Nitrofurans in the treatment of uncomplicated urinary tract infections

Indications for use

Nitrofuran preparations are used to treat infectious diseases caused by bacteria sensitive to them: intestinal infections, acute bacterial diarrhea, kidney and urinary tract infections (pyelonephritis, pyelitis, cystitis, urethritis), infections of the skin and soft tissues, infections of burn wounds, prostatitis, and also for bacterial infections of the female reproductive system.

Furazolidone is additionally used for giardiasis and trichomonas infections.

Nitrofural is used exclusively topically, as an antiseptic both for the treatment and for the prevention of purulent-inflammatory processes: skin and soft tissues (purulent wounds, ulcers, burns, bedsores), eyes (blepharitis, conjunctivitis), ear (otitis, external boils ear canal), gums and oral cavity (gingivitis, stomatitis), tonsillitis.

NITROIMIDAZOLE DERIVATIVES

MODERN ANTIMICROBIAL CHEMOTHERAPY

MODERN ANTIMICROBIAL CHEMOTHERAPY

L.S. Strachunsky, S.N. Kozlov. Guide for doctors

Antibacterial drugs

The main drug in this group is metronidazole; tinidazole and ornidazole are also used. Their main clinical significance is their high activity against protozoa, anaerobes (especially B.fragilis

) and
H. pylori
. The drugs are practically equivalent in most basic characteristics and differ in half-life, therefore they are used in different doses.

METRONIDAZOLE

Klion, Metrogyl, Trichopolum, Flagyl, Efloran

The most commonly used nitroimidazole. It is the main antianaerobic drug, and resistance of anaerobes to it is extremely rare.

Activity spectrum

Pharmacokinetics

Well absorbed from the gastrointestinal tract. Bioavailability (80%) is not significantly affected by food. It is very well distributed in the body and penetrates the placenta through the blood-brain barrier. Metabolized in the liver, excreted in urine and stool. T1/2 - 6-8 hours, does not change with renal failure.

Adverse reactions

• Dyspeptic symptoms (nausea, vomiting, anorexia, metallic taste in the mouth).
• Hematotoxicity (leukopenia, neutropenia).
• Neurotoxicity (headache, loss of coordination, tremors, convulsions).
• Disulfiram-like effect.

Indications

• Anaerobic infections of various locations: intra-abdominal, pelvic, central nervous system, etc.
• Eradication of H. pylori
  (necessarily in combination with other antibiotics and antisecretory drugs).
• C. difficile
  - associated diarrhea (pseudomembranous colitis).
• Rosacea (orally or topically).
• Protozoal infections: trichomoniasis, giardiasis, amoebiasis.
• Perioperative antibiotic prophylaxis in abdominal surgery and gynecology.

Dosage

Adults

Orally - 0.25-0.5 g every 8 hours; intravenously (if oral administration is not possible) - 0.5 g every 8 hours. For trichomoniasis - 2.0 g once, or 0.25 g every 8 hours, or 0.375 g every 12 hours for 7 days. For eradication of H. pylori

- 0.5 g every 8-12 hours for 7 or 14 days (depending on the regimen). For perioperative prophylaxis, 0.5 g intravenously 1 hour before surgery in combination with antibiotics active against aerobic flora (cephalosporins, fluoroquinolones).

Children

Orally and intravenously, 7.5 mg/kg every 8 hours.

It is prescribed orally regardless of food.

Release forms

Tablets of 0.2 g, 0.25 g, 0.4 g and 0.5 g; ampoules, vials and plastic bags with solution, 5 mg/ml; bottles of 0.5 g and 3.0 g of powder for preparing a solution for infusion; gel, 0.75%.

TINIDAZOLE

Fazizhin

Differences from metronidazole:

• longer T1/2 (11-12 hours);
• It is used only internally.

