Biseptol tablets are used to treat infections caused by pathogenic microorganisms sensitive to the drug, in cases where the benefit of such treatment outweighs the possible risk (it is necessary to decide whether only one antibacterial agent can be used):
- infections of the ENT organs and respiratory tract: sinusitis, otitis media, acute and chronic bronchitis, bronchiectasis, pneumonia (including those caused by Pneumocystis carinii), pharyngitis, tonsillitis (for infections caused by β-hemolytic streptococci of group A, the eradication frequency is not entirely sufficient );
- kidney and urinary tract infections: acute and chronic cystitis, pyelonephritis, urethritis, prostatitis, chancroid;
- digestive tract infections: typhoid and paratyphoid fever, shigellosis (caused by susceptible strains of Shigella flexneri and Shigella sonnei, if antibiotic therapy is indicated), traveler's diarrhea caused by enterotoxic strains of Escherichia coli, cholera (in addition to fluid and electrolyte restoration);
- other bacterial infections: acute and chronic osteomyelitis, brucellosis, nocardiosis, actinomycosis, toxoplasmosis, South American blastomycosis.
Contraindications
- hypersensitivity to trimethoprim and sulfamethoxazole (including sulfonamide derivatives, sulfonylurea antidiabetics, and thiazide diuretics) and other components of the drug;
- acute hepatitis, impaired liver function, severe liver failure, including diagnosed damage to the liver parenchyma, porphyria;
- blood diseases, hematopoiesis disorders, severe hematological disorders, megaloblastic anemia caused by folic acid deficiency, glucose-6-phosphate dehydrogenase deficiency (threat of hemolysis);
- severe renal failure, which is characterized by creatinine clearance less than 15 ml/minute, if it is not possible to determine the concentration of the drug in the blood plasma (except in cases of hemodialysis);
- the drug is contraindicated in patients undergoing chemotherapy;
- the drug should not be prescribed in combination with dofetilide.
Biseptol
Use during pregnancy and breastfeeding
During pregnancy, the drug should be prescribed only if the expected benefit from its use outweighs the possible risk to the fetus, since both trimethoprim and sulfamethoxazole cross the placental barrier and thus can affect folic acid metabolism.
In late pregnancy, the use of the drug should be avoided due to the possible risk of developing kernicterus in newborns.
Due to the fact that trimethoprim and sulfamethoxazole pass into breast milk, the use of co-trimaxazole during lactation is contraindicated.
Pregnant women receiving the drug are recommended to take 5 mg of folic acid per day.
Use for liver dysfunction
Contraindicated:
- liver failure.
Use for renal impairment
Contraindicated:
- renal failure (creatinine clearance less than 15 ml/min).
Use in children
Contraindicated:
- children up to 2 months or up to 6 weeks at birth from a mother with HIV infection.
Children: from 2 months (or 6 weeks at birth from mothers with HIV infection) to 5 months - 120 mg, from 6 months to 5 years - 240 mg, from 6 to 12 years - 480 mg every 12 hours, which approximately corresponds to a dose of 36 mg/kg per day.
special instructions
Co-trimoxazole should be prescribed only in cases where the advantage of such combination therapy over other antibacterial monotherapy drugs outweighs the possible risk.
Because the sensitivity of bacteria to antibacterial drugs in vitro varies across different geographic areas and over time, local patterns of bacterial susceptibility should be taken into account when selecting a drug.
With long courses of treatment, regular blood tests are necessary, since there is a possibility of hematological changes (most often asymptomatic). These changes can be reversible with the administration of folic acid (3-6 mg/day), which does not significantly impair the antimicrobial activity of the drug.
Particular caution should be exercised when treating elderly patients or patients with suspected underlying folate deficiency.
The administration of folic acid is also advisable for long-term treatment in high doses.
If there is a significant decrease in the number of any blood cells, the drug should be discontinued.
