Composition, form of production and packaging
Capsules hard gelatinous, size в„–0, opaque, with yellow hull and yellow lid; the contents of the capsules are white to white powder with a yellowish hue of color.
nalidixic acid 500 mg
Excipients: silicon colloidal dioxide - 19 mg, stearic acid - 11 mg.
The composition of the capsule shell: dye quinoline yellow (E104) - 0.75%, dye sunset yellow (E110) - 0.0059%, titanium dioxide (E171) - 2%, gelatin - up to 100%.
56 pcs. - vials of polystyrene (1) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
The product description was approved by the manufacturer for the 2009 print edition.
Nalidixic acid has a pronounced antibacterial activity against gram-negative bacteria, including Proteus mirabilis, P. morganii, P. vulgaris and P.rettgeri; Escherichia coli, Enterobacter (Aerobacter), and Klebsiella. Pseudomonas strains are usually resistant to the action of the drug.
Nalidixic acid acts by selective inhibition of bacterial DNA synthesis. It is bactericidal and bacteriostatic (depending on the sensitivity of the microorganism and the concentration of the drug).
At low concentrations, nalidixic acid acts only on proliferating microorganisms by suppressing DNA replication. In the case of a longer exposure, it also inhibits the bacterial synthesis of RNA and protein. Its minimum inhibitory concentration (MIC) is 5 - 75 Ојg / ml, but already at a concentration below 10 Ојg / ml it is effective against many microorganisms.
Nalidixic acid is rapidly absorbed from the digestive tract, partially metabolized in the liver and quickly excreted through the kidneys. Bioavailability of 96%.
Unchanged nalidixic acid appears in the urine together with its active metabolite, hydroxynadic acid, which has antibacterial activity similar to that of the parent compound. Hydroxy-metabolite represents 30% of the biologically active drug in the blood and 85% in the urine. C max of the active drug in the blood serum averages 20-50 Ојg g / ml 2 hours after taking 1 g of nalidixic acid on an empty stomach. T 1/2 is 1 to 2.5 hours, but with more accurate methods of determination, 6-7 hours have been obtained. About 93% of nalidixic acid and 63% of hydroxyanalidic acid bind to plasma proteins. C max of the active drug in the urine after taking a single dose of 1 g about 250 Ојg / ml after 3-6 hours. Approximately 4% of nalidixic acid is excreted with feces.
Nalidixic acid penetrates the placenta, and its small amounts appear in breast milk.
Treatment of infections caused by microorganisms that are sensitive to the drug:
- a pyelonephritis;
- Gastrointestinal infections;
Prevention of infections in operations on the kidneys, ureters, bladder.
The average dose for adults (including the elderly) is 4 g (2 capsules (1 g) - 4 times / day) for a period of at least 7 days. In case the use of the drug is required to continue, the dose may be reduced to 1 caps. (0.5 g) - 4 times / day.
For children older than 12 years (weighing more than 40 kg), a daily dose of 50 mg / kg, divided into 3-4 doses, is recommended.
Capsules Nevigramon should be taken one hour before meals.
Influence on the central nervous system: drowsiness; weakness; headache; dizziness. There are rare reports of toxic psychosis, increased intracranial pressure or convulsions (in the presence of predisposing diseases - epilepsy, cerebral arteriosclerosis). Individual cases of paralysis of the sixth cranial nerve were described. The mechanism of these reactions is unknown, but the signs and symptoms of these reactions usually quickly pass without consequences after discontinuation of the drug.
Influence on vision : visual impairment (diplopia, reduced visual acuity, difficulty of focusing) and color perception. Usually, these effects quickly disappeared when the dose was reduced or the drug was withdrawn.
Gastrointestinal complaints: epigastric pain, nausea, vomiting and diarrhea.
Allergic reactions: rash, itching, urticaria, eosinophilia, arthralgia with stiffness and swelling of the joints, rarely - angioedema, anaphylactic shock and anaphylactoid reactions.
Skin reactions: photosensitivity reactions: redness and the appearance of bubbles on the skin, completely passing during a period of two weeks to two months after the abolition of nalidixic acid; However, it is possible again the appearance of bubbles under the influence of sunlight or with minor damage to the skin surface up to three months after the drug is discontinued.
