Overview of the second generation cephalosporin antibiotics of Youlexin. It is stable to β -lactamase and has stronger antibacterial activity against gram-positive bacteria than the first generation, and also has better antibacterial activity against some gram-negative bacteria. Suitable for respiratory tract, abdominal cavity, urinary tract, bone and joint infection, skin and soft tissue infection and septicemia caused by sensitive bacteria.
3 Instructions for Youlexin 3. 1 Drug Name Youlexin
3.2 English name Cefuroxime
3.3 Youlexin alias cefuroxime; Cefuroxime; Xin Fuxin; Cefuroxime axetil; New fungus spirit; Youlexin ester; Xi Lixin; Zinacef Zinnat; Cefuroxime axetil; Kefurox cefuroxime sodium
3.4 Classification of antibiotics >; Cephalosporin >: the second generation
3.5 dosage form 1. Injection: 0.75g,1.5g, 0.25g, 0.5g. ..
2. Tablets: 0.125g, 0.25g, 0.5g. ..
3.6 The pharmacological action of Youlexin is stronger than that of the first generation cephalosporins in terms of activity against Gram-negative bacilli and stability against Gram-negative bacilli β-lactamases. The effect on gram-positive cocci (including enzyme-resistant Staphylococcus aureus) is similar to or slightly worse than that of the first generation cephalosporins, but stronger than that of the third generation cephalosporins. Youlexin has strong antibacterial activity against Streptococcus pneumoniae, Neisseria gonorrhoeae, Klebsiella pneumoniae, Streptococcus, Meningococcus, Proteus mirabilis, Staphylococcus, Haemophilus influenzae, Salmonella, Moraxella catarrhalis, Escherichia coli and Shigella. It also has certain antibacterial activity against anaerobic bacteria (except Bacteroides fragilis). Acinetobacter, Serratia, MRSA, Enterobacter, Indole-positive Proteus, Bacteroides fragilis, Pseudomonas aeruginosa, Enterococcus, Mycoplasma and Chlamydia.
3.7 Pharmacokinetics of Youlexin The absolute bioavailability of male volunteers taking 0.5g on an empty stomach is 36%, and that after meals is 52%. Taking it with food and milk can increase the absorption of drugs. Take 250 ~ 500 mg immediately after meals. After about 2 hours, the average serum Cmax was 4. 1mg/L and 7mg/L respectively. After 65438 0.2 hours, the amount of the prototype Youlexin recovered in urine is about 43% ~ 52% of the drug dose. After intramuscular injection of 750mg, the peak time of blood drug concentration was about 45min, and the average blood drug concentration was 27 μ g/ml. After intravenous injection of 1g, the peak plasma concentration was 144μg/ml. After absorption, the drug is well distributed in body fluids and tissues, and can enter inflammatory cerebrospinal fluid (patients with bacterial meningitis are injected 3g intravenously every 8 hours, and the concentration of cerebrospinal fluid can reach 0. 1 ~ 22.8μ g/ml). After intramuscular injection of 750mg every 8 hours, the drug concentration in sputum was 0.17.8 μ g/ml; The drug concentration in bile was 65438 0.5 ~ 65438 0.5 μ g/ml 2.5h after injection. After intramuscular injection of 750mg or intravenous injection of 1.5g, the drug concentration in bone tissue can reach 2.4μg/ml and 19.4μg/ml respectively. The drug concentration of skin blister fluid is close to that of blood. The drug concentration of amniotic fluid after intramuscular injection is similar to that of blood. Youlexin can also be distributed in parotid fluid, aqueous humor and milk. The binding rate of serum protein of Youlexin was 365,438+0% ~ 465,438+0%. Most drugs are excreted through glomerular filtration and renal tubular secretion within 24 hours after administration. The half-life of drug serum is 1.2h, which can be extended for newborns and patients with renal insufficiency. Hemodialysis can reduce the plasma concentration of Youlexin.
3.8 Indications of Youlexin 1. Lower respiratory tract infection.
2. Urinary tract infection.
3. Bone and joint infections.
4. Skin and soft tissue infections.
5. Acute purulent meningitis (used to treat meningitis caused by meningococcus and Haemophilus influenzae resistant to sulfonamides, penicillin or ampicillin).
6. Sepsis and other serious infections.
7. Simple gonorrhea caused by penicillin-resistant strains. Youlexin can also be used for preoperative preventive medication.
3.9 Contraindications to Youlexin are allergic to Youlexin or other cephalosporins.
3. 10 Precautions 1. Allergy to one cephalosporin may be allergic to other cephalosporins; People who are allergic to penicillin, penicillin derivatives or penicillamine may also be allergic to cephalosporins.
2. Use with caution: (1) Pregnant and lactating women; (2) Premature infants and newborns; (3) Patients with a history of gastrointestinal diseases, especially ulcerative colitis, localized enteritis or antibiotic-associated pseudomembranous colitis; (4) Severe liver and renal insufficiency; (5) people with high allergies; (6) the elderly and infirm.
3. Influence of drugs on test value or diagnosis: (1) Direct anti-human globulin (Coombs) test can produce positive reaction; (2) The blood glucose test of ferricyanide was false negative; (3) Copper sulfate urine glucose test is false positive, but it does not affect the regularity of glucoamylase test.
