Biseptol suspension 240mg 5ml 80ml
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Active ingredients
Co-trimoxazole [Sulfamethoxazole + Trimethoprim]
Release form
Suspension
Composition
At 5 ml of active ingredients purified.
Pharmacological effect
Co-trimoxazole is a combined antimicrobial drug consisting of sulfamethoxazole and trimethoprim in the ratio of 5: 1. Sulfamethoxazole, similar in structure to para-aminobenzoic acid (PABA), interferes with the synthesis of dihydrofolic acid in bacterial cells, preventing the incorporation of PABA into its molecule. Trimethoprim enhances the action of sulfamethoxazole by disrupting the reduction of dihydrofolic acid to tetrahydrofolic acid - an active form of folic acid, which is responsible for protein metabolism and microbial cell division. Both components thus disrupt the formation of folic acid, which is necessary for the synthesis of purine compounds and then nucleic acids by microorganisms (RNA and DNA). This disrupts the formation of proteins and leads to the death of bacteria. In vitro is a broad-spectrum bactericidal agent, however, sensitivity may depend on geographic location. Typically sensitive pathogens (minimum inhibitory concentration (MIC) less than 80 mg / l for sulfamethoxazole): Moraxella (Branhamella) catarrhalis, Haemophilus influenzae (beta-lactamase-forming and beta -lactamazone-forming strains), Haemophilus parainfluenzae, Escherichia coli (including enterotoxogenic strains), Citrobacter spp. (including Citrobacter freundii), Klebsiella spp. (including Klebsiella pneumoniae, Klebsiella oxytoca), Enterobacter cloaceae, Enterobacter aerogenes, Hafnia alvei, Serratia spp. (including Serratia marcescens, Serratia liquefaciens), Proteus mirabilis, Proteus vulgaris, Morganella morganii. Shigella spp. (including Shigella flexneri. Shigella sonnet). Yersinia spp. (including Yersinia enterocolitica), Vibrio cholerae, Edwardsiella tarda, Alcaligenes faecalis, Burkholderia (Pseudomonas) cepacia, Burcholderia (Pseudomonas) pseudomallei. However, Brucella can also help you with the help of a name of a person in an affair, in-country, Pseudomonas, Pseudomallei. Cyclospora cayetanensis. Partly sensitive pathogens (MIC 80-160 mg / l for sulfamethoxazole): coagulase-negative strains of Staphylococcus spp. (including methicillin-sensitive and methicillin-resistant strains of Staphylococcus aureus). Streptococcus pneumoniae (penicillin-sensitive and penicillin-resistant strains), Haemophilus ducreyi, Providencia spp. (including Providencia rettgeri), Salmonella typhi. Salmonellais, Saphan empirically, it is necessary to take into account local peculiarities of drug resistance of possible pathogens of a specific infectious disease.For infections that may be caused in part by susceptible microorganisms, it is recommended to test for sensitivity in order to eliminate the resistance of the pathogen.
