Shared Flashcard Set

Details

Inhibitors of Cell Syn 1
Whitlock
74
Medical
Professional
04/03/2009

Additional Medical Flashcards

 


 

Cards

Term
this lecture focuses primarily on the function of
Definition
penicllin
Term
pencillin discovered by
Definition
accident by fleming
Term
fleming was studying microbes in lab growing cultures, when whe came back one of the cultures had been contaminated by a mold and around that mold there was no
Definition
bacterial growth
Term
in the vicinity of the contamination no growth of
Definition
stpahloccoccus
Term
fleming wondered why there was no
Definition
growth
Term
penicillium notatum
Definition
priduced a substance that killed the acteria
Term
florey and chain developed a purification method for
Definition
penicillin
Term
Fleming's experiment was
Definition
1928
Term
floery and chain also showed
Definition
how it could cure incrable abacteria
Term
n principle drugs that inhibit
Definition
bacterial cell wall synthesis.
Term
penicllin has a narrow spectrum against
Definition
gram negative cocci.
Term
we can change the penicllin molecule to alter its
Definition
affect
Term
because of their safet and lack of toxicity-they are
Definition
The bacteria of choice.
Term
bactericidal and non toxic to human cells
Definition
beta lactam drugs
Term
drug resistance is usually due to the
Definition
creation of a beta lacatamse
Term
pharmaceutical companies have created
Definition
beta lactamase inhibitors
Term
there are some beta lactamases that can't bind to the
Definition
target
Term
MRSA is due to
Definition
a target alteration in a penicillin binding protien.
Term
classes of beta lactams
Definition
penicillin
cealosporin
monobactam
cephalosporins
carpapenams
Term
the hydrogens in carpapenams are in
Definition
trans may confer resistance to beta lactamases
Term
bacterial cell wall syntehseis
Definition
1) syntehssiz the moomer
2) polymerize
3) cross link
Term
nacetyl glucosamine and n acetyl muriamic acid created
Definition
Term
monosacharride with 5 amino acid
Definition
Term
target is unique to bacteria and this makes them
Definition
selectively toxic
Term
each type of beta lactam- you can change subsiituents
Definition
differ in their target, differing ability to traverse porins,

various biological activitie, resistance to beta lactamase.
Term
mono sacchardie plus five amino acids two sugars to which amino acids are added and the process requires UTP

2 alanines on the end are the target

beta lactams
penta peptide attached to a lipid carrier
Definition
Term
bactoprenol transfers the monomer to teh
Definition
outside
Term
the polymer is
Definition
cross linked
Term
the more cross linking the more
Definition
rigid is the plastic
Term
various drugs inhibit different steps.
Definition
bacitracin inhibits monomer
vanvomycin inhibits polymerizations
beta lactams inhibits cross linking
Term
bacitracin inhibits the creation of the
Definition
monomer
Term
vancomycin inhibts
Definition
polymerizations
Term
beta lactams inhibits
Definition
cross linking
Term
cross linking involves a trans peptidase reaction
Definition
d-ala-d-ala
glycine attacks and transpeptidases
glycine--> alanine
Term
penicilling G resemebles
Definition
d-ala d-ala
Term
d-ala d-ala is the substrate for
Definition
transpeptidase
Term
normally there is a transient complex form
Definition
between transpeptidase and dala dala but if it attaches to pencillin then it is a stable bond
Term
penicllin binding proteins
Definition
1) pencillin carbon 14
2) incubate the pencillin with ecoli
3) proteins covalently bond
turns out htey are transpeptidases
Term
some transpeptidases responsible for
Definition
rounded and rod shaped
Term
pencillin binding proteins differe among _____
Definition
bacterial species
Term
PBPs differ in their affinitites towards
Definition
Pencillin binding proteins.
Term
bacteria can differ in their susceptibility to beta lactam drugs because their _____ enaymes are different
Definition
transpeptidase
Term
mutations in ____ can confer resistance to ______
Definition
PBP
beta lactam drugs
Term
why does a staphlyococcus explode
Definition
the cell wall is weakened and the itnernal osmotic presure (hypertonic) so it explodes
Term
What would happen if it were in a hypertonic envronment?
Definition
It might remain intact because without a cell wall
Term
enzymes that cleave beta lactams
Definition
beta lactamase at the n-c bond in bpenicllin-usually acquired via horizontal transmission in plasmid

pencillin acylase-removes acyl subsitituent formt eh beta lactam ring

6-aminipenicllianic acid-a lead compund for generationg new semi-syntehtic penicllins with novel properties. ( new types of drug development)

100 different beta lactamases.

there are drugs that inhibit beta lactamases.
Term
beta lactamase
Definition
c-n bond in the penicllin
Term
penicillin acylase
Definition
the r subsitutent of the penicllin which leaves the 6 aminopenicllanic acid
Term
penicillin acylase
Definition
the r subsitutent of the penicllin which leaves the 6 aminopenicllanic acid
Term
6 aminopenicllanic acid
Definition
lead peptide for new drug development
Term
what properties of penicllin do we want to influence? What ened to happen for a beta lactam to kill a gram negative bacteria?
Definition
beta lactams must penetrate the outer membrane
escape inactivation
bind to target enzymess

resistance can be due to
lack of membrane penetration
inactivation by beta lactams
altered target PBPs
Term
it must be water_______
Definition
to get in to throught he otuer membrane
Term
gram positive makes lots/little beta lactamse
Definition
lots because other wise it will diffuse
Term
in gram negative htey pridcue mroe or less beta lactamse
Definition
less because the outer membrane
Term
resistance cna be due ot
Definition
lack fo membrane penetration
inactivation of beta lactamase
altered target PBPs
Term
semi syntehti drugs
Definition
improve pentration trhough porins
decrease beta lactamase susceptibility, broadening spectrum
alter PBP ninding pattern
Term
pharmacokinetics
Definition
oral forms of various penicllins
subject to inactivation by gastric acid
Term
repository forms (procain penicillin G nad benzathine penicllin G
Definition
absorbed slowly producing prolonged concentrations of drug
Term
procaine
Definition
over a day
Term
benzathine
Definition
over a month
Term
procaine is not used much due to resistance
Definition
Term
benzathine
Definition
sterp pyogenes
strep throat
rehumatic fever/glomerular nefritis
sequelae could kill you
Term
penicllin only enters the CNS
Definition
when the meninges are inflamed
Term
pencillins are _____ and eliminated by the _____
Definition
polar
kidney
Term
Should you increase or reduce the dosage in a person with sever kidne damage
Definition
decrease
Term
many organic acids such as pencillin are secreted via
Definition
kidney
Term
prebenicid is administered, secretions go _____-
Definition
down
Term
when pencillin was first introudced they collected the urine and recrystallized the pencillin
Definition
Term
main type of pencillin toxicity
Definition
hypersensitiity
Term
pencillin G undergoes isomerization t benzopenacyllemic acid and this combines with a protein
Definition
leads to an IgG and an IgE reaction
Term
allergic reactions include
Definition
skin rash, serum sickness, anaphylaxis (IgE)
Term
Go can occur due to aleterations in
Definition
guy flora.
Term
colitis (staph aureus) and mucositis (overgrwoth of c. albicans)
Definition
results from changes to normal flora
Term
in renal filure _____ and ____ can cause seizures
Definition
sodium and potassium
Supporting users have an ad free experience!