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HHD Pharm Chapter 43 Beta lact
chapter 43
82
Medical
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04/02/2009

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Term
penicillins and cephalosporins are the major antibiotics that
Definition
inhibit bacterial cell wall synthesis
Term
beta lactams
Definition
4 member ring with three carbons and one nitrogen
Term
vancomycin is/is not a beta lactam
Definition
not
Term
narrow spectrum cephalosporings
Definition
1st generation
Term
broad spectrum cephalosporin
Definition
2nd 3rd and 4th generation
Term
Pencillins are derivative of
Definition
6 aminopenicallanic acid
cotnain a beta lactam ring structure that is essential for antibacterial activity.
Term
penicillins vary in their resistance to _______ and therefore in their oral_______
Definition
gastric acid
bioavailability
Term
pencillins are ____ compunds that are not _____ extensivley
Definition
polar
metabolized
Term
penicillins are usually___ in the urine via
Definition
excreted
glomerular filtration and tubular secretion.
Term
probenecid inhibits
Definition
tubular secretion
Term
nafcillin is excreted in the
Definition
bile
Term
____ undergoes enteroheepatic cyclign
Definition
ampiciliin
Term
plasma half lives of penicillin
Definition
30 minutes to onne hour
Term
procaine and benzathine forms of penicillin G are adminsitered ______ and have long half lives because________
Definition
intramuscularly
the active drug is released slowly into the blood stream
Term
most penicillins cross the blood brain barrier only when
Definition
the meninges is inflamed
Term
beta lactams are _______ drugs
Definition
bactericidal
Term
steps in beta lactam bactericidal action
Definition
1) binding of drug to the penicillin binding protein in the cell membrane
2) inhibition of the transpeptidatyion reactiont hat cross links linearpeptidoglycan chain contituents of the cell wall
3) activation of autolytic enzyes that lesions the ell wall.
Term
enzymatic hydrolosis of beta lactam ring cuases
Definition
loss of antibacterial activity
Term
The formation of beta-lactamases by ______ and many gram______ organisms
Definition
staphlcocci and gram negative organizms is a cause of resitance.
Term
what inhibits beta lactamases?
Definition
clavulanic acid
sulbactam
tazobacam
Term
what is another mechanism of resistance
Definition
structural changes in the penicillin binding protiens
Term
pneumococcus can get reistant to _______ by alterations int he
Definition
penicillin G
penicillin binding protein
Term
METHICILLIN RSITANCE IS CAUSED BY
Definition
pbp alterations in staph aureus
Term
In some gram negative bacteria like _____, porin changes stop Pencillin from entering and binding to PBP
Definition
psudomonas
Term
narrow spectrum penicillinase suseptible agents
Definition
penicllin G which
sterptococcus has developed resistance to (Pencillin resistance resistant strep pneumo)
Term
penicillin G
Definition
prototype of the subcalass of penicllins that have limited anti bacterial activit ynad are susceptible to beta lactamaases
Term
pencillin G is no good for...still good for
Definition
penicliin G is good for syphillus
no good for gonohrrhea
Term
Pencillin V is
Definition
an oral drug used mainly in oropharyngeal infections
Term
Very narrow spectrum pencillinase resistant drugs
Definition
methicillin
nafcillin
oxacillin
suspected staph inffections
Term
wide spectrum penicillinase susceptible drugs
ampicillin and amoxicilin
Definition
ampicilling and amxocillin
same as peniclling G but remains susceptible to penicillinases

in addition to pen G can do enterococci, listeria, ecoli, proteus heamophlius inf, moraxella

can be combined with inhibitiors of penicllinases
Term
piperacillin and ticarcillin
Definition
activity against several gram - bacteria including
pseudomonas, enterobacter, and some klesiella

synergistic with aminoglycosides
Term
name all the pencillins we know
Definition
g
V
methicllin
naficillin
oxacillin
ampicillin
amoxicillin
peracillin
ticarcilin
Term
Penicllin G
Definition
sterptococci
menigococci
gram positive bacilli
spirochetes
Term
many pneumococci are resistant to
Definition
pencillin
Term
cephalosporins
Definition
dderviatives of 7 aminocephalosporanic acid
contain beta lactam ring
Term
pharmacokinetics of cepalosporin
Definition
some are given orally but most are parentally (iv or intramuscualar)
Term
what is the primary way of excreting cephalosporins
Definition
there is hepatic metaolismbut mainly remal excretion via tbular secretion
Term
Which ceph drugs are excreted in bile?
Definition
cefoperazone
ceftriaxone
Term
even during inflammation _______ and ______ genereation cephalospornis do not cross the ________
Definition
1st and 2nd
meninges
Term
mechanism of cephalosporin
Definition
same as penicillin bind to pbp precent transpeptidases
Term
cephalosporins are less suceptible to ______ than pencillin
Definition
penicillinases prduced by staphlococci
Term
many bacteria can still produce _______ ______ that provide resistnace to cephalosporin
Definition
beta lactamases.
Term
What is another way that resistance to cephalosporins can develop
Definition
decreased permeability o cephalosporin.
Term
MRSA is also resitant to ________
Definition
cephalosporins
Term
First generation cephalospron
Definition
cefazolin (parenteral)
ceohalexin (oral)


