Nitrofurantoin: Targeted Relief for Urinary Tract Infections

Nitrofurantoin

Nitrofurantoin

Nitrofurantoin is used for treating and preventing urinary tract infections caused by certain bacteria.
Product dosage: 100mg
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Nitrofurantoin is a prescription antibacterial medication specifically indicated for the treatment and prophylaxis of uncomplicated urinary tract infections (UTIs) caused by susceptible strains of Escherichia coli, Enterococcus faecalis, Staphylococcus aureus, and certain strains of Klebsiella and Enterobacter species. It belongs to the nitrofuran class of antibiotics and is distinguished by its unique mechanism of action and its concentration within the urinary tract, making it ineffective for systemic infections outside this anatomical site. This product card provides a comprehensive, expert-level overview for healthcare professionals to support informed clinical decision-making.

Features

  • Active Pharmaceutical Ingredient (API): Nitrofurantoin (available as macrocrystals or monohydrate/macrocrystals)
  • Standard Available Strengths: 50 mg, 100 mg oral capsules; 25 mg/5 mL oral suspension
  • Pharmacologic Class: Antibacterial; Nitrofuran derivative
  • Mechanism of Action: Disruption of bacterial ribosomal proteins, inhibition of acetylcoenzyme A, and other enzymatic processes, leading to broad antibacterial effects.
  • Bioavailability: Rapid and complete gastrointestinal absorption, with food enhancing bioavailability and reducing gastric upset.
  • Primary Excretion: Renal, achieving high concentrations in urine.

Benefits

  • Provides highly targeted bactericidal activity within the urinary tract, minimizing impact on systemic flora.
  • Effective against many uropathogens that demonstrate resistance to other common antibiotic classes like sulfonamides and penicillins.
  • Offers formulations for both acute treatment (short-course) and long-term prophylaxis for recurrent UTIs.
  • Low incidence of Clostridioides difficile-associated diarrhea compared to broad-spectrum antibiotics.
  • Well-established safety and efficacy profile with decades of clinical use.

Common use

Nitrofurantoin is primarily prescribed for the treatment of acute, uncomplicated cystitis caused by susceptible bacteria. It is also widely used as a prophylactic agent to prevent recurrent urinary tract infections in appropriate patient populations. Its use is confined to urinary tract infections due to its pharmacokinetic profile, which ensures the drug is concentrated in the urine. It is not indicated for the treatment of pyelonephritis or perinephric abscesses due to inadequate tissue penetration.

Dosage and direction

Dosage is contingent upon the indication (treatment vs. prophylaxis), renal function, and the specific formulation.

  • For acute, uncomplicated UTIs (treatment):

    • Nitrofurantoin macrocrystals/monohydrate: 100 mg orally twice daily for 5 days (for non-pregnant patients) or 7 days (standard course).
    • Nitrofurantoin macrocrystals: 50 to 100 mg orally four times daily.
    • Should be taken with food or milk to improve absorption and minimize nausea.
  • For long-term prophylaxis of UTIs:

    • Typically, 50 to 100 mg orally once daily at bedtime.

Critical Note: Dosage must be adjusted in patients with impaired renal function (creatinine clearance under 60 mL/min or clinically significant elevated serum creatinine) due to reduced efficacy and an increased risk of toxicity. Use is contraindicated in patients with a creatinine clearance below 60 mL/min for treatment and under 40-60 mL/min for prophylaxis. Always adhere to the specific prescribing information.

Precautions

  • Pulmonary Reactions: Acute, subacute, or chronic pulmonary reactions (e.g., interstitial pneumonitis, pulmonary fibrosis) have been reported and can be fatal. Monitor for pulmonary symptoms (dyspnea, cough, fever). Discontinue immediately if they occur.
  • Hepatic Reactions: Rare instances of hepatic toxicity, including hepatitis and cholestatic jaundice, can occur. Monitor liver function in patients with pre-existing liver disease.
  • Hemolytic Anemia: May occur in patients with glucose-6-phosphate dehydrogenase (G6PD) deficiency. Use with caution in patients near term during pregnancy, neonates, and those of Mediterranean, African, or Asian descent. Screen for G6PD deficiency if suspected.
  • Peripheral Neuropathy: Potentially irreversible sensory or motor polyneuropathy has been reported. Risk factors include renal impairment, anemia, diabetes, electrolyte imbalance, vitamin B deficiency, and debilitating disease.
  • Clostridioides difficile-Associated Diarrhea (CDAD): Reported with nearly all antibacterial agents. Evaluate if diarrhea occurs during or after therapy.

