Tigeron - Instructions For Use, Price, Tablets 500 Mg, 750 Mg

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Tigeron

Tigeron: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. Drug interactions
13. 13. Analogs
14. 14. Terms and conditions of storage
15. 15. Terms of dispensing from pharmacies
16. 16. Reviews
17. 17. Price in pharmacies

Latin name: Tigeron

ATX code: J01MA12

Active ingredient: levofloxacin (levofloxacin)

Manufacturer: Kusum Healthcare (India)

Description and photo updated: 2018-23-11

Tigeron is an antibacterial drug of the quinolone group with a broad spectrum of action.

Release form and composition

Dosage forms of Tigeron:

• coated tablets: capsule-like, pink, embossed on one side "500" or "750" (depending on the dosage) (in a cardboard box 1 blister of 5 or 10 tablets);
• solution for intravenous infusion: transparent, from greenish-yellow to yellow, without foreign inclusions (in a cardboard box 1 bottle of 100 ml).

Composition of 1 tablet:

• active substance: levofloxacin - 500 or 750 mg (in the form of levofloxacin hemihydrate);
• auxiliary components: povidone K29 / 32, microcrystalline cellulose, crospovidone, magnesium stearate, anhydrous colloidal silicon dioxide;
• shell: Opadry 03B84681 pink (hypromellose, titanium dioxide, polyethylene glycol, red and yellow iron oxide).

Composition of 1 ml of infusion solution:

• active substance: levofloxacin (in the form of levofloxacin hemihydrate) - 5 mg;
• auxiliary components: anhydrous glucose, disodium edetate, citric acid monohydrate, hydrochloric acid, water for injection.

Pharmacological properties

Pharmacodynamics

Levofloxacin has a broad spectrum of antibacterial action. It has a quick effect due to the inhibition of the bacterial enzyme gyrase, which belongs to type II topoisomerases. As a result of this inhibition, it becomes impossible for the bacterial DNA (deoxyribonucleic acid) to pass from a state of relaxation to a super-folded state. This, in turn, prevents further multiplication (division) of bacterial cells.

Levofloxacin is active against gram-positive and gram-negative bacteria, including non-fermenting ones.

There is cross-resistance between levofloxacin and other fluoroquinolones, while the development of cross-resistance is not observed between levofloxacin and antibacterial agents of other classes (due to the mechanism of action).

The following microorganisms are sensitive to the action of Tigeron:

• gram-negative aerobes, including Citrobacter freundii, Acinetobacter baumannii, Enterobacter cloacae, Enterobacter agglomerans, Eikenella corrodens, Escherichia coli, Haemophilus para-influenzae, Haemophilus influenzae ampi-S / R, Klebsiella pneumoniae, Klebsiella pneumoniae, Klebsella morganhalx -, Pseudomonas aeruginosa, Pasteurella multocida, Proteus vulgaris, Proteus mirabilis, Providencia stuartii, Providencia rettgeri, Serratia marcescens (for hospital infections caused by P. aeruginosa, a combination therapy may be required);
• gram-positive aerobes, including Staphylococcus aureus methi-S, Enterococcus faecalis, Staphylococcus haemolyticus methi-S, Streptococcus agalactiae, Staphylococcus saprophyticus, Streptococci group C, G, Streptococcus i pneumonia / pencoccius
• anaerobes, including Peptostreptococcus, Clostridium perfringens, Bacteroides fragilis;
• others: H. pylori, Ureaplasma, Legionella pneumophila, Chlamydia psittaci, Chlamydia pneumoniae, Mycoplasma pneumonia.

Inconsistently sensitive to the action of levofloxacin:

• gram-positive / gram-negative aerobes: Burkholderia cepacia, Staphylococcus haemolyticus methi-R;
• anaerobes: Clostridium difficile, Bacteroides vulgaris, Bacteroides thetaiotaomicron, Bacteroides ovatus.

Gram-positive aerobes Staphylococcus aureus methi-R are resistant to the action of the drug.

In relation to spirochetes, Tigeron, like other fluoroquinolones, is not active.

Pharmacokinetics

Pharmacokinetics of levofloxacin after intravenous and oral administration does not differ significantly.

Levofloxacin is rapidly and almost completely absorbed, the maximum plasma concentration is reached in about 1 hour. The absolute bioavailability is almost 100%.

