Enrofloxacin

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Enrofloxacin
Systematic (IUPAC) name
1-Cyclopropyl-7-(4-ethyl-1-piperazinyl)-6-Fluoro-1,4-Dihydro-4-Oxo-3-Quinolonecarboxylic Acid
Identifiers
CAS number 93106-60-6
ATC code  ?
PubChem 71188
Chemical data
Formula C19H22FN3O3 
Mol. mass 359.4
Pharmacokinetic data
Bioavailability 80% in dogs, 65-75% in sheep [1]
Metabolism Renal and non-renal[2]
Half life 4-5 hours in dogs, 6 hours in cats, 1.5 - 4.5 hours in sheep.
Excretion Renal
Therapeutic considerations
Pregnancy cat.

B3(AU) C(US)
Legal status

Prescription Only (S4)(AU) POM(UK)
Routes Oral, subcutaneous injection, topical (ear drops)

Enrofloxacin is a fluoroquinolone antibiotic sold by the Bayer Corporation under the trade name Baytril(r). Enrofloxacin is currently FDA-approved for treatment of individual pets and domestic animals in the United States. In September of 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.[3] Fluoroquinolones such as ciprofloxacin are widely used in the treatment of human disease.

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.

Contents

[edit] Activity

Enrofloxacin is a synthetic chemotherapeutic 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. Its mechanism of action is not thoroughly understood, but it is believed to act by inhibiting bacterial DNA-gyrase (a type-II topoisomerase), thereby preventing DNA supercoiling and DNA synthesis.

Variable activity against:

Ineffective against anaerobes.

[edit] Contraindications/Precautions

[edit] Adverse Effects/Warnings

seizures are possible in cats.

[edit] Overdosage/Acute Toxicity

It is unlikely 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 LD50: Greater than 5000 mg/kg
  • DERMAL LD50: Greater than 2000 mg/kg
  • INHALATION LC50: Greater than 3547 mg/m3 (4 hr. exposure
  • EYE EFFECTS: Irritant; reversible in less than 7 days

[edit] References

  1. ^ Plumb DC. Enrofloxacin. Veterinary Druh Handbook, fifth edition.
  2. ^ Plumb DC. Enrofloxacin. Veterinary Drug Handbook, fifth edition.
  3. ^ http://www.fda.gov/cvm/FQWithdrawal.html FDA statement on withdrawal of Baytril for use in poultry
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Antibacterials for systemic use: quinolones (J01M)
Fluoroquinolones
Alatrofloxacin‡ • Ciprofloxacin • Danofloxacin§ • Difloxacin§ • Enoxacin • Enrofloxacin§ • Fleroxacin‡ • Garenoxacin • Gatifloxacin • Gemifloxacin • Grepafloxacin‡ • Ibafloxacin§ • Levofloxacin • Lomefloxacin • Marbofloxacin§ • Moxifloxacin • Norfloxacin • Ofloxacin • Orbifloxacin§ • Pazufloxacin • Pefloxacin • Pradofloxacin§ • Prulifloxacin • Rufloxacin • Sarafloxacin§ • Sitafloxacin† • Sparfloxacin • Temafloxacin‡ • Tosufloxacin • Trovafloxacin‡
Other quinolones
†Undergoing clinical trials. ‡ Withdrawn from market. § Veterinary use medications.
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