Biseptol - Instructions, Use For Children, Price, Tablets, Suspension

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Biseptol

Biseptol: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Biseptol

ATX code: J01EE01

Active ingredient: co-trimoxazole (sulfamethoxazole + trimethoprim) [co-trimoxazole (sulfamethoxazole + trimethoprim)]

Producer: Pabianice Pharmaceutical Works Polfa (Poland), Medana Pharma, SA (Poland)

Description and photo update: 2019-19-08

Prices in pharmacies: from 28 rubles.

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Biseptol is a combined antibacterial drug.

Release form and composition

Biseptol form of release:

• tablets of 120 and 480 mg: flat, round, yellowish (in blisters of 20 pcs., 1 blister in a cardboard box);
• oral suspension: light cream, with the smell of strawberries (in dark glass bottles of 80 ml, 1 bottle in a cardboard box).

1 tablet contains:

• sulfamethoxazole - 100 mg or 400 mg;
• trimethoprim - 20 mg or 80 mg.

5 ml of suspension contains:

• sulfamethoxazole - 200 mg;
• trimethoprim - 40 mg.

Pharmacological properties

Pharmacodynamics

Co-trimoxazole - the active substance of Biseptol - is a combined antimicrobial drug consisting of sulfamethoxazole and trimethoprim in a 5: 1 ratio.

Sulfamethoxazole is structurally similar to PABA (para-aminobenzoic acid), in bacterial cells it disrupts the synthesis of dihydrofolic acid, which prevents the incorporation of PABA into its molecule.

Trimethoprim enhances the action of sulfamethoxazole, which occurs due to a violation of the reduction of dihydrofolic acid to tetrahydrofolic acid, which is an active form of folic acid, which is responsible for microbial cell division and protein metabolism.

With the combined action of the components, the process of formation of folic acid is disrupted, which is required for the synthesis of purine compounds by microorganisms, and after that of nucleic acids - DNA and RNA (deoxyribonucleic and ribonucleic acids). This leads to a violation of the formation of proteins and the death of bacteria.

Biseptol is one of the broad-spectrum bactericides, but the sensitivity of its effects may depend on geographic location.

Usually sensitive pathogens [MIC (minimum inhibitory concentration) for sulfamethoxazole - less than 80 mg / l)]: Haemophilus influenzae (beta-lactamase-forming and beta-lactamase-forming strains), Moraxella (Branhamella) catarrhalis, Escherichia coli (including enterotoxin strains), Vibrio cholerae, Alcaligenes faecalis, Edwardsiella tarda, Proteus vulgaris, Proteus mirabilis, Morganella morganii, Shigella spp. (including S. flexneri. S. sonnet), Yersinia spp. (including Y. enterocolitica), Burkholderia (Pseudomonas) pseudomallei, Burkholderia (Pseudomonas) cepacia, Haemophilus parainfluenzae, Citrobacter spp. (including C. freundii), Klebsiella spp. (including K. pneumoniae, K. oxytoca), Enterobacter aerogenes, Enterobacter cloacae, Hafnia alvei, Serratia spp. (including S. marcescens, S. liquefaciens).

Also, sensitivity to Biseptol can be manifested by Listeria monocytogenes, Cyclospora cayetanensis, Nocardia asteroides, Pneumocystis carinii, Brucella spp.

Partially sensitive pathogens (MIC for sulfamethoxazole - 80–160 mg / l): coagulase-negative strains of Staphylococcus spp. (including methicillin-sensitive and methicillin-resistant strains of Staphylococcus aureus), Streptococcus pneumoniae (penicillin-resistant and penicillin-susceptible strains), Aeromonas hydrophila, Acinetobacter baumannii, Acinetobacter lwoffii, Haemophilus, Provyphilus (including Providencia rettgeri), Salmonella enteritidis, Salmonella typhi, Stenotrophomonas maltophilia (Xanthomonas maltophilia).

Resistant pathogens (MIC for sulfamethoxazole - more than 160 mg / l): Pseudomonas aeruginosa, Mycoplasma spp., Treponema pallidum, Mycobacterium tuberculosis.

When empirically prescribing Biseptol, local features of resistance to its effects of possible causative agents of a specific infectious disease should be taken into account. When treating infections that may be caused by partially sensitive microorganisms, a sensitivity test is recommended to exclude the resistance of the pathogen.

