Enrofloxacin

359.39

359.39

5307824

618-911-2

3DX3XEK1BN

758616

DTXSID1045619

Pale Yellow to Light Beige

29339900

65.78000

-0.2

Solid

1.385±0.06 g/cm3(Predicted)

225 °C

560.5±50.0 °C(Predicted)

292.8±30.1 °C

1.634

Soluble in chloroform. Slightly soluble in water. Also soluble in dilute KOH

Keep tightly closed.

LD50 in male, female mice (mg/kg): >5000, 4336 orally; ~200, ~200 i.v.; in male rats, male rabbits (mg/kg): >5000, 500-800 orally (Altreuther)

6.43±0.41(Predicted)

190.6 Ų [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]|194.8 Ų [M+H]+ [CCS Type: TW]|194.9 Ų [M+H]+ [CCS Type: TW, Method: calibrated with Waters Major Mix]|204.7 Ų [M+Na]+ [CCS Type: TW, Method: calibrated with Waters Major Mix]|195.5 Ų [M+H]+

Sealed in dry,2-8°C

NONH for all modes of transport

3

Xi

26-36/37-24/25

VB1993650

Xi: Irritant;

Stable at normal temperatures and pressures.

P201, P202, P260, P261, P264, P270, P272, P273, P280, P281, P285, P301+P312, P302+P352, P304+P341, P308+P313, P314, P321, P330, P333+P313, P342+P311, P363, P391, P405, P501

36/37/38

SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.

Tolerances for residues of new animal drugs in food. ... Chickens and turkeys: A tolerance of 0.3 ppm is established for residues of enrofloxacin (marker residue) in muscle (target tissue) of chickens and turkeys. ... Cattle: A tolerance of 0.1 ppm for desethylene ciprofloxacin (marker residue) has been established in liver (target tissue) of cattle.|Ophthalmic and topical dosage form new animal drugs. Enrofloxacin, silver sulfadiazine emulsion. ... Indications for use: For the treatment of otitis externa in dogs. /Enrofloxacin, silver sulfadiazine emulsion/|Implantation or injectable dosage form new animal drugs. Enrofloxacin solution. ... Indications for use: Dogs for management of diseases associated with bacteria susceptible to enrofloxacin. ... Indications for use: For treatment of bovine respiratory disease (BRD) associated with Pasteurella haemolytica, Pasteurella multocida, and Haemophilus somnus.|Enrofloxacin tablets. ... Indications for use: Dogs and cats for management of diesases associated with bacteria susceptible to enrofloxacin.|Enrofloxacin oral solution. ... It is used in drinking water as follows: Chicken and turkeys. ... Indications: Chickens: control of mortality associated with E.coli susceptible to enrofloxacin. Turkeys: Control of mortality associated with E.coli and Pasteurella multocida (fowl cholera) susceptible to enrofloxacin.

Drugs Future 13 (Apr): 305-7 (1988). A ... monograph describing enrofloxacin synthesis, pharmacology and pharmacokinetics is presented.|Lizondo M et al; Physicochemical Properties of Endrofloxacin; J Pharm Biomed Anal 15 (12): 1845-9 (1997). /A review of the/ spectral, solubility, and related physicochemical characteristics of enrofloxacin are reported, including dissociation constants and partition coefficients.

|Danger|H302 (94.85%): Harmful if swallowed [Warning Acute toxicity, oral]|P201, P202, P260, P261, P264, P270, P272, P273, P280, P281, P285, P301+P312, P302+P352, P304+P341, P308+P313, P314, P321, P330, P333+P313, P342+P311, P363, P391, P405, and P501|Aggregated GHS information provided by 103 companies from 10 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

The objective of the study was to determine the in vitro interaction between enrofloxacin and ciprofloxacin against Escherichia coli and staphylococcal isolates from dogs. The microdilution checkerboard assay was used to determine the interaction of the drugs against 50 E. coli and 50 beta-haemolytic staphylococcal clinical isolates. The checkerboard assay revealed that the activity of enrofloxacin and ciprofloxacin was additive against E. coli and staphylococcal clinical isolates. It was concluded that for bacterial species against which ciprofloxacin is more potent than enrofloxacin, the in vivo transformation of enrofloxacin to ciprofloxacin may enhance the efficacy of enrofloxacin, if additivity of the drugs is confirmed in vivo.

