Application of Ceftriaxone
in Anti-infective Therapy I. Introduction Infectious diseases have always been one of the important factors endangering human health worldwide, and timely and effective anti-infective therapy is essential for the rehabilitation of patients. Ceftriaxone, as the third generation cephalosporin, has been widely used in the treatment of various infectious diseases, showing good antibacterial activity, pharmacokinetic properties and relatively good safety. This article will introduce the relevant information of ceftriaxone in anti-infective therapy in detail, including its antibacterial spectrum, mechanism of action, pharmacokinetic characteristics, clinical application, adverse reactions and precautions. 2. Antimicrobial spectrum of ceftriaxone Ceftriaxone has a wide antimicrobial spectrum and has significant antimicrobial effect on a variety of Gram-positive and Gram-negative bacteria. In terms of Gram-positive bacteria, it has good antibacterial activity against Streptococcus pneumoniae (including penicillin-resistant strains) and Streptococcus pyogenes, and can effectively inhibit the growth and reproduction of these bacteria, thus playing an important role in the treatment of respiratory tract infections, skin and soft tissue infections and other diseases caused by these pathogens. For Gram-negative bacteria, the antibacterial ability of ceftriaxone is more prominent. It has strong bacteriostatic and bactericidal effects on common gram-negative pathogens such as Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis and Haemophilus influenzae. This makes ceftriaxone become one of the commonly used anti-infective drugs in the treatment of urinary tract infections, abdominal infections, biliary tract infections, lower respiratory tract infections and many other diseases caused by Gram-negative bacteria. In addition, ceftriaxone also has a certain antibacterial effect on some anaerobic bacteria, although its antibacterial activity is slightly weaker than that of aerobic bacteria, but in some cases of mixed infection, it can also contribute to the anti-infective treatment. 3. Mechanism of action of ceftriaxone The antibacterial mechanism of ceftriaxone is mainly achieved by inhibiting the synthesis of bacterial cell wall. The cell wall of bacteria is essential for maintaining the morphology, structure and survival of bacteria. Ceftriaxone can bind to penicillin-binding proteins (PBPs), a key enzyme in bacterial cell wall synthesis, thus interfering with the normal steps of cell wall synthesis. Specifically, when ceftriaxone binds to PBPs, the synthesis of bacterial cell wall is blocked, making it impossible for bacteria to form a complete and strong cell wall. With the growth and division of bacteria, due to the defect of cell wall, bacterial cells will gradually expand, deform, and eventually rupture and die, so as to achieve the purpose of killing bacteria. This mechanism of action enables ceftriaxone to play an antibacterial role specifically against bacteria, while the impact on human cells is relatively small, because human cells do not have cell wall structure, so at normal doses, ceftriaxone generally does not cause significant damage to human cells. 4. Pharmacokinetic characteristics of ceftriaxone Ceftriaxone has some unique advantages in pharmacokinetics, which are also conducive to its wide clinical application. First, ceftriaxone has good tissue permeability. It can be widely distributed in various tissues and body fluids of the human body, including blood, cerebrospinal fluid (which can enter cerebrospinal fluid through the blood-brain barrier during inflammation), bile, pleural effusion, ascites and so on. This enables ceftriaxone to play an effective antibacterial role in the treatment of systemic infections and some special infections (such as central nervous system infections, biliary tract infections, etc.). Secondly, the plasma half-life of ceftriaxone is longer, generally up to about 7-8 hours. A longer half-life means that the drug will stay in the body for a relatively long time and does not need to be administered frequently. In clinical practice, effective blood concentration can be maintained only once or twice a day, which not only facilitates the medication of patients, but also improves the compliance of patients. In addition, ceftriaxone is mainly metabolized by kidney and liver, of which about 50% -60% is excreted in urine in its original form, while the rest is excreted through bile. This dual route of excretion allows ceftriaxone to be used relatively safely even in patients with some impairment of renal or hepatic function, although the dosage may need to be adjusted according to the patient’s specific situation. 5. Clinical application of ceftriaxone Ceftriaxone has a wide range of clinical applications, covering a variety of different types of infectious diseases. 1. Respiratory tract infection: Whether it is upper respiratory tract infection or lower respiratory tract infection, as long as it is caused by pathogenic bacteria sensitive to ceftriaxone, ceftriaxone can be considered for treatment. For example, in the treatment of pneumonia, ceftriaxone is often an important part of the treatment regimen for community-acquired pneumonia caused by Streptococcus pneumoniae, Haemophilus influenzae, etc. 2. Urinary tract infection: Ceftriaxone has strong antibacterial activity against common pathogens of urinary tract infection such as Escherichia coli and Proteus mirabilis, so it can effectively remove pathogens and alleviate symptoms of patients in the treatment of acute pyelonephritis, cystitis and other urinary tract infection diseases. 