Biseptol, ampoules 480mg, 5ml, 10pcs

Composition

Active ingredients:

sulfamethoxazole 80.00 mg + trimethoprim 16.00 mg

Auxiliary substances:

propylene glycol,

sodium hydroxide,

ethanol,

benzyl alcohol,

sodium metabisulfite,

d/i water.

Pharmacological action

A combined antibacterial drug containing sulfamethoxazole, which has an average duration of action, inhibits the synthesis of folnic acid by competitive antagonism with paraaminobenzoic acid, and trimetolrim, an inhibitor of bacterial dihydrofolic acid reductase. The combination of both drugs gives an energic effect of antibacterial action, and therefore bacterial resistance is less pronounced compared to other drugs.

Biseptol has a broad spectrum of antibacterial action. It is active against : Streptococcus (Streptococcus pneumoniae), Neisseria meningitidis, Neisseria gonorrhoeae (including enterotoxogenic strains), Staphylococcus, Escherichia coli, Klebsiella, Enterobacter, Proteus mirabilis, Proteus spp., 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. Mycobacterium leprae), Citrobacter, Enterobacter spp., Legionella pneumonia, Providencia, some Pseudomonas species (except P. aegideposa), 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 vital activity of Escherichia 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

• acute and chronic urinary and genital tract infections: urethritis, pyelonephritis, cystitis, pyelitis, prostatitis, epididymitis, gonorrhea, chancroid, lymphogranuloma venereum, granuloma inguinal;
• respiratory tract infections: bronchitis (acute and chronic) bronchiectasis, lobar pneumonia, pneumonia, Pneumocystis pneumonia, empyema, lung abscess;
• infections of ENT organs: otitis media, sinusitis, laryngitis, tonsillitis, scarlet fever;
• gastrointestinal tract infections: typhoid, paratyphoid, salmonellosis, cholera, dysentery, cholecystitis, cholangitis, gastroenteritis, enterotoxicity caused by strains of E. coli;
• infections of skin and soft tissues: acne, furunculosis, pyoderma, abscess and wound infections, infections after surgery;
• sepsis, acute brucellosis, toxoplasmosis, osteomyelitis, infection osteoarticulares, South American blastomycosis, malaria (Plasmodium falciparum), pertussis ( in the complex therapy).

Contraindications

• megaloblastic anemia in the background of folic acid deficiency, aplastic anemia, In₁₂deficiency anemia, agranulocytosis, leukopenia;
• deficiency of glucose-6-phosphate dehydrogenase;
• hyperbilirubinemia in children;
• liver and/or renal failure creatinine clearance less than 15 ml/min);
• the age of 6 (only for the/m introduction);
• pregnancy;
• lactation;
• increased individual sensitivity to sulfonamides or trimethoprim.

Do not use the drug in premature infants, newborns and children under 2 months of life.

It is used with caution for folic acid deficiency, bronchial asthma, thyroid diseases, liver and kidney dysfunction.

Side effects

Biseptol is usually well tolerated by patients. However, the following effects may occur in:

From the gastrointestinal tract:  anorexia, gastritis, abdominal pain, glossitis, stomatitis, cholestasis, increased activity of hepatic transaminases, hepatitis, pseudomembranous enterocolitis, nausea, vomiting, diarrhea, liver necrosis.

From the central nervous system:  headaches and dizziness. In some cases-aseptic meningitis, depression, apathy, tremor, peripheral neuritis.

Respiratory system disorders:  bronchospasm, pulmonary infiltrates.

From the side of hematopoietic organs:  rarely-neutropenia, agranulocytosis, megaloblastic anemia, leukopenia, thrombocytopenia, hypoprothrombinemia.

From the urinary system:  polyuria, interstitial nephritis, impaired renal function, crystalluria, hematuria, increased urea content, hypocreatininemia, toxic nephropathy with oliguria and anuria.

Musculoskeletal disorders:  arthralgia, myalgia.

Allergic reactions:  skin rashes and pruritus, photosensitivity, rash, erythema multiforme, exfoliative dermatitis, allergic myocarditis, fever, angioedema, redness of the sclera.

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

Other services:  hypoglycemia

Interaction

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

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

Concomitant use with cyclosporine reduces its concentration in the blood.

Do not administer the drug intravenously in combination with medications and solutions containing bicarbonates.