Substances that inhibit the growth or reproduction of BACTERIA. (See all compounds classified as Anti-Bacterial Agents.)

Pharmacokinetics and bioavailability of enrofloxacin were determined after single intravenous (IV) and intramuscular (IM) administrations of 5 mg/kg body weight (BW) to 5 healthy adult Angora goats. Plasma enrofloxacin concentrations were measured by high performance liquid chromatography. Pharmacokinetics were best described by a 2-compartment open model. The elimination half-life and volume of distribution after IV and IM administrations were similar (t1/2beta, 4.0 to 4.7 hr and Vd(ss),1.2 to 1.5 L/kg, respectively). Enrofloxacin was rapidly (t1/2a, 0.25 hr) and almost completely absorbed (F, 90%) after IM administration. Mean plasma concentrations of enrofloxacin at 24 hr after IV and IM administration (0.07 and 0.09 microg/mL, respectively) were higher than the minimal inhibitory concentration (MIC) values for most pathogens. In conclusion, once-daily IV and IM administration of enrofloxacin (5 mg/kg BW) in Angora goats may be useful in treatment of infectious diseases caused by sensitive pathogens.|Plasma, urine, and skin drug concentrations were determined for dogs (n=12) given five daily oral doses of marbofloxacin (MAR) (2.75 mg/kg), enrofloxacin (ENR) (5.0 mg/kg) or difloxacin (DIF) (5.0 mg/kg). Concentrations of the active metabolite of ENR, ciprofloxacin (CIP), were also determined. The three-period, three-treatment crossover experimental design included a 21-day washout period between treatments. Area under the plasma drug concentration vs. time curve (AUC0-last, microg/mlxhr of MAR was greater than for ENR, CIP, ENR/CIP combined, and DIF. Maximum concentration (Cmax) of MAR was greater than ENR, CIP, and DIF. Time of maximum plasma concentration (Tmax) was similar for MAR and DIF; Tmax occurred earlier for ENR and later for CIP. Plasma half-life (t1/2) of MAR was longer than for ENR, CIP, and DIF. Urine concentrations of DIF were less than MAR or ENR/CIP combined, but urine concentrations of MAR and ENR/CIP combined did not differ. DIF skin concentrations were less than the concentrations of MAR or ENR/CIP combined 2 h after dosing, but skin concentrations of MAR and ENR/CIP combined did not differ.|Serum concentrations and pharmacokinetics of enrofloxacin were studied in 6 mares after intravenous (IV) and intragastric (IG) administration at a single dose rate of 7.5 mg/kg body weight. In experiment 1, an injectable formulation of enrofloxacin (100 mg/ml) was given IV. At 5 min after injection, mean serum concentration was 9.04 microg/mL and decreased to 0.09 microg/mL by 24 hr. Elimination half-life was 5.33 +/- 1.05 hr and the area under the serum concentration vs time curve (AUC) was 21.03 +/- 5.19 mg x hr/L. In experiment 2, the same injectable formulation was given IG. The mean peak serum concentration was 0.94 +/- 0.97 microg/ml at 4 hr after administration and declined to 0.29 +/- 0.12 microg/ml by 24 hr. Absorption of this enrofloxacin preparation after IG administration was highly variable, and for this reason, pharmacokinetic values for each mare could not be determined. In experiment 3, a poultry formulation (32.3 mg/ml) was given IG. The mean peak serum concentration was 1.85 +/- 1.47 microg/ml at 45 min after administration and declined to 0.19 +/- 0.06 microg/mL by 24 h. Elimination half-life was 10.62 +/- 5.33 h and AUC was 16.30 +/- 4.69 mg x h/L. Bioavailability was calculated at 78.29 +/- 16.55%. Minimum inhibitory concentrations of enrofloxacin were determined for equine bacterial culture specimens submitted to the microbiology laboratory over an 11-month period. The minimum inhibitory concentration of enrofloxacin required to inhibit 90% of isolates (MIC90) was 0.25 microg/ml for Staphylococcus aureus, Escherichia coli, Salmonella spp., Klebsiella spp., and Pasteurella spp. The poultry formulation was well tolerated and could be potentially useful in the treatment of susceptible bacterial infections in adult horses. The injectable enrofloxacin solution should not be used orally.|Concentrations of enrofloxacin equivalent activity were determined by microbiological assay in the plasma of healthy and E. coli-infected broilers following single intravenous and oral administrations at 10 mg/kg. Tissue distribution and residue-depletion following multiple oral doses (10 mg/kg for 3 successive days) were investigated. Pharmacokinetic variables were determined using compartmental and non-compartmental analytical methods. Plasma enrofloxacin concentrations after intravenous dosing to healthy and infected birds were best described by a two-compartments model. Enrofloxacin concentrations in plasma of infected birds were lower than those of healthy ones. The disposition kinetics of intravenously administered drug in healthy and infected birds were somewhat different. The elimination half-life (t1/2 beta) was 4.75 vs. 3.63 hr; mean residence time (MRT) was 6.72 vs 4.90 hr; apparent volume of the central compartment (Vc) was 1.11 vs 1.57 l/kg; rate constant for transfer from peripheral to central compartment (k21) was 1.15 vs 1.41 hr-1 and total body clearance (ClB) was 0.35 vs 0.53 l/hr/kg in healthy and infected birds, respectively. After oral administration, the absorption half-life (t1/2abs) in the infected birds was significantly longer than in healthy birds, while elimination half-life (t1/2el) and MRT were significantly shorter. Bioavailability was higher in infected birds (72.50%) as compared to healthy ones (69.78%). Enrofloxacin was detected in the tissues of healthy and infected birds after daily oral dosing of 10 mg/kg for 3 days. It was more concentrated in liver, kidney, and breast muscle. The minimal inhibitory concentration (MIC) of enrofloxacin against E. coli was 0.064 microgram/ml. On the basis of maintaining enrofloxacin plasma concentrations over the MIC, a dose of 10 mg/kg given intravenously every 20.14 hr or orally every 20.86 hr should provide tissue concentrations effective against E. coli infection in chickens.|For more Absorption, Distribution and Excretion (Complete) data for ENROFLOXACIN (6 total), please visit the HSDB record page.

