МАКЛЕВО Uses, Dosage, Side Effects and more

МАКЛЕВО exerts antibacterial action by inhibiting bacterial topoisomerase IV and DNA gyrase, the enzymes required for DNA replication, transcription repair and recombination. It has in vitro activity against a wide range of gm-ve and gm+ve microorganisms.

МАКЛЕВО is bactericidal and exerts its antimicrobial effects via inhibition of bacterial DNA replication. It has a relatively long duration of action in comparison with other antibiotics that allows for once or twice daily dosing. МАКЛЕВО is associated with QTc-interval prolongation and should be used with caution in patients with other risk factors for prolongation (e.g. hypokalemia, concomitant medications).

МАКЛЕВО has demonstrated in vitro activity against a number of aerobic gram-positive and gram-negative bacteria and may carry some activity against certain species of anaerobic bacteria and other pathogens such as Chlamydia and Legionella. Resistance to levofloxacin may develop, and is generally due to mutations in DNA gyrase or topoisomerase IV, or via alterations to drug efflux. Cross-resistance may occur between levofloxacin and other fluoroquinolones, but is unlikely to develop between levofloxacin and other antibiotic classes (e.g. macrolides) due to significant differences in chemical structure and mechanism of action.

As antimicrobial susceptibility patterns are geographically distinct, local antibiograms should be consulted to ensure adequate coverage of relevant pathogens prior to use.

Attribute	Details
Trade Name	МАКЛЕВО
Availability	Prescription only
Generic	Levofloxacin
Levofloxacin Other Names	(S)-Ofloxacin, L-Ofloxacin, Levofloxacin, Levofloxacine, Levofloxacino, Levofloxacinum
Related Drugs	amoxicillin, prednisone, doxycycline, ciprofloxacin, cephalexin, metronidazole, azithromycin, clindamycin, ceftriaxone, Augmentin
Type
Formula	C18H20FN3O4
Weight	Average: 361.3675 Monoisotopic: 361.143784348
Protein binding	Levofloxacin is 24-38% protein-bound in plasma, primarily to albumin. The extent of protein-binding is independent of its plasma concentration.
Groups	Approved, Investigational
Therapeutic Class	4-Quinolone preparations
Manufacturer
Available Country	Russia
Last Updated:	January 7, 2025 at 1:49 am

Uses

МАКЛЕВО Tablet is used for Acute maxillary sinusitis , Acute bacterial exacerbation of chronic bronchitis , Nosocomial pneumonia Community acquired pneumonia, Uncomplicated urinary tract infections Complicated urinary tract infections, Acute pyelonephritis, Uncomplicated & complicated skin and skin structure infections, Chronic bacterial prostatitis

МАКЛЕВО Injection is used to treat Acute maxillary sinusitis, acute bacterial exacerbation of chronic bronchitis, nosocomial pneumonia, community acquired pneumonia, uncomplicated urinary tract infections, complicated urinary tract infections, acute pyelonephritis, uncomplicated & complicated skin and skin structure infections including abscesses, cellulitis, furuncles, impetigo, pyoderma, wound infections, chronic bacterial prostatitis and typhoid fever.

МАКЛЕВО Injection has

• Proven clinical success in hospital infections
• Reaches high concentrations in lung, urine, skin and prostate
• Ensures excellent gram-positive and gram-negative bacterial coverage, Offers better option for switch therapy

МАКЛЕВО Eye drops is used for the treatment of corneal ulcer caused by susceptible strains of the following bacteria:

• Gram-positive Bacteria: Corynebacterium species, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Viridans group streptococci
• Gram-negative Bacteria: Pseudomonas aeruginosa, Serratia marcescens.