3. 1 1 Adverse reactions of Youlexin The adverse reactions of Youlexin are mild and short-lived, and the rash is the most common, which can reach about 5%. About 5% patients may have elevated serum transaminase, increased eosinophils and decreased hemoglobin. Pain in intramuscular injection area is common, but mild. Phlebitis is rare.
3. Usage and dosage of 1 2 Youlexin1 (1) intramuscular injection: ① mild to moderate infection: 2.25~4.5g daily, every 8 hours 1 time. ② Severe infection: it can be increased to 6g per day, and the dosage is 1.5g, once every 6 hours. ③ Meningitis: The daily dose should not exceed 9g. ④ Simple gonorrhea: single dose 1.5g, oral probenecid 1g, can treat simple gonorrhea caused by penicillin-resistant strains. (2) Intravenous administration: ① Mild to moderate infection: 2.25~4.5g per day, every 8 hours 1 time. ② Severe infection: it can be increased to 6g per day, and the dosage is 1.5g, once every 6 hours. ③ Meningitis: The daily dose should not exceed 9g. (3) Dose of renal insufficiency: The dosage scheme for patients with renal insufficiency is based on creatinine clearance rate: ① For patients with creatinine clearance rate greater than 20ml minutes, 0.75 ~ 1.5g each time, 3 times a day; ② creatinine clearance rate 10 ~ 20ml per minute, 0.75g each time, twice a day; ③ The creatinine clearance rate is less than 10ml per minute, 0.75g each time, one day 1 time. (4) Dialysis dosage: 750mg after each dialysis.
2. Children: (1) intramuscular injection: 50 ~ 100 mg/kg daily, every 6 ~ 8 hours 1 time; For infants older than 3 months, every 8 hours 16.7 ~ 33.3 mg/kg. Bone infection, 50mg/kg every 8 hours. Bacterial meningitis, 200 ~ 240 mg/kg daily, every 6 ~ 8 hours 1 time. (2) Intravenous administration: 50 ~ 100 mg/kg daily, every 6 ~ 8 hours 1 time. For infants older than 3 months, every 8 hours 16.7 ~ 33.3 mg/kg. Bone infection, 50mg/kg every 8 hours. Bacterial meningitis, 200 ~ 240 mg/kg daily, every 6 ~ 8 hours 1 time.
3. 13 drug interaction 1. The combination of Youlexin and aminoglycosides has synergistic antibacterial effect, but it may increase nephrotoxicity.
2. Combined with probenecid can prolong the plasma half-life of Youlexin and increase its plasma concentration.
3. The combination of Youlexin and furosemide can increase nephrotoxicity.
4. The combination of Youlexin and live typhoid vaccine can weaken the immune response of the body to live typhoid vaccine, and the possible mechanism is that Youlexin has antibacterial activity against Salmonella typhi.
3. 14 Experts commented that Youlexin is a second-generation broad-spectrum semi-synthetic cephalosporin, which has strong antibacterial effect on almost all strains sensitive to cefotaxime and cefotaxime, and is effective on a wide range of gram-negative bacilli including Enterobacter and Indole-positive Proteus. The clinical and bacteriological effective rate of Youlexin in treating respiratory tract, facial features, bone and soft tissue infection, meningitis and simple urinary tract infection is 70% ~ 100%, and the prevention of postoperative infection after trauma is also satisfactory. Youlexin is very effective in treating acute gonorrhea and urinary tract infection caused by gonococcal infection. A hospital 169 patients with gonorrhea were given a single dose 1.5g intramuscular injection, 160 patients were given intramuscular injection 1 ~ 5 days. Blister disappeared and the cure rate was 97.7%. The short-term and long-term bacteriological cure rates of Youlexin were 55% and 48%, respectively.
4 Youlexin poisoning Youlexin (cefuroxime, Celine, Mingkexin, Rifalao) belongs to the second generation of cephalosporin antibiotics. It is stable to β -lactamase and has stronger antibacterial activity against gram-positive bacteria than the first generation, and also has better antibacterial activity against some gram-negative bacteria. Suitable for respiratory tract, abdominal cavity, urinary tract, bone and joint infection, skin and soft tissue infection and septicemia caused by sensitive bacteria. The plasma protein binding rate of the drug is 3 1% ~ 4 1%, and the half-life is 1. 1 ~ 1.4h, which can be extended to 15 ~ 22h in severe renal failure. The incidence of allergic reaction to penicillin is about 5%. Intramuscular injection or intravenous drip. The usual dose for adults is 750 ~ 1500mg, three times a day; In case of severe infection, 100mg/kg can be given in 3 ~ 4 times. [ 1]
4. 1 Clinical manifestations [1]
1. The adverse reactions were mild and short-lasting. The incidence of rash is about 5%; About 5% patients have elevated serum transaminase; Occasionally, eosinophilia, hemoglobin decrease or Combs test is positive.
2. Local pain caused by intramuscular injection is common, and thrombophlebitis is rare.
4.2 The treatment points of Youlexin poisoning are [2]:
1. This drug is prohibited for people who are allergic to penicillin or cephalosporin.