Bi-sept

Bi-sept is a combination antimicrobial drug that contains two active ingredients: sulfamethoxazole and trimethoprim. This drug is usually used to treat infections caused by bacteria sensitive to its components.

1. Sulfamethoxazole: This component is a sulfa antibiotic that inhibits the growth and reproduction of bacteria by inhibiting the synthesis of folic acid, an important component required for bacterial growth.
2. Trimethoprim: Trimethoprim is also an antibiotic that inhibits the activity of a bacterial enzyme needed to synthesize folic acid. The combination of sulfamethoxazole and trimethoprim has a synergistic effect, enhancing the antibacterial action of the drug.

Indications Bi-sept

It is used for various infections, against the background of which inflammations are observed, provoked by the action of bacteria sensitive to the therapeutic agent:

• infections affecting the urogenital system;
• diseases affecting the lungs with bronchi and ENT organs;
• prevention of the occurrence of inflammation due to exposure to Pneumocystis carinii in people at risk;
• infections in the digestive system (paratyphoid fever with typhoid fever, cholecystitis with cholera, as well as colitis, dysentery and acute intestinal infections);
• disorders affecting soft tissues and epidermis;
• combination treatment for scarlet fever, meningitis with sepsis, and also for toxoplasmosis, osteomyelitis, cladotrichosis and Malta fever.

[ 1 ], [ 2 ]

Release form

The substance is released in tablets of 480 mg, inside blister packs, in the amount of 20 pieces. The box contains 1 blister pack.

Pharmacodynamics

The antimicrobial effect of sulfamethoxazole is based on the processes of antagonism towards PABA synthesized by bacteria. The drug selectively slows its entry into DHPA and inhibits the binding of dihydropteroate synthetase, which disrupts the formation of microbial nucleic acids, causing the death of the bacteria.

Trimethoprim disrupts the activity of the enzyme dihydrofolate reductase - blocks the formation of amino acids. Sulfamethoxazole with trimethoprim have a bacteriostatic effect and enhance their antimicrobial effect, thereby potentiating the antibacterial activity.

Bi-sept demonstrates activity against Escherichia coli, Brucella with Streptococcus, and also indol-positive strains of Proteus (common and Mirabilis), Shigella with Klebsiella, bacteria that provoke the development of malaria, Enterobacter and Influenza bacilli. In addition, the list includes Moraxella catarrhalis, Listeria monocytogenes, causative agents of pneumocytosis, as well as Morgan's bacteria and Nocardia asteroides.

The drug does not affect fungi and viruses.

[ 3 ], [ 4 ]

Pharmacokinetics

The drug is absorbed from the gastrointestinal tract, its Cmax values are recorded after 2 hours. The therapeutic effect lasts for a maximum of 12 hours, while the required level of the drug in the blood is maintained.

Synthesis of trimethoprim with albumin reaches 70%, and sulfamethoxazole – up to values within 44-62%. Peak values of the drug are observed in bronchial secretions, bile, kidneys and prostate.

The half-life of Bi-sept is 10 hours. The drug undergoes metabolic processes in the liver. Elimination occurs with urine.

[ 5 ], [ 6 ], [ 7 ]

Dosing and administration

The medicine is taken orally, with a 12-hour interval after meals. The medicine should be washed down with at least 0.3 liters of liquid.

Average dosages of the drug for adults: 2 tablets 2 times a day (with long-term maintenance treatment, take 1 tablet 2 times a day). Children aged 6-12 years are required to take 1 tablet 2 times a day. Children aged 3-6 years - 0.5 tablet 2 times a day.

As a prophylactic substance, Bi-sept can be used within 3-12 months.

In acute stages of infections, an average 7-14-day therapy cycle is required. In case of typhoid fever – 28-90 days. During Malta fever – up to 28 days.

For a child with inflammation in the urinary tract or otitis media, it is necessary to use portions calculated according to the scheme 48 mg/kg per day (divide the dosage into 2 uses).

During therapy for gonorrhea, take 4-6 tablets of the drug 3 times a day. For pharyngitis of gonorrheal origin - 9 tablets once for 5 days.

In case of inflammation inside the respiratory system caused by the activity of Рneumосуsтіs саrіnіі, take 90-120 mg/kg of the substance per day, at 6-hour intervals, for 2-3 weeks. Children should take 0.5 tablets 2 times per day; the treatment cycle lasts within 5-14 days.

