Вы находитесь на странице: 1из 6

Enrofloxacin is a broad-spectrum bactericidal antibiotic.

Although the mechanism of action is not well-


understood, Enrofloxacin is effective against a broad spectrum of gram- positive and gram-negative bacteria
including most species of the following: Pseudomonas aeruginosa, Klebsiella, E.coli., Enterobacter,
Campylobacter, Shigella, Salmonella, Aeromonas, Haemophillus, Proteus, Yersinia, Serratia, Vibrio, Brucella,
Chlamydia, Staphylocci (including some methicillin resistant strains), Mycoplasma and Mycobacterium. It is
not effective against anaerobic bacteria and may be variably effective against Streptococcus infections.
Enrofloxacin has a similar spectrum of activity as ciprofloxacin but enrofloxacin has been shown to have
better bioavailability. With the exception of cerebral-spinal fluid, enrofloxacin attains therapeutic levels in
most tissues of the body. This makes it a very attractive antibiotic choice for difficult-to-treat infections,
particularly those that need long-term antibiotics. Some examples might be osteomyelitis, sinus infections,
otitis, difficult soft-tissue infections, peritonitis, and pleuritis or pneumonia.

Enrofloxacin is eliminated by both renal and hepatic metabolism. Animals with impaired kidney or liver
function may need extra monitoring and dose adjustments to prevent excess drug accumulation.

Dogs and Cats

Enrofloxacin is approved for use in dogs and cats. In dogs it may be given orally, intramuscularly or intra-
venously. It is approved only for oral use in cats although there is published information regarding
intramuscular use. One of the positive features of enrofloxacin is that it is well-absorbed orally and in many
cases may be given once per day.

Fluroquinolones including enrofloxacin have been shown to cause articular cartilage abnormalities when the
drug is given at high dose-levels. The age and breed of the patient should be considered when using
enrofloxacin. Large and giant breeds may be more at risk because of a longer period of growth. Enrofloxacin
has been shown to be safe in pregnant dogs and lactating dogs, however because of the problems with
articular cartilage it should be avoided unless the benefits clearly outweigh the risk to the puppies. This work
has not been repeated in cats.

Horses

Enrofloxacin is well-absorbed orally and intravenously. It generally is not used intramuscularly because it is
too irritating. Although studies have not been done in the horse, there is the risk of developmental cartilage
abnormalities with the fluorquinolone antibiotics. Since horses are expected to be athletes, the use of
enrofloxacin in the young horse should be weighed carefully against the potential risk of cartilage
abnormality.

Side Effects

 Enrofloxacin and the other fluroquinolone antibiotics can cause developmental cartilage
abnormalities. As a consequence most veterinarians try to avoid these drugs in young animals.
 Dogs: GI side-effects including vomiting, diarrhea and elevated liver enzymes; Rare CNS signs
including ataxia seizures, depression and anxiety.
 Cats: GI side effects include vomiting, diarrhea, anorexia, elevated liver enzymes. CNS signs include
ataxia, seizures, depression; vocalization and aggression. Rare ocular toxicity may occur.
 Horses: When injectable enrofloxacin is given orally, it can cause mucous membrane irritation,
redness, slobbering and swelling.

Precautions
 Animals with severe kidney or liver problems may need a reduced dose of enrofloxacin. Hydration
should be monitored and fluid therapy used in animals at risk for dehydration.
 Enrofloxacin should be used with caution or avoided in animals at risk for seizures. This drug is not
used in humans due to central nervous system stimulation.
 Enrofloxacin should not be used for regional antibiotic perfusion because it is too irritating and will
cause vasculitis.

Chemistry - A fluoroquinolone antibiotic, enrofloxacin occurs as a pale yellow, crystalline


powder. It is slightly soluble in water. Enrofloxacin is related structurally to the human-approved
drug ciprofloxacin (enrofloxacin has an additional ethyl group on the piperazinyl ring).
 
Storage/Stability/Compatibility - Unless otherwise directed by the manufacturer, enrofloxacin
tablets should be stored in tight containers at temperatures less than 30°C. Protect from strong
UV light.
 
Pharmacology - Enrofloxacin is a bactericidal agent. The bactericidal activity of enrofloxacin is
concentration dependent, with susceptible bacteria cell death occuring within 20-30 minutes of
exposure. Enrofloxacin has demonstrated a significant post-antibiotic effect for both gram - and
+ bacteria and is active in both stationary and growth phases of bacterial replication.
 
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.
 
