TAVANIC®“ L E V O F L O X A C I N ”

-MODE OF ACTION……. – It interferes with bacterial DNA synthesis by inhibiting 2

important bacterial enzymes:

1. Topoisomerase II, – Topoisomerase II (DNA gyrase) is responsible for

relaxing supercoiled DNA during normal transcription.

2. Topoisomerase IV. – Topoisomerase IV interferes with separation of

chromosomal DNA during cell division.

-PHARMACOKINETICS……. RA P I D , C O M P L E T E A B S O R P T I O N A F T E R

O R A L A D M I N I S T R AT I O N 1 0 0 % B I O AVA I L A B L E T- M A X : 1 H O U R I V A N D O RA L F O R M U L AT I O N S A R E

B I O E Q U I VA L E N T S W I TC H / S E Q U E N T I A L T H E R A P Y .

M I N I M A L H E PAT I C M E TA B O L I S M ; 2 M E TA B O L I T E S I D E N T I F I E D I N U R I N E ( < 5 % O F T O TA L L E V O F L OX A C I N )

H A L F L I F E I S 6 – 8 H O U R S O N C E D A I LY D O S A G E

-PHARMACOKINETICS……. With equal dosing of oral levofloxacin and IV

levofloxacin (mg per mg), the area under the serum concentration-time curve (AUC) is comparable

Therefore, the oral & IV routes are interchangeable.

skin infections

sinusitis

severe pneumonia

Bronchitis

Typhoid fever

UTI chronic prostatitis

pyelonephritis

Indications

-TAVANIC SPECTRUM……1. For sinusitis

– due to S. pneumoniae, H. influenzae or M. catarrhalis. 2. For bronchitis

– due to S. aureus, S. pneumoniae, H. influenzae, H. parainfluenzae or M. catarrhalis.

3. For severe pneumonia – pathogens, which include the aforementioned organisms in

addition to K. pneumoniae, C. pneumoniae, L. pneumophila, or M. pneumoniae.

4. For uncomplicated / complicated skin infections – caused by S. aureus or S. pyogenes where Levofloxacin

superior to ciprofloxacin in infections caused by S. aureus5. For UTI, chronic prostatitis and pyelonephritis

– Due to E. faecalis, E. cloacae, E. coli, K. pneumoniae, Proteus mirabilis or Pseudomonas nut not active against MRSA.

6. For typhoid– Extremely effective against gram -ve bacteria making it an

excellent antibiotic for infections of the gastrointestinal tract

-DOSAGE……..

-COVERAGE OF MAIN RTI PATHOGENS…….

-LEVOFLOXACIN IN UTI……. L E V O F L OX A C I N D E M O N S T R AT E D R A P I D

B A C T E R I C I D A L A C T I V I T Y A G A I N S T E C O L I I N T H E U R I N E ( W I T H M I C S ≤ 3 2 Μ G / M L AT 1 . 5 H R ) .

0 4 8 12 16 20 24 time (hr)

050

100150200250300350400450500

levofloxacinciprofloxacin

Urin

e co

ncen

tratio

n (µ

g\m

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-SIGNIFICANTLY HIGH SUCCESS IN PROSTATITIS…..

• Various studies for chronic bacterial prostatitis have shown that mean duration of drug administration = 40 days.

• Clinical cure at 8 weeks = 88.9%• Bacteriological eradication rate = 79.2% • The take home message –

– Minimum duration of therapy is 6-8 weeks– Significant decrease in PSA after treatment

with levofloxacin.

-ACTIVITY IN COMPLICATED SSTI………

• One study compared levofloxacin & Ticarcillin / Amoxy-claevulanic acid regimens in complicated SSTIs.

-TYPHOID AND LEVOFLOXACIN………

-SIDE EFFECTS AND ADRS………• Gastrointestinal distress, • Skin rashes, phototoxicity, • Headache, dizziness, insomnia, • Tendinitis. • Theophylline increases concentration of

ciprofloxacin but not of levofloxacin • May be associated with QT interval

prolongation.• Absorption with agents containing Al,

Mg, Ca, Zn, Fe.

-SUMMARY………