Gatispan

Gatispan is a drug from the quinolone/fluoroquinolone category. It has a broad spectrum of antibacterial action.

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Indications Gatispan

It is indicated for the elimination of infectious and inflammatory pathologies caused by microbes sensitive to the active component of the drug - gatifloxacin. Among these:

• infectious processes in the urinary system: cystitis and prostatitis, as well as pyelonephritis in acute or chronic form;
• chronic infectious processes within the urinary tract;
• infectious processes in the respiratory organs: acute forms of sinusitis and bronchitis, as well as pulmonary abscess and pneumonia, as well as exacerbation of COPD and cystic fibrosis;
• infectious processes in soft tissues and skin;
• infectious processes in joints and bones;
• sexually transmitted diseases (urethritis, proctitis, and also cervicitis).

Release form

Available in tablet form. One blister contains 5 tablets. The package contains 1-5 or 10 blister strips.

Pharmacodynamics

The main active component of the drug is gatifloxacin, which has a wide range of antibacterial action. It is active against most gram-negative and gram-positive bacteria. The properties of the drug are realized through DNA gyrase (an enzyme participating in DNA replication, which provokes the development of infection), as well as topoisomerase IV (an enzyme that acts as the main engine in the division of bacterial cells - it separates DNA chromosomes). The range of action of Gatispan includes pathogens that are resistant to cephalosporins with penicillins and aminoglycosides, as well as microbes with multiresistant properties.

It is active against the following gram-positive bacteria: Staphylococcus aureus, Streptococcus pyogenes, pneumococcus (including strains sensitive and resistant to penicillin), Staphylococcus saprophyticus, streptococci from groups C, G, and F, Staphylococcus epidermidis (strains sensitive to methicillin), and Streptococcus agalactiae. It also fights against gram-negative microbes: Influenza bacillus (also with strains that produce β-lactamase), Escherichia coli, Haemophilus parainfluenzae, Klebsiella pneumoniae, Neisseria gonorrhoeae (also with strains that produce β-lactamase), Moraxella catarrhalis (also with strains that produce β-lactamase), Proteus mirabilis and Acinetobacter iwoffii, as well as Citrobacter freundii, Enterobacter aerogenes, Citrobacter koseri and Enterobacter cloacae, as well as Klebsiella oxytoca, Proteus vulgaris and Morgan's bacillus. In addition to other microbes: Legionella pneumophila, Mycoplasma pneumoniae and Chlamydophila pneumoniae.

The drug also exhibits pronounced activity against anaerobes, including peptostreptococci.

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Pharmacokinetics

The pharmacokinetic properties of the drug are linear (in the case of use in dosages of 200-800 mg for 2 weeks) and do not depend on the time frame of use.

The drug is effectively absorbed through the gastrointestinal tract after oral administration. The absolute bioavailability index is 96%. The peak plasma concentration usually occurs 1-2 hours after administration.

Approximately 20% of gatifloxacin is synthesized with plasma protein (regardless of the concentration of the substance). The component with high activity is distributed inside the body - in its tissues: bronchial mucosa, cervix, alveolar macrophages, and also in the vagina. Due to the high distribution rate of the substance inside the tissues, the drug quickly accumulates inside the target organs.

Within the body, the substance undergoes limited biotransformation. Approximately 1% of the dosage is excreted as methylethylenediamine and ethylenediamine breakdown products (along with urine), and another 5% is excreted with feces. Approximately 70% of the substance is excreted through the kidneys - in the first 48 hours, unchanged.

There are some differences in the pharmacokinetics of the drug in women. An increase in the peak concentration (+21%) and AUC 0- (+32%) was recorded when taken by elderly women. At the same time, slow excretion of the drug is observed in young girls.

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Dosing and administration

Before starting treatment with Gatispane, a skin sensitivity test must be performed.

Gatispan is used daily, by intravenous drip infusion. The amount of the drug and the duration of its use depend on the type and severity of the infectious lesion.

• To treat an exacerbation of chronic bronchitis, 400 mg of Gatispan is prescribed for a week.
• For acute sinusitis, 400 mg of Gatispan is prescribed for ten days.
• For community-acquired pneumonia, 400 mg of Gatispan is prescribed for 1-2 weeks.
• For uncomplicated infectious lesions of the urinary system, 200-400 mg of Gatispan is used as a single injection or over the course of three days.
• In case of complicated infectious lesions of the urinary system, 400 mg of Gatispan is used for a week.
• For acute pyelonephritis, 400 mg of Gatispan is prescribed for a week.
• For the treatment of urethral gonorrhea in male patients, a single administration of 400 mg of Gatispan is used.
• For the treatment of endocervical and rectal gonorrhea in female patients, a single administration of 400 mg of Gatispan is used.

Gatispan should be taken orally - in the amount of 200-400 mg once a day. The duration of the course depends on the severity of the infectious process, indications, and also the effectiveness of the drug.