During treatment, it is also inadvisable to consume foods containing large quantities of PABA - green parts of plants (cauliflower, spinach, legumes), carrots, tomatoes.
For long-term courses (especially in cases of renal failure), it is necessary to regularly conduct a general urine test and monitor kidney function.
To prevent crystalluria, it is recommended to maintain a sufficient volume of urine excreted.
The likelihood of toxic and allergic complications of sulfonamides increases significantly with a decrease in the filtration function of the kidneys. At the first appearance of skin rash or any other severe adverse reaction, the drug should be discontinued.
If cough or shortness of breath suddenly appears or worsens, the patient should be re-examined and discontinuation of drug treatment should be considered.
Excessive sunlight and ultraviolet radiation should be avoided.
The risk of side effects is significantly higher in patients with AIDS.
It is not recommended for use in diseases caused by group A beta-hemolytic streptococcus due to widespread strain resistance.
Cases of pancytopenia have been described in patients taking co-trimoxazole.
Trimethoprim has low affinity for human dehydrofolate reductase, but may increase the toxicity of methotrexate, especially in the presence of other risk factors such as old age, hypoalbuminemia, renal impairment, bone marrow suppression. Such adverse reactions are more likely if methotrexate is prescribed in large doses. To prevent myelosuppression, it is recommended to prescribe folic acid or calcium folinate to such patients.
Trimethoprim disrupts phenylalanine metabolism, but this does not affect patients with phenylketonuria provided they follow an appropriate diet.
Patients whose metabolism is characterized by “slow acetylation” are more
The duration of treatment should be as short as possible, especially in elderly and senile patients.
Co-trimoxazole and, in particular, trimethoprim, which is part of it, can affect the results of determining the concentration of methotrexate in serum, carried out by the competitive protein binding method using bacterial dihydrofolate reductase as a ligand. However, when methotrexate is determined by the radioimmune method, interference does not occur.
Trimethoprim and sulfamethoxazole can affect the results of the Jaffe test (determination of creatinine by reaction with picric acid in an alkaline medium), and in the normal range the results are overestimated by approximately 10%.
Impact on the ability to drive vehicles and operate machinery
Considering the possibility of developing significant side effects, during the treatment period it is necessary to be careful when driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Mode of application
Adults and children over 12 years old. Usually the initial dose is two tablets 2 times a day (morning and evening). The tablets should be taken after meals with plenty of liquid. For severe infections, higher daily doses can be prescribed - up to 3 tablets 2 times a day. For maintenance therapy lasting more than 14 days, it is recommended to take one tablet 2 times a day.
Children 6-12 years old. The recommended daily dose for children is 6 mg of trimethoprim and 30 mg of sulfamethoxazole per kg of body weight. This dose should be divided into two doses.
The recommended daily dose for children aged 6 to 12 years is one tablet 2 times a day.
Duration of treatment: for acute infections, with the exception of gonorrhea, treatment should continue for at least 5 days or another 2 days after the symptoms of the disease disappear. A three-day course of treatment may be sufficient for women with uncomplicated acute cystitis. However, children with this disease are recommended to use the drug for 5-7 days.
Features of application
Pregnant
This drug should not be used during pregnancy and breastfeeding.
Children
The drug is used to treat children over 6 years of age.
Drivers
The drug does not cause a decrease in psychophysical activity and the ability to drive vehicles and operate machinery. If during treatment side effects from the nervous system develop (dizziness, headache, convulsions, nervousness, feeling tired), which can cause a decrease in the speed of psychomotor reactions, you should avoid driving vehicles and working with complex mechanisms.
Overdose
It is unknown what dose of the drug can be life-threatening. In case of an overdose of sulfonamides, loss of appetite, colicky pain, nausea, vomiting, diarrhea, dizziness, headache, drowsiness, and loss of consciousness are observed. Fever, hematuria and crystalluria may appear; with chronic overdose, bone marrow suppression and hepatitis may develop. In case of an acute overdose of trimethoprim, nausea, vomiting, dizziness, headache, mental depression, confusion, and suppression of bone marrow function may occur.
