Zanotsin - description of the drug, instructions for use, reviews

Pharmacological properties of the drug Zanotsin

Pharmacodynamics. Ofloxacin ((±)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido[1,2,3]-de-1 ,4-benzoxazine-6-carboxylic acid) is an antimicrobial agent of the fluoroquinolone group. The bactericidal effect of ofloxacin, like other fluorinated quinolones, is due to its ability to block the bacterial enzyme DNA gyrase. The antibacterial spectrum of the drug covers microorganisms resistant to penicillins, aminoglycosides, cephalosporins, as well as microorganisms with multiple resistance. Zanocin OD is a drug with prolonged release of the active substance - ofloxacin. The drug is taken 1 time per day. 1 tablet of Zanocin OD 400 or 800 mg, taken 1 time per day, provides a therapeutic effect equivalent to taking 2 regular tablets of ofloxacin 200 and 400 mg, respectively, taken 2 times a day. Zanocin in tablet form is active against a wide range of bacteria. Aerobic gram-negative bacteria: E. coli, Klebsiella spp., Salmonella spp., Proteus spp., Shigella spp., Yersinia spp., Enterobacter spp., Morganella morganii, Providencia spp., Vibrio spp., Citrobacter spp., Serratia spp. , Campylobacter spp., Pseudomonas aeruginosa, P. cepacia, Neisseria gonorrhoeae, N. meningitidis, Haemophilus influenzae, H. ducreyi, Acinetobacter spp., Moraxella catarrhalis, Gardnerella vaginalis, Pasteurella multocida, Helicobacter pylori. Brucella melitensis have varying sensitivity to the drug . Aerobic gram-positive bacteria: staphylococci, including penicillinase-producing and methicillin-resistant strains, streptococci (especially Streptococcus pneumoniae ), Listeria monocytogenes, Corynebacterium spp. Ofloxacin is more active than ciprofloxacin against Chlamydia trachomatis . Also active against Mycobacterium leprae and Mycobacterium tuberculosis and some other Mycobacterium . There are reports of the synergistic effect of ofloxacin and rifabutin against M. leprae . Treponema pallidum , viruses, fungi and protozoa are not susceptible to ofloxacin. Pharmacokinetics. The drug is quickly and almost completely absorbed in the digestive tract. The absolute bioavailability of ofloxacin is 96% after oral administration. Plasma concentrations reach 3–4 mcg/ml 1–2 hours after administration of a dose of 400 mg. Eating food does not reduce the absorption of ofloxacin, but may slightly slow down the rate of absorption. The half-life of the drug is 5–8 hours. Since ofloxacin is mainly excreted by the kidneys, its pharmacokinetics changes significantly in patients with impaired renal function (creatinine clearance ≤50 ml/min) and therefore they require dose adjustment. Hemodialysis slightly reduces the plasma concentration of ofloxacin. Ofloxacin is widely distributed in tissues and body fluids, including CSF; volume of distribution - from 1 to 2.5 l/kg. About 25% of the drug binds to blood plasma proteins. Ofloxacin crosses the placenta and into breast milk. Reaches high concentrations in most tissues and biological fluids of the body, including ascitic fluid, bile, saliva, bronchial secretions, gallbladder, lungs, prostate gland, bone tissue. Ofloxacin has a pyridobenzoxazine ring, which reduces the rate of metabolism of the parent compound. The drug is primarily excreted unchanged in the urine, with 65–80% excreted within 24–48 hours. Less than 5% of the dose is excreted in the urine as dimethyl or N-oxide metabolites. 4–8% of the dose taken is excreted in the feces. A small amount of ofloxacin is excreted in the bile. There were no differences in the volume of distribution of the drug in elderly people; the drug is excreted from the body primarily by the kidneys in unchanged form, although in a smaller volume. Since ofloxacin is excreted primarily by the kidneys, and elderly patients are more likely to have impaired renal function, the dose of the drug is adjusted if renal function is impaired, as recommended for all patients. The pharmacokinetic features of Zanocin OD facilitate its systemic use. Food does not affect the degree of absorption of the drug. Extended-release ofloxacin tablets are absorbed more quickly and have a greater degree of absorption compared to regular ofloxacin tablets taken 2 times a day. After oral administration of Zanocin OD 400 mg, the maximum concentration of ofloxacin in the blood plasma is achieved after 6.778 ± 3.154 hours and is 1.9088 μg/ml ± 0.46588 μg/ml. AUC0–1 is 21.9907±4.60537 µg•g/ml. After oral administration of Zanocin OD at a dose of 800 mg, the maximum concentration of the drug in the blood plasma is reached after 7.792 ± 3.0357 hours and is 5.22 ± 1.24 μg/ml. The AUC0-t level is 55.64±11.72 µg•g/ml. In vitro , the drug binds to plasma proteins by approximately 32%. The equilibrium concentration of the drug in the blood plasma is achieved after 4 doses of the drug, and the AUC is approximately 40% greater than that after a single dose. The elimination of ofloxacin from the body is two-phase. With repeated oral administration, the half-life of the drug is about 4-5 hours and 20-25 hours. Total clearance and volume of distribution are approximately similar for single or repeated use.

Release form and composition

The drug is available in the form:

• Zanocin tablets 200 mg;
• Long-acting tablets Zanocin OD 400 mg and 800 mg;
• Solution for infusion Zanocin 2 mg/ml.

The active ingredient of the drug is ofloxacin.

Tablets contain as excipients:

• Lactose:
• Microcrystalline cellulose;
• Corn starch;
• Polysorbate 80;
• Magnesium stearate;
• Purified talc;
• Sodium starch glycolate;
• Anhydrous colloidal silicon dioxide.

Shell composition: purified talc, macrogol 400, hydroxypropyl methylcellulose, titanium dioxide E171.

