Gatifloxacin

Antibiotics are not in vain called one of the greatest achievements of mankind, because it is difficult to even count how many people they have saved lives and restored health. Particular attention should be paid to antimicrobial drugs from the fluoroquinolone group, because these are the drugs that come to the rescue in severe cases of bacterial pathologies, with purulent wounds and abscesses, when other drugs are not effective enough. One of the most popular fluoroquinolones is the antibacterial drug "Gatifloxacin" with the active substance of the same name.

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Indications Gatifloxacin

The antimicrobial drug "Gatifloxacin" has a wide spectrum of antibacterial activity. In this regard, it has found wide application in the therapy of infectious and inflammatory pathologies of moderate and severe severity. For its appointment it is enough that the pathogenic microflora is sensitive to the active substance of the drug.

This medicine is used to treat the following diseases:

• Infectious lesion of the respiratory organs
  • used for the treatment of bronchitis: therapy of acute and chronic bronchitis in the acute stage,
  • inflammation of the lungs (pneumonia),
  • cystic fibrosis, in which thick mucus builds up in the lungs, making breathing difficult.
• Infectious pathologies of ENT organs
  • acute stage of sinusitis,
  • sinusitis,
  • severe cases of otitis (inflammation of the middle ear), eustachitis (inflammation localized in the auditory tube) and other similar diseases,
• Bacterial pathologies affecting the kidneys and urinary tract:
  • complicated and uncomplicated infections, such as kidney inflammation (pyelonephritis and glomerulonephritis), inflammation of the bladder (cystitis) and prostate gland (prostatitis).
• Infectious lesions of the skin and soft tissues, including purulent wounds,
• Infections affecting bones and joints.
• Infectious inflammatory process in the genitourinary system
  • It is used to treat various types of gonorrhea in people of both sexes: women with vaginal (endocervical) and rectal gonorrhea, men with uncomplicated urethral pathology,
  • urogenital infections in female patients.

With the help of "Gatifloxacin" it is possible to fight against mycobacterium tuberculosis, the pathogenic microorganism Helicobacter pylori, which causes inflammatory pathologies of the gastrointestinal tract (gastritis, duodenitis, gastric ulcer and duodenal ulcer), postoperative complications.

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Release form

In pharmacies, the antimicrobial drug "Gatifloxacin" can be found in two forms:

• In the form of tablets, the dosage of which is either 0.2 or 0.4 mg.

The coated tablets are packed in blisters of 10 pieces.

• In the form of an infusion solution in 0.2 or 0.4 l bottles.

Each bottle of the drug is placed in a separate package.

The active substance of the drug in any form of release is the 4th generation fluoroquinolone gatifloxacin.

The tablet form of the drug contains the following excipients:

• starch,
• cellulose,
• calcium hydrogen phosphate,
• propyl para-hydroxybenzoate
• sodium methyl para-hydroxybenzoate,
• stearic acid,
• sodium starch glycolate,
• PEG 6000,
• talc,
• stabilizer hydroxypropyl methylcellulose,
• white food coloring titanium dioxide,
• Tablet shell softener dibutyl phthalate.

Additional components of the solution:

• hydrochloric acid,
• magnesium hydroxide
• dextrose
• water for injection.

Excipients of medicines usually act as building materials or preservatives and do not have a therapeutic effect. However, they must be taken into account in case of hypersensitivity. After all, intolerance to at least one component of the entire composition of the medicine is a contraindication to the use of the drug, since it can lead to serious consequences.

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Pharmacodynamics

"Gatifloxacin" is a 4th generation fluoroquinolone antibiotic, the therapeutic effect of which differs from other popular narrow- and broad-spectrum antibiotics (penicillins, cephalosporins, tetracyclines, aminoglycosides, macrolides).

Microorganisms reproduce by dividing cells. The enzymes topoisomerase IV and DNA gyrase, produced by the microorganisms themselves, participate in this process. Thanks to them, chromosomes are divided, and the new cell acquires the properties of the parent cell.

Gatifloxacin has the ability to inhibit the production of these enzymes, and the process of reproduction of pathogenic microorganisms subsides.

