Bi-tol

Bi-tol is an antimicrobial drug used for systemic therapy.

Indications Bi-tol

It is used for diseases, the development of which is provoked by the activity of bacteria sensitive to the drug:

• lesions in the respiratory tract (pneumonia with bronchitis, and in addition, pneumocystis pneumonia);
• inflammations affecting the middle ear and lateral sinuses;
• infections in the kidneys and urinary tract (pyelitis with urethritis, as well as pyelonephritis or cystitis);
• genital lesions of bacterial origin;
• diseases affecting the gastrointestinal tract and caused by the activity of strains of Shigella with Salmonella and E. coli;
• dermatitis of a purulent nature.

[ 1 ], [ 2 ]

Release form

The drug is released in the form of a suspension for oral administration, in 0.1 l bottles or jars, also equipped with a measuring cup.

Pharmacodynamics

The drug is complex, it contains the component sulfamethoxazole (a sulfanilamide that slows down the binding of vitamin B9), and in addition trimethoprim, which is a derivative of diaminopyridinium (it slows down the reductase of bacteria of dehydrofolic acid with a proportion of 5 to 1).

The drug has bactericidal and bacteriostatic properties. It has a wide range of therapeutic activity - relative to indole-positive strains of Proteus (this includes the common Proteus), Escherichia coli (this also includes enteropathogenic strains), Klebisella, Enterobacter with Morgan's bacteria, and in addition to Proteus mirabilis, Haemophilus influenzae, Pneumocystis carinii, Pneumococcus and Shigella flexneri with Shigella Sonnei.

[ 3 ], [ 4 ], [ 5 ], [ 6 ]

Pharmacokinetics

The drug is absorbed at high speed in the gastrointestinal tract. Serum Cmax values are noted after 1-4 hours, and the effect itself lasts for about 12 hours.

The substance passes into fluids with tissues: into the tonsils, lung tissue, cerebrospinal fluid secreted by the inner ear, kidneys, prostate, as well as vaginal and bronchial secretions. In addition, it is excreted with breast milk and passes through the placenta. The distribution volume index of sulfamethoxazole is 0.36 l/kg; trimethoprim - 2 l/kg. Metabolic processes of the drug occur in the liver.

Excretion of both substances occurs mainly through the kidneys. The biological half-life of sulfamethoxazole is 9-11 hours, and trimethoprim is 2 hours. The half-life of the drug in children is determined by their age: up to 12 months - within 7-8 hours; 1-10 years - 5-6 hours.

[ 7 ], [ 8 ], [ 9 ], [ 10 ]

Dosing and administration

The suspension is taken orally, after meals. Before use, the substance must be shaken to obtain a homogeneous mixture. The bottle also comes with a special measuring cup with divisions.

The medication is prescribed in the following doses:

• infants aged 0.5-2 years – in the amount of 2.5 ml (equivalent to 0.12 g) at 12-hour intervals;
• child's age within 3-5 years – dosage 5 ml (equivalent to 0.24 g) at 12-hour intervals;
• at the age of 6-12 years – take 10 ml (equivalent to 0.48 g) with 12-hour breaks;
• For adolescents aged 12 years and over and adults – use 20 ml (equivalent to 0.96 g) at 12-hour intervals.

The therapeutic cycle lasts 10-14 days (for infections in the gastrointestinal tract it is 5 days).

If the infection is caused by Pneumocystis carinii, it is necessary to use 0.1 g/kg of sulfamethoxazole per day, as well as 20 mg/kg of trimethoprim in equal portions, at 6-hour intervals, for 2-3 weeks.

[ 13 ]

Use Bi-tol during pregnancy

It is prohibited to take Bi-tol during pregnancy or breastfeeding.

Contraindications

Main contraindications:

• severe sensitivity to medicinal elements;
• renal or hepatic insufficiency of severe severity;
• anemia caused by vitamin B9 deficiency;
• agranulocytosis.

It is prohibited to prescribe to children suffering from hyperbilirubinemia, pharyngitis or tonsillitis of streptococcal origin.

[ 11 ]

Side effects Bi-tol

Taking the suspension can provoke the development of some side effects:

• Gastrointestinal dysfunction: vomiting with nausea and loss of appetite. Occasionally, abdominal pain, diarrhea, or inflammation of the gastric mucosa may occur;
• Allergy symptoms: often urticaria and rashes. Occasionally, itching, photosensitivity, erythema multiforme and exfoliative dermatitis may occur. Chills or fever may occur;
• disorders of hematopoiesis: neutro- or thrombocytopenia. Occasionally, megaloblastic anemia or agranulocytosis occurs;
• Others: dizziness, parenchymatous hepatitis, sleep disorders and treatable CNS dysfunctions occasionally develop, as well as hallucinations, headaches and renal dysfunction (hematuria, crystalluria or hypercreatininemia).

Rarely, severe adverse reactions to sulfonamides may occur: such as TEN and Stevens-Johnson syndrome. In addition, pancreatitis, acute liver necrosis, allergic myocarditis, aseptic meningitis, inflammation of the oral mucosa, apathy or depression, and pain in the muscles and joints may occur. Stomatitis, myalgia, pseudomembranous colitis, glossitis, pulmonary infiltration, arthralgia, and photophobia are observed occasionally.

[ 12 ]

Overdose

Intoxication with the drug results in the development of pronounced signs of adverse reactions. Among them are dizziness, nausea, drowsiness, colic, headaches, vomiting, visual disturbances and loss of consciousness. In addition, a feverish or depressive state, hematuria, a feeling of disorientation and crystalluria develop. Prolonged poisoning causes the development of jaundice, leukopenia or thrombocytopenia, as well as megaloblastic anemia.

To eliminate the disorders, stop taking the drug, perform gastric lavage and induce vomiting. It is also necessary to consult a medical specialist. Taking into account the damage that has occurred, symptomatic procedures are carried out. Hemodialysis will be ineffective.

[ 14 ]

Interactions with other drugs

Diphenin, hypoglycemic drugs, NSAIDs, barbiturates and anticoagulants with an indirect type of influence increase the likelihood of adverse effects.

Ascorbic acid increases the possibility of crystalluria formation.

Diuretics, especially thiazide diuretics, increase the risk of thrombocytopenia in the elderly. Bitol can increase serum digoxin levels in such patients.

Combination with tricyclics leads to a weakening of their medicinal properties.

The drug can potentiate the effect of diphenyl, anticoagulants and phenytoin, and at the same time reduce the effectiveness of oral contraception. In addition, the drug increases the serum values of the free fraction of methotrexate.

[ 15 ], [ 16 ]

Storage conditions

Bi-tol must be stored in a place out of reach of children, at a temperature of no more than 25ºС.

Shelf life

Bi-tol can be used within 36 months from the date of manufacture of the pharmaceutical product. After opening the package, the shelf life of the drug is 28 days.

Application for children

Should not be administered to infants under 6 months of age.

[ 17 ]

Analogues

Analogues of the drug are the drugs Baktiseptol, Oriprim, Triseptol and Baktrim with Groseptol. In addition, the list includes Bel-septol, Brifeseptol with Bi-sept, Co-trimoxazole and Bikotrim with Sumetrolim, as well as Raseptol, Biseptol, Soluseptol and Biseptrim.