Ofloxacin Stada (Tablets) Instructions for Use

Marketing Authorization Holder

Nizhpharm JSC (Russia)

Manufactured By

Skopinsky Pharmaceutical Plant, CJSC (Russia)

ATC Code

J01MA01 (Ofloxacin)

Active Substance

Ofloxacin (Rec.INN registered by WHO)

Dosage Form

Ofloxacin Stada

Film-coated tablets, 200 mg: 10 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white or almost white, biconvex, with slight roughness; on the cross-section, two layers are visible: an inner layer (core) of white with a yellowish tint.

Excipients: microcrystalline cellulose, croscarmellose sodium, low molecular weight polyvinylpyrrolidone, magnesium stearate, colloidal silicon dioxide, hypromellose, polyethylene glycol, titanium dioxide, talc.

10 pcs. – blister packs (1) – cardboard packs.

Clinical-Pharmacological Group

Antibacterial drug of the fluoroquinolone group

Pharmacotherapeutic Group

Antimicrobial agent – fluoroquinolone

Pharmacological Action

Broad-spectrum antibacterial drug from the fluoroquinolone group, acts on the bacterial enzyme DNA gyrase, which provides supercoiling and, thus, the stability of bacterial DNA (destabilization of DNA chains leads to their death). It has a bactericidal effect.

Active against microorganisms producing beta-lactamases and fast-growing atypical mycobacteria. Sensitive are Staphylococcus aureus, Staphylococcus epidermidis, Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Citrobacter spp., Klebsiella spp. (including Klebsiella pneumonia), Enterobacter spp., Hafhia spp., Proteus spp. (including Proteus mirabilis, Proteus vulgaris, both indole-positive and indole-negative), Salmonella spp., Shigella spp. (including Shigella sonnei), Yersinia enterocolitica, Campilobacter jejuni, Aeromonas hydrophila, Plesiomonas aeruginosa, Vibrio cholerae, Vibrio parahaemolyticus, Haemophilus influenzae, Chlamydia spp., Legionella spp., Gerratia spp., Providencia spp., Haemophilus ducreyi, Bordetella parapertussis, Bordetella pertussis, Moraxella catarrhalis, Propionibacterium acnes, Staphylococcus spp., Brucella spp.

Variable sensitivity to the drug is possessed by Enterococcus faecalis, Streptococcus pyogenes, pheumonis and viridans, Serrratio marcescens, Pseudomonas aeruginosa, Acinetobacter, Mycoplasma hominis and pneumoniae, Mycobacterium tuberculosis, as well as Mycobacterium fortuim, Ureaplasma urealyticum, Clostridium perfringens, Corynebacterium spp., Helicobacter pylori, Listeria monocytogenes, Gardnerella vaginalis.

In most cases, not sensitive are Nocardia asteroides, anaerobic bacteria (for example, Bacteroides spp., Peptococcus spp., Peptostreptococcus spp., Eubacterium spp., Fusobacterium spp., Clostridium difficile). Does not act on Treponema pallidum.

Pharmacokinetics

Absorption

After oral administration, Ofloxacin is rapidly and almost completely (95%) absorbed from the gastrointestinal tract. Bioavailability is over 96%, plasma protein binding is 25%, C_max is reached 1-2 hours after oral administration and after a dose of 100 mg, 300 mg, 600 mg is 1, 3, 4 and 6.9 mg/l, respectively: after a single dose of 200 mg and 400 mg, it is 2.5 µg/ml and 5 µg/ml, respectively. Taking with food may slow absorption but does not significantly affect bioavailability.

Distribution

Apparent V_d is 100 L. Ofloxacin penetrates into leukocytes, alveolar macrophages, skin, soft tissues, bones, abdominal and pelvic organs, respiratory system, urine, saliva, bile, prostate secretion. It crosses the blood-brain barrier, placental barrier, and is excreted in breast milk. It penetrates into the cerebrospinal fluid with inflamed and non-inflamed meninges (14-60%).

Metabolism and Excretion

It is metabolized in the liver (about 5%) with the formation of N-oxide ofloxacin and dimethylofloxacin. T_1/2 is 4.5-7 hours (dose-independent). Excreted by the kidneys – 75-90% (unchanged), about 4% – with bile. Non-renal clearance is less than 20%. After a single dose of 200 mg, it is detected in urine for 20-24 hours.

