Levaquin

Levaquin Uses, Dosage, Side Effects, Food Interaction and all others data.

Levaquin 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.

Levaquin 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. Levaquin 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).

Levaquin 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.

Trade Name Levaquin
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
Weight 250mg, 500mg, , 25mg/ml, 750mg, 250mg/50ml, 500mg/100ml, 750mg/150ml
Type Tablet, Film Coated, Intravenous, Injection, Oral Solution, Oral Tablet, Intravenous Solution
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 Micro Labs, Barrett Hodgson Pakistan (pvt) Ltd,, Saja-saudi Arabian Japanese Pharmaceutical Co
Available Country India, Pakistan, Canada, Saudi Arabia, United States,
Last Updated: September 19, 2023 at 7:00 am
Levaquin
Levaquin

Uses

Levaquin 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

Levaquin 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.

Levaquin 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

Levaquin 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.

Levaquin 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 Levaquin works

Levaquin, 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

Levaquin 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

Levaquin 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:

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

Levaquin 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 Levaquin (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. Levaquin 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 Levaquin 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.

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

While taking Levaquin adequate amount of water should be drunk to avoid risk of crystalluria. Dose adjustment should be exercised during Levaquin 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.

Levaquin 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.

Volume of Distribution

Levaquin 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. Levaquin 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 Tmax is generally attained 1-2 hours following administration and the Cmax is proportional to the given dose - an intravenous dose of 500mg infused over 60 minutes resulted in a Cmax of 6.2 ± 1.0 µg/mL whereas a 750mg dose infused over 90 minutes resulted in a Cmax of 11.5 ± 4.0 µg/mL. Oral administration with food prolongs the Tmax by approximately 1 hour and slightly decreases the Cmax, 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

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

Contraindication

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

Special Warning

Use in Children: From clinical studies, it is evident that Levaquin 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

Levaquin 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.

Innovators Monograph

You find simplified version here Levaquin

Levaquin contains Levofloxacin see full prescribing information from innovator Levaquin Monograph, Levaquin MSDS, Levaquin FDA label

FAQ

What is Levaquin used for?

Levaquin is used to treat certain infections such as pneumonia, and kidney, prostate , and skin infections.

How safe is Levaquin?

Levaquin generally safe.It can cause serious side effects, including tendon problems, side effects on your nerves , serious mood or behavior changes, or low blood sugar (which can lead to coma).

How does Levaquin work?

Levaquin works by stopping the growth of bacteria.Levaquin treats only bacterial infections.

What are the common side effects of Levaquin?

Common side effects of Levaquin may include:

  • nausea, constipation, diarrhea;
  • headache, dizziness; or.
  • trouble sleeping.

Is Levaquin safe during pregnancy?

Levaquin should be used during pregnancy only if the benefit outweighs the risk to the fetus.According to some authorities, use is contraindicated.

Is Levaquin safe during breastfeeding?

Use of Levaquin is acceptable in nursing mothers with monitoring of the infant for possible effects on the gastrointestinal flora, such as diarrhea or candidiasis.Avoiding breastfeeding for 4 to 6 hours after a dose should decrease the exposure of the infant to levofloxacin in breastmilk.

Can I drink alcohol with Levaquin?

It is safe to drink alcohol in moderation while taking Levaquin.

Can I drive after taking Levaquin?

Do not drive or operate machinery if levofloxacin makes you feel dizzy or tired. Avoid alcohol.

When should be taken of Levaquin?

You can take Levaquin before or after meals. If you are taking one dose a day, it is preferable to take it in the morning. If you are taking more than one dose a day, try to space out your doses so ideally, take a tablet every 12 hours.

Should I take Levaquin at night?

Levaquin is best to take the doses at evenly spaced times, day and night.

Can Levaquin be taken on an empty stomach?

You may take Levaquin tablets with or without food. Take Levaquin oral solution (liquid) on an empty stomach, at least 1 hour before or 2 hours after a meal.

How long does it take for Levaquin to work?

Levaquin will begin working within a matter of hours, but it can be two to three days before symptoms begin to improve. Take the full course of antibiotics as prescribed by a healthcare provider, even if you feel better after a few days.

How long does Levaquin stay in my system?

If the patient generally has good health, the body can eliminate Levaquin in about 30 to 40 hours, or about a day and a half to two days, but some side effects of the drug can show up as long as two months or longer after taking Levaquin.

What happens if I take too much Levaquin?

Liver damage can happen in people who take Levaquin. Call your doctor right away if you have unexplained symptoms such as: nausea or vomiting. stomach pain.

Is Levaquin bad for kidneys?

Case reports have indicated acute kidney injury with use, and prescription labels carry a warning of kidney failure.

Who should not use Levaquin?

Should only be used by adults. Not suitable for people with myasthenia gravis, certain heart rhythm disturbances, or pediatric patients.

Is Levaquin safe for heart patients?

In general, clinicians should be aware that azithromycin and Levaquin are relatively safe for patients without complications or additional risk factors of QT prolongation, and decision regarding the initiation of medication therapy should be made on a case by case basis.

Can Levaquin cause heart palpitations?

If you have low blood potassium or an abnormally slow heartbeat,Levaquin may increase your risk of having a fast, slow, or irregular heartbeat, loss of consciousness, or fainting spells. If these symptoms occur, tell your doctor right away.

What happens if I stop taking Levaquin?

If you experience any of the following symptoms, stop taking Levaquin and call your doctor immediately: numbness, tingling, pain, burning, or weakness in the arms or legs; or a change in your ability to feel light touch, vibrations, pain, heat, or cold.

What happens if I miss a dose of Levaquin?

If you miss a dose of your Levaquin, take it as soon as you remember. If you remember relatively close to the time you take your next dose then you should skip the missed dose. You should then take your next dose and continue on with your normal dosing schedule. Do not double up on doses if you have missed one to avoid an overdose.

*** Taking medicines without doctor's advice can cause long-term problems.
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