Both enrofloxacin and ciprofloxacin have similar spectrums of activity. These agents have good
activity against many gram negative bacilli and cocci, including most species and strains of
Pseudomonas aeruginosa, Klebsiella sp., E. coli, Enterobacter, Campylobacter, Shigella,
Salmonella, Aeromonas, Haemophilus, Proteus, Yersinia, Serratia, and Vibrio species. Of the
currently commercially available quinolones, ciprofloxacin and enrofloxacin have the lowest MIC
values for the majority of these pathogens treated. Other organisms that are generally
susceptible include Brucella sp, Chlamydia trachomatis, Staphylococci (including penicillinase-
producing and methicillin-resistant strains), Mycoplasma, and Mycobacterium sp. (not the
etiologic agent for Johne’s Disease).
 
The fluoroquinolones have variable activity against most Streptococci and are not usually
recommended to be used for these infections. These drugs have weak activity against most
anaerobes and are ineffective in treating anaerobic infections.
 
Resistance does occur by mutation, particularly with Pseudomonas aeruginosa, Klebsiella
pneumonia, Acinetobacter and enterococci, but plasmid-mediated resistance is not thought to
occur.
 
Uses/Indications - Enrofloxacin is approved for use in dogs and cats (oral only) for the
management of of diseases assicaited with bacteria susceptible to enrofloxacin. It is also been
approved for use in cattle (not dairy cattle or veal calves) and for chickens and turkeys.
 
Pharmacokinetics - Both enrofloxacin and ciprofloxacin are well absorbed after oral
administration in most species. But in dogs, enrofloxacin’s bioavailability (approximately 80%) is
about twice that of ciprofloxacin after oral dosing. 50% of Cmax is reportedly attained within 15
minutes of dosing and peak levels (Cmax) occur within one hour of dosing. The presence of
food in the stomach may delay the rate, but not the extent of absorption.
 
Enrofloxacin/ciprofloxacin are distributed throughout the body. Volume of distribution in dogs is
at least 2.8 L/kg. Only about 27% is bound to canine plasma proteins. Highest concentrations
are found in the bile, kidney, liver, lungs, and reproductive system (including prostatic fluid and
tissue). Therapeutic levels are also attained in bone, synovial fluid, skin, muscle, aqueous
humor and pleural fluid. Low concentrations are found in the CSF, and levels may only reach 6-
10% of those found in the serum.
 
Enrofloxacin/ciprofloxacin is eliminated via both renal and non-renal mechanisms.
Approximately 15-50% of the drugs are eliminated unchanged into the urine, by both tubular
secretion and glomerular filtration.
 
Enrofloxacin/ciprofloxacin are metabolized to various metabolites that are less active than the
parent compounds. Approximately 30-40% of circulating enrofloxacin is metabolized to
ciprofloxacin. These metabolites are eliminated both in the urine and feces. Because of the dual
(renal and hepatic) means of elimination, patients with severely impaired renal function may
have slightly prolonged half-lives and higher serum levels which may not require dosage
adjustment. The elimination half-lives in dogs are approximately 4-5 hours and in cats, 6 hours.
 
Contraindications/Precautions/Reproductive Safety - Enrofloxacin is contraindicated in
small and medium breed dogs from 2 months to 8 months of age. Bubble-like changes in
articular cartilage have been noted when the drug was given at 2-5 times recommend doses for
30 days, although clinical symptoms have only been seen at the 5X dose. Large and giant
breed dogs may be in the rapid-growth phase for periods longer than 8 months of age, so longer
than 8 months may be necessary to avoid cartilage damage. Quinolones are also
contraindicated in patients hypersensitive to them.
 
Because ciprofloxacin has occasionally been reported to cause crystalluria, animals should not
be allowed to become dehydrated during therapy with either ciprofloxacin or enrofloxacin. In
humans, ciprofloxacin has been associated with CNS stimulation and should be used with
caution in patients with seizure disorders. Patients with severe renal or hepatic impairment may
require dosage adjustments to prevent drug accumulation.
 
The safety of enrofloxacin in pregnant dogs has been investigated. Breeding, pregnant and
lactating dogs receiving up to 15 mg/kg day demonstrated no treatement related effects.
However, because of the risks of cartilage abnormalities in young animals, the fluoroquinolones
are not generally recommended to be used during pregnancy unless the benefits of therapy
clearly outweigh the risks. Limited studies in male dogs at various dosages have indicated no
effects on male breeding performance. Safety in breeding, pregnant, or lactating cats has not
been established.
 
