Co-trimoxazole Sulfamethoxazole, Trimethoprim

Brand Polfa

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Available since: 2019-09-19

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Clinical Pharmacology

Clinico-pharmacological group: Antibacterial sulfanilamide drug

Pharmaco-therapeutic group: Antimicrobial combined agent

pharmachologic effect

The combined antibacterial drug contains sulfamethoxazole and trimethoprim.

Sulfamethoxazole, similar in structure to PABA, disrupts the synthesis of dihydrofolic acid in bacterial cells, preventing the incorporation of PABA into its molecule.

Trimethoprim enhances the action of sulfamethoxazole, disrupting the reduction of dihydrofolic acid to tetrahydrofolic acid - the active form of folic acid, which is responsible for protein metabolism and microbial cell division.

It is a bactericidal agent with a broad spectrum of action.

Active against gram-positive aerobic bacteria: Streptococcus spp., Including Streptococcus pneumoniae (hemolytic strains are more susceptible to penicillin), Staphylococcus spp., Bacillus anthracis, Listeria spp., Nocardia asteroides, Enterococcus faeceecerosis ecology, Iterocerosis, Icteria ster. (including Mycobacterium leprae, excluding Mycobacterium tuberculosis); Gram-negative aerobic bacteria: Neisseria meningitidis, Neisseria gonorrhoeae, Escherichia coli (including enterotoxogenic strains), Salmonella spp. (including Salmonella typhi and Salmonella paratyphi); Vibrio cholerae, Haemophilus influenzae (including ampicillin-resistant strains), Bordetella pertussis, Klebsiella spp., Proteus spp., Pasteurella spp., Francisella tularensis, Brucella spp., Citrobacter spp., Enterobacter sf. except Pseudomonas aeruginosa), Serratia marcescens, Shigella spp., Yersinia spp., Morganella spp., and also with regard to Chlamydia spp. (including Chlamydia trachomatis, Chlamydia psittaci); against gram-positive anaerobes: Actinomyces israelii; for the simplest: Plasmodium spp., Toxoplasma gondii; pathogenic fungi: Coccidioides immitis, Histoplasma capsulatum, Pneumocystis carinii, Leishmania spp.

Resistant to the drug: Corynebacterium spp., Pseudomonas aeruginosa, Mycobacterium tuberculosis, Treponema spp., Leptospira spp., Viruses.

Inhibits the vital activity of Escherichia coli, which leads to a decrease in the synthesis of thiamine, riboflavin, nicotinic acid and other B vitamins in the intestine.

The duration of therapeutic action is 7 hours.

Pharmacokinetics

Suction

After taking the drug inside the active substances are completely absorbed from the gastrointestinal tract. Cmax in plasma is reached within 1-4 hours after ingestion.

Distribution

Trimethoprim penetrates well into the tissues and biological environment of the body: lungs, kidneys, prostate, bile, saliva, sputum, cerebrospinal fluid. The binding of trimethoprim to plasma proteins is 50%; sulfamethoxazole - 66%.

Removal

T1 / 2 trimethoprim - 8.6-17 h, sulfamethoxazole - 9-11 h. The main route of elimination is the kidneys; while trimethoprim is displayed unchanged up to 50%; sulfamethoxazole - 15-30% in active form.

Indications

Treatment of infectious and inflammatory diseases caused by microorganisms sensitive to the drug:

- respiratory tract infections (including bronchitis, pneumonia, lung abscess, pleural empyema);

- otitis, sinusitis;

- infections of the genitourinary system (including pyelonephritis, urethritis, salpingitis, prostatitis);

- gonorrhea;

- gastrointestinal infections (including typhoid fever, paratyphoid fever, bacterial dysentery, cholera, diarrhea);

- infections of the skin and soft tissues (including furunculosis, pyoderma).

Composition

1 tablet contains:

- Active substances
- Sulfamethoxazole 100 mg.
- Trimethoprim 20 mg.

- Excipients Potato starch, talc, magnesium stearate, polyvinyl alcohol, methyl parahydroxybenzoate, propyl parahydroxybenzoate, propylene glycol.

Co-trimoxazole Sulfamethoxazole, Trimethoprim is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Biseptol	Polfa	Poland	pills
Biseptol pills	Polfa	Poland	pills
Co-trimoxazole	Pharmstandard	Russia	pills
Biseptol	Medana Pharma	Poland	suspension

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Dosage and Administration

The drug is taken orally after a meal, drinking a sufficient amount of liquid. Dose set individually.

