Ceftiofur

523.57

523.56

1308068-626-2

DTXSID7046702

QJ01DD90

2941905700

256.26000

2.05

White to off-white powder

1.8±0.1 g/cm3

1.820

In water, 23 mg/L at 25 °C (est)

0-6°C

5.9X10-20 mm Hg at 25 °C (est)

Henry's Law constant = 2.2X10-25 atm-cu m/mol at 25 °C (est)

pKa = 3.7 (carboxylic acid) (est)

Mol wt: 545.55 /Monosodium salt/|Mol wt: 560.03 /Monohydrochloride/|Hydroxyl radical reaction rate constant = 1.6X10-10 cu cm/molecule-sec at 25 °C (est)

NONH for all modes of transport

2

24/25

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.

Implantation or injectable dosage form new animal drugs. Ceftiofur crystalline free acid. ... (1) Swine. Indications for use: For the treatment of swine respiratory disease (SRD) associated with Actinobacillus pleuropneumoniae, Pasteurella multocida, Haemophilus parasuis, and Streptococcus suis. ... (2) Cattle. Indications for use. For the treatment of bovine respiratory disease (BRD, shipping fever, pneumonia) associated with Mannheimia haemolytica, Pasteurella multocida, and Histophilus somni in beef, non-lactating dairy, and lactating dairy cattle. For the control of respiratory disease in beef and non-lactating dairy cattle which are at high risk of developing BRD associated with M. haemolytica, P. multocida, and H. somni. /Ceftiofur crystalline free acid/|Implantation or injectable dosage form new animal drugs. Ceftiofur hydrochloride. ... (1) Swine. Indications for use: For treatment and control of swine bacterial respiratory disease (swine bacterial pneumonia) associated with Actinobacillus pleuropneumoniae, Pasteurella multocida, Salmonella choleraesuis, and Streptococcus suis. ... (2) Cattle. Indications for use: For treatment of bovine respiratory disease (BRD, shipping fever, pneumonia) associated with Mannheimia haemolytica, P. multocida, and Histophilus somni; acute bovine interdigital necrobacillosis (foot rot, pododermatitis) associated with Fusobacterium necrophorum and Bacteroides melaninogenicus; and acute metritis (0 to 14 days post-partum) associated with bacteria susceptible to ceftiofur. /Ceftiofur hydrochloride/|Implantation or injectable dosage form new animal drugs. Ceftiofur sodium. ... (1) Swine. Indications for use: For treatment and control of swine bacterial respiratory disease (swine bacterial pneumonia) associated with Actinobacillus pleuropneumoniae, Pasteurella multocida, Salmonella choleraesuis, and Streptococcus suis. ... (2) Cattle. Indications for use: For treatment of bovine respiratory disease (shipping fever, pneumonia) associated with Mannheimia haemolytica, P. multocida, and Histophilus somni in beef and dairy cattle; and for treatment of acute bovine interdigital necrobacillosis (foot rot, pododermatitis) associated with Fusobacterium necrophorum and Bacteroides melaninogenicus. ... (3) Sheep. Indications for use: For treatment of sheep respiratory disease (pneumonia) associated with M. haemolytica and P. multocida. ... (4) Goats. Indications for use: For treatment of caprine respiratory disease (goat pneumonia) associated with M. haemolytica and P. multocida. ... (5) Chickens. Indications for use: For control of early mortality associated with Escherichia coli organisms susceptible to ceftiofur in day-old chicks. ... (6) Turkeys. Indications for use: For control of early mortality associated with E. coli organisms susceptible to ceftiofur in day-old poults. ... (7) Horses. Indications for use: For treatment of respiratory infections in horses associated with Streptococcus zooepidemicus. ... (8) Dogs. Indications for use: For treatment of canine urinary tract infections associated with E. coli and Proteus mirabilis. /Ceftiofur sodium/|Intramammary dosage forms. Ceftiofur. ... (1) Lactating cows. Indications for use. For the treatment of clinical mastitis in lactating dairy cattle associated with coagulase-negative staphylococci, Streptococcus dysgalactiae, and Escherichia coli. ... (2) Dry cows. For the treatment of subclinical mastitis in dairy cattle at the time of dry off associated with Staphylococcus aureus, Streptococcus dysgalactiae, and Streptococcus uberis.|For more FDA Requirements (Complete) data for CEFTIOFUR (6 total), please visit the HSDB record page.