Pharmacokinetics

Absorption of Biseptol when taken orally is fast and almost complete (90%).

After a single use of 160 mg of trimethoprim + 800 mg of sulfamethoxazole C _max (maximum concentration of the substance) of trimethoprim and sulfamethoxazole is 1.5–3 μg / ml and 40–80 μg / ml, respectively. Time to reach C _max in blood plasma is from 1 to 4 hours. After a single dose, the therapeutic level of concentration is maintained for 7 hours. With repeated use with a break of 12 hours, the minimum C _ss (equilibrium concentrations) are stabilized in the range of 1.3–2.8 μg / ml and 32–63 μg / ml for trimethoprim and sulfamethoxazole, respectively. C _{ss is} achieved in 2–3 days.

Co-trimoxazole is well distributed in the body. The V _d (volume of distribution) of trimethoprim and sulfamethoxazole is approximately 130 L and 20 L, respectively.

Penetrates through the blood-brain and placental barriers, as well as into breast milk. In urine and lungs, it creates concentrations that are higher than plasma concentrations.

Trimethoprim slightly better than sulfamethoxazole penetrates into non-inflamed prostate tissue, vaginal secretions, bile, seminal fluid, saliva, inflamed and healthy lung tissue. Both active components penetrate equally well into the aqueous humor of the eye and cerebrospinal fluid.

Trimethoprim (large amounts) and sulfamethoxazole (slightly smaller amounts) enter the interstitial and other extravasal body fluids from the bloodstream. The concentration of active substances is higher than the MIC for most pathogenic microorganisms.

Plasma protein binding: sulfamethoxazole - 66%, trimethoprim - 45%.

Metabolism takes place in the liver. Sulfamethoxazole is metabolized mainly by N4-acetylation, to a lesser extent by conjugation with glucuronic acid. Some metabolites have antimicrobial activity.

It is excreted mainly in the form of metabolites (within 72 hours - 80%) and as an unchanged substance (sulfamethoxazole - 20%, trimethoprim - 50%). A small part of the dose is excreted through the intestines.

Both substances and their metabolites are excreted by the kidneys (both by glomerular filtration and tubular secretion). As a result, the concentration of both active components in the urine significantly exceeds the concentration in the blood.

T _1/2 (half-life): sulfamethoxazole - 9-11 hours, trimethoprim - 10-12 hours. In children, this indicator is much lower and depends on age: under 1 year old - from 7 to 8 hours, 1-10 years old - from 5 to 6 hours.

In elderly patients and / or patients with impaired renal function (with creatinine clearance 15–20 ml / min) T _1/2 increases (dose adjustment is necessary).

Indications for use

According to the instructions, Biseptol is prescribed for the treatment of infections:

• genitourinary system: pyelonephritis, urethritis, salpingitis, prostatitis;
• respiratory tract: bronchitis, pneumonia, lung abscess, pleural empyema, otitis media, sinusitis;
• skin and soft tissues: pyoderma, furunculosis;
• gastrointestinal tract: dysentery, cholera, typhoid fever, paratyphoid fever, diarrhea.

Contraindications

Absolute:

• severe blood diseases, including megaloblastic anemia, aplastic anemia, B ₁₂ deficiency anemia, leukopenia, agranulocytosis, anemia associated with folic acid deficiency;
• deficiency of glucose-6-phosphate dehydrogenase (associated with the risk of hemolysis);
• severe renal failure (with creatinine clearance less than 15 ml / min);
• diagnosed damage to the liver parenchyma (tablets);
• severe impairment of renal function in cases of inability to control the plasma concentration of the drug in the blood (tablets);
• hyperbilirubinemia in pediatric patients (tablets);
• liver failure (suspension);
• combined use with dofetilide (suspension);
• age up to 8 weeks, or up to 6 weeks at birth from a mother with HIV infection (suspension), or up to 3 years (tablets);
• lactation period;
• pregnancy (pills);
• individual intolerance to the components of the drug and sulfonamides.

Relative (Biseptol is prescribed under medical supervision):

• thyroid disease;
• bronchial asthma;
• folic acid deficiency;
• porphyria (suspension);
• burdened history of severe allergic reactions (suspension);
• pregnancy (suspension).

