药品信息:
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中文名称:氟氯西林
中文别名:(2S,5R,6R)-6-[[3-(2-氯-6-氟苯基)-5-甲基-1,2-恶唑-4-甲酰]氨基]-3,3-二甲基-7-氧代-4-硫杂-1-氮杂双环[3.2.0]庚烷-2-羧酸; 福氯平; 氟氯西林酸;
英文名称:flucloxacillin
作用应用
对溶血性链球菌等链球菌属,肺炎链球菌和不产青霉素酶的葡萄球菌具有良好抗菌作用。对肠球菌有中等度抗菌作用,淋病奈瑟菌、脑膜炎奈瑟菌、白喉棒状杆菌、炭疽芽孢杆菌、牛型放线菌、念珠状链杆菌、李斯特菌、钩端螺旋体和梅毒螺旋体对本品敏感。本品对嗜血杆菌和百日咳鲍特氏菌亦具一定抗菌活性,其他革兰阴性需氧或兼性厌氧菌对本品敏感性差.本品对梭状芽孢杆菌属、消化链球菌、厌氧菌以及产黑色素拟杆菌等具良好抗菌作用,对脆弱拟杆菌的抗菌作用差。青霉素通过抑制细菌细胞壁四肽则链和五肽交连桥的结合而阻碍细胞壁合成而发挥杀菌作用。对革兰阳性菌有效,由于革兰阴性菌缺乏五肽交连桥而青霉素对其作用不大。
药代动力学
本品口服不吸收。肌注1g后,血药峰浓度于0.8h后到达,为44.6mg/L,生物利用度89.5%。分布容积广,為20.6L。消除半减期1.9h。静脉推注1g(推注10min)的即刻血药浓度134mg/L:24h内约70%以原形由尿液排出,约1%~2%由粪排出。4h血透可清除本品,25%~50%,6h腹膜透析仅清除10%。本品蛋白结合率45%~60%。体内分布广,能分布到全身组织和体液中,乳汁中含量少;脑膜炎时脑脊液内可达有效浓度。
注意事项
1、氟氯西林与青霉素类、头孢菌素类或青霉胺有交叉过敏。
2、对本品及其它青霉素类、头孢菌素类或青霉胺过敏者禁用。
3、有肝、肾功能障碍的患者慎用,有哮喘史或对其它药物产生过敏型反应的患者慎用。
4、氟氯西林治疗期间或治疗后出现发热、皮疹、皮肤瘙痒症状的患者,应监测肝脏功能。建议住院病人在治疗前和口服或静脉用氟氯西林7天后,检查肝脏功能。
不良反应
1、口服给药时较常见胃肠道反应,如恶心、呕吐、腹胀、腹泻、食欲不振等。
2、大剂量使用氟氯西林可出现神经系统反应,如抽搐、痉挛、神志不清、头痛等。
3、大剂量使用氟氯西林偶见中性粒细胞减少,对特异体质者可致出血倾向。
4、少数患者用药后可致急性胆汁淤积和氨基转移酶升高。
5、用药后可见药疹、药物热等过敏反应。
6、长期用药可致菌群失调,发生二重感染。
7、肌内注射或静脉给药时可致注射部位疼痛、
硬结,严重者可致血栓性静脉炎。
药物相互作用
1、本药与阿米卡星联用可增强对金葡菌的抗菌作用。
2、氟氯西林与伤寒活疫苗同用,可使伤寒活疫苗的免疫反应降低。
3、丙磺舒可影响本药排泄从而升高本药的血药浓度
4、氟氯西林与氨甲蝶呤同用,可使氨甲蝶呤的药物浓度时间曲线下面积(AUC)下降,但这种结果只有统计学上的显著差异,而无临床意义。
5、有报道,氟氯西林与氨基糖苷类联用将导致氨基糖苷类体内和体外失活,使氨基糖苷类的药效下降。
6、食物可显著延迟呋氯西林的吸收,并使其血浆峰浓度降低50%
Chinese name: Flucloxacillin
Chinese alias: (2S,5R,6R)-6-[[3-(2-chloro-6-fluorophenyl)-5-methyl-1,2-oxazole-4-formyl]amino ]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid; ciclopine; flucloxacillin;
English name: flucloxacillin
Action Application
It has a good antibacterial effect against Streptococcus such as Streptococcus hemolyticus, Streptococcus pneumoniae and Staphylococcus which does not produce penicillinase. Moderate antibacterial effect against Enterococcus, Neisseria gonorrhoeae, Neisseria meningitidis, Corynebacterium diphtheriae, Bacillus anthracis, Actinomycetes, Streptococcus faecalis, Listeria, Leptospira and Treponema pallidum This product is sensitive. This product also has certain antibacterial activity against Haemophilus and B. pertussis. Other Gram-negative aerobic or facultative anaerobic bacteria have poor sensitivity to this product. This product is against Clostridium, digestive streptococci, and nausea. Oxygen bacteria and Bacteroides-producing bacteria have good antibacterial activity, and have poor antibacterial activity against Bacteroides fragilis. Penicillin exerts a bactericidal action by inhibiting the cell wall synthesis by inhibiting the binding of the bacterial cell wall tetrapeptide chain and the pentapeptide cross-linking bridge. It is effective against Gram-positive bacteria, and penicillin is not effective because Gram-negative bacteria lack a pentapeptide cross-linking bridge.
Pharmacokinetics
