پنجشنبه ۹ مرداد ۱۳۹۳

 

 

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هشدار : تجویز نوع و مقدار دارو بر عهده دامپزشک معالج بوده و دام دارو هیچگونه مسئولیتی در قبال مصرف خودسرانه داروها ندارد

دسته دارویی

انروفلوکساسین Enrofloxacin

نام دارو :alt

انروفلوكساسين 10%

گروه دارويي :

آنتي بيوتيك

شكل دارو :

محلول خوراكي يك و پنج ليتري

تركيب :

هر ميلي ليتر حاوي 100 ميلي گرم انروفلوكساسين مي باشد.

Enrofloxacine     100 mg / ml

حيوان هدف :

طيور

مكانيسم عمل دارو :

انروفلوكساسين دارويي باكتريسيد و وسيع الطيف از گروه فلوروكينولون ها مي باشد كه از طريق مهار عمل آنزيم (topoisomerase) gyrase DNA باعث توقف همانند سازي DNA و در نتيجه مرگ باكتري ها مي شود.اين دارو براي درمان و كنترل بيماري هاي ناشي از باسيل ها و كوكسي هاي گرم منفي هوازي (اشريشيا كلي، سالمونلا، پاستورلا، هموفيلوس و مايكوپلاسماها) و باكتري هاي گرم مثبت استفاده مي گردد.

موارد مصرف :

انروفلوكساسين براي مصرف در بوقلمون ها، جوجه هاي گوشتي، مرغ هاي مادر گوشتي جهت درمان بيماري هاي تنفسي و روده اي ناشي از باكتري ها يا مايكوپلاسما ها (مثل پاستورلوز، مايكوپلاسموز، كلي-باسيلوز، كلي-سپتيسمي، و سالمونلوز) استفاده ميشود در صورتي كه تجربيات كلينيكي و انجام تست هاي حساسيت ارگانيسم هاي مولد اين عفونت ها مصرف انروفلوكساسين را به عنوان داروي انتخابي تثبيت نموده باشد.

مقدار و روش مصرف :

محلول انروفلوكساسين از طريق آب آشاميدني تجويز مي شود آب حاوي دارو بايد بلافاصله پيش از مصرف تهيه شود. افزودن دارو به آب آشاميدني بايد در طي دوره درمان بطور مداوم انجام شود و هيچ منبع آب ديگري در دسترس حيوانات نبايد قرار گيرد. دز معمول 10 ميلي گرم انروفلوكساسين براي هر كيلو گرم وزن بدن به مدت 10-3 روز است. وزن كل بدن حيوانات تحت درمان و مقدار كل مصرف آب روزانه آن ها بايد به دقت محاسبه شود. در شرايط عادي 5/0 ميلي ليتر محلول انروفلوكساسين 10% در هر ليتر آب (50ppm ) كافي است. طيور بالغ نظير مرغ هاي مادر ممكن است به يك ميلي ليتر در هر ليتر آب نياز داشته باشند. محول انروفلوكساسين را مي توان مستقيما" به تانك آب آشاميدني يا از طريق پمپ توزيع آب نازل ها اضافه نمود. براي درمان سالمونلوز با پاستورلوز يك دوره درماني 10-5 روز بايد اعمال شود براي شرايط ديگر مدت درمان 5-3 روز است.

موارد منع مصرف :

اين محصول نبايد به طيوري كه تخم آنها به مصرف غذايي انسان مي رسد، تجويز شود.

عوارض جانبي :

به طور كلي عوارض جانبي انروفلوكساسين محدود و بيشتر شامل عوارض گوارشي نظير تهوع، استفراغ و اسهال مي باشد. تجويز انروفلوكساسين براساس دز توصيه شده هيچگونه عارضه جانبي ايجاد نمي كند و اكثر حيوانات اين دارو را به خوبي تحمل مي كنند.

دوران پرهيز از مصرف :

پرهيز دارويي در مرغان تخمگذار 9 روز، براي مرغان گوشتي 9 روز و براي بوقلمون هاي گوشتي 11 روز قبل از كشتار مي باشد.

شرايط نگهداري :

در جاي خنك (زير 25 درجه سانتي گراد) نگهداري شود. آب حاوي دارو حداكثر تا 24 ساعت قابل مصرف مي باشد.

نوع بسته بندي :

بطري پلاستيكي 1 ليتري

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 bac-

terial 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

JohneÕs Disease).