Extended-release tablets contain as excipients:

• Sodium bicarbonate;
• Crospovidone;
• Purified water;
• Magnesium stearate;
• Xanthan gum;
• Sodium alginate;
• Hydroxypropyl methylcellulose;
• Carbomer;
• Anhydrous colloidal silicon dioxide;
• Lactose monohydrate (400 mg tablets).

Shell composition: isopropyl alcohol, purified water, dyes Opadry 31B 58910 white and Opacode-1-17734 black.

Excipients included in the solution:

• Sodium chloride;
• Disodium edeate;
• Water for injections;
• Hydrochloric acid;
• Sodium hydroxide.

Indications for use of the drug Zanotsin

Infections caused by microorganisms sensitive to the drug:

• genitourinary system - acute and chronic pyelonephritis, prostatitis, epididymitis, surgical urinary tract infections, infections caused by Pseudomonas aeruginosa and other multidrug-resistant microorganisms, nosocomial urinary tract infections, acute uncomplicated urethral and cervical gonorrhea caused by Neisseria gonorrhoeae , mixed urethral and cervical infections caused by Chlamidia trachomatis and Neisseria gonorrhoeae , uncomplicated cystitis caused by Citrobacter diversus, Enterobacter aerogenes, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis or Pseudomonas aeruginosa , complicated and recurrent urinary tract infections caused by Klebsiella pneumoniae, Proteus mirabilis, Citrobacter diversus (1) or P seudomonas aeruginosa 1, non-gonococcal urethritis and cervicitis caused by C. trachomatis ;
• respiratory tract - pleurisy, pleural empyema, infected bronchiectasis, lung abscess, cystic fibrosis, exacerbation of chronic bronchitis caused by Haemophilus influenzae or Streptococus pneumoniae , community-acquired pneumonia caused by Haemophilus influenzae or Streptococus pneumoniae;
• ENT organs, including otitis media, sinusitis, tonsillitis, etc.;
• uncomplicated infections of the skin and subcutaneous tissues caused by methicillin-sensitive microorganisms Staphylococcus aureus, Streptococcus pyogenes, Proteus mirabilis;
• acute inflammatory diseases of the pelvic organs (including severe infectious diseases) caused by Chlamydia trachomatis and/or Neisseria gonorrhoeae ;
• sexually transmitted diseases - infections of the urethra, cervix, rectum, pharynx caused by penicillin-resistant gonococci, chlamydia and other microorganisms;
• other infectious diseases - typhoid fever, salmonellosis, shigellosis, abdominal organs and biliary tract;
• in the complex treatment of septicemia, endocarditis, osteomyelitis, mycobacterial infections, leprosy, prevention of infectious complications in patients with immunodeficiency or neutropenia;
• perioperative prevention or postoperative treatment of surgical infections.

1 Although the treatment of infectious diseases caused by these microorganisms (for this organ system) has demonstrated clinically significant results, the effectiveness of therapy has been studied in fewer than 10 patients.

To prevent the development of drug-resistant microorganisms and maintain the effectiveness of ofloxacin and other antibacterial drugs, ofloxacin is prescribed for the treatment and prevention only of infectious diseases caused (confirmed or most likely) by microorganisms sensitive to the drug. When the culture and sensitivity of the microorganism are established, the appropriate selective or combined antibacterial therapy is determined. In the absence of the above information, as well as epidemiological and sensitivity data, the drug can be prescribed as empirical therapy. The culture and sensitivity of the pathogen should be determined before starting treatment. Treatment with ofloxacin can be started before test results are obtained, and therapy is continued after results are obtained. As with other drugs in this series, some strains of Pseudomonas aeruginosa can quickly become resistant to the action of ofloxacin. Periodically during treatment, a culture should be isolated and the sensitivity of the pathogen should be determined (monitoring the effectiveness of treatment with an antibacterial drug and the possible development of bacterial resistance).

Zanotsin od 400 mg 10 pcs. extended-release film-coated tablets

pharmachologic effect

Bactericidal, broad spectrum antibacterial.

Composition and release form Zanotsin od 400 mg 10 pcs. extended-release film-coated tablets

Film-coated tablets, prolonged action - 1 tablet:

• active ingredients: ofloxacin - 400 mg;
• excipients: crospovidone; sodium bicarbonate; hypromellose; purified water*; sodium alginate; xanthan gum; carbopol; lactose monohydrate; magnesium stearate; colloidal silicon dioxide;
• film shell: Opadry white dye 31B58910 (hypromellose, lactose monohydrate, titanium dioxide, macrogol), purified water*; isopropanol*;
• ink for inscription: Opacode S-1-17823 black (shellac 45% (20% esterified) in SD-45 alcohol, black iron oxide dye, n-butanol, propylene glycol, methanol, isopropanol, ammonium hydroxide 28%); isopropanol*.

* evaporates during the production process.

There are 5 pcs in a blister; There are 1 or 2 blisters in a cardboard box.

Description of the dosage form

Zanocin® OD 400 mg are biconvex oval-shaped, film-coated tablets, almost white in color with the inscription ZNT/400 and OD in black edible ink on one side and smooth on the other.

Directions for use and doses

Inside, after eating, without chewing or breaking, with a sufficient amount of liquid.

Recommended dosages of Zanocin® OD for adults

Dosage regimen in patients with impaired renal function: After the initial normal dose, the dosage regimen should be adjusted according to the following schedule:

If only the plasma creatinine concentration is known, the creatinine clearance is calculated using the following formula:

• men - Cl creatinine (ml/min) = Weight (kg) x (140−age) / 72 x plasma creatinine concentration (mg%);
• women - 0.85 x the value calculated for men.

In patients with impaired liver function, as well as in cases of cirrhosis or ascites, the daily dose of 400 mg should not be exceeded (a slight decrease in the rate of elimination of ofloxacin may be observed).

