Biseptol 480, concentrate 80+16 mg/ml 5 ml 10 pcs.

A combination antibacterial drug containing sulfamethoxazole with medium duration of action inhibiting folic acid synthesis by competitive antagonism with para-aminobenzoic acid and trimetholrim inhibitor of bacterial dihydrofolic acid reductase. The combination of both drugs gives an energic effect of antibacterial action due to which bacterial resistance is less frequent compared to other drugs.

Biseptol has a wide spectrum of antibacterial action. It is active against : Streptococcus (Streptococcus pneumoniae), Neisseria meningitidis, Neisseria gonorrhoeae (including enterotoxigenic strains), Staphylococcus, Escherichia coli, Klebsiella, Enterobacter, Proteus mirabilis, Proteus arr, Haemophilus influenzae, Salmonella spp. (including Salmonella typhi and Salmonella paratyphi), Vibrio cholerae, Bacillus anthracis, Listeria spp., Nocardia asteroides, Bordclella pertussis, Enterococcus faecalis, Pasteurella spp, Brucella spp., Mycobacterium spp. (including Mycobacterium leprae), Citrobacter, Enterobacter spp., Legionella pneumonia, Providencia, some Pseudomonas species (except P. aerugenosa), Serratia marcescens, Yersinia spp, Morganella spp., Chlamydia spp. (including Chlamydia trachomatis, Chlamydia psittaci), Shigella, Plasmodium spp., Toxoplasma gondii, Pneumocystis carini, Actinomyces israelii, Coccidioides immitis, Histoplasma capsulatum, Leishmania spp.

Resistant to the drug: Corynebacterium spp., Pseudomonas aerugenosa, Mycobacterium tuberculosis, Troponema spp., Leptospira spp., viruses.

Inhibits the activity of E. coli, leads to a decrease in the synthesis of thiamine, riboflavin, nicotinic acid and other B vitamins in the intestine. The duration of the therapeutic effect is 7 hours.

Indications

Active ingredient

Composition

Active ingredients:

Sulfamethoxazole 80.00 mg + trimethoprim 16.00 mg

Associates:

propylene glycol,

sodium hydroxide,

ethanol,

benzyl alcohol,

sodium metabisulfite,

d/i water.

How to take, the dosage

The drug should be administered by IV drip, after dilution (e.g. 5% dextrose solution, 0.9% sodium chloride solution, Ringer’s solution or 0.45% sodium chloride solution with 2.5% dextrose solution). The solution for infusion should be prepared immediately before administration by mixing thoroughly. After dilution, the resulting solution should be used within 6 h.

The drug should not be used as a rapid intravenous injection.

Adults and children over 12 years of age are prescribed 960 mg (2 ampoules of 5 ml diluted in 250 ml solution) every 12 hours. In particularly severe cases 1,440 mg (3 ampoules) 2-3 times a day should be prescribed.

In children under 12 years of age the daily dose is given at the rate of 36 mg/kg of body weight in two equal doses.

Patients with renal insufficiency (with creatinitis clearance of 15-30 ml/min) are prescribed 50% of the average therapeutic dose.

Interaction

Biseptol increases the effect of phenytoin, oral hypoglycemic agents, warfarin derivatives (prolongation of prothrombin time, bleeding).

In elderly patients in combination with diuretics (particularly thiazide diuretics), the risk of thrombocytopenia increases.

Concomitant use with cyclosporine decreases its blood concentrations.

The drug should not be administered intravenously in combination with drugs and solutions containing bicarbonates.

Biseptol is pharmaceutically compatible with the following drugs: dextrose for IV infusion 5%, sodium chloride for IV infusion 0.9%, mixture of 0.18% sodium chloride and 4% dextrose for IV infusion, 6% dextran 70 for IV infusion in 5% dextrose or saline solution, 10% dextran 40 for IV infusion in 5% dextrose or saline solution, Ringer’s solution for injection.

It increases the anticoagulant activity of indirect coagulants, increases the effect of hypoglycemic agents and methotrexate.

Limits the intensity of hepatic metabolism of phenytoin (prolongs its TT1/2 by 39%) and warfarin, increasing their effect.

Rifampicin shortens the T1/2 of trimethoprim.

Pyrimethamine at doses greater than 25 mg/week increases the risk of megaloblastic anemia.

Diuretics (often thiazides) increase the risk of thrombocytopenia.

Decreases the effect of benzocaine, procaine, procainamide and other drugs that hydrolyze to form PABA.

A cross-allergic reaction may develop between diuretics (thiazides, furosemide, etc.) and oral hypoglycemic drugs (sulfonylurea derivatives) on the one hand and antimicrobial sulfonamides on the other.

Pheninoin, barbiturates, PASC increase the manifestation of folic acid deficiency.

Salicylic acid derivatives increase the effects.

Ascorbic acid, hexamethylantetramine and other drugs that acidify the urine increase the risk of crystalluria.

