Biseptrim suspension

General characteristics. Structure:

Active agents: sulfamethoxazole of 100.0 mg (for 120 mg / 5 ml), 200.0 mg (for 240 mg / 5 ml); Trimethoprimum of 20.0 mg (for 120 mg / 5 ml), 40.0 mg (for 240 mg / 5 ml).

Excipients: cellulose microcrystallic and carboxymethylcellulose of sodium, methylparahydroxybenzoate, пропилпарагидроксибензоат, sorbitol of 70%, polysorbate 80, fragrance banana, fragrance vanilla, the water purified.

Pharmacological properties:

Pharmacokinetics. Drug is quickly soaked up at intake; the maximum concentration in blood is noted in 1-3 hours after reception and remains within 7 hours. High concentration are created in lungs and kidneys. It is allocated in a significant amount with urine (during 24 h 40-50% of Trimethoprimum and about 60% of sulfamethoxazole, mainly, in an acetylized form are allocated). Sulfamethoxazole and Trimethoprimum are metabolized in a liver. Half-life of sulfamethoxazole makes – 9-11 hours, Trimethoprimum – 10-11 hours (children have 5-8 hours).

Pharmacodynamics. Biseptrim - an antimicrobic microbicide of a broad spectrum of activity. The combined drug, contains co-trimoxazole – mix of Trimethoprimum and sulfamethoxazole (1:5). The effect is connected with the double blocking effect of drug on metabolism of bacteria. Sulfamethoxazole breaks synthesis of dihydrofolic acid in bacterial cells, and Trimethoprimum interferes with transformation of dihydrofolic acid into tetrahydrofolic. High concentration of drug is created in tissues of lungs, kidneys, a prostate, in cerebrospinal fluid, bile, bones.

Biseptrim is active concerning gram-positive bacteria: streptococci (Streptococcus pneumoniae, S. agalactiae, S. viridans), stafilokokk (Staphylococcus aureus, Staphylococcus epidermidis), Listeria monocytogenes, Nocardia asteroides and gram-negative, including majority of sticks of Enterobacteriaceae (types of Salmonella, Shigella, Klebsiella, Proteus mirabilis, Enterobacter, part of strains of Escherichia coli), part of strains of H.influenzae, Legionella spp., Yersinia enterocolitica, Brucella spp., Neisseria meningitidis, Neisseria gonorrhoeae, and also Pneumocystis carinii. Sticks (Mycobacteriaceae), viruses, the majority of anaerobic bacteria and mushrooms are steady against drug.

Indications to use:

- urethritis, cystitis, pyelitis, pyelonephritis, prostatitis, gonorrhea;

- bronchitis (acute and chronic), bronchoectatic disease, lung fever, bronchial pneumonia;

- average otitis, sinusitis;

- meningitis;

- sepsis;

- typhoid, paratyphoid, salmonellonositelstvo, cholera, dysentery;

- pyoderma, abscess and wound fever;

- osteomyelitis (acute and chronic);

- brucellosis (acute);

- infections of soft tissues and a skeleton (at children).

Route of administration and doses:

Drug is accepted inside, in the morning and in the evening, after food.

To children depending on age appoint:

- aged from 3 up to 6 months – 2 times a day on 1 teaspoon (5 ml);

- from 6 months to 6 years - 2 times a day on 2 teaspoons (10 ml);

- from 6 to 12 years - 2 times a day on the 2nd dessertspoons (20 ml).

To adults and children 12 years – 2 times a day on the 4th dessertspoons (40 ml) are more senior.

It is recommended to shake up contents of a bottle before each use.

Duration of a course of treatment is determined by the attending physician, on average, from 5 to 7 - 10 days.

Features of use:

It is only necessary to appoint co-trimoxazole when advantage of such combination therapy before other antibacterial mono drugs exceeds possible risk.

As sensitivity of bacteria to the antibacterial drugs in vitro changes in different geographical areas and in time, at the choice of drug it is necessary to consider local features of bacterial sensitivity.

With care children of early age should apply. Patients with a renal failure a dose should reduce and control concentration of drug in blood.

With care to apply at patients of advanced age with a renal failure, because of increase in risk of development of a hyperpotassemia.

If during treatment skin rash or other intensive undesirable symptoms is shown, it is necessary to stop drug use immediately.

Appoint with care to patients with the possible deficit of folic acid burdened by the allergic anamnesis, bronchial asthma, abnormal liver functions and a thyroid gland with a serious illness of heart and blood. In these cases the dose of drug needs to be reduced, and to increase intervals between receptions.

At long courses of treatment 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. Extra care has to be shown at treatment of elderly patients or patients with suspicion on initial shortage of folates. Purpose of folic acid is reasonable also at prolonged treatment in high doses. At considerable decrease in number of any blood cells drug should be cancelled.

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.

At long courses (especially at a renal failure), it is regularly necessary to do the general analysis of urine and to control function of kidneys.

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.

At sudden emergence or increase of cough or asthma it is necessary to inspect repeatedly the patient and to consider a question of the treatment termination by drug.

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 diseases caused by a beta and hemolitic streptococcus of group A because of eurysynusic resistance of strains.