Use in elderly patients: There are no restrictions on the use of fluoroquinolones. However, in patients with reduced renal excretory function, it is necessary to adjust the dosage regimen of the drug.

Pharmacodynamics

A fluorine derivative of carboxyquinolone. Suppresses the action of the enzyme topoisomerase II (DNA gyrase) in bacterial cells. Topoisomerases are responsible for introducing negative nucleotide rings into DNA. Fluoroquinolones reduce the introduction of negative rings into DNA and cause rapid disruption of DNA replication. Characterized by a wide spectrum of antibacterial action. Active against the vast majority of the following microorganisms:

• aerobic gram-positive microorganisms: Staphylococcus aureus (methicillin-sensitive strains), Streptococcus pneumoniae (penicillin-sensitive strains), Streptococcus pyogenes;
• aerobic gram-negative microorganisms: Citrobacter (diversus) koseri, Enterobacter aerogenes, Escherichia coli, Haemophilus influenzae, Klebsiella pneumoniae, Neisseria gonorrhoeae, Proteus mirabilis, Pseudomonas aeruginosa;
• other microorganisms: Chlamydia trachomatis.

In vitro MIC determined to be 2 µg/ml or less for most (90%) strains of the following microorganisms:

• aerobic gram-positive microorganisms: Staphylococcus epidermidis (methicillin-sensitive strains); Streptococcus pneumoniae (penicillin-resistant strains), Staphylococcus saprophyticus;
• aerobic gram-negative microorganisms: Acinetobacter calcoaceticus, Bordetella pertussis, Citrobacter freundii, Enterobacter cloacae, Haemophilus ducreyi, Klebsiella oxytoca, Moraxella catarrhalis, Morganella morganii, Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Serratia marcescens;
• anaerobic microorganisms: Clostridium perfringens;
• other microorganisms: Chlamydia pneumoniae, Gardnerella vaginalis, Legionella pneumophila, Mycobacterium tuberculosis, Mycoplasma hominis, Mycoplasma pneumoniae, Ureaplasma urealyticum.

Has no activity against Treponema pallidum. Many strains of Streptococcus and Enterococcus, as well as anaerobic microorganisms, are resistant to ofloxacin.

Pharmacokinetics

Zanocin® OD is capable of releasing ofloxacin for a long time, which makes the use of the drug - once a day - more convenient. A single use of Zanocin® OD tablets 400 and 800 mg is equivalent in the amount of released ofloxacin to the use of conventional ofloxacin tablets 200 and 400 mg twice a day.

When taken orally, ofloxacin is rapidly absorbed (absorption - 95%). Bioavailability - over 96%. After a single dose of 400 or 800 mg, Cmax in plasma is 2.09 ± 0.46 and 5.15 ± 1.07 μg/ml, respectively, and is achieved within 6–8 hours.

The apparent volume of distribution is 100 l. Distributed into cells (leukocytes, alveolar macrophages), skin, soft tissues, bones, abdominal and pelvic organs, including the uterus, ovaries, prostate, respiratory system, including lungs, urine, saliva, bile, prostate secretions , penetrates well through the BBB into the cerebrospinal fluid (14–60%), through the placental barrier, and is secreted into breast milk.

Plasma protein binding - 25%, T1/2 when taking regular tablets - 6-8 hours. Metabolized in the liver (about 5%).

Excreted mainly through the kidneys: about 70–90% unchanged in the urine, less than 5% in the form of metabolites, incl. dimethyl- or N-oxidofloxacin.

Ofloxacin clearance is reduced in patients with impaired renal function (Cl creatinine ≤50 ml/min); in such patients, adjustment of the dosage regimen is necessary.

Hemodialysis removes 10–30% of the drug.

Indications for use Zanotsin od 400 mg 10 pcs. extended-release film-coated tablets

• infections of the lower respiratory tract, including pneumonia caused by Haemophilus influenzae and Streptococcus pneumoniae, exacerbation of chronic bronchitis;
• infections of the upper and lower urinary system;
• acute uncomplicated or complicated urethral or cervical form of gonorrhea;
• urethritis and cervicitis caused by Chlamydia trachomatis;
• mixed urethral and cervical infections caused by Chlamydia trachomatis and Neisseria gonorrhoeae;
• uncomplicated skin and soft tissue infections;
• acute inflammatory diseases of the pelvic organs (including severe infections). Prostatitis of any etiology;
• tuberculosis (as part of complex therapy, as a second-line drug).

Contraindications

• hypersensitivity to ofloxacin or fluoroquinolone drugs;
• deficiency of glucose-6-phosphate dehydrogenase;
• epilepsy (including history);
• decreased seizure threshold (including after TBI, stroke or inflammatory processes in the central nervous system);
• pregnancy;
• breastfeeding period;
• age up to 18 years (skeletal growth is not yet complete);
• Creatinine Cl

Application Zanotsin od 400 mg 10 pcs. extended-release film-coated tablets during pregnancy and lactation

Contraindicated. Data on the use of the drug in pregnant women and nursing mothers are insufficient to predict its safety in these groups.

special instructions

Use with caution in patients with CNS diseases in the past, incl. a history of cerebrovascular accidents, atherosclerosis of cerebral vessels, organic lesions of the central nervous system; for chronic renal failure.

Patients with hypersensitivity to any fluoroquinolone or any quinolone derivatives may also be sensitive to ofloxacin.

Phototoxicity reactions have been observed in some patients receiving fluoroquinolones. During treatment, prolonged exposure to direct sunlight should be avoided. If signs of phototoxicity appear, you must stop taking the drug.

When used together with antidiabetic agents, careful monitoring of plasma glucose concentrations is recommended.

It is not the drug of choice for pneumonia caused by pneumococci.

Not indicated for the treatment of acute tonsillitis.

Rarely, tendinitis can lead to tendon rupture (mostly the Achilles tendon), especially in older patients. If signs of tendinitis occur, you should immediately stop treatment, immobilize the Achilles tendon and consult an orthopedist.

