medicalmeds.eu Medicines Antimicrobic means, фторхинолон. Levozin

Levozin

Препарат Левозин. АО «Нобел Алматинская Фармацевтическая Фабрика» Республика Казахстан

Producer: JSC Nobel Almatinskaya Pharmatsevticheskaya Fabrika Republic of Kazakhstan

Code of automatic telephone exchange: J01MA12

Release form: Firm dosage forms. Tablets.

Indications to use: Acute sinusitis. Chronic bronchitis. Extra hospital pneumonia. Chronic prostatitis. Infections of urinogenital system. Acute pyelonephritis.

General characteristics. Structure:

Active ingredient: 250 mg, 500 mg or 750 mg of a levofloksatsin of a gemigidrat equivalent to a levofloksatsin.

Excipients: cellulose microcrystallic PH 102, hydroxypropyl methyl cellulose (фармакоат 603 W), кросповидон (коллидон), sodium stearit fumarating,

Structure of a cover: No. VIII of an opadra Y I 7000 white (gidroksipropilmetiltsellyuloz (gipromelloz), titanium dioxide, polyethyleneglycol 400 (macrogoal 400).

Antibiotic of a ftorkhinolonovy number of a broad spectrum of activity.

Pharmacological properties:

Pharmacodynamics. Levozin - antimicrobic drug from group of ftorkhinolon. Possesses a wide range of antimicrobic action. The bactericidal effect is shown at the expense of DNA synthesis inhibition.

Levozin has a wide range of antibacterial activity against the majority of gram(s) and grams (+) microorganisms, is active concerning the bacteria steady against action of other antibiotics (aminoglycosides, macroleads and beta lactams). Resistance to a levofloksatsin owing to natural mutations of in vitro is an exceptional case (ranging from 10-9 till 10-10).

Though cross stability was observed between levofloksatsiny and other ftorkhinolona, some microorganisms steady against other ftorkhinolonovy drugs can be sensitive to a levofloksatsin.

Levozin is active concerning the majority of strains of microorganisms:

- aerobic gram (+) microorganisms: Enterococcus faecalis (many strains are only moderately sensitive), Staphylococcus aureus (Methicillinum - sensitive strains), Staphylococcus epidermidis (Methicillinum - sensitive strains), Staphylococcus saprophyticus, Streptococcus pneumoniae (including penicillin - resistant strains), Streptococcus pyogenes.

- aerobic microorganisms of gram(s): Enterobacter cloacae, Escherichia coli, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Legionella pneumophila, Moraxella catarrhalis, Proteus mirabilis, Pseudomonas aeruginosa, Serratia marcescens.

As well as with other drugs of this row, during treatment levofloksatsiny at some strains of Pseudomonas aeruginosa stability can develop quickly enough.

- other microorganisms: Chlamydia pneumoniae, Mycoplasma pneumoniae.

Pharmacokinetics. After intake levofloxacin is quickly and almost completely soaked up from the digestive tract (DT) with achievement of the maximum concentration in 1-2 h. Absolute bioavailability at oral administration makes about 99%. Linkng with proteins makes 24-38%.

Drug is well distributed in body tissues. In pulmonary fabric concentration exceeds concentration of plasma by 2-5 times. Levofloxacin is exposed to limited metabolism. The elimination half-life of a levofloksatsin averages 6-8 h. After intake about 87% of the accepted dose it is removed with urine in not changed look during 48 h. Less than 5% of the accepted dose to be removed with urine in the form of the metabolites which do not have pharmacological activity.

Indications to use:

- acute sinusitis;

- exacerbation of chronic bronchitis;

- community-acquired pneumonia;

- intrahospital pneumonia;

- the complicated and uncomplicated infections of skin and a hypodermic fatty tissue;

- chronic prostatitis;

- the complicated and uncomplicated infections of urinary tract;

- acute pyelonephritis.

Route of administration and doses:

Tablets of a levofloksatsin are appointed by the adult orally as it is specified in the table:

Infection	Dosage	Frequency (times/days)	Treatment duration * (days)
Community-acquired pneumonia	500 mg	1	7 - 10 days
Community-acquired pneumonia	750 mg	1	5 days
Intrahospital pneumonia	750 mg	1	7 - 10 days
The complicated infections of skin and soft tissues	750 mg	1	7 - 10 days
Exacerbation of chronic bronchitis	500 mg	1	7 days
Acute sinusitis	500 mg	1	7 - 10 days
Uncomplicated skin of infections and hypodermic fatty tissue	500 mg	1	7 - 10 days
Chronic prostatitis	500 mg	1	10 days
The complicated infections of urinary tract	250 mg	1	10 days
Acute pyelonephritis	250 mg	1	10 days
Uncomplicated infections of urinary tract	250 mg	1	3 days

Step therapy can be appointed at the discretion of the doctor.

Efficiency of this alternative mode was noted only at the infections caused penicillin - sensitive microorganisms of Streptococcus pneumoniae, Haemophilius influenzae, Mycoplasma pneumoniae and Chlamydia pneumoniae.

Pill should be taken entirely, without chewing, washing down with a large amount of water. A pill of a levofloksatsin can be taken irrespective of meal.

Patients with an impaired renal function. Clearance of creatinine from 20 to 49 ml/min. Initial dose of 500 mg/days; subsequent doses of 250 mg/days.