LD50 Mouse (female) im approximately 3400 mg/kg bw|LD50 Mouse (female) iv approximately 2000 mg/kg bw|LD50 Rat (female) 2200 mg/kg bw|LD50 Rat (female) im 1250 mg/kg bw|LC50 Rat inhalation > 8.3 mg/L/4 hr

Ceftiofur's production and use as a veterinary antibacterial medicine(1,2) may result in its release to the environment through various waste streams(SRC).

TERRESTRIAL FATE: Based on a classification scheme(1), an estimated Koc value of 3,700(SRC), determined from a structure estimation method(2), indicates that ceftiofur is expected to have slight mobility in soil(SRC). An estimated pKa of 3.7 (carboxylic acid)(SRC), calculated using a method based on linear free energy relationships and perturbed molecular orbital theory(3), indicates that this compound will exist primarily as an anion in the environment and anions generally have higher mobility in soils than their neutral counterparts(4). Volatilization of ceftiofur from moist soil surfaces is not expected to be an important fate process(SRC) since anions do not volatilize. Ceftiofur is not expected to volatilize from dry soil surfaces(SRC) based upon an estimated vapor pressure of 6X10-20 mm Hg(SRC), determined from a fragment constant method(6). Half-lives reported for the aerobic biodegradation of cefiofur sodium in clay loam at pH 5, sand at pH 7, and silty clay loam at pH 9 were 22.2, 49, and 41.1 days, respectively(7-9).|AQUATIC FATE: Based on a classification scheme(1), an estimated Koc value of 3,700(SRC), determined from a structure estimation method(2), indicates that ceftiofur is expected to adsorb to suspended solids and sediment(SRC). However, an estimated pKa of 3.7 (carboxylic acid)(SRC), calculated using a method based on linear free energy relationships and perturbed molecular orbital theory(3), indicates that this compound will exist primarily as an anion in the environment, and anions do not adsorb to sediment as strongly as their neutral counterparts(4). Volatilization from water surfaces is not expected because anions do not volatilize. According to a classification scheme(5), an estimated BCF of 3(SRC), from an estimated log Kow of 1.6(6) and a regression-derived equation(7), suggests the potential for bioconcentration in aquatic organisms is low(SRC). Half-lives reported for the aqueous hydrolysis of ceftiofur sodium were 22.2 days at pH 5, 49 days at pH 7, and 41.1 days at pH 9(8,9). Half-lives reported for the aerobic biodegradation of ceftiofur sodium in clay loam at pH 5, sand at pH 7, and silty clay loam at pH 9 were 22.2, 49, and 41.1 days, respectively(8-10).|ATMOSPHERIC FATE: According to a model of gas/particle partitioning of semivolatile organic compounds in the atmosphere(1), ceftiofur, which has an estimated vapor pressure of 6X10-20 mm Hg(SRC), determined from a fragment constant method(2), is expected to exist solely in the particulate phase in the ambient atmosphere. Particulate-phase ceftiofur may be removed from the air by wet or dry deposition(SRC). Ceftiofur contains chromophores that absorb at wavelengths >290 nm indicating that this substance may be susceptible to direct photolysis by sunlight(3); however photodegradation of ceftiofur sodium has been reported to be minimal(4).

