Zolev

Zolev is a systemic antibacterial drug from the category of fluoroquinolones.

Indications Zoleva

It is used in the treatment of infections, the development of which is provoked by the activity of bacteria that are sensitive to drugs:

• pneumonia ;
• acute sinusitis;
• chronic bronchitis in the exacerbation phase;
• septicemia or bacteremia;
• infectious lesions affecting the system of urination (with complications and without them) - for example, pyelonephritis;
• lesions of soft tissues and epidermis;
• prostatitis ;
• infection in the intra-abdominal zone.

Release form

The release is made in tablet form, in an amount of 5 pieces packed in a blister plate. In the box - 1 blister.

Zolev infusions

Infusion fluid is released in containers with a volume of 0.1 or 0.15 liters. Inside the package there is one such container.

Pharmacodynamics

Levofloxacin has a large range of antibacterial therapeutic activity. The bactericidal effect develops by suppressing the bacterial enzyme DNA-gyrase related to the second kind of topoisomerases by the active substance of the drug. Due to this suppression, the DNA transition of the bacterium from relaxation to a twisted state becomes impossible, which prevents the subsequent multiplication of pathogenic cells. Gram-negative and-positive microbes with non-fermenting microorganisms fall into the spectrum of the drug's influence.

The following bacteria have a sensitivity to drugs:

• Gram-positive germs: Enterococcus fecal, Staphylococcus aureus, methy-Staphylococcus aureus, Streptococcus agalactia, Pyogenetic streptococcus, and besides staphylococcus a coagulase negative type methi-S (1), Streptococci from the category C and G, and pneumococcus peni-I / S / R ;
• aerobes of a gram-negative nature: Baumann akinetobacterium, Enterobacter agglomerans, citrobacter frowni, Eikenella corrodens, enterobacter cloaca, E. Coli, klebsiella oxytoca, hemiphilic rod ampi-S / R, and Haemophilus parainfluenzae, Morgan bacteria, Klebsiella pneumonia, proteus mirabilis, moraxella cataralis β +/- and ordinary protei. In addition to the list of the multicid pasteurella, the Providence of Rettger and Stewart's Providence, the Pseudomonas aeruginosa and the Marcecens serration;
• anaerobes: phagillis bacteroids, peptostreptococci and clostridium perforingens;
• Other: legionella pneumophilus, ureaplasma, chlamydophile pneumonia, mycoplasma pneumonia, chlamydophile psittaci and Helicobacter pylori.

Inconsistent sensitivity is possessed by:

• aerobes of Gram-positive type: Staphylococcus aureus methi-R .;
• aerobes of the gram-negative type: Burkholderia cepacia;
• anaerobes: bacterium tetiothaomicron, Bacteroides ovatus, clostridium difffile and Bacteroides vulgaris.

Resistant to the action of Zolev: Gram-positive aerobes - Staphylococcus aureus methi-R, as well as staphylococcus a coagulase of the negative category of methi-S (1).

Like other fluoroquinolones, the element levofloxacin does not have an effect on the activity of spirochetes.

Pharmacokinetics

Absorption.

Levofloxacin is absorbed at high speed and absorbed almost completely, reaching the highest plasma marks after 60 minutes from the time of ingestion.

The absolute bioavailability is almost 100%. The drug has pharmacokinetic characteristics of the linear type with the use of therapeutic portions, which are within the range of 0.05-0.6 g. The intake of food does not affect the degree of absorption.

Distribution processes.

Approximately 30-40% of the substance is synthesized with a plasma protein. Cumulation of the drug with a single daily use of 0.5 g does not have clinical significance, so it is allowed to disregard. It also assumes an insignificant cumulation of the substance with a twice daily use of 0.5 g of drugs. Stable digits of distribution are noted after 3 days.

The level of Cmax of the drug in the area of the bronchial mucosa and epithelial secretion after applying a portion of 0.5 g per os reached 8.3, and in addition 10.8 μg / ml, respectively.

In the field of lung tissue, the achievement of Cmax of the drug after using a dosage of 0.5 g per os was observed after 4-6 hours, and this value was approximately 11.3 μg / ml. The pulmonary values of the drug were constantly higher than its plasma indices.

