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Levofloxacin (Levaquin)
- Generic name: Levofloxacin
- Brand names: Levaquin, Tavanic; Oftaquix, Quixin, Iquix
- Dosages:
Tablets 250 mg, 500 mg, 750 mg;
Solution, oral 25 mg/mL;
Injection (concentrate) 500 mg (25 mg/mL), 750 mg (25 mg/mL);
Injection (premix) 250 mg (5 mg/mL), 500 mg (5 mg/mL), 750 mg (5 mg/mL).
- Pharmacologic category: Fluoroquinolone antibiotic
- FDA approved: December 20, 1996
- Pregnancy risk factor: C
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Medical uses
Levofloxacin is a broad-spectrum a fluoroquinolone antibiotic
marketed by Ortho-McNeil under the brand name Levaquin.
Levofloxacin indicated uses include:
- Respiratory Tract Infections: community-acquired pneumonia
(CAP), nosocomial pneumonia, acute exacerbations of chronic
bronchitis (AECB), acute sinusitis.
- Genitourinary Tract infections: chronic bacterial prostatitis,
uncomplicated UTI, acute pyelonephritis, complicated UTI
- Complicated skin & skin structure infections
- Uncomplicated skin and skin structure infections
Nausea, diarrhea, headache, insomnia, and dizziness are
the most common side effects associated with levofloxacin 4. |
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Pharmacological characteristics
- Absorption: Rapid and complete.
- Metabolism: Undergoes limited hepatic metabolism.
- Elimination half-life: 6 to 8 h
- Excretion: 87% excreted as unchanged drug in urine,
less than 4% in the feces.
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Benefits
- broad spectrum of activity
- one of the safest new fluoroquinolones 4
- less phototoxicity potential 3
- less CNS disturbances 3
- less cardiac effects 3
- does not have any major drug interactions (with warfarin,
theophylline, or cyclosporin), compared to some of the other fluoroquinolones
- rapidly absorbed and extensively distributed into the tissues,
the concentrations of the drug are typically found to be higher
in the tissues or body fluids than in plasma
- increased drug concentration - higher concentrations of levofloxacin
also may help prevent the emergence of resistant organisms,
a serious problem associated with fluoroquinolone use
- two mechanisms of action for bactericidal activity, one requiring
RNA and protein synthesis, and another which does not
- excellent bioavailability both orally and intravenously
- highly active against Klebsiella species
- active against the organisms causing atypical pneumonias
- may be useful in persons with liver disease in whom other
fluoroquinolones may be contraindicated
- enhanced activity against gram-positive bacteria (including
Streptococcus pneumoniae) compared with the older fluoroquinolones
- once-daily dose regimen
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Concerns
- tendon rupture, tendonitis and arthropathies (can occur during
or after the treatment with levofloxacin)
- peripheral neuropathy (nerve damage)
- expensive
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Unlabeled uses
- Disseminated gonococcal infections
- Pelvic inflammatory disease
- Typhoid fever 2
- Gynecological infections 5
- Legionnaires disease 6
- Community-acquired pneumonia in children 7
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Mode of action
Levofloxacin is the L-isomer of the racemate, ofloxacin, a quinolone
antibiotic. The antibacterial activity of ofloxacin resides primarily
in the L-isomer. The mechanism of action of levofloxacin and other
fluoroquinolone antimicrobials involves the inhibition of bacterial
topoisomerase IV and DNA gyrase (both of which are Type II topoisomerases),
enzymes required for DNA replication, transcription, repair, and
recombination.
As the S (-) enantiomer of the fluoroquinolone, ofloxacin, levofloxacin,
inhibits DNA-gyrase in susceptible organisms thereby inhibits
relaxation of supercoiled DNA and promotes breakage of DNA strands.
DNA gyrase (topoisomerase II), is an essential bacterial enzyme
that maintains the superhelical structure of DNA and is required
for DNA replication and transcription, DNA repair, recombination,
and transposition. |
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Reviews & Discussions
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References
- Levaquin official website
- 1. U.S. FDA.
Levofloxacin (Levaquin) Prescribing Information
- 2. Nelwan RH, Chen K, Nafrialdi, Paramita D. Open study on efficacy and
safety of levofloxacin in treatment of uncomplicated typhoid fever. Southeast Asian J Trop Med Public
Health. 2006 Jan;37(1):126-30.
- 3. Yagawa K. Latest industry information on the safety profile of levofloxacin in
Japan. Chemotherapy. 2001;47 Suppl 3:38-43; discussion 44-8.
- 4. Kahn JB. The safety profile of levofloxacin in the US.
Chemotherapy. 2001;47 Suppl 3:32-7; discussion 44-8.
- 5. Mikamo H, Sato Y, Hayasaki Y, Hua YX,
Tamaya T. Levofloxacin in the different treatment schedules of Chlamydia trachomatis uterine cervicitis.
Chemotherapy. 2000 Mar-Apr;46(2):150-2.
- 6. Yu VL, Greenberg RN, Zadeikis N, Stout JE, Khashab MM, Olson WH, Tennenberg AM.
Levofloxacin efficacy in community-acquired legionellosis.
Chest. 2004 Jun;125(6):2135-9.
- 7. Bradley JS, Arguedas A, Blumer JL, Sa'ez-Llorens X, Melkote R, Noel GJ.
Comparative study of levofloxacin in the treatment of children with community-acquired pneumonia.
Pediatr Infect Dis J. 2007 Oct;26(10):868-78. PubMed
Last modified: August, 2011 |
Interesting facts
- Levofloxacin was developed in Japan, and a myriad of large clinical
studies are available evaluating its efficacy in the Japanese population.
- In Europe, it is marketed by Sanofi-Aventis under the trade name
of "Tavanic", and in Asia it is marketed by Daiichi under the trade name of Cravit.
- Chemically, levofloxacin is the S-enantiomer (L-isomer) of ofloxacin,
and has approximately twice the potency of ofloxacin.
- Levofloxacin is currently the only respiratory fluoroquinolone
approved by the US FDA for the treatment of nosocomial pneumonia.
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