Ofloxacin (Tablets, Solution) Instructions for Use

ATC Code

J01MA01 (Ofloxacin)

Active Substance

Ofloxacin (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Antibacterial drug of the fluoroquinolone group

Pharmacotherapeutic Group

Systemic antibacterial agents; quinolone derivatives; fluoroquinolones

Pharmacological Action

A broad-spectrum antimicrobial drug from the fluoroquinolone group. It 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.

The drug is active against microorganisms producing beta-lactamases and fast-growing atypical mycobacteria.

The drug is sensitive to Staphylococcus aureus, Staphylococcus epidermidis, Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Citrobacter spp., Klebsiella spp. (including Klebsiella pneumoniae), Enterobacter spp., Hafnia spp., Proteus spp. (including Proteus mirabilis, Proteus vulgaris – indole-positive and indole-negative strains), Salmonella spp., Shigella spp. (including Shigella sonnei), Yersinia enterocolitica, Campylobacter jejuni, Aeromonas hydrophila, Plesiomonas aeruginosa, Vibrio cholerae, Vibrio parahaemolyticus, Haemophilus influenzae, Chlamydia spp., Legionella spp., Serratia spp., Providencia spp., Haemophilus ducreyi, Bordetella parapertussis, Bordetella pertussis, Moraxella catarrhalis, Propionibacterium acnes, Brucella spp.

Various sensitivity to the drug is possessed by: Enterococcus faecalis, Streptococcus pyogenes, Streptococcus pneumoniae, Streptococcus viridans, Serrratia marcescens, Pseudomonas aeruginosa, Acinetobacter spp., Mycoplasma hominis, Mycoplasma pneumoniae, Mycobacterium tuberculosis, Mycobacterium fortuitum, Ureaplasma urealyticum, Clostridium perfringens, Corynebacterium spp., Helicobacter pylori, Listeria monocytogenes, Gardnerella vaginalis.

The drug is resistant to Nocardia asteroides, anaerobic bacteria (Bacteroides spp., Peptococcus spp., Peptostreptococcus spp., Eubacterium spp., Fusobacterium spp., Clostridium difficile).

The drug is inactive against Treponema pallidum.

Pharmacokinetics

Absorption

After oral administration, absorption is rapid and complete (95%). Bioavailability is more than 96%.

Distribution

Plasma protein binding is 25%. C_max after oral administration of a dose of 100 mg, 300 mg and 600 mg is 1 mg/l, 3.4 mg/l and 6.9 mg/l, respectively, and is achieved in 1-2 hours. After a single dose of 200 mg and 400 mg, C_max is 2.5 µg/ml and 5 µg/ml, respectively. Food intake may slow absorption but does not significantly affect bioavailability.

Apparent V_d is 100 L. Ofloxacin is distributed in leukocytes, alveolar macrophages, skin, soft tissues, bones, abdominal and pelvic organs, respiratory system, urine, saliva, bile, and prostate secretion. It penetrates well through 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%). Does not accumulate.

Metabolism

Metabolized in the liver (about 5%) to form N-oxide ofloxacin and dimethylofloxacin.

Excretion

T_1/2 is 4.5-7 hours (independent of dose). Excreted by the kidneys unchanged – 75-90%, with bile – about 4%. 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 or hepatic insufficiency, excretion may be slowed.

Indications

• Infectious and inflammatory diseases of the respiratory tract (bronchitis, pneumonia);
• Infectious and inflammatory diseases of the ENT organs (sinusitis, pharyngitis, otitis media, laryngitis);
• Infectious and inflammatory diseases of the skin and soft tissues;
• Infectious and inflammatory diseases of bones and joints;
• Infectious and inflammatory diseases of the abdominal cavity (including gastrointestinal infections) and biliary tract;
• Infectious and inflammatory diseases of the kidneys (pyelonephritis) and urinary tract (cystitis, urethritis);
• Infectious and inflammatory diseases of the pelvic organs (endometritis, salpingitis, oophoritis, cervicitis, parametritis, prostatitis) and genital organs (colpitis, orchitis, epididymitis);
• Gonorrhea;
• Chlamydia;
• Meningitis;
• Prevention of infections in patients with impaired immune status (including neutropenia).

ICD codes

Dosage Regimen

Solution

The drug is administered intravenously by drip. Doses are selected individually depending on the location and severity of the infection, the sensitivity of microorganisms, the general condition of the patient, and liver and kidney function.

Therapy is started with intravenous drip (over 30-60 minutes) administration of the drug at a dose of 200 mg. When the patient’s condition improves, they are switched to oral administration of the drug at the same daily dose.

For urinary tract infections, the drug is prescribed 100 mg 1-2 times/day; for kidney and genital infections – from 100 to 200 mg 2 times/day; for respiratory tract infections, as well as ENT organ infections, skin and soft tissue infections, bone and joint infections, abdominal infections, septic infections – 200 mg 2 times/day. If necessary, the dose can be increased to 400 mg 2 times/day.

For prevention of infections in patients with severe immunodeficiency – 400-600 mg/day.

In patients with impaired renal function (with CC from 50 to 20 ml/min), a single dose should be 50% of the average recommended dose with a frequency of administration of 2 times/day. A full single dose can be administered once a day. With CC less than 20 ml/min, the initial single dose is 200 mg, then the drug is administered at 100 mg/day every other day.

During peritoneal dialysis and hemodialysis, the drug is administered at 100 mg every 24 hours.

In hepatic insufficiency, the maximum daily dose is 400 mg.

