Is ceftiofur a cephalosporin?

Posted on  March 31, 2021, Edited by Jason, Category  

What is ceftiofur?

1. Definition

Ceftiofur is white to light yellow powder. It is insoluble in water, slightly soluble in acetone, and almost insoluble in ethanol. Ceftiofur is semi-synthetic third-generation animal-specific cephalosporin.

Cephalosporin antibacterial drugs are effective drugs for veterinary treatment, and now they are used more and more widely in the livestock and poultry breeding industry. From the point of view of drug molecular structure, all cephalosporin drug molecules contain the structure of cephem, so they belong to beta lactam antibiotics, which is the 7-aminocephalosporan acid (7-ACA) in beta lactam antibiotics, so they have similar sterilization mechanisms.

From the perspective of antibacterial action mechanism, this kind of antibacterial drugs can destroy the cell wall of bacteria and show the strongest bactericidal effect during the reproduction period. It has strong selective effect on bacteria, but almost no toxicity to the animal body; and has the advantages of broad antibacterial spectrum, strong antibacterial effect, resistance to penicillinase, and less common allergic reactions than penicillins. Therefore, they are a kind of important antibiotics with high efficiency, low toxicity and wide clinical application.

2. Pharmacodynamics

It is the third generation cephalosporins for animals with strong antibacterial activity, broad antibacterial spectrum. It has strong effects against Gram-negative bacteria such as Escherichia coli, Salmonella, Pasteurella multocida, and Actinobacillus pleuropneumoniae, etc.; the effect against gram-positive bacteria is weaker than that of the first generation.

This product is not absorbed by oral administration. It is rapidly absorbed by intramuscular and subcutaneous injection, and is widely distributed. The effective blood concentration is maintained for a long time. It first metabolized into active deoxyfuroyl ceftiofur, and then metabolized into non-live milk products. Most of them are eliminated by urine and feces within 24h after intramuscular injection.

Compared with the previous two generations, the third-generation cephalosporins have reduced activity against G+ cocci, enhanced stability to G-bacillus lactamase, and effective anti-G-bacillus effect, which is significantly better than the first and second generations; the antibacterial spectrum has been significantly expanded, and the antibacterial effect on anaerobic bacteria and Pseudomonas aeruginosa has been increased. The third-generation cephalosporins can reach different tissues, synovial cavity and body fluids, and can directly reach the cerebrospinal fluid of patients with meningeal inflammation; no nephrotoxicity. Representative drugs mainly include ceftiofur.

The third-generation cephalosporins are the most widely used cephalosporins in hospitals. They are divided into two categories according to their characteristics of killing gram-negative bacilli. One type mainly kills Enterobacteriaceae bacteria such as Escherichia coli, Proteus, Klebsiella, and also has the effect of killing Gram-positive bacteria. Commonly used are ceftriaxone and ceftiofur, etc.; the other is mainly to kill Pseudomonas aeruginosa, and also includes other gram-negative bacilli.

3. Pharmacokinetics

This product is quickly absorbed after intramuscular and subcutaneous injection, with high drug concentration in the blood and tissues, and the effective blood drug concentration is maintained for a long time, the elimination is slow, and the half-life is long. After intramuscular injection to cattle and pigs, it is quickly absorbed within 15min and forms the first-level metabolite Desfuroyl ceftiofur (DFC) in the plasma. Since the lactam ring is not damaged, its antibacterial activity is consistent with that of Ceftiofur. DFC can further form inactive DFC cysteine ​​difluid in the tissue. The apparent volume of distribution of this product ≤ 1L/KG. Pigs, sheep, and cattle have the highest concentration in the kidney after intramuscular injection of multiple doses, followed by lung, liver, fat and muscle, which can generally maintain a concentration higher than MIC.