Women taking ofloxacin are not recommended to use Tampax tampons due to the increased risk of developing thrush.

During treatment, the course of myasthenia gravis may worsen and attacks of porphyria may increase in predisposed patients.

May lead to false negative results in the bacteriological diagnosis of tuberculosis (prevents the isolation of Mycobacterium tuberculosis).

False-positive results are possible when determining opiates and porphyrins in urine.

In patients with impaired liver and kidney function, monitoring of drug concentrations in plasma is necessary. In case of severe renal and liver failure, the risk of developing toxic effects increases (dose reduction is required).

When using almost all antibacterial drugs, including ofloxacin, the development of pseudomembranous colitis of varying severity, from mild to life-threatening, is possible. Therefore, first of all, it is necessary to exclude the possibility of this disease in patients with diarrhea that occurs during the use of antibacterial drugs. For pseudomembranous colitis, confirmed colonoscopically and/or histologically, the administration of vancomycin and metronidazole orally is indicated.

During the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions, and you should not drink alcohol.

Overdose

An overdose may lead to side effects.

There is no specific antidote for ofloxacin.

Treatment: symptomatic, including the following measures - induction of vomiting, gastric lavage, maintaining adequate hydration of the body, and maintenance therapy.

It is not removed by hemodialysis or peritoneal dialysis.

Side effects Zanotsin od 400 mg 10 pcs. extended-release film-coated tablets

The incidence of side effects was assessed as follows: often - more than 1 case per 100 prescriptions; uncommon - less than 1 case per 100 prescriptions; rarely - less than 1 case per 1000 prescriptions.

From the gastrointestinal tract and liver: often - nausea, vomiting, diarrhea (may be a symptom of enterocolitis, in some cases - hemorrhagic), abdominal pain, gastralgia, flatulence; uncommon - loss of appetite, increased levels of liver transaminases and/or bilirubin; rarely - the development of cholestatic jaundice, hepatitis or severe liver dysfunction is possible; pseudomembranous colitis (most often caused by Clostridium difficile) - in this case, you should immediately stop taking the drug. Drugs that reduce intestinal motility should not be used.

From the nervous system and sensory organs: often - headache, dizziness, feeling tired; uncommon - uncertainty of movements, convulsions, psychomotor agitation, phobias, increased intracranial pressure, confusion, imbalance, nightmares, anxiety, depression, hallucinations and psychotic reactions, insomnia, unsteady gait and tremor (as a result of impaired muscle coordination), neuropathy , a feeling of numbness and paresthesia or hyperesthesia, impaired vision, color vision, diplopia, impaired taste and olfactory perception (in rare cases, temporary loss of function); rarely - hearing loss (including hearing loss). If these reactions are observed in patients after taking the first dose of ofloxacin, therapy should be discontinued immediately.

From the cardiovascular system: tachycardia and temporary decrease in blood pressure; infrequently - circulatory collapse (as a result of a rapid decrease in blood pressure).

From the hematopoietic system: rarely - anemia, leukopenia (including agranulocytosis), thrombocytopenia, pancytopenia, possible development of hemolytic and aplastic anemia.

From the genitourinary system (kidneys): infrequently - impaired renal function;

rarely - acute interstitial nephritis or acute renal failure with a progressive increase in serum creatinine concentration, increased urea content.

Allergic reactions and effects on the skin: often - skin rash, itching; uncommon - photodermatitis, possible development of immediate and delayed allergic reactions, usually including skin manifestations (for example, exudative erythema, Stevens-Johnson syndrome, Lyell's syndrome and vasculitis). In rare cases, other signs of anaphylaxis may develop: tachycardia, fever, allergic pneumonitis, allergic nephritis, Quincke's edema, bronchospasm, dyspnea, shock, angioedema, vasculitis-like reactions, eosinophilia (use of the drug should be stopped immediately); rarely - eosinophilic pneumonia.

From the musculoskeletal system: rarely - tendonitis, pain in muscles and joints (in rare cases, may be a sign of rhabdomyolysis), tendovaginitis, tendon rupture. Even if there are minor signs of tendon inflammation, you should immediately stop taking the drug.

Other: rarely - superinfection, hyper- or hypoglycemia, weakness, intestinal dysbiosis, vaginitis.

In some patients (with special predisposition), the use of ofloxacin may provoke an attack of porphyria.

With the exception of very rare cases (including disturbances of taste, smell and hearing), side effects are temporary and disappear after stopping use of the drug.

Changes in laboratory parameters: increase in enzyme activity indicators - ALP, AST, ALT, LDH.

Drug interactions

Antacid drugs, sucralfate, metal cations, multivitamins reduce the absorption of fluoroquinolones (simultaneous use should be avoided). Food products, antacids containing Al3+, Ca2+, Mg2+ or iron salts reduce the absorption of ofloxacin, forming insoluble complexes (the interval between doses of these drugs should be at least 2 hours).

NSAIDs increase the side effects of fluoroquinolones on the central nervous system.

Most fluoroquinolones inhibit the activity of cytochrome P450 to varying degrees, and when used together with fluoroquinolones, an increase in T1/2 of drugs that are also metabolized by cytochrome P450 (for example, cyclosporine, theophylline/methylxanthine, warfarin, etc.) is possible.

When cyclosporine was co-administered with some fluoroquinolones, an increase in cyclosporine plasma concentrations was observed. Drug interaction reactions between cyclosporine and ofloxacin have not been studied.

Reduces the clearance of theophylline by 25% (with simultaneous use, the dose of theophylline should be reduced).

Fluoroquinolones enhance the effects of warfarin and its derivatives, therefore, when used together, incl. and with other vitamin K antagonists, blood coagulation parameters should be carefully monitored.

Cimetidine alters the elimination rate of some fluoroquinolones, resulting in a significant increase in AUC.