active agains gram positve coci including staph and strep

e coli
k penumoniae

surgical proopholaxis
minimal effect against gram negatives, mrsa
Term
2nd generation
Definition
less effective against gram pos
more effective against gram negative when compared with 1st gerenation drugs.
Term
clinic use of second generation
Definition
bacteroides fragilis
h influenzae
moraxella
Term
cefotetan
cefoxitin
Definition
bacteroides fragilis
Term
cefamandole
cefuroximine
cefaclor
Definition
m catrahallios
h influenzae
Term
3rd generation characteristc
Definition
ceftazidime
cefapperazone
cefotaxaime
icnreased activity against g- organisms resistant to other beta lactams

ability to penetrate the blood brain barier
except for (cefoperazone and cefixime)
Term
Third generations are active against
Definition
providenciam, serratia anbd beta lactamase producing h influenzae and neisseria
Term
most active antibiotics to PRSP
Definition
ceftriaxone (parenteral)
cefiximide (oral)
Term
3rd generation cephalosporins
Definition
serious bbusiness infections....gonohrrhea exception
one injhection of ceftriaxone is as effective as 10 days of amoxicillin
Term
4th generation cefepime
Definition
more resistant to beta lactamases produced by fam negative ofganisms including enterobacter
h influenzae neisseria and some penicilling resistant penumococi

combines gram positive of first genreation with broad gram negative affect of thrid generation
Term
allergy to cephalosporins
Definition
allergic reaction from skin rashes to anaphylactic shock


less frequently with cephalosporins than with penicllins

cross hypersensititbity should be assumed.

little cross sesnitivity bw cephalosporins and penicillins
Term
adverse cephalosporin events
Definition
pain at intramuscular injection sitse and phlebitis after iv admin
Term
aztreonam
Definition
monobactam that is resistant to beta lactamases produced by klebsiella, pseudomonas, serratia

no activity against gram positive bnacteria or anerobes

inhibits cell wall syntehsis
administered iv and is eliminated via renal tubular secreation

half life prolonged in renal failure
Term
carbapenems
Definition
contain beta lactam ring but different than peicilin

gram + cocci
for pseudomonas used along with an aminoglycoside.
administred parenreally
MRSA is resistant to these

drug of choice for enterobbacter
meropenem,, ertapenem, imipenem
Term
beta lactamase inhibitors
Definition
clavulanic acid
sulbactam
tazobactan
fixed combinations with certain penicllins (hydrolyzable)
most active against plasmid econded beta lactamases such as those produced by gonococci, streptococi , ecoli and hinfluenzae
Term
vancomycin
Definition
bactericidal glycoprotien that binds to the dala dala terminal of the nascent peptidoglycan pentapeptide side chain and inhinits transglycosolation. itnerferes with corsslinking
Term
vancomycin used for
Definition
srious infection cause dby drug resistant gram positive prganizms
Term
vacp,ycin resistant enterococci are increasing
Definition
Term
vancomycin has a narrow spercturm of activityy
Definition
Term
teicoplanin is like which drug
Definition
vancomycin
Term
toxic effects of vancomucin
Definition
chills, fever, phlenitis, ototoxicity and nephrotoxicity
Term
fosfomycin
Definition
antimetabolite inhibnitor of cytosolic enolpyruvate transferase prevention Nacetyl muriamic acid
Term
bacitiracin
Definition
peptide antibiotic that itnerferes with a late stage in cell wall snthesis in gram positvie organisms

because o fnephrotoxicity dont eat it
Term
cycloserin
Definition
blocks d-ala into pentapeptide side chain of the peptidoglycan -only used as n atlernative tb drug bbecause of neruotoxicity
Term
daptomycin
Definition
new cyclic lipopeptide actiuve against vancomyicn resiustant straisn of entercoocci
may cause myopathy
Term
O2 saturation
Definition
percentaghe of available binding sites that have O2 attached
Term
o2 saturation of arterial blood with Po2 of 100 mm Hg
Definition
97.5 percent
Term
venous blood o2 saturation
Definition
75 percent
Term
oxygenated form of hemoglobin is the
deoxygenated form is
Definition
relaxed state
tense state
Term
advantages of physiology of the sigmoidal hg binding curve
Definition
flat upper poriton means that evenin oif the PO2 falls a but in alveolar gass, loading of O2 will be little affected
Term
steep lower part of the dissociation curve means that
Definition
peripheral tissue can withdraw o2 with small drops in capillary o2
Term
lwo arterial 02 causes
Definition
cyanosis
Term
what causes a right shift
Definition
lower affinity of o2 and hb
increase in h plus, tempartur and 2.3 DPG
Term
higher affinity of 02 and HGb is seen as
Definition
a left shift. this is caused by lower h plus, tmmeparature and 2,3 dpg
Term
a right shift means more unloading of o2 at a given p02 in capillary
Definition
Term
usual p50
Definition
27 mmhg
Term
carbon monoide interfreres with the 02 transport function of blood by combining with Hb to form
Definition
carboxyhemogloin
Term
CO binds to Hb ____ times more than oxygen
Definition
240
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