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64 Cards in this Set

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what are all penicilans derived from?
6 aminopenicillanic acid and contain a beta lactam ring essential for antibio activity.
Are they polar compounds?
How are they excreted?
yes, they are polar and are not metabolized extensively.

they are usually excreted unchanged in the urine via gf and ts, ts being inhibited by probenecid.
where are ampilcilin and nafcilin partly excreted?
bile
what are the normal halflives for most penicilans?
from one half to 1 hr.
which penys are administered IM and what are there halflives?
procaine and benzathine forms of peny with a long half life due to slow release into the bloodstream.
when do they cross the bbb?
only when the meninges are inflamed
what is the MOA of beta lactams?
bactericidal and act through the following steps.
1. binding of the drugs to specific receptors (peni binding receptors located in the bact. cytoplasm.
2. inhibit the transpeptidase enz that acts to cross link linear peptidoglycan chains which form part of the cell wall.
3. activation of the autolytic enzymes that cause lesions in the bac cell wall.
what is a major mechanism for bacterial resistance?
beta lactamases formation by most staphylococci and gram -
what are used in combination with penys, to inhibit bacterial enzymes inactivation
clavulanic acid, sulbactam, tazobactam
what is responsible for the methacilin resitance in staph and for peni g resistance in pnuemococci?

in which bateria is a change in the porin structure in the outer membrane contribute to resistance?
structural changes in the PBP

in gram- rods like pseudomonas aeruginosa, therefore impeding the access to PBP´s.
what is the proto of the subclass of penys with limited spectrum of antibio act and are still susceptible to beta-lac?

which is the drug used for oropharyngeal infections?
peni g and used in infections for strep, meningococci, gram + bacilli and spirochetes. DOG of syphylis, active against enterocci enhanced by aminoglycosidic antibiotics

peni-V
how are most strains of staph aureus and n.gonorraea resistant to peny´s?
through the production of beta lactamases.
What are in the subclass of very narrow spectrum, peni-resistan drugs?
methicillin (proto)
nafcilin, and oxacilin used to treat known staphylococcal infections. if resistant to methicilin (MRSA) then also resistant to others.
what are the wider spectrum peni-suseptible drugs?
ampicilin and amoxicilin broader activity than peni g used in similiar infections where peni g is used. include: enterococci, listeria monocytogenes, escherichia coli, proteus mirabilis, h influenza, and moraxella catarrahlis. when treating enterococci and listeria, ampicilin is synergistic with aminoglycosides.
which drugs are used for gram- rods, pseudomonas, enterobacter, and in some cases, klebsiella species?
peperacillin and ticarcillin, and also exhibit enhanced activity with penicilinases.
what are the alergic rxs of penys?
urticuria, severe pruritis, fever, joint pain, swelling, hemolytic anemia, nephritis and anaphalaxis
which peni causes nephritis more often?
methicilin
which is with associated with neutopenia?
nafcilin
what are some antigenic determinants of peny´s?
degredation products like penicilloic acid, and complete cross allerginicity between penis should be assumed.
is the macular popular rash caused by which an alergic reaction?
no, not an allergic reaction by ampicilin
what is the proto of the subclass of penys with limited spectrum of antibio act and are still susceptible to beta-lac?

which is the drug used for oropharyngeal infections?
peni g and used in infections for strep, meningococci, gram + bacilli and spirochetes. DOG of syphylis, active against enterocci enhanced by aminoglycosidic antibiotics