If symptoms of overdose appear, you must stop using the drug, induce vomiting, take a large amount of fluid if diuresis is insufficient and renal function is normal. Acidification of urine will speed up the elimination of trimethoprim, but will increase the risk of sulfonamide crystallization in the kidneys. The patient's blood picture, serum electrolytes and other biochemical parameters should be monitored. If bone marrow damage or symptoms of hepatitis occur, the usual treatment for such cases should be applied. Hemodialysis is ineffective. Peritoneal dialysis is ineffective.
In chronic poisoning, depression of spinal cord function is observed, manifested by thrombocytopenia, leukopenia or megaloblastic anemia. In this case, leucovorin (5-15 mg per day) should be used.
Biseptol® 480 (Biseptol® 480)
Hypersensitivity and allergic reactions:
At the first appearance of skin rash or any other severe adverse reaction, the drug should be discontinued. Patients with a tendency to allergic reactions and bronchial asthma should be prescribed co-trimoxazole with caution.
Infiltrates in the lungs (like eosinophilic and allergic alveolitis) can manifest themselves with symptoms such as cough or shortness of breath. If these symptoms appear or suddenly increase, it is necessary to re-examine the patient and consider stopping treatment with co-trimoxazole.
Kidney disorders:
Sulfonamides, including co-trimoxazole, may increase diuresis, especially in patients with edema caused by heart failure. Careful monitoring of renal function and serum potassium concentrations is necessary in patients receiving high doses of co-trimoxazole (including in the treatment of pneumonia caused by P. jirovecii), as well as in the following groups of patients: patients with a history of impaired potassium metabolism receiving standard doses drug; patients with renal failure; patients receiving drugs that contribute to the development of hyperkalemia.
Serious adverse reactions:
Fatalities, although rare, have been reported due to adverse reactions such as blood abnormalities, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), drug reaction with eosinophilia and systemic manifestations (DRESS syndrome) and fulminant liver necrosis.
Special patient groups:
in elderly and senile patients, as well as in patients with concomitant diseases, for example, impaired renal and/or liver function, or while taking other drugs, there is an increased risk of severe adverse reactions; in these cases, the risk is related to the dose and duration of therapy. Patients should be informed of the signs and symptoms of these serious side effects and closely monitored for skin reactions.
The risk of severe skin reactions is greatest in the first few weeks of treatment. If signs or symptoms of severe skin reactions occur (eg, progressive rash, often with blisters or associated mucosal lesions), cotrimoxazole therapy should be discontinued. The course of these reactions is largely determined by early diagnosis and immediate cessation of all suspected medications, which improves the prognosis. Following the occurrence of severe skin reactions associated with the use of co-trimoxazole, the patient should never re-use co-trimoxazole.
The duration of treatment with co-trimoxazole should be as short as possible, especially in elderly and senile patients.
If renal function is impaired, the dose should be adjusted. Patients with severe renal impairment (creatinine clearance 15-30 ml/min) receiving co-trimoxazole should be carefully monitored for the development of symptoms of toxicity (nausea, vomiting, hyperkalemia).
In elderly and senile patients, as well as in patients with pre-existing folic acid deficiency or renal failure, hematological changes characteristic of folic acid deficiency may occur. They disappear after administration of folic acid.
Due to the possibility of hemolysis, co-trimoxazole should not be prescribed to patients with glucose-6-phosphate dehydrogenase deficiency.
As with any sulfonamides, caution must be exercised in patients with thyroid dysfunction.
Patients whose metabolism is characterized by “slow acetylation” are more likely to develop idiosyncrasy to sulfonamides.
Long-term therapy:
with long-term administration of co-trimoxazole, it is necessary to regularly determine the number of blood cells.
If there is a significant decrease in the number of any blood cells, co-trimoxazole should be discontinued.
