Bicotrim

Bicotrim is an artificial antibacterial substance from the sulfonamide category. It is a combination drug containing trimethoprim and sulfamethoxazole.

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

Trimethoprim potentiates the activity of sulfamethoxazole by preventing the reduction of dihydrofolic acid with its conversion to tetrahydrofolic acid (an active form of vitamin B9), which is responsible for protein metabolism and bacterial cell division.

Indications Bicotrima

It is used for the following infections:

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

Release form

The drug is produced in the form of a children's oral suspension (0.24 g/5 ml) - inside bottles with a capacity of 60 or 100 ml. The kit also contains a measuring cup.

Pharmacodynamics

A bactericidal drug with a wide range of action against the following bacteria:

• streptococci (hemolytic strains sensitive to penicillin), staphylococci, pneumococci and gonococci with meningococci;
• salmonella (including Salmonella paratyphi and Salmonella typhi), Escherichia coli (including enterotoxogenic strains), Listeria, Vibrio cholerae, Haemophilus influenzae (strains that demonstrate sensitivity to ampicillin), Klebsiella and anthrax bacilli;
• whooping cough bacilli, Nocardia asteroids, Proteus, faecal enterococci, Pasteurella, Brucella and tularemia bacilli;
• mycobacteria (including Hansen's bacilli), enterobacter with citrobacter, providencia, morganella and legionella pneumophila;
• Serratia marcescens, certain varieties of pseudomonads (excluding Pseudomonas aeruginosa), Yersinia with Shigella, Pneumocystis carinii and Chlamydia (this includes Chlamydophila psittaci and Chlamydia trachomatis);
• simple: coccidioides immitis, pathogenic fungi, plasmodia, Toxoplasma gondii, Histoplasma capsulatum, Actinomyces israelii and leishmania.

Resistance is demonstrated by: Pseudomonas aeruginosa, treponemas, corynebacteria, Koch's bacilli, viruses and Leptospira spp.

Weakens the activity of intestinal bacteria, due to which the levels of riboflavin with thymine, B-vitamins and niacin in the intestines decrease. The medicinal effect lasts for 7 hours.

Pharmacokinetics

Absorption after oral administration is 90%. TCmax values are 1-4 hours. With a single administration, the drug maintains a therapeutic concentration for 7 hours.

The drug is uniformly distributed within the body, overcoming histohematic barriers. In urine and lungs, indicators are formed that exceed the plasma level. Smaller volumes of the drug accumulate within vaginal secretions, tissues and secretions of the prostate, cerebrospinal fluid, bronchial secretions, middle ear fluid, saliva with bile, breast milk, bones and aqueous eye fluid with interstitial fluid. Intraplasmic protein binding is 66% (for sulfamethoxazole) and 45% (for trimethoprim).

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

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

The half-life of sulfamethoxazole is 9-11 hours, and trimethoprim is 10-12 hours. In children, this indicator is almost unnoticeable and depends on age; up to 12 months - 7-8 hours; within 1-10 years - is 5-6 hours.

In people with kidney problems and the elderly, the half-life is increased.

Dosing and administration

In cases of uncomplicated infections:

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

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Use Bicotrima during pregnancy

It is prohibited to use the medicine during breastfeeding or pregnancy.

Contraindications

Main contraindications:

• strong personal sensitivity (also to sulfonamides);
• renal or hepatic insufficiency;
• aplastic or pernicious anemia;
• leukopenia or agranulocytosis;
• deficiency of the G6PD component.

Side effects Bicotrima

Side effects include:

• dysfunction of the nervous system: dizziness or headaches. Possible development of depression, tremor, aseptic meningitis, peripheral neuritis and apathy;
• problems with 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, pseudomembranous enterocolitis, increased activity of intrahepatic transaminases and hepatonecrosis;
• damage to the hematopoietic organs: thrombocyto-, leuko- or neutropenia, megaloblastic anemia and agranulocytosis;
• urinary tract infections: crystalluria, polyuria, hematuria, tubulointerstitial nephritis, increased urea levels, renal dysfunction, toxic nephropathy (with anuria and oliguria) and hypercreatininemia;
• problems related to the functioning of the musculoskeletal system: myalgia or arthralgia;
• signs of allergy: rash, Quincke's edema, fever, itching, MEE (this includes SJS), photosensitivity, allergic myocarditis, TEN, exfoliative dermatitis and hyperemia affecting the sclera;
• other symptoms: hypoglycemia.

Overdose

Poisoning may cause confusion, vomiting, or nausea.

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

Interactions with other drugs

It has drug compatibility with the following substances: 5% and 10% dextrose (intravenous infusions), 5% levulose (intravenous infusions), 0.9% NaCl (intravenous infusions), and a combination of 0.18% NaCl with 4% dextrose (intravenous infusions). The list also includes 6% dextran 70 or 10% dextran 40 (intravenous infusions) in combination with 5% dextrose or 0.9% NaCl, as well as Ringer's injection solution.

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

Reduces the severity of intrahepatic metabolism of phenytoin (prolongs its half-life by 39%) and warfarin, potentiating their effect.

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

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

Pyrimethamine in doses greater than 25 mg per week increases the likelihood of megaloblastic anemia.

Diuretics (mainly thiazides) increase the risk of thrombocytopenia.

Therapeutic efficacy is reduced when combined with procaine, benzocaine or procainamide (and other drugs that, when hydrolyzed, form PABA).

A cross-allergic effect may occur between diuretic drugs (furosemide, thiazides, etc.), as well as orally taken antidiabetic drugs (sulfonylurea derivatives) on the one hand, and also antimicrobial sulfonamides on the other.

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

Salicylic acid derivatives potentiate the effect of Bicotrim.

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

A decrease in the absorption of the drug is observed when combined with cholestyramine - because of this, the latter is used 1 hour after or 4-6 hours before the administration of co-trimoxazole.

Medicines that suppress hematopoietic processes in the bone marrow increase the likelihood of myelosuppression.

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Storage conditions

Bicotrim must be stored in a tightly sealed bottle. Temperature – no more than 25°C. It is prohibited to freeze the suspension.

Shelf life

Bicotrim can be used within a 2-year period from the date of manufacture of the drug.

Application for children

Do not prescribe to children if they have been diagnosed with hyperbilirubinemia.

Analogues

Analogues of the drug are the drugs Baktiseptol, Groseptol, Biseptol with Baktrim, and in addition to this, Oriprim, Bel-septol, Solyuseptol with Bi-sept, Biseptrim and Triseptol. Also on the list are Bi-tol, Raseptol, Brifeseptol with Sumetrolim and Co-trimoxazole.