Biseptolum

General characteristics. Structure:

Active ingredients: 100 mg of sulfamethoxazole and 20 mg of Trimethoprimum or 400 mg of sulfamethoxazole and 80 mg of Trimethoprimum.

Excipients: potato starch – 42,25 mg, talc - 3,75 mg, magnesium stearate – 1,25 mg, polyvinyl alcohol - 0,75 mg, metilparagidro-xybenzoate – 0,15 mg, пропилпарагидроксибензоат – 0,10 mg, propylene glycol – 1,75 mg.

The combined bactericidal drug of a broad spectrum of activity.

Pharmacological properties:

Pharmacodynamics. The combined antimicrobic drug consisting of sulfamethoxazole and Trimethoprimum. The sulfamethoxazole similar on a structure to PABK, breaks synthesis of dihydrofolic acid in bacterial cells, interfering with inclusion of PABK in its molecule. Trimethoprimum strengthens effect of sulfamethoxazole, breaking recovery of dihydrofolic acid in tetrahydrofolic - the active form of folic acid responsible for protein metabolism and division of a microbic cell.

Is bactericidal drug of a broad spectrum of activity, it is active concerning the following microorganisms: Streptococcus spp. (hemolitic strains are more sensitive to penicillin), Staphylococcus spp., Streptococcus pneumoniae, Neisseria meningitidis, Neisseria gonorrhoeae, Escherichia coli (including enterotoksogenny strains), Salmonella spp. (including Salmonella typhi and Salmonella paratyphi); Vibrio cholerae, Bacillus anthracis, Haemophilus influenzae (including ampitsillinoustoychivy strains), Listeria spp., Nocardia asteroides, Bordetella pertussis, Enterococcus faecalis, Klebsiella spp., Proteus spp., Pasteurella spp., Francisella tularensis, Brucella spp., Mycobacterium spp. (including Mycobacterium leprae), Citrobacter, Enterobacter spp., Legionella pneumophila, Providencia, some types of Pseudomonas (except Pseudomonas aeruginosa), Serratia marcescens, Shigella spp., Yersinia spp., Morganella spp., Pneumocystis carinii, Chlamydia spp. (including Chlamydia trachomatis, Chlamydia psittaci); protozoa: Plasmodium spp., Toxoplasma gondii, natogenny mushrooms, Actinomyces israelii, Coccidioides immitis, Histoplasma capsulatum, Leishmania spp.

Are steady against drug: Corynebacterium spp., Pseudomonas aeruginosa, Mycobacterium tuberculossis, Treponema spp., Leptospira spp., viruses.

Colibacillus life activity oppresses that leads to reduction of synthesis of thymine, Riboflavinum, niacin, etc. group B vitamins in intestines. Duration of therapeutic effect makes 7 h.

Pharmacokinetics. At intake both components of drug are completely soaked up from digestive tract. The maximum concentration of active components of drug is observed in 1-4 hours.

Trimethoprimum differs in good penetration into cells and through fabric barriers - in lungs, kidneys, prostates, bile, saliva, a phlegm, liquor. Linkng of Trimethoprimum with proteins of 50%, an elimination half-life is normal of it from 8,6 to 17 hour.
The main way of removal of Trimethoprimum - through kidneys, 50% in not changed look. Sulfamethoxazole: its linkng with proteins of plasma of 66%, an elimination half-life is normal from 9 to 11 hour. The main way of elimination - a kidney, and, from 15 to 30% in an active form.

Indications to use:

Drug is used for treatment of infections: respiratory tracts (bronchitis, pneumonia, lung abscess, pleura empyema, otitis, sinusitis), urinogenital system (pyelonephritis, urethritis, salpingitis, prostatitis), including gonorrheal nature, gastrointestinal (dysentery, cholera, typhoid, paratyphoid, diarrhea), skin and soft tissues (pyoderma, furunculosis, etc.).

Route of administration and doses:

Drug is accepted inside after food with enough liquid. The dose is appointed individually.

To children from 3 to 5 years: on 2 tablets (120 mg) 2 times a day.

Children are from 6 to 12 years old: on 4 tablets (120 mg) or on 1 tablet (480 mg) 2 times a day.

At pneumonia - 100 mg/kg/days (at the rate of sulfamethoxazole), an interval between receptions - 6 hours, a course of treatment - 14 days.

At gonorrhea - 2 g of sulfamethoxazole 2 times a day with an interval of 12 hours.