In patients receiving fluoroquinolones and antidiabetic drugs simultaneously, both hypo- and hyperglycemia are observed.

When prescribed with glucocorticoids, the risk of tendon rupture increases, especially in the elderly.

When used together with drugs that alkalinize urine (carbonic anhydrase inhibitors, citrates, sodium bicarbonate), the likelihood of crystalluria and nephrotoxic effects increases.

Food may slow down absorption, but does not have a significant effect on bioavailability: Tmax increases, but Cmax and AUC of the drug do not change (the interval between doses should be at least 2 hours).

Compatible with the following infusion solutions: 0.9% NaCl solution, Ringer's solution, 5% fructose solution, 5% dextrose solution. Do not mix with heparin (risk of precipitation).

Use of the drug Zanotsin

Zanocin: The dose depends on the type of microorganism and the severity of the infection, age, body weight and kidney function of the patient. In most cases, the course of treatment is 7-10 days, treatment must be continued for another 2-3 days after the symptoms of the infection have resolved. For severe and complicated infections, therapy can be extended. The dose of the drug is 200–400 mg/day in 2 divided doses. A dose of 400 mg (2 tablets) can be taken at one time, preferably in the morning. A single dose of 400 mg can be recommended for acute, fresh, uncomplicated gonorrhea. A dose of 400 mg is recommended by WHO for the treatment of leprosy. A dose of 200 mg (100 ml) is administered intravenously at a rate of 400 mg/hour, 200–400 mg 2 times a day. If renal function is impaired, the dose is set taking into account the severity of renal failure and creatinine clearance. The recommended initial dose of the drug for impaired renal function is 200 mg; in the future, the dose is adjusted taking into account creatinine clearance: at a level of 50–20 ml/min - at the usual dose every 24 hours; less than 20 ml/min - 100 mg (1/2 t tablet) every 24 hours. It is not recommended to continue treatment with the drug for more than 2 months. Zanocin OD is taken 1 time per day along with food. The daily dose is set according to the table (see below). These recommendations apply to patients with normal renal function (creatinine clearance 50 ml/min). The tablets are swallowed whole.

1 The causative agent of the disease has been identified.

If renal function is impaired, the dose is adjusted when creatinine clearance is ≤50 ml/min. After the usual initial dose when using Zanocin OD 400 mg, the dose is adjusted as follows:

When using Zanocin OD 800 mg, there is currently no sufficient data regarding changes in recommended doses for patients with creatinine clearance ≤50 ml/min. If only the plasma creatinine concentration is known, creatinine clearance can be determined using the formula:

• for men:

• for women: creatinine clearance (ml/min) = 0.85 the value of creatinine clearance for men.

Plasma creatinine concentrations are monitored to determine the status of renal function. Liver dysfunction/cirrhosis. Ofloxacin excretion may be reduced in severe liver dysfunction (liver cirrhosis with or without ascites), so the maximum dose of ofloxacin should not be exceeded - 400 mg per day. In elderly patients, there is no need to adjust the dose, except in cases where renal or hepatic dysfunction is observed.

Drug interactions Zanotsin

• Zanocin increases plasma levels of glibenclamide and reduces the clearance of theophylline;
• When using Zanocin together with cimetidine, methotrexate or furosemide, the level of ofloxacin in the body increases;
• When taking vitamin K, blood clotting should be monitored;
• With the simultaneous use of Zanocin and non-steroidal anti-inflammatory drugs, toxic reactions sometimes occur;
• Do not prescribe Zanotin together with GCS drugs (tendon rupture is possible);
• While taking the drug, it is not recommended to consume foods that contain iron, Al3+, Ca2+, Mg2+;
• It is acceptable to mix Zanocin with a solution of sodium chlorine, fructose, Ringer and dextrose.