Children aged 3 to 5 years, the drug is prescribed 240 mg (2 tab. 120 mg) 2 times / day; children aged 6 to 12 years old - 480 mg each (4 pills of 120 mg or 1 tablet of 480 mg) 2 times / day.

In pneumonia, the drug is prescribed at the rate of 100 mg of sulfamethoxazole per 1 kg of body weight / day. The interval between doses is 6 hours, the duration of treatment is 14 days.

In gonorrhea, the dose of the drug is 2 g (in terms of sulfamethoxazole) 2 times / day with an interval between doses of 12 hours.

Adults and children over 12 years old are prescribed 960 mg 2 times / day, with long-term therapy, 480 mg 2 times / day.

Duration of treatment is from 5 to 14 days. In severe cases of the disease and / or in chronic infections, a single dose may increase by 30-50%.

With the duration of the course of therapy for more than 5 days and / or increasing the dose of the drug, it is necessary to monitor the peripheral blood picture; when pathological changes occur, folic acid should be administered at a dose of 5–10 mg / day.

In case of missing a dose, the drug should be taken as soon as possible. If the time of the next dose is coming, the previous dose should be skipped. Do not take a double dose in order to compensate for the missed.

In patients with renal insufficiency with a CC of 15-30 ml / min, the standard dose of the drug should be reduced by 50%, and with a CC of less than 15 ml / min, the drug is not recommended.

Adverse reactions

The drug is generally well tolerated.

Of the nervous system: headache, dizziness; in some cases - aseptic meningitis, depression, apathy, tremor, peripheral neuritis.

On the part of the respiratory system: bronchospasm, asphyxiation, cough, pulmonary infiltrates.

On the part of the digestive system: nausea, vomiting, decreased appetite, diarrhea, gastritis, abdominal pain, glossitis, stomatitis, cholestasis, increased activity of hepatic transaminases, hepatitis, sometimes with cholestatic jaundice, hepatonecrosis, pseudomembranous enterocolitis, pancreatitis.

On the part of the hematopoietic system: leukopenia, neutropenia, thrombocytopenia, agranulocytosis, megaloblastic anemia, aplastic and hemolytic anemia, eosinophilia, hypoprothrombinemia, methemoglobinemia.

On the part of the urinary system: polyuria, interstitial nephritis, renal dysfunction, crystalluria, hematuria, increased urea concentration, hypercreatininemia, toxic nephropathy with oliguria and anuria.

From the musculoskeletal system: arthralgia, myalgia.

Allergic reactions: pruritus, photosensitization, urticaria, drug fever, rash, multiforme exudative erythema (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell syndrome), exfoliative dermatitis, allergic myocarditis, hemorrhage, hemorrhage, hemorrhage, hemorrhage, hemorrhage, hemorrhage, hemorrhage, hemorrhagic, hemorrhagic, hemorrhagic, hemorrhoids hyperemia of sclera.

Metabolism: hypoglycemia, hyperkalemia, hyponatremia.

Contraindications

- established damage to the liver parenchyma;

- pronounced renal dysfunction in the absence of the ability to control the concentration of the drug in the blood plasma;

- renal failure severe (CC less than 15 ml / min);

- severe blood diseases (aplastic anemia, B12-deficient anemia, agranulocytosis, leukopenia, megaloblastic anemia, anemia associated with folic acid deficiency);

- hyperbilirubinemia in children;

- deficiency of glucose-6-phosphate dehydrogenase (risk of hemolysis);

- pregnancy;

- lactation;

- children's age up to 3 years (for this dosage form);

- hypersensitivity to the drug;

- hypersensitivity to sulfonamides.

The drug is prescribed with caution when there is a deficiency of folic acid in the body, bronchial asthma, and diseases of the thyroid gland.

Drug interactions

With simultaneous use of the drug with thiazide diuretics there is a risk of thrombocytopenia and bleeding (combination is not recommended).

Co-trimoxazole increases the anticoagulant activity of indirect anticoagulants, as well as the action of hypoglycemic drugs and methotrexate.

Co-trimoxazole reduces the intensity of hepatic metabolism of phenytoin (increases its T1 / 2 by 39%) and warfarin, enhancing their action.

Rifampicin reduces T1 / 2 trimethoprim.

With simultaneous use of pyrimethamine in doses exceeding 25 mg / week., Increases the risk of megaloblastic anemia.

With the simultaneous use of diuretics (often thiazide) increases the risk of thrombocytopenia.