Inside the pemphigus fluid, the Cmax Zolev index, when consumed 0.5 g 1-2 times a day, reaches, respectively, 4, as well as 6.7 μg / ml.

Levofloxacin demonstrates a weak passage into the CSF.

When the drug was taken orally for 3 days (0.5 g portion, once a day), the average medication within the prostate was 8.7, and in addition 8.2 and 2 μg / g after 2, 6- and 24 hours. The average ratio of medication within the prostate / blood plasma is 1.84.

The average values of levofloxacin within the urine in the period of 8-12 hours after the application of a 1-time portion of 0.15, 0.3 or 0.5 g per os reached, respectively, 44, 91 and 200 μg / ml.

Exchange processes.

The process of levofloxacin exchange is extremely weak, its decay products are the components of dysmethyl-levofloxacin, as well as levofloxacin N-oxide. Such substances make up less than 5% of the dosage of drugs excreted in the urine.

Excretion.

When ingested, the process of plasma excretion of levofloxacin proceeds rather slowly (the half-life is 6-8 hours). Excretion mostly occurs through the kidneys (more than 85% of the portion). A marked difference in the pharmacokinetics of drugs with intravenous and oral use is not observed.

Dosing and administration

The scheme of taking tablets.

Drug use should be 1-2 times a day. The size of the portion is determined by the degree of severity and the type of infection. The duration of therapy is associated with the course of the disease, but is a maximum of 2 weeks. It is recommended to continue the course in the period of 48-72 hours after the temperature returned to normal level or confirmed by data from microbiological studies of elimination of bacterial pathogens.

The medicine is swallowed whole, without chewing, washing down with liquid. Consumption occurs without binding to the reception of food. Tablets with a volume of 0.5 and 0.75 g can be divided in half.

It is required to adhere to the following dosage regimen Zoleva for therapy in adults with healthy renal function (KK level> 50 ml / minute):

• sinusitis, having a sharp form - per day taken once for 0.5 g of drugs. Therapy lasts 10-14 days;
• chronic stage of bronchitis at the stage of exacerbation - one-time intake of 0.25-0.5 g per day. Treatment lasts about 7-10 days;
• ambulatory pneumonia - for one day take 1-2 times for 0.5-1 g of substance, for 1-2 weeks;
• infections affecting the urethra (without complications) - 1-time intake per day 0.25 g of drugs. The therapy lasts 3 days;
• prostatitis - 1-fold use of 0.5 g of medicament per day. The treatment cycle should last 28 days;
• infections that affect the urethra (with complications - for example, pyelonephritis) - a single dose of 0.25 grams of medication per day. Therapy lasts 7-10 days;
• affecting the hypodermic layer and the epidermis of infection - 1-2-fold use per day 0.5-1 g of substance. The duration of the course is 7-14 days;
• bacteremia or septicemia - 0.5-1 g of medicament 1-2 times per day. The treatment period is 10-14 days;
• infections that develop in the intra-abdominal zone * - 0.5 g of LS 1-fold per day. Take the drug need 7-14 days.

* Combination with antibiotics that affect the anaerobes.

Serving sizes for people with impaired renal function - CC values are <50 ml / minute:

• the QC value is within the range of 50-20 ml / minute: with the mild form of the disease, the first dosage is 0.25 g, and the subsequent dosage is 0.125 g (24 hours). With a moderate form, the size of the first portion is 0.5 g, and the subsequent - 0.25 (for 24 hours). In severe form - the first portion is 0.5 g, and the subsequent - 0.25 g (for 12 hours);
• the level of QC within 19-10 ml / minute: an easy degree of pathology - the first dosage is 0.25 g, the subsequent - 0.125 g (48 hours). Moderate degree - the first portion is 0.5 g, the subsequent - 0.125 g (for 24 hours). Severe degree - the first dose is 0.5 g, the subsequent - 0.125 g (for 12 hours);
• values of CC <10 (also people on hemodialysis or HAD): mild disease - the first portion is 0.25 g, the next - 0.125 g (48 hours). Moderate and severe character - the first dosage is 0.5 g, the subsequent - 0.125 g (for 24 hours).