Gatifloxacin has a broad spectrum of antibacterial activity, and it is effective even against microorganisms that are insensitive to other types of AMP. It does not exhibit cross-resistance with other antibiotics.

Bacteria that are sensitive to gatifloxacin:

• gram-positive - Staphylococcus aureus, pneumococcal infection, Streptococcus pyogenes (causative agent of tonsillitis, rheumatism, glomerulonephritis)
• gram-negative - Haemophilus influenzae, Klebsiella pneumoniae, Moraxella catarrhalis, Escherichia coli, Enterobacter cloacae, gonococcal infection

They exhibit relative sensitivity:

• gram-positive - streptococci (varieties: milieribus, mitis, agalactia, dysgalaxia), staphylococci (varieties: kochni epidermidis, hemolytic, saprophytic, hominis, simulans), corynebacterium (the causative agent of diphtheria)
• gram-negative – whooping cough bacillus, Klebsiella oxytoca (the causative agent of inflammatory pathologies of the intestines and urinary system), enterobacteria (varieties: aerogenes, agglomerans, intermedius, sakazaki), proteus mirabilis and vulgaris, morganella providencia (rettgeri and stuartii).

Most anaerobes also show relative sensitivity to gatifloxacin: bacteroides (species: distasonis, eggertii, fragilis, ovatus, thetaiotaomicron, uniformis), fusobacteria, porphyromonas (species: typical, anaerobius, magnus), prevotella, propionibacteria, clostridia (perfringens and ramosum).

Pathogens that are considered atypical and remain sensitive to gatifloxacin: chlamydia (pneumoniae and trachomatis - pathogens of community-acquired pneumonia and chlamydia), mycoplasma pneumoniae, ureaplasma.

Legionella pneumophila and Coxiella burnetii (causative agents of pneumonia and Q fever) are considered relatively sensitive.

Bacteria resistant to beta-lactam AMPs and macrolides do not develop resistance to gatifloxacin.

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Pharmacokinetics

The drug is absorbed quite quickly when taken orally, penetrating into various tissues and body fluids. The maximum concentration of gatifloxacin in the blood is observed in the period from 1 to 2 hours after taking the drug. The bioavailability of the active substance is more than 95%.

Only one fifth of the drug binds to blood proteins, so its content in tissues can be significantly higher than in blood plasma.

High concentrations of the drug are found in the bronchi and lung tissue, in the middle ear and paranasal sinuses, in various layers of the skin, prostate, mucous membranes and tissues of the internal female genital organs. In addition to blood, the antibiotic can be found in sperm, bile, and breast milk.

Only a small amount of gatifloxacin is metabolized, and the metabolites are subsequently excreted in the urine. About 70% of the active substance is excreted from the body through the kidneys in its original form. The half-life of the drug ranges from 7 to 14 hours.

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Dosing and administration

Gatifloxacin tablets have gained wider popularity than the solution used for intravenous drip administration. Tablets can be taken at any time, food intake does not affect their effectiveness. Tablets are swallowed whole with water.

For most infectious pathologies, Gatifloxacin is prescribed at a dosage of 400 mg per day. The daily dose can be taken at one time, as recommended for uncomplicated gonorrhea, or divided into 2 doses of 0.2 g.

The course of treatment usually lasts 10 days. In case of acute sinusitis, therapy can last up to 2 weeks.

Treatment of cystitis requires a lower daily dosage (0.2 g) and duration of therapy (3 days).

For patients with impaired renal function, dose adjustment is required during long-term treatment or twice-daily administration.

Infusion solution in vials (1 ml - 2 mg gatifloxacin) is used for intravenous slow administration in severe pathologies, as well as if it is not possible to carry out therapy with tablets. Drip time is 1 hour. It is administered once a day. The solution can be mixed with 5% dextrose solution, 0.9% sodium chloride solution, Ringer's solution. A skin test for tolerance is mandatory.

For cystitis and gonorrhea, a single infusion of the drug in a dosage of 400 ml is sufficient. For the treatment of other pathologies, droppers are administered once a day for 7-10 days.