Tablets

Doses are selected individually depending on the location and severity of the infection, the sensitivity of microorganisms, the general condition of the patient, and liver and kidney function.

The drug is prescribed orally to adults – 200-800 mg/day, frequency of administration – 2 times/day. The course of treatment is 7-10 days. A dose of up to 400 mg/day can be prescribed in a single dose, preferably in the morning.

For acute gonorrhea – 400 mg once.

In patients with impaired renal function (with CC from 50 to 20 ml/min), a single dose should be 50% of the average dose with a frequency of administration of 2 times/day, or a full single dose is prescribed once a day. With CC<20 ml/min, a single dose is 200 mg, then – 100 mg/day every other day.

During hemodialysis and peritoneal dialysis, the drug is prescribed at 100 mg every 24 hours.

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

The average daily dose for children with severe infections is 7.5 mg/kg of body weight, the maximum dose is 15 mg/kg.

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

The duration of the treatment course is determined by the sensitivity of the pathogen and the clinical picture; treatment should be continued for another 3 days after the symptoms of the disease disappear and the temperature has completely normalized.

For treatment of salmonellosis, the course of treatment is 7-8 days; for uncomplicated lower urinary tract infections – 3-5 days.

Adverse Reactions

From the digestive system anorexia, nausea, vomiting, diarrhea, flatulence, abdominal pain (including gastralgia), increased activity of hepatic transaminases, hyperbilirubinemia, cholestatic jaundice, pseudomembranous enterocolitis.

From the CNS headache, dizziness, unsteadiness of movements, tremor, convulsions, numbness and paresthesia of the extremities, vivid dreams, nightmares, psychotic reactions, anxiety, increased excitability, phobias, depression, confusion, hallucinations, increased intracranial pressure; impaired color perception, diplopia, disturbances of taste, smell, hearing and balance.

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

From the cardiovascular system tachycardia, vasculitis, collapse.

From the skin petechiae, bullous hemorrhagic dermatitis, papular rash, vasculitis.

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

From the urinary system acute interstitial 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, erythema multiforme; rarely – anaphylactic shock.

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 CNS);
• Age under 18 years (because skeletal growth is not complete);
• Pregnancy;
• Lactation (breastfeeding);
• Hypersensitivity to the components of the drug.

With caution, the drug should be prescribed for cerebral atherosclerosis, cerebrovascular accidents (in history), chronic renal failure, organic lesions of the CNS.

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 CC from 50 to 20 ml/min), a single dose should be 50% of the average dose with a frequency of administration of 2 times/day, or a full single dose is prescribed once a day. With CC<20 ml/min, a single dose is 200 mg, then – 100 mg/day every other day.

During hemodialysis and peritoneal dialysis, the drug is prescribed at 100 mg every 24 hours.

Pediatric Use

The drug is contraindicated in children and adolescents under 18 years of age, because skeletal growth is not complete.

In children, Ofloxacin-AKOS is prescribed only in life-threatening situations, taking into account the expected benefit and the potential risk of side effects, when it is impossible to use other, less toxic drugs.

Special Precautions

It is not the drug of choice for pneumonia caused by pneumococci. Not indicated for the treatment of acute tonsillitis.

It is not recommended to use the drug for more than 2 months. Exposure to sunlight, UV radiation (mercury-quartz lamps, solarium) should be avoided.

In case of side effects from the CNS, allergic reactions, pseudomembranous colitis, discontinuation of the drug is necessary. For pseudomembranous colitis, confirmed by colonoscopy and/or histologically, oral administration of vancomycin and metronidazole is indicated.

It should be taken into account that when using Ofloxacin-AKOS, rarely occurring tendinitis can lead to tendon rupture (primarily the Achilles tendon), especially in elderly patients. If symptoms of tendinitis occur, it is necessary to immediately stop treatment, immobilize the Achilles tendon and consult an orthopedist.

When using the drug, women are not recommended to use tampons like Tampax, due to the increased risk of developing vaginal candidiasis.

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

When using the drug, false-negative results are possible 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 treatment with the drug, alcohol consumption should be avoided.

Use in Pediatrics

In children, Ofloxacin-AKOS is prescribed only in life-threatening situations, taking into account the expected benefit and the potential risk of developing side effects, when it is impossible to use other, less toxic drugs.

Effect on the Ability to Drive Vehicles and Operate Machinery

During treatment, it is necessary to refrain from driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

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

Treatment gastric lavage, administration of symptomatic therapy.

Drug Interactions

Food, antacids containing aluminum, calcium, magnesium, or iron salts reduce the absorption of ofloxacin by forming insoluble complexes (therefore, the interval between the administration of Ofloxacin-AKOS and these drugs should be at least 2 hours).

Ofloxacin reduces the clearance of theophylline by 25%. Therefore, when used concomitantly, the dose of theophylline should be reduced.

Cimetidine, furosemide, methotrexate, and drugs that block tubular secretion increase the plasma concentration of ofloxacin.

Ofloxacin increases the plasma concentration of glibenclamide.

When ofloxacin is taken concomitantly with vitamin K antagonists, the blood coagulation system should be monitored.

When Ofloxacin-AKOS is prescribed with NSAIDs, nitroimidazole derivatives, and methylxanthines, the risk of neurotoxic effects increases.

When Ofloxacin-AKOS is prescribed concomitantly with glucocorticosteroids, the risk of tendon rupture increases, especially in the elderly.

When Ofloxacin-AKOS is prescribed with drugs that alkalinize the 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

The shelf life is 2 years.

Dispensing Conditions

The drug is dispensed by prescription.

Dispensing Status

Rx Only

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.