NITROFURANTOIN

Mark Scyld L.Magboo 2a-ph

USES

. Current indications are treatment of acute and prophylaxis against chronic or recurrent urinary tract infections due to susceptible organisms. For treatment of acute infections, the recommended regimen is 50 to 100 mg orally four times daily for one week. For prophylaxis against chronic or recurrent infections,

USES

THE recommended dose is 50 to 100 mg daily long-term. Generic formulations are available (25, 50, and 100 mg); specific commercial names include Macrodantin, Macrobid and Furadantin among others.

STRUCTURE

The chemical name of nitrofurantoin macrocrystals is 1-[[[5-nitro-2furanyl]methylene]amino]-2,4imidazolidinedione. The chemical structure is the following Molecular Weight: 238.16

STRUCTURE

The chemical name of nitrofurantoin monohydrate is 1-[[[5-nitro-2furanyl]methylene]amino]-2,4imidazolidinedione monohydrate. The chemical structure is the following:

Molecular Weight: 256.17

DILUENTS

Inactive Ingredients: Each capsule contains carbomer 934P, corn starch, compressible sugar, D&C Yellow No. 10, edible gray ink, FD&C Blue No. 1, FD&C Red No. 40, gelatin, lactose, magnesium stearate, povidone, talc, and titanium dioxide.

MECHANISM OF ACTION
Nitrofurantoin, a synthetic, broadspectrum, weakly acidic antibacterial, is generally bactericidal Nitrofurantoin is reduced by bacterial flavoproteins to reactive intermediates, which inactivate or alter bacterial ribosomal proteins and other macromolecules. { These inactivations or alterations of bacterial ribosomal proteins and macromolecules

MECHANISM OF ACTION

cause the inhibition of vital biochemical processes of aerobic energy metabolism and the syntheses of bacterial deoxyribonucleic acid (DNA), ribonucleic acid (RNA), cell wall, and protein

SUSCEPTIBLE ORGANISM
Nitrofurantoin is only clinically proven for use against E. coli or Staph. saprophyticus. It may also have in vitro activity against: Coagulase negative staphylococci Enterococcus faecalis, Staphylococcus aureus, Streptococcus agalactiae, Citrobacter species, and Klebsiella species,

RESISTANT ORGANISM
Enterobacter species[5] Klebsiella species[5] Acinetobacter species, Morganella species, Proteus species,[5] Providentia species, Serratia species, Pseudomonas species.[5]

RESISTANCE

The fact that nitrofurantoin interferes with a variety of bacterial processes may explain the lack of acquired bacterial resistance to nitrofurantoin. The multiple and simultaneous mutations of the target macromolecules that would be required to achieve resistance would probably be lethal to the bacteria

RESISTANCE

Antimicrobial resistances at 126 institutions in the United States testing 100 or more urinary isolates of E. coli against four antimicrobials in 2001.

ABSORPTION
MacrocrystallineMore slowly absorbed and usually causes less gastrointestinal irritation The monohydrate forms a gel matrix upon exposure to gastric and intestinal fluids that releases nitrofurantoin over time. MicrocrystallineRapidly and completely absorbed in the small intestine

REFERENCES
http://www.drugs.com/mmx/nitrofurant oin.html http://www.ncbi.nlm.nih.gov/pmc/articl es/PMC127340/figure/f2/ http://www.ncbi.nlm.nih.gov/pmc/articl es/PMC127340/