Patients receiving long-term treatment with co-trimoxazole (especially with renal failure) should regularly undergo a general urine test and monitor kidney function. During treatment, it is necessary to ensure sufficient fluid intake and adequate diuresis to prevent crystalluria.
Pseudomembranous colitis caused by Clostridium difficile
, may appear both during long-term use and 2-3 weeks after stopping treatment; manifested by diarrhea, leukocytosis, fever, abdominal pain (sometimes accompanied by the release of blood and mucus in the stool). If these phenomena occur, in mild cases, it is sufficient to discontinue treatment and use ion exchange resins (colestyramine, colestipol); in severe cases, replacement of the loss of fluid, electrolytes and protein, and the appointment of oral vancomycin or metronidazole are indicated. Do not use medications that inhibit intestinal motility.
The drug Biseptol 480 should not be used in the treatment of pharyngitis caused by beta-hemolytic streptococci from group A. The eradication of these bacteria in the nasopharynx with this drug is less effective than with the use of penicillin.
The administration of co-trimoxazole should be avoided in patients with established porphyria or in patients at risk of developing porphyria. Both trimethoprim and sulfonamides (although not specific to sulfamethoxazole) are associated with clinical exacerbations of porphyria.
Due to the propylene glycol content (2000 mg/5 ml), the drug may cause symptoms similar to those that occur after drinking alcohol.
One ampoule of the drug contains 12.4% vol. ethanol (alcohol), i.e. up to 500 mg/5 ml, which is equivalent to 11.88 ml beer or 4.95 ml wine. It is harmful for patients with alcohol disease. The alcohol content should be taken into account when using the drug in pregnant or breastfeeding women, children and patients at high risk, such as those with liver disease or epilepsy.
Biseptol 480 contains sodium disulfite (5 mg/5 ml), which in rare cases can cause severe hypersensitivity reactions and bronchospasm.
The drug Biseptol 480 contains sodium (39 mg/5 ml). This should be taken into account in patients on a controlled sodium diet.
Biseptol 480 contains two antibacterial components. The drug Biseptol 480 should be used only in cases where, in the opinion of the doctor, the expected benefit from its use exceeds any possible risk; the possibility of using single-component effective antibacterial drugs should be considered.
Interaction
Zidovudine: in some cases, the simultaneous use of co-trimoxazole and zidovudine increases the risk of hematological disorders caused by Biseptol. If it is necessary to use co-trimoxazole and zidovudine simultaneously, blood counts should be monitored.
Folinic acid Supplementation with folic acid has been shown to influence the antimicrobial efficacy of trimethoprim-sulfamethoxazole. This was observed in the prevention and treatment of pneumonia caused by Pneumocystis jiroveci.
Biseptol®
Pharmacokinetic interaction
Trimethoprim is an inhibitor of organic cation transporter 2 (OCT2), as well as a weak inhibitor of the CYP2C8 isoenzyme. Sulfamethoxazole is a weak inhibitor of the CYP2C9 isoenzyme.
Systemic exposure to drugs transported by OCT2 (eg, dofetilide, amantadine, memantine, and lamivudine) may be increased when trimethoprim-sulfamethoxazole is coadministered.
Trimethoprim-sulfamethoxazole and dofetilide should not be used simultaneously. Trimethoprim inhibits the renal excretion of dofetilide, increases the area under the concentration-time curve AUC by 103% and the maximum concentration of dofetilide by 93%. Increasing concentrations of dofetilide may cause serious ventricular arrhythmias with QT prolongation, including torsades de pointes.
Patients receiving amantadine or memantine have an increased risk of developing nervous system adverse events (such as delirium and myoclonus).
Systemic exposure to drugs predominantly metabolized by CYP2C8 (e.g., paclitaxel, amiodarone, dapsone, repaglinide, rosiglitazone and pioglitazone) may be increased when trimethoprim-sulfamethoxazole is coadministered.