МАКЛЕВО is also used to associated treatment for these conditions: Abscesses caused by susceptible bacteria, Acute Bacterial Exacerbation of Chronic Bronchitis (ABECB) caused by susceptible bacteria, Acute Pyelonephritis caused by Infection Due to Escherichia Coli, Bacterial Conjunctivitis caused by susceptible bacteria, Cellulitis caused by susceptible bacteria, Community Acquired Pneumonia (CAP) caused by susceptible bacteria, Furuncle caused by susceptible bacteria, Impetigo caused by susceptible bacteria, Nosocomial Pneumonia caused by Pseudomonas Infections, Nosocomial Pneumonia caused by susceptible bacteria, Plague caused by Yersinia pestis, Pyoderma caused by susceptible bacteria, Wound Infections caused by susceptible bacteria, Acute bacterial sinusitis caused by susceptible bacteria, Chronic Bacterial prostatitis caused by susceptible bacteria, Chronic Pseudomonas Infections, Complicated Urinary Tract Infection caused by susceptible bacteria, Complicated skin and skin-structure infections caused by susceptible bacteria, Inhaled anthrax caused by Bacillus anthracis, Uncomplicated Urinary Tract Infection caused by susceptible bacteria, Uncomplicated skin and skin-structure infections caused by susceptible bacteria

How МАКЛЕВО works

МАКЛЕВО, like other fluoroquinolone antibiotics, exerts its antimicrobial activity via the inhibition of two key bacterial enzymes: DNA gyrase and topoisomerase IV. Both targets are type II topoisomerases, but have unique functions within the bacterial cell. DNA gyrase is an enzyme found only in bacteria that introduces negative supercoils into DNA during replication - this helps to relieve torsional strain caused by the introduction of positive supercoils during replication, and these negative supercoils are essential for chromosome condensation and the promotion of transcription initiation. It is comprised of four subunits (two A subunits and two B subunits) of which the A subunits appear to be the target of fluoroquinolone antibiotics. Bacterial topoisomerase IV, in addition to contributing to the relaxation of positive supercoils, is essential at the terminal stages of DNA replication and functions to “unlink” newly replicated chromosomes to allow for the completion of cell division.

Inhibition of these enzymes by levofloxacin likely occurs via complexation with the topoisomerase enzymes. The end result is a blockade of DNA replication, thus inhibiting cell division and resulting in cell death.

Dosage

Acute sinusitis: 500 mg once daily for 10-14 days or 750 mg once daily for 5 days

Exacerbation of chronic bronchitis: 500 mg once daily for 7 days

Community acquired pneumonia: 500 mg once daily for 7-14 days or750 mg once daily for 5 days

Nosocomial pneumonia: 750 mg once daily for 7-14 days

Uncomplicated urinary tract infections: 250 mg once daily for 3 days

Complicated urinary tract infections and acute pyelonephritis: 250 mg once daily for 10 days

Complicated urinary tract infections and acute pyelonephritis: 750 mg once daily for 5 days

Uncomplicated skin and skin structure infections: 500 mg once daily for 7-10 daysComplicated skin and skin structure infections: 750 mg once daily for 7-14 days

Chronic bacterial prostatitis: 500 mg once daily for 28 days

МАКЛЕВО solution for infusion is administered by slow intravenous infusion once or twice daily. The dosage depends on the type and severity of the infection and the sensitivity of the causative pathogen. The duration of treatment varies according to the severity of the disease.Adult:

• Community-acquired pneumonia: 500 mg once or twice daily,
• Complicated urinary tract infections (including pyelonephritis): 250 mg once daily,
• Chronic bacterial prostatitis: 500 mg once daily,
• Skin and soft tissue infections: 500 mg twice daily
• Enteric fever: 500 mg once daily.

Children:

МАКЛЕВО can be used in children aged as low as 6 months. The usual dose for children in community acquired pneumonia is:

• Children aged 6 months to less than 5 years: 10 mg/kg b.i.d. (up to 500 mg per day) for 10 days,
• Children aged 5 years to 16 years: 10 mg/kg q.d. (up to 500 mg per day) for 10 days.

The usual dose for children in recurrent or persistent Acute Otitis Media is:

• Children aged 6 months to less than 5 years: 10 mg/kg per day (maximum dose: 500 mg/day) given twice daily for 10 days.

Paediatric Use: МАКЛЕВО is not recommended for children less than 6 (six) months of age.

МАКЛЕВО ophthalmic solution:

• Days 1 through 3: Instill one to two drops in the affected eye(s) every 30 minutes to 2 hours while awake and approximately 4 and 6 hours after retiring.
• Day 4 through treatment completion: Instill one to two drops in the affected eye(s) every 1 to 4 hours while awake.