Benzocaine, procainum, procainamide (as well as other drugs, as a result of the hydrolysis of which PABK is formed) reduce the effectiveness of the drug Biseptol®.

Between diuretics (including thiazides, furosemide) and oral hypoglycemic agents (sulfonylurea derivatives), on the one hand, and sulfonamide antibacterial agents, on the other hand, a cross-allergic reaction is possible.

Phenytoin, barbiturates, PAS increase the manifestations of folic acid deficiency while using with Biseptol.

Derivatives of salicylic acid enhance the effect of Biseptol.

Ascorbic acid, hexamethylenetetramine (like other urinary acidifying drugs) increase the risk of crystalluria during the use of Biseptol.

Kolestiramin reduces absorption while taking it with other drugs, so it should be taken 1 h after or 4-6 h before taking co-trimoxazole.

With simultaneous use with drugs that inhibit bone marrow hematopoiesis, the risk of myelosuppression increases.

Biseptol® can increase the concentration of digoxin in the blood plasma in some elderly patients.

Biseptol® can reduce the effectiveness of tricyclic antidepressants.

Patients after kidney transplantation, with simultaneous use of co-trimoxazole and cyclosporine, show a dysfunction of the transplanted kidney, manifested by an increase in serum creatinine concentrations, which is probably caused by trimethoprim.

Biseptol® reduces the effectiveness of oral contraception (inhibits the intestinal microflora and reduces the enterohepatic circulation of hormonal drugs).

Pregnancy and Lactation

Biseptolum is contraindicated for use during pregnancy and lactation (breastfeeding).

Special instructions

With caution, the drug is prescribed with a deficiency of folic acid in the body, bronchial asthma, diseases of the thyroid gland, burdened with an allergic history.

It is not recommended to use the drug for tonsillitis and pharyngitis caused by? -Hemolytic group A streptococcus, due to the widespread resistance of the strains.

With long (more than a month) courses of treatment, regular blood tests are necessary, since there is a likelihood of hematological changes (most often asymptomatic). These changes may be reversible with the appointment of folic acid (3-6 mg / day), which does not significantly violate the antimicrobial activity of the drug. Special care is necessary in the treatment of elderly patients or patients with suspected initial folate deficiency. Appointment of folic acid is also advisable with long-term drug treatment in high doses.

Against the background of treatment, it is also inappropriate to use food products containing a large amount of PABA, such as green parts of plants (cauliflower, spinach, legumes), carrots, and tomatoes.

Excessive solar and UV radiation should be avoided.

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

Trimethoprim can change the results of determining the level of methotrexate in serum, given by the enzymatic method, but does not affect the result when choosing a radioimmunological method.

Co-trimoxazole can increase by 10% the results of the reaction of Jaffe with picric acid for the quantitative determination of creatinine.

- Application for violations of the liver function The drug is contraindicated in case of established damage to the liver parenchyma.

- Use in cases of impaired renal function. The drug is contraindicated in cases of marked impaired renal function (creatinine clearance (CK) of less than 15 ml / min). In patients with renal insufficiency with CC 15-30 ml / min, the standard dose of Biseptol should be reduced by 50%. For the prevention of crystalluria, it is recommended to maintain a sufficient amount of urine. The probability of toxic and allergic complications of sulfonamides increases significantly with a decrease in the filtration function of the kidneys.

Overdosage

Symptoms: in case of an overdose of sulfonamide - lack of appetite, intestinal colic, nausea, vomiting, dizziness, headache, drowsiness, loss of consciousness, fever, hematuria, crystalluria are also possible. Later, bone marrow depression and jaundice may develop.

After acute poisoning with trimethoprim, nausea, vomiting, dizziness, headache, depression, disorder of consciousness, and bone marrow depression are possible.

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

Chronic poisoning: the use of co-trimoxazole in high doses over a prolonged period can lead to inhibition of bone marrow function, manifested by thrombocytopenia, leukopenia or megaloblastic anemia.

Treatment: removal of the drug and taking measures aimed at its removal from the gastrointestinal tract (gastric lavage no later than 2 hours after taking the drug or cause vomiting), drink plenty of water if diuresis is insufficient, and the kidney function is preserved. Introduce calcium folinate (5-10 mg / day). Acid urine accelerates excretion of trimethoprim, but may also increase the risk of sulfonamide crystallization in the kidneys.

The blood picture, electrolyte composition in plasma and other biochemical parameters should be monitored. Hemodialysis is moderately effective, and peritoneal dialysis is ineffective.