药品信息:
药理药动
本品为胶囊剂。
本品主要成分为头孢羟氨苄，其化学名为(6R,7R)-3-甲基-7-[(R)-2-氨基-2-(4-羟基苯基)乙酰氨基]-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-甲酸一水合物。
分子式：C16H17N3O5S·H2O
分子量：381.41
1．药理：头孢羟氨苄为第一代口服头孢菌素，对产青霉素酶和不产青霉素酶的金葡菌，凝固酶阴性葡萄球菌、肺炎链球菌、A组溶血性链球菌等大部分菌株具良好抗菌作用。对大肠埃希菌、奇异变形杆菌、沙门菌属、志贺菌属、流感嗜血杆菌和淋球菌亦有一定抗菌活性。甲氧西林耐药葡萄球菌、肠球菌属、吲哚阳性变形杆菌属、肠杆菌属、沙雷菌属等肠杆菌科细菌、铜绿假单胞菌属及脆弱拟杆菌等对本品耐药。
2．毒理：头孢羟氨苄属低毒。给新生大鼠12600mg/kg的高剂量未发生死亡；犬每日口服本品600mg/kg，大鼠每日口服本品1000mg/kg，连续6个月，对各组织器官未产生毒性反应。
药代动力学：
本品吸收良好，空腹口服0.5g后16mg/L的血药峰浓度(Cmax)于给药后1.5小时到达。给药后12小时尚可测得微量，血消除半衰期(t1/2β)为1.27～1.5小时。食物对血药峰浓度和t1/2β均无明显影响。头孢羟氨苄自胃肠道的吸收较头孢氨苄和头孢拉定缓慢，但维持的血药浓度较后两者持久。本品的蛋白结合率为20%。本品体内分布广泛，口服1.0g后2～5小时，痰、胸水和肺组织中的浓度分别为1.3mg/L，11.4mg/L，7.4mg/L（mg/kg）；骨骼、肌肉和滑囊液中的药物浓度分别为同期血药浓度的23%，31%和43%。胆汁药物浓度较血药浓度为低。本品可进入胎盘，也可进入乳汁。24小时累积排出给药量的86%。本品能为血液透析清除。
适 应 症
适用于敏感细菌所致的尿路感染、皮肤软组织感染以及急性扁桃体炎、急性咽炎、中耳炎和肺部感染等。本品为口服制剂，不宜用于重症感染。
用法用量
成人常用量：口服，一次0.5～1.0g，一日2次。
儿童常用量：一次按体重15～20mg/kg，一日2次。A组溶血性链球菌咽炎及扁桃体炎每12小时15mg/kg，疗程至少10天；成人肾功能减退者首次剂量为1g饱和量，然后根据肾功能减退程度予以延长给药间期。肌酐清除率为25～50ml/min、10～25ml/min和0～10ml/min时，分别每12小时、24小时和36小时服药500mg。
不良反应
本品不良反应发生率约为5%，以恶心、上腹部不适等胃肠道反应为主，少数患者尚可发生皮疹等过敏反应。偶可发生过敏性休克，也可出现尿素氮、血清氨基转移酶、血清碱性磷酸酶一过性升高。
禁忌症
对有头孢菌素类药物过敏史者和有青霉素过敏性休克史者或即刻反应史者禁用。
药物相互作用
丙磺舒可提高本品血药浓度，延缓肾排泄。
储藏：遮光，密封，在凉暗处保存。
Pharmacology pharmacokinetics
Cymbalta capsules.
The product is mainly composed cefadroxil, and its chemical name (6R, 7R) -3- methyl -7 - [(R) -2- amino-2- (4-hydroxyphenyl) acetamido] -8 oxo-5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-carboxylic acid monohydrate.
Formula: C16H17N3O5S · H2O
Molecular Weight: 381.41
1. Pharmacology: cefadroxil for the first-generation oral cephalosporin, against penicillinase and non-penicillinase of Staphylococcus aureus, coagulase-negative staphylococci, with most strains of Streptococcus pneumoniae, A group hemolytic streptococcus good antibacterial effect. Escherichia coli, Proteus mirabilis, Salmonella, Shigella, Haemophilus influenzae and Neisseria gonorrhoeae have a certain antibacterial activity. Methicillin-resistant Staphylococcus aureus, Enterococcus, indole-positive Proteus, Enterobacter, Serratia and other Enterobacteriaceae, Pseudomonas aeruginosa, and Bacteroides fragilis resistant to the chemicals and other.
2. Toxicology: cefadroxil low toxicity. To newborn rats 12600mg / kg of high dose not death occurred; dog daily oral administration of 600mg / kg, rats daily oral administration of 1000mg / kg, six months in a row, did not produce the various tissues and organs of toxicity.
Pharmacokinetics:
This product is well absorbed after oral fasting 0.5g 16mg / L of the peak plasma concentration (Cmax) arrives in 1.5 hours after administration. 12 hours after administration of fashion can be measured trace, blood elimination half-life (t1 / 2β) of 1.27 to 1.5 hours. Food for peak plasma concentrations and t1 / 2β were not significantly affected. Cefadroxil self-absorption in the gastrointestinal tract than the cephalexin and cephradine slowly but maintain blood concentration than the latter two lasting. The product of protein binding rate of 20%. This product is widely distributed in the body, 2 to 5 hours after oral administration of 1.0g, sputum, pleural effusion, and lung tissue concentrations of 1.3mg / L, 11.4mg / L, 7.4mg / L (mg / kg); bone, muscle and drug concentration in the synovial fluid of blood concentration over the same period were 23%, 31% and 43%. Bile drug concentration is lower than the plasma concentration. It can be used to enter the placenta, may also enter the milk. 24 hours 86% of the cumulative discharge of the dose. This product can do for hemodialysis.
Indications
Suitable for sensitive bacteria caused by urinary tract infections, skin and soft tissue infections and acute tonsillitis, acute pharyngitis, otitis media, and lung infections. This product is an oral formulation, not for severe infections.
Dosage
Dosage: Orally, 0.5 ~ 1.0g, 2 times a day.
Children in common: a body weight 15 ~ 20mg / kg, 2 times a day. Group A streptococcal pharyngitis and tonsillitis every 12 hours 15mg / kg, treatment for at least 10 days; adult renal dysfunction first dose of 1g saturated amount, and then be extended period of administration according to the degree of renal dysfunction. Creatinine clearance rate of 25 ~ 50ml / min, 10 ~ 25ml / min and 0 ~ 10ml / min, the separately every 12 hours, 24 hours and 36 hours taking 500mg.
Adverse reactions
This product adverse reactions occur in approximately 5%, with nausea, abdominal discomfort, gastrointestinal reactions, but a few can still be rash and other allergic reactions in patients. Can occur even anaphylactic shock can also occur urea nitrogen, serum aminotransferase, a transient increase in serum alkaline phosphatase.
Contraindications
To have the cephalosporins penicillin allergy history and a history of anaphylactic shock or immediate reaction history is disabled.
Drug Interactions
Probenecid may increase the plasma concentration of this product and delay renal excretion.
Storage: shading, sealed in a cool dark place. |
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