0.5%ophthalmic solution:

• Days 1 and 2: Instill one to two drops in the affected eye(s) every 2 hours while awake, up to 8 times per day.
• Days 3 through 7: Instill one to two drops in the affected eye(s) every 4 hours while awake, up to 4 times per day.

Administration of МАКЛЕВО (solution for infusion) should be continued for a minimum of 48 to 72 hours after the patient has become febrile or evidence of bacterial eradication has been obtained. МАКЛЕВО solution for infusion is only intended for slow intravenous infusion; it is administered once or twice daily. The infusion time must be at least 30 minutes for 250 mg or 60 minutes for 500 mg МАКЛЕВО solution for infusion. It is possible to switch from an initial intravenous application to the oral route at the same dosage after a few days.

Side Effects

The most frequently reported adverse events were headache and a taste disturbance following instillation. Other adverse events included decreased/blurred vision, diarrhea, dyspepsia, fever, infection, instillation site irritation/discomfort, ocular infection, nausea, ocular pain/discomfort, and throat irritation.

Toxicity

The LD₅₀ following oral administration in mice and rats is 1803 mg/kg and 1478 mg/kg, respectively.

МАКЛЕВО exhibits low potential for acute toxicity - following a single high dose of levofloxacin in several different test animals (e.g. mice, rats, monkeys) observed symptoms included ataxia, ptosis, decreased motor activity, dyspnea, tremors, and convulsions. Treatment of acute overdosage should involve stomach emptying (e.g. with activated charcoal) and general supportive measures. Consider monitoring of the patient's ECG to ensure QTc values remain within range. МАКЛЕВО is not efficiently removed by dialysis (peritoneal or hemodialysis) and is therefore of little benefit in cases of overdose.

Precaution

The following measures should be taken during administration of МАКЛЕВО: While taking МАКЛЕВО adequate amount of water should be drunk to avoid risk of crystalluria. Dose adjustment should be exercised during МАКЛЕВО ingestion in presence of renal insufficiency & hepatic insufficiency.

While taking МАКЛЕВО adequate amount of water should be drunk to avoid risk of crystalluria. Dose adjustment should be exercised during МАКЛЕВО ingestion in presence of renal insufficiency & hepatic insufficiency.

Infusion of fluid should be immediately discontinued if rigor arises for any reason during the process. Do not use if the solution is cloudy, contains particles or after expiry date.

If an allergic reaction to levofloxacin occurs, discontinue the drug. Serious acute hypersensitivity reactions may require immediate emergency treatment. Oxygen and airway management should be administered as clinically indicated.

Prolonged use may result in overgrowth of non-susceptible organisms, including fungi. If superinfection occurs, discontinue use and institute alternative therapy. Patients should be advised not to wear contact lenses if they have signs and symptoms of corneal ulcer. Avoid contaminating the applicator tip with material from the eye, fingers or other source.

Interaction

Specific drug interaction studies have not been conducted with this drug. However, the systemic administration of some quinolones has been shown to elevate plasma concentrations of theophylline, interfere with the metabolism of caffeine, and enhance the effects of the oral anticoagulant warfarin and its derivatives, and has been associated with transient elevations in serum creatinine in patients receiving systemic cyclosporine concomitantly.

Food Interaction

• Take with or without food. Food slightly alters kinetics but not to any clinically significant extent.

[Moderate] ADJUST DOSING INTERVAL: Food may reduce the oral absorption and bioavailability of levofloxacin.

According to the drug product labeling, administration of levofloxacin 500 mg with food prolonged the time to peak concentration by 1 hour and decreased the Cmax decreased by 25% following administration of the oral solution and by 14% following administration of the oral tablet.

MANAGEMENT: To ensure maximal and consistent oral absorption, levofloxacin oral solution should be taken at least one hour before or two hours after meals.

For administration of the oral solution with continuous enteral nutrition, some experts recommend that the tube feeding should be interrupted for one hour before and two hours after the dose of levofloxacin.

The oral tablets may be taken without regard to food.

МАКЛЕВО multivitamins interaction

[Moderate] ADJUST DOSING INTERVAL: Oral preparations that contain magnesium, aluminum, or calcium may significantly decrease the gastrointestinal absorption of quinolone antibiotics.