Indications

• Anaerobic infections of various locations: intra-abdominal, pelvic, central nervous system, etc.
• Eradication of H. pylori
  (necessarily in combination with other antibiotics and antisecretory drugs).
• C. difficile
  - associated diarrhea (pseudomembranous colitis).
• Protozoal infections: trichomoniasis, giardiasis, amoebiasis.
• Perioperative antibiotic prophylaxis in abdominal surgery and gynecology.

Dosage

Adults

Orally - on the 1st day 2.0 g in one dose, then 1.0 g / day in 1-2 doses; for prevention - 2.0 g 12 hours before surgery.

Children

Orally - 50-60 mg/kg/day in one dose.

Prescribed regardless of food.

Release forms

Tablets of 0.3 g and 0.5 g.

ORNIDAZOLE

Tiberal

Differences from metronidazole:

• longer T1/2 (12-14 hours);
• does not have a disulfiram-like effect;
• It is used only internally.

Indications

• Anaerobic infections of various locations: intra-abdominal, pelvic, central nervous system, etc.
• C. difficile
  - associated diarrhea (pseudomembranous colitis).
• Protozoal infections: trichomoniasis, giardiasis, amoebiasis.

Dosage

Adults

Orally - 0.5 g every 12 hours, regardless of food.

Children

Orally - 25-40 mg/kg/day in 1-2 doses, regardless of food.

Release form

Tablets 0.5 g.

The main nitrofuran drugs include nitrofural ( furatsilin

), nitrofurantoin (
furadonin
), furazidin (
furagin
) and furazolidone. Nitrofurans have a wide spectrum of activity, which includes bacteria, viruses, protozoa, and are able to act on strains resistant to some antibiotics. Microflora resistance to them rarely develops. The main problem with the use of nitrofurans is the high frequency of adverse drug reactions, as well as the lack of parenteral dosage forms.

Activity spectrum

Resistant anaerobes, P. aeruginosa

, Protea, Serration, Acinetobacter.

Adverse reactions

• Dyspeptic symptoms are most often nausea and vomiting, so nitrofurans should be taken during or after meals.
• Hepatotoxicity.
• Hematotoxicity.
• Neurotoxicity - damage to the central nervous system and peripheral parts, especially with renal failure and long courses (more than 1.5 months).
• Pulmonary reactions - described when taking nitrofurantoin:

a) acute (90%) - pulmonary edema, bronchospasm; b) chronic (10%) - pneumonitis, accompanied by difficulty breathing, fever, eosinophilia; are more often observed in women over 60 years of age with long-term use.

Contraindications

• Pregnancy.
• Age less than 1 month.
• Glucose-6-phosphate dehydrogenase deficiency.
• Severe liver pathology (furazolidone).
• Renal failure (nitrofurantoin, furazidine).

CHARACTERISTICS OF DRUGS

NITROFURAL

Furacilin

Use locally for rinsing in the form of a 0.02% solution. It should be borne in mind that many types of hospital flora (Klebsiella, Pseudomonas aeruginosa, etc.) are resistant to the drug, therefore it is ineffective as an antiseptic. May cause local allergic reactions.

NITROFURANTOIN

Furadonin

The most famous of the nitrofurans. It is well absorbed from the gastrointestinal tract (bioavailability is about 100%), creating low concentrations in the blood and high concentrations in the urine. T1/2 - about 1 hour. The effect of the drug increases with acidic urine and is weakened when its pH ≥ 8.

Indications

• Acute cystitis.
• Long-term suppressive therapy for chronic pyelonephritis.

Warning

Do not prescribe for acute pyelonephritis, since the drug does not create a high concentration in the kidney tissue.

Dosage

Adults

Orally - 0.05-0.1 g every 6 hours during or after meals.

Children over 1 month

Orally - 5-7 mg/kg/day in 4 divided doses during or after meals.

Release forms

Tablets of 0.03 g (for children), 0.05 g and 0.1 g.

