Name : Hafsa Farid

Roll no :5855

Levofloxacin
Introduction:
Second generation of Flouroquinolones
Levofloxacin, gatifloxacin, gemifloxacin, and moxifloxacin—called respiratory
fluoroquinolones

 Synthetic fluorinated analogs of Nalidixic acid

 Achieve bactericidal levels in blood and tissues
Mechanism of Action:
 Quinolones block bacterial DNA synthesis by inhibiting bacterial topoisomerase
II (DNA gyrase) and topoisomerase IV.
 Inhibition of DNA gyrase (topoisomerase IV) prevents the relaxation of
positively supercoiled DNA that is required for normal transcription and
replication.
 Inhibition of topoisomerase IV interferes with separation of replicated
chromosomal DNA into the respective daughter cells during cell division.

Antibacterial Spectrum:
→Excellent gram-ve activity and →Moderate to Good activity ag. Gram+ve
bacteria
 →MICs for Gram-ve—1-2mcg/ml
 Enterobacter sp.
 P. aeruginosa
 Neisseria meningitidis
 Haemophilus sp
 Campylobacter jejuni
 Chlamydia
 Legionella pneumophila
 MSSA

(Ciprofloxacin—most active ag. Gram –ve (P aeruginosa in particular)

(Levofloxacin –L-isomer of ofloxacin:
Superior activity ag. Gram+vee.g. S pneumoniae,
MSSA,
Stenotrophomonas maltophilia
Mycobacterium tuberculosis
Mycobacterium avium complex (MAC)
Resistance:
i. Resistant organisms emerge in about one of every 107 –109 organisms,
especially among staphylococci, P aeruginosa , and Serratia marcescens
Resistance to one fluoroquinolone, particularly if it is of high level, generally
confers cross-resistance to all other members of this class
Resistance is due to:
ii. One or more point mutations in the quinolone binding region of the
target enzyme—confer high-level resistance.
To a change in the permeability of the organism
iii. More recently two types of plasmid-mediated resistance have been
described. Both mechanisms confer low-level resistance.
iv. The first type utilizes Qnr proteins, which protect DNA gyrase from the
fluoroquinolones.
v. The second is a variant of an aminoglycoside acetyltransferase capable
of modifying ciprofloxacin.
Pharmacokinetics:
Route: Oral, IV, drops
Absorption: Well absorbed
Bioavailability: 80–95%
Distribution: Body fluids& tissues
Serum half-lives: 3 – 10 hrs
→relatively long half-lives of levo, gemi, gati, and moxi—permit once-
daily dosing
Absorption impaired by: divalent and trivalent cations, including those
in antacids
→Therefore, oral fluoroquinolones should be taken 2 hrs bfr or 4 hours
after any products containing these cations
Elimination: Renal either tubular secretion or glomerular filtration
→ moxifloxacin—Nonrenal
Dosage adjustment: Required for patients with creatinine clearances
˂50 mL/min
Clinical uses:
 UTI (P aeruginosa)
 Typhoid fever --Norfloxacin
 Diarrhea (Shigella , Salmonella , toxigenic E coli, Campylobacter)
  Infections of soft tissues, bones, and joints and in intra-
abdominal and respiratory tract infections, (Pseudomonas and
Enterobacter)
●→ Ciprofloxacin is a drug of choice for:
prophylaxis and treatment of anthrax
●→Ciprofloxacin, levofloxacin:
Chlamydial urethritis or cervicitis
●→ Ciprofloxacin, levofloxacin, or moxifloxacin:
Treatment of TB and atypical mycobacterial infections
eradication of meningococci from carriers or for prophylaxis of infection
in neutropenic cancer patient
●→Respiratory fluoroquinonlones:
treatment of upper and lower RTI
Adverse effects:
a. GIT: nausea, vomiting, and diarrhea
b. headache, dizziness, insomnia, skin rash, or abnormal liver
function tests
c. Photosensitivity (lomefloxacin and pefloxacin)
d. QTc prolongation may occur (with Respiratory
fluoroquinonlones)
e. Hyperglycemia in diabetic patients (Gatifloxacin)
f. Damage growing cartilage -- cause an arthropathy
g. Tendonitis -- reported in adults, potentially more serious
because of the risk of tendon rupture

Contraindications:
Levofloxacin is contraindicated in patients with a history of
hypersensitivity to this drug and other quinolone antibacterial or to
any excipient of the product.
Dose:
Adults : 250-750mg once a day
Pediatric : 8mg/kg 2 times a day
Brand name :
Levid, Lofox, Phlevo, Levaquin
Reference :
PHRAMA PEDIA
 https://www.mayoclinic.org/drugs-
supplements/levofloxacin-oral-route/proper-use/drg-20064518