Paclitaxel and amiodarone have a low therapeutic index; their simultaneous use with trimethoprim-sulfamethoxazole is not recommended.
Dapsone and trimethoprim-sulfamethoxazole may cause the development of methemoglobinemia, as there is a potential for their pharmacokinetic and pharmacodynamic interactions. Patients receiving dapsone and trimethoprim-sulfamethoxazole should be closely monitored for the development of methemoglobinemia. If necessary, alternative therapy should be prescribed. Patients receiving repaglinide or pioglitazone should be regularly monitored for the development of hypoglycemia.
Systemic exposure to drugs predominantly metabolized by the CYP2C9 isoenzyme (for example, coumarins (warfarin, acenocoumarol), phenytoin and sulfonylurea derivatives (glibenclamide, gliclazide and glipizide)) may be increased when combined with trimethoprim-sulfamethoxazole.
Blood clotting should be monitored in patients receiving coumarins. Biseptol may inhibit the hepatic metabolism of phenytoin. After administration of standard doses of trimethoprim and sulfamethoxazole, an increase in the half-life of phenytoin by 39% and a decrease in its clearance by 27% were observed. Patients receiving phenytoin should be monitored for phenytoin toxicity. Patients receiving sulfonylurea derivatives (glibenclamide, gliclazide and glipizide) should be monitored for the development of hypoglycemia.
The drug Biseptol can reduce the effectiveness of oral contraceptives. During therapy with Biseptol, women are recommended to use additional methods of contraception.
The simultaneous use of trimethoprim-sulfamethoxazole and indomethacin may cause an increase in the concentration of sulfamethoxazole in the blood plasma.
Biseptol may increase serum digoxin concentrations, especially in elderly patients, so monitoring of serum digoxin concentrations is necessary.
Pharmacodynamic interactions and interactions with unknown mechanism
The incidence and severity of myelotoxic and nephrotoxic adverse events may be increased with concomitant use of trimethoprim-sulfamethoxazole and other drugs that have a myelosuppressive effect or can cause renal impairment (nucleoside analogues, tacrolimus, azathioprine or mercaptopurine). Patients receiving such drugs concomitantly with trimethoprim-sulfamethoxazole should be monitored for the development of hematologic and/or renal toxicity.
Concomitant use with clozapine should be avoided, since the latter is known to cause agranulocytosis.
In elderly and senile patients, with the simultaneous use of certain diuretics (mainly thiazide), an increase in the number of cases of thrombocytopenia was observed.
In patients receiving diuretics, platelet levels in the blood should be regularly monitored.
Patients receiving trimethoprim-sulfamethoxazole and cyclosporine after renal transplantation may experience a reversible deterioration in renal function.
Sulfonamides, including sulfamethoxazole, may compete for protein binding and renal transport of methotrexate, thereby increasing free methotrexate concentrations and systemic effect.
Cases of pancytopenia have been described in patients taking trimethoprim and methotrexate. Trimethoprim has low affinity for human dehydrofolate reductase, but may increase the toxicity of methotrexate, especially in the presence of risk factors such as old age, hypoalbuminemia, renal impairment, bone marrow suppression, and in patients receiving high doses of methotrexate. To prevent myelosuppression, such patients should be prescribed folic acid or calcium folinate.
It can be assumed that when trimethoprim-sulfamethoxazole is co-administered to patients receiving pyrimethamine for malaria prophylaxis in doses greater than 25 mg per week, they may develop interregional anemia. Caution must be exercised during the simultaneous use of trimethoprim-sulfamethoxazole and drugs that increase the concentration of potassium in the blood serum (such as ACE inhibitors, angiotensin receptor blockers, potassium-sparing diuretics and prednisolone), due to the potassium-sparing effect of trimethoprim-sulfamethoxazole.
In addition to other drugs that may cause hyperkalemia, the combined use of trimethoprim-sulfamethoxazole (co-trimoxazole) and spironolactone may result in clinically significant hyperkalemia.