This product is not absorbed orally. After intramuscular injection of 1g, the peak concentration of blood reached 0.8h after 4h, and the bioavailability was 89.5%. The distribution volume is wide, which is 20.6L. Eliminate the half-life by 1.9h. The immediate blood concentration of 134 mg/L of intravenous bolus 1g (bolus 10min): about 70% within 24h is discharged from the urine in the original form, and about 1% to 2% is excreted by the feces. 4h hemodialysis can remove this product, 25% to 50%, and only 10% of 6h peritoneal dialysis. The protein binding rate of this product is 45% to 60%. It is widely distributed in the body and can be distributed in whole body tissues and body fluids. The content in milk is small; in meningitis, the effective concentration in cerebrospinal fluid can be reached.
Notes
1. Flucloxacillin has cross-allergy to penicillins, cephalosporins or penicillamine.
2. It is forbidden to be allergic to this product and other penicillins, cephalosporins or penicillamine.
3, patients with liver and kidney dysfunction should be used with caution, and patients with a history of asthma or allergic reactions to other drugs should be used with caution.
4. Patients with fever, rash, and itching during or after flucloxacillin should be monitored for liver function. It is recommended that inpatients check liver function before treatment and 7 days after oral or intravenous flucloxacillin.
Adverse reactions
1, more common gastrointestinal reactions, such as nausea, vomiting, bloating, diarrhea, loss of appetite, etc..
2, high-dose flucloxacillin can cause nervous system reactions, such as convulsions, convulsions, confusion, headache and so on.
3, high-dose flucloxacillin occasional neutropenia, can cause bleeding tendency for those with normal constitution.
4, a small number of patients can cause acute cholestasis and elevated aminotransferase after administration.
5, after drug use, drug rash, drug fever and other allergic reactions can be seen.
6. Long-term medication can cause dysbacteriosis and double infection.
7, intramuscular injection or intravenous administration can cause pain at the injection site,
Induration, severe cases can cause thrombophlebitis.
Drug interaction
1. This medicine can be combined with amikacin to enhance the antibacterial effect against Staphylococcus aureus.
2. Flucloxacillin and typhoid live vaccine can reduce the immune response of live typhoid vaccine.
3, probenecid can affect the excretion of this drug to increase the blood concentration of the drug
4. Flucloxacillin and methotrexate can reduce the area under the drug concentration time curve (AUC) of methotrexate, but this result is only statistically significant, but has no clinical significance. .
5. It has been reported that the combination of flucloxacillin and aminoglycoside will result in the inactivation of aminoglycosides in vivo and in vitro, and the effect of aminoglycosides is lowered.
6. Food can significantly delay the absorption of furacillin and reduce its plasma peak concentration by 50%
Storage: (+15° ~ +25°C)
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