Ksenakvin (Tablets) Instructions for Use

Marketing Authorization Holder

Promed Exports, Pvt. Ltd. (India)

ATC Code

J01MA07 (Lomefloxacin)

Active Substance

Lomefloxacin (Rec.INN registered by WHO)

Dosage Form

Ksenakvin

Film-coated tablets, 400 mg: 5 or 1000 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets orange in color, oblong, with beveled edges; on the break – yellowish-white in color.

Excipients: microcrystalline cellulose, talc, magnesium stearate, colloidal silicon dioxide, croscarmellose sodium, hypromellose, titanium dioxide, dichloromethane (methylene chloride), isopropyl alcohol, dye Sunset Yellow Lake.

5 pcs. – blisters (1) – cardboard boxes.
1000 pcs. – plastic jars.

Clinical-Pharmacological Group

Antibacterial drug of the fluoroquinolone group

Pharmacotherapeutic Group

Antimicrobial agent – fluoroquinolone

Pharmacological Action

Lomefloxacin is a synthetic antimicrobial drug of the fluoroquinolone group with a broad spectrum of bactericidal action. It inhibits the activity of bacterial DNA gyrase, forming a complex with its tetramer (gyrase subunits A2B2) and disrupts DNA transcription and replication, leading to the death of the microbial cell. Beta-lactamases produced by pathogens do not affect the activity of lomefloxacin.

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

In vitro with a minimum inhibitory concentration (MIC) of 2 µg/ml, it is active against the following microorganisms (however, clinical efficacy in infections caused by these microorganisms has not been studied in strictly controlled trials): gram-positive aerobic microorganisms: Staphylococcus aureus (including methicillin-resistant strains), Staphylococcus epidermidis (including methicillin-resistant strains); gram-negative aerobic microorganisms: 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, Serratia marcescens; other microorganisms: Legionella pneumophila.

The following are resistant to the drug: Streptococcus spp. groups A, B, D and G, Streptococcus pneumoniae, Pseudomonas cepacia, Ureaplasma urealyticum, Mycoplasma hominis and anaerobic bacteria.

It acts on both extracellularly and intracellularly located Mycobacterium tuberculosis, reduces the time of their excretion from the body, and ensures faster resorption of infiltrates. It acts on most microorganisms at low concentrations (the concentration required to suppress the growth of 90% of strains is usually not more than 1 µg/ml).

Pharmacokinetics

After oral administration, Lomefloxacin is almost completely absorbed from the gastrointestinal tract (absorption – 93-98%; food intake reduces it by 12%). After a 400 mg dose, C_max in plasma is reached in 1-2 hours and is 3-5.2 mg/L. Food intake reduces C_max by 18%.

Steady-state plasma concentration is reached within 48 hours. Plasma protein binding is 9-11%. It penetrates well into organs and tissues (respiratory tract, ENT organs, soft tissues, bones, joints, abdominal organs, pelvic organs, genitals), where the concentration of lomefloxacin is 2-7 times higher than in plasma.

A small part of the drug is metabolized to form metabolites.

T_1/2 – 8-9 hours; average renal clearance – 143-147 ml/min.

In elderly patients, plasma clearance decreases by 25%. When creatinine clearance decreases to 10-40 ml/min, T_1/2 increases. 70-80% is excreted by the kidneys via tubular secretion (mainly unchanged, 9% as glucuronides, 0.5% as other metabolites); 20-30% is excreted through the intestines.

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;
• Pulmonary tuberculosis (as part of combination 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

Orally (regardless of food intake, with a sufficient amount of fluid), once a 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.

Exacerbation of chronic bronchitis 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 the surgical intervention.

Tuberculosis 400 mg/day, for 14 – 28 days or more.

In patients with creatinine clearance less than 30 ml/min and patients on hemodialysis, the initial dose is 400 mg/day, followed by a reduction to 200 mg/day.

Adverse Reactions

From the digestive system nausea, vomiting, dry mouth, gastralgia, abdominal pain, diarrhea or constipation, flatulence, pseudomembranous colitis, dysphagia, change in tongue color, anorexia or bulimia, taste perversion, dysbacteriosis, increased activity of “liver” transaminases.

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

From the genitourinary system glomerulonephritis, dysuria, polyuria, anuria, albuminuria, urethral bleeding, crystalluria, hematuria, urinary retention, edema; 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 hemostasis system and hematopoietic organs bleeding from the gastrointestinal tract organs, thrombocytopenia, purpura, increased fibrinolysis, nosebleed, lymphadenopathy.

From the respiratory system shortness of breath, bronchospasm, cough, increased sputum secretion, flu-like symptoms.

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

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

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

Effect on the fetus fetotoxic effect (arthropathy) has been described in experiments.

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

Contraindications

• Hypersensitivity (including to other fluoroquinolones);
• Pregnancy, lactation period;
• Age under 18 years (period of skeletal formation and growth);
• Lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

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

Use in Pregnancy and Lactation

Contraindicated during pregnancy and lactation.

Use in Renal Impairment

In patients with creatinine clearance less than 30 ml/min and patients on hemodialysis, the initial dose is 400 mg/day, followed by a reduction to 200 mg/day.

Pediatric Use

Contraindicated in children under 18 years of age.

Special Precautions

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

During treatment, prolonged exposure to sunlight and the use of artificial ultraviolet illumination should be avoided (evening intake reduces the risk of reaction to ultraviolet radiation). At the first signs of photosensitivity (increased skin sensitivity, burn, hyperemia, swelling, blistering, rash, itching, dermatitis) or hypersensitivity, manifestations of neurotoxicity (agitation, convulsions, tremor, photophobia, confusion, toxic psychoses, hallucinations), therapy should be discontinued.

Effect on ability to drive vehicles and operate machinery

During treatment, it is necessary to refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions (only possible after assessing the patient’s individual response).

Overdose

Treatment induction of vomiting or gastric lavage, adequate hydration, symptomatic therapy. Hemodialysis and peritoneal dialysis are not very effective in case of overdose.

Drug Interactions

Antacid agents and sucralfate should not be taken within 4 hours before and 2 hours after taking lomefloxacin (it forms chelate compounds with them, which reduces its bioavailability).

When treating patients with tuberculosis, Lomefloxacin is used together with isoniazid, pyrazinamide, streptomycin and ethambutol (combination with rifampicin is not recommended – antagonism).

Does not affect the pharmacokinetics of isoniazid. Does not interact with theophylline, caffeine.

Drugs that block tubular secretion slow down excretion. There is no cross-resistance with penicillins, cephalosporins, aminoglycosides, co-trimoxazole, metronidazole.

Increases the activity of indirect anticoagulants and increases the toxicity of non-steroidal anti-inflammatory drugs.

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

Storage Conditions

Store at a temperature not exceeding 25°C (77°F) in a dry place, protected from light. Keep out of the reach of children.

Shelf Life

Shelf life – 3 years.

Dispensing Status

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.