Levofloxacin (Levaquin)


Indicated for the treatment of acute bacterial sinusitis due to Streptococcus pneumoniae, Haemophilus influenzae or Moraxella catarrhalis.

Utilization associated with high concentrations in blood and sinuses.

A broad-spectrum antibiotic of the fluoroquinolone drug class.

Levofloxacin, sold under the trade names Levaquin.

It is active against both Gram-positive and Gram-negative bacteria.

It functions by inhibiting the DNA gyrase and topoisomerase IV, the latter is necessary to separate DNA that has been replicated prior to bacterial cell division.

If the DNA not being separated, the bacterium cannot divide.

DNA gyrase is responsible for supercoiling the DNA, and it’s inhibition amounts to killing the bacterium.

It acts as a bactericidal agent.

An antibiotic used to treat a number of bacterial infections including acute bacterial sinusitis, pneumonia, urinary tract infections, respiratory infections, chronic prostatitis, and some types of gastroenteritis, cellitis, anthrax, endocarditis, meningitis, pelvicj inflammatory disease, traveler’s diarrhea, tuberculosis, and plague.o

It is available by mouth, intravenous and in eye drop form.

US FDA: Pregnancy category US: C (Risk not ruled out)

A Fluoroquinolone.

Bioavailability 99%.

Protein binding 31%.

Metabolism <5% desmethyl and N-oxide metabolites?

Elimination half-life is 6.9 hours.

Excretion is renal and mostly unchanged (83%).

Common side effects include:nausea, diarrhea, and trouble sleeping.

Serious side effects include: tendon rupture, tendon inflammation, seizures, psychosis, and potentially permanent peripheral nerve damage.

The experience of tendon damage may appear months after treatment is completed.

Exposed patients may also sunburn more easily.

Myasthenia gravis muscle weakness and breathing problems may worsen.

Use during pregnancy is not recommended, but risk appears to be low.

The safety of use in breastfeeding is unclear.

US Food and Drug Administration (FDA) recommended that serious side effects associated with fluoroquinolone antibacterial drugs generally outweigh the benefits for patients with acute sinusitis, acute bronchitis, and uncomplicated urinary tract infections who have other treatment options.

It is recommended that fluoroquinolones should be reserved for those who do not have alternative treatment options, for the above problems.

Levofloxacin and other respiratory fluoroquinolines as first line treatment for community acquired pneumonia when co-morbidities such as heart, lung, or liver disease are present or when in-patient treatment is required.

It plays an important role in recommended treatment regimens for ventilator-associated and healthcare-associated pneumonia.

It is recommended as a first-line treatment option for catheter-associated urinary tract infections in adults.

It is recommended in combination with metronidazole it is recommended as one of several first-line treatment options for adult patients with community-acquired intra-abdominal infections of mild-to-moderate severity.

It is recommended in combination with rifampicin as a first-line treatment for prosthetic joint infections, and as a first-line treatment to prevent bacterial prostatitis when the prostate is biopsied.

Due to its widespread use, common pathogens such as Escherichia coli and Klebsiella pneumoniae have developed resistance, and resistance rates among healthcare-associated infections with these pathogens exceeds 20%.

Levofloxacin is also used as antibiotic eye drops to prevent bacterial infection.

Pregnancy category C, and is not recommended for breast feeding mothers.

Not approved in most countries for the treatment of children except in unique and life-threatening infections because it is associated with an elevated risk of musculoskeletal injury in this population.

Approved for the treatment of anthrax and plague in children over six months of age.

Recommended as a first-line treatment for pediatric pneumonia caused by penicillin-resistant Streptococcus pneumoniae, and as a second-line agent for the treatment of penicillin-sensitive cases.

It is less active than ciprofloxacin against Gram-negative bacteria, especially Pseudomonas aeruginosa.

Has moderate activity against anaerobes, and is about twice as potent as ofloxacin against Mycobacterium tuberculosis and other mycobacteria, including Mycobacterium avium complex.

Its spectrum includes most strains of bacterial pathogens responsible for respiratory, urinary tract, gastrointestinal, and abdominal infections, including Gram negative organisms Escherichia coli, Haemophilus influenzae, Klebsiella pneumoniae, Legionella pneumophila, Moraxella catarrhalis, Proteus mirabilis, and Pseudomonas aeruginosa, and Gram positive organisms as methicillin-sensitive but not methicillin-resistant Staphylococcus aureus, Streptococcus pneumoniae, Staphylococcus epidermidis, Enterococcus faecalis, and Streptococcus pyogenes, and atypical bacterial pathogens Chlamydophila pneumoniae and Mycoplasma pneumoniae.

Levofloxacin is available in tablet form, injection, and oral solution.

Like all fluoroquinolines, levofloxacin is contraindicated in patients with epilepsy or other seizure disorders.

Use is contraindicated patients who have a history of quinolone-associated tendon rupture.

May prolong the QT interval in some people, especially the elderly.

Should not be used for people with a family history of Long QT syndrome, or who have long QT, chronic low potassium, it should not be prescribed with other drugs that prolong the QT interval.

Doess not appear to deactivate the drug metabolizing enzyme CYP1A2, like ciprofloxacin.

Therefore, drugs that use that enzyme, like theophylline, do not interact with levofloxacin.

A weak inhibitor of CYP2C9, suggesting potential to block the breakdown of warfarin.

The use of non-steroidal anti-inflammatory drugs in combination with high dose fluoroquinolone therapy may lead to seizures.

When taken with anti-acids containing magnesium hydroxide or aluminum hydroxide, the two combine to form insoluble salts that are difficult to absorb from the intestines, with peak serum concentrations of levofloxacin may be reduced by 90%.

Similar impaired absorption results have been reported when levofloxacin is taken with iron supplements and multi-vitamins containing zinc.

Side effects can involve the tendons, muscles, joints, nerves, and central nervous system.

Tendon rupture, has been observed up to 6 months after cessation of treatment.

The risk of tendon rupture is increased in the elderly, transplant patients, corticosteroid use, and with high doses.

Risk of exacerbation of the symptoms of myasthenia gravis.

Uncommon but serious adverse events include: anaphylaxis, hepatotoxicity, central nervous system effects including seizures and psychiatric effects, prolongation of the QT interval, blood glucose disturbances, and photosensitivity.

In trials 4.3% discontinued treatment due to adverse drug reactions.

Adverse reactions leading to discontinuation are gastrointestinal, including nausea, vomiting, and constipation.

As with broad spectrum antibiotics, it is associated with Clostridium difficile associated diarrhea.

Fluoroquinoline administration may be associated with the acquisition of a virulent Clostridium strain.

It is not efficiently removed by hemodialysis or peritoneal dialysis in cases of overdose.

It is rapidly and essentially completely absorbed after oral administration.

Its oral administration plasma concentration profile over time that is essentially identical to that obtained from intravenous administration.

It undergoes widespread distribution into body tissues.

Peak levels in skin are achieved 3 hours after administration and exceed those in plasma by a factor of 2.

Lung tissue concentrations range from two-fold to five-fold higher than plasma concentrations in the 24 hours after a single dose.

The half-life of levofloxacin ranges from approximately 6 to 8 hours following single or multiple doses of levofloxacin given orally or intravenously.

Elimination occurs mainly via excretion of unmetabolized drug in the urine.

It is a second-generation fluoroquinolone, being one of the isomers of ofloxacin.


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