)

DOC of Atypica

Organisms

macrolides/ketolid

DOC of C Diff

Metronidazole

May have to use it afterampicillin side effect

2nd DOC = oral vancomycKAPLAN FACT

DOC of Salmonella(typhoid) and

bordatella pertussi

Azythromycin

(macrolide)

DOC to treat

syphillis

Drugs that are

contraindicated

in children

Daptomycin

Tetracycline

(tigecycline)

Enterococcus

infection would be

suitable to be treate with Aztreonam

False only use

False...only use

this drug with

gram - rods

Extended Range

Ampicillin/AmoxicilliPenicillins Tx what

bugs? what clinical use

B.H. HEELS

Borrelia, H pylori, H influenzae,Entorocci, E coli, Listeria, Strep pneum

Otitis media, sinusitis, pneumonia, Ulyme

Give an exampl

oxazolidione

Linezolid = first in

Blocks 50s initiatioBacteriostatic

Gray-Baby

Syndrome

Chloramphenicol can be

conjugated because of

immaturity/decreased lev

of glucuronsyl transferas

Groups/Names of drug

that inhibit bacterialprotein synthesis

(translocation)

Aminoglycosides

Chloramphenicol

MacrolidesTetracyclines

Streptogramins

LinezolidClindamycin

Tigecycline

Idiosyncratic/dosrelated aplastic

anemia

chloramphenico

toxicity

If i use combo a

tetracycline with a betlactam how would you

describe the relationshi

Antagonistic

Static and Cidal

If it ends in "-

thromycin"

Macrolides

Imipenem

excretion

Administered with Cilastatin which

inhibits renal inactivation

(dehydropeptidase effect) to prevekidney metabolism from occurring

too quickly

Dont mix...co-administer

Possible seizure side effect

Imipenem toxicit

can cause

seizures and/o

renal failure

Inhibit cell wallsynthesis

(6 categories/drugs

Penicillins

Cephalosporins

Aztreonam

Meropenem/Imipenem

VancomycinDaptomycin

Inhibits

cytochrome

Chloramphenicol

Macrolides

(exception =azithromycin)

Jarish

Herxheimer

Systemic side effects results frompenicillin during treatment of syphill

Also seen with Tetracyclines

Linezolid has

bioavailability?

yes 100%

Linezolid

mechanism of

resistance

decreased affinity of

antimicrobial agent to bacterial target site

(target alteration)

Linezolid would be

preferred over whic

cell wall inhibitor?

Loves the bone and

stays active

Used to txosteomyelitis

Clindamycin

Kaplan fact

Macrolides

mechanism of

action

bind to 50s subunit

prevents ribosomaltranslocation down mRN

Bacteriostatic

Mechanism of

action of

Aminoglycoside

Binds to 30s subunit of

bacterial ribosome

Bacteriocidal Inhibitor of

protein synthesis

Mechanism of

action of

synercid

binds to 50 s

preventstranslocation

Bacteriocidal

production of inactivating

enzyme (methyltransferases)

Target alteration that alters 5 binding

increased effluxdecrease permeability

Most potent

lactam

Imipenem/meropene

Name 3

tetracyclines

doxycycline

minocycline (tigecyclinetetracycline

Kaplan fact: demeclocyli

Only one in its class

(protein translationinhibitor)

Rarely used today in the U because of feared toxicit

Chloramphenico

Oxacillin

NafacillinDicloxacillin

MethicillinCloxacillin

Penicillinase-

Resistant

Penicillin

Penicillin G and V

used to tx all strain

Syphilis

GAS (strp

pyogenes)

Pharmacology of

Aminoglycosides?Oral?

excretion?activity is _____ depende

Not absorbed orally, the

are polarRenal excretion

pH dependent - acidosimay decrease activity

Precludes widespread us

drug interactions, phlebi40%, jaundice 30%,

arthralgia and myalgia 20

Synercid

Toxicity

Probenecid

Blocks

Penicillin

Excretion

Protein Inhibitors

Contraindicated in

pregnancy

Aminoglycosides

TetracyclineMacrolides (excep

azithromycin)

These protein synthesis

inhibitors work on the 30

subunit

Aminoglycosides

block initiationTetraclycines block

These Protein Synthesi

inhibitors work on the 50

subunit

Linezolide - blocks initiation

Streptogramins block A site

hl h i l bl id

Chloramphenicol blocs peptid bond

Macrolides/Clindamycin bloctranslocation

Psuedotumor

Tetracycline toxicity

( i li )

(tigecycline)impairs CSF reabsorption

-> increase cranial pressu

Macrolide toxicity

KAPLAN FACT lid

KAPLAN FACT --> macrolideincrease GI distress by

stimulating motlin receptors -increased peristalsis

Red Man

syndrome...otherside effects in sam

Side effect of this

drug can be contac

dermatitis

Neomycin - aminoglycosi

Found in triple Ab ointme

(neosporin) used topicall

KAPLAN FACT

Side effects includ

transient muscle

weakness, myalgia

Daptomycin

Side effects of

P i ilil

Penicililn

Toxicity

Allergic hypersensitivity, rash, urticaria

GI distress, diarrhea

Seizures

SeizuresHametologic -penias, anemia (coombs

nephritis (especially Methicillin)

drug fever

Chl h i

Chloramphenico

Someone has a macrolid

resistnat strain of

resistnat strain of pneumococci...what drug

I give

Someone Has a Staph

infection hat o ld b

infection, what would bthe progression of dru

to use to try to cure?

Penicillin/Methicill

--> Vanco -->Linezolide -->

Daptomycin

Someone is allergic to

Penicillin, and has a

Pseudomonal

infection...what drug

should i give them?