Side effects of the drug Zanocin

As a result of clinical studies, the most commonly observed events with repeated use of ofloxacin were: nausea (3%), headache (1%), dizziness (1%), diarrhea (1%), vomiting (1%), rash (1%), itching skin (1%), itching of the external genitalia in women (1%), vaginitis (1%), dysgeusia (1%). In clinical studies, the most common side effects that occurred regardless of the duration of use of the drug were nausea (10%), headache (9%), dyssomnia (7%), itching of the external genitalia in women (6%), dizziness (5). %), vaginitis (5%), diarrhea (4%), vomiting (4%). In clinical studies, the most common side effects, which occurred regardless of the duration of drug use and were observed in 1-3% of patients, were abdominal pain and colic, chest pain, decreased appetite, dry lips, dysgeusia, fatigue, flatulence, and mental disorders. Gastrointestinal tract, nervousness, pharyngitis, itching, fever, rash, dyssomnia, drowsiness, body pain, vaginal discharge, blurred vision, constipation. Side effects that were noted in clinical studies in less than 1% of cases, regardless of the duration of use of the drug: general disorders: asthenia, chilliness, malaise, pain in the extremities, nosebleeds; from the cardiovascular system: cardiac arrest, edema, hypertension, arterial hypotension, feeling of increased heartbeat, vasodilation; from the gastrointestinal tract: dyspepsia; from the genitourinary system: sensation of heat, irritation, pain and rash in the genital area in women, dysmenorrhea, metrorrhagia; from the musculoskeletal system: arthralgia, myalgia; from the central nervous system: convulsions, anxiety, impaired cognitive function, depression, abnormal dreams, euphoria, hallucinations, paresthesia, disturbances of consciousness, vertigo, tremor; from the metabolic side: thirst, weight loss; from the respiratory system: respiratory arrest, cough, rhinorrhea; allergic and skin reactions: angioedema, hyperhidrosis, urticarial rash, vasculitis; from the senses: decreased hearing acuity, ringing in the ears, photophobia; from the urinary system: dysuria, frequent urination, urinary retention. Changes in laboratory parameters were detected in ≥1% of patients with repeated use of ofloxacin. These changes are caused both by taking the drug and by the underlying disease: from the blood system: anemia, leukopenia, leukocytosis, neutropenia, neutrophilia, band neutrophyllosis, lymphocytopenia, eosinophilia, lymphocytosis, thrombocytopenia, thrombocytosis, increased ESR; from the hepatobiliary system: increased levels of alkaline phosphatase, AST, ALT; laboratory parameters: hyperglycemia, hypoglycemia, hypercreatininemia, increased urea levels, glucosuria, proteinuria, alkalinuria, hyposthenuria, hematuria, pyuria. Post-marketing experience Additional side effects that occurred regardless of the duration of use of the drug were noted as a result of marketing studies of quinolones, including ofloxacin. From the cardiovascular system: cerebral thrombosis, pulmonary edema, tachycardia, arterial hypotension/shock, fainting, ventricular tachycardia of the pirouette type. From the endocrine system and metabolism: hyper- or hypoglycemia, especially in patients with diabetes using insulin therapy or oral hypoglycemic drugs. From the gastrointestinal tract: hepatonecrosis, jaundice (cholestatic or hepatocellular), hepatitis, intestinal perforation, liver failure (including fatal cases), pseudomembranous colitis (symptoms of pseudomembranous colitis can occur both during and after the end of antibacterial therapy), bleeding from the gastrointestinal tract, hiccups, soreness of the oral mucosa, heartburn. From the genitourinary system: vaginal candidiasis. From the blood system: anemia (including hemolytic and aplastic), hemorrhage, pancytopenia, agranulocytosis, leukopenia, reversible depression of bone marrow function, thrombocytopenia, thrombocytopenic purpura, petechiae, subcutaneous hemorrhage/bruising. From the musculoskeletal system: tendinitis, tendon ruptures, weakness, acute necrosis of skeletal muscles. From the central nervous system: nightmares, suicidal thoughts or actions, disorientation, psychotic reactions, paranoia, phobia, agitation, anxiety, aggressiveness/hostility, mania, emotional lability, peripheral neuropathy, ataxia, loss of coordination, possible exacerbation of myasthenia gravis and extrapyramidal disorders; dysphasia, dizziness. From the respiratory system: dyspnea, bronchospasm, allergic pneumonitis, wheezing. Allergic and skin reactions: anaphylactic/anaphylactoid reaction/shock, purpura, serum sickness, erythema multimorpha/Stevens-Johnson syndrome, erythema nodosum, exfoliative dermatitis, hyperpigmentation, toxic epidermal necrolysis, conjunctivitis, photosensitivity/phototoxicity reactions, vesiculobullous rash. From the senses: diplopia, nystagmus, blurred vision, dysgeusia, impaired smell, hearing and balance, which usually disappear after stopping the drug. From the urinary system: anuria, polyuria, kidney stones, renal failure, interstitial nephritis, hematuria. Laboratory indicators: prolongation of prothrombin time, acidosis, hypertriglyceridemia, increased cholesterol, potassium, liver function tests, including gamma-glutamyl transpeptidase, LDH, bilirubin, albuminuria, candiduria. In clinical trials, repeated use of quinolones has been associated with ophthalmic abnormalities, including cataracts and pinpoint opacities of the lens. The connection between taking the drug and the appearance of these disorders has not yet been established. Crystalluria and cylindruria have been reported with other quinolones.

Reviews about Zanotsin

Quinolones are widely used in the treatment of gynecological and urological diseases, as evidenced by reviews. Many patients were prescribed this drug for the treatment of salpingo-oophoritis , perimetritis , metroendometritis on an outpatient basis. The treatment was highly effective and rational, since according to gynecologists, ofloxacin is the most effective drug for the treatment of these diseases. The treatment was well tolerated. Only a few experienced minor nausea, anorexia and diarrhea . Manifestations of photosensitivity during treatment in the summer.

Ofloxacin is excreted in the urine by the kidneys, which makes it possible to successfully treat urological diseases of an inflammatory nature. Already on days 5-7 bacteriuria and overall health improved. The treatment was carried out with a low level of side effects.

Norbactin and Zanocin are effective against pseudomonas and Escherichia coli , which makes it possible to use these drugs for the treatment of purulent-inflammatory diseases. The drug Zanocin, in addition to a wide spectrum of bactericidal action has an immunomodulatory effect , which makes it the drug of choice for the treatment of diseases in patients with weakened immune systems ( AIDS , cancer patients ).

