【药品名称】 通用名称：注射用头孢拉定 英文名称：Cefradine for Injection 汉语拼音：Zhusheyong Toubao Lading 【成份】本品主要成份为头孢拉定 化学名称：(6R,7R)-7[(R)-2-氨基-2-(1,4-环己烯基)乙酰氨基]-3-甲基-8-氧代-5-硫杂-1-氮杂双环[4、2、0]辛-2-烯-2-羧酸。 化学结构式： 分子式：C16H19N3O4S 分子量：349.40 【性状】本品为白色或类白色粉末。 【适应症】适用于敏感菌所致的急性咽炎、扁桃体炎、中耳炎、支气管炎和肺炎等呼吸道感染、泌尿生殖道感染及皮肤软组织感染等。 【规    格】按C16H19N3O4S 计算  0.5g  【用法用量】静脉滴注、静脉注射或肌内注射，成人，一次0.5～1.0g，每6小时1次，一日最高剂量为8g。儿童(1周岁以上)按体重一次12.5～25mg/kg，每6小时1次。 肌酐清除率大于20ml/min、5～20ml/min或小于5ml/min时，剂量宜调整为每6小时0.5g、0.25g和每12小时0.25g。 配制肌内注射用药时，将2ml注射用水加入0.5g装瓶内，须作深部肌内注射。 配制静脉注射液时，将至少10ml注射用水或5%葡萄糖注射液注入0.5g装瓶内。于5分钟内注射完毕。 配制静脉滴注液时，将适宜的稀释液10ml注入0.5g装瓶内，然后再以氯化钠注射液或5%葡萄糖液作进一步稀释。 【不良反应】本品不良反应较轻，发生率也较低，约6%。恶心、呕吐、腹泻、上腹部不适等胃肠道反应较为常见。药疹发生率约1%～3%，伪膜性肠炎、嗜酸性粒细胞增多、直接Coombs试验阳性反应、周围血象白细胞及中性粒细胞减少等见于个别患者。少数患者可出现暂时性血尿素氮升高，血清氨基转移酶、血清碱性磷酸酶一过性升高。本品肌内注射疼痛明显，静脉注射后有发生静脉炎的报道。 【禁忌】对头孢菌素过敏者及有青霉素过敏性休克或即刻反应史者禁用本品。 【注意事项】 1．在应用本品前须详细询问患者对头孢菌素类、青霉素类及其他药物过敏史，有青霉素类药物过敏性休克史者不可应用本品，其他患者应用本品时必须注意头孢菌素类与青霉素类存在交叉过敏反应的机会约有5%～7%，需在严密观察下慎用。一旦发生过敏反应，立即停用药物。如发生过敏性休克，须立即就地抢救，包括保持气道通畅、吸氧和肾上腺素、糖皮质激素的应用等措施。 2．本品主要经肾排出，肾功能减退者须减少剂量或延长给药间期。 3．应用本品的患者以硫酸铜法测定尿糖时可出现假阳性反应。 【孕妇及哺乳期妇女用药】因本品可透过血-胎盘屏障进入胎儿血循环，孕妇用药需有确切适应症。本品亦少量可进入乳汁，虽至今尚无哺乳期妇女应用头孢菌素类发生问题的报告，但应用时仍须权衡利弊。 【儿童用药】 未进行此项试验。 【老年用药】伴有肾功能减退的老年患者，应适当减少剂量或延长给药间期。 【药物相互作用】 1.头孢菌类可延缓苯妥英钠在肾小管的排泄。 2.保泰松与头孢菌素类抗生素合用可增加肾毒性。 3.与呋塞米、依他尼酸、布美他尼等强利尿药合用，可增加肾毒性，与卡氮芥、链佐星等抗肿瘤药合用也有增加肾毒性的可能。 4.与美西林联合应用，对大肠埃希菌、沙门菌属等革兰阴性杆菌具有协同作用。 5.丙磺舒可延迟本品肾排泄。 6. 本品与氨基糖苷类抗生素可相互灭活，当两药同时给予时，应在不同部位给药，两类药物不能混入同一容器内。 【药物过量】 未进行此项试验 【药理毒理】本品为第一代头孢菌素，对不产青霉素酶和产青霉素酶金葡菌、凝固酶阴性葡萄球菌、A组溶血性链球菌、肺炎链球菌和草绿色链球菌等革兰阳性球菌的部分菌株具良好抗菌作用。厌氧革兰阳性菌对本品多敏感，脆弱拟杆菌对本品呈现耐药。耐甲氧西林葡萄球菌属、肠球菌属对本品耐药。本品对革兰阳性菌与革兰阴性菌的作用与头孢氨苄相似。本品对淋球菌有一定作用，对产酶淋球菌也具活性；对流感嗜血杆菌的活性较差。 【药代动力学】静脉滴注本品0.5g，5分钟后血药浓度为46mg/L，肌内注射0.5g后平均6mg/L的血药峰浓度(Cmax)于给药后1～2小时到达。肌内注射吸收较口服为差，但血药浓度维持较久。血消除半衰期(t1/2b)为0.8～1小时。本品在组织体液中分布良好。肝组织中的浓度与血清浓度相等。在心肌、子宫、肺、前列腺和骨组织中皆可获有效浓度。脑脊液中药物浓度仅为同期血药浓度的8%～12%。本品可透过血-胎盘屏障进入胎儿血循环，少量经乳汁排出。血清蛋白结合率为6%～10%。静脉给药后6小时尿中累积排出量为给药量的90%以上；肌内注射后6小时尿中累积排出给药量的66%。尿中浓度甚高，多可超过1000mg/L。少量本品可自胆汁排泄，后者的浓度可为血清浓度的4倍。本品在体内很少代谢，能为血液透析和腹膜透析清除。丙磺舒可减少本品经肾排泄。 【贮    藏】密闭，在凉暗处(不超过20℃)保存。 【包    装】抗生素瓶装，10瓶/盒。 【有 效 期】  24个月 【执行标准】《中国药典》2005年版二部 【批准文号】 国药准字H20058003 【生产企业】广东博洲药业有限公司 Cefmore ™ Cefmore™头孢拉定（美国药典） Cephradine (USP) Cephradine is an antibiotic that belongs to a group of drugs called cephalosporins. Cephradine stops the bacteria from making their protein cell wall, so the bacteria die. Cephradine is used to treat bacterial infections of the respiratory tract, urinary tract, skin, and bone and joint. Cephradine is aW broad-spectrum bacterial antibiotic active against both Gram-positive and Gram-negative bacteria. It is also highly active against most strains of penicillinase -producing staphylococci.     Cephradine is an oral first-generation cephalosporin antibiotic similar in structure and activity to cephalexin. The in vitro antibacterial activity of cephradine includes excellent gram-positive but limited gram-negative coverage. Cephradine is indicated for the treatment of urinary tract infections, skin and skin structure infections, respiratory tract infections, and otitis media. Cephradine has been administered parenterally, however, the parenteral product is no longer available in the United