Colesteramine reduces absorption, so it should be taken 1 h after or 4-6 h before taking cotrimoxazole.

Decreases the reliability of oral contraception (inhibits intestinal microflora and reduces intestinal hepatic circulation of hormonal compounds).

Special Instructions

In AIDS patients treated with cotrimoxazole due to Pneumocystis carinii infection, undesirable effects are more common: skin rashes, increased body temperature, leukopenia.

It is advisable to determine the plasma concentration of sulfamethoxazole every 2-3 days immediately before the next infusion. If the sulfamethoxazole concentration exceeds 150 µg/ml, treatment should be interrupted until it drops below 120 µg/ml.

In long-term treatment, peripheral blood, hepatic and renal function tests should be performed systematically.

In elderly patients additional folic acid administration (3-6 mg/day) is recommended, which does not significantly compromise the antimicrobial activity of the drug. Particular caution should be exercised when treating elderly patients with suspected initial folate deficiency.

In order to prevent crystalluria, it is recommended to maintain an adequate volume of urine excreted.

The likelihood of toxic and allergic complications of sulfonamides is greatly increased when renal filtration function is compromised.

It is also inadvisable to consume foods containing large amounts of PABA-green plant parts (cauliflower, spinach, legumes), carrots, and tomatoes during treatment.

Excessive sunlight and ultraviolet exposure should be avoided.

It is not recommended for tonsillitis, pharyngitis caused by group A beta-haemolytic streptococcus because of widespread strain resistance.

Impact on driving and operating machinery

The drug has no effect on the ability to drive vehicles and operate moving machinery.

Features

The drug quickly penetrates into tissues and body fluids.

The drug is well distributed. It penetrates through the BBB, the placental barrier and into breast milk. In lungs and urine it generates concentrations higher than in plasma. To a lesser extent accumulates in bronchial secretion, vaginal discharge, prostate secretion and tissues, middle ear fluid, cerebrospinal fluid, bile, bones, saliva, aqueous humor of the eye, breast milk, interstitial fluid. The distribution of both drugs is different: sulfamethoxazole is distributed exclusively in the extracellular space, while trimethoprim is distributed both within cells and in the extracellular space. Binding to plasma proteins is 66% for sulfamethoxazole and 45% for trimethoprim. Both drugs are metabolized in the liver.

Sulfamethoxazole is metabolized to a greater extent (with the formation of acetylated derivatives); the metabolites have no antimicrobial activity.

Extracted by the kidneys, both by filtration and by active secretion by tubules, as metabolites (80% within 72 hours) and in unchanged form (20% sulfamethoxazole, 50% trimethoprim ), the concentration of active substances in urine is significantly higher than in blood. A small amount of the drug is excreted through the intestine. T1/2 for sulphamethoxazole – 9-11 hours, for trimethoprim – 10-12 hours, in children – much less and depends on age: up to 1 year – 7-8 hours, 1-10 years – 5-6 hours. In the elderly and patients with impaired renal function T1/2 increases.

Contraindications

Side effects

Biseptol is usually well tolerated by patients. However, the following effects may be noted:

Gastrointestinal disorders: anorexia, gastritis, abdominal pain, glossitis, stomatitis, cholestasis, increased liver transaminase activity, hepatitis, pseudomembranous enterocolitis, nausea, vomiting, diarrhea, liver necrosis.

CNS disorders: headaches and dizziness. In individual cases – aseptic meningitis, depression, apathy, tremor, peripheral neuritis.

Respiratory system: bronchospasm, pulmonary infiltrates.

Hematopoietic disorders: rarely – neutropenia, agranulocytosis, megaloblastic anemia, leukopenia, thrombocytopenia, hypoprothrombinemia.

Urinary system disorders: polyuria, interstitial nephritis, renal dysfunction, crystalluria, hematuria, increased urea, hypocreatininemia, toxic nephropathy with oliguria and anuria.

Muscular system disorders: arthralgia, myalgia.

Allergic reactions: skin rash and itching, photosensitization, rash, erythema polymorphicum, exfoliative dermatitis, allergic myocarditis, increased body temperature, Quincke’s edema, redness of sclerae.

Local reactions: thrombophlebitis (at the site of venipuncture), pain at the site of injection.

Other: hypoglycemia

Overdose

Symptoms: nausea, vomiting, intestinal colic, dizziness, headache, drowsiness, depression, fainting, confusion, visual disturbances, fever, hematuria, crystalluria; in prolonged overdose – thrombocytopenia, leukopenia, megaloblastic anemia.

Treatment: gastric lavage, acidification of urine increases trimethoprim excretion, oral fluid administration, intramuscular – 5-15 mg /day, calcium folinate (eliminates the effect of trimethoprim on bone marrow), with suppression of bone marrow hematopoietic functions caused by trimethoprim, intramuscular folic acid preparations (3-6 mg / day) are used to stimulate erythropoiesis. The course of treatment is 5-7 days), and hemodialysis if necessary.

Similarities