Special instructions for the use of the drug Zanotsin

Convulsions, increased intracranial pressure and toxic psychosis have been reported in patients taking quinolone drugs, including ofloxacin. Quinolones, including ofloxacin, may also have a stimulant effect on the central nervous system, which may lead to tremor, restlessness/agitation, nervousness/anxiety, dizziness, confusion, hallucinations, paranoia and depression, nightmares, dyssomnia, and rarely, suicidal thoughts and actions. Such reactions may occur after taking the first dose. If such symptoms occur in patients taking ofloxacin, the drug should be discontinued and appropriate measures taken. Dyssomnia is the most common disorder with ofloxacin than with other quinolone drugs. Like all quinolones, ofloxacin is used with caution in cases of established/suspected disorders of the nervous system, since these drugs can provoke convulsions or a decrease in the threshold of convulsive readiness (severe cerebral atherosclerosis, epilepsy), or with other risk factors (on the background of continuous therapy, impaired renal function), which can provoke seizures or a decrease in the seizure threshold. Severe and fatal (rare) hypersensitivity reactions and/or anaphylactic reactions have been reported in patients receiving quinolones, including ofloxacin. Such reactions were often noted after taking the first dose. Some reactions have been accompanied by cardiovascular collapse, hypotension/shock, seizures, loss of consciousness, tinnitus, angioedema (including swelling of the tongue, larynx, pharynx or face), airway obstruction (including bronchospasm, dyspnea and acute respiratory failure), dyspnea, urticarial rash, itching and other severe skin reactions. The drug is immediately discontinued at the first sign of skin rash or other hypersensitivity reactions. In severe acute hypersensitivity reactions, epinephrine therapy and other resuscitation measures may be necessary, including oxygen therapy, fluid resuscitation, antihistamines, corticosteroids, vasopressor amines, and airway management. Other severe and sometimes fatal cases associated with hypersensitivity reactions or unknown etiologies have been reported rarely during therapy with quinolones, including ofloxacin. Such cases could be severe and generally occurred after repeated doses of the drug. The drug is immediately discontinued at the first manifestation of a skin rash, jaundice or other symptoms of hypersensitivity and symptomatic therapy is prescribed. During treatment with quinolones, including ofloxacin, isolated cases of sensory or sensorimotor neuronal polyneuropathy involving small and/or large neurons, manifested by paresthesia, hypoesthesia, dysesthesia and weakness, have been reported. To prevent the development of irreversible conditions, treatment with ofloxacin is discontinued if symptoms of neuropathy (pain, burning sensation, tingling, numbness and/or weakness) or other disturbances in tactile, pain, temperature, positional, vibration sensitivity develop. Diarrhea associated with Clostridium difficile with almost all antibacterial agents, including ofloxacin; The disease can range from mild diarrhea to fatal colitis. Treatment with antibacterial drugs affects the normal intestinal microflora and leads to increased growth of Clostridium difficile. Clostridium difficile- associated diarrhea should be considered in all cases of diarrhea occurring after taking antibacterial drugs. Clostridium difficile- associated diarrhea have been reported 2 months after stopping antibiotic use. If diarrhea associated with Clostridium difficile , antibacterial drugs whose action is not directed at Clostridium difficile are discontinued. Tendon ruptures of the upper (shoulder tendon), lower (Achilles tendon), and other tendons requiring surgery or causing long-term disability have been reported in patients treated with quinolones, including ofloxacin. Post-marketing studies indicate that the risk of musculoskeletal disorders increases with the combined use of GCS, especially in elderly patients. Ofloxacin is discontinued if pain, inflammation or tendon rupture occurs. The patient is recommended to rest in bed and limit movement until tendonitis or tendon rupture is confirmed/excluded. Tendon ruptures can occur both during and after treatment with quinolone drugs, including ofloxacin. Ofloxacin is not effective against syphilis. Antibacterial therapy, prescribed in high doses and for a short period for the treatment of gonorrhea, can mask or delay the manifestations of the incubation period of syphilis. All patients with gonorrhea undergo a serologic test for syphilis during the diagnostic workup. When using ofloxacin to treat gonorrhea, perform a serological test for syphilis 3 months after treatment and prescribe appropriate antibiotic therapy if the test result is positive. If ofloxacin is prescribed in the absence of data regarding the confirmed or most likely causative agent of the disease, or for prophylactic treatment, the benefit to the patient is unlikely; this increases the risk of developing bacterial resistance to the drug. To prevent the development of crystalluria, ensure adequate fluid intake. After taking quinolone antibacterial drugs and subsequent exposure to solar or ultraviolet irradiation, moderate to severe photosensitivity/phototoxicity reactions may occur, which are manifested by sunburn (redness, erythema, exudation, vesicles, edema) on exposed skin areas (face, anterior neck , extensor surface of the forearm, dorsal surface of the upper limbs). Therefore, during the treatment period, sun exposure should be avoided. Some quinolones, including ofloxacin, may cause prolongation of the QT on the ECG and rarely arrhythmia. Isolated cases of torsade de pointes (TdP) in patients taking quinolones, including ofloxacin, have been reported during post-marketing studies. Ofloxacin should not be prescribed in cases of established prolongation of the QT , uncorrected hypokalemia, and in patients taking class IA (quinidine, procainamide) or class III antiarrhythmic drugs (amiodarone, sotalol). During pregnancy and breastfeeding . Reliable and controlled studies of the use of the drug during pregnancy have not been conducted. The safety and effectiveness of the use of ofloxacin during pregnancy have not been established, therefore the drug is not prescribed during this period. When taking ofloxacin during breastfeeding in a single dose of 200 mg, the level of drug concentration in breast milk corresponded to a similar level in blood plasma. Since there is a risk of severe adverse reactions in infants, breastfeeding should be stopped or the drug should be discontinued (depending on the clinical significance of taking the drug for the woman). Children . Ofloxacin is not indicated for the treatment of children and adolescents under 18 years of age. The ability to influence reaction speed when driving vehicles or working with machinery. Since isolated cases of drowsiness, dizziness and visual impairment associated with taking the drug have been reported, you should not drive or operate other machinery during the treatment period.

Contraindications

The use of Zanotsin is contraindicated in:

• Hypersensitivity to ofloxacin or any other fluoroquinolone drug;
• Hypersensitivity to any auxiliary component of the drug;
• Epilepsy, including a history;
• Reducing the seizure threshold, including after inflammatory processes in the central nervous system, traumatic brain injury or stroke;
• Tendinitis, including a history;
• Uncorrectable hypokalemia;
• Increased QT interval on ECG;
• Glucose-6-phosphate dehydrogenase deficiency;
• A history of indications of tendon damage due to the use of fluoroquinolones.

Also, Zanotin is not prescribed:

• Children and teenagers under 18 years of age;
• Pregnant and breastfeeding women;
• Simultaneously with antiarrhythmic drugs (quinidine, cordarone, procainamide, sotalol).