In the dose range of 50-600 mg, linear pharmacokinetics are observed. Some slowdown in absorption occurs due to food intake.

From 30 to 40% of levofloxacin binds to blood plasma proteins. When applied once a day at a dose of 500 mg, the cumulative effect of clinical significance is not. A slight accumulation exists when using Tigeron 2 times a day, 500 mg. Equilibrium concentration is achieved in three days.

When used in a dose of 500 mg or more, the maximum concentration of levofloxacin in the lung tissues is approximately 11.3 mg / ml, the time to reach it is 4–6 hours. The concentration in the lungs constantly exceeds the plasma concentration.

The maximum concentration of levofloxacin in the secretion of the bronchial epithelium and the bronchial mucosa during therapy at a dose of 500 mg is 10.8 and 8.3 mg / ml, respectively.

The substance penetrates into the cerebrospinal fluid poorly.

After using 500 mg of levofloxacin 1 or 2 times a day, its maximum concentration in body fluids is 4 and 6.7 mg / ml, respectively.

The average concentration of levofloxacin in urine after a single dose of 150, 300 or 500 mg for 8 hours is 44, 91 mg / ml, for 12 hours this figure is 200 mg / ml.

The substance is metabolized slightly. Its metabolites are levofloxacin N-oxide and dismethyl-levofloxacin. They make up less than 5% of the amount of the drug excreted in the urine.

It is excreted from plasma relatively slowly, T _1/2 (half-life) is in the range from 6 to 8 hours. The main route of excretion is in the urine (more than 85% of the dose).

Indications for use

According to the instructions, Tigeron is prescribed for the treatment of the following infections that are sensitive to the action of levofloxacin:

• chronic bronchitis during an exacerbation;
• acute sinusitis;
• infections of soft tissues and skin;
• pneumonia;
• complicated / uncomplicated urinary tract infections (including pyelonephritis);
• chronic bacterial prostatitis.

Contraindications

• burdened history of adverse reactions from tendons after previous use of quinolones;
• epilepsy;
• pregnancy and lactation;
• age up to 18 years;
• individual intolerance to the components of Tigeron, as well as other quinolones.

Instructions for the use of Tigeron: method and dosage

Given the biological equivalence of oral and parenteral forms of Tigeron, the same dosage is possible.

Tigeron tablets 500 mg or 750 mg are taken orally, regardless of food intake, without chewing and drinking plenty of fluids. For ease of dosing, they can be divided. Frequency rate of admission - 1-2 times a day. The dose and duration of therapy is determined by the type and severity of the infection and is up to 14 days. After normalization of body temperature or eradication of pathogens, confirmed by microbiological tests, therapy should be continued for another 2-3 days.

Tigeron solution is administered intravenously slowly, by drop infusion. The duration of administration of one bottle (100 ml containing 500 mg of levofloxacin) is at least 60 minutes. After improving the condition, after a few days, the patient can be transferred to the oral form of the drug without dose adjustment.

After perforating the rubber stopper of the vial, Tigeron's solution should be injected within three hours (in order to prevent bacterial contamination). No light protection is required during infusion.

In the absence of impaired renal function with CC (creatinine clearance) more than 50 ml / min, Tigeron is used according to indications according to the following schemes (daily dose / frequency of use per day / duration of the course):

• exacerbation of chronic bronchitis: 250-500 mg / 1 time / 7-10 days;
• acute sinusitis: 500 mg / 1 time / 10-14 days;
• community-acquired pneumonia: 500–1000 mg / 1–2 times / 7–14 days;
• prostatitis: 500 mg / 1 time / 28 days;
• complicated infections of the urinary tract, including pyelonephritis: 250 mg / 1 time / 7-14 days (when using an infusion solution in severe cases, the dose may be increased);
• uncomplicated urinary tract infections: 250 mg / once / 3 days;
• septicemia / bacteremia: 500-1000 mg / 1-2 times / 10-14 days;
• infections of soft tissues and skin: 500-1000 mg / 1-2 times / 7-14 days;
• intra-abdominal infections: 500 mg / 1 time / 7-14 days (therapy should be carried out in combination with antibiotics that affect anaerobic pathogens).

