The pharmacokinetics of levofloxacin are linear and predictable with single and multiple drug administration. The plasma profile of levofloxacin concentrations after intravenous administration is similar to that of tablets.

Therefore, the oral and intravenous routes of administration may be considered interchangeable.

The plasma protein binding is 30-40%. It penetrates well into organs and tissues: lungs, mucous membrane of bronchi, sputum, urinary system organs, genitals, bone tissue, cerebrospinal fluid, prostate, polymorphonuclear leukocytes, alveolar macrophages.

The average volume of distribution of levofloxacin is from 89 to 112 liters after single and multiple intravenous administration of 500 mg.

The pharmacokinetic characteristics after single intravenous administration of levofloxacin at a dose of 500 mg, respectively, are: maximum concentration (6.2 ± 1.0) µg/ml, time required to reach maximum concentration – (1.0 7 ± 0.1)h, elimination half-life – (6.4 ± 0.7) h.

Levofloxacin is mainly excreted unchanged by the kidneys.

In case of renal failure the decrease of clearance of the drug and its excretion through the kidneys depends on the degree of decrease of creatinine clearance.

Indications

Infectious inflammatory diseases caused by bacteria sensitive to levofloxacin:

lower respiratory tract (community-acquired pneumonia);

urinary tract and kidney (including acute pyelonephritis);

chronic bacterial prostatitis;

Skin and soft tissue (suppurative atheromas, abscesses, furuncles);

septicemia/bacteremia associated with the above indications;

intra-abdominal infections.

Active ingredient

Levofloxacin

Composition

Composition per 100 ml of the drug:

Active ingredient: Levofloxacin hemihydrate (in terms of Levofloxacin) – 500 mg;

Excipients: sodium chloride – 900 mg, water for injections – up to 100 ml.

How to take, the dosage

Intravenously drip slowly 1-2 times a day. Doses are determined by the nature and severity of the infection, as well as the sensitivity of the suspected pathogen.

Patients with normal renal function (creatinine clearance >50 ml/min) may be recommended the following dosing regimen:

Out-of-hospital pneumonia: 500 mg of levofloxacin (100 ml of drug) 1-2 times a day, for 7-14 days;

uncomplicated urinary tract infections: 250 mg of levofloxacin (50 ml of the drug) once a day for 3 days;

complicated urinary tract infections (including acute pyelonephritis): 250 mg of levofloxacin (50 ml of the drug) once a day, for 7-10 days;

Skin and soft tissue infections (suppurated atheromas, abscesses, furuncles): 500 mg (100 ml of the drug) 2 times a day, for 7-14 days.

Chronic bacterial prostatitis: 500 mg of levofloxacin (100 ml of drug) once daily, for 28 days;

Septicemia/bacteremia: 500 mg of levofloxacin (100 ml of the drug) 1-2 times daily, for 10-14 days;

intraabdominal infection: 500 mg of levofloxacin (100 ml of drug) once daily, for 7-14 days (in combination with antibacterials acting on anaerobic flora).

Patients with impaired renal function require adjustment of the dosing regimen depending on the creatinine clearance value.

The dosing regimen:

Creatinine clearance	250mg/24h.	500 mg/24 hours.		500 mg/12 hour;
Creatinine clearance	First dose: 250 mg	first dose: 500 mg	first dose: 500 mg
	50-20 ml/min.	Thereafter: 125 mg at 125 mg/24 hours.	then: 250 mg/24 hr.	then: 250 mg/12 hr.
19-10 ml/min.		Then at 125 mg/48 hours.	Then: 125 mg/24 hours.	then: 125 mg/12 hr.
		Then at 125 mg/48 hours.	Then: 125 mg/24 hr.		then: 125 mg/24 hr.

1 – No additional doses are required after hemodialysis or long-term ambulatory peritoneal dialysis (DAPD).

In case of hepatic impairment, no special dosage adjustment is required because levofloxacin is only metabolized to a very minor extent in the liver.