To adults and children 12 years are more senior: on 960 mg 2 times a day, at long therapy on 480 mg 2 times a day.

Duration of a course of treatment is from 5 to 14 days. At a heavy current and/or at a chronic form of infectious diseases increase in a single dose by 30-50% is admissible.

In case of extension of a course of treatment more than 5 days and/or increases in a dose it is necessary to carry out hematologic control; in case of change of a picture of blood purpose of folic acid on 5-10 mg a day is necessary.

Dosage at patients with a renal failure: at patients with clearance of creatinine of 15-30 ml/min. it is necessary to apply a half of a standard dose; if the clearance of creatinine less than 15 ml/min. is not recommended to apply co-trimoxazole.

Features of use:

With care appoint drug at deficit of folic acid in an organism, bronchial asthma, the burdened allergological anamnesis.

At long courses of treatment (over a month) regular blood tests as there is a probability of emergence of hematologic changes are necessary (most often symptomless). These changes can be reversible at purpose of folic acid (3-6 mg/days) that significantly does not break antimicrobic activity of drug. The special ostokrozhnost has to be shown at a lekcheniya of elderly patients or patients with suspicion on initial shortage of folates. Naznakcheniye of folic acid reasonablly also at prolonged treatment in high doses.

For prevention of a crystalluria it is recommended to support the sufficient volume of the emitted urine. The probability of toxic and allergic complications of streptocides considerably increases at decrease in filtrational function of kidneys. It is inexpedient to use also against the background of treatment the foodstuff containing in large numbers of PABK - green parts of plants (a cauliflower, spinach, bean), carrots, tomatoes.

It is necessary to avoid excessive solar and UF-radiations.

The risk of side effects is much higher at patients with AIDS.

It is not recommended to apply at the tonsillitis and pharyngitises caused by a beta and hemolitic streptococcus of group A because of eurysynusic resistance of strains.

Influence on results of laboratory researches. Trimethoprimum can change results of determination of level of the methotrexate in serum which is carried out by an euzymatic method, however does not influence result at the choice of a radio immunological method.

Co-trimoxazole can increase for 10% results of reaction of Jaffe with picric acid for quantitative definition of creatinine.

The product contains parahydroxybenzoates which can cause allergic reactions, and also propylene glycol which can cause the symptoms similar to those at alcohol intake.

In case of the admission of reception of a dose of medicine. In case of the admission of reception of a dose drug should be accepted as soon as possible unless time of reception of the following dose comes. Then the previous dose should be passed. It is not necessary to accept a double dose for the purpose of completion of the passed dose.

Influence on ability to manage vehicles, mechanisms. Medicine, as a rule, does not influence psychophysical sposobknost and an opportunity to service moving mechanisms, and also to manage the vehicle during the movement.

But if there are such undesirable symptoms as a headache, a tremor, nervousness, feeling of fatigue, sledukt to be extremely careful during management of a transport sredkstvo and service of cars.

Special precautionary measures at destruction of unused medicine. Medicines cannot be thrown out in the sewerage or in house containers for waste. It is necessary to take an interest at the druggist what to do with medicines unnecessary already. It will promote environment protection.

Side effects:

Usually drug is well transferred.
From a nervous system: headache, dizziness; in some cases - aseptic meningitis, a depression, apathy, a tremor, peripheral neuritis.

From respiratory system: bronchospasm, suffocation, cough, pulmonary infiltrates.

From the alimentary system: nausea, vomiting, a loss of appetite, diarrhea, gastritis, an abdominal pain, a glossitis, stomatitis, a cholestasia, increase in activity" hepatic" transaminases, hepatitis, sometimes with cholestatic jaundice, гепатонекроз, a pseudomembranous coloenteritis, pancreatitis.

From bodies of a hemopoiesis: leukopenia, neutropenia, thrombocytopenia, agranulocytosis, megaloblastny anemia, aplastic and hemolitic anemia, eosinophilia, prothrombinopenia, methemoglobinemia.

From an urinary system: a polyuria, intersticial nephrite, a renal failure, a crystalluria, a hamaturia, increase in concentration of urea, a giperkreatininemiya, a toxic nephropathy with an oliguria and an anury.

From a musculoskeletal system: arthralgia, mialgiya.

Allergic reactions: itch, photosensitization, urticaria, medicinal fever, rash, multiformny exudative erythema (including Stephens-Johnson's syndrome), toxic epidermal necrosis (Lyell's disease), exfoliative dermatitis, allergic myocarditis, fervescence, Quincke's disease, hyperemia of scleras.