Other: rarely occur cholestasis, paresthesia, metabolic acidosis, thrombocytopenia, leukopenia or hemolytic anemia, sometimes accompanied by a deficiency of glucose-6-phosphate dehydrogenase.
Such side effects as: dysphoria and myalgia were not noted for Nevigramon.
- known hypersensitivity to nalidixic acid or other components of the drug;
- Parkinson's disease;
- Atherosclerosis of cerebral vessels (severe form);
renal and / or hepatic insufficiency;
- deficiency of glucose-6-phosphate dehydrogenase;
- children's age till 12 years;
- I trimester of pregnancy;
- the period of breastfeeding.
Be wary of appointing persons between 12 and 18 years of age
PREGNANCY AND LACTATION
The safety of Nevigramon during pregnancy is not established. Therefore, the drug should be used during pregnancy only if the expected benefit exceeds the potential risk, especially in the first trimester of pregnancy (nalidixic acid penetrates the placental barrier and affects the tissue of developing cartilage) and in the last month of pregnancy, due to the effects on the newborn : a significant increase in the level of nalidixic acid in the blood of a newborn immediately after birth.
Since nalidixic acid penetrates into the mother's milk, it is contraindicated in the period of breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindication: renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindication: liver failure.
APPLICATION FOR CHILDREN
Contraindication: children under 12 years. With an island age of 12 to 18 years.
APPLICATION IN ELDERLY PATIENTS
Correction of the dose is not required.
It has been shown that nalidixic acid and related compounds cause erosion in the cartilaginous tissue of the joints and other signs of arthropathy in most animals that have not reached puberty. Before determining the clinical significance of this phenomenon, caution should be exercised in prescribing nalidixic acid to persons under the age of 18 years. If arthralgia is manifested, treatment with nalidixic acid should be discontinued.
Patients should be warned about the need to avoid exposure to direct sunlight, and with the development of photosensitivity treatment course Nevigramon should be discontinued.
Care should be taken and discontinuation if the patient develops signs or symptoms of increased intracranial pressure, psychosis or other toxic manifestations.
If bacterial resistance develops to nalidixic acid, this usually occurs within the first 48 hours. Cross-resistance between nalidixic acid and other quinolone derivatives, such as oxolinic acid and cinoxacin, has been observed.
If methods based on copper reduction, such as solutions of Benedict or Feling, are used to analyze the urine of patients receiving Nevigramon, a false positive reaction to glucose can be obtained. Therefore, it is recommended to use specific glucose-oxidase methods of investigation.
False values вЂ‹вЂ‹can be obtained by determining 17-keto and ketogenic steroids in urine in assays based on the measurement of vanillminal acid in urine. In such cases, you can use the Porter-Silber test for 17-hydroxycorticosteroids.
Impact on the ability to drive vehicles and manage mechanisms
During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Patients who took a dose exceeding the recommended dose may experience: toxic psychosis, seizures, increased intracranial pressure, or metabolic acidosis. Also after an overdose can be observed: nausea, vomiting and lethargy.
In case of symptoms of overdose, careful medical supervision of the patient in a hospital environment is recommended. Treatment should be symptomatic and supportive.
Nalidixic acid can enhance the effect of oral anticoagulants, such as warfarin or bis-hydroxycoumarin, as a result of competitive binding to plasma proteins. In case of simultaneous application, appropriate monitoring of prothrombin time or the international normalization index (INR) is necessary, and it may be necessary to change the dose of anticoagulant.
Since the expression of antibacterial action of nalidixic acid is necessary for the manifestation of antibacterial action of bacterial cells, the action of nalidixic acid can be suppressed in the presence of other antibacterial compounds, especially bacteriostatic substances such as tetracycline, chloramphenicol or nitrofurantoin (the latter is an antagonist of nalidixic acid in vitro ).
Probenecid suppresses the secretion of nalidixic acid in the renal tubules and can reduce its effectiveness in relation to infections of the genitourinary system, while increasing the risk of systemic side effects.
Combined use of nalidixic acid and melphalan was accompanied by gastrointestinal toxicity.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
Store in a dark place at a temperature of no higher than 25 В° C. Keep out of the reach of children. Shelf life - 5 years. Do not use the drug after the expiration date.