Pharmacokinetics in Special Clinical Cases

In renal/hepatic insufficiency, excretion may be slowed. Does not accumulate. During hemodialysis, 10-30% of the drug is removed.

Indications

Treatment of infectious and inflammatory diseases caused by pathogens sensitive to the drug:

• Respiratory tract infections (bronchitis, pneumonia);
• ENT infections (sinusitis, pharyngitis, otitis media, laryngitis);
• Skin and soft tissue infections;
• Bone and joint infections;
• Infectious and inflammatory diseases of the abdominal cavity and biliary tract (except bacterial enteritis);
• Kidney infections (pyelonephritis), urinary tract infections (cystitis, urethritis);
• Pelvic infections (endometritis, salpingitis, oophoritis, cervicitis, parametritis, prostatitis);
• Genital infections (colpitis, orchitis, epididymitis);
• Gonorrhea;
• Chlamydia;
• Septicemia (only for intravenous administration);
• Meningitis.

Prevention of infections in patients with impaired immune status (including neutropenia).

ICD codes

Dosage Regimen

The dosage regimen is set individually depending on the location and severity of the infection, the sensitivity of microorganisms, the general condition of the patient, and indicators of liver and kidney function.

The average recommended dose for adults is 200-800 mg/day. The course of treatment is 7-10 days, frequency of administration is 2 times/day. A dose up to 400 mg/day can be prescribed in 1 dose, preferably in the morning.

For gonorrhea – 400 mg once.

In patients with impaired renal function (with CrCl 50-20 ml/min) a single dose should be 50% of the average dose with a frequency of administration of 2 times/day or the full single dose is administered 1 time/day. With CrCl less than 20 ml/min a single dose is 200 mg, then – 100 mg every other day.

For hemodialysis and peritoneal dialysis – 100 mg every 24 hours.

The maximum daily dose for hepatic insufficiency is 400 mg/day.

The duration of the treatment course is determined by the sensitivity of the pathogen and the clinical picture; treatment should be continued for at least another 3 days after the symptoms of the disease disappear and the temperature completely normalizes. When treating salmonellosis the course of treatment is 7-8 days, for uncomplicated lower urinary tract infections the course of treatment is 3-5 days.

The tablets should be taken whole, with water before or during meals.

Adverse Reactions

From the digestive system: gastralgia, anorexia, nausea, vomiting, diarrhea, flatulence, abdominal pain, increased activity of liver transaminases, hyperbilirubinemia, cholestatic jaundice, pseudomembranous enterocolitis.

From the central and peripheral nervous system: headache, dizziness, unsteadiness of movements, tremor, convulsions, numbness and paresthesia of the extremities, vivid dreams, nightmares, psychotic reactions, anxiety, agitation, phobias, depression, confusion, hallucinations, increased intracranial pressure.

From the musculoskeletal system: tendinitis, myalgia, arthralgia, tenosynovitis, tendon rupture.

From the senses: impaired color perception, diplopia, disturbances of taste, smell, hearing and balance.

From the cardiovascular system: tachycardia, decreased blood pressure, vasculitis, collapse.

From the hematopoietic system leukopenia, agranulocytosis, anemia, thrombocytopenia, pancytopenia, hemolytic and aplastic anemia.

From the urinary system nephritis, impaired renal function, hypercreatininemia, increased urea content.

Allergic reactions: skin rash, itching, urticaria, allergic pneumonitis, allergic nephritis, eosinophilia, fever, angioedema, bronchospasm, Stevens-Johnson syndrome, Lyell’s syndrome, photosensitivity, exudative erythema multiforme, anaphylactic shock.

Dermatological reactions: petechiae, hemorrhagic bullous dermatitis, papular rash with crusting, indicating vascular damage (vasculitis).

Other: dysbacteriosis, superinfection, hypoglycemia (in diabetic patients), vaginitis.

