In stock
Guaranteed refund or reship if you haven't received your order
Secure and encrypted payment processing
We ship to over 40 countries including the USA, UK, Europe, Australia and Japan

Biseptol 480 is an antibacterial drug containing two active substances - sulfamethoxazole and trimethoprim.

Trimethoprim is excreted mainly by the kidneys, and approximately 50% unchanged within 24 hours with urine. Several metabolites of trimethoprim have been identified in urine. Sulfamethoxazole is a weak acid with pKa = 6.0. The concentration of the active form of sulfamethoxazole in the amniotic fluid, bile, cerebrospinal fluid, middle ear secretion, sputum, synovial fluid, intracellular fluid is from 20% to 50% sulfamethoxazole in the blood plasma.

Approximately 66% of sulfamethoxazole binds to plasma proteins. The half-life of individuals with normal renal function is from 9 to 11:00. In individuals with impaired renal function, a change in the half-life of the active form of sulfamethoxazole has not been established, but an increase in the half-life of the main acetylated metabolite is observed if creatinine clearance is less than 25 ml / min.

Sulfamethoxazole is excreted primarily by the kidneys, from 15% to 30% of the administered dose is found in urine in an active form. In elderly patients, a decrease in renal clearance of sulfamethoxazole is observed.

Indications for use

The indications of co-trimoxazole in the form of a concentrate for the preparation of a solution for infusion are the same as for oral forms.

  • Urinary tract infections: treatment of severe uncomplicated urinary tract infections (for the initial symptoms of unsteady urinary tract infections, it is recommended that you use an effective single drug compared to combination treatment)
  • treatment and prevention of pneumonia caused by Ppeitosustis jiroveci (formerly R. carinii) (PCP)
  • treatment and prevention of toxoplasmosis.


  • Hypersensitivity to active substances, to sulfonamides or trimethoprim, or to any of the excipients.
  • Severe parenchymal liver disease.
  • Severe renal impairment (creatinine clearance <15 ml / min), if it is not possible to periodically determine the concentration of trimethoprim and sulfamethoxazole in the blood plasma.
  • Megaloblastic anemia due to folate deficiency.
  • Immune thrombocytopenia caused by the use of trimethoprim and / or sulfonamides.
  • Hematologic disorders.
  • Combination with dofetilide.
  • Glucose-6-phosphate dehydrogenase deficiency.
  • Age during the first 6 weeks of life and premature babies, with the exception of the prevention of PCP in children from 4 weeks of life.

Dosage and administration

Biseptol 480, a concentrate for the preparation of a solution for infusion, is intended only for intravenous administration. Dilute before use.

The drug Biseptol 480 must be diluted immediately before use. When mixing Biseptol 480 with infusion solutions, the resulting mixture must be shaken vigorously for complete mixing. If sediment is detected or when crystals appear in the diluted concentrate, it should be destroyed and a new infusion should be prepared. The recommended wiring scheme of the drug Biseptol 480:

  • 1 ampoule (5 ml) of the drug Biseptol 480 in 125 ml of solution for infusion;
  • 2 ampoules (10 ml) of Biseptol 480 in 250 ml of solution for infusion;
  • 3 ampoules (15 ml) of Biseptol 480 in 500 ml of infusion solution.

To dilute Biseptol 480, use such solutions for infusion

  • 5% and 10% glucose solution
  • 0.9% sodium chloride solution
  • ringers solution;
  • 0.45% sodium chloride solution with 2.5% glucose solution.

Do not use other solutions for breeding the drug Biseptol 480, except for the above.

The prepared solution of the drug should not be mixed with other drugs.

The infusion of the drug should last about 60-90 minutes and depends on the degree of hydration of the patient.

If the patient is contraindicated in the introduction of a large amount of liquid, a higher concentration of co-trimoxazole is allowed - 5 ml in 75 ml of 5% glucose. The finished solution of the drug should be administered no more than 1:00.

Unused solution should be poured.


The maximum dose tolerated by humans is unknown. Symptoms of acute overdose: nausea, vomiting, diarrhea, colic, headache, vertigo, dizziness, drowsiness, loss of consciousness, confusion, fever, intellectual and visual disturbances, jaundice, impaired blood composition, in severe cases - crystalluria, hematuria and anuria.

Symptoms of chronic overdose: inhibition of blood formation (thrombocytopenia, leukopenia, megaloblastic anemia), as well as other pathological changes in the blood picture due to folic acid deficiency.

Treatment. In case of an established, suspected or accidental overdose, the drug should be discontinued immediately. Increased renal excretion by forced diuresis (alkalinization of the urine helps to eliminate sulfamethoxazole), hemodialysis (peritoneal dialysis is ineffective). It is necessary to control the blood picture and the level of electrolytes. With severe pathological changes in the picture of blood or jaundice, prescribe a specific treatment. To eliminate the effect of trimethoprim on hematopoiesis, calcium folinate at a dose of 3-6 mg can be prescribed for 5-7 days.

special instructions

Use during pregnancy or lactation


There is no reliable data on the use of co-trimaxosole in pregnant women. Studies have shown a possible relationship between the action of folic acid antagonists and the development of damage to the fetus. Trimethoprim is a folic acid antagonist, in studies conducted on animals, both active substances caused abnormalities in the development of the fetus.

Co-trimaxosole should not be used during pregnancy, especially in the first trimester, except in cases of absolute necessity. If necessary, its use by pregnant women should consider the use of folic acid.

Sulfamethoxazole competes with bilirubin for binding to plasma albumin. If the drug was used by the mother immediately before delivery, significant concentrations of the drug received from the mother are stored in the newborn for several days, and there is a risk of deposition of bilirubin or increased hyperbilirubinemia, which theoretically involves the risk of developing nuclear jaundice. This is especially true for newborns with an increased risk of developing hyperbilirubinemia, especially in premature babies and in children with a deficiency of glucose-6-phosphate dehydrogenase.


Since trimethoprim and sulfamethoxazole pass into breast milk, breast-feeding while taking Biseptol 480 is not recommended, especially for children with hyperbilirubinemia or the risk of developing it.

In addition, co-trimaxosole should be avoided in infants younger than 8 weeks, given the tendency to develop neonatal hyperbilirubinemia.


Use in children from 6 weeks old.

The ability to influence the reaction rate when driving vehicles or other mechanisms

Biseptol 480 usually does not directly affect the ability to drive vehicles or work with other mechanisms. However, there is the likelihood of side effects from the nervous system and psyche, which can affect this ability, in some cases - to a large extent.


active substances: sulfamethoxazolum, trimethoprimum;

1 ml of concentrate contains 80 mg sulfamethoxazole, 16 mg trimethoprim

Excipients: propylene glycol, ethanol 96%, benzyl alcohol, sodium metabisulfite (E 223), sodium hydroxide, sodium hydroxide 10%, water for injection

1 ampoule (5 ml of concentrate) contains 400 mg sulfamethoxazole and 80 mg trimethoprim.

Storage conditions

Store in the original packaging at a temperature not exceeding 25 ° C. Do not freeze.

Keep out of the reach of children.

Shelf life is 5 years.

Do not use after expiration date.

Tags: Sulfamethoxazole, Trimethoprim