3. Abdominal infection: Abdominal infection is often caused by mixed infection of a variety of pathogenic bacteria, of which Gram-negative bacteria account for a large proportion. Ceftriaxone plays an important role in the treatment of abdominal infections, such as peritonitis caused by appendicitis perforation, cholecystitis and biliary tract infection caused by cholelithiasis. 4. Skin and soft tissue infections: For skin and soft tissue infections caused by Streptococcus pyogenes and Staphylococcus aureus, such as furuncle, carbuncle and impetigo, ceftriaxone can also alleviate the symptoms of patients and promote wound healing by inhibiting the growth and reproduction of pathogenic bacteria. 5. Central nervous system infection: In the state of inflammation, ceftriaxone can enter the cerebrospinal fluid through the blood-brain barrier, which has a certain therapeutic effect on meningitis and other central nervous system infections caused by meningococcus and Streptococcus pneumoniae. However, in the treatment of central nervous system infections, higher doses and combinations with other anti-infective drugs are usually required to ensure adequate antimicrobial efficacy. 6. Adverse reactions of ceftriaxone Although ceftriaxone performs well in anti-infective therapy, there are also some possible adverse reactions. 1. Allergic reaction: This is one of the most common adverse reactions during the use of ceftriaxone. Patients may have skin rash, itching, Urticaria and other skin allergy symptoms, serious cases may appear anaphylactic shock, life-threatening. Therefore, before using ceftriaxone, patients must be asked about their allergic history, and patients with allergic history of cephalosporins or penicillins should be used with great caution. 2. Gastrointestinal reactions: Some patients will have gastrointestinal discomfort after using ceftriaxone, such as nausea, vomiting, diarrhea, abdominal pain and other symptoms. These symptoms are generally relatively mild and usually resolve gradually after the drug is stopped. 3. Hematological reactions: a small number of patients may have adverse reactions in the hematological system, such as leukopenia, thrombocytopenia, anemia, etc. These adverse reactions usually need to be detected by regular blood routine examination, and once they occur, the medication regimen may need to be adjusted. 4. Liver and kidney function damage: Although ceftriaxone is metabolized by kidney and liver, the damage to liver and kidney function is relatively small under normal use. However, in the case of long-term high-dose use or patients with their own liver and kidney function problems, further damage to liver and kidney function may occur, so close attention should be paid to the liver and kidney function indicators of patients when using in these cases. 7. Precautions for the use of ceftriaxone In order to ensure the safe and effective use of ceftriaxone in anti-infective treatment, the following are some precautions. 1. Allergic history inquiry: Before using ceftriaxone, be sure to inquire about the patient’s allergic history in detail, including whether there is an allergic history of cephalosporins, penicillins and other antibiotics. For patients with a history of allergies, other appropriate anti-infective drugs should be used cautiously or selected. 2. Dosage adjustment: adjust the dosage of ceftriaxone according to the patient’s age, weight, liver and kidney function and other factors. In patients with a certain degree of impairment of renal or hepatic function, it may be necessary to reduce the dose appropriately to avoid the accumulation of drugs in the body, leading to an increase in adverse reactions. 3. Incompatibility: Ceftriaxone has some incompatibility in the solution, for example, it can not be mixed with calcium-containing solutions (such as calcium gluconate, calcium chloride, etc.), otherwise it may form insoluble precipitates, affect the efficacy of the drug, and may even lead to adverse reactions. 4. Monitoring indicators: In the process of using ceftriaxone, it is necessary to regularly monitor the vital signs, blood routine, liver and kidney function and other indicators of patients, so as to detect possible adverse reactions in time and take appropriate measures to deal with them. 8. Conclusion Ceftriaxone, as an important third-generation cephalosporin antibiotic, plays an important role in anti-infective therapy. It has a broad antibacterial spectrum, unique mechanism of action, good pharmacokinetic characteristics, and can effectively treat various types of infectious diseases. However, it is also necessary to pay attention to the possible adverse reactions and precautions in the use process to ensure its safe and effective anti-infective treatment for patients. With the continuous development of medicine, our understanding and application of ceftriaxone will continue to deepen, so that it will continue to play an important role in the field of anti-infective treatment in the future.