Use of a drug solution.

The medicine is injected 1-2 times a day, at a low speed. The size of the portion is determined by taking into account the severity and type of the disease, and besides this, the sensitivity of the exciter bacterium in relation to drugs. After the initial use of the intravenous form of the drug, you can continue therapy with the use of tablets (if this method is acceptable for the patient). Taking into account the bioequivalence of the oral and parenteral forms of drugs, it is allowed to use the same dosages.

The duration of the infusion used is at least half an hour (at a dose of 0.25 g) or 1 hour (with a serving of 0.5 g).

[2]

Use Zoleva during pregnancy

Because of the lack of tests regarding the use of Zolev in humans, and the likelihood of damage to articular cartilage under the influence of quinolones during the growth stage of the child's body, it is forbidden to use it in lactation or pregnancy. When pregnancy occurs while taking drugs, you need to notify the doctor about it.

Contraindications

The main contraindications:

• the presence of intolerance in relation to levofloxacin, other quinolones or other components of the drug;
• seizures of epilepsy;
• patients with complaints about the development of negative symptoms in the field of tendons after the earlier taking quinolones.

Side effects Zoleva

The use of medication can cause some side effects:

• lesions that are infectious or invasive in nature: fungal forms of infections (including candida fungi), as well as reproduction of other resistant microbes;
• disorders affecting the activity of lymph and blood flow: eosinophilia, hemolytic form of anemia, leuko-, neutro-, thrombocyto- and pancytopenia, as well as agranulocytosis;
• immune disorders: symptoms of increased sensitivity, including anaphylaxis and anaphylactoid shock, Quinck edema, as well as anaphylactic and anaphylactoid manifestations. Sometimes these symptoms can appear immediately after applying the first dose;
• problems with the nutritional process and metabolism: hypoglycemia (especially in diabetics), anorexia, as well as hyperglycemia or hypoglycemic coma;
• mental disorders: agitation, a feeling of nervousness, confusion, anxiety and anxiety, insomnia, psychotic disorders (among such paranoia and hallucinations) and the state of depression. In addition, nighttime delirium and pathological dreams, as well as psychotic disorders, accompanied by self-destructive actions (suicidal thoughts and suicide attempts);
• disorders of the function of the NS: a feeling of drowsiness, dizziness, convulsions, headaches, paresthesia and tremor. In addition, the weakening of tactile sensations, polyneuropathy sensorimotor or sensory character and dysgeusia, which can be accompanied by parosmia, agevia and anosmia. The list also includes syncope, dyskinesia, increased levels of ICP (benign), extrapyramidal disorders and other motor coordination disorders (eg, walking);
• lesions affecting the visual system: visual fogging or frustration, transient loss of vision;
• problems with auditory function and labyrinth: hearing disorder, vertigo, hearing loss and ear noise;
• disorders of the heart: heartbeat, tachycardia and VT, which can cause heart failure. In addition, there is ventricular arrhythmia and pirouette tachycardia (often in individuals with the likelihood of prolonging the QT-interval), and prolongation of QT-interval on ECG;
• vascular lesions: an allergic vasculitis and a decrease in blood pressure;
• disorders of mediastinal or respiratory function, as well as the activity of the organs of the sternum: spasm of bronchi, dyspnea and pneumonitis, allergic;
• digestive disorders: loss of appetite, diarrhea, abdominal pain, stomatitis, vomiting, and in addition symptoms of dyspepsia, pancreatitis, flatulence and nausea. Also, hemorrhagic diarrhea can occur, which can occasionally be a sign of enterocolitis (also a pseudomembranous form of colitis);
• problems with the work of the hepatobiliary system: an increase in the level of liver enzymes (alkaline phosphatase with ALT and AST, and in addition GGTP) and blood values of bilirubin. In addition, jaundice, hepatitis and hepatic disease develop in severe cases (this includes cases of acute liver failure) - mainly in people with severe forms of underlying pathologies;
• damage to the subcutaneous layers and epidermis: itching, intolerance to UV and solar radiation, rashes, TEN, urticaria, hyperhidrosis, Stevens-Johnson syndrome, MEE and photosensitivity. At times, signs from the mucous and epidermis appear after the first use;
• disorders in the area of connective tissue, musculature and bones: manifestations affecting tendons - among such tendonitis, myalgia, arthritis and arthralgia, as well as rupture of ligaments, tendons or muscles. There may be muscle weakness, which is especially important for people with rhabdomyolysis or a severe form of myasthenia gravis;
• disorders in the system of urination and kidneys: increased plasma values of creatinine and arthritis (eg, due to tubulointerstitial nephritis);
• systemic signs: a feeling of general weakness, painful reactions (in the limbs, back and sternum), asthenia, fever and porphyria attacks in people with this disease.

