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Anti-folates - Coggle Diagram
Anti-folates
ADME
admin
oral
im
iv
topical
high bioavailability
high plasma binding
may have intestin-limited sulfas
moderate Vd
good tissue penetration
metabolism
phase I
phase II conjugation
acetylation
not in dogs though
sulfa short half life
filter at glomerulus
excreted in urine
types by t1/2
short acting
water soluable
rapidly absorbed
rapidly excreted
ex. sulfadiazine
intermediate acting
rapidly absorbed
slowly excreted
ex. sulfadimethoxine
only FD-approved sulfa for dairy cows
intestine-limited
poor soluability
oral bioavailability
bacteriostatic
anti-inflammatory
ex. sulfasalazine
topical
sulfacetamide
silver sulfadiazine
know...
mechanism and specturm
mode of target cell resistance
phrmalogical proerpties
indications
contraindications
toxic effect
resistance
older drug therefore much resistance
types
pseudomonas
intracellular bacteria
many anaerobes
drug susceptibilty testing
mechanisms
change substrate binding site
overwhelm drug with increased target substrate/enzyme
decrease drug entry
trimethoprin-sulf (TMS)
-prims
combo sulfa + diaminopyrimidine "prim"
block two segments of PABA pathway
bacteriostate
faster acting
used alone ofr UTIs
more potent
"potentiated" sulfamide
broader spectrum of action
20:1 is bactericidal
lower = bacteriostatic
genitourinary tissues
airway
grater "prim" drug entry
best ratio for
ocular aqueous humor
synovial fluid
effective against
Nocardia
mechanism
pathway
selective toxicity
inhibit microbial tetrahydrofolic acid synthesis
:red_cross: amino acid synthesis
:red_cross:purines
:red_cross: nucleotide synthesis
Enterococci
uses dietary folate so these won't work on them
bacteria that use PABA to synthesize folic acid
sulfoamides acts as false substrate
broad spectum
bacteriostatic
effective against
aerobes
anaerobes
Clyamidia
characteristics
weak acids
addition of Na salts improve water soluability
unbuffered injections can cause tissue damage
uses
neonatal scours
prostatitis
cystitis
resp infections
UTIs
adverse effects
stopped at 1:16:20