For people with chronic renal failure, the dose is reduced by half, and if the SCF is below 15 ml/minute, the drug is not prescribed.

[ 17 ], [ 18 ]

Use Bi-sept during pregnancy

The drug should not be prescribed to pregnant or breastfeeding women, because it crosses the placenta and is also excreted in breast milk.

• Risk of congenital anomalies:

  • Studies suggest that use of trimethoprim and sulfamethoxazole in the first trimester of pregnancy may be associated with an increased risk of congenital anomalies, such as neural tube defects and cardiovascular anomalies. One study found an increased risk of congenital anomalies in women taking trimethoprim-sulfamethoxazole early in pregnancy (Czeizel et al., 2001).

• Effect on pregnancy:

  • According to a retrospective study, the use of trimethoprim-sulfamethoxazole during pregnancy is associated with an increased risk of preterm birth and low birth weight. The use of this drug was found to increase the risk of preterm birth (aOR 1.51) and low birth weight (aOR 1.67) (Yang et al., 2011).

• Fetotoxicity:

  • Studies have shown that sulfamethoxazole crosses the placenta and can reach significant concentrations in fetal tissues, which may be harmful to the developing embryo (Prokopczyk et al., 1979).

• Use in infections:

  • Despite potential risks, trimethoprim-sulfamethoxazole may be necessary to treat serious infections in pregnant women. In such cases, its use should be carefully weighed against the benefits and risks (Muanda et al., 2018).

Contraindications

Main contraindications:

• use in people with severe intolerance to the components of the drug;
• megaloblastic form of anemia, accompanied by a deficiency of vitamin B9, against which the SCF values are also noted to be below 15 ml/minute.

[ 8 ], [ 9 ], [ 10 ], [ 11 ], [ 12 ], [ 13 ]

Side effects Bi-sept

Bi-sept is usually tolerated without complications. Among the most frequently occurring negative symptoms are signs of dyspepsia. If the patient has individual hypersensitivity, allergic manifestations may occur in the form of erythema, itching and urticaria. Cases with the development of pseudomembranous colitis, inflammation in the liver and pancreas, and in addition to this, inflammation such as myalgia or arthralgia and symptoms of thrombophlebitis have also been recorded.

Occasionally, TEN, acute liver necrosis, hemolytic or aplastic anemia, allergic purpura, agranulocytosis and suppression of bone marrow activity appear.

The drug may cause symptoms of renal dysfunction, hypoglycemia or neuritis, as well as the appearance of tremor, tubulointerstitial nephritis or headaches.

Photosensitivity symptoms occur occasionally.

[ 14 ], [ 15 ], [ 16 ]

Overdose

When administering too large doses of the drug, headaches, dyspeptic symptoms, a feeling of drowsiness and a tendency to lose consciousness due to dizziness may occur. To provide assistance in such cases, gastric lavage and symptomatic procedures are performed.

If large doses of the drug are administered over a long period of time, the processes of red blood cell formation are suppressed, which can lead to thrombocytopenia and leukopenia.

[ 19 ], [ 20 ]

Interactions with other drugs

The combination of the drug and thiazide diuretics in elderly people causes potentiation of the suppression of bone marrow activity processes.

The medication enhances the properties of indirect anticoagulants and hypoglycemic agents from the sulfonylurea category.

Bi-sept can suppress the metabolic processes of phenytoin, due to which the duration of its medicinal effect increases.

The drug increases blood levels of cyclosporine, which increases the likelihood of developing negative symptoms of the latter along with potentiation of signs of nephrotoxicity.

The combination of methotrexate with trimethoprim may potentiate the symptoms of pancytopenia.

The drug increases the free fraction of methotrexate when used simultaneously due to the disruption of the synthesis of the latter with blood protein.

The drug and dofetilide cannot be combined, as this may lead to the development of ventricular arrhythmias.

[ 21 ], [ 22 ], [ 23 ], [ 24 ]

Storage conditions

Bi-sept should be kept in a place protected from moisture and small children. Temperature marks are within 15-25°C.

[ 25 ], [ 26 ]

Shelf life

Bi-sept can be used within 36 months from the date of production of the therapeutic drug.

[ 27 ], [ 28 ], [ 29 ]

Application for children

The medication should not be prescribed to children under 3 years of age.

Analogues

Analogues of the drug are Co-trimoxazole and Biseptol with Bactrim suspension.

[ 30 ], [ 31 ], [ 32 ]