Pharmacokinetics
When taken orally, absorption is fast and almost complete - 90%. After a single dose of 160 mg of trimethoprim + 800 mg of sulfamethoxazole Cmax of trimethoprim - 1.5-3 μg / ml, and sulfamethoxazole - 40-80 μg / ml. Сmax in plasma is achieved in 1-4 hours; therapeutic level of concentration is maintained for 7 hours after a single dose. When taken repeatedly with an interval of 12 hours, the minimum equilibrium concentrations stabilize within 1.3-2.8 mcg / ml for trimethoprim and 32-63 mcg / ml for sulfamethoxazole. Css of the drug is achieved within 2-3 days. It is well distributed in the body. Vd of trimethoprim is about 130 liters, sulfamethoxazole is about 20 liters. It penetrates the blood-brain barrier, the placental barrier and into breast milk. In the lungs and urine creates concentrations exceeding the content in plasma. Trimethoprim is slightly better than sulfamethoxazole penetrates the non-inflammatory tissue of the prostate gland, seminal fluid, vaginal secretions, saliva, healthy and inflamed lung tissue, bile, while the spinal fluid and the aqueous humor of the eye penetrate the same way. Large amounts of trimethoprim and slightly smaller amounts of sulfamethoxazole come from the bloodstream to interstitial and other extravasal body fluids, while the concentrations of trimethoprim and sulfamethoxazole exceed BMD for most pathogens. Plasma protein binding - 66% in sulfamethoxazole, in trimethoprim - 45%. Metabolized in the liver. Some metabolites have antimicrobial activity. Sulfamethoxazole is metabolized primarily by N4-acetylation and, to a lesser extent, by conjugation with glucuronic acid. Excreted by the kidneys as metabolites (80% for 72 hours) and unchanged (20% sulfamethoxazole, 50% trimethoprim); a small amount through the intestines. Both substances, as well as their metabolites, are excreted by the kidneys, both by glomerular filtration and tubular secretion, as a result of which the concentration of both active substances in the urine is much higher than in the blood. T1 / 2 of sulfamethoxazole is 9-11 h, trimethoprim is 10- 12 h, in children, significantly less and depends on age: up to 1 year - 7-8 h, 1-10 years - 5-6 h. In elderly patients and / or patients with impaired renal function (creatinine clearance (CK) 15 -20 ml / min) T1 / 2 increases, which requires dose adjustment.
Indications
Infectious and inflammatory diseases caused by microorganisms susceptible to the drug: - respiratory tract infections: chronic bronchitis (exacerbation), pneumocystis pneumonia (treatment and prevention) in adults and children; - ENT organs: otitis media (in children); - urinary infections organs: urinary tract infections, soft chancre; - gastrointestinal infections: typhoid fever, paratyphoid fever, shigellosis (caused by sensitive strains of Shigella flexneri and Shigella sonnei); - travelers' diarrhea caused by enterotoxic strains of Escherichia coli, cholera (in Completion of fluid and electrolyte replenishment); - other bacterial infections (possible combination with antibiotics): nocardiosis, brucellosis (acute), actinomycosis, osteomyelitis (acute and chronic), South American blastomycosis, toxoplasmosis (as part of complex therapy).
Contraindications
- hepatic and / or renal failure (creatinine clearance less than 15 ml / min); - aplastic anemia, B12-deficient anemia, agranulocytosis, leukopenia; - glucose-6-phosphate dehydrogenase deficiency; - simultaneous administration with dofetilide; - lactation period; - children age up to 2 months or up to 6 weeks at birth from a mother with HIV infection; - hypersensitivity to sulfonamides, trimethoprim and / or to other components of the drug. With caution: thyroid dysfunction, severe allergic reactions in the anamnesis, bronchial asthma, folic acid deficiency, porphyria, pregnancy.
Use during pregnancy and lactation
In pregnancy, the drug should be prescribed only if the expected benefit from its use exceeds the possible risk to the fetus, since both trimethoprim and sulfamethoxazole penetrate the placental barrier and, thus, can affect folic acid metabolism. In late pregnancy It is necessary to avoid the use of the drug because of the possible risk of developing nuclear jaundice in newborns. Due to the fact that trimethoprim and sulfamethoxazole penetrates into breast milk, the use of co-trimaxoxol in the period l ktatsii protivopokazano.Beremennym women receiving the drug, it is recommended to assign to 5 mg of folic acid per day.