The pharmacokinetics of enrofloxacin and its active metabolite ciprofloxacin were investigated in goats after a single intramuscular administration of enrofloxacin at 2.5 mg/kg body weight. The plasma concentrations of enrofloxacin and ciprofloxacin were determined simultaneously by a HPLC method. The peak concentrations (Cmax) of enrofloxacin (1.13 microg/ml) and ciprofloxacin (0.24 microg/ml) were observed at 0.8 and 1.2 hr, respectively. The elimination half-life (t1/2beta), volume of distribution (Vd(area)), total body clearance (Cl(B)) and mean residence time (MRT) of enrofloxacin were 0.74 hr, 1.42 l/kg, 1329 ml/hr per kg and 1.54 hr, respectively. The t1/2beta, area under the plasma concentration-time curve (AUC) and the MRT of ciprofloxacin were 1.38 h, 0.74 microg h/ml and 2.73 h, respectively. The metabolic conversion of enrofloxacin to ciprofloxacin was appreciable (36%) and the sum of the plasma concentrations of enrofloxacin and ciprofloxacin was maintained at or above 0.1 microg/ml for up to 4 hr. Enrofloxacin appears to be useful for the treatment of goat diseases associated with pathogens sensitive to this drug.

Basic treatment: Establish a patent airway. Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with normal saline during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 ml/kg up to 200 ml of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool ... . Cover skin burns with dry sterile dressings after decontamination ... . /Poison A and B/|Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in respiratory arrest. Positive pressure ventilation techniques with a bag valve mask device may be beneficial. Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start an IV with D5W /SRP: "To keep open", minimal flow rate/. Use lactated Ringer's if signs of hypovolemia are present. Watch for signs of fluid overload. Consider drug therapy for pulmonary edema ... . For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam (Valium) ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Poison A and B/

Bay Vp 2674

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