States. Pharmacokinetics: Cephradine is administered orally. Following oral administration, the drug is rapidly and almost completely absorbed from the GI tract. In healthy patients, peak serum concentrations occur within 1 hour and average 9 mcg/ml following a single 250-mg dose, 15—18 mcg/ml after a single 500-mg dose, and 23.5—24.2 mcg/ml following a single 1-g dose. Administration with food lowers peak serum concentrations and Tmax; the total amount of drug absorbed is unchanged. Once in the systemic circulation, there is minimal binding (8—17%) to serum proteins. Cephradine does not cross the blood-brain barrier to any appreciable extent. Greater than 90% of the absorbed drug is excreted unchanged in the urine within 6 hours. Peak urine concentrations are approximately 1600 mcg/ml, 3200 mcg/ml, and 4000 mcg/ml following single doses of 250 mg, 500 mg, and 1 g, respectively. The elimination half-life is 1.3 hours in patients with normal renal function and 6—15 hours in patients with impaired renal function.   Mechanism of Action: Cephradine inhibits the third and final stage of bacterial cell wall synthesis by preferentially binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall. Penicillin-binding proteins are responsible for several steps in the synthesis of the cell wall and are found in quantities of several hundred to several thousand molecules per bacterial cell. Penicillin-binding proteins vary among different bacterial species. Thus, the intrinsic activity of cephradine as well as other cephalosporins and penicillins against a particular organism depends on their ability to gain access to and bind with the necessary PBP. Like all beta-lactam antibiotics, the ability of cephradine to interfere with PBP-mediated cell wall synthesis ultimately leads to cell lysis. Lysis is mediated by bacterial cell wall autolytic enzymes (i.e., autolysins). The relationship between PBPs and autolysins is unclear, but it is possible that the beta-lactam antibiotic interferes with an autolysin inhibitor. As a rule, first-generation cephalosporins are more active against gram-positive organisms than are second- and third-generation cephalosporins, but they have relatively little activity against gram-negative species. Gram-positive coverage includes nonpencillinase- and pencillinase-producing staphylococci (e.g., S. aureus) and streptococci (except enterococci). The gram-negative spectrum is limited to some strains Escherichia coli, Klebsiella pneumoniae, and Proteus mirabilis. Cephradine is inactive against enterococci (e.g., Enterococcus faecalis), methicillin-resistant staphylococci, Bacteroides fragilis, Citrobacter sp., Enterobacter sp., Listeria monoytogenes, Proteus sp. other than P. mirabilis, Providencia sp., Pseudomonas sp., and Serratia sp. Cephradine is designated chemically as (6R,7R)-7-[(R)2-amino-2-(1,4-cyclohexadien-1-yl)acetamido]-3-methyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid. Dosage Form        Oral Suspension & Capsules Indications To treat a variety of bacterial infections, including those of the ear, nose, tonsils, and throat, skin and soft tissues, genitourinary tract, and the respiratory