For example, pigs are injected intramuscularly at 3 mg/kg once a day for 3 days. The tissue concentrations are: plasma 3.25, respiratory tract 0.60, skin 0.57, lung 0.49, tonsil 0.30, and joint fluid 0.29. Cows were injected intramuscularly at 1 mg/kg, once a day for 5 days, and their tissue concentrations were plasma 1.0 (7.5H after injection), joint fluid 0.65 (2.5H after injection), lung 0.36, and jejunum 0.34. It mainly appears in the formation of the inactive free metabolite-DFC cysteine ​​disulfide in milk. Cefoxifur is excreted slowly, and its half-lives on animals are significantly different (T1/2 for horses, cattle, sheep, pigs, dogs, chickens, and turkeys) are 3.15, 7.12, 2.83, 14.5, 4.12, 6.77 and 7.45H. But most of them can be excreted in urine and feces within 24 hours after intramuscular injection. DFC is rapidly degraded to inactive compounds in the feces of cattle, pigs and chickens.

Ceftiofur Uses


1. Indications

It is used for animal respiratory and urinary tract infections caused by sensitive bacteria, such as bovine transportation fever and pneumonia, yellow diarrhea, actinobacillus haemophilus causing porcine pleuropneumonia, equine respiratory tract infection caused by streptococcus, Escherichia coli and Proteus mirabilis canine urinary tract infection caused by E. coli infection in chickens.

  • Infectious pleuropneumonia of swine is a contagious disease caused by Actinobacillus pleuropneumonia. It is a second-class infectious disease and parasitic disease. It is an important respiratory disease in pigs. It is prevalent in countries raising pigs and has become one of the world's five major diseases of industrialized pig raising, causing significant economic losses. Porcine infectious pleuropneumonia is a worldwide disease, which is widely distributed in all pig-raising countries in the world, including the United Kingdom, Germany, Switzerland, Denmark, Australia, Canada, Mexico, Argentina, Sweden, Poland, Japan, the United States, and China. In particular, the prevalence of this disease has been on the rise in the past ten years, and it is recognized internationally as one of the important diseases that endanger the modern pig industry.
  • Beef transportation fever is a stress syndrome, which is caused by infection with a variety of pathogenic microorganisms. The main characteristics are high fever and interstitial and lobar pneumonia. Animals have been transported over long distances, facing cold or heat, fright, close contact and cross-infection, resulting in a rapid decline in beef cattle resistance, imbalance of the body, potential bacteria, often in rapid outbreaks of pathogenic bacteria, such as cold viruses, pasteurella, Mycoplasma, respiratory syncytial virus, viral diarrhea, foot-and-mouth disease, etc. The main symptoms of sick cows are high fever, purulent conjunctivitis, constant tears, runny nose, frequent coughing, difficulty breathing, and foamy saliva. Usually fattening cattle are prone to this disease, and it is also one of the causes of cattle death.

2. Uses

It has broad potential sterilization effect. It is effective against both gram-positive and blue-negative bacteria. The antibacterial activity is stronger than ampicillin, and the activity against streptococcus is better than that of quinolones. This product is quickly absorbed after intramuscular injection, and is mainly used for respiratory diseases (transportation fever, pneumonia) caused by Pasteurella hemolyticus, Pasteurella multocida and Haemophilus saccharum. It is also effective for respiratory infections such as Corynebacterium pyogenes. It can also treat foot rot caused by Fusobacterium necrosis and Bacteroides niger.

  • It is mainly used for respiratory diseases (transportation fever, pneumonia) caused by hemolytic Pasteurella, Pasteurella multocida and Haemophilus saccharomyces. It is also effective for respiratory infections such as Corynebacterium pyogenes.
  • Pigs: Used for respiratory diseases (porcine bacterial pneumonia) caused by Actinobacillus pleuropneumoniae, Pasteurella multocida, Salmonella cholerae and Streptococcus suis.
  • Horse: Mainly used for respiratory infections caused by veterinary streptococcus. It is also effective for respiratory infections such as Pasteurella, Streptococcus equi, Proteus, Moraxella, etc.
  • Dogs: used for urinary tract infections caused by Escherichia coli and Proteus mirabilis.
  • One-day-old chickens: control colibacillosis related to early death of chickens.