At the patients accepting co-trimoxazole pancytopenia cases were described. Trimethoprimum has low affinity to a degidrofolatreduktaza  of the person, however  can increase toxicity of a methotrexate, especially in the presence of other risk factors, such as senile age, a hypoalbuminemia, a renal failure, oppression of marrow. Similar side reactions are more probable if the methotrexate is appointed in high doses. For prevention of a miyelosupressiya such patients are recommended to appoint folic acid or calcium фолинат.

Trimethoprimum breaks phenylalanine exchange, however it does not influence patients with a fenilketonuriya on condition of observance of the corresponding diet.

Patients of whose metabolism "slow acetylation" is characteristic are more inclined to development of an idiosyncrasy to sulfonamides.

Considering side effects of medicine it is necessary to be careful when driving or potentially dangerous mechanisms.

Side effects:

- lack of appetite, nausea, vomiting, diarrhea, abdominal pains;

- stomatitis, a glossitis, pancreatitis, pseudomembranous colitis, emergence of dysbacteriosis and risk of developing of a candidosis infection is possible;

- headache, dizziness;

- anemia is hemolitic, thrombocytopenia, a leukopenia, an agranulocytosis, an eosinophilia;

- prothrombinopenia, methemoglobinemia;

- crystalluria, renal failure, intersticial nephrite, toxic nephropathy;

- skin itch, small tortoiseshell, skin rash, hyperemia of a conjunctiva and scleras, exfoliative dermatitis, polymorphic erythema, fever, fever; in isolated cases, Stephens-Johnson's syndrome, a Lyell's disease, anaphylactic reactions, a Quincke's disease, allergic myocarditis, an allergic alveolitis, a hemorrhagic vasculitis, a nodular periarteritis, a volchanochnopodobny syndrome;

- frustration of a dream, sleeplessness, aseptic meningitis, disorder of coordination, a peripheral neuropathy, a ring in ears, the movements, a depression, apathy, an ataxy, spasms, hallucinations;

- arthralgias, mialgiya;

- suffocation, cough, infiltrates in lungs;

- hypopotassemia, hyponatremia;

- hepatitis, acute necrosis of a liver;

- hypoglycemia.

Interaction with other medicines:

Increases activity of a methotrexate (competes for linkng with proteins and renal transport of a methotrexate, increasing concentration of a free methotrexate), peroral hypoglycemic medicines.

Pyrimethaminum in the doses exceeding 25 mg/week increases risk of development of megaloblastny anemia.

Increases serumal concentration of digoxin, especially at elderly patients (control is necessary) concentration of digoxin in serum.

Reduces efficiency of tricyclic antidepressants.

At the patients accepting co-trimoxazole and cyclosporine after renal transplantation the reversible deterioration in function of kidneys which is shown a giperkreatininemiya can be observed.

The medicines oppressing a marrowy hemopoiesis increase risk of a miyelosupressiya.

At simultaneous use with indometacin increase in concentration of sulfamethoxazole in blood is possible.

At simultaneous use with APF inhibitors, especially at elderly patients, development of a hyperpotassemia is possible.

Trimethoprimum, inhibiting transport system of kidneys, increases AUC by 103% and Cmax for 93% of a dofetilid that increases risk of development of ventricular arrhythmias with lengthening of an interval of Q-T, including arrhythmia like "pirouette". Simultaneous use of a dofetilid and Trimethoprimum is contraindicated.

Diuretics (is more often thiazide and at elderly patients) increase risk of development of thrombocytopenia.

Can extend a prothrombin time at the patients accepting anticoagulants (for example, warfarin).

Strengthens action of anti-diabetic means, sulphonylurea derivatives.

Slows down metabolism of Phenytoinum in a liver (raises its half-life to 39%). Can also increase concentration of a free methotrexate in a blood plasma (increases release of a methotrexate from its connections with proteins).

Biseptrim can break reaction of definition of creatinine with use of an alkaline pikrinat of Jaffe (increases creatinine level approximately for 10%).

Contraindications:

- hypersensitivity to streptocides, Trimethoprimum and/or to other components of drug;

- deficit glyukozo-6-fosfatdegidrogenazy;

- the expressed abnormal liver functions or kidneys (the clearance of creatinine is lower than 15 ml/min.);

- aplastic anemia, B12-scarce anemia, leukopenia, agranulocytosis;

- treatment of streptococcal quinsy;

- premature, newborns and children up to 3 months of life;

- pregnancy and period of a lactation.

Overdose:

Symptoms - anorexia, nausea, vomiting, weakness, abdominal pains, a headache, drowsiness, a hamaturia and a crystalluria.

Treatment - a gastric lavage, correction of electrolytic disturbances. If necessary – a hemodialysis. Oppression of marrow is characteristic of chronic overdose (pancytopenia).

Storage conditions:

To store in the dry, protected from light place at a temperature not above 30 °C. To store in the place, unavailable to children!

Issue conditions:

According to the recipe

Packaging:

On 100 ml in the bottles from glass melt corked by the screwed metal caps with a control ring.

On each bottle paste the label from paper label.

Each bottle together with the approved instruction in the state and Russian languages and a dosing spoon is placed in a pack from a cardboard.

The text from the approved instruction on a medical use in the state and Russian languages is allowed to apply on a pack.