Gatifloxacin

Antibiotics are not for nothing called one of the greatest achievements of mankind, it is difficult even to calculate how many people they saved life and regained their health. Particular attention should be paid to antimicrobial drugs from the group of fluoroquinolones, because these drugs come to help 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 same active ingredient.

[1], [2], [3], [4], [5], [6],

Indications of the gatifloxacin

Antimicrobial drug "Gatifloxacin" has a large spectrum of antibacterial activity. In connection with this, he found wide application in the treatment of infectious-inflammatory pathologies of medium and high severity. For its purpose, it is sufficient that the pathogenic microflora is sensitive to the active substance of the drug.

With the help of this medicine, the following diseases are treated:

• Infectious respiratory infection
  • is used to treat bronchitis: acute therapy, as well as chronic bronchitis in the acute stage,
  • inflammation of the lungs (pneumonia),
  • cystic fibrosis, in which thick mucus accumulates in the lungs, making it difficult to breathe.
• Infectious pathology of ENT organs
  • acute stage of sinusitis,
  • sinusitis,
  • serious cases of otitis media (inflammation of the middle ear), eustachiitis (inflammation with localization 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), inflammatory process in 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
  • is used to treat various types of gonorrhea in persons of different sex: 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 with mycobacteria of tuberculosis, the pathogenic microorganism Helicobacter pilori, which causes inflammatory pathologies of the digestive tract (gastritis, duodenitis, stomach and duodenal ulcer), postoperative complications.

[7], [8], [9],

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.

Tablets in the shell are packed in blisters of 10 pieces.

• In the form of an infusion solution in vials 0.2 or 0.4 liters.

Each vial of the preparation is placed in a separate package.

The active substance of the drug of any of the forms of release is fluoroquinolone 4 generations of gatifloxacin.

As auxiliary substances the tablet form of the preparation contains:

• starch,
• cellulose,
• calcium hydrogenorthophosphate,
• propyl para-hydroxybenzoic acid
• sodium methyl p-hydroxybenzoate,
• stearic acid,
• sodium starch glycolate,
• PEG 6000,
• talc,
• stabilizer hydroxypropylmethylcellulose,
• white food color titanium dioxide,
• softener of the tablet shell dibutyl ester phthalic acid.

Additional components of the solution:

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

Auxiliary components of drugs usually play the role of building material or preservatives and do not bear therapeutic effect. However, they must be considered in case of hypersensitivity. After all, intolerance of at least one component from the entire composition of the drug is a contraindication to the use of the drug, since it can lead to serious consequences.

[10], [11], [12], [13], [14], [15], [16],

Pharmacodynamics

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

Reproduction of microorganisms occurs by dividing cells. In this process, enzymes of topoisomerase IV and DNA-gyrase, produced by the microorganisms themselves, are involved. Thanks to them, the chromosomes are divided, and the new cell gets the properties of the parent.

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

Gatifloxacin has a broad spectrum of antibacterial activity, and it is effective even against microorganisms that are insensitive to other types of AMP. For him, there is no cross-resistance with other antibiotics.

Bacteria that show sensitivity to gatifloxacin:

• Gram-positive - Staphylococcus aureus, pneumococcus, streptococcus piogenes ( the causative agent of tonsillitis, rheumatic fever, glomerulonephritis)
• gram-negative - hemophilic rod ,  Klebsiella pneumonia, moraxella cataris,  E. Coli, enterobacter cloaca, gonococcal infection 

They show relative sensitivity:

• gram-positive - streptococci (varieties: mileribus, mitis, agalactia, disgalaxy), staphylococcus (varieties: kohni epidermidis, hemolytic, saprophytic, hominis, simulans), corynebacterium (causative agent of diphtheria)
• Gram-negative - pertussis wand, oxytocell klebsiella (causative agent of inflammatory pathologies to the intestine and urinary system), enterobacteria (varieties: aerogenes, agglomerants, intermediate, sakazaks), proteus mirabilis and vulgaris, morganella providentia (rettgeri and stuartii).

Relative sensitivity to gatifloxacin is also evident in most anaerobes: bacteroides (varieties: distasonis, eggeri, fragilis, ovatus, thetaiotaomicron, uniformis), fusobacteria, porphyromonads (varieties: typical, anaerobius, magnus), prevotella, propionibacteria, clostridia (perfringens and ramosum).

Pathogens that are considered to be atypical and remain sensitive to gatifloxacin: clamamidia (pneumoniae and trachomatis are pathogens of out-of-hospital pneumonia and chlamydosis), mycoplasma pneumonia, ureaplasma.

Relatively sensitive are the legionella pneumophyll and the coxaeella Burnet (causative agents of pneumonia and ku-fever).

In bacteria resistant to beta-lactam AMP and macrolides, resistance to gatifloxacin does not develop.

