Bikotrim

Bikotrim is an artificial antibacterial substance from the category of sulfonamides. It is a combined agent containing trimethoprim as well as sulfamethoxazole.

Sulfamethoxazole is similar in its structure to PABA; it destroys the binding of dihydrofolic acid inside microbial cells, preventing the incorporation of PABA into its molecule.

Trimethoprim potentiates the activity of sulfamethoxazole, preventing the restoration of dihydrofolic acid with its conversion to tetrahydrofolic acid (a type of B9-vitamin with activity), which is responsible for protein metabolism and division of the bacterial cell.

Indications Bikotrima

It is used for the following infections:

• infections of the urogenital tract: cystitis, prostatitis with urethritis, pyelonephritis and pyelitis, and in addition chancroid, gonorrhea (both men and women), epididymitis, groin granuloma and donovanosis;
• lesions of the respiratory tract: bronchopneumonia, as well as croupous pneumonia, bronchitis (active and chronic phases), pneumocystosis and bronchiectasis;
• diseases affecting the ENT organs: sinusitis with sore throat, and at the same time otitis media, scarlet fever or laryngitis;
• gastrointestinal infections: paratyphoid fever, cholecystitis, salmonellosis with typhoid fever, and in addition cholangitis, dysentery, cholera and gastroenteritis, provoked by the action of enterotoxic strains of E. Coli;
• lesions of the subcutaneous layers and the epidermis: pyoderma, acne, infections of a traumatic nature and furunculosis;
• osteomyelitis (in chronic or active phase) and other infections of osteoarthritic character, active stage of brucellosis, paracoccidioidosis, malaria (plasmodium falciparum) and toxoplasmosis (combination therapy).

Release form

The release of drugs is made in the form of a child's oral suspension (0.24 g / 5 ml) - inside the bottle with a capacity of 60 or 100 ml. The kit also contains a measuring cup.

Pharmacodynamics

Bactericidal medicine with a large range of influence with respect to such bacteria:

• streptococci (hemolytic strains that are sensitive to penicillin), staphylococci, pneumococci and gonococci with meningococci;
• Salmonella (among them Salmonella paratyphi with Salmonella typhi), intestinal sticks (this includes enterotoxinic strains), Listeria, Vibrio cholerae, hemophilic sticks (strains that demonstrate sensitivity with respect to ampicillin), Klebsiella and Bacillus anthrax;
• Pertussis sticks, Nocardia asteroids, proteas, fecal enterococci, pasteurella, brucella and tularemia sticks;
• mycobacteria (among them Bacillus Hansen), enterobacteria with citrobacteria, Providencia, morganella and legionella pneumophilus;
• serrations of marzescense, some varieties of pseudomonads (excluding Pseudomonas bacilli), Yersinia with shigella, Pneumocystis carinii and chlamydia (this includes chlamydophilia psittaci and Chlamydia trachomatis);
• simple: coccidioides immitis, pathogenic fungi, plasmodia, Toxoplasma gondii, Histoplasma capsulatum, Actinomyces Israel and Leishmania.

Resistance is demonstrated by: Aseptic purulent bacilli, treponemas, Corynebacteriums, Koch sticks, viruses, and Leptospira spp.

Weakens the activity of Escherichia coli, thanks to which the indices of riboflavin with thymine, B-vitamins and niacin decrease inside the intestine. Drug effect lasts 7 hours.

Pharmacokinetics

Absorption after oral administration is 90%. Values TCmax are 1-4 hours. When administered once, the drug retains a therapeutic concentration for 7 hours.

The drug is subjected to a uniform distribution within the body, overcoming histohematogenous barriers. Inside urine and lungs, indicators are formed that exceed the plasma level. Smaller volumes of drugs accumulate inside the vaginal secretions, tissues and secretions of the prostate, cerebrospinal fluid, bronchial secretions, sredneuschnaya fluid, saliva with bile, breast milk, bones and aqueous ophthalmic moisture with interstitial fluid. Intraplasmic protein binding is 66% (for sulfamethoxazole) and 45% (for trimethoprim).

The exchange processes of sulfamethoxazole mainly proceed with the formation of acetyl derivatives. Metabolic components do not have an antimicrobial effect.

Excreted by the kidneys - in the form of metabolic elements (80% in 72 hours), as well as in an unchanged state (20% sulfamethoxazole and 50% trimethoprim); the remainder is excreted by the intestines.

The term half-life of sulfamethoxazole is 9-11 hours, and trimethoprim is 10-12 hours. In children, this indicator is almost not noticeable and depends on age; up to 12 months - 7-8 hours; within 1-10 years - 5-6 hours.

In people with kidney problems and the elderly, the term half-life increases.