tract. Cephradine is effective only against infections caused by bacteria; it is ineffective against those caused by viruses, fungi, or other microorganisms. Range and Frequency Oral suspension and capsules-- Adults and teenagers: 250 to 500 mg every 6 hours, or 500 to 1,000 mg every 12 hours. Children: 6.25 to 25 mg every 6 hours. Onset of Effect  1 hour. Duration of Action  Unknown Dietary Advice Cephradine may be taken on a full or empty stomach, but taking it with food will reduce stomach irritation. Storage Store in a tightly sealed container away from heat, moisture, and direct light. Keep liquid form refrigerated, but do not allow it to freeze. Missed Dose Take it as soon as you remember. This will help keep a constant level of medication in your system. If it is near the time for the next dose, skip the missed dose and resume your regular dosage schedule. Do not double the next dose. Stopping the Drug Take it as prescribed for the full treatment period, even if you begin to feel better before the scheduled end of therapy. Stopping cephradine prematurely may slow your recovery or lead to a rebound infection, also known as super infection, in which the heartier strains of bacteria survive and multiply, leading to a more serious and drug-resistant infection. When taking this drug to treat a streptococcal (strep) infection, it is particularly important to take it for the entire treatment period. Serious heart and kidney problems can develop later if it is discontinued prematurely. Prolonged Use Cephradine is generally prescribed for short-term therapy (10 to 14 days). Use of cephradine beyond this period increases the risk of adverse effects and super infection. Over 60 Adverse reactions may be more likely and more severe in older patients. Driving and Hazardous Work Do not drive or engage in hazardous work until you determine how the medicine affects you. Alcohol :  Avoid alcohol. Pregnancy Adequate studies of cephalosporin use during pregnancy have not been done. Consult your doctor for specific advice. Breast Feeding Cephradine passes into breast milk; caution is advised. Consult your doctor for specific advice. Infants and Children Cephradine may be used by children age 1 and older. Consult your pediatrician for specific advice. Special Concerns People who are allergic to penicillin may have equally serious allergic reactions to cephalosporin antibiotics such as cephradine. This drug is useful only against bacteria that are susceptible to its effects, not against colds, flu, or other viral infections. If your condition has not improved within a few days of starting cephradine, or instead has worsened Overdose Symptoms Seizures, severe abdominal pain, bloody diarrhea, vomiting. Drug Interactions Consult your doctor for specific advice if you are taking carbenicillin injection, heparin, divalproex, anticoagulants, sulfinpyrazone, dipyridamole, pentoxifylline, plicamycin, ticarcillin, probenecid, or valproic acid. Food Interactions                       No known food interactions Disease Interactions Caution is advised when taking Cephradine. Consult your doctor if you have a history of kidney disease or colitis.