In case of impaired renal function, the dosage regimen is determined by QC and the severity of the infection. Tigeron can be used in one of the following regimens (first dose, then subsequent doses):

• infusion rate from 50 to 20 ml / min: 250 mg, then 125 mg in 24 hours; 500 mg, then 250 mg at 24 hours; 500 mg, then 250 mg at 12 hours;
• infusion rate from 19 to 10 ml / min: 250 mg, then 125 mg at 48 hours; 500 mg, then 125 mg at 24 hours; 500 mg, then 125 mg at 12 hours;
• infusion rate less than 10 ml / min (as well as in hemodialysis and chronic ambulatory peritoneal dialysis; additional doses in this case are not required): 250 mg, then 125 mg at 48 hours; 500 mg, then 125 mg at 24 hours; 500 mg, then 125 mg every 24 hours.

Side effects

• immune system: hypersensitivity reactions, including anaphylactic / anaphylactoid shock, angioedema, urticaria, dyspnea, bronchospasm, edema of the skin and mucous membranes, shock, sudden drop in blood pressure, prolongation of the QT interval;
• lymphatic system and blood: hemolytic anemia, eosinophilia, leukopenia, agranulocytosis, neutropenia, pancytopenia, thrombocytopenia, in which an increased tendency to bleeding / hemorrhage may develop;
• nervous system: drowsiness, sleep disturbance, dizziness, headache, numbness, confusion, paresthesia, tremor, dysgeusia, convulsions, seizures, decreased tactile sensitivity, peripheral sensory / sensorimotor neuropathy, impaired sense of smell (including anosmia), dysgeusia, dysgeusia, dysgeus disorders syncope, taste disturbance / loss, benign intracranial hypertension;
• urinary system and kidneys: increased levels of creatinine in blood plasma, acute renal failure (in particular, associated with interstitial nephritis);
• hepatobiliary system: increased levels of liver enzymes and bilirubin, hepatitis, jaundice, severe liver damage (including acute liver failure, sometimes fatal; observed mainly against the background of severe underlying diseases);
• cardiovascular system: increased heart rate, tachycardia, ventricular arrhythmia, ventricular tachycardia and polymorphic ventricular tachycardia of the torsades de pointes type (mainly in the presence of risk factors for prolongation of the QT interval, which can cause cardiac arrest, prolongation of the QT interval on the ECG), hypotension, allergic vasculitis, collapse (shock-like);
• digestive system: lack of appetite, constipation, vomiting, nausea, diarrhea, abdominal pain, indigestion, dyspepsia, bloating, hemorrhagic diarrhea (may be a symptom of enterocolitis, including pseudomembranous colitis), pancreatitis;
• respiratory system: shortness of breath, allergic pneumonitis, bronchospasm;
• metabolism and nutrition: hypoglycemic coma, hyperglycemia, lack of appetite, anorexia, hypoglycemia (especially against the background of diabetes; signs of hypoglycemia include increased appetite, increased sweating, nervousness, trembling limbs);
• infections / invasions: fungal infections, including fungi of the genus Candida, proliferation of other resistant microorganisms, the development of a secondary infection, disruption of the normal intestinal microflora;
• psyche: feelings of fear, unusual dreams, insomnia, nightmares, nervousness, agitation, anxiety, psychotic disorders (including hallucinations, paranoia), depression, anxiety, anxiety, psychotic reactions with self-destructive behavior, including suicidal tendencies of actions or thinking;
• organs of vision and hearing: blurred vision, blurring or temporary loss of vision, visual impairment, hearing impairment / loss, vertigo, ringing / tinnitus;
• skin and subcutaneous tissues: stomatitis, exudative erythema multiforme, rash, pruritus, hyperhidrosis, urticaria, toxic epidermal necrolysis, hypersensitivity to solar / ultraviolet radiation, Stevens-Johnson syndrome, photosensitivity, leukocytoclastic vasculitis;
• musculoskeletal system and connective tissue: myalgia, arthralgia, tendon damage (including inflammation, in particular of the Achilles tendon), muscle weakness (of particular importance for patients with myasthenia gravis), rhabdomyolysis, rupture of ligaments, muscles and tendons, arthritis, muscle and joint pain;
• local reactions: pain / redness at the infusion site, inflammation of the veins (phlebitis);
• general disorders: general weakness, asthenia, fever, pain (including in the back, chest and extremities), porphyria attacks (against the background of porphyria).

During treatment with Tigeron, there may be disorders associated with their influence on the normal microflora of the human body. For this reason, a secondary infection may develop, requiring additional therapy.