Half-lives reported for the aqueous hydrolysis of cefiofur sodium were 22.2 days at pH 5, 49 days at pH 7, and 41.1 days at pH 9(1,2). Ceftiofur contains chromophores that absorb at wavelengths >290 nm indicating that this substance may be susceptible to direct photolysis by sunlight(3); however photodegradation of ceftiofur sodium has been reported to be minimal(4); data supporting this conclusion were not provided by the authors.

An estimated BCF of 3 was calculated for ceftiofur(SRC), using an estimated log Kow of 1.6(1) and a regression-derived equation(2). According to a classification scheme(3), this BCF suggests the potential for bioconcentration in aquatic organisms is low(SRC).

Using a structure estimation method based on molecular connectivity indices(1), the Koc of ceftiofur can be estimated to be 3,700(SRC). According to a classification scheme(2), this estimated Koc value suggests that ceftiofur is expected to have slight mobility in soil. However, an estimated pKa of 3.7 (carboxylic acid)(SRC), calculated using a method based on linear free energy relationships and perturbed molecular orbital theory(3), indicates that this compound will exist primarily as an anion in the environment and anions generally have higher mobility in soils than their neutral counterparts(4).

An estimated pKa of 3.7 (carboxylic acid)(1), calculated using a method based on linear free energy relationships and perturbed molecular orbital theory(2), indicates that this compound will exist primarily as an anion in the environment. Volatilization from moist soil or water surfaces is not expected(SRC) since anions do not volatilize. Ceftiofur is not expected to volatilize from dry soil surfaces(SRC) based upon an estimated vapor pressure of 6X10-20 mm Hg(SRC), determined from a fragment constant method(3).

Occupational exposure to ceftiofur may occur through dermal contact with this compound at workplaces where ceftiofur is produced or used. Exposure of the general population is expected to be limited to those who administer this substance to animals and those who eat foods made from animals containing residues of this substance. (SRC)

Pigs, , , Treatment of bacterial respiratory disease associated with Actinobacillus pleuropneumoniae, Pasteurella multocida, Haemophilus parasuis and Streptococcus suis., Treatment of septicaemia, polyarthritis or polyserositis associated with Streptococcus suis infection., , , Cattle, , , Treatment of acute interdigital necrobacillosis in cattle also known as Panaritium or foot rot., Treatment of acute post-partum (puerperal) metritis in cattle, in cases where treatment with another antimicrobial has failed., ,

MEDICATION (VET): Ceftiofur is used in the treatment of respiratory infections in cattle and pigs.|THERAP CAT (VET): Antibacterial|MEDICATION (VET): Ceftiofur is an injectable cephalosporin approved for respiratory disease in horses and cattle and for treatment of canine bacterial urinary tract infections caused by E coli and Proteus.|MEDICATION (VET): Dogs: ... Ceftiofur sodium for injection are indicated in the treatment of urinary tract infections caused by susceptible organisms, including E. coli, P. mirabilis, and S. aureus. /Ceftiofur sodium/|For more Therapeutic Uses (Complete) data for CEFTIOFUR (13 total), please visit the HSDB record page.

The cephalosporins are relatively nontoxic, ... . IM injections can be painful, and repeated IV administration may lead to local phlebitis. Nausea, vomiting, and diarrhea may occasionally be seen. Hypersensitivity reactions of several forms have been seen, particularly in animals with a history of acute penicillin allergy. Superinfection may arise with the use of cephalosporins, and Pseudomonas or Candida spp are likely opportunistic pathogens. /Cephalosporins/|Ceftiofur is associated with a duration and dose-related thrombocytopenia and anemia in dogs, which would not be expected with the recommended dosage regimen.|Ceftiofur concentrations in an infected and uninfected environment were compared and the efficacy of locally administered ceftiofur was evaluated in an experimental infection with Staphylococcus aureus in tissue cages. Eight ponies had tissue cages (TCs) implanted sc on each side of the neck. Into one of the cages 150 mg of ceftiofur was administered and fluid samples were taken to determine ceftiofur concentrations. After 1 week the other TC was infected with S. aureus and subsequently treated with 150 mg ceftiofur administered locally into the TC once daily for 21 days. Samples of fluid were taken to determine ceftiofur concentrations and for bacterial counts. Ceftiofur concentrations did not differ significantly in the infected and uninfected environments after single dose of 150 mg of ceftiofur. Concentrations were considerably in excess of the minimum inhibitory concentration (MIC) of the S. aureus strain used. A marked decrease of viable bacteria in tissue cage fluid (TCF) occurred. In five of seven ponies; however, the infection was not eliminated and abscess formation occurred. Therefore, local application of ceftiofur alone is not advisable for infections with S. aureus in secluded sites in horses, but should be used only with adjunctive therapy.|Horses: Diarrhea with ceftiofur.|Anemia and thrombocytopenia have been seen in dogs given ceftiofur at high doses (three to five times the labeled dose) or for long periods of time (5 to 6 weeks). These side effects appear to be reversible when treatment is discontinued.