3. Dosage

Intramuscular injection: One dose per 1kg body weight, cattle 1.1~2.2mg, horse 2.2~4.4mg, once a day for 3 days.

Subcutaneous injection: once per 1 kg body weight Dog 2.2 mg once a day, continuous use for 5 to 14 days

One-day-old chickens 0.08~0.20mg per bird (under the skin)

Preparation and specifications: Ceftiofur Hydrochloride Suspension Injection 100ml:5g

Ceftiofur side effects


1. Adverse Reactions

  • Allergic reactions, mainly erythema and urticaria, itching, drug fever, occasionally angioedema, asthma and hypotension.
  • Gastrointestinal reactions such as nausea, vomiting and diarrhea.
  • Serum alanine aminotransferase may be slightly elevated.
  • Local intramuscular injection can cause pain, and intravenous injection can cause phlebitis or thrombophlebitis.
  • Nervous system reactions such as headache, dizziness and sensory disturbances can be seen.
  • Patients who are allergic to cephalosporin antibiotics should not be used.

2. Incompatibility

Cephalosporins are widely used for both human and veterinary use, and there are many varieties, but when we use them, we must pay attention to their compatibility. It is best to follow the doctor's instructions for medication, and do not use them randomly, otherwise the losses are large! Among them, ceftiofur cannot be compatible with dexamethasone, hydrocortisone and other drugs.

Ceftiofur is a third-generation cephalosporin with a broad-spectrum antibacterial effect.

Dexamethasone is a long-acting anti-inflammatory, anti-toxin, and anti-allergic adrenal glucocorticoid drug. Ceftiofur is oxidizing (contains multiple imino groups and amide groups), and dexamethasone is reductive (contains two ethylenic bonds). If the two are mixed together, redox reaction or polymerization reaction will occur.

These two drugs are widely used in veterinary clinics. Especially in the case of infection accompanied by fever, more attention should be paid.

  • Aminoglycoside antibiotics: the combination has a synergistic effect, but the nephrotoxicity increases, and those with poor renal function should be used with caution.
  • Probenecid: Combined used to delay the excretion of cephalosporins and increase the blood concentration.
  • Coumarin anticoagulant: combined used to enhance anticoagulant effect.
  • Antibacterial drugs: combined use reduces the efficacy of this product.
  • Cholestyramine: combined with cephalexin in the intestinal tract, slows down the absorption and lowers the blood concentration, but the total absorption is not affected.
  • Strong diuretics: combined use aggravates nephrotoxicity.
  • Compatibility with the following drugs: terramycin hydrochloride, aureomycin hydrochloride, tetracycline hydrochloride, colistin sulfate, polymyxin E, erythromycin lactobionate, lincomycin, sulfaoxazole, Calcium chloride, etc.

3. Warnings

  • Horses who use ceftiofur under stress conditions are prone to acute diarrhea, which can be fatal. Once it occurs, the drug should be stopped immediately and corresponding treatment should be taken.
  • Ceftiofur sodium for injection should be used in accordance with the prescribed dose, treatment course and route of administration, and there is no pro-slaughter drug period and milk waste period.
  • Withdrawal period: Ceftiofur sodium for injection, 3d for cattle, 2d for pigs; Ceftiofur for injection, 1d for pigs.
  • It is mainly excreted through the kidneys, and the dosage should be adjusted for animals with renal insufficiency.
  • Before using ceftiofur sodium for injection, dissolve it in water so that each ML contains 50 mg of ceftiofur (refrigerated protection at 2~8 °C for 7 days, and protection at 15~30 °C for 12 hours at room temperature).


Ceftiofur is the first animal-specific third-generation cephalosporin antibiotic. It has the characteristics of broad antibacterial spectrum and strong antibacterial activity. After administration, it is absorbed rapidly, with high bioavailability, long half-life and lasting efficacy. In recent years, ceftiofur has been widely used in veterinary area.

Ceftiofur belongs to beta lactams. And BALLYA provides a betalactam test to tell you if there are beta lactams residues in dairy products you eat every day.


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