Брифесептол®

General characteristics. Structure:

Active ingredient: 0,12 g or 0,48 g of co-trimoxazole.

 Excipients: potato starch, talc, polyvinyl alcohol or polyvinylpirrolidone, magnesium stearate, propylene glycol, Kolidon CL.

The combined antibacterial drug.

Pharmacological properties:

Pharmacodynamics. Brifeseptol – chemotherapeutic drug with a wide range of bactericidal action, caused by blocking of biosynthesis of folates in microbic cells: sulfamethoxazole breaks synthesis of dihydrofolic acid, and Trimethoprimum interferes with transformation of dihydrofolic acid into tetrahydrofolic.

Activity of drug is found concerning almost all groups of microorganisms: Streptococcus spp. (hemolitic strains are more sensitive to penicillin), Staphylococcus spp., Streptococcus pneumoniae, Neisseria meningitidis, Neisseria gonorrhoeae, Escherichia coli (including enterotoksogenn strains), Salmonella spp. (including Salmonella typhi and Salmonella paratyphy), Vibrio cholerae, Bacillus anthracis, Haemophilus influenzae (including ampitsillinstoyky strains), Listeria spp., Nocardia asteroides, Bordetella pertussis, Enterococcus faecalis, Klebsiella spp., Proteus spp., Pasteurella spp., Francisella tularensis, Brucella spp., Mycobacterium spp. (including Mycobacterium leprae), Citrobacter, Enterobacter spp., Legionella pneumopnia, Providencia, some types of Pseudomonas (except Ps.aeruginosa), Serratia marcescens, Shigella spp., Yersinia spp., Morganella spp., Pneumocystis carini; Chlamydia spp. (in t. h Chlamydia trachomatis, Chlamydia psittaci); protozoa: Plasmodium spp., Toxoplasma gondii, pathogenic fungi, Actinomyces israelii, Coccidiodes immitis, Histoplasma capsulatum, Leishmania spp.

Resistant to drug: Corynebacterium spp., Pseudomonas aemginosa, Mycobacterium tuberculosis, Treponema spp., Leptospira spp., viruses.

Suppresses colibacillus life activity that leads to decrease in synthesis of thymine, Riboflavinum, niacin and other vitamins of group B in intestines.

Duration of therapeutic effect makes the 7th hour.

Pharmacokinetics. At intake both components of drug are completely soaked up in digestive tract. The maximum concentration of active components of drug is observed in 1-4 hour.

Trimethoprimum well gets into fabrics and through fabric barriers – into lungs, kidneys, a prostate gland, bile, saliva, liquor. Linkng of Trimethoprimum with proteins of a blood plasma makes 50%, the elimination half-life is normal of it - from 8, 6 to 17 hour. The main way of removal of Trimethoprimum – through kidneys, 50% is removed in an invariable look.

Sulfamethoxazole: binding it with proteins of plasma is made by 66%, the elimination half-life - is normal from 9 to 11 hour. The main way of elimination – a kidney, and, from 15 to 30% - in an active form.

Indications to use:

Drug is used for treatment of inflammatory respiratory diseases (bronchitis, pneumonia, abscess of lungs, a pleura empyema, otitis, sinusitis), meningitis, abscess of a brain, inflammatory diseases of urinogenital system (pyelonephritis, an urethritis, a salpingitis, prostatitis, etc.), including the gonorrheal nature, infectious diseases of digestive tract (dysentery, cholera, gastric typhus, a paratyphoid, diarrhea), inflammatory damages of skin and soft tissues (a pyoderma, a furunculosis, etc.).

Route of administration and doses:

The dosage mode - individual, depending on weight of a disease, sensitivity and a type of the activator, age of the patient. At not complicated infectious diseases appoint:

- to children age from 6 to 12 years - on 1 tablet of 480 mg 2 times a day;

- seniors are 12 years old and the adult - on 1-2 tablets on 480 mg 2 times a day.

Children up to 6 years are recommended to use drug in the form of tablets 120 mg.

At heavier course of a bacterial infection the adult drug is appointed on 2-3 tablets on 480 mg by 2 times a day.

Duration of a course of treatment makes from 5 to 14 days. At an acute brucellosis – 3-4 weeks, at gastric typhus and a paratyphoid – 1-3 months. At a heavy current and/or at a chronic form of an infectious disease increase in a single dose by 30-50% is allowed. The maximum daily dose for adults at the heavy course of a bacterial infection - 3 tablets on 480 mg 2 times a day.

For prevention of a recurrence of persistent infections of urinary tract by the adult and to children 12 years – on 1 tablet of 480 mg of 1 times a day for the night, to children up to 12 years – at the rate of 12 mg of sulfamethoxazole on body weight kg a day are more senior. Duration of treatment is determined by the doctor.

The adult at gonorrhea – 4-6 tablets (1920-2880 mg/days) on 3 receptions.