The drug is used with caution when:

• Renal porphyria;
• Chronic renal failure;
• Liver failure;
• Predisposition to convulsive reactions;
• Cerebral circulation disorders, incl. in the anamnesis;
• Diabetes mellitus;
• Myasthenia;
• Atherosclerosis of cerebral vessels;
• Organic lesions of the central nervous system;
• Psychosis and other mental disorders, including a history of;
• Heart diseases, including heart failure, bradycardia, myocardial infarction;
• The need to use drugs that prolong the QT interval (antifungals, antihypertensives and some antihistamines, tetracyclic and tricyclic antidepressants, neuroleptics, imidazole derivatives, macrolides, barbiturates, class IA and III antiarrhythmic drugs).

Drug interactions Zanocin

Antacids, sucralfate, metal cations, multivitamins . Quinolones form chelates with alkaline agents and metal cation transporters. The use of quinolones in combination with antacids containing calcium, magnesium or aluminum, sucralfate, di- or trivalent cations (iron), multivitamin preparations containing zinc, didanosine can significantly reduce the absorption of quinolones, thereby reducing their systemic concentrations. The above drugs are taken 2 hours before or after taking ofloxacin. Caffeine. No interaction detected. Cyclosporins . There are no reports of increased plasma levels of cyclosporine when combined with quinolones. Potential interactions between quinolones and cyclosporines have not been studied. Cimetidine caused a violation of the elimination of some quinolones, namely, it led to an increase in the half-life of the drug and AUC. The possible interaction between ofloxacin and cimetidine has not been studied. Drugs that are metabolized by cytochrome P450 enzymes . Most quinolone drugs inhibit the enzyme activity of cytochrome P450. This may lead to a prolongation of the half-life of drugs that are metabolized by the same system (cyclosporine, theophylline/methylxanthines, warfarin) when used in combination with quinolones. NSAIDs. The combined use of NSAIDs and quinolones, including ofloxacin, may lead to an increased risk of CNS stimulant effects and seizures. Probenecid . The combined use of probenecid and quinolones may affect renal tubular excretion. The effect of probenecid on the excretion of ofloxacin has not been studied. Theophylline. Plasma levels of theophylline may increase when combined with ofloxacin. Like other quinolones, ofloxacin may prolong the half-life of theophylline, increase plasma theophylline levels and the risk of theophylline side effects. Plasma theophylline levels should be regularly determined and the dose adjusted when coadministered with ofloxacin. Side effects (including seizures) may occur with or without an increase in plasma theophylline levels. Warfarin. Some quinolones may enhance the effects of oral administration of warfarin or its derivatives. Therefore, when quinolones are combined with warfarin or its derivatives, prothrombin time and other blood coagulation parameters are regularly monitored. Antidiabetic agents (insulin, glyburide/glibenclamide) . Changes in blood glucose levels, including hyper- and hypoglycemia, have been reported during concomitant use of quinolone drugs and antidiabetic agents; therefore, glycemia should be closely monitored when the above drugs are used in combination. Drugs affecting renal tubular excretion (furosemide, methotrexate). With the simultaneous administration of quinolones and drugs that affect renal tubular excretion, excretion disturbances and an increase in the level of quinolones in the blood plasma may occur. Interference with laboratory or diagnostic tests . Some quinolones, including ofloxacin, may produce false-positive results for urinary opiates when administered with oral immunoassays. In the absence of data on the compatibility of the solution with other infusion solutions or drugs, Zanocin in the form of solution for infusion must be used separately. The drug is compatible with isotonic sodium chloride solution, Ringer's solution, 5% glucose or fructose solution.

Side effects of Zanotsin

According to reviews, Zanotin may cause the following side effects:

• stomach cramps, nausea, diarrhea, vomiting, decreased appetite, hyperbilirubinemia, jaundice, enterocolitis, flatulence;
• headache, unsteady gait, numbness of extremities, psychotic reactions, overexcitation, anxiety, hallucinations, increased blood pressure;
• tendon rupture, tendinitis and arthralgia;
• impairment of the perception of taste, color, smell, balance and hearing;
• tachycardia and blood pressure disorders, collapse;
• skin rashes, itching, swelling, fever, bronchospasm, vasculitis, Lyell's syndrome, anaphylactic shock, pinpoint hemorrhages, dermatitis;
• anemia, leukopenia, thrombocytopenia;
• disruptions in the normal functioning of the kidneys, nephritis, increased urea content;
• vaginitis, intestinal dysbiosis, hypoglycemia, thrombophlebitis, as well as local pain with the intravenous route of drug administration.

Overdose of the drug Zanotin, symptoms and treatment

Data on overdose with ofloxacin are limited. Symptoms: confusion, drowsiness, lethargy, disorientation, dizziness, nausea, vomiting. Treatment: there is no specific antidote. In case of overdose, the stomach is washed, adsorbents and sodium sulfate are prescribed (if possible, during the first 30 minutes), and antacids are used to protect the gastric mucosa. The patient is examined and, if necessary, hydrated. Forced diuresis accelerates the elimination of ofloxacin from the body. Hemodialysis or peritoneal dialysis are ineffective.

Analogs

"Eleflox"

Ranbaxy, India Price from 400 to 800 rub.

Eleflox is an antibacterial agent that has a pronounced bactericidal effect. Available in the form of tablets or solution, the active ingredient of which is levofloxacin.

Pros:

• Effective in the treatment of infectious and inflammatory diseases
• Rarely causes adverse reactions
• Bioavailability is almost 100%.

Minuses:

• Expensive
• Concomitant use with glucocorticoids is not prescribed, as there is a high probability of tendon rupture
• Dispensed by prescription.

"Sparflo"

Doctor Reddis, India Price from 299 to 340 rubles.

Sparflo is an antibacterial drug and has an antimicrobial and bactericidal effect. The active ingredient of this drug is sparfloxacin, available in tablets.

Pros:

• Allows you to effectively treat various infectious and inflammatory diseases
• Fast acting
• Affordable price.

Minuses:

• Not recommended for use with iron-containing medications
• Toxicity
• Causes multiple adverse reactions.