Laboratory research
Trimethoprim-sulfamethoxazole and, in particular, trimethoprim, which is part of it, may affect the results of determining the concentration of methotrexate in serum, carried out by the competitive protein binding method using bacterial dihydrofolate reductase as a ligand. However, when methotrexate is determined by the radioimmune method, there is no influence.
Trimethoprim and sulfamethoxazole can also affect the results of the Jaffe test (determination of creatinine by reaction with picric acid in an alkaline medium), and in the normal range the results are overestimated by approximately 10%.
Note!
Description of the drug Biseptol table. 400mg/80mg No. 20 on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.
BISEPTOL (tablets)
– can be crushed.
Each tablet is marked with a “Bs” sign and has a notch. This means that it can be divided: Many people are interested in this question: Is Biseptol an antibiotic or not? No, this drug belongs to the sulfonamides, but these drugs have a common goal - to fight microbes. And not only with pathogenic ones, therefore, during or after treatment, these drugs also need to restore the intestinal microflora.
The main composition can be seen on the packaging:
Pay attention to excipients, in particular preservatives. Yes, yes, you were not mistaken, these are the same parabens that so scare ardent supporters of natural cosmetics. Many people are afraid of creams with parabens like fire, not even suspecting that they are ingesting them with some medications and even food products.
Why are they added there? Yes, because these are the cheapest and most studied preservatives to date. They provide a fairly long shelf life to the products they are added to and are well tolerated by the body.
Some time ago, rumors appeared about their involvement in the occurrence of cancer and other unpleasant diseases. But these are just hypotheses that do not yet have any scientific confirmation and require careful additional research.
In the wake of these rumors, manufacturers, fearing to scare off consumers, add other, less studied preservatives to cosmetics, etc., which may be even more dangerous than these. After all, without preservatives, nothing can be stored for more than a few days. But natural options cannot provide such a long shelf life.
Therefore, I am loyal to parabens. But, naturally, I don’t abuse them. After all, as Paracelsus said: “Everything is poison, and everything is medicine. Both are determined only by the dose.”
And here are the storage conditions:
The full composition, as well as indications, contraindications and recommendations for use can be read in the attached instructions:
HOW IS CHILDREN'S BISEPTOL 120 DIFFERENT FROM ADULT 480?
First of all, the dosage, so the packaging is much more compact:
Their composition is identical in terms of the presence of certain substances:
The instructions are the same (see above). Therefore, Biseptol 480 can also be given to children by adjusting the dose (remember the notch that allows you to divide the tablet).
And, of course, the size of the tablet:
Here the diameter is about 8 mm. Here's a comparison photo:
IMPRESSIONS OF USE
So, I have about 20 years of experience using this product. I think this is a fair amount of time to draw appropriate conclusions.
I took it myself and gave it to my son (in the past, pediatricians often prescribed Biseptol to children). Basically, the intake was associated with the occurrence of complications after suffering from acute respiratory viral infections in the form of otitis, sinusitis, tracheitis and bronchitis. I can’t say anything bad about it - the drug has always worked conscientiously. Despite the impressive list of side effects, no negative reactions were observed in me, my husband, or my son during all this time.
I don’t even remember how much these drugs cost. Now the price of such Biseptol 480 in online pharmacies is about 100 rubles.
CONCLUSION
I haven't used Biseptol for several years now. The medications in the photo were purchased just in case for a trip to the village (the pharmacy is far away - you never know if you need it urgently). The adult version recently came in handy for my husband - he still loves it. I never gave it to my daughter at all.
The fact is that now many new antibacterial agents have appeared with a less impressive range of possible side effects and a wider spectrum of action. Often they have virtually no serious contraindications. And the microbes have not yet had time to adapt to them. Of course, I'm inclined to choose them.
But if the need arises and there is no new generation drug at hand, I will use Biseptol without hesitation.