Instructions for the use of Biseptol: method and dosage

The regimen for taking the drug is determined by the doctor individually. Both dosage forms should be taken before meals.

Suspension and tablets Biseptol children over 12 years old and adults are usually prescribed 960 mg 2 times a day, with prolonged therapy, a single dosage is reduced by 2 times. The duration of therapy is determined by the disease and ranges from 5 to 14 days.

Dosing regimen of Biseptol for children:

• tablets: from 6 to 12 years old - 4 tablets of 120 mg or 1 tablet of 480 mg; from 3 to 5 years - 2 tablets of 120 mg;
• suspension: from 6 to 12 years - 480 mg each, from 6 months to 5 years - 240 mg each, from 2 to 5 months - 120 mg each.

The frequency of taking Biseptol is 2 times a day, observing a 12-hour interval between doses.

When treating pneumonia, the dose is calculated based on body weight - 100 mg / kg / day. The interval between doses should not exceed 6 hours, the duration of therapy is 2 weeks.

In the treatment of gonorrhea, Biseptol is taken twice a day, 2000 mg (in terms of sulfamethoxazole) with an interval of 12 hours.

The standard dosage of Biseptol can be increased by 30-50% during the treatment of chronic diseases, and a lower dosage is usually used in cases of long-term treatment.

Side effects

The use of Biseptol can lead to disruption from various body systems:

• respiratory system: eosinophilic infiltrate, allergic alveolitis;
• nervous system: nervousness, headache, hallucinations, aseptic meningitis, dizziness, peripheral neuritis, ataxia, convulsions, depression, ringing in the ears, apathy;
• hematopoietic organs: anemia, neutropenia, leukopenia, eosinophilia, thrombocytopenia, hypoprothrombinemia, agranulocytosis, methemoglobinemia;
• digestive system: acute pancreatitis, stomatitis, hyperbilirubinemia, hepatonecrosis, gastritis, nausea, decreased appetite, vomiting, diarrhea, abdominal pain, glossitis, cholestasis, increased activity of hepatic transaminases, hepatitis;
• musculoskeletal system: myalgia, arthralgia, rhabdomyolysis;
• urinary system: impaired renal function, interstitial nephritis, hematuria, hypercreatininemia, crystalluria.

Also, while taking Biseptol, various allergic reactions can develop, usually manifested as an increase in body temperature, angioedema, pruritus, photosensitivity, skin rash, urticaria, exudative erythema multiforme, toxic epidermal necrolysis, exfoliative dermatitis, conjunctival hyperemia, nodules, peri-arthritis, lupus-like syndrome.

Among other side effects during the use of Biseptol were noted: insomnia, hypoglycemia, hyperkalemia, fatigue, weakness, candidiasis.

Overdose

The main symptoms are:

• sulfamethoxazole: vomiting, nausea, intestinal colic, lack of appetite, headache, dizziness, loss of consciousness, drowsiness; development of fever, hematuria, crystalluria is also possible. Later symptoms include jaundice and bone marrow suppression;
• trimethoprim (acute poisoning): depression, vomiting, nausea, headache, dizziness, bone marrow suppression, impaired consciousness.

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

Chronic poisoning with co-trimoxazole (with long-term use in high doses) can lead to depression of bone marrow function, manifested by thrombocytopenia, megaloblastic anemia or leukopenia.

Therapy: the abolition of Biseptol and the implementation of measures aimed at removing it from the gastrointestinal tract (no later than two hours after taking the drug, wash the stomach or induce vomiting), drink plenty of fluids in cases where diuresis is insufficient, and renal function is not impaired … Also shown is the introduction of calcium folinate (intramuscularly, 5-15 mg per day). The excretion of trimethoprim is accelerated by the acidic environment of urine, but in this case, the likelihood of crystallization of sulfonamide in the kidneys increases.

Monitoring of the blood picture, the composition of electrolytes in the plasma and other biochemical parameters is recommended. Hemodialysis is of moderate effectiveness; peritoneal dialysis is ineffective in case of overdose.

special instructions

It is recommended to avoid excessive sun and ultraviolet radiation during therapy.

The risk of developing side effects is significantly higher in patients with AIDS.

Biseptol is not recommended for pharyngitis and tonsillitis caused by group A beta-hemolytic streptococcus.

With prolonged courses of treatment (longer than 1 month), due to the high likelihood of hematological changes, blood tests must be performed regularly.