Drug is accepted inside during the period or after reception of food. In the course of treatment it is recommended to drink water in a large number.

In case of continuation of a course of treatment more than 5 days and/or increase in a dose it is necessary to carry out hematologic control; in case of change of a picture of blood it is necessary to appoint folic acid on 5-10 mg a day.

Features of use:

At long courses of treatment it is regularly necessary to do blood tests as the probability of emergence of hematologic changes is. These shifts can be the return at purpose of folic acid (3-6 mg/days) that significantly does not break antimicrobic effect of drug.

It is necessary to avoid excessive ultra-violet radiation.

The risk of side effects is much higher at patients with AIDS.

It is not recommended to apply at the tonsillitis and pharyngitises caused by a beta and hemolitic streptococcus of group A owing to distribution of resistance of strains.

Side effects:

Drug is well transferred. Such side effects are in some cases observed:

- from a nervous system: aseptic meningitis, peripheral neuritis;

- from respiratory system: bronchospasm, pulmonary infiltrates;

- from system digestion: anorexia, gastritis, glossitis, stomatitis, increase in activity of "hepatic" transaminases, гепатонекроз;

- from an urinary system: a renal failure, a crystalluria, a hamaturia, increase in contents of urea, a giperkreatininemiya, a toxic nephropathy with an oliguria and an anury;

- from a musculoskeletal system: arthralgia, mialgiya;

- allergic reactions: photosensitization, allergic myocarditis, rash, diarrhea, Quincke's edema, reddening of scleras. Polimorfna erythema, Stephens-Johnson's syndrome;

- from the hemopoietic system: leukopenia, neutropenia, thrombocytopenia, agranulocytosis, megaloblastichesky anemia;

- others: hypoglycemia.

Interaction with other medicines:

Patients of advanced age have Brifeseptol's combinations to some diuretics, especially tiazidam, increases risk of injury of marrow.

Brifeseptol can strengthen effect of some drugs which slow down blood turnings that demands a dose decline of these drugs.

Brifeseptol slows down metabolism of Phenytoinum: at persons who accept both drugs action of Phenytoinum lasts.

Trimethoprimum exponentiates effect of the antidiabetic drugs derivative of sulphonylurea.

Rifampicin reduces Trimethoprimum elimination half-life.

Sharing of Brifeseptol and cyclosporine after kidney operations worsens a condition of patients.

Joint purpose of drug with salicylates, Butadionum, Naproxenum and derivatives of paraaminobenzoic acid is not recommended.

Piritamin in doses which exceed 25 mg/week increases risk of development of megaloblastichesky anemia.

Benzocaine, Procainum, procaineamide reduce Brifeseptol's effect (and other medicines owing to which hydrolysis paraaminobenzoic acid is formed).

Between diuretics (tiazida, furosemide, etc.) and peroral hypoglycemic drugs (sulphonylurea derivatives) from one side, and antimicrobic streptocides – from another, development of cross allergic reaction is possible.

Phenytoinum, barbiturates, p-aminosalicylic acid strengthen definitions of deficit of folic acid.

Derivatives of salicylic acid strengthen Brifeseptol's action.

Ascorbic acid, hexamethylenetetramine (and other medicines which acidify urine) increase risk of development of a crystalluria.

Holestiramin reduces absorption therefore he should be accepted in 1 hour later, or in 4-6 hour prior to reception of a kotorymoksazol.

Reduces reliability of peroral contraception (suppresses intestinal microflora and reduces enterohepatic circulation of hormonal connections).

Contraindications:

Hypersensitivity to Trimethoprimum and/or streptocides, pregnancy, a lactation, a serious cardial, hepatic, renal and hematologic illness, deficit glyukozo-6-fosfatdegidrogenazy, a liver and/or renal failure, aplastic anemia, B12 – is scarce anemia, an agranulocytosis, a leukopenia, children's age up to 2 years, a hyperbilirubinemia at children.

With care appoint drug at deficit of folic acid in an organism, bronchial asthma, diseases of a thyroid gland.

Overdose:

Symptoms – nausea, vomiting, dizziness, intestinal colic, a headache, drowsiness, a depression, a vision disorder, a diarrhea, a hamaturia, a crystalluria; at prolonged use – thrombocytopenia, a leukopenia, megaloblastichesky anemia, jaundice.

Treatment: drug withdrawal, a gastric lavage (not later than 2 hours after reception of an overdose), the uses of a large amount of water, an artificial diuresis, acidulation of urine increases removal of Trimethoprimum, intramusculary - 5-15 mg/days of calcium of a folinat (eliminates action of Trimethoprimum on marrow), if necessary – a hemodialysis.

Storage conditions:

Store in protected from light and the place, unavailable to children, at the room temperature. A period of storage - 2 years.

Issue conditions:

According to the recipe