Bigaflon

Bigaflon is a systemic antibacterial drug.

Indications Bigaflon

It is used for diseases of infectious and inflammatory origin, and caused by the action of bacteria that are sensitive to the drug:

• lesions affecting the throat, ears, respiratory tract, epidermis with soft tissues, and also the kidneys, abdominal organs and urinary tract;
• gynecological infections;
• gonorrhea, dysentery, osteomyelitis, salmonellosis, and in addition septicemia and tuberculosis.

It is also used for prophylaxis before surgical procedures and for postoperative therapy of surgical infections in individuals with weakened immune systems.

Release form

The substance is released in the form of a 0.4% infusion liquid in bottles with a volume of 0.05, 0.1 or 0.2 liters. It can also be released in packages with a capacity of 0.1 or 0.2 liters.

Pharmacodynamics

The medicinal effect develops by slowing down the activity of topoisomerase IV together with DNA gyrase.

Gatifloxacin, an 8-methoxyfluoroquinolone, has antibacterial activity against a relatively wide range of microbes (gram-positive and -negative).

Sensitivity to drugs is demonstrated by:

• Gram-positive bacteria: pneumococci with Staphylococcus aureus and pyogenic streptococci;
• Gram-negative microbes: Klebsiella pneumoniae, Escherichia coli, Influenza bacilli (including strains that produce β-lactamase), Enterobacter cloacae, Haemophilias parainfluenzae, Moraxella catarrhalis (with strains that produce β-lactamase), and gonococci (the list also includes strains that produce β-lactamase);
• atypical pathogens: ureaplasma, chlamydophila pneumoniae with mycoplasma pneumoniae, and also C. trachomatis and legionella pneumophila.

The following bacteria have moderate sensitivity:

• microbes of the gram-positive subtype: streptococci agalactiae, Streptococcus milieri, Str.mitior, epidermal staphylococci (including methicillin strains) and Streptococcus dysgalactiae. In addition, hemolytic staphylococci, Staphylococcus hominis, Staphylococcus cohnii, saprophytic staphylococci, Koch's bacillus and Staphylococcus simulans with diphtheria corynebacterium;
• Gram-negative bacteria: Klebsiella oxytoca, Proteus mirabilis, Providencia Rettgerii, Morgan's bacteria, Providencia Stewartii, and also Enterobacter agglomerans, common Proteus with Enterobacter aerogenes, Enterobacter sakazaki, whooping cough bacillus and Enterobacter intermedius;
• anaerobes: fusobacteria, Bacteroides distasonis, bacteroides fragilis, Bacteroides ovatus, Porphyromonas spp. and the bacterium thetayotaomicron, as well as Bacteroides eggerthii, Porphyromonas anaerobius together with Bacteroides uniformis, Porphyromonas asaccharolyticus with prevotella, Porphyromonas magnus, clostridia perfringens with propionibacteria and Clostridium ramosum;
• pathogenic microbes that have an atypical form: Legionella pneumophila and Coxiella burnettii.

Helicobacter pylori and Mycobacterium tuberculosis are sensitive to gatifloxacin.

The antibacterial properties of gatifloxacin are developed by inhibiting topoisomerase IV and DNA gyrase. The latter is an important enzyme involved in microbial DNA replication. At the same time, topoisomerase IV is an enzyme that is an important participant in the processes of DNA chromosome separation during microbial cell division.

Pharmacokinetics

Gatifloxacin has a good absorption rate in the gastrointestinal tract after oral administration. Absolute values of the element's bioavailability are 96%. Plasma Cmax is recorded 60-120 minutes after administration of the drug.

Protein synthesis occurring within the blood plasma accounts for 20%.

Gatifloxacin has a good ability to penetrate into the body tissues. Then it is distributed at high speed inside various biological fluids: high rates are noted inside the bronchial mucosa with pulmonary tissues, paranasal sinuses, and in addition inside alveolar macrophages, epidermis, secretions and prostate tissues. It is also found inside the tissues of the middle ear, bile with saliva, seminal fluid, ovaries with the uterus, vagina, and at the same time inside the fallopian tubes of the myo- and endometrium.

The substance undergoes metabolic processes within the body.

Gatifloxacin is excreted through the kidneys. The half-life is within 7-14 hours; it is not determined by the mode of use and the size of the drug dose.

