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HHD Pharm 46/47
Sulfonamides, Trimethoprim, Fluorquinolones, anti TB drugs
30
Medical
Post-Graduate
04/11/2009

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Term
antimetabolites
Definition
alter cellular metabolism by virture of their structural resplance to endogenous compounds

sulfonamides resemble par aminobenzoic acid
Trimethoprim resembles pteridine
Term
sulfonamides and trimethoprim inhibit
Definition
folic acid synthesis
Term
combination of sulfonamides and trimethoprim
Definition
synergistic ant-bacterial effect
Term
resistance is common with
Definition
sulfonamides
Term
fluorqunilones
Definition
selectively inhibit microbial nucleic acid metabolism
Term
sulfonamides
Definition
modest tissue penetrtation, heaptic metabolism
excrection of both intact and acetylated metabolites in the urine
Term
solubility of sulfonamides
Definition
decreases in acidic urine
Term
types of sulfonamides
Definition
short acting
intermediate actiong
long acting
Term
trimethoprin is a structurally similar to
Definition
folic acid
weak base trapped ina na acidic environment
Term
sulfonamide mechanism
Definition
bacteriostatic inhibtors of folic acid syntehsis. mamallian cells don't produce folic acid
Term
trimethoprim action
Definition
slective inhinbtor of bacterial dihydrofolate reductase---> folic acid
Term
the combination oif sulfonamides and trimethorpim
Definition
sequential blockadeof folic acid
Term
resistance to sulfonamides is
Definition
common
plasma mediated
Term
suflonamides action
Definition
gram positive and gram negative proganisms, chlamyidae and nocardia
Term
uses of sulfonamides
Definition
simple urinary tract infetion oral
ocular infections
burn infections
ulcerative colitis
toxoplamosis
Term
suflomethoxazole-trimetoprim
Definition
effective orally in the treatment of urinary tract infections and in resporatory ear and sunus infections caused by H, Influenzae and ,. Cathrhalls
Term
sulfonamides TOxICITY
Definition
HYPERSENSITIVITY
GI
Hematoxicity
nephrotoxicity
drug interactions
Term
fluorquinolone generations
Definition
1st norflexacin gran negativ e bacteria

2nd generations-ciprofolxacina nd ofloxacin have greater activity against gram- bacteria, many gram +cocci, mycobacteria and agents of atypical pneumonia


3rd generation less against - more against + than 2nd genreation

gemifloxacin, moxifloxacin broadest to date
Term
fluoroquinolone pharmacokinetics
Definition
good oral bioavailability and penetrate most tisse. half lives range 3-8 hours
elimination kidney
Term
fluoroquinolone inhibnit
Definition
topoisomerase II DNA gyrase
Term
fluoroquiolones do or do not exhibit post antibiotic effect
Definition
yes like aminioglycosides
Term
resistance to fluoroquinolones
Definition
efflux pumps
Term
fluoroquinolones are effective atgainsts
Definition
urogenitala nad gastroitnestinal gram negatives.

gonococci, e coli klebsiella, camplobacter, enterobacter, psudomonas, almonella, shigella
Term
toxicity to fluoroquinolones
Definition
skin rashes, headache, dizziness, insomnia, abnormal liver function, opportumom,s by c albicans and strepto cocci.
Term
major drugs used in tb
Definition
isonizid, ripamfin, pyrazinamide, ethambutol, streptomycin
Term
isoniazid
Definition
emchanism: inhibitis of mycolic acids,
resistance: emerge if used alone, deletion of kat G gene, or knh A genebactericidal

Pharmkinetics: well absorbed orally and penetrates cells to act on intracellular mycobacteria
acetylation by liver
fast acetylators includign NA-60 -90 minutes
Term
rifampion
Definition
bactericidal
resistance via changes in drug sensitivity of the polymerase often emerges rapidly if the drug is used alone

orally well absorbed

tratment of latent tb can be used alone
helps prevent resistance to dapsone in leprosy

rifampin may be used with vancomycin against mrsa or PRSP
Term
ethambutol
Definition
inhibtis cell wall
rsistance in emb gene
Term
pyrazinamide
Definition
mechanism not known
bacteriostatic
rsoatamce pccirs voa ,uutations in genses tahat encode enzymes involved in
Term
leprosy drug
Definition
dapsone- sulfone
inhibiton of folic acid
acedapsone-
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