Enrofloxacin

Enrofloxacin (ENR) is a fluoroquinolone antibiotic sold by the Bayer Corporation under the trade name Baytril. It is sold by in a generic form by Bimeda Inc. under the name EnroMed 100. Enrofloxacin is currently approved by the FDA for the treatment of individual pets and domestic animals in the United States. In September 2005, the FDA withdrew approval of Baytril for use in water to treat flocks of poultry, as this practice was noted to promote the evolution of fluoroquinolone-resistant strains of the bacterium ''Campylobacter'', a human pathogen.

It is a bactericidal agent. The bactericidal activity of enrofloxacin is concentration-dependent, with susceptible bacteria cell death occurring within 20–30 minutes of exposure. Enrofloxacin has demonstrated a significant post-antibiotic effect for both Gram-negative and Gram-positive bacteria and is active in both stationary and growth phases of bacterial replication. Enrofloxacin is partially deethylated by CYP450 into the active metabolite ciprofloxacin, which is also a fluoroquinolone antibiotic.

While widely used in veterinary medicine, enrofloxacin has hallucinogenic effects that prohibit use in humans.

Activity and susceptibility data

Enrofloxacin is a synthetic antibacterial agent from the class of the fluoroquinolone carboxylic acid derivatives. It has antibacterial activity against a broad spectrum of Gram-negative and Gram-positive bacteria. It is effective against:
* ''Pseudomonas aeruginosa''
* ''Klebsiella''
* ''Escherichia coli''
* ''Enterobacter''
* ''Campylobacter''
* ''Shigella''
* ''Salmonella''
* ''Aeromonas''
* ''Haemophilus''
* ''Proteus''
* ''Yersinia''
* ''Serratia''
* ''Vibrio''
* '' Brucella''
* '' Chlamydia trachomatis''
* ''Staphylococcus'' (including penicillinase-producing and methicillin-resistant strains)
* ''Mycoplasma''
* ''Mycobacterium''

Variable activity against:
* ''Streptococcus''

Ineffective against:
* Anaerobes

The following data represent minimum inhibitory concentration ranges for a few medically significant bacterial pathogens:
* ''Escherichia coli'' - 0.022 - 0.03 µg/ml
* ''Staphylococcus aureus'' - 0.0925 - 64 µg/ml
* ''Pseudomonas aeruginosa'' - 0.05 µg/ml

Adverse effects/warnings

Enrofloxacin was banned for poultry use in the United States in 2005.

Overdosage/acute toxicity

It is unlikely that an acute overdose of either compound would result in symptoms more serious than either anorexia or vomiting, but the adverse effects noted above could occur. Dogs receiving 10 times the labeled dosage rate of enrofloxacin for at least 14 days developed only vomiting and anorexia. Death did occur in some dogs when fed 25 times the labeled rate for 11 days, however.
* Oral : greater than 5000 mg/kg
* Dermal LD₅₀: greater than 2000 mg/kg
* Inhalation LD₅₀: greater than 3547 mg/m3 (4-hour exposure)
* Eye effects: irritant; reversible in less than 7 days. In cats, it can produce sudden onset blindness when administered by injection, as it is retinotoxic.

Degradation

The brown rot fungus ''Gloeophyllum striatum'' can degrade the fluoroquinolone enrofloxacin using hydroxyl radicals.

References

Acta Crystallogr. (2014). E70, o200-o201

https://doi.org/10.1107/S1600536814001421

Enrofloxacinium oxalate

T. S. Yamuna, M. Kaur, B. J. Anderson, J. P. Jasinski and H. S. Yathirajan{{QuinoloneAntiBiotics

Fluoroquinolone antibiotics
Veterinary drugs
Piperazines
Cyclopropanes
Carboxylic acids