Adverse Effects/Warnings - With the exception of potential cartilage abnormalities in young
animals (see Contraindications above), the adverse effect profile of these drugs appears to be
minimal. GI distress (vomiting, anorexia) is the most common, yet infrequently reported adverse
effect. Although not reported thus far in animals, hypersensitivity reactions, crystalluria and CNS
effects (dizziness, stimulation) could potentially occur.
 
Overdosage/Acute Toxicity - It is unlikely an acute overdose of either compound would result
in symptoms more serious than either anorexia and vomiting. 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.
 
Drug Interactions - Antacids containing cations (Mg++, Al+++, Ca++) may bind to
enrofloxacin/ciprofloxacin and prevent its absorption. Sucralfate may inhibit absorption of
enrofloxacin/ciprofloxacin, separate doses of these drugs by at least 2 hours. 
Enrofloxacin/ciprofloxacin administered with theophylline may increase theophylline blood
levels. Probenecid blocks tubular secretion of enrofloxacin/ciprofloxacin and may increase its
blood level and half-life. Synergism may occur, but is not predictable, against some bacteria
(particularly Pseudomonas aeruginosa or other Enterobacteriaceae) with these compounds and
aminoglycosides, 3rd generation cephalosporins agents, and extended-spectrum
penicillins. Although enrofloxacin/ciprofloxacin has minimal activity against anaerobes, in vitro
synergy has been reported when used with clindamycin against strains of Peptostreptococcus,
Lactobacillus and Bacteroids fragilis. Nitrofurantoin may antagonize the antimicrobial activity of
the fluoroquinolones and their concomitant use is not recommended. Fluoroquinolones may
exacerbate the nephrotoxicity of cyclosporine (used systemically). Because the
fluoroquinolones are relatively new additions to the therapeutic armamentarium, more
interactions may be forthcoming.
 
Drug/Laboratory Interactions - In some human patients, the fluoroquinolones have caused
increases in liver enzymes, BUN, and creatinine and decreases in hematocrit. The clinical
relevance of these mild changes is not known at this time.
 
Doses -
Horses:
Note: Usage of enrofloxacin in horses is controversial. While there has been much
discussion regarding the potential for cartilage abnormalities or other arthropathies in
horses, objective data are lacking. At the present time however, it probably should only be
used in adult horses when other antibiotics are inappropriate with the client informed of,
and agrees to accept the risks for any potential adverse effects.
a) 2.5 mg/kg q12h (Whittem 1993)
 
Elephants:
a) 1.07 – 1.25 mg/kg orally BID.  No adverse effects noted after 2 weeks (Schmidt, 1986).
 
b) 1.5 – 2.8 mg/kg orally once daily. Blood levels evaluated on one elephant found that once
daily dosing maintained blood levels (Houck, 1986).
 
c) 2.5 mg/kg PO (Sanchez, 2005).
 
Elephant References:
a) Schmidt, M.J: Senior Research Veterinarian, Washington Park Zoo, Portland, Oregon,
personal communication, 1986. In: Olsen,J.H., 1999. Antibiotic therapy in elephants. In:
Fowler,M.E. and Miller R.E. (Editors), Zoo and Wild Animal Medicine: Current Therapy 4.
W.B. Saunders, Philadelphia, PA,USA p. 538
 
b) Houck, R: Senior Veterinarian, Ringling Brothers and Barnum and Bailey Circus, 8607
Westwood Center Drive, Vienna, Virginia, 22182, personal communication, 1986. In: Olsen,J.H.,
1999. Antibiotic therapy in elephants. In: Fowler,M.E. and Miller R.E. (Editors), Zoo and Wild
Animal Medicine: Current Therapy 4. W.B. Saunders, Philadelphia, PA,USA p.538
 
c) Sanchez, C.R. Murray, S.Z., Isaza, R., Papich, M.G. 2005. Pharmacokinetics of a single dose
of enrofloxacin administered orally to captive Asian elephants (Elephas maximus). Am J Vet
Res. 66 (11):1948-53.
 