Absorption may also be reduced by sucralfate, which contains aluminum, as well as other polyvalent cations such as iron and zinc.

The mechanism is chelation of quinolones by polyvalent cations, forming a complex that is poorly absorbed from the gastrointestinal tract.

The bioavailability of ciprofloxacin has been reported to decrease by as much as 90% when administered with antacids containing aluminum or magnesium hydroxide.

When coadministration cannot be avoided, quinolone antibiotics should be dosed either 2 to 4 hours before or 4 to 6 hours after polyvalent cation-containing products to minimize the potential for interaction.

When coadministered with Suprep Bowel Prep (magnesium

Please consult individual product labeling for specific recommendations.

Drug Interaction

Moderate: aspirin, albuterol / ipratropium, albuterol, budesonide / formoterolUnknown: amoxicillin / clavulanate, diphenhydramine, apixaban, omega-3 polyunsaturated fatty acids, furosemide, pregabalin, metoprolol, metoprolol, acetaminophen / hydrocodone, acetaminophen, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, alprazolam, cetirizine

Disease Interaction

Major: colitis, CNS disorders, myasthenia gravis, peripheral neuropathy, QT interval prolongation, tendonitisModerate: crystalluria, diabetes, hemodialysis, renal dysfunction

Volume of Distribution

МАКЛЕВО is widely distributed in the body, with an average volume of distribution following oral administration between 1.09-1.26 L/kg (~89-112 L). Concentrations in many tissues and fluids may exceed those observed in plasma. МАКЛЕВО is known to penetrate well into skin tissue, fluids (e.g. blisters), lung tissue, and prostatic tissue, amongst others.

Elimination Route

Absorption of levofloxacin following oral administration is rapid and essentially complete, with an oral bioavailability of approximately 99%. Due to its nearly complete absorption, the intravenous and oral formulations of levofloxacin may be interchangeable. The T_max is generally attained 1-2 hours following administration and the C_max is proportional to the given dose - an intravenous dose of 500mg infused over 60 minutes resulted in a C_max of 6.2 ± 1.0 µg/mL whereas a 750mg dose infused over 90 minutes resulted in a C_max of 11.5 ± 4.0 µg/mL. Oral administration with food prolongs the T_max by approximately 1 hour and slightly decreases the C_max, but these changes are not likely to be clinically significant.

Systemic absorption following oral inhalation is approximately 50% lower than that observed following oral administration.

Half Life

The average terminal elimination half-life of levofloxacin is 6-8 hours.

Clearance

The average apparent total body clearance of levofloxacin ranges from 8.64-13.56 L/h, and its renal clearance ranges from 5.76-8.52 L/h. The relative similarity of these ranges indicates a small degree of non-renal clearance.

Elimination Route

The majority of administered levofloxacin is excreted unchanged in the urine. Following the administration of a single oral dose of levofloxacin, approximately 87% was eliminated unchanged in the urine within 48 hours and less than 4% was eliminated in the feces within 72 hours.

Pregnancy & Breastfeeding use

МАКЛЕВО is not recommended for use during pregnancy or nursing, as the effects on the unborn child or nursing infant are unknown.

Contraindication

МАКЛЕВО is contraindicated in patients with a history of hypersensitivity to МАКЛЕВО, quinolone antimicrobial agents, or any other components of this product.

Special Warning

Use in Children: From clinical studies, it is evident that МАКЛЕВО can be used in children aged as low as 6 months.The usual dose for children in community acquired pneumonia (CAP) is-

• Children aged 6 months to less than 5 years: 10 mg/kg b.i.d. (up to 500 mg per day) for 10 days.
• Children aged 5 years to 16 years: 10 mg/kg q.d. (up to 500 mg per day) for 10 days.

The usual dose for children in recurrent or persistent Acute Otitis Media (AOM) is Children aged 6 months to less than 5 years: 10 mg/kg per day (maximum dose: 500 mg/day) given twice daily for 10 days.

Acute Overdose

МАКЛЕВО exhibits a low potential for acute toxicity. However, in the events of an acute overdosage, the stomach should be emptied. The patients should be kept under observation and appropriate hydration should be maintained.

Storage Condition

Store in a cool & dry place, protected from light. Keep out of the reach of children.

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