peni-V
how are most strains of staph aureus and n.gonorraea resistant to peny´s?
through the production of beta lactamases.
What are in the subclass of very narrow spectrum, peni-resistan drugs?
methicillin (proto)
nafcilin, and oxacilin used to treat known staphylococcal infections. if resistant to methicilin (MRSA) then also resistant to others.
what are the wider spectrum peni-suseptible drugs?
ampicilin and amoxicilin broader activity than peni g used in similiar infections where peni g is used. include: enterococci, listeria monocytogenes, escherichia coli, proteus mirabilis, h influenza, and moraxella catarrahlis. when treating enterococci and listeria, ampicilin is synergistic with aminoglycosides.
which drugs are used for gram- rods, pseudomonas, enterobacter, and in some cases, klebsiella species?
peperacillin and ticarcillin, and also exhibit enhanced activity with penicilinases.
what are the alergic rxs of penys?
urticuria, severe pruritis, fever, joint pain, swelling, hemolytic anemia, nephritis and anaphalaxis
which peni causes nephritis more often?
methicilin
which is with associated with neutopenia?
nafcilin
what are some antigenic determinants of peny´s?
degredation products like penicilloic acid, and complete cross allerginicity between penis should be assumed.
is the macular popular rash caused by which an alergic reaction?
no, not an allergic reaction by ampicilin
which oral peny is associated with d and vom?
ampicilin (also associated with psuedomembranous colitis).
Gi upset can be caused by what?
GI irritation or direct overgrowth of g+ or yeasts.
what need to be cautioned when a patient as renal and cadiovascular ds.?
toxic effects of Na and K when high doses of peni´s salts are used.
what are cephalosporins derived from?
7 aminocephalosporanic acid and also contain the betalactam ring. and classified as 1, 2, 3, and 4 generation in order of their introduction
what is the major admin of cefs?
parenterally and some orally.
cefs with wide chains undergo what type of metabolism?
hepatic but major elimination is through renal excretion via active tubular secretion.
which are excreted mainly inthe bile?
cefoperazone and ceftriaxone
do 1 and 2 generation cefs enter the meninges when the brain is inflamed?
no
MOA?
same as peni´s and are cidal against suseptibal organisms. due to their structure, cefs are less suseptible to penicillases produced by staph, but other bac produce cilases that inactivate cefs. most MRSA are also resistant to cefs.
what are 1 gen cefs?
cefazolin and cephalexin and used against gram + cocci including staphand common strep. e. coli and k. pneumonia are also sensitive. these can also be used in surgical prophilaxis in selected conditions.

what are they not affecive against? gram - cocci, entero cocci, meth resistan cocci and most gram - rods
2 generation are?
have an extended g - activity but less effective against g+
which 2nd gen are used for bacteroides fragilis?
cefotetan and cefoxitin
which are used for h. influenza or moraxella catarrhalis?
cefuroxime and cefactor
what are the istics of 3rd gen?
(cefoperazone, cefatoxime)increased g- activity of org. that are resistant to other beta lactams and ability to penetrate the bbb, except for cefoperazone and cefixime.
what are most 3rd act against?
enterobactor, providencia, serratia marcescens, and betalactamase producing stains of h. influenza and neisseria. (3rds, usually reserved for meningitis.)
which is active against pseudomonas?
ceftazidime
act. against b. fragilis?
ceftizoxime
which are the DOC of gonorrhea?
ceftriaxone (also for acute otitis media active for 10 days) and cefixime
4th?
cefipime, more resistant to betalactamases produced by g- including, enterobacter, heamophilus, neisseria.
toxicity range from ?
allergic rx to anaphilactic shock but occure less frecuently than with peny´s. incomplete cross reaction between penis and cefs. never give cefs to patient with anaphylaxis to peni´s.
adverse effects?
pain in the IM injection site and phlebitis after iv. may increase nephrotox of aminoglycosides when combined.
which can cause hypoprothrombinemia and disulfiram like rxns?
methylthiotetrazole group (cefoperazone, cefotetan, moxalactam--can decrease platelet fx and cause severe bleeding)
which is the monobactam that preferentially binds to PBP3
aztreonam, and adverse effects include possible super infection, vertigo and headache, and rare hepatotoxicity. NO cross rx with peni´s
which have low suseptibility to betalactamases?
carbapenams (imipenam--doc of enterobacter and meropenam), against g-cocci, g+rods, anaerobes
adverse effects by imi are?
gi distress, at high Cp cns toxicity (confusion, encephalopathy, seizures) mero--no seizures
where are beta lactam inhibitors useless (clavu, etc)
inducible chromosomal beta lactamases formed by enterobactor and pseudomonas.
which binds to the d-ala, d-ala terminal of the nascent peptidoglycan and inhibits transglycosolation?
vancomycin, therefore interferes with elongation and cross linkage. can become resistant when change end to d-ala, d-lactate.

used in MRSA, peni resistant pneumococci, and c.difficle!
inhibits enolpyruvate transferase
fosfomycin, therefore prevents formation of n-acetlymuramic acid, the precursor molecule of peptido glycan chain formation. synergistic with beta lactam and quinolone antibxs.
interferes with the late stage cell wall formation in g+, and only used topically do to it´s nephrotox
bacitracin
blocks the incorp. of d-ala into the pentapetide chain of the peptidoglycan. used only to treat TB caused by organisms resistant to first line TB agents?
cycloserine (potential neurotox---tremors, seizures, psychosis
proto for 4?
cefepime
proto for 3?
cefoperazone
2?
cefamandole
1?
cefazoline