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

A study of 4 male and 4 female Sprague-Dawley rats treated intramuscularly with (14)C-ceftiofur (2 mg/kg bw) revealed that 55% of the administered dose was excreted in the urine and about 30% in the GI tract and feces. The major urinary metabolite was desfuroylceftiofur (DFC). The metabolism of ceftiofur was similar in calves administered (14)C-ceftiofur (2 mg/kg bw) via the i.m. route. Unmetabolized ceftiofur was also present in the urine (4.4-21% of total radioactivity).|A group of Sprague-Dawley rats (7/sex) received single oral doses of (14)C-ceftiofur (200 mg/kg bw) in a comparative study with calves. Approximately 55% of the total dose was recovered in the urine and the rest was present in the feces and GI tract. Plasma concentration at 6 hr was 1 mg/kg and trace amounts of ceftiofur were present in all tissues (i.e. liver, muscle and fat). The highest residue levels (0.7 mg/kg) were present in kidney.|A study of lactating cows treated with (14)C-ceftiofur (2.3 mg/kg bw/day for 5 days) revealed that 32-38% of the radioactivity was present in the milk as free metabolites. The major metabolite was desfuroylceftiofur cysteine disulfide representing 7-9% of the total radioactivity. No parent compound was detected in the milk.|A study of im administration of (14)C-ceftiofur in a bull revealed that 55% of the administered dose was excreted in the urine and approximately 30% in the GI tract and feces. The initial metabolite in both urine and plasma was desfuroylceftiofur. HPLC analysis of radioactive metabolites was similar to the results found in the rat studies. A number of metabolites were produced, the major metabolite (87% of total urinary metabolites) being desfuroylceftiofur acetamide conjugates. No parent compound was observed in the urine.|For more Absorption, Distribution and Excretion (Complete) data for CEFTIOFUR (13 total), please visit the HSDB record page.

A study of 4 male and 4 female Sprague-Dawley rats treated intramuscularly with (14)C-ceftiofur (2 mg/kg bw) revealed that 55% of the administered dose was excreted in the urine and about 30% in the GI tract and faeces. The major urinary metabolite was desfuroylceftiofur (DFC). The metabolism of ceftiofur was similar in calves administered (14)C-ceftiofur (2 mg/kg bw) via the i.m. route. Unmetabolized ceftiofur was also present in the urine (4.4-21% of total radioactivity).|A group of Sprague-Dawley rats (7/sex) received single oral doses of (14)C-ceftiofur (200 mg/kg bw) in a comparative study with calves. Approximately 55% of the total dose was recovered in the urine and the rest was present in the feces and GI tract. ... The major urinary metabolite was ceftiofursulfoxide cysteine thioester.|HPLC analysis of metabolites of (14)C-ceftiofur formed by arochlor-induced rat liver S-9 fractions in vitro revealed that desfuroylceftiofur was the major metabolite. Low doses (119 mg/kg bw) of ceftiofur were completely metabolized within 15 minutes. Higher doses (857 mg/kg bw) were converted to desfuroylceftiofur after 60 minutes of incubation.|A study in 8-week old Sprague-Dawley rats (7/sex) treated with (14)C-ceftiofur (800 mg/kg bw/day) by oral gavage for 5 days revealed several urinary metabolites, including desfuroylceftiofur, ceftiofur sulfoxide, and cysteine disulfide.|For more Metabolism/Metabolites (Complete) data for CEFTIOFUR (15 total), please visit the HSDB record page.