Others: hypoglycemia, hyperpotassemia, hyponatremia.

Interaction with other medicines:

Drug is not recommended to be accepted along with thiazide diuretics because of risk of thrombocytopenia (bleeding). Co-trimoxazole increases anticoagulating activity of indirect anticoagulants, and also action of hypoglycemic HP and a methotrexate. Reduces intensity of hepatic metabolism of Phenytoinum (extends it with T1/2 for 39%) and warfarin, strengthening their effect.

Rifampicin reduces Trimethoprimum T1/2. Pyrimethaminum in the doses exceeding 25 mg/week increases risk of development of megaloblastny anemia.

Diuretics (tiazida are more often) increase risk of development of thrombocytopenia.

Benzocaine, Procainum, procaineamide reduce effect (etc. Hp as a result of which hydrolysis PABK is formed).

Between diuretics (tiazida, furosemide, etc.) and peroral hypoglycemic HP (sulphonylurea derivatives), on the one hand, and antimicrobic streptocides - with another, development of cross allergic reaction is possible. Phenytoinum, barbiturates, PASK strengthen manifestations of deficit of folic acid. Derivatives of salicylic acid strengthen action.

Ascorbic acid, hexamethylenetetramine (etc. The hp acidifying urine) increase risk of development of a crystalluria.

Colestyraminum reduces absorption therefore it should be taken in 1 hour after or for 4-6 h before co-trimoxazole reception.

The HP oppressing a marrowy hemopoiesis increase risk of a miyelosupressiya. Can increase concentration of digoxin in plasma at some patients of advanced age.

Can reduce efficiency of tricyclic antidepressants.

At patients is after transplantation of the kidneys accepting co-trimoxazole and cyclosporine the taking place dysfunction of a transplantirovanny kidney which is shown increase in concentration of creatinine in serum that is possibly caused by action of Trimethoprimum is noted.

Reduces reliability of peroral contraception (oppresses intestinal microflora and reduces enterohepatic circulation of hormonal connections).

Contraindications:

Hypersensitivity to co-trimoxazole, Trimethoprimum, streptocides or any making drug, pregnancy, a lactation, children's age up to 3 years (for this dosage form), the established diagnosis of damage of a parenchyma of a liver, a heavy renal failure if is not present a possibility of definition of concentration of drug in a blood plasma (use at clearance of creatinine is not recommended lower than 15 ml/min.), a serious hematologic illness (aplastic anemia, V-12-defitsitnaya anemia, an agranulocytosis, the leukopenia, megaloblastny anemia, a hyperbilirubinemia at children connected with deficit of folic acid), deficit glyukozo-6-fosfatdegidrogenazy (probability of development of hemolysis).

With care. Drug should be used with care at patients with deficit of folic acid, bronchial asthma and diseases of a thyroid gland.

Overdose:

It is not known what dose of co-trimoxazole can be life-threatening.

At overdose sulfonamide notes: lack of appetite, intestinal colic, nausea, vomiting, dizziness, headache, drowsiness, loss of consciousness. There can also come fever, a hamaturia, a crystalluria. Later oppression of marrow and jaundice can develop. After acute poisoning with Trimethoprimum there can come nausea, vomiting, dizziness, a headache, a depression, disorder of consciousness, oppression of function of marrow. Treatment is based on drug withdrawal and removal it from digestive tract (a gastric lavage - no later than 2 h after administration of drug or it is necessary to cause vomiting), plentiful drink if the diuresis is insufficient and function of kidneys is kept. To enter фолинат calcium (5-10 mg/days).

Acid medium of urine accelerates removal of Trimethoprimum, but can also increase risk of crystallization of sulfonamide in kidneys.

It is necessary to control a blood pattern, composition of electrolytes in plasma and other biochemical parameters.

The hemodialysis is moderately effective, and peritoneal dialysis is inefficient. Chronic poisoning: use of high doses of co-trimoxazole during the long period can lead to oppression of function of marrow, shown thrombocytopenia, a leukopenia or megaloblastny anemia.

Storage conditions:

To store at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity of 5 years.

Issue conditions:

According to the recipe

Packaging:

Tablets on 120 mg and 480 mg. On 20 tablets in the blister from PVC / Аl a foil. On 1 blister in a cardboard pack with the application instruction.