Levofloxacin infusion solution 500 mg (100 ml) is administered intravenously by slow drip.

The duration of infusion of 1 vial of levofloxacin 500 mg (100 ml) solution should be at least 60 minutes. After intravenous administration after a few days, it is possible to switch to oral administration at the same dose.

The treatment with levofloxacin is recommended to continue for at least 48-72 hours after normalization of body temperature or after reliable eradication of the pathogen.

Interaction

When combined treatment with phenbufen and similar non-steroidal anti-inflammatory drugs, theophylline, the drug may increase the seizure threshold.

Glucocorticoids increase the risk of tendon rupture (especially in the elderly).

Levofloxacin excretion is slightly delayed by cimetidine and probenecid. Levofloxacin causes a slight increase in the blood plasma elimination half-life of cyclosporine.

Concomitant use with warfarin increases prothrombin time and risk of bleeding (close monitoring of INR; prothrombin time and other coagulation indices, as well as monitoring of possible bleeding signs is necessary).

Alcohol may exacerbate central nervous system side effects (dizziness, somnolence).

In diabetic patients receiving oral hypoglycemic agents or insulin hypo- and hyperglycemic states are possible while taking levofloxacin (close monitoring of blood glucose concentration is recommended).

In concomitant use with drugs prolonging the QT interval (antiarrhythmic drugs of classes IA and III, tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungals, imidazole derivatives, some antihistamines, including astemizole, terfenadine, ebastine) QT interval prolongation is possible.

Infusion solution is compatible with 0.9% sodium chloride solution, 5% dextrose (glucose) solution, 2.5% Ringer’s solution with dextrose, combined solutions for parenteral nutrition (amino acids, carbohydrates, electrolytes).

Special Instructions

In severe pneumonia caused by pneumococci, the therapeutic effect of Leflobact may be insufficient.

After normalization of body temperature, it is recommended to continue treatment for at least 48-72 hours.

The duration of intravenous infusion of 500 mg (100 ml infusion solution) should be at least 60 minutes.

A sensation of palpitation; transient decrease of blood pressure may be observed in individual cases during the infusion. If there is a significant decrease in blood pressure, the infusion should be stopped immediately.

At the time of treatment it is necessary to avoid sunlight and artificial ultraviolet irradiation in order to avoid skin damage (photosensitization).

In case of signs of tendinitis, pseudomembranous colitis and allergic reactions levofloxacin should be stopped immediately.

It should be noted that patients with a history of brain damage (stroke, severe trauma) may have seizures, with insufficiency of glucose-6-phosphate dehydrogenase – risk of hemolysis.

Because levofloxacin is excreted mainly through the kidneys, in patients with impaired renal function it is necessary to monitor renal function and adjust the dosing regimen. Very rare cases of QT interval prolongation have been reported in patients receiving fluoroquinolones, including levofloxacin. When using fluoroquinolones, including levofloxacin, care should be taken in patients with known risk factors for QT interval prolongation: older age; electrolyte imbalance (hypokalemia, hypomagnesemia); congenital QT interval prolongation syndrome; heart disease (heart failure, myocardial infarction, bradycardia); simultaneous use of drugs that can prolong the QT interval. Patients receiving fluoroquinolones, including levofloxacin, have experienced sensory and sensory-motor peripheral neuropathy, the onset of which may be rapid. If the patient develops symptoms of neuropathy, the use of levofloxacin should be discontinued. This minimizes the possible risk of developing irreversible changes.

Alcohol consumption should be avoided during treatment.

Effect on the ability to drive vehicles and vehicles:

During treatment it is necessary to refrain from driving and potentially dangerous activities that require high concentration and rapid psychomotor reactions.

Contraindications

hypersensitivity (including to other quinolones);
epilepsy;
tendon involvement in previous quinolone treatment;
pregnancy;
lactation period; childhood and adolescence (under 18 years).

With caution:

Elderly age, due to the high likelihood of concomitant decreased renal function (glucose-6-phosphate dehydrogenase deficiency).

