Description
Levofloxacin Pharmacodynamics
Levofloxacin is a synthetic antibiotic of the group of fluoroquinolones, optically active left-handed isomer ofloxacin – (-)-(8)-enantiomer. It has a wide spectrum of antimicrobial activity.
It inhibits DNA-enzyme (topoisomerase II) and topoisomerase IV, breaks supercoiling and cross-linking of DNA, inhibits DNA replication, causes profound morphological changes in cytoplasm, cell wall and membranes of microorganisms.
Levofloxacin is active against most strains of microorganisms both in vitro and in vivo.
Indications
Treatment of infectious and inflammatory diseases caused by microorganisms sensitive to levofloxacin:
– community-acquired pneumonia;
– complicated urinary tract infections, including pyelonephritis;
– chronic bacterial prostatitis;
– Skin and soft tissue infections;
– For the complex treatment of drug-resistant forms of tuberculosis;
– Prevention and treatment of anthrax with an airborne route of infection.
For treatment of the following infectious and inflammatory diseases Levofloxacin may be used only as an alternative to other antimicrobial agents:
– uncomplicated cystitis.
When using Levofloxacin, the official national recommendations on the appropriate use of antibacterial agents as well as the sensitivity of pathogens in a particular country should be taken into account (see section “Special indications”).
Contraindications
Hypersensitivity to levofloxacin, excipients of the drug or other quinolones; epilepsy; tendon lesions when using fluoroquinolones in the anamnesis; pseudoparalytic myasthenia gravis; childhood and adolescence before 18 years of age (due to incomplete skeletal growth, as the risk of cartilaginous growth points damage cannot be completely excluded); pregnancy (the risk of fetal cartilaginous growth points damage cannot be completely excluded); breastfeeding (the risk of cartilaginous bone growth points damage in the child cannot be completely excluded).
Dosage and administration method
- Intravenous drip.
- Dosage regimen and duration of treatment are determined by the localization, nature and severity of the infection, as well as the sensitivity of the suspected pathogen. Treatment shall not be interrupted or terminated prematurely without the physician’s instructions.
- Depending on the patient’s condition and the possibility of taking medicines per os, after several days of treatment it is possible to switch from intravenous infusion to taking the same dose of the drug in tablets (due to the fact that the bioavailability of levofloxacin when taking tablets is 99-100 %).
- If the drug is accidentally missed, the missed dose should be administered as soon as possible and then levofloxacin should be continued according to the recommended dosing regimen.
- Recommended dosing regimen and duration of treatment in patients with normal renal function (CKG >50 ml/min):
Indications
Single dose
Frequency
Daily dosage
Duration - Community-acquired pneumonia
500 mg
1-2 times a day
500-1000 mg
7-14 days - Skin and soft tissue infections
500 mg
1 -2 times/day
500-1000 mg
7-14 days - Complicated urinary tract infections
500 mg
1 time/day
500 mg
7-14 days - Pyelonephritis
500 mg
1 time/day
500 mg
7-10 days - Uncomplicated urinary tract infections
250 mg
1 time/day
250 mg
3 days - Chronic bacterial prostatitis
500 mg
1 time/day
500 mg
28 days - Complex treatment of drug-resistant forms of tuberculosis
500 mg
1 -2 times/day
500-1000 mg
Up to 3 months.
Prophylaxis and treatment of anthrax in case of airborne infection
500 mg
1 time/day
500 mg
Up to 8 weeks. - Dosing regimens in patients with impaired renal function (CK=50 ml/min): levofloxacin is mainly excreted by kidneys; therefore during treatment of patients with impaired renal function the drug dose should be decreased (see table below).
Creatinine clearance, ml/min - Dosing regimen
250 mg / 24 hours
500 mg / 24 hours
500 mg / 12 h
first dose 250 mg
first dose 500 mg
first dose 500 mg
50-20 ml/min
then 125 mg every 24 hours.
Then 250 mg every 24 hours
then 250 mg every 12 hours
19-10
125 mg every 48 hours
125 mg every 24 hours
125 mg every 12 h
< 10
125 mg every 48 hours
125 mg every 24 hours
125 mg every 24 h
Haemodialysis*
125 mg every 48’h
125 mg every 24 hours
125 mg every 24 hours
Peritoneal dialysis*
125 mg every 48 hours
125 mg every 24 hours
125 mg every 24 hours
* – No additional doses are required after hemodialysis or continuous ambulatory peritoneal dialysis (CAPD). - Patients with liver dysfunction do not require dosage regimen adjustment since levofloxacin is only slightly metabolized in the liver.
- Elderly patients do not require dosing regimen adjustment, except in cases of reduced IQ to 50 ml/min or lower.