Contraindications

Nitrofurantoin is contraindicated in patients with:

  • Known hypersensitivity to nitrofurantoin or other nitrofuran derivatives.
  • Significant renal impairment (creatinine clearance < 60 mL/min or clinically significant elevated serum creatinine) due to inadequate drug delivery to the urine and increased risk of systemic toxicity.
  • A history of cholestatic jaundice or hepatic dysfunction previously associated with nitrofurantoin use.
  • Pregnancy at term (38-42 weeks gestation), during labor and delivery, or when the onset of labor is imminent, due to the risk of hemolytic anemia in the neonate.
  • Infants under one month of age, due to the risk of hemolytic anemia.

Possible side effect

Common side effects are typically gastrointestinal and often dose-related. More serious reactions, while less common, require immediate medical attention.

  • Very Common (>10%): Nausea, headache.
  • Common (1-10%): Anorexia, vomiting, flatulence, abdominal pain, diarrhea, drowsiness, dizziness.
  • Uncommon (0.1-1%): Pulmonary sensitivity reactions (dyspnea, cough, chest pain), rash, pruritus, urticaria, transient alopecia.
  • Rare (<0.1%): Anaphylaxis, angioedema, asthmatic attack, hepatitis, cholestatic jaundice, pancreatitis, peripheral neuropathy, optic neuritis, leukopenia, granulocytopenia, hemolytic anemia, megaloblastic anemia, eosinophilia.

Drug interaction

  • Probenecid and Sulfinpyrazone: Concomitant use is not recommended. These uricosuric drugs inhibit the renal tubular secretion of nitrofurantoin, resulting in increased serum levels and decreased urinary levels, thereby reducing antimicrobial efficacy and increasing the risk of systemic toxicity.
  • Antacids containing Magnesium Trisilicate: May reduce the absorption and bioavailability of nitrofurantoin, leading to lower urinary concentrations and potential therapeutic failure. Administer nitrofurantoin at a different time.
  • Drugs with Neurotoxic Potential: Co-administration with other drugs known to induce peripheral neuropathy may increase this risk.
  • Uricosuric Agents: See Probenecid.

Missed dose

  • If a dose is missed, it should be taken as soon as it is remembered.
  • However, if it is almost time for the next scheduled dose, the missed dose should be skipped, and the regular dosing schedule resumed.
  • Do not double the dose to make up for a missed one.

Overdose

  • Symptoms: Primarily expected to be nausea and vomiting due to the drug’s local GI irritant effects.
  • Management: Emesis may occur spontaneously. Treatment is supportive and symptomatic. There is no specific antidote. Hemodialysis may be of limited value due to nitrofurantoin’s rapid elimination and high protein binding but may be considered in severe cases.

Storage

  • Store at room temperature (20°C to 25°C or 68°F to 77°F), in a tight, light-resistant container.
  • Keep out of reach of children and pets.
  • Do not use after the expiration date printed on the packaging.
  • Do not flush medications down the toilet or pour them into a drain unless instructed to do so.

Disclaimer

This information is intended for educational and informational purposes only for healthcare professionals and is not a substitute for professional medical advice, diagnosis, or treatment. The content provided is based on general prescribing information and may not encompass all possible uses, directions, precautions, interactions, or adverse effects. Always seek the advice of a qualified physician or other authorized health provider with any questions you may have regarding a medical condition or before making any changes to a treatment plan. Never disregard professional medical advice or delay in seeking it because of something you have read here.

Reviews

  • “Nitrofurantoin remains a first-line cornerstone in my practice for uncomplicated cystitis. Its targeted action and favorable resistance profile make it invaluable, though vigilance for pulmonary and hepatic reactions is paramount.” – Urologist, 15 years experience.
  • “An excellent choice for UTI prophylaxis in appropriate patients with normal renal function. The once-daily dosing promotes excellent adherence.” – Infectious Disease Specialist.
  • “While effective, the GI side effect profile can be challenging for some patients. Administering with food is non-negotiable for tolerability.” – General Practitioner.
  • “Its contraindication in renal impairment is a critical prescribing point that cannot be overemphasized to avoid treatment failure and toxicity.” – Clinical Pharmacist.