Overdose

The main symptoms: erosion of mucous membranes, dizziness, confusion, seizures, impaired consciousness, hallucinations, nausea, tremor, prolongation of the QT interval.

Therapy: symptomatic, no specific antidote. Given the likelihood of lengthening the QT interval, it is necessary to monitor the indicators of the electrocardiogram (ECG). In case of an obvious overdose, gastric lavage is prescribed. In order to protect the gastric mucosa, it is possible to use antacids. Hemodialysis, including chronic ambulatory peritoneal dialysis and peritoneal dialysis, is ineffective for removing levofloxacin from the body.

special instructions

For methicillin-resistant S. aureus (MRSA), there is a very high likelihood of Tigeron bore resistance. The drug is not recommended for the treatment of infections, the known / suspected causative agent of which is MRSA, unless the sensitivity of the causative agent to levofloxacin is confirmed by laboratory tests.

Tigeron can be used in the treatment of acute bacterial sinusitis and exacerbation of chronic bronchitis after proper diagnosis.

Resistance to E. coli (the most common causative agent of urinary tract infections) varies from country to country. When prescribing Tigeron, the local prevalence of E. coli resistance to this group of antibacterial drugs should be taken into account.

Sometimes, during the use of the drug, tendonitis appears. In most cases, this is related to the Achilles tendon and can lead to tendon rupture. This violation can occur within two days after the start of therapy and be bilateral. The likelihood of tendonitis and tendon rupture increases in patients over 60 years of age, with the use of Tigeron at a dose of 1000 mg per day, as well as during therapy with corticosteroids. The daily dose for elderly patients should be adjusted depending on the CC. When Tigeron is assigned to this group, their condition should be closely monitored. If symptoms of tendonitis appear, discontinue therapy and consult a doctor.

If diarrhea occurs, especially in a severe degree, persistent and / or with an admixture of blood that occurs during / after treatment with Tigeron (including for several weeks after therapy), it is necessary to consider the likelihood of developing a disease caused by Clostridium difficile. Pseudomembranous colitis is a severe form of this disease. In cases of suspicion of pseudomembranous colitis, Tigeron is immediately canceled and appropriate treatment is prescribed. The use of drugs that suppress intestinal peristalsis is contraindicated.

On the background of quinolone therapy, it is possible to lower the seizure threshold and the occurrence of seizures. With a burdened history of epilepsy, Tigeron is not prescribed. In the case of a tendency to seizures, as well as in the course of combined therapy with drugs that lower the seizure threshold, Tigeron should be used with extreme caution. If a convulsive attack occurs, levofloxacin is canceled.

Patients with obvious / latent impairments to glucose-6-phosphate dehydrogenase activity may have a tendency to hemolytic reactions during therapy with quinolone antibiotics. If it is necessary to prescribe Tigeron to this group of patients, their condition should be monitored (associated with the possible occurrence of hemolysis).

The use of levofloxacin can lead to serious, potentially fatal hypersensitivity reactions. Sometimes these disorders occur at the beginning of treatment (after the first dose). In such cases, Tigeron is canceled and appropriate treatment is prescribed.

There is evidence of the appearance of severe bullous reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis. If during the period of therapy any reactions from the skin / mucous membranes occur, you should immediately stop using levofloxacin and consult a doctor, if necessary, appropriate treatment is prescribed.

Cases of changes in blood glucose levels during therapy with quinolones were reported, among which the development of hyper- and hypoglycemia was noted. Usually, this disorder was recorded in patients with diabetes mellitus receiving concomitant treatment with oral hypoglycemic drugs or insulin. There are reports of cases of hypoglycemic coma. Patients with diabetes mellitus are advised to closely monitor blood glucose levels.

In order to prevent the development of photosensitization during treatment and for 48 hours after its completion, it is recommended to avoid exposure to artificial sources of UV rays or exposure to strong solar radiation.

When conducting combined therapy with a vitamin K antagonist (in particular, warfarin), the level of blood coagulation indicators may increase or the frequency of hemorrhagic complications may increase. In such cases, monitoring of blood coagulation indicators is required.

If the patient experiences psychotic reactions during the use of Tigeron, the therapy is canceled. With a history of psychotic disorders or mental illness, the drug should be administered with caution.