[17], [18], [19], [20], [21]

Pharmacokinetics

The drug is quickly absorbed during oral administration, penetrating into various tissues and body fluids. The maximum concentration of gatifloxacin in the blood is observed in the interval from 1 to 2 hours after taking the drug. Bioavailability of the active substance is more than 95%.

With blood proteins bind only a fifth of the drug, so in tissues, its content can be significantly higher than in blood plasma.

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

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

[22], [23], [24], [25], [26]

Dosing and administration

Tablets "Gatifloxacin" received a wider popularity than the solution, which is used for intravenous drip. Take pills at any time, eating does not affect their effectiveness. The tablets are swallowed whole, washed down with water.

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

The course of treatment usually lasts 10 days. In the case of acute sinusitis, therapy can be delayed 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 with long-term treatment or a double dose, dose adjustment is required.

Infusion solution in vials (1 ml - 2 mg gatifloxacin) is used for intravenous slow administration in severe pathologies, and also if there is no possibility of taking tablets. The time of the dropper is 1 hour. Put it once a day. The solution can be mixed with 5% r-r of dextrose, 0.9% sodium chloride solution, Ringer's solution. It is mandatory to carry out a skin test for tolerability.

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

[29], [30], [31], [32]

Use of the gatifloxacin during pregnancy

The antibiotic "Gatifloxacin" has a good penetrating ability, being found in various tissues and liquids. Thus, he can penetrate the protective placental barrier, getting into the fetus, which can cause him irreparable harm. The same consequences can be expected if gatifloksatsin gets into the body of the baby along with breast milk.

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

Contraindications

In addition to pregnancy, lactation and childhood, as well as hypersensitivity to the main and auxiliary components of "Gatifloxacin," the drug has no other contraindications to use.

With caution, you need to use an antibiotic in patients with diabetes.

[27]

Side effects of the gatifloxacin

In most cases, the appearance of side effects of the drug does not cause significant harm to the health of the patient and does not require the withdrawal of the drug. The most common symptoms in the treatment of gatifloxacin are: nausea, vaginitis, diarrhea, headaches and dizziness, tenderness and irritation at the site of injection (injection).

P hedgehog patients complain of unpleasant side symptoms:

• cardiovascular system (strong palpitation, increased blood pressure),
• digestive tract (pain in epigastrium, 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 muscles of the legs),
• nervous system (increased excitability and anxiety, sleep disorders, confusion, impaired body sensitivity, tremor, etc.),
• skin (dryness, itching and rash on the skin, hyperhidrosis),
• metabolism (severe thirst, edematous syndrome, increased blood sugar).

In addition, there may be allergic reactions, pains from the chest and back, chills, fever, dyspnea, impaired vision, tinnitus, change in taste perception, dysuria. With prolonged use, there may be a violation of the microflora of the body, so in parallel with the antibiotic prescribe drugs to restore it.

[28]

Overdose

If the drug is used in a large dosage for a long time, the appearance of such a symptom that indicates an overdose with a medicine may occur: nausea and vomiting, lethargy, superficial rare breathing, trembling in the body, convulsive syndrome, impaired consciousness, psychosis.

Treatment of overdose with oral administration is to remove the remnants of the drug from the stomach. To do this, it is necessary to induce vomiting or rinse the stomach with slightly salted water. Then symptomatic treatment is performed.

[33], [34], [35], [36]

Interactions with other drugs

During therapy with Gatifloxacin, alcohol and alcohol-containing medications are not recommended. It should also avoid the use of gatifloxacin in the same system as other drugs.

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

The use of fluoroquinolone concomitantly with non-steroidal anti-inflammatory drugs (NSAIDs) can lead to increased CNS excitability and the occurrence of seizures.

Parallel reception gatifloksatsina and digoxin often leads to an increase in the concentration of the latter. Therefore, the dose of the heart drug should be reduced for the duration of therapy with an antibiotic.

Probenicid is able to increase the bioavailability of gatifloxacin, which requires correction of the dose of the antibiotic.

Antibiotic therapy for diabetic patients who are forced to take hypoglycemic drugs should be carried out with constant monitoring of blood glucose.

Coagulation monitoring should be performed with simultaneous treatment with warfarin and gatifloxacin. It is possible to enhance the effect of anticoagulant.

With care, it is necessary to prescribe treatment for elderly patients and women with cardiovascular pathologies. There is a risk of developing ventricular arrhythmias.

[37], [38], [39], [40], [41]

Storage conditions

Store the product manufacturer recommends at room temperature, away from moisture and heat. Avoid direct sunlight. When the air temperature is above 25 degrees, the shelf-life of the antibacterial agent may decrease due to premature deterioration of the drug.

Keep away from children. The drug is not used to treat children, and studies in this area have not been carried out, so presumably even a low dose of the drug, according to imprudence accepted by the child, can have dangerous consequences.

[42], [43], [44], [45]

Shelf life

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

The solution should be used immediately after opening the vial. Remains are utilized.

[46], [47], [48]