Animal studies have shown that gatifloxacin crosses the placenta without complications and is also excreted in breast milk.

Dosing and administration

Bigaflon is used in a dose of 0.4 g once a day (if the CC indicators are >40 ml/minute).

In case of exacerbation of chronic bronchitis, it is necessary to use 0.4 g (0.1 l) of the substance, once a day for 7-10 days.

Acute stages of sinusitis are treated by taking 0.4 g (0.1 l) of the medication once a day for 10 days.

In case of community-acquired pneumonia, it is necessary to administer 0.4 g (0.1 l) of the drug 1-2 times a day for 1-2 weeks.

During lesions of the urethra (without complications), 0.4 g of the drug is administered once (or 0.2 g of the substance over a period of 3 days). If the disorder occurs with complications, 0.4 g of the substance must be administered once a day (over a period of 7-10 days).

To eliminate lesions affecting the epidermis with soft tissues, 0.2 g of the drug is administered over 5-7 days.

Therapy for tuberculosis (taking into account the severity and form of the pathology) includes the use of 0.8 g of the drug once a day.

Because gatifloxacin is primarily excreted via the kidneys, dose adjustments are required in patients with creatinine clearance <40 ml/min and in patients undergoing continuous ambulatory peritoneal hemodialysis.

The scheme is as follows: the initial dosage is 0.4 g per day; then 0.2 g is used daily.

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Use Bigaflon during pregnancy

The lack of sufficient clinical information regarding the use of Bigaflon during breastfeeding or pregnancy requires caution in the case of such a prescription - it should be used only in situations where the potential benefit to the woman is more expected than the risk of negative consequences for the fetus.

Contraindications

Main contraindications:

• severe hypersensitivity to the drug and other quinolones;
• because the administration of the drug may lead to prolongation of the QT interval on the ECG, its use should be avoided in people with such ECG symptoms (due to the lack of the necessary amount of clinical information);
• myocardial ischemia;
• bradycardia of a pronounced nature.

It is necessary to use the drug very carefully in people with diseases associated with the central nervous system, as well as with severe vascular atherosclerosis in the brain. This is due to the fact that the drug causes an increase in intracranial pressure, which can cause psychosis in the patient.

Side effects Bigaflon

The use of the medication may cause some side effects:

• disorders affecting the gastrointestinal tract: sometimes diarrhea, nausea with vomiting, hyperbilirubinemia and pseudomembranous colitis appear;
• disorders affecting the function of the central nervous system: a feeling of fatigue, general depression or anxiety, as well as psychosis, headaches, motor agitation, dizziness and sleep disorders;
• allergic reactions: itching, facial swelling or swelling in the vocal cord area, as well as photosensitivity and rashes;
• problems with hematopoietic activity: thrombocyto- or leukopenia, eosinophilia and agranulocytosis, as well as an increase in AST or ALT values;
• lesions affecting the urinary system: nephrotic syndrome. In addition, renal failure in the acute stage may sometimes occur;
• other symptoms: arthralgia, tachycardia, myalgia, and along with this, decreased blood pressure and visual impairment.

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Overdose

Signs of Bigaflon poisoning include vomiting, motor agitation, tachycardia, nausea and headaches.

In case of acute intoxication, it is necessary to stop the administration of the drug and perform the necessary hydration; ECG monitoring is also performed. In addition, symptomatic measures are carried out.

Interactions with other drugs

It is prohibited to use the medicine while taking antiarrhythmic medications.

Administration of the drug together with digoxin causes an increase in the serum levels of the latter.

The use of Bigaflon potentiates the properties of anticoagulants with an indirect type of influence.

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Storage conditions

Bigaflon must be kept in a place inaccessible to small children. The drug must not be frozen. The temperature must not exceed 25°C. The medicinal substance can be kept in the light for a maximum of 3 days.

Shelf life

Bigaflon can be used within 24 months from the date of manufacture of the pharmaceutical product.

Application for children

Because the administration of the drug causes the development of arthropathies, as well as chondropathies, it is not used in pediatrics (persons under 18 years of age).

Analogues

Analogues of the drug are such medications as Gaflox with Gatimak, Gatifloxacin and Ozerlik, as well as Gatispan with Gatilin and Gaticin-N.