Dosage and administration
Inside, after a diet with a sufficient amount of liquid. Adults and children over 12 years: 960 mg every 12 hours; in severe infections, 1440 mg every 12 hours; with urinary tract infections - 10-14 days, with exacerbation of chronic bronchitis - 14 days, with travelers' diarrhea and shigellosis - 5 days.The minimum dose and dose for long-term treatment (more than 14 days) - 480 mg every 12 hours. Children: from 2 months (or 6 weeks at birth from mothers with HIV infection) to 5 months - 120 mg, from 6 months to 5 years - 240 mg, from 6 to 12 years - 480 mg every 12 hours, which roughly corresponds to the dose of 36 mg / kg per day. The course of treatment for urinary tract infections and acute otitis media is 10 days, and shigellosis is 5 days. In severe infections, doses for children can be increased by 50%. In acute infections, the minimum duration of treatment is 5 days; after the symptoms disappear, therapy is continued for 2 days. If there is no clinical improvement after 7 days of treatment, the patient's condition should be re-evaluated for possible correction of treatment. Soft chancre - 960 mg every 12 hours; if after 7 days of healing of the skin element does not occur, it is possible to extend therapy for another 7 days. However, the lack of effect may indicate pathogen resistance. For women with acute uncomplicated urinary tract infections, a single dose of 1920–2880 mg is recommended, possibly in the evening after meals or before bedtime. For pneumonia caused by Pneumocystis carinii, 30 mg / kg 4 times / day with an interval 6 hours in 14-21 days. For the prevention of pneumonia caused by Pneumocystis carinii, adults and children over 12 years old - 960 mg / day. For children under 12 years old - 450 mg / m2 every 12 hours, for 3 days in a row every week. The total daily dose should not exceed 1920 mg. You can use the following guidelines: on 0.26 m2 of body surface - 120 mg, respectively, on 0.53 m2 - 240 mg, on 1.06 m2 - 480 mg. For other bacterial infections, the dose is adjusted individually depending on age, body weight, kidney function and severity. diseases, for example, in adult nocardiosis - 2880-3840 mg / day for at least 3 months (sometimes up to 18 months). The course of treatment for acute brucellosis is 3-4 weeks, with typhoid and paratyphoid fever 1-3 months.
Side effects
Nervous system disorders: headache, dizziness, aseptic meningitis, peripheral neuritis, convulsions, ataxia, tinnitus, depression, hallucinations, apathy, nervousness. On the respiratory system: pulmonary infiltrates: eosinophilic infiltration, allergic alveolitis (cough, shortness of breath) . On the part of the digestive system: nausea, vomiting, loss of appetite, diarrhea, gastritis, abdominal pain, glossitis, stomatitis, cholestasis, increased activity of hepatic transaminases, hepatitis (includingcholestasis .In the urinary system: interstitial nephritis, renal dysfunction, hematuria, elevated blood urea, hypercreatininemia, toxic nephropic affection with huria and anuria, crystalluria. For musculoskeletal system: arthralgia, myalgia, rhabdomyolysis (mainly in AIDS patients). Allergic reactions: fever, angioedema, pruritus, photosensitization, skin rash, urticaria, multiforme exudative erythema (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), exfoliative dermatitis, allergic myocarditis, conjunctival hyperemia, sclera, anaphylactic / anaphylactoid reactions, serum sickness, hem orragic vasculitis (Schoenlein-Henoch purpura), periarteritis nodosa, lupus-like syndrome. Others: hyperkalemia (mainly in AIDS patients with pneumocystic pneumonia), hyponatremia, hypoglycemia, weakness, fatigue, insomnia, candidiasis.
Overdose
Symptoms: nausea, vomiting, intestinal colic, dizziness, headache, drowsiness, depression, fainting, confusion, fever, hematuria, crystalluria; with prolonged overdose - thrombocytopenia, leukopenia, megaloblastic anemia, jaundice. Treatment: gastric lavage, forced diuresis, acidification of urine increases the excretion of trimethoprim, calcium folinate (eliminates the effect of trimethoprim on bone marrow), if necessary - hemodialysis.