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Use Gatifloxacin during pregnancy

The antibiotic "Gatifloxacin" has good penetrating ability, being found in various tissues and fluids. Thus, it can penetrate the protective placental barrier, getting into the fetus's body, which can cause irreparable harm. The same consequences can be expected if gatifloxacin gets into the baby's body with breast milk.

In connection with the above, the drug is prohibited for use in the treatment of pregnant women and nursing mothers. By the way, it is also not used in pediatrics.

Contraindications

Apart from pregnancy, lactation and childhood, as well as hypersensitivity to the main and auxiliary components of Gatifloxacin, the drug has no other contraindications for use.

The antibiotic should be used with caution in patients suffering from diabetes mellitus.

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Side effects Gatifloxacin

In most cases, the occurrence of side effects of the drug does not cause significant harm to the patient's health and does not require discontinuation of the drug. The most common symptoms during gatifloxacin therapy are: nausea, vaginitis, diarrhea, headaches and dizziness, pain and irritation at the injection site.

Less often, patients complain about the appearance of unpleasant symptoms from:

• cardiovascular system (heart palpitations, increased blood pressure),
• digestive tract (epigastric pain, constipation, vomiting, bloating, inflammation of the mucous membranes of the mouth and stomach, the appearance of rashes and ulcers in the oral cavity),
• musculoskeletal system (arthralgia, spastic pain in the leg muscles),
• nervous system (increased excitability and anxiety, sleep disturbances, confusion, impaired body sensitivity, tremors, etc.),
• skin (dryness, itching and rashes on the skin, hyperhidrosis),
• metabolism (intense thirst, edema syndrome, increased blood sugar).

In addition, allergic reactions, chest and back pain, chills, fever, shortness of breath, blurred vision, tinnitus, changes in taste perception, dysuria may be observed. With prolonged use, a violation of the body's microflora is possible, therefore, in parallel with the antibiotic, drugs are prescribed to restore it.

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Overdose

If the drug is used in high doses for a long time, the following symptoms may appear, indicating an overdose of the drug: nausea and vomiting, lethargy, shallow, rare breathing, tremors in the body, convulsions, impaired consciousness, psychosis.

Treatment of an overdose when taken orally consists of removing the remnants of the drug from the stomach. This requires inducing vomiting or rinsing the stomach with slightly salted water. Symptomatic treatment is then administered.

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Interactions with other drugs

During therapy with Gatifloxacin, it is not recommended to consume alcohol or alcohol-containing medications. It is also necessary to avoid using Gatifloxacin in the same system with other medications.

The absorption of the antibiotic is adversely affected by taking antacids, vitamin and mineral complexes, zinc preparations, and drugs containing iron sulfate. Therefore, it is advisable to observe a 2-hour interval between taking gatifloxacin and the above-mentioned drugs.

The use of a fluoroquinolone simultaneously with nonsteroidal anti-inflammatory drugs (NSAIDs) may lead to increased CNS excitability and the occurrence of seizures.

Concomitant use of gatifloxacin and digoxin often leads to an increase in the concentration of the latter. Therefore, the dose of the cardiac drug should be reduced during antibiotic therapy.

Probenecid can increase the bioavailability of gatifloxacin, which requires a dose adjustment of the antibiotic.

Antibacterial therapy for patients with diabetes mellitus who are forced to take hypoglycemic drugs should be carried out with constant monitoring of blood glucose levels.

Coagulation monitoring should be performed during concomitant treatment with warfarin and gatifloxacin. Potential enhancement of anticoagulant action.

Treatment should be administered with caution to elderly patients and women with cardiovascular pathologies. There is a risk of developing ventricular arrhythmias.

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Storage conditions

The manufacturer recommends storing the drug at room temperature, away from moisture and heat. Avoid exposure to direct sunlight. At air temperatures above 25 degrees, the shelf life of the antibacterial agent may decrease due to premature deterioration of the drug.

Keep out of reach of children. The drug is not used to treat children, and no studies have been conducted in this area, so even a low dose of the drug, inadvertently taken by a child, can presumably have dangerous consequences.

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Shelf life

The shelf life of the drug in the original packaging under appropriate conditions is 2 years. It is prohibited to use the antibiotic after the expiration date.

The solution should be used immediately after opening the bottle. Any leftovers should be disposed of.

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