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Urinary Antiseptics

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Also Known As

Urinary tract antiinfective agents, urinary antibacterials, urinary tract antimicrobials, urinary tract disinfectants, urinary chemotherapeutic agents, UTI prophylactic agents

Definition

Urinary antiseptics are oral agents that exert antibacterial activity in the urine but have little or no systemic antibacterial effect.1 These medications are specifically designed to achieve therapeutic concentrations only in the urine, making them effective for treating and preventing urinary tract infections (UTIs).2 Their primary purpose is to inhibit or kill microorganisms in the urinary tract while minimizing systemic effects.3

Urinary antiseptics work through various mechanisms depending on the specific agent. For example, nitrofurantoin, a common urinary antiseptic, is bactericidal for many gram-positive and gram-negative bacteria through rapid intracellular conversion to highly reactive intermediates by bacterial reductases.4 These intermediates react nonspecifically with ribosomal proteins and disrupt the synthesis of proteins, RNA, DNA, and metabolic processes.4 Other agents like methenamine work by releasing formaldehyde in acidic urine, which has antibacterial properties.5

The usefulness of urinary antiseptics is primarily limited to lower urinary tract infections, though some agents like nitrofurantoin may also be effective against upper tract infections.1,6 Prolonged suppression of bacteriuria with urinary antiseptics may be desirable in chronic or recurrent urinary tract infections in which eradication of infection by short-term systemic therapy has not been possible.1

Clinical Context

Urinary antiseptics are primarily used in the management of uncomplicated lower urinary tract infections, particularly acute cystitis.1 They are also valuable for prophylaxis and suppression of recurrent urinary tract infections when short-term systemic therapy has not been effective.1,6

Patient selection for urinary antiseptic therapy typically includes individuals with:

  • Acute, uncomplicated symptomatic bladder bacteriuria1
  • Recurrent urinary tract infections requiring prophylaxis2
  • Chronic urinary tract infections where eradication by short-term therapy has failed1
  • Patients who cannot tolerate systemic antibiotics3

Specific agents have particular clinical applications. Nitrofurantoin is versatile and effective against upper tract infection, recurrent bacteriuria, and serves as a long-term suppressive agent in children and pregnant patients with only a low incidence of resistance development.1 It is bactericidal for many gram-positive and gram-negative bacteria, though Pseudomonas aeruginosa and many Proteus strains are inherently resistant.4

Methenamine, when used with proper understanding of its pharmacokinetic behavior, is effective in females with uncomplicated recurrent bacteriuria, including those with multiply resistant pathogens, and as a prophylactic agent in males with recurrent infection.1,5 For optimal efficacy, methenamine requires acidic urine (pH below 5.5) to release formaldehyde, which provides the antibacterial effect.5

The typical dosage for nitrofurantoin in adults is 100 mg orally taken four times daily for acute infections, or a single daily dose of 100 mg for prophylaxis.4 For methenamine mandelate, the standard dosage is 1 g four times daily, or for methenamine hippurate, 1 g twice daily.5

Success rates for urinary antiseptics in treating uncomplicated UTIs range from 70-95%, depending on the specific agent and patient factors.3,6 However, their effectiveness is generally limited to lower urinary tract infections, and they are not recommended for pyelonephritis or complicated UTIs with systemic symptoms.2

Scientific Citation

[1] Mayrer AR, Andriole VT. Urinary tract antiseptics. Med Clin North Am. 1982 Jan;66(1):199-208. DOI: 10.1016/s0025-7125(16)31453-5

[2] Kalpana Gupta, Barbara W. Trautner. Urinary Tract Infections, Pyelonephritis, and Prostatitis. In: Harrison's Principles of Internal Medicine, 20e. McGraw Hill; 2018. DOI: 10.1036/1097-8542.722800

[3] Milo G, Katchman EA, Paul M, Christiaens T, Baerheim A, Leibovici L. Duration of antibacterial treatment for uncomplicated urinary tract infection in women. Cochrane Database Syst Rev. 2005;(2):CD004682. DOI: 10.1002/14651858.CD004682.pub2

[4] Katzung BG, Trevor AJ. Basic & Clinical Pharmacology, 14e. McGraw Hill; 2018. Chapter 46: Urinary Antiseptics. DOI: 10.1036/1259641155

[5] Guay DR. An update on the role of nitrofurans in the management of urinary tract infections. Drugs. 2001;61(3):353-64. DOI: 10.2165/00003495-200161030-00004

[6] Huttner A, Verhaegh EM, Harbarth S, Muller AE, Theuretzbacher U, Mouton JW. Nitrofurantoin revisited: a systematic review and meta-analysis of controlled trials. J Antimicrob Chemother. 2015;70(9):2456-64. DOI: 10.1093/jac/dkv147

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