AZTREONAM

resistant to beta lactamases

resistant to beta lactamasesTx gram - rods

NO CROSS ALLERGENICITY WIPENICILLS/CEPHALOSPORIN

Specturm of

Linezolid

All aerobic gram +

i i ll

organisms especiall

resistant strains

Streptogramins

(Synercid) typicall

used to treat?

VRSA/VRE

according to

Kaplan

e amples of

examples of

aminoglycoside

Tetracycline

mechanism of

action

Bacteriostatic

Binds reversible to 30

Binds reversible to 30subunit of ribosome

Inhibits A-site

Tetracycline

mechanism of

resisitance

facilitated efflux o

decreased entry

Tetracycline

toxicity

GI - nausea, abd pain, diarrheaFetal and childhood effects on bon

and teeth

Liver necrosis with doxy

Nephrotoxic

Photosensitivity/toxicity --> get rain sun

Tetracyclines

cannot be taken

with food...why

chelators

(ca/mg)

Tetracyclines

usually used to

Atypicals (mycoplasma,chlamydia, chancroid,

rickettsia, borrelia, entamoeb

**macrolides are preferred DOfor atypicals

This cell wall

inhibitor is known t

inhibitor is known thave a "post-

antibiotic effect"

Daptomycin

This cell wall

inhibitor is not

lactam

Vancomycin

This cephalosporin is know

to cause biliary obstructio

when rapidly infused

Ceftriaxone (3r

generation) >

generation) -->

excreted in bile

This macrolide is considered

be safer for use during

pregnancy because it is more

water soluble then the rest of

class and does not inhibit p45

Azithromycin

This penicillin

causes interstital

nephritis

This penicillin is

mostly excreted int

the biliary tract

This protein synthesis inhibitmay be associated with

incidence of d b liti ?

pseudomembranous colitis?

which cell wall inhibitor isrelated?

Clindamycin

Ampiciliin

This specific tetracyclin

is metabolized in lived h ti

is metabolized in liveand can cause hepatic

necrosis

Thrombocytopenia,

neutropenia

Reversible Bone marrow

suppression

weak MAO inhibitor

Linezolid toxicity

Ticarcillin and

Piperacillin tx

Gram negative microbesEspecially Pseudomonas,

Bacteroides and E. Coli, ProtePiper > Ticar

Piper > Ticar

Tx mixed-intra abdominalabscesses

Tigecycline is used

for what spectrumdi ? d h

for what spectrum diseases? and wha

clinical uses

Tigecycline

mechanism of

action

new glycylcycline derivative of minocycline for IV use only

High affinity binding to 30s unit o

ribosome to block A site

No known resistance yet

Aminoglycosidedecrease ACh, similar to

Botulism

Gentamycin specifically

Treats gram -b i f ti

Treats gram bone infection

quinilones

(dont confuse withclindamycin)

( clindamycin)

KAPLAN FACT

Used for bell'sl

Used for bell spalsy

tetracycline

Vancomycin

mechanism of

action

binds to D-ala-D-alamuramyl pentapeptide --

blocks transglycosylation

> block elongation of

peptidoglycal cell wall

Vancomycin

used to tx wha

organisms

MRSA, MRSE, Pnemococc

(Gram +)C Diff (but not DOC....that i

C Diff (but not DOC....that i

metronidazole)

What are mechanisms o

microbial resistance to

penicillin?

What are the carbapenem

What is a monobactam

example?

Meropenem (p)Imipenem (p)

Ertapenem (p)

ex of mono = aztreonam (

What does first

generationcephalosporins trea

gcephalosporins trea

Gram +

(strep/staph), somGram -

( p/ p ),Gram -

Cefazolin (p)

What is a unique

characteristic of aztreonam, imipenem

aztreonam, imipenem

and meropenem

All are resistant tobeta-lactamases

beta-lactamases

What is penicillin'

chief mechanism o

action?

What is reccommende

dosage of Aminoglycosides to

Aminoglycosides to

avoid toxicity?

1 or 2 large daildoses each day

What isSynercid?

streptogramin combinaton(quinupristin/dalfopristin)

metabolized and excreted by t

Only IV

What is the

mechanism of reaction for

reaction for

aminoglycosides

Plasmid mediated formation oinactivating enzymes --> grou

transferasesporin protein mutation

decreased affinity of 30s

subunit target

What is the

mechanism of resistance of

resistance of

Vancomycin

D-ala-D-lactatemutation

mutation

it is not a lactam

used to tx Gram +IV only

IV only

NO CNS

What organisms d

Aminoglycosides

work on?

Gram - aerobes

Pseudo-Keeps

Pseudomonas

Klebsiella

E coliEnterobacter

Proteus

Serratia

some gram +

Where is tigecyclinemetabolized/excrete

Liver/biliary

Which carbapenem

is known to

penetrate the CN

Meropenem

Which carbapenem

is not effective

against anaerobes?

Ertapenem

Whichcephalosporins hav

been proven to reac

good CNS levels?

3rd generationCefotaxime (p)

Ceftriaxone (p)Ceftazidime (p)

Ceftazidime (p)

Cefdinir (o)

Which generationcephalosporins use

to tx meningitis?

name the drugs?

Which generation ocephalosporins ha

the best effect

against anaerobes?

2ndCefoxitin (p)

Cefotetan (p)Cefuroxime (o)

Cefuroxime (o)

Cefprozil (o)

Which penicillin is knowto cause GI distress and

lead to C DIFFsuperinfection

superinfection

(pseudomembrane colliti

Ampicillin

Antimicrobials Pharm

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Transcript of Antimicrobials Pharm

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