Six Friesian calves (3/sex) were treated with ceftiofur according to different protocols including one single im and iv injection at 1 mg/kg bw, and 5 i.m. injections at 1 mg/kg bw at 24 hr intervals. ... The half life (0.07 hr) was short due to rapid metabolism to desfuroylceftiofur. The t1/2 of desfuroylceftiofur after im and iv administration were similar (9.7 and 8.6 hr, respectively).|A study of 4 calves (sex and breed unspecified) administered ceftiofur intramuscularly daily for 4 days at 2 dose levels (2.2 or 4.4 mg/kg bw/day) demonstrated a plasma half life of 3.5 hr. ... Plasma half life of the metabolite desfuroylceftiofur was 9.7 h after im administration.|A study of 4- to 5-month old Yorkshire-Hampshire pigs (6/sex) treated with 3 daily im injections of (14)C-ceftiofur (5.2 mg/kg bw) produced similar results to those observed in rats and cattle. ... The half life of desfuroylceftiofur was 13.5 hr after im treatment and 12.2 hr after iv treatment. /Desfuroylceftiofur/

Ceftiofur sodium is a third generation broad-spectrum cephalosporin, formulated as an intramuscular injection, which is used to treat respiratory diseases in swine, ruminants and horses. The thioester bond on ceftiofur is rapidly cleaved to give desfuroylceftiofur which is further metabolized to a disulfide dimer and various desfuroylceftiofur-protein and amino acid conjugates.|Cephalosporins ... bind to penicillin-binding proteins located beneath the cell wall and thereby interfere with the action of transpeptidase and other cell-wall enzymes. A residual antibacterial effect is also evident with the cephalosporins. /Cephalosporins/

/SRP:/ Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). 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 0.9% saline (NS) 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 ... . /Poisons A and B/|/SRP:/ Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in severe respiratory distress. Positive-pressure ventilation techniques with a bag valve mask device may be beneficial. Consider drug therapy for pulmonary edema ... . Consider administering a beta agonist such as albuterol for severe bronchospasm ... . Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start IV administration of D5W /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam or lorazepam ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Poisons A and B/

ceftiofur

Veterinary-labeled product(s): 50 mg per mL (Rx) (Naxcel). /Ceftiofur sodium for injection/|Veterinary-labeled product(s): 50 mg per mL (Rx) (Excenel RTU). /Ceftiofur hydrochloride injection/

... approved for use in cows and dogs

Analyte: ceftiofur; matrix: milk; procedure: high-performance liquid chromatography with ultraviolet detection at 295 nm; limit of quantitation: 2-5 ppb|Analyte: ceftiofur; matrix: milk; procedure: high-performance liquid chromatography with ultraviolet detection at 210 nm|Analyte: ceftiofur; matrix: blood, milk; procedure: high-performance liquid chromatography with ultraviolet detection at 265.8 nm; limit of detection: 50 ppb|Analyte: ceftiofur; matrix: milk; procedure: high-performance liquid chromatography with ultraviolet detection at 293 nm; limit of detection: 4 ppb|For more Clinical Laboratory Methods (Complete) data for CEFTIOFUR (7 total), please visit the HSDB record page.

Veterinary drugs -> Naxcel -> EMA Drug Category|Antibacterials for systemic use -> Veterinary pharmacotherapeutic group|Veterinary Drug -> ANTIMICROBIAL_AGENT; -> JECFA Functional Classes

Veterinary Drug -> ANTIMICROBIAL_AGENT;