Interaction with other drugs
The anticoagulant activity of indirect anticoagulants (anticoagulant dose adjustment), as well as the action of hypoglycemic drugs and methotrexate (competes for protein binding and renal transport of methotrexate, increasing the concentration of free methotrexate). ), enhancing its effect and toxic effect. With simultaneous use of co-trimoxazole with pyrimethamine in doses exceeding 25 mg / week,increases the risk of megaloblastic anemia. Diuretics (more often thiazides and in elderly patients) increase the risk of thrombocytopenia. It can increase serum concentrations of digoxin, especially in elderly patients, it is necessary to monitor serum concentrations of digoxin. Efficacy of tricyclic antidepressants when combined with co-trimoxazole can be reduced. Patients receiving co-trimoxazole and cyclosporine after kidney transplantation may experience a reversible deterioration in kidney function, as manifested by Creatinine level. Drugs that inhibit bone marrow hematopoiesis, increase the risk of myelosuppression. When co-trimoxazole is used together with indomethacin, the concentration of sulfamethoxazole in the blood can be increased. One case of toxic delirium after co-trimoxazole and amantadine is described simultaneously. , especially in elderly patients, hyperkalemia may develop. Trimethoprim, by inhibiting the kidney transport system, increases the AUC of dofetilide by 103% and Сma x dofetilide by 93%. With increasing concentrations, dofetilide can cause ventricular arrhythmias with prolonged QT interval, including pirouette arrhythmias. The simultaneous appointment of dofetilide and trimethoprim is contraindicated.
special instructions
Co-trimoxazole should be prescribed only in cases where the advantage of such a combination therapy over other antibacterial drugs outweighs the possible risk. Since the sensitivity of bacteria to antibacterial drugs in vitro changes in different geographic areas and over time, the local characteristics of bacterial sensitivity should be taken into account when choosing a drug. With long courses of treatment, regular blood tests are necessary, since there is a likelihood of hematological and 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. Particular caution should be exercised in the treatment of elderly patients or patients with suspected initial folate deficiency. Appointment of folic acid is also appropriate for long-term treatment in high doses. With a significant decrease in the number of any blood cells, the drug should be discontinued. It is also inappropriate to use food products containing large amounts of PABA during treatment, - green parts of plants (cauliflower,spinach, legumes), carrots, tomatoes. During long courses (especially in case of kidney failure), urinalysis should be carried out regularly and kidney function monitored. To prevent crystalluria, it is recommended to maintain a sufficient amount of urine. The probability of toxic and allergic complications of sulfonamides increases significantly while reducing renal filtration function. At the first appearance of a skin rash or any other severe adverse reaction, the drug should be canceled. In case of sudden appearance or increase of cough or shortness of breath, the patient should be re-examined and consideration should be given to discontinuing the drug treatment. AIDS. It is not recommended for use in diseases caused by beta-hemolytic streptococcus group A, due to the widespread resistance of the strains. cases of pancytopenia have been reported to take co-trimoxazole. Trimethoprim has a low affinity for human dehydrofolate reductase, but it can increase the toxicity of methotrexate, especially in the presence of other risk factors such as age, hypoalbuminemia, impaired kidney function, bone marrow depression. Such side reactions are more likely if methotrexate is prescribed in large doses. For the prevention of myelosuppression, it is recommended that such patients be given folic acid or calcium folinate. Trimethoprim disrupts phenyl alanine metabolism, but this does not affect patients with phenylketonuria under the appropriate dietary conditions. Patients whose metabolism is characterized by “slow acetylation” should be longer as short as possible, especially in patients of elderly and senile age. definiteness methotrexate concentration in serum conducted by competitive binding with proteins using bacterial dihydrofolate reductase as a ligand. However, when determining methotrexate by the radioimmune method, interference does not occur. Trimethoprim and sulfamethoxazole may affect the results of the Jaffe reaction (determination of creatinine by reaction with picric acid in an alkaline medium),at the same time, in the range of normal values, the results are overestimated by about 10%. Impact on the ability to drive vehicles and control mechanisms Considering the possibility of significant side effects, during the treatment period, care must be taken when driving vehicles and engaging in potentially hazardous activities that require increased concentration and quickness psychomotor reactions.