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

Increases the anticoagulant activity of indirect coagulants, enhances the effect of hypoglycemic agents and methotrexate.

Reduces the intensity of hepatic metabolism of phenytoin (extends egoT 1/2 by 39%) and warfarin, enhancing their effect.

Rifampicin reduces T_1/2 of trimethoprim.

Pyrimethamine in doses exceeding 25 mg / week increases the risk of megaloblastic anemia.

Diuretics (most commonly thiazides) increase the risk of developing thrombocytopenia.

Reduce the effect of benzocaine, procaine, procainamide and other drugs, as a result of hydrolysis of which PABA is formed.

Between diuretics (thiazides, furosemide, etc. ) and oral hypoglycemic drugs (sulfonylureas) on the one hand and antimicrobial sulfonamides on the other, a cross – allergic reaction may develop.

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

Salicylic acid derivatives enhance the action.

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

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

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

How to take, course of use and dosage

The drug should be administered intravenously, after dilution (for example,5% dextrose solution,0.9% sodium chloride solution, Ringer’s solution or 0.45% sodium chloride solution with 2.5% dextrose solution). The infusion solution should be prepared immediately before use, thoroughly mixed. After dilution, the resulting solution should be applied for 6 hours.

Do not use the drug 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 of solution) every 12 hours. In particularly severe cases,1440 mg (3 ampoules) should be prescribed 2-3 times a day.

Children under 12 years of age are prescribed a daily dose of 36 mg / kg of body weight in two equal doses.

Patients with renal insufficiency (with a creatinine clearance of 15-30 ml / min) prescribe 50% of the average therapeutic dose.

Overdose

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

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

Functional features

The drug quickly penetrates into the tissues and body fluids of the body.

Well distributed. Penetrates through the BBB, placental barrier and into breast milk. In the lungs and urine creates concentrations exceeding the content in plasma. To a lesser extent, they accumulate in bronchial secretions, vaginal secretions, prostate secretions and tissues, middle ear fluid, spinal fluid, bile, bones, saliva, watery eye moisture, breast milk, interstitial fluid.The distribution of both drugs is different: sulfamethoxazole is distributed exclusively in the extracellular space, while trimethoprim is distributed both inside cells and in the extracellular space. Binding to plasma proteins was 66% for sulfamethoxazole and 45% for trimethoprim. Both drugs are metabolized in the liver.

Sulfamethoxazole is mostly metabolized (with the formation of acetylated derivatives), the metabolites do not have antimicrobial activity.

They are excreted by the kidneys, both by filtration and by active secretion by the tubules, in the form of metabolites (80% for 72 hours) and in unchanged form (20% of sulfamethoxazole,50% of trimethoprim), the concentration of active substances in the urine is significantly higher than in the blood. A small amount of the drug is excreted through the intestines. T_1/2 of sulfamethoxazole – 9-11 hours, trimethoprim-10-12 hours, in children – significantly less and depends on age: up to the first year-7-8 hours,1-10 years – 5-6 hours. In the elderly and patients with impaired renal function, T_1/2 increases.

Special instructions

In AIDS patients treated with cotrimoxazole, due to Pneumocystis carinii infection, undesirable effects are more often noted: skin rashes, fever, leukopenia.

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

With long-term treatment, it is necessary to systematically conduct studies of peripheral blood, the functional state of the liver and kidneys.

Elderly patients are recommended to receive additional folic acid (3-6 mg/day), which does not significantly interfere with the antimicrobial activity of the drug. Special care should be taken when treating elderly patients with suspected initial folate deficiency.

To prevent crystalluria, it is recommended to maintain a sufficient volume of urine excreted.

The probability of toxic and allergic complications of sulfonamides is significantly increased when the filtration function of the kidneys is complicated.

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

Excessive sun and ultraviolet exposure should be avoided.

It is not recommended to use for tonsillitis, pharyngitis caused by beta-hemolytic streptococcus group A due to widespread resistance of the strains.

Influence on the ability to drive motor vehicles and manage mechanisms

The drug does not affect the ability to drive vehicles and maintain moving mechanisms.

Storage conditions

List B. In a place protected from light, at a temperature not exceeding 30°C.

Shelf

life is 5 years.

Active ingredient

Co-trimoxazole Sulfamethoxazole, Trimethoprim

Conditions of release from pharmacies

By prescription

Dosage form

infusion solution