FURAZIDINE

Furagin

Compared with nitrofurantoin, it is thought to be better absorbed and better tolerated, but produces lower concentrations in urine. However, in general, pharmacokinetics, including in children, and adverse reactions have been practically not studied.

Indications

• Acute cystitis.
• Long-term suppressive therapy for chronic pyelonephritis.

Dosage

Adults

Orally - 0.1-0.2 g every 6-8 hours during or after meals.

Children

Orally - 7.5 mg/kg/day in 2-3 doses during or after meals.

Release form

Tablets 0.05 g.

FURAZOLIDONE

It acts predominantly on gram-negative bacteria, as well as Giardia and Trichomonas.

Unlike nitrofurantoin, it does not create therapeutic concentrations in the urine. Metabolized in the liver. High concentrations of the drug are observed in the intestinal lumen.

Previously, it was widely used for intestinal infections, especially in children. However, the sensitivity of microflora to furazolidone has not been sufficiently studied, and no controlled clinical studies have been conducted.

Indications

• Giardiasis.

Warning

Do not prescribe for UTI infections.

Dosage

Adults

Orally - 0.1 g every 6 hours after meals.

Children

Orally - 6-7 mg/kg/day in 4 divided doses after meals.

Release forms

Tablets 0.05 g; granules for preparing a suspension.

NIFUROXAZIDE

Ersefuril

Active against a number of gram-positive and gram-negative bacteria (see page 143). Practically not absorbed into the gastrointestinal tract. Does not have a negative effect on normal intestinal microflora.

The drug is recommended for acute infectious diarrhea (however, clinical effectiveness was confirmed in only one placebo-controlled study).

Dosage

Adults

Orally - 0.2 g every 6 hours.

Children

From 1 month to 2.5 years

Orally - 0.1 g every 8-12 hours, regardless of meals.

Over 2.5 years old

Orally - 0.2 g every 8 hours, regardless of meals.

Release forms

Tablets 0.2 g; suspension, 4%.

8-hydroxyquinoline derivatives were popular in the 60-70s of the 20th century in the treatment of intestinal infections and UTI infections.

For intestinal infections, chlorine-iodine-hydroxyquinoline ( enteroseptol

), dibromohydroxyquinoline (
intestopan
),
mexaform
(combination drug). The drugs have antibacterial and antiprotozoal effects. In addition to hydroxyquinoline derivatives, their composition includes surfactants that enhance the therapeutic effect. However, due to reports of severe adverse reactions, these drugs are no longer used in most countries. With their long-term use, the development of subacute myelo-optic neuropathy (SMON syndrome), which manifests itself as severe peripheral polyneuritis and optic nerve atrophy, is possible.

Of the drugs related to 8-hydroxyquinoline derivatives, nitroxoline is used in Russia.

NITROXOLINE

5-NOK

Activity spectrum

The main clinical significance is activity against gram-negative bacteria from the family Enterobacteriaceae

(
E. coli
, etc.).

Pharmacokinetics

It is well absorbed from the gastrointestinal tract, mainly metabolites enter the urine. In general, pharmacokinetics have not been studied enough and have not been studied in children at all.

Adverse reactions

• Neurotoxicity: headache, dizziness, paresthesia, polyneuropathy.
• Dyspeptic symptoms, diarrhea.

Indications

• Acute uncomplicated cystitis - treatment, prevention (second-line drug).

Contraindications

• Premature and newborns.
• Pregnancy.
• Breast-feeding.
• Severe liver diseases.
• Diseases of the peripheral nervous system.
• Diseases of the optic nerve.
• Kidney failure.

Warning

The course should not be prescribed for more than 10 days.

Dosage

Adults

Orally - 0.1-0.2 g every 6 hours 1 hour before meals.

Children

Orally - 5-8 mg/kg/day in 2-3 divided doses.

Release form

Tablets 0.05 g.

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Last modified date: 05/24/2004 18:56