The initial dose does not need to be adjusted for people with renal failure. Subsequent dosages are adjusted based on the CC level.

Use Gatispan during pregnancy

Gatispane is prohibited for use by pregnant women.

Contraindications

Contraindications include: lactation period, intolerance to the active component of the drug or other fluoroquinolones, as well as age under 18 years and a deficiency of G6PD in the body.

Side effects Gatispan

Taking the tablets may provoke the development of the following side effects:

• digestive system organs: abdominal pain, nausea with vomiting, constipation, dyspeptic symptoms, bloating, development of anorexia, gingivitis, stomatitis, gastritis or glossitis, as well as bleeding in the gastrointestinal tract and oral candidiasis;
• CNS and PNS organs: headaches, as well as dizziness, the occurrence of migraines, as well as insomnia and other sleep disorders, as well as the development of nervousness, a feeling of anxiety or drowsiness, an excited state. In addition, the development of leg muscle cramps, paresthesia, the appearance of confusion, paranoia, depressive syndrome, panic attacks and depersonalization. Also the occurrence of ataxia, photophobia, ocular photosensitivity, hyperesthesia, a feeling of hostility, visual disorders, and along with this, disorders of taste and olfactory receptors and the development of polyneuropathy;
• cardiovascular system: bradycardia with tachycardia and increased blood pressure;
• musculoskeletal system: pain in the bones and joints, and in addition, an increased risk of tendon rupture;
• respiratory system: hyperventilation, as well as bronchial spasms;
• allergies: swelling of the face, as well as the oral mucosa with the tongue, also generalized swelling, the appearance of maculopapular or vesiculobullous rashes;
• others: feeling thirsty, chest or ear pain, and also development of hematuria, hypoglycemia or vaginitis, as well as fever. In addition, the appearance of uterine bleeding and dry skin.

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Overdose

There have been no reports of drug overdose.

In case of accidental overdose, treatment aimed at eliminating the symptoms of the disorder is necessary. Gastric lavage and, if necessary, a hydration therapy procedure are performed. Hemodialysis is not very effective for the excretion of gatifloxacin - only about 14% of the drug can be removed within 4 hours. Forced diuresis is also not very helpful - about 11% of the drug can be removed within 8 days.

It is necessary to closely monitor the condition of patients, including regular electrocardiography. At the first signs of overdose, symptomatic and supportive treatment should be started immediately.

It is important to maintain water and electrolyte balance in the body.

Hemodialysis is considered ineffective: no more than 14% of the total amount of the drug taken is removed from the bloodstream over four hours. With continuous stationary peritoneal dialysis, 11% is removed over eight days.

Interactions with other drugs

In case of using the medicine for diabetes (people using oral antidiabetic drugs), the blood sugar level may change. Therefore, such people need to constantly monitor glucose levels.

People who use dietary supplements (containing zinc or iron or magnesium), aluminum/magnesium-containing antacids, and also iron sulfates should take Gatispan 4 hours before using the above-mentioned products.

As a result of combination with probenecid, the rate of excretion of gatifloxacin increases. Combination with warfarin does not affect blood coagulation parameters, but since individual fluoroquinolones can increase its properties (as well as other indirect anticoagulants), it is necessary to monitor the main blood coagulation parameters.

The combined use of the drug and various NSAIDs may increase the manifestation of side effects from the central nervous system.

Caution is required when combining Gatispana with antipsychotics, cisapride and erythromycin.

Concomitant use with digoxin does not significantly affect the pharmacokinetic properties of gatifloxacin, but people taking digoxin should be monitored by a doctor to promptly notice the onset of toxicity symptoms. In the event of the development of the first signs of digitalis poisoning, it is necessary to determine the serum digoxin levels, and then adjust the dose of the drug.

Gatispan does not affect the systemic clearance rates after intravenous injection of midazolam. A single intravenous injection of midazolam at 0.0145 mg/kg does not change the kinetic properties of Gatispan.

The combination of taking Gatispan and Theophylline did not have any mutual influence of the drugs on each other.

The combination of Gatispane and Glyburide (once a day) in patients with type 2 diabetes mellitus did not affect the pharmacological parameters of the drugs: blood sugar levels did not change.

The elimination of Gatispane from the bloodstream is increased when combined with Probenecid.

In patients treated with Warfarin, concomitant administration of Gatispand did not cause significant changes in blood coagulation. However, in such a situation, there is a need to monitor the prothrombin index.

It has been found that the combination of nonsteroidal anti-inflammatory drugs and quinolones can lead to the development of seizures and central nervous system disorders.

The combination of Gatispane with tricyclic antidepressants, phenothiazine drugs, as well as erythromycin and cisapride increases the risk of arrhythmia.

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Storage conditions

Gatispana is kept in a place protected from sunlight and moisture. The place should be inaccessible to small children. The temperature should not exceed 25°C.

Shelf life

Gatispan is permitted to be used for 2 years from the date of release of the drug.