Clearance of creatinine <20 ml/min. Initial dose of 500 mg; subsequent doses of 250 mg / 48 hours

Patients with pyelonephritis and other complicated infections of an urinary system. Initial dose of 250 mg; subsequent doses of 250 mg / 48 hours.

Features of use:

The patients accepting hinolonovy drugs can have ruptures of sinews of a shoulder, hands, an Achilles tendon or other sinews which demands the traumatologic help and results in long disability. The risk of a rupture of sinews increases at the patients who are at the same time accepting corticosteroid drugs, especially at elderly. Levofloxacin has to be stopped to use if the patient notes pain, an inflammation or a rupture of a sinew. Patients have to refrain from a course of treatment until the diagnosis of a tendinitis or rupture of a sinew completely is not excluded.

Pseudomembranous colitis is observed at use of almost all antibacterial agents and can vary on weight from easy degree to life-threatening states. Therefore it is very important to establish the diagnosis at patients who have a diarrhea after purpose of antibacterial agents. Treatment by antibacterial agents changes flora of a large intestine and can lead to excessively rapid growth of clostridiums. The toxin produced by Clostridium difficile is primary reason "an antibiotic - the caused colitis". After establishment of the diagnosis of pseudomembranous colitis therapeutic measures have to be begun. Mild cases of pseudomembranous colitis usually take place only drug withdrawal. At moderate and heavy degree solutions for infusions and electrolytes, proteins and antibacterial drug clinical effective have to be appointed at the colitis caused by Clostridium difficile.

At the patients receiving hinolonovy drugs including levofloxacin, spasms and toxic psychoses were noted. As well as other hinolonovy drugs, levofloxacin it has to be applied with care at patients with suspicion or the known diseases of the central nervous system or with other risk factors which can contribute to attacks or lower a threshold of attacks (for example, cerebral arteriosclerosis, epilepsy, treatment by theophylline, a renal failure).

Patients with deficit glyukozo-6-fosfatdegidrogenazy should carry out purpose of drug with care in view of development of hemolitic reactions during treatment by hinolonovy drugs.

Correction of the mode of a dosage is necessary for patients with an impaired renal function.

In order to avoid development of a photosensitization by the patient it is recommended not to be exposed to power solar or artificial ultra-violet irradiation. At emergence of a photosensitization treatment has to be suspended.

Use for geriatric patients. Dose adjustment is not required from elderly patients with normal function of kidneys

Features of influence of medicine on ability to manage the vehicle or potentially dangerous mechanisms. Patients should be informed on the danger connected with control of automobiles, service of the mechanical equipment and other potentially dangerous types of activity.

Side effects:

- itch, erubescence, anaphylactic and anaphylactoid reactions, shock, syndrome;

- Stephens-Johnson, toxic epidermal necrolysis, exudative multiformny erythema;

- photosensitization;

- nausea, diarrhea, appetite loss, vomiting, abdominal pains, digestion disturbances;

- increase in level of bilirubin in blood serum, hepatitis;

- headache, dizziness, drowsiness, sleep disorder, concern, condition of fear, hallucination, depression;

- vision disorder, hearing, flavoring sensitivity and sense of smell;

- damage of sinews, joint and muscular pains, rupture of an Achilles tendon, muscular weakness, рабдомиолиз;

- increase in level of creatinine in blood serum;

- an eosinophilia, a leukopenia, a neutropenia, thrombocytopenia, the expressed agranulocytosis, hemolitic anemia, a pancytopenia.

Interaction with other medicines:

At simultaneous use Levozin with:

- antacids, i.e. polyvalent cationic drugs (magnesium / aluminum antacids, сукральфат, диданозин) or drugs calciferous, iron or zinc (chewable tablet and children's powder), absorption of a levofloksatsin can significantly decrease that will lead to the fact that levels in serum and urine will be much lower than expected. These drugs have to be accepted, at least, in two hours or in two hours after reception of a levofloksatsin

- theophylline, can lead to increase in concentration in serum of theophylline and to extension of time of semi-removal. It can end with the fact that the risk of the side effects connected with reception of theophylline will increase. If combined use cannot be avoided, then theophylline level in serum has to be controlled and suitable correction of a dose has to be carried out

- warfarin, the prothrombin time, the international normalized ratio (INR) (international normalized ratio-NMR) or other suitable anticoagulating tests has to be controlled. Patients also have to be under observation on a bleeding case

- cyclosporine, digoxin, probenetsidy, Cimetidinum, correction of a dose of a levofloksatsin or the listed drugs is not required

- non-steroidal anti-inflammatory drugs (except for acetylsalicylic acid), in a combination with very high dose of hinolonovy drugs, on preclinical trials, provoked spasms

- hypoglycemic drugs, glucose level in blood at patients has to be controlled carefully.

Contraindications:

- hypersensitivity to hinolonovy antimicrobic means and any other components of drug;

- epilepsy;

- pregnancy and period of a lactation;

- children's and teenage age up to 18 years.

Overdose:

Symptoms: confusion of consciousness, dizziness, disturbances of consciousness and attacks of spasms, nausea, damage of mucous membranes.

Treatment: there is no specific antidote. Symptomatic therapy. The hemodialysis or peritoneal dialysis is inefficient.

Storage conditions:

To store at a temperature not above 25 °C in the dry, protected from light place. To store in the place, unavailable to children! Period of storage 2 years. Not to apply after a period of storage.