Pefloxacin Property

Melting point:

270-272° (dec)

Boiling point:

529.1±50.0 °C(Predicted)

Density 

1.320±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

Aqueous Acid (Slightly), Methanol (Slightly), Water (Slightly)

form 

Solid

pka

0.16±0.20(Predicted)

color 

White to Off-White

CAS DataBase Reference

70458-92-3(CAS DataBase Reference)

Safety

Toxicity

LD50 in mice (mg/kg): 225 i.v., 1000 orally; in rats (g/kg): 1.5 i.p., 2.5 orally (Goueffon)

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

Pefloxacin Chemical Properties,Usage,Production

Uses

antibacterial;DNA gyrase inhibitor

Uses

Pefloxacin Mesylate Dihydrate is an analog of norfloxacin that inhibits topoisomerase.

Definition

ChEBI: A quinolone that is 4-oxo-1,4-dihydroquinoline which is substituted at positions 1, 3, 6 and 7 by ethyl, carboxy, fluorine, and 4-methylpiperazin-1-yl groups, respectively.

Pharmaceutical Applications

A 6-fluoro, 7-piperazinyl quinoline available for oral and intravenous administration. The in-vitro activity is very similar to that of norfloxacin . It is active against H. ducreyi, V. cholerae and Legionella spp., but Campylobacter and Acinetobacter spp. and pseudomonads are not susceptible. It has poor activity against pneumococci, chlamydiae, mycoplasmas and ureaplasmas. L. monocytogenes, Nocardia spp. and anaerobes are resistant.
A plasma concentration of c. 5 mg/L is achieved 1–1.5 h after a 400 mg oral dose. The plasma elimination half-life is 8.5–15 h. It is widely distributed, concentrations in bone, brain, blister fluid, CSF, saliva, sputum and prostate all approximating, and in some cases exceeding, the simultaneous plasma concentration. It is extensively metabolized to the desmethyl (= norfloxacin) and N-oxide derivatives. Some 60–70% of a dose, only about 10% of which is unchanged, appears in the urine; 25% of a dose appears in the feces, a small part contributed by elimination in the bile.
The half-life increases with hepatic impairment, but is virtually unaffected by renal failure. In patients on continuous ambulatory peritoneal dialysis (CAPD) given 800 mg followed by 400 mg every 12 h for 10–12 days, there was no significant accumulation of pefloxacin or its metabolite, norfloxacin, but concentrations of pefloxacin N-oxide rose continuously in plasma and dialysate; all concentrations fell rapidly when treatment was discontinued.
Adverse reactions are those common to the group . Most common are gastrointestinal tract disturbances, although some typical CNS reactions have been encountered. Skin eruptions (some photosensitive) occur and rashes appeared in about one-third of a group of patients who were given longterm therapy. Clinical uses are similar to those of ofloxacin.