Patients who have the following risk factors for QT interval prolongation need special attention:

• congenital / acquired QT prolongation syndrome;
• heart disease (myocardial infarction, heart failure, bradycardia);
• electrolyte imbalance (hypomagnesemia, hypokalemia);
• combination therapy with drugs that can prolong the QT interval.

In elderly patients, there is a great sensitivity to drugs that prolong the QT interval, which requires caution when using Tigeron in combination with these drugs.

If symptoms of sensorimotor peripheral / sensory neuropathy appear, in order to timely prevent an irreversible condition, Tigeron therapy should be canceled.

Against the background of the use of levofloxacin (mainly in severe underlying diseases, for example, sepsis), liver necrosis may develop, sometimes to liver failure with a fatal outcome. If symptoms such as dark urine, jaundice, anorexia, pain / itching in the abdomen appear, Tigeron therapy is recommended to be interrupted.

Fluoroquinolones, including levofloxacin, can lead to neuromuscular blockade and exacerbation of muscle weakness in patients with myasthenia gravis. In the post-registration period, in patients with this disease against the background of the use of Tigeron, serious adverse reactions were noted, including conditions in which measures to support breathing were required, and deaths. Levofloxacin is not recommended for use with a history of myasthenia gravis.

In cases of development of visual impairment / any side effects from the side of vision, you should immediately consult an ophthalmologist.

During Tigeron therapy, when determining opiates in urine, a false-positive result is possible, which may require confirmation using more specific methods.

Levofloxacin can lead to false negative results in the bacteriological diagnosis of tuberculosis (by inhibiting the growth of Mycobacterium tuberculosis).

Influence on the ability to drive vehicles and complex mechanisms

During the period of therapy, it is necessary to assess the individual response to Tigeron. With the development of adverse reactions in the form of drowsiness, dizziness or visual impairment, it is recommended to refuse from driving vehicles and performing other potentially hazardous types of work.

Application during pregnancy and lactation

Tigeron is not prescribed during pregnancy / lactation.

When diagnosing pregnancy, you must inform your doctor.

Pediatric use

Tigeron is not prescribed for patients under 18 years of age.

With impaired renal function

In case of impaired renal function, correction of the dosage regimen is required.

Drug interactions

Possible interactions:

• zinc and iron salts, antacids containing aluminum or magnesium, didanosine (this refers to dosage forms of didanosine with aluminum or magnesium-containing buffer agents), multivitamins containing zinc: absorption of levofloxacin is significantly reduced (the recommended interval between their use is 2 hours);
• sucralfate: the bioavailability of levofloxacin is significantly reduced (the recommended interval between their use is 2 hours);
• theophylline, fenbufen or similar non-steroidal anti-inflammatory drugs: the likelihood of a significant decrease in the seizure threshold must be taken into account;
• cyclosporin: its T _1/2 increases;
• probenecid, cimetidine: excretion of levofloxacin decreases; if combined therapy is necessary, care must be taken, especially in renal failure;
• drugs that prolong the QT interval (class II A and III antiarrhythmics, tricyclic antidepressants, macroliths and antipsychotic drugs): therapy requires caution;
• vitamin K antagonists: it is necessary to control the coagulation parameters.

Solution for infusion Tigeron is compatible with the following infusion solutions: 0.9% sodium chloride solution, 5% dextrose solution, Ringer's solution, combined solutions for parenteral nutrition (carbohydrates, amino acids, electrolytes). It is impossible to mix Tigeron with heparin or solutions with an alkaline reaction (in particular, with a solution of sodium bicarbonate).

Analogs

Tigeron's analogs are Roflox-Scan, Floracid, Leflobact, Haileflox, Flexid, Glevo, Tavanik, Lefoktsin, Levolet, Eleflox, Remedia, Levofloxacin and others.

Terms and conditions of storage

Store in a place protected from light at temperatures up to 25 ° C. Keep out of the reach of children.

Shelf life: tablets - 2 years; infusion solution - 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Tigeron

Reviews about Tigeron are quite controversial. Some of them note a quick effect, ease of use, and almost complete absence of side effects. Other users point out that the drug does not have the proper therapeutic effect, various negative reactions develop during use, and also note its high cost.

The price of Tigeron in pharmacies

The price of Tigeron tablets with a dosage of 750 mg per package of 5 pcs. is about 700 rubles. The cost of Tigeron tablets 500 mg is 500–600 rubles. per package of 5 pcs.

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!