Dosing and administration

When infections occur without complications:

• infants 2-5 months of age - 2.5 ml of the substance 2 times a day;
• children of 0.5-5 years old - 5 ml of the drug 2 times a day;
• Children 6-12 years of age - 10 ml of drugs 2 times a day.

[1]

Use Bikotrima during pregnancy

It is forbidden to use the drug during breastfeeding or pregnancy.

Contraindications

The main contraindications:

• strong personal sensitivity (also in relation to sulfonamides);
• lack of kidney or liver function;
• anemia of aplastic or pernicious nature;
• leukopenia or agranulocytosis;
• lack of G6FD component.

Side effects Bikotrima

Among the adverse events:

• dysfunction of the NA: dizziness or headaches. Perhaps the development of depression, tremor, as well as having the aseptic nature of meningitis, peripheral neuritis and apathy;
• problems with the work of the respiratory system: infiltrates inside the lungs and bronchial spasms;
• digestive disorders: diarrhea, abdominal pain, vomiting, stomatitis, loss of appetite, glossitis and nausea. In addition, hepatitis, cholestasis, enterocolitis of pseudomembranous nature, an increase in the activity of intrahepatic transaminases and hepatonecrosis;
• lesions of the blood-forming organs: thrombocyto-, leuko- or neutropenia, anemia of a megaloblastic nature and agranulocytosis;
• infections of the urinary system: crystalluria, polyuria, hematuria, tubulointerstitial nephritis, an increase in urea, kidney disorder, toxic nephropathy (with anuria and oliguria) and hypercreatininemia;
• problems associated with the work of musculoskeletal system: myalgia or arthralgia;
• signs of allergy: rash, angioedema, fever, itching, IEE (this includes SSD), photosensitivity, myocarditis of an allergic nature, PET, exfoliative type of dermatitis and hyperemia, affecting the sclera;
• other symptoms: hypoglycemia.

Overdose

When poisoning occurs, confusion, vomiting or nausea.

It is necessary to stop the application of Bicotrim, to conduct gastric lavage (maximum after 2 hours from the moment of intoxication) and to give the victim to drink plenty of fluids. Intensive diuresis is also performed, and Ca folinate is prescribed (5-10 mg per day).

Interactions with other drugs

It has drug compatibility with such substances: 5% and 10% dextrose (intravenous infusions), 5% levulose (intravenous infusions), 0.9% NaCl (w / w infusion), and a combination of 0, 18% NaCl with 4% Dextrose (w / w infusion). Still on the list is 6% dextran 70 or 10% dextran 40 (by intravenous infusion) in combination with 5% dextrose or 0.9% NaCl, and besides this, Ringer's injection solution.

The drug increases the anticoagulant effect of indirect anticoagulants and the activity of methotrexate and antidiabetic agents.

Weakens the severity of intrahepatic metabolism of phenytoin (39% prolongs its half-life term) and warfarin, potentiating their effects.

Reduces the reliability of oral contraceptives (suppresses intestinal flora and reduces the circulation of hormonal elements inside the liver and intestines).

The term half-life of trimethoprim is reduced when combined with rifampicin.

Pyrimethamine in portions of more than 25 mg per week increases the likelihood of anemia of a megaloblastic nature.

Diuretic substances (mainly thiazides) increase the risk of thrombocytopenia.

Therapeutic efficacy decreases when combined with procainum, benzocaine or procainamide (and other drugs, during the hydrolysis of which PABK is formed).

Between diuretic drugs (furosemide, thiazides, etc.), as well as oral anti-diabetic drugs (sulfonylurea derivatives) on the 1st side, and in addition antimicrobial sulfonamides with the 2nd, there can be a cross-allergic effect.

Barbiturates with phenytoin and PASK potentiate the symptoms of B9-vitamin deficiency.

Salicylic acid derivatives potentiate the Bicotrim effect.

Vitamin C and hexamethylenetetramine (and other substances that acid urine) increase the likelihood of crystalluria.

The weakening of the absorption of drugs is observed when combined with Kolestiramine - because of this, the latter is used after 1 hour after or 4-6 hours before the introduction of co-trimoxazole.

Medications suppress the hematopoietic processes inside the bone marrow, increase the likelihood of myelosuppression.

[2], [3]

Storage conditions

Bikotrim needs to be stored inside a tightly corked bottle. Temperature - not more than 25 ° С. It is forbidden to freeze the suspension.

Shelf life

Bikotrim can be applied within the 2-year term from the moment of manufacture of the drug.

Application for children

Not prescribed to children if they are diagnosed with hyperbilirubinemia.

Analogs

Analogues of the drug are drugs Bakteptol, Groseptol, Biseptol with Bactrim, and in addition, Oriprim, Bel-septol, Solyuceptole with Bi-septa, Biseptrim and Trisptol. Also on the list are Bi-tol, Raseptol, Blepeseptol with Sumetrolim and Co-Trimoxazole.