Contraindications

• Glucose-6-phosphate dehydrogenase deficiency;
• Epilepsy (including history);
• Lowered seizure threshold (including after traumatic brain injury, stroke, or inflammatory processes in the central nervous system);
• Age under 18 years (until skeletal growth is complete);
• Pregnancy;
• Lactation (breastfeeding);
• Hypersensitivity to the components of the drug.

With caution the drug is used for cerebral atherosclerosis, cerebrovascular accident (in history); in patients with chronic renal failure, organic lesions of the central nervous system.

Use in Pregnancy and Lactation

The drug is contraindicated for use during pregnancy and during lactation (breastfeeding).

Use in Hepatic Impairment

The maximum daily dose for hepatic insufficiency is 400 mg/day.

Use in Renal Impairment

In patients with impaired renal function (with CrCl 50-20 ml/min) a single dose should be 50% of the average dose with a frequency of administration of 2 times/day or the full single dose is administered 1 time/day. With CrCl less than 20 ml/min a single dose is 200 mg, then – 100 mg every other day.

For hemodialysis and peritoneal dialysis – 100 mg every 24 hours.

Pediatric Use

The drug is contraindicated in children and adolescents under 18 years of age (until skeletal growth is complete).

In children, it is used only in life-threatening situations, taking into account the expected benefit and potential risk of side effects, when it is impossible to use other, less toxic drugs. The average daily dose in this case is 7.5 mg/kg, maximum – 15 mg/kg.

Special Precautions

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

Not intended for the treatment of acute tonsillitis.

It is not recommended to use for more than 2 months.

During the use of the drug, avoid sun exposure and UV irradiation (mercury-quartz lamps, solarium).

If side effects from the central nervous system, allergic reactions, pseudomembranous colitis occur, the drug should be discontinued.

For pseudomembranous colitis, confirmed by colonoscopy and/or histologically, oral administration of vancomycin and metronidazole is indicated.

Rarely occurring tendinitis can lead to tendon rupture (primarily the Achilles tendon), especially in elderly patients. If signs of tendinitis appear, it is necessary to immediately stop treatment, immobilize the Achilles tendon and consult an orthopedist.

Women are not recommended to use tampons while using the drug due to the increased risk of developing thrush.

During treatment, worsening of myasthenia gravis, increased frequency of porphyria attacks in predisposed patients is possible.

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

In patients with impaired liver or kidney function, monitoring of the plasma concentration of ofloxacin is necessary. In severe renal and hepatic insufficiency, the risk of toxic effects increases (dose adjustment is required).

During the use of the drug, alcohol should not be consumed.

Use in pediatrics

In children, it is used only in life-threatening situations, taking into account the expected benefit and potential risk of side effects, when it is impossible to use other, less toxic drugs. The average daily dose in this case is 7.5 mg/kg, maximum – 15 mg/kg.

Effect on ability to drive vehicles and mechanisms

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.

Overdose

Symptoms dizziness, confusion, lethargy, disorientation, drowsiness, vomiting.

Treatment gastric lavage, symptomatic therapy. Hemodialysis removes 10-30% of the drug.

Drug Interactions

Food, antacids containing aluminum, calcium, magnesium ions, or iron preparations reduce the absorption of ofloxacin by forming insoluble complexes (the time interval between the administration of these drugs should be at least 2 hours).

With simultaneous use, Ofloxacin reduces the clearance of theophylline by 25% (when using such a combination, the dose of theophylline should be reduced).

With simultaneous use, cimetidine, furosemide, methotrexate and drugs that block tubular secretion increase the plasma concentration of ofloxacin.

With simultaneous use, Ofloxacin increases the plasma concentration of glibenclamide.

When taken simultaneously with indirect anticoagulants, it is necessary to monitor blood coagulation parameters.

With simultaneous use with NSAIDs, nitroimidazole derivatives and methylxanthines, the risk of neurotoxic effects increases.

With simultaneous administration with glucocorticosteroids, the risk of tendon rupture increases, especially in the elderly.

With simultaneous use with drugs that alkalinize urine (carbonic anhydrase inhibitors, citrates, sodium bicarbonate), the risk of crystalluria and nephrotoxic effects increases.

Storage Conditions

List B. The drug should be stored in a dry, light-protected place, out of the reach of children, at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 3 years.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.