OBJECTIVE: To determine the pharmacokinetics of enrofloxacin after oral administration to
captive elephants. ANIMALS: 6 clinically normal adult Asian elephants (Elephas maximus).
PROCEDURE: Each elephant received a single dose of enrofloxacin (2.5 mg/kg, PO). Three
elephants received their complete diet (pellets and grain) within 2 hours after enrofloxacin
administration, whereas the other 3 elephants received only hay within 6 hours after
enrofloxacin
administration. Serum concentrations of enrofloxacin and ciprofloxacin were measured by use
of high-performance liquid chromatography. RESULTS: Harmonic mean half-life after oral
administration was 18.4 hours for all elephants. Mean +/- SD peak serum concentration of
enrofloxacin was 1.31 +/- 0.40 microg/mL at 5.0 +/- 4.2 hours after administration. Mean area
under the curve was 20.72 +/- 4.25 (microg x h)/mL. CONCLUSIONS AND CLINICAL
RELEVANCE: Oral administration of enrofloxacin to Asian elephants has a prolonged
elimination half-life, compared with the elimination half-life for adult horses. In addition,
potentially therapeutic concentrations in elephants were obtained when enrofloxacin was
administered orally at a dosage of 2.5 mg/kg. Analysis of these results suggests that
enrofloxacin administered with feed in the manner described in this study could be a potentially
useful antimicrobial for use in treatment of captive Asian elephants with infections attributable to
organisms, such as Bordetella spp, Escherichia coli, Mycoplasma spp, Pasteurella spp,
Haemophilus spp, Salmonella spp, and Staphylococcus spp.
 
 
 
Monitoring Parameters -1) Clinical efficacy; 2) Adverse effects
 
Client Information - Do not crush tablets as drug is very bitter tasting.
 
Dosage Forms/Preparations/FDA Approval Status/Withholding Times -
 
Veterinary-Approved Products: (Note: See additional dosage forms in the dosage section for
cattle and birds)
Enrofloxacin Oral Tablets 22.7 mg, 68 mg; Baytril®  (Miles); (Rx)  Approved for use in dogs
and cats.
 
Enrofloxacin Injection 22.7 mg/ml in 20 ml vials; Baytril®  (Miles); (Rx)  Approved for use in
dogs. A non-approved method for diluting the IM injectable product for IV administration
has been described: Dilute 1 part of Baytril® injection with 2 parts of sterile water for
injection and administer IV over 20 minutes or so.
 
Human-Approved Products: None. Note: Use of enrofloxacin by humans cannot be
recommmended due to a high degree of CNS effects.
 

 Description
Enrofloxacin is a used to treat infections in animals caused by .
Enrofloxacin belongs to a general class of antibiotics known as fluoroquinolones. Other related drugs in this class
include ciprofloxacin.
Enrofloxacin is thought to inhibit the synthesis of DNA within the bacteria, resulting in bacterial death.

INDICATIONS
Indicated for infections caused by various kinds of sensitive bacteria or mixed infections.
1) Yellow scour of newborn pigs (under 7 days old) and white scour (under 1 mouth
old) caused by E. coli
2) Hemorrhagic enteritis, diarrhea, alimentary toxicosis, typhoid fever or paratyphoid
fever caused by sensitive bacteria, as well as secondary infections caused
by epidemic diarrhea
3) Common scour, lamb dysentery and pasteurellosis caused by sensitive bacteria
4) Swine streptococcosis and hydropsy caused by E. coli
5) Swine enzootic pneumonia, atrophic rhinitis, pneumonia and bronchitis
6) White diarrhea, colibacillosis, fowl cholera and chronic respiratory disease

DOSAGE AND ADMINISTRATION


Intramuscular injection, a single dose of 0.2ml/kg body weight for cattle, sheep,
pigs, fowls and deer, and 0.2ml/kg body weight for dogs and rabbits for one treatment
period. Curative effect can be achieved after one injection. For severe infections
one more injection can be added 24 hours after the first injection.
animals with serious dehydration can be treated concurrently with oral rehydration
salt. Halve the dosage for prophylactic treatments.

SIDE EFFECTS
Enrofloxacin and the other fluroquinolone antibiotics can cause developmental cartilage abnormalities. As a
consequence most veterinarians try to avoid these drugs in young animals.

WITHDRAWAL PERIOD
Cattle 14 days, pig 10 days.

PRECAUTIONS
Animals with severe kidney or liver problems may need a reduced dose of enrofloxacin. Hydration should be
monitored and fluid therapy used in animals at risk for dehydration.

Enrofloxacin should be used with caution or avoided in animals at risk for seizures. This drug is not used in humans
due to central nervous system stimulation.

Enrofloxacin should not be used for regional antibiotic perfusion because it is too irritating and will cause vasculitis.

STORAGE
Tightly sealed and store in a cold place, avoid lights.

PACKING
In a 50ml or

Вам также может понравиться