[1]

Overdose

Signs of an overdose: a disorder of consciousness, nausea, dizziness, seizures of erosion in the mucosa, prolongation of the QT-interval or intensification of the symptoms of other adverse reactions. When poisoning, you need to closely monitor the patient's condition (including ECG indicators).

Symptomatic measures are carried out. Procedures for hemodialysis (including HAFA or peritoneal dialysis) do not allow the excretion of levofloxacin. Also, the medicine has no antidotes.

Interactions with other drugs

Aluminum-or magnesium-containing antacids, as well as medicines containing zinc or iron salts, and addition of didanosine.

Absorption of the drug is markedly reduced when combined with the aforementioned agents. The combined intake of fluoroquinolones and multivitamins, which contain zinc, causes a decrease in the degree of absorption of the latter. It is necessary to observe the intervals between the use of such medications (their duration is at least 120 minutes).

Calcium salts have only a minimal effect on the absorption of levofloxacin.

Sucralfate.

The level of bioavailability of levofloxacin is significantly reduced when combined with sucralfate. The gap between the application of these drugs should last at least 2 hours.

Fenbufen with theophylline or similar NSAIDs.

There can be an extremely strong decrease in the limits of the convulsive threshold in the case of a combination of quinolones with the above drugs and other elements that have a similar medicinal effect. The level of levofloxacin when using fenbufen increases by about 13%.

Cimetidine with probenecidoma.

It has been statistically proven that the above agents affect the character of the excretion of levofloxacin. The values of the clearance of the substance inside the kidneys are reduced by 34% (with probenecid) and by 24% (with cimetidine). Such properties allow these drugs to block the excretion of Zolev through the tubules.

The pharmacokinetic parameters of levofloxacin remain unchanged when combined with digoxin, calcium carbonate, warfarin, and ranitidine and glibenclamide.

Ciclosporin.

The half-life of cyclosporine is increased by 33% when combined with a medication.

Medicines that exert antagonistic effects on vitamin K.

Co-administration with such drugs (for example, warfarin) increases the level of coagulation indicators (INR or PTV) or increases the severity of bleeding. Because of this, people taking these drugs together with levofloxacin, it is necessary to monitor coagulation values.

Medications prolonging QT-interval.

Like other fluoroquinolones, levofloxacin should be used carefully in people who use drugs such as macrolides, tricyclics, antipsychotics and antiarrhythmic drugs of categories 1A and 3.

Levofloxacin has no effect on the pharmacokinetic properties of theophylline, the metabolism of which mainly occurs with the participation of CYP 1A2, from which it can be concluded that levofloxacin does not slow the activity of CYP 1A2.

The drug does not interact with food, so it can be used without reference to its reception. It is forbidden to drink alcohol during treatment with levofloxacin.

[3], [4]

Storage conditions

Zolev should be kept in a dark and dry place, which is inaccessible to small children. The solution should not be frozen. The temperature values are a maximum of 30 ° C (tablets) or 25 ° C (solution).

Shelf life

Zolev can be used within 2 years of the release of the therapeutic drug.

Application for children

The appointment of a medication to persons under the age of 18 is prohibited, because there is a risk of damage to the cartilage in the joint area.

Analogues

Analogues of the drug are the drugs Tavanik, Levomak with Levot and Flexin, and besides Leflotsin, Leflok, Levofloxacin and Levobakt.