Название документа

Pharmacological properties

Pharmacodynamics

Levofloxacin — synthetic antibacterial medicine from group of ftorkhinolon which is s-enantiomerom of racemic mix of an ofloksatsin.

action Mechanism

Levofloksatsin affects with

complex DNK-DNK-girazy and topoisomerase IV.

Ratio the pharmacokinetics/pharmacodynamics

Degree of bacterial activity of a levofloksatsin depends on a ratio With _max in blood plasma or AUC and MIK.

resistance Mechanism

Main mechanism of resistance is

a consequence of a mutation in gyr-A genes. In vitro exists cross resistance between levofloksatsiny and other ftorkhinolona. Thanks to the action mechanism the cross resistance between levofloksatsiny and other classes of antibacterial means usually is not noted.

Boundary values the MIK boundary values Recommended by the European committee on testing of antimicrobic sensitivity (EUCAST) for a levofloksatsin which separate sensitive microorganisms from organisms it is intermediate sensitive (moderately resistant) and is intermediate sensitive from resistant organisms, are provided in the table of testing of MIK (mg/l).

MIK EUCAST Clinical boundary values for a levofloksatsin (20.06.2006)

Pathogen	Sensitive, mg/l	Resistant, mg/l
Enterobacteriacae	≤1	2
Pseudomonas spp.	≤1	2
Acinetobacter spp.	≤1	2
Staphylococcus spp.	2
S. pneumoniae ¹	≤2	2
Streptococcus A, B, C, G	≤1	2
H. influenzae M. catarrhalis ²	≤1	2
Boundary values which are not connected with types ³	≤1	2

¹ MIK Boundary value between sensitive is also intermediate ≤1 sensitive (moderately resistant) strains was increased from 1.0 to 2.0 for the purpose of growth inhibition of wild strains of this microorganism that shows variability of this parameter. Boundary values concern therapy in high doses.

² Strains with sizes MIK above boundary value between sensitive it is also intermediate sensitive (moderately resistant) strains note very seldom or about them it was not reported. It is necessary to repeat tests for identification and antimicrobial sensitivity on any such isolate and if the result is confirmed, to send it to help laboratory.

MIK Boundary values which are not connected with types were determined by

³ mainly proceeding from data of a pharmacokinetics/pharmacodynamics and are independent of distribution of MIK of certain types. They are used only for types by which the boundary value specific for the sake of appearances was not determined, and not used for types where testing for sensitivity is not recommended or for which there are not enough proofs of rather doubtful types (Enterococcus, Neisseria, gram-negative anaerobe bacterias).

Recommended CLSI (Institute of clinical and laboratory standards, earlier — NCCLS) the MIK boundary values for a levofloksatsin which separate sensitive from it is intermediate sensitive organisms, and is intermediate sensitive from resistant organisms, are provided in the table below for testing of MIK (mkg/ml) or disco - a diffusion method (diameter of a zone (mm) with use of a disk from levofloksatsiny 5 mkg).

MIK boundary values and disco Recommended to CLSI - a diffusion method for a levofloksatsin (M100-S17, 2007):

Pathogen	Sensitive	Resistant
Enterobacteriacae	≤2 mkg/ml ≥17 mm	≥8 mkg/ml ≤13 mm
He Enterobacteriacae	≤2 mkg/ml ≥17 mm	≥8 mkg/ml ≤13 mm
Acinetobacter spp.	≤2 mkg/ml ≥17 mm	≥8 mkg/ml ≤13 mm
Stenotrophomonas maltophilia	≤2 mkg/ml ≥17 mm	≥8 mkg/ml ≤13 mm
Staphylococcus spp.	≤2 mkg/ml ≥17 mm	≥8 mkg/ml ≤13 mm
Enterococcus spp.	≤2 mkg/ml ≥17 mm	≥8 mkg/ml ≤13 mm
H. influenzae M. catarrhalis ¹	≤2 mkg/ml ≥17 mm	≥8 mkg/ml ≤13 mm
Streptococcus pneumoniae	≤2 mkg/ml ≥17 mm	≥8 mkg/ml ≤13 mm
β-hemolytic Streptococcus	≤2 mkg/ml ≥17 mm	≥8 mkg/ml ≤13 mm

¹ Absence or rare distribution of resistant strains excludes previously determination of any other categories of results, except "sensitive". For strains which yield the results demonstrating insensitive category the identification of organisms and results of tests for antimicrobic sensitivity have to be confirmed with help laboratory with use of a reference method of cultivations of CLSI.

Antibacterial range

Prevalence of resistance can geographically vary

also on time for the chosen types; also it is desirable receive

Characteristics
Active ingredients	Levofloxacin
Amount of active ingredient	5 mg/ml
Applicant	Yury-pharmaceutical
Code of automatic telephone exchange	J01MA12 Levofloxacin
Interaction with food	It doesn't matter
Light sensitivity	Sensitive
Market status	The branded generic
Origin	Chemical
Prescription status	According to the prescription
Primary packing	bottle
Producer	YURY OF PHARMACEUTICAL LTD COMPANY
Quantity in packing	100 ml
Release form	solution for infusions
Route of administration	Infusional
Sign	Domestic
Storage temperature	from 5 °C to 25 °C
Trade name	Leflotsin