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Nitrofurantoin: Tejal Khade Assistant Professor KGRDCP & Ri

Nitrofurantoin is an antibiotic used to treat and prevent urinary tract infections. It is activated by bacterial enzymes and forms reactive intermediates that damage DNA, allowing it to selectively kill bacteria in the urinary tract. It is effective against many E. coli and enterococci strains but most Proteus, Pseudomonas, Enterobacter, and Klebsiella are resistant. It is absorbed from the GI tract and excreted unchanged in the urine, achieving high concentrations to treat urinary infections. Common side effects include nausea and hypersensitivity reactions. It is contraindicated in patients with renal impairment or hepatic disease.

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102 views10 pages

Nitrofurantoin: Tejal Khade Assistant Professor KGRDCP & Ri

Nitrofurantoin is an antibiotic used to treat and prevent urinary tract infections. It is activated by bacterial enzymes and forms reactive intermediates that damage DNA, allowing it to selectively kill bacteria in the urinary tract. It is effective against many E. coli and enterococci strains but most Proteus, Pseudomonas, Enterobacter, and Klebsiella are resistant. It is absorbed from the GI tract and excreted unchanged in the urine, achieving high concentrations to treat urinary infections. Common side effects include nausea and hypersensitivity reactions. It is contraindicated in patients with renal impairment or hepatic disease.

Uploaded by

Akshada bhangre
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© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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NITROFURANTOIN

Tejal Khade
Assistant Professor
KGRDCP & RI
Introduction
• Nitrofurantoin is a synthetic nitrofuran that is used
for the prevention and treatment of infections of
the urinary tract.
Antimicrobial Activity
• Enzymes capable of reducing nitrofurantoin appear to be crucial for its
activation.
• Highly reactive intermediates are formed, and these seem to be responsible
for the observed capacity of the drug to damage DNA.
• Bacteria reduce nitrofurantoin more rapidly than do mammalian cells, and this
is thought to account for the selective antimicrobial activity of the compound.
• Bacteria that are susceptible to the drug rarely become resistant during
therapy.
• Nitrofurantoin is active against many strains of E. coli and enterococci.
• However, most species of Proteus and Pseudomonas and species of
Enterobacter and Klebsiella are resistant.
• Nitrofurantoin is bacteriostatic for most susceptible microorganisms at
concentrations of ≤32 μg/mL or less and is bactericidal at concentrations of
≥100 μg/mL.
• The antibacterial activity is higher in an acidic urine.
Pharmacology
• Nitrofurantoin is absorbed rapidly and completely
from the GI tract.
• The macrocrystalline form of the drug is absorbed
and excreted more slowly.
• The plasma t1/2 is 0.3-1 hour; ~40% is excreted
unchanged into the urine.
• The average dose of nitrofurantoin yields a
concentration in urine of ~200 μg/mL.
• This concentration is soluble at pH >5, but the urine
should not be alkalinized because this reduces
antimicrobial activity.
• Nitrofurantoin colors the urine brown.
• The oral dosage of nitrofurantoin for adults is 50-
100 mg four times a day with meals and at
bedtime, less for the macrocrystalline formulation
(100 mg every 12 hours for 7 days).
• The daily dose for children is 5 to 7 mg/kg but may
be as low as 1 mg/kg for long-term therapy.
• A course of therapy should not exceed 14 days, and
repeated courses.
Adverse Events
• Nausea, vomiting, and diarrhea; the macrocrystalline preparation is
better tolerated than traditional formulations.
• Various hypersensitivity reactions occur occasionally like chills, fever,
leukopenia, granulocytopenia, hemolytic anemia (associated with G6PD
deficiency), cholestatic jaundice, and hepatocellular damage.
• Chronic active hepatitis is an uncommon but serious side effect.
• Acute pneumonitis with fever, chills, cough, dyspnea, chest pain,
pulmonary infiltration, and eosinophilia may occur within hours to days of
the initiation of therapy; these symptoms usually resolve quickly after
discontinuation of the drug.
• Elderly patients are especially susceptible to the pulmonary toxicity of
nitrofurantoin.
• Megaloblastic anemia is rare.
• Various neurological disorders are observed occasionally. Headache,
vertigo, drowsiness, muscular aches are readily reversible, but severe
polyneuropathies with demyelination and degeneration of both sensory
and motor nerves have been reported.
• Contraindicated in renal impairment, pregnancy and neonates.
Clinical Uses
• Nitrofurantoin is approved only for the treatment of
urinary tract infections caused by microorganisms
known to be susceptible to the drug.
• Currently, bacterial resistance to nitrofurantoin is
more frequent than resistance to fluoroquinolones
or trimethoprim-sulfamethoxazole, making
nitrofurantoin a second line agent for treatment of
urinary tract infections.
• Nitrofurantoin is not recommended for treatment
of pyelonephritis or prostatitis.

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