In patients with brain damage; history (stroke or severe trauma) (possible development of seizures).

In patients with pseudoparalytic myasthenia gravis; with known risk factors for QT interval prolongation.

In patients with diabetes mellitus.

The use of levofloxacin concomitantly with other QT interval prolonging agents is not recommended because the risk of cardiac arrhythmias increases.

Predisposition to seizure reactions (cerebral atherosclerosis, cerebral circulatory disorders (in anamnesis), organic diseases of the central nervous system), renal failure, congenital prolongation of the QT interval syndrome, heart disease (heart failure, myocardial infarction, bradycardia), electrolyte imbalance (e.g. in hypokalemia, hypomagnesemia), psychosis and other mental disorders in the history, hepatic porphyria/ concurrent use of drugs that prolong the QT interval, (antiarrhythmic drugs of classes IA and III, tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungals, imidazole derivatives, some antihistamines, including astemizole, terfenadine, ebastine) and lowering the threshold, seizure readiness of the brain (phenbufen, theophylline).

Side effects

Digestive system disorders: nausea, vomiting, diarrhea, decreased appetite, abdominal pain, pseudomembranous colitis; increased liver transaminase activity, hyperbilirubinemia, hepatitis, dysbacteriosis, severe liver failure, including cases of acute liver failure, especially in patients with severe underlying disease (eg, sepsis).

Cardiovascular system disorders: decreased blood pressure, vascular collapse, tachycardia, prolonged QT interval.

Metabolic disorders: hypoglycemia (increased appetite, increased sweating, shivering), porphyria attacks.

Nervous system disorders, headache, dizziness, weakness, drowsiness, insomnia, paresthesias, peripheral sensory and sensorimotor neuropathy, anxiety, fear, psychotic reactions, self-harming behavior, including suicidal thoughts and actions, hallucinations, confusion, depression, movement disorders, seizures, tremor, extrapyramidal disorders, agitation (agitation), nightmares.

Sense organs: agueusia, dysgeusia (perversion of taste), loss of taste sensation, parosmia (disorder of sense of smell, especially subjective sense of smell, objectively absent), including loss of smell, vertigo (feeling of deviation or twisting or own body or surrounding objects), ringing in ears, hearing loss.

Musculoskeletal system: arthralgia, myasthenia, myalgia, tendon rupture, tendinitis, rhabdomyolysis.

Urinary system disorders: hypercreatininemia, interstitial nephritis, acute renal failure.

Hematopoietic disorders: eosinophilia, hemolytic anemia, leukopenia, neutropenia; agranulocytosis, thrombocytopenia, pancytopenia, hemorrhages.

Allergic reactions: itching, hyperemia, swelling of the skin and mucous membranes, urticaria, erythema malignant exudative (Stevens-Johnson syndrome), toxic epidermal necrolysis, bronchospasm, choking, shortness of breath, anaphylactic shock, allergic pneumonitis, vasculitis.

Local reactions: phlebitis and periphlebitis.

Others: exacerbation of porphyria, photosensitization, persistent fever, development of superinfection, asthenia.

Overdose

Symptoms: confusion, dizziness, seizures, QT interval prolongation.

Treatment: symptomatic, dialysis is ineffective.

Pregnancy use

It is contraindicated in pregnancy. Breastfeeding should be stopped during treatment.

Similarities

Signicef, Tavanic, Oftavix, Flexid, Levolet R, Levofloxacin-Teva, Glevo, Haileflox, L-Optik Romfarm, Levofloxacin, Korfecin

Additional information

Weight	0.206 kg
Shelf life	2 years. Do not use after the expiration date printed on the package.
Conditions of storage	In a place protected from light at a temperature of 15 to 25 ° C. The infusion solution can be stored without light protection for no more than 3 days. Freezing is not allowed. Store in places out of the reach of children.
Manufacturer	Sintez OAO, Russia
Medication form	solution for infusion
Brand	Sintez OAO

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