The treatment of elderly patients and patients with suspected baseline folate deficiency requires special care.

The appointment of folic acid is advisable with long-term use of Biseptol in high doses.

Influence on the ability to drive vehicles and complex mechanisms

When driving vehicles during the period of therapy, the likelihood of developing such adverse reactions as fatigue, headache, nervousness, tremor should be taken into account.

Application during pregnancy and lactation

During pregnancy, Biseptol tablets are contraindicated, the suspension can be used after evaluating the benefit-risk ratio. In late pregnancy, it is recommended to avoid taking the drug, which is associated with the likelihood of kernicterus in newborns. Biseptol can affect the metabolism of folic acid, therefore, while using the drug, pregnant women are prescribed 5 mg of folic acid per day.

During lactation: therapy is contraindicated.

Pediatric use

Contraindications to Biseptol for children:

• suspension: up to 8 weeks, or up to 6 weeks at birth from a mother with HIV infection;
• tablets: up to 3 years.

With impaired renal function

Biseptol therapy is contraindicated in case of severe renal dysfunction (with creatinine clearance less than 15 ml / min).

When prescribing Biseptol in the form of tablets, patients with creatinine clearance of 15-30 ml / min should use half the standard dose.

For violations of liver function

Contraindication:

• tablets: diagnosed damage to the liver parenchyma;
• suspension: hepatic failure.

Use in the elderly

For elderly and senile patients, Biseptol should be prescribed as short a course as possible.

Drug interactions

• phenytoin: the intensity of hepatic metabolism of phenytoin decreases, due to which its effect and toxic effect are enhanced;
• diuretics (most often thiazides and in elderly patients): the risk of thrombocytopenia increases;
• drugs that inhibit bone marrow hematopoiesis: the risk of myelosuppression increases;
• ACE (angiotensin converting enzyme) inhibitors: hyperkalemia may develop (the risk is especially high in elderly patients);
• indirect anticoagulants: anticoagulant activity increases (correction of doses of anticoagulants is required);
• digoxin: its serum concentration may increase, and therefore it is required to monitor serum digoxin concentrations (especially high risk in elderly patients);
• dofetilide: the C _{max of} dofetilide increases by 93%, AUC - by 103%, such an increase in the concentration of dofetilide can cause ventricular arrhythmias with prolongation of the QT interval, including arrhythmias like feasts (this combination is contraindicated).

Analogs

Biseptol analogs are:

• by active ingredients: Co-trimoxazole, Bi-Septin, Briefseptol, Dvaseptol, Metosulfabol, Bactrim;
• by therapeutic action: Sulfaton.

Terms and conditions of storage

Shelf life up to 25 ° C:

• tablets - 5 years;
• suspension - 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Biseptol

According to reviews, Biseptol is used in the treatment of various inflammatory and infectious diseases. The cost of the drug is estimated to be affordable. In many cases, its high efficiency is noted in a short time. Some users point to a lack of therapeutic action.

The main disadvantage of Biseptol is the development of side reactions, among which allergic reactions are most often distinguished. It is also noted that 480 mg tablets are difficult to swallow due to their large size.

Biseptol in the form of a suspension has many positive reviews due to its convenient form of administration and the possibility of using it by both adults and children. Other advantages include pleasant aroma and taste, long shelf life after opening the package.

Price for Biseptol in pharmacies

The approximate price for Biseptol is: tablets (20 pcs. 120 mg each) - 25-37 rubles, tablets (28 pcs. 480 mg each) - 80-95 rubles, suspension (1 bottle of 80 ml each) - 111-137 rub.

Biseptol: prices in online pharmacies

Drug name Price Pharmacy

Biseptol 120 mg tablets 20 pcs. 28 RUB Buy

Biseptol tablets 120mg 20 pcs. RUB 33 Buy

Biseptol 480 mg tablets 28 pcs. RUB 85 Buy

Biseptol 240 mg / 5 ml oral suspension 80 ml 1 pc. RUB 98 Buy

Biseptol tablets 480mg 28 pcs. RUB 100 Buy

Biseptol 480 mg tablets 20 pcs. RUB 100 Buy

Biseptol 480 96 mg / ml concentrate for preparation of solution for infusion 5 ml 10 pcs. 383 r Buy

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!