The  fluoroquinolones  have variable activity  against most  Streptococci and are not usually rec-

ommended 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 man-

agement 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 adminis-

tration in most species. But in dogs, enrofloxacinÕs  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 carti-

lage 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.296                                                                                           

The safety of enrofloxacin in pregnant dogs has  been investigated. Breeding, pregnant and  lac-

tating  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 out-

weigh 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 en-

rofloxacin/ciprofloxacin and  prevent  its absorption.  Sucralfate may inhibit absorption of en-

rofloxacin/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 gen-

eration cephalosporins agents, and extended-spectrum  penicillins. Although en-

rofloxacin/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 in-

creases in  liver enzymes, BUN, and creatinine and decreases in hematocrit. The clinical rele-

vance of these mild changes is not known at this time.

Doses -

Dogs:

For susceptible infections:

a) 5- 20 mg/kg per day PO, may be given once daily or divided  and  given twice daily

(q12h). Treatment  should  continue  for at least  2-3 days beyond cessation of  clinical

signs, to a maximum duration of therapy is 30 days. (Package insert; Baytril¨ÑBayer)

b) Enrofloxacin: 2.5 mg/kg PO q12h up to 10 days.  Injectable product is to be given IM

for the first dose and then followed by oral therapy. (Package insert; Baytril¨ÑMiles)

d) Enrofloxacin: 2.5 - 5 mg/kg PO or IM q12 h

Avoid or reduce dosage of  these  drugs in  animals with severe renal failure; avoid in

young animals or in pregnant or breeding animals (Vaden and Papich 1995)

Cats:

For susceptible infections:

a) 5- 20 mg/kg per day PO, may be given once daily or divided  and  given twice daily

(q12h). Treatment  should  continue  for at least  2-3 days beyond cessation of  clinical

signs, to a maximum duration of therapy is 30 days. (Package insert; Baytril¨ÑBayer)

b) Enrofloxacin: 2.5 - 5 mg/kg PO or IM q12 h

Avoid or reduce dosage of  these  drugs in  animals with severe renal failure; avoid in

young animals or in pregnant or breeding animals (Vaden and Papich 1995)

Pocket Pets/Rodents:

For empiric antibiotic therapy:

a) 5 - 15 mg/kg q12h PO; tablets may be crushed and mixed with simple syrup (Oglesbee

1995)

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 horsesDRUG MONOGRAPHS  - ENROFLOXACIN                                                                              297

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)

Cattle:

Enrofloxacin (Baytril¨ 100) has very  recently been approved  for  the treatment of bovine  res-

piratory disease associated  with  Pasteurella haemolytica,  Pasteurella multocida, and

Haemophilus  sommus. It is administered by injection and is intended to be  used for the

treatment of individual animals. The reprted dosage is: 2.5 - 5 mg/kg subQ once daily  for 3-5

days or 7.5 - 12.5 mg/kg once. The product is prescription only and is not for use in  cattle

intended for dairy production or in veal calves. Animals intended for human consumption must

not be slaughtered within 28 days from  the last treatment. Extralabel use of fluoroquinolones

in food animals has been prohibited by the FDA.

Birds:

For susceptible gram negative infections:

a) Using ciprofloxacin 500 mg  tablets: 20 - 40 mg/kg PO  bid. Crushed  tablet  goes  into

suspension well, but must be shaken well before administering. (McDonald 1989)

b) Ciprofloxacin (using crushed tablets): 20 mg/kg PO q12h

Enrofloxacin: 15 mg/kg PO, or IM or 250 mg/L of drinking water.  (Bauck and Hoefer

1993)

c) Ciprofloxacin (using crushed tablets or  suspend) 10 - 15 mg/kg PO q12h (Hoeffer

1995)

A method to make a 10.2 mg/ml oral suspension of enrofloxacin has been described: Make a

stock solution of ÒHMC 0.15%Ó by mixing 7.5 ml of Lubrivet¨ with 92.5 ml of water. Crush

three  (3)  whole 68 mg tablets with a  ÒpinchÓ of  citric acid. Add  crushed  mixture to a

dispensing vial and and 15 ml of ÒHMC0.15%Ó. Shake well to dissolve tablet coating. qs ad

to 20 ml with ÒHMC 0.15%Ó  and allow to stand at room temperature for 30 minutes to  allow

tablet coating to completely diossolve. Shake well before use and keep refrigerated. A 14 day

expiration date has been assigned. By crushing six (6)  tablets a 20.4 mg/ml suspension may

be compounded using the same technique.

Note: 3.23% concentrate is also available and is approved for use (in drinking water at either

25 or 50 ppm for 3-7 days) in chickens and turkeys.

Reptiles:

For susceptible infections:

a) For most species: For respiratory infections:5 mg/kg IM every 5 days for 25 days; For

chronic respiratory infections in tortoises: 15 mg/kg IM  every 72  hours for 5-7  treat-

ments. (Gauvin 1993(

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 recom-

mmended due to a high degree of CNS effects.

 


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