Lofox^® (Tablets, Drops) Instructions for Use

ATC Code

J01MA07 (Lomefloxacin)

Active Substance

Lomefloxacin (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Antibacterial drug of the fluoroquinolone group

Pharmacotherapeutic Group

Antimicrobial agent – fluoroquinolone

Pharmacological Action

A broad-spectrum antimicrobial drug from the fluoroquinolone group (subgroup of difluoroquinolones).

It acts on the bacterial enzyme DNA gyrase, which provides supercoiling of DNA, forms a complex with its tetramer (subunits of gyrase A2B2) and disrupts DNA transcription and replication, leading to the death of the microbial cell. It acts bactericidally.

Beta-lactamases produced by pathogens do not affect the activity of lomefloxacin.

Highly active against gram-negative aerobes Citrobacter diversus, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae, Klebsiella pneumoniae, Moraxella catarrhalis, Proteus mirabilis, Pseudomonas aeruginosa (only for urinary tract infections); gram-positive aerobes Staphylococcus saprophyticus.

Moderately sensitive to the drug are gram-positive microorganisms Staphylococcus aureus (including methicillin-resistant strains), Staphylococcus epidermidis (including methicillin-resistant strains); gram-negative aerobes Aeromonas hydrophila, Citrobacter freundii, Enterobacter aerogenes, Enterobacter agglomerans, Haemophilus parainfluenzae, Hafnia alvei, Klebsiella oxytoca, Klebsiella ozaenae, Morganella morganii, Proteus vulgaris, Providencia alcalifaciens, Providencia rettgeri, Serratia liquefaciens and Serratia marcescens, other microorganisms Legionella pneumophila.

It has anti-tuberculosis activity. It acts on both extracellularly and intracellularly located Mycobacterium tuberculosis, reduces the time of their excretion from the body, and ensures faster resorption of inflammatory infiltrates. It acts on most microorganisms at low concentrations (the concentration required to suppress the growth of 90% of strains is usually no more than 1 µg/ml).

Resistance develops rarely.

Resistant to the drug are Streptococcus spp. groups A, B, D and G, Streptococcus pneumoniae, Pseudomonas cepacia, Ureaplasma urealyticum, Mycoplasma hominis, Treponema pallidum and anaerobic bacteria.

There is no cross-resistance with penicillins, cephalosporins, aminoglycosides, co-trimoxazole, metronidazole.

Pharmacokinetics

Absorption

Absorption – 95-98%; food intake reduces absorption by 12%. T_max – 0.8-1.5 h. C_max after oral administration – 3-5.2 µg/ml. Food intake reduces C_max by 18% and increases T_max to 2 h.

Distribution

C_ss in plasma is determined after 48 h. Binding to plasma proteins – 10%. It penetrates well into organs and tissues (respiratory tract, ENT organs, soft tissues, bones, joints, abdominal organs, pelvic organs, genital organs), where the concentration of lomefloxacin is 2-7 times higher than in plasma.

Metabolism

A small part of the drug is metabolized.

Excretion

T_1/2 – 8-9 h; average renal clearance – 145 ml/min. 70-80% is excreted by the kidneys by tubular secretion (mainly unchanged, 9% as glucuronides, 0.5% as other metabolites); through the intestine – 20-30%.

Pharmacokinetics in special clinical cases

In elderly patients, plasma clearance decreases by 25%.

When creatinine clearance decreases to 10-40 ml/min/1.73 m², T_1/2 increases.

Indications

• Uncomplicated urinary tract infections caused by Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis or Staphylococcus saprophyticus;
• Complicated urinary tract infections caused by Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa, Citrobacter diversus or Enterobacter cloacae;
• Prevention of urinary tract infections during transrectal prostate biopsy, transurethral surgical interventions;
• Exacerbation of chronic bronchitis caused by Haemophilus influenzae or Moraxella catarrhalis;
• Urogenital chlamydia;
• Pulmonary tuberculosis (as part of complex therapy) – extensive caseous-necrotic tissue lesions, pronounced nonspecific component of inflammation, drug resistance of mycobacteria to rifampicin or poor tolerance to rifampicin.

ICD codes

Dosage Regimen

Tablets

The drug is taken orally, regardless of food intake, with a sufficient amount of liquid; frequency of administration – 1 time/day. The dose and duration of treatment depend on the severity of the disease and the sensitivity of the pathogen.

Uncomplicated cystitis in women caused by Escherichia coli – 400 mg/day for 3 days.

Uncomplicated cystitis caused by Klebsiella pneumoniae, Proteus mirabilis or Staphylococcus saprophyticus – 400 mg/day for 10 days.

Complicated urinary tract infections – 400 mg/day for 14 days.

Prevention of urinary tract infections: during transrectal prostate biopsy – 400 mg as a single dose 1-6 hours before the procedure; transurethral surgical interventions – 400 mg as a single dose 2-6 hours before surgery.

Exacerbation of chronic bronchitis caused by Haemophilus influenzae or Moraxella catarrhalis – 400 mg/day for 14 days.

Urogenital chlamydia – 400 mg/day, duration of treatment – up to 28 days.

Pulmonary tuberculosis (as part of complex therapy) – 400 mg/day for 14-28 days or more.

Drops

Adults are prescribed 1 drop 2-3 times/day into the lower conjunctival sac for 7-9 days. At the beginning of treatment, more frequent application is necessary: 5 drops within 20 minutes (1 drop at 5-minute intervals) or 1 drop/hour for 6-10 hours.

For treatment of chlamydial conjunctivitis, 1 drop of the drug is instilled into the conjunctival sac of the affected eye 2-4 times/day for 1-2 months.

Adverse Reactions

From the digestive system nausea, vomiting, dry mouth, gastralgia, abdominal pain, diarrhea or constipation, flatulence, pseudomembranous enterocolitis, dysphagia, discoloration of the tongue, decreased appetite or bulimia, taste perversion, dysbacteriosis, increased activity of hepatic transaminases.

From the nervous system fatigue, malaise, asthenia, headache, dizziness, insomnia, hallucinations, convulsions, hyperkinesis, tremor, paresthesia, nervousness, anxiety, depression, agitation.

From the urinary system glomerulonephritis, dysuria, polyuria, anuria, albuminuria, urethral bleeding, crystalluria, hematuria, urinary retention, edema.

From the reproductive system in women – vaginitis, leukorrhea, intermenstrual bleeding, perineal pain, vaginal candidiasis; in men – orchitis, epididymitis.

From the metabolism hypoglycemia, gout.

From the musculoskeletal system arthralgia, vasculitis, calf muscle cramps, back and chest pain.

From the hematopoietic system bleeding from the gastrointestinal tract, thrombocytopenia, purpura, increased fibrinolysis, nosebleed, lymphadenopathy.

From the respiratory system dyspnea, respiratory tract infections, cough, hypersecretion of sputum, flu-like symptoms.

From the sensory organs visual impairment, pain and tinnitus, eye pain.

From the cardiovascular system fainting, decreased blood pressure, tachycardia, bradycardia, extrasystole, arrhythmias, progression of heart failure, angina pectoris, pulmonary embolism, myocardiopathy, phlebitis.

Allergic reactions skin itching, urticaria, malignant exudative erythema (Stevens-Johnson syndrome), bronchospasm.

Other candidiasis, increased sweating, chills, thirst, superinfection, photosensitivity.

Contraindications

• Pregnancy;
• Lactation period (breastfeeding);
• Age under 18 years (period of skeletal formation and growth);
• Renal failure (creatinine clearance less than 30 ml/min);
• Hypersensitivity to the components of the drug and to other fluoroquinolones.

Lomefloxacin should not be prescribed to patients with QT interval prolongation.

With caution cerebral atherosclerosis, epilepsy and other CNS diseases with epileptic syndrome, QT interval prolongation, hypokalemia, simultaneous use of antiarrhythmic drugs of class I A (quinidine, procainamide) and class III A (amiodarone, sotalol).

Use in Pregnancy and Lactation

Lofox^® is contraindicated for use during pregnancy and during lactation (breastfeeding).

In experimental studies, fetotoxic effects (arthropathy) have been described.

Use in Hepatic Impairment

In liver cirrhosis, no dose adjustment is required (provided renal function is normal).

Use in Renal Impairment

Contraindicated in renal failure (creatinine clearance less than 30 ml/min).

Pediatric Use

The drug is contraindicated for use under the age of 18 years.

Special Precautions

In liver cirrhosis, no dose adjustment is required (with normal renal function).

During treatment, prolonged exposure to the sun and exposure to artificial UV radiation should be avoided (evening intake reduces the risk of reaction to UV radiation).

At the first signs of photosensitivity (increased skin sensitivity, burn, redness, swelling, blistering, rash, itching, dermatitis) or hypersensitivity, manifestations of neurotoxicity (agitation, convulsions, tremor, photophobia, confusion, toxic psychoses, hallucinations), therapy should be discontinued.

Effect on the ability to drive vehicles and mechanisms

During the treatment period, caution must be exercised when driving vehicles or engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

Information on overdose of Lofox^® is very limited.

Treatment if necessary, symptomatic therapy is carried out. Hemodialysis and peritoneal dialysis are not very effective in case of overdose.

Drug Interactions

With simultaneous use, Lomefloxacin does not affect the pharmacokinetics of isoniazid; does not interact with theophylline, caffeine.

With simultaneous use, Lomefloxacin increases the activity of oral anticoagulants and increases the toxicity of NSAIDs.

When prescribed simultaneously, antacids and sucralfate should not be taken within 4 hours before and 2 hours after taking lomefloxacin, because it forms chelate compounds with them, which reduces its bioavailability.

In the treatment of tuberculosis, Lomefloxacin is used together with isoniazid, pyrazinamide, streptomycin and ethambutol (combination with rifampicin is not recommended due to antagonism of action).

With simultaneous use, drugs that block tubular secretion slow down the excretion of lomefloxacin.

Vitamins with mineral supplements should be taken 2 hours before or 2 hours after taking lomefloxacin.

When used concomitantly with antiarrhythmic drugs of classes I A (quinidine, procainamide) and III (amiodarone, sotalol), QT interval prolongation is possible.

Storage Conditions

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.