Clinical and pharmacological group: & nbsp

Quinolones / fluoroquinolones

Included in the formulation
  • Nevigramon®
    capsules inwards 
  • АТХ:

    J.01.M.B.02   Nalidixic acid

    Pharmacodynamics:

    The mechanism of action is a violation of DNA replication, inhibition of the DNA-gyrase enzyme. Pharmacological effects: antibiotic: bacteriostatic or bactericidal, depending on the concentration. Spectrum of antimicrobial activity: Gram-negative microorganisms: Escherichia coli, Salmonella spp., Shigella spp., Proteus spp., Klebsiella spp., Enterobacter spp., Strains resistant to antibiotics and sulfonamides. Not sensitive: Gram-positive microorganisms, anaerobes, Pseudomonas spp.

    Pharmacokinetics:

    Bioavailability is 96%. Achieved high concentrations in the kidney and urine. The connection with plasma proteins is 93%, hydroxyanaldic acid is 63%. Biotransformation in the liver (30%) to active hydroxyanalidixic acid. Half-life 1.1-2.5 hours Elimination by the kidneys (2-3% unchanged, 13% in the form of an active metabolite, 80% in the form of inactive metabolites); 4% with feces.

    Indications:

    Cystitis, anti-relapse therapy of chronic pyelonephritis, urethritis; prostatitis; intestinal infections; prevention of infections during surgery or invasive diagnostic tests conducted on the kidneys, ureters, bladder.

    XIV.N30-N39.N30.9   Cystitis, unspecified

    XIV.N30-N39.N30.0   Acute cystitis

    XIV.N30-N39.N30   Cystitis

    XIV.N30-N39.N34.2   Other urethritis

    XIV.N30-N39.N34.1   Nonspecific urethritis

    XIV.N30-N39.N34   Urethritis and urethral syndrome

    XIV.N10-N16.N11.9   Chronic tubulointerstitial nephritis, unspecified

    XIV.N10-N16.N11   Chronic tubulointerstitial nephritis

    XIV.N10-N16.N10   Acute tubulointerstitial nephritis

    XIV.N40-N51.N41.1   Chronic prostatitis

    XIV.N40-N51.N41.0   Acute prostatitis

    Contraindications:

    Hypersensitivity, cerebral artery atherosclerosis (severe form), Parkinsonism, epilepsy, deficiency of glucose-6-phosphate dehydrogenase, porphyria, hepatic and / or renal failure (glomerular filtration rate less than 50 ml per minute), pregnancy, lactation, children under 18 years (the risk of joint disorders during the growth of the skeleton, which until now have been shown only in animal experiments).

    Carefully:

    Renal failure with creatinine clearance less than 20 ml per minute (dose reduction required).

    Pregnancy and lactation:

    Category FDA FROM.

    The use is contraindicated in pregnancy due to the risk of arthropathy in the fetus. Penetrates into breast milk, at the time of treatment should stop breastfeeding

    Dosing and Administration:

    Take inside 1 g 4 times a day for 7 days. With a longer treatment, the dose can be reduced to 500 mg 4 times a day.

    For children, the daily dose is 60 mg / kg in 3-4 divided doses.

    Side effects:

    From the nervous system and sensory organs: dysphoria, headache, dizziness, vertigo, drowsiness, weakness, paresthesia.

    Rare: toxic psychosis or short cramps, usually when used in high doses. Seizures were noted in patients with predisposing diseases (epilepsy, cerebral atherosclerosis).

    In children and infants who received nalidixic acid in therapeutic doses, there was sometimes an increase in intracranial pressure with protrusion of the fontanel, edema of the optic nerve disk and headache.

    Several cases of paralysis of a pair of cranial nerves were noted. The mechanism of these reactions is unknown, signs and symptoms of them usually quickly pass without consequences after the withdrawal of drugs.

    Rarely were there subjective visual impairments without objective disturbances, such as excessive brightness of color perception, violation of color perception,difficulty focusing and reducing visual acuity, diplopia (usually observed during the first days of treatment and quickly disappeared with a lower dose or abolishment of drugs).

    On the part of the intestine: dyspeptic phenomena, nausea, vomiting, diarrhea, gastralgia, bleeding from the digestive tract, cholestasis.

    Allergic reactions: skin rash, itching, angioedema.

    Others: myalgia; with prolonged use, thrombotic and leukopenia, hemolytic anemia, photosensitivity, convulsions are possible.

    Overdose:

    Symptoms: toxic psychosis, seizures, increased intracranial pressure or metabolic acidosis. There may also be: nausea, vomiting and lethargy.

    Treatment: recommended thorough medical supervision of the patient in a hospital; symptomatic and supportive therapy.

    Interaction:

    Symptoms: toxic psychosis, seizures, increased intracranial pressure or metabolic acidosis. There may also be: nausea, vomiting and lethargy.

    Treatment: recommended thorough medical supervision of the patient in a hospital; symptomatic and supportive therapy.

    Special instructions:

    During the period of nalidixic acid, exposure to direct sunlight should be avoided, and with the development of photosensitization, treatment with nalidixic acid should be discontinued.

    In the course of treatment, the development of resistance is possible.

    Cases of rupture of tendons of the shoulder, arm, Achilles tendon, requiring surgical treatment or leading to a permanent disability of the limb, were reported in patients receiving quinolones, including nalidixic acid. In postmarketing studies, there is an increased risk of rupture of tendons against simultaneous use of corticosteroids, especially in elderly patients. If pain, inflammation, or rupture of the tendon occurs, nalidixic acid should be immediately discontinued; the patient should be at rest and avoid stresses until the diagnosis "tendonitis" or "tendon rupture" is completely eliminated. Rupture of tendons